DOKUMEN123.COM

inhibitory concentration (IC50) is a measure of the potency of a substance in inhibiting a specific biological or biochemical function. IC50 is a quantitative...

amoebas Dictyostelium discoideum (IC50 = 4.4 nM), Acanthamoeba castellanii (IC50 = 2.0 μM), and Acanthamoeba comandoni (IC50 = 3.1 μM) which cause infections...

5HT2a (IC50 = 92 nM) by Ca+ mobilization. CBP is also an antagonist on 5HT2b (IC50 = 100 nM). CBP and nCBP are functional antagonists on 5HT2c (IC50 = 0...

agonists (e.g. flumazenil). Low IC50 or high pIC50 values indicate tighter binding (pIC50 of 8.0 = IC50 of 10nM, pIC50 of 9.0 = IC50 of 1nM, etc.) These are non...

potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)...

potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)...

potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)...

(x axis). For competition binding assays and functional antagonist assays IC50 is the most common summary measure of the dose-response curve. For agonist/stimulator...

factor receptor (VEGFR) 1/2 receptor family tyrosine kinases inhibitor with IC50 of 2, 6, 77, 59 nM for EGFR, ErbB2, KDR, and Flt-1. In cells, growth factor-induced...

of potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). [...] Chlorphentermine was a very potent 5-HT releaser (IC50 = 18.2 nM), a weaker...

potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)...

potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)...

n-pentyl group (IC50 = 13,3 nM), n-butyl (IC50 = 119 nM), phenyl with 2-furyl (IC50 = 0,720) or 3-thiophenyl (IC50 = 0,772). As seen in table 1, the in vitro...

Rev-ErbA) with a half-maximum inhibitory concentration (IC50) = 670 nM for Rev-ErbAα and IC50 = 800 nM for Rev-ErbAβ. In an animal study, some of its...

(IC50=7.5μM) TDZD-8 (IC50=2μM) NP00111 (IC50=2μM) NP031115 (IC50=4μM) Tideglusib (IC50=60nM) HMK-32 (IC50=1.5μM) L803-mts (IC50=20μM) L807-mts (IC50=1μM)...

of [125I] RTI-55 (IC50 = 4.82 ± 0.05 μM, n=3) to human recombinant DAT expressed in CHO-K1 cells and inhibition of DA uptake (IC50 = 14.5 ± 1.6 μM, n=2)...

antagonist, with an IC50 binding affinity of ~500-1,000 nM (0.5-1 μM), but displays higher potency at extrasynaptic NMDA receptors (IC50 = ~22 nM), suggesting...

of 1,700 nM. It is also a weak dopamine reuptake inhibitor (DRI), with an IC50 of 3,040 nM at the dopamine transporter (DAT). The drug shows weak affinity...

Intercity, often shortened to IC ([iːˈtseː] ), is the second-highest train classification in Germany, after the Intercity Express (ICE). Intercity services...

tyrosine-kinase inhibitor with activity against EGFR (IC50 0.8 nM), HER-2 (IC50 19 nM) and ErbB-4 (IC50 7 nM). By 2015, Pfizer had discontinued development...

Rev-ErbAα with a half-maximum inhibitory concentration (IC50) = 790 nM for Rev-Erbα and IC50 = 560 nM for Rev-ErbAβ. It has been used in the study of...

potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)...

Tesofensine has IC50 of 8.0, 3.2 and 11.0nM at the DAT, NET, and SERT. More recently, though, the following data was submitted: IC50 (nM) NET 1.7, SERT...

potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)...

of [125I] RTI-55 (IC50 = 4.82 ± 0.05 μM, n=3) to human recombinant DAT expressed in CHO-K1 cells and inhibition of DA uptake (IC50 = 14.5 ± 1.6 μM, n=2)...

inhibits the reuptake of norepinephrine, dopamine, and serotonin with an IC50 ratio of 1:6:14, respectively. In 2011, Euthymics Bioscience spun off its...

of [125I] RTI-55 (IC50 = 4.82 ± 0.05 μM, n=3) to human recombinant DAT expressed in CHO-K1 cells and inhibition of DA uptake (IC50 = 14.5 ± 1.6 μM, n=2)...

potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)...

testing determined APICA to have an IC50 of 175 nM at CB1, only slightly less potent than JWH-018 which had an IC50 of 169 nM, but over four times more...

potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)...

potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)...

potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)...

potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)...

transporter (DAT) has been reported to be 6,360 nM and its functional inhibition (IC50) of the DAT has been reported to be 3,780 to 8,800 nM. These values were...

antagonist is usually defined by its half maximal inhibitory concentration (i.e., IC50 value). This can be calculated for a given antagonist by determining the...

hydroxyflutamide as the active form. It has been reported to possess an IC50 of 700 nM for the androgen receptor (AR), which is about 4-fold less than...

norepinephrine reuptake, respectively, toludesvenlafaxine has respective in vitro IC50 values of 723 nM, 763 nM, and 491 nM for serotonin, norepinephrine, and dopamine...

leaves of Piper betle. It is a more potent inhibitor of xanthine oxidase (IC50=16.7 μM) than allopurinol. It might be a useful new compound in treating...

chemokine CXCR3 receptor antagonist, with an affinity (IC50) of 54 nM and an inhibitory potency (IC50) of 18 to 74 nM. Unlike NIBR2130, LSD itself is completely...

non-hydrogen atoms. It can be transformed to the equation: LE = 1.4(−log IC50)/N Some suggest that better metrics for ligand efficiency are percentage/potency...

Sclerotiorin is an aldose reductase inhibitor (IC50=0.4 μM) as well as a reversible lipoxygenase inhibitor (IC50=4.2 μM). Chidananda, C; Rao, LJ; Sattur, AP...

the receptor. Ligand affinities are most often measured indirectly as an IC50 value from a competition binding experiment where the concentration of a...

potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)...

potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)...

MDPHP acts as a potent norepinephrine-dopamine reuptake inhibitor. The IC50 values for MDPHP are 60-935 nM at NET, 8.4-50 nM at DAT and 9000 nM at SERT...

acts as a serotonin reuptake inhibitor (IC50 = 2.1 nM; Ki = 0.1 nM) and 5-HT1A receptor partial agonist (IC50 = 0.2 nM; IA = ~60–70%). It has negligible...

hydrolase (FAAH), with an IC50 of 9.1nM, and 870x selectivity for FAAH over the related enzyme MAGL, which it inhibits with an IC50 of 7900nM. It is also...

negative allosteric modulator of the α7-nicotinic acetylcholine receptor (IC50 = 55 nM). For this reason, similarly to hydroxynorketamine (HNK), it has...

1, 2, 3 inhibitor Fruquintinib was found to inhibit VEGFR2 (KDR) with an IC50 of 25 nmol/L in the Z-lyte assay. The kinase selectivity of fruquintinib...

have much higher affinity for serotonin receptors than RU-27849 itself (IC50 ≈ 50 nM). A number of other derivatives also exist, including FHATHBIN (6-hydroxy)...

selective full agonist of the androgen receptor (IC50 = 12 nM) and inhibitor of 5α-reductase types I and II (IC50 = 6 and 10 nM, respectively). Structurally...

potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)...

of MAO-A (IC50 = 5,630 nM), but was about 13-fold less potent than 2-NAP. Neither 2-NAP or 1-NAP inhibited monoamine oxidase B (MAO-B) (IC50 > 100,000 nM)...

which acts as a selective antagonist of Toll-like receptor 3 (TLR3), with an IC50 of 3.44 μM. It is used for research into the function of TRL3 and its role...

cell line (IC50: 19.25 µg/mL after 24 hours), while the water sub-extract showed activity against the MDA-MB-231 breast cancer cell line (IC50: 15.20 µg/mL)...

benzo[b]furan isostere. The tryptamine IC50 of 38 nM was about 13-fold lower than the benzofuran, which had an IC50 of 500 nM. Nichols DE (2012). "Structure–activity...

parameters of the dose response curve reflect measures of potency (such as EC50, IC50, ED50, etc.) and measures of efficacy (such as tissue, cell or population...

Tranexamic acid also directly inhibits the activity of plasmin with weak potency (IC50 = 87 mM), and it can block the active-site of urokinase plasminogen activator...

kinase (IC50 = 1.8 and 1.7 nmol/L, respectively). At higher concentrations it is also an efficient inhibitor of serine/threonine protein kinases (IC50 of 10...

concentration is 25μM, the IC50 of andrographolide for GSK-3β is 5.58±0.40μM. When the substrate concentration is increased to 90μM, the IC50 increases to 37.7μM...

spectabilis. It can be consumed orally, smoked, or snorted. It is a potent (IC50 < 1 μM) selective inhibitor of the serotonin transporter (SERT) (that is...

acts as a serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI) with IC50 values of 3.13, 18, and 0.79 nM, respectively. In animal studies, dichloropane...

a IC50 5.0 ug/mL, nonetheless, human cathepsin L is involved in many diseases, gallinamide A was tested in HeLa cervical cancer cells with a IC50 12...

its IC50 was nearly 128 μL, so we confirmed that LDH absorbance was not affected by this peptide." p. 262, "Moreover, the results showed the IC50 of mast...

nicotinic acetylcholine receptor in nanomolar range (IC50 = 19 ± 8 nM). The peptide is less effective (IC50 ≈ 3 μM) at α7 nicotinic acetylcholine receptors...

hence is a phytoestrogen (IC50 for estrogen receptor binding = 1 μM). It has also been found to act as a tyrosinase inhibitor (IC50 = 3.5 μM) and to inhibit...

diseases. Tofacitinib to a lesser extent also inhibits JAK1 (IC50 = 100 nM) and JAK2 (IC50 = 20 nM), which in turn blocks IFN-γ and IL-6 signalling and...

acid, 4-butylresorcinol has been found to be the most powerful inhibitor by IC50, but the mode of inhibition is reversible. 4-Butylresorcinol can be used...

inhibitor of protein kinase JAK-2 with IC50=6 nM; related kinases FLT3 and RET are also sensitive, with IC50=25 nM and IC50=17 nM, respectively. Significantly...

of [125I] RTI-55 (IC50 = 4.82 ± 0.05 μM, n=3) to human recombinant DAT expressed in CHO-K1 cells and inhibition of DA uptake (IC50 = 14.5 ± 1.6 μM, n=2)...

concentration (IC50) of 5.9 nM and Janus kinase 2 with an IC50 of 5.7 nM. Tyrosine kinase 2, which belongs to the same enzyme family, is affected less (IC50 = 53 nM)...

that acts as a potent and selective α1A-adrenergic receptor antagonist. The IC50 of nicergoline in vitro has been reported to be 0.2 nM. The primary action...

alkaloid mitragynine. Rhynchophylline is a non-competitive NMDA antagonist (IC50 = 43.2 μM) and a calcium channel blocker. Uncaria species have had a variety...

receptor antagonist, which is a non-competitive AMPA receptor antagonist (IC50 values are 10-20, ~ 450 and >> 50 μM for AMPA-, kainate- and NMDA-induced...

defined as the pIC50 (or pEC50) of interest minus the LogP of the compound. LiPE = pIC 50 − log ⁡ P {\displaystyle {\ce {LiPE}}={\ce {pIC50}}-\log P} In...

employ ultra-toxic payloads with picomolar IC50 values, SN-38 is considered a moderately toxic agent with IC50 in the nanomolar range, potentially allowing...

hormone receptor (GnRHR), with a half-maximal inhibitory concentration (IC50) of 0.12 nM. A dosage of relugolix of 40 mg once per day has been found to...

concentration = 33–700 nM) and a very weak dopamine reuptake inhibitor (IC50 = 12,000 nM). Conversely, it is not a dopamine transporter (DAT) substrate...

castellanii (IC50: ~1.7 µM) and Dictyostelium discoideum (IC50: ~0.1 µM). Nocuolin A is effective against protozoa such as Trypanosoma brucei (IC50 = 3.99 µM)...

potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)...

Channels IC50 Cav3.1 0.01 μM Nav1.7 0.007 μM Nav1.3 0.12 ± 0.06 μM Nav1.5 No significant effect (up to 2 μΜ) Nav1.8 No significant effect (0.93 μM)...

collection of experimentally measured binding affinity data (Kd, Ki, and IC50) for the protein-ligand complexes deposited in the Protein Data Bank (PDB)...

vitro((250.1 ± 36.2) pg/mL at 1.0 mmol/L),weak cytotoxicity against PC12 cells (IC50: 73.7 μmol/L),Anti‐methicillin-resistant Staphylococcus aureus (MRSA) activity...

strength, and resilience of rubber products. DHEA-caproate ester (#121) has a IC50 of 0.049nM for the 5-alpha-reductase enzyme. List of carboxylic acids List...

permeable inhibitor of Ca2+/calmodulin-dependent kinase type II (CaMK II) with IC50 of 900nM, charactered by hydrophobicity. KN-62 also potently inhibits the...

phosphodiesterase inhibitor, selective for the subtypes PDE5, PDE6, PDE9 and PDE11. IC50 values are 0.76, 0.15, 29.0, and 12.0 μM, respectively. Zaprinast inhibits...

their uses. ɑIC50 for displacement of [3H]cocaine. IC50 for cocaine = 67.8 ± 8.7 (nM) bIC50 values for displacement of [3H]WIN 35428 cIC50 values for displacement...

potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)...

However, it retains higher affinity for the dopamine D1 receptor (IC50 = 198 nM). Its IC50 values are 19 nM for the α1-adrenergic receptor, 4,945 nM for the...

antagonists, half maximal inhibitory concentration (IC50) is used to measure the potency of antagonists. IC50 means the concentration of antagonist needed to...

of flunitrazepam and has been sold online as a designer drug. It has an IC50 value of 1.499 nM for the GABAA receptor. Nitrazolam Phenazepam List of benzodiazepine...

7,600–28,000 IC50 Human α3β2-nACh 1,000 IC50 Human α3β4-nACh 1,800 IC50 Human α4β2-nACh 12,000 IC50 Human α4β4-nACh 12,000–14,000 IC50 Human α7-nACh...

order of potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Chlorphentermine was a very potent 5-HT releaser (IC50 = 18.2 nM), a weaker...

class which acts as a selective serotonin releasing agent (SSRA). It has IC50 values of 121 nM, 6,436 nM, and 3,371 nM for inhibiting the reuptake of serotonin...

pericine has been shown to bind to mu opioid receptors in vitro, and has an IC50 of 0.6 μmol, within the range of a weak analgesic. It may also have convulsant...

substance which acts as a potent agonist at the 5-HT7 receptor, with an IC50 of 0.83 nM. It reverses the amnesia induced by drugs such as scopolamine...

truly not understood at this time. TSA inhibits HDACs 1, 3, 4, 6 and 10 with IC50 values around 20 nM. TSA represses IL (interleukin)-1β/LPS (lipopolysaccharide)/IFNγ...

with an IC50 of 31,000 nM. For comparison, the IC50 of AMT for MAO-A inhibition was 380 nM (~82-fold more potent than 5-MeO-AMT) and the IC50 values of...

steroidal antiprogestogen (IC50 = 0.025 nM for the PR), as well as an antiglucocorticoid (IC50 = 2.2 nM for the GR) and antiandrogen (IC50 = 10 nM for the AR)...

and 3,349 nM for serotonin in rat brain synaptosomes. Similarly, MDPV's IC50 values for monoamine reuptake inhibition were 10 nM for dopamine, 80 nM for...

binding domain of PCSK9 and inhibits its interaction with the receptor with an IC50 of 2.5 ±0.1 nM. A 2025 review paper of cholesterol-lowering drugs with PCSK9...

disulfide bridges. Jingzhaotoxins can target multiple channels. The following IC50 values have been determined: '*' Only a dissociation constant (Kd) was measured...

inhibitor and dopamine reuptake inhibitor. It binds to transporters with IC50 values of 37 nM (dopamine transporter), 105 nM (norepinephrine transporter)...

5-HT)) and 5-HT2B receptor antagonist (IC50 = 29 nM). It is also a very weak antagonist at the 5-HT2A receptor (IC50 = 1,650 nM), though this action is not...

dosage of mazindol is only 2-4 mg per day. Ciclazindol is reported to have an IC50 of 1.3 nM for the dopamine transporter (cmp 23). Mazindol Setazindol Swaisland...

a potent and selective inhibitor for the TRPV5 calcium channel, with an IC50 of 177 nM and high selectivity for TRPV5 over TRPV6 and the other subtypes...

agonist (Emax = 55%) of the androgen receptor (IC50 = 30 nM) and inhibitor of 5α-reductase types I and II (IC50 = 2 and 3 nM, respectively). TFM-4AS-1 shows...

development for treatment of hematological malignancies. It has lowest nM IC50 values against TYK2, JAK1, JAK2, JAK3, FMS, and SYK. It is being developed...

than that of PCP or 3-MeO-PCP, with half maximal inhibitory concentration (IC50) values of 26.67 μM (3-MeO-PCMo), 2.02 μM (PCP) and 1.51 μM (3-MeO-PCP)....

is a known inhibitor of monoamine oxidase A and monoamine oxidase B, with IC50 values of 1 μM for MAO-A and 15.5 μM for MAO-B, suggesting that it is more...

potency, displaying IC50 values in the low-nanomolar range. In addition, it binds to the CB1 receptor in rat brain membrane preparations (IC50 = 20 nM), but...

potencies comparable to cocaine (IC50 values <2.5 μM), but with less potent effects at serotonin transporters (IC50 values >80 μM). At sufficient doses...

adrenergic receptor agonist (IC50 = 9.1 nM). It also acts as an α1-adrenergic receptor agonist to a far lesser extent (IC50 = 4.85 μM). In hypertensive...

and related anxiolytic drugs. The half-maximal inhibitory concentration (IC50) of bicuculline on GABAA receptors is 2 μM +/-0.1 at 40 μM of GABA (GABA...

channels (IC50=25.4 nM). It has a less potent inhibitory effect on Nav1.1 (IC50=4.1 μM), Nav1.2 (IC50=813 nM) or on Nav1.6 channels (IC50=15.2 μM). Recent...

potent at blocking the hERG channel with an IC50 of ~12 μM. Levomethadone has a lower affinity, with an IC50 of ~29 μM at the hERG channel. Methadone is...

BAY 36-7620 is an antagonist at mGluR1 receptors. It has a IC50 value of 160 nM at the receptor. This compound has been used to study metabotropic glutamate...

acetylcholinesterase inhibitor, with IC50 binding affinity of ~82 nM. It is also a weak NMDA receptor antagonist, with IC50 of ~65,000–82,000 nM (65–82 μM);...

of [125I] RTI-55 (IC50 = 4.82 ± 0.05 μM, n=3) to human recombinant DAT expressed in CHO-K1 cells and inhibition of DA uptake (IC50 = 14.5 ± 1.6 μM, n=2)...

5-fold less potent at inhibiting the reuptake of serotonin (IC50 = 330 nM) and dopamine (IC50 = 2,343 nM), respectively, and is about 3-fold less potent...

Crane and Specialized Transport IC50" (PDF). Archived from the original (PDF) on 2010-02-17. Retrieved 2009-07-22. "IC50 2010 Listing" (PDF). Archived from...

inhibitor (Ki = 479 nM; IC50 = 2,400 nM). Conversely, it shows little or no effect on the reuptake of dopamine and norepinephrine (Ki and IC50 > 10,000 nM). Nonetheless...

respectively. It inhibits the reuptake of dopamine and norepinephrine with IC50 values of 2.9 μM and 4.4 μM, respectively. It has weak affinity for the serotonin...

NEFA is a moderate affinity NMDA antagonist (IC50 = 0.51 μM). It is a structural analog of phencyclidine. It was first synthesized by a team at Parke-Davis...

vincristine sensitivity, the cells were cultured in RPMI 1640 medium. The IC50 value was used to determine vincristine sensitivity. In addition, a Western...

been reported to inhibit α3β4 nicotinic acetylcholine receptors, with an IC50 value of 14 μM. Threohydrobupropion circulates at higher concentrations than...

NETTooltip Norepinephrine transporter ND (Ki) ND (IC50) ND (EC50) DATTooltip Dopamine transporter ND (Ki) ND (IC50) ND (EC50) Notes: The smaller the value, the...

has the highest affinity with an IC50 of 193 nM, followed by TLTx2 with an IC50 of about 800 nM. For TLTx3 the IC50 has not been measured. TLTx1 acts...

bioactivity data against drug targets. Bioactivity is reported in Ki, Kd, IC50, and EC50. Data can be filtered and analyzed to develop compound screening...

integrated stress response when measured by eIF2α phosphorylation with an IC50 of 5 nM. It has been shown to inhibit eIF2α phosphorylation-induced stress...

thiorphan, inhibits enkephalinase enzymes in the intestinal epithelium with an IC50 of 6.1 nM, protecting enkephalins from being broken down by these enzymes...

identification of cyclohexyl acids with excellent potency (pIC50 = 8.6), cellular activity (pIC50 = 7.7) and moderate unbound clearance and oral bioavailability...

diverse biological activities. It exhibits the antiacetylcholinesterase(AChE; IC50 = 15 μM), antiallergic, antinociceptive, and gastric emptying activities...

comparisons difficult (Figure 1; Cmpd 3: hTAAR1 IC50 = 9 μM, ET-54: rTAAR1 IC50 = 3 μM, ET-78: rTAAR1 IC50 = 4 μM). Cichero E, Espinoza S, Franchini S, Guariento...

transporter 13,000 (Ki) 150–420 (IC50) 47–108 (EC50) (rat) DATTooltip Dopamine transporter >26,000 (Ki) 890–20,500 (IC50) 106–190 (EC50) (rat) 5-HT1A 3...

Especially, Carpaine possessed significant anti-plasmodial activity in vitro (IC50 of 0.2 μM) and high selectivity towards the parasites. Circulatory effects...

only slightly larger than a phenyl ring by itself. ɑIC50 value for displacement of [3H]cocaine ɑIC50 value for displacement of [3H]cocaine The hydroxylated...

γ-butyrobetaine hydroxylase gives a half maximal inhibitory concentration (IC50) value of 62 micromolar, which other study authors have described as "potent...

adenosine receptor antagonist. As a phosphodiesterase inhibitor, IBMX has IC50 = 2–50 μM and does not inhibit PDE8 or PDE9. Essayan, DM (November 2001)...

C-terminal carboxyl is replaced by an amide. ShK-186 blocks Kv1.3 with an IC50 of 69 pM and exhibits the same specificity for Kv1.3 over closely related...

benzimidazole-benzimidazole structure on inhibitory activity Structure Activity X IC50 (nM) Inhibitory activity >44 None >44 None 11 Very weak 1.7 Weak 0.50 Moderate...

potassium channel (IC50 of 28 nM). Comparing this channel potency to other potassium channels clearly shows high selectivity for Kv1.3 as the IC50 for Kv1.1 is...

decreasing in vitro affinities for the D2 receptor (IC50 = 27, 120 and 181 nM) and the D3 receptor (IC50 = 3.6, 4.8 and 17.5 nM). Though it was long widely...

about 90-fold less potent at the rat TAAR1 (IC50 = 748 nM) and 140-fold less potent at the mouse TAAR1 (IC50 = 1,190 nM) compared to the human TAAR1. Surprisingly...

weaker serotonin reuptake inhibitor (IC50 = 1,500 nM) and as a weak antagonist of the 5-HT2A and 5-HT2C receptors (IC50 = 950 and 980, respectively; notably...

has been described as very potent in its inhibition of rat 3α-HSD, with an IC50 of 0.2 μM and a Ki (in rat testicular homogenates) of 0.42 μM. However, inhibition...

Species Myosin type IC50 Rabbit Skeletal muscle myosin S1 1.3 μM, 9.22 μM, 0.98 μM Dictyostelium discoideum Myosin II motor domain 6.6 μM, 8.5 μM Human...

fentanyl and has been sold online as a designer drug. In animal studies the IC50 (the half maximal inhibitory concentration for acrylfentanyl to displace...

enzyme choline acetyltransferase (ChAT). B115 inhibits human ChAT with an IC50 of 4.3 μM. During in vivo testing, B115 has been found to partially protect...

concentration = 9,900 nM), but did not affect dopamine or norepinephrine reuptake (IC50 = >50,000–100,000 nM). The drug fully substituted for LSD in rodent drug...

cancer cells. It demonstrates a strong inhibitory effect on CDK9, with an IC50 of 79 nM, while showing considerably weaker activity against other cyclin-dependent...

phosphoinositide 3-kinases (PI3Ks). It has an in vitro inhibitory concentration (IC50) of around 5 nM, making it a more potent inhibitor than LY294002, another...

order of potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Chlorphentermine was a very potent 5-HT releaser (IC50 = 18.2 nM), a weaker...

competitive inhibitor of activity of ROCK1 (IC50 of 5 nM), ROCK2 (IC50 of 50 nM), MRCKα (IC50 of 10 nM) and MRCKβ (IC50 of 100 nM) kinases without affecting...

than enoxolone (glycyrrhetinic acid) or carbenoxolone in vitro (IC50 = 0.9 nM; IC50 = 5 nM in transfected cells). The compound has been found to be highly...

27,000–30,500 (Ki) 360–405 (IC50) 54–110 (EC50) (rat) DATTooltip Dopamine transporter 6,500–>10,000 (Ki) 1,440–21,000 (IC50) 51–278 (EC50) (rat) 5-HT1A...

required to cause a given toxicological endpoint (LC50, EC50, IC50). 1TU=LC50 or 1TU=IC50 for inhibition of growth Since the mass or molar based concentrations...

demonstrates affinity for the dopamine transporter (IC50 0.4 μmol/L) and norepinephrine transporter (IC50 0.7 μmol/L). Trodusquemine suppresses appetite,...

high affinity and potency at the GABAA receptor (binding IC50 = 49; Ki = 90 nM; functional IC50 = 370 nM). It has been said to be markedly more potent than...

IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells with an IC50 of 5.6 pM. The IL-23 pathway plays a central role in the inflammatory cascade...

17α,20-lyase than its enantiomer (IC50 values of 0.05 and 2.38 μM, respectively) and in inhibiting 11β-hydroxylase (IC50 values of 0.152 and 0.608 μM, respectively)...

ACT-462206 is a dual orexin receptor antagonist (IC50 for OX1 = 60nM, OX2 = 11nM) which has been investigated for the treatment of insomnia. In human trials...

transporter 0.45–18 (Ki) 0.92–4.9 (IC50) >10,000 (EC50) SERTTooltip Serotonin transporter 39–272 (Ki) 54–94 (IC50) >10,000 (EC50) SERT2Tooltip Serotonin...

and low libido. This table compares inhibitory (blocking) concentrations (IC50, unit: nM) of three antimineralocorticoids. Mineralocorticoid receptor inhibition...

interactions with hNET and hDAT (IC50 166 micromolar and 240 micromolar, respectively) was also observed. [42] The IC50 values for 2C-B and 25X-NBOMes were...

the degradation of enkephalins and other endogenous regulatory peptides (IC50 = 10 μM), though the clinical significance of this property is uncertain...

respectively). In addition, its serotonin reuptake inhibition is very weak as well (IC50 = 3,400 nM). In contrast to other β-carbolines, THH shows minimal affinity...

2) Low boost circuit in the 2nd VCA. 3) DC supply current boost circuit (IC50)." In February 1985, Roland started producing a new revision of MKS-80, known...

disease Inhibitory Concentration, as in half maximal inhibitory concentration (IC50) Inspiratory capacity, a measure of lung volumes Irreducible complexity,...

variant of EGFR. Neratinib has an IC50 of 59 nM against HER2 and shows weak inhibition against KDR and Scr with IC50 values of 0.8 μM and 1.4 μM, respectively...

Norepinephrine transporter 5,900 (Ki) 25,000 (IC50) ND (EC50) DATTooltip Dopamine transporter 8,600 (Ki) 67,000 (IC50) ND (EC50) Notes: The smaller the value...

higher than the concentration necessary to inhibit N-type calcium channels (IC50 of piracetam in rat neurons was 3 μM). Piracetam was first made some time...

neurotransmitter release at glutamatergic synapses in hippocampus and cortex with IC50 of 980 μM, a brain concentration seen in classical phenylketonuria, whereas...

potency profile against multiple HCV genotypes 1–6 and key mutants (GT1b, IC50 = 0.2–0.4 nM; replicon GT1b, EC50 = 1.6 nM). Danoprevir has been evaluated...

000 (Ki) ND (IC50) ND (EC50) DATTooltip Dopamine transporter >8,000 (Ki) ND (IC50) ND (EC50) MAO-ATooltip Monoamine oxidase A >100,000 (IC50) MAO-BTooltip...

>10,000 σ2 2,765 SERTTooltip Serotonin transporter 248–483 (Ki) 373–423 (IC50) NETTooltip Norepinephrine transporter, DATTooltip Dopamine transporter >10...

antagonist, its affinity (Ki) and half maximal inhibitory concentration (IC50) are 1,253 nM and 5,900 nM, respectively. Finally, at the human vasopressin...

it is an extremely potent uncoupler of oxidative phosphorylation with an IC50 of about 1 micromolar (≈500 nanograms per milliliter or parts per billion)...

acetylcholine receptors. Lupinine was found to have an IC50 value of >500 μM for nicotinic receptors and an IC50 value of 190 μM for muscarinic receptors. However...

Half-maximal inhibitory concentration = 0.86 μM), purine P2X3 receptor antagonist (IC50 = 0.87 μM), and serotonin 5-HT2A receptor antagonist (IC50Tooltip Half-maximal...

lesser extent as a partial agonist of the μ-opioid receptor (Ki = 0.25 nM; IC50 = 3.4 nM; Imax = 29%) with lower relative intrinsic activity and marked antagonistic...

inhibitor. Quilostigmine displays inhibition of the AChE enzyme with an IC50 value of 0.148 μM. Quilostigmine was initially studied by AstraZeneca for...

the IC50 values were determined and gave values of 230 and 430 nM respectively. Calciseptine also has an effect on the cardiac function. The IC50 value...

5-HT1A receptor. Whereas the serotonin 5-HT1A receptor affinities (Ki or IC50) of tryptamine and DMT were 125 nM and 170 nM, respectively, the affinities...

study, morin was found to be a weak inhibitor of fatty acid synthase with an IC50 of 2.33 μM. Morin was also found to inhibit amyloid formation by islet amyloid...

amphetamine class. It acts as a selective serotonin releasing agent (SSRA), with IC50 values of 93nM, 12,000nM, and 1,937nM for serotonin, dopamine, and norepinephrine...

produce monoamine reuptake inhibition. However, no functional inhibition (IC50) of the human monoamine transporters has been observed with ketamine or its...

a previously unreported compound with significant antioxidant activity (IC50 = 8.72 mg/L in DPPH radical scavenging). Density functional theory (DFT)...

muscle myosin S1 IC50=0.4 μM, for Dictyostelium discoideum myosin II motor domain IC50=2.3 μM, for human β-cardiac myosin subfragment 1 IC50=13 μM, for heavy...

enzyme sirtuin 2 (SIRT2). It has moderate potency, inhibiting SIRT2 with an IC50 of 3 μM, and shows broad-spectrum antiviral effects against both RNA and...

5–33 (IC50) MAO-BTooltip Monoamine oxidase B 100,000 (IC50) DYRK1ATooltip Dual specificity tyrosine-phosphorylation-regulated kinase 1A 4,600 (IC50) Notes:...

interactions with the other serotonin receptors. Whereas vortioxetine has IC50 or EC50 values of 5.4 nM for the SERT and 12 nM for the 5-HT3 receptor, its...

EMD-59983, has high affinity for the sigma receptors (IC50 = 24 nM) and the dopamine D2 (IC50 = 23 nM) and D3 receptors, with potent antidopaminergic...

5-bisphosphate 3-kinase P110 gamma|catalytic subunit gamma isoform. With an IC50 of 1.4 μM it is somewhat less potent than wortmannin, another well-known...

Species Myosin type IC50 Rabbit Skeletal muscle myosin S1 0.4 μM, 0.1 μM Dictyostelium discoideum Myosin II motor domain 2.3 μM, 9 μM Human β-Cardiac myosin...

kidney injury. It acts as a non-selective melanocortin receptor agonist, with IC50 values of 2.9 nM, 1.9 nM, 3.7 nM, and 110 nM at the MC1, MC3, MC4, and MC5...

been shown that THC is also a partial autotaxin inhibitor, with an apparent IC50 of 407 ± 67 nM for the ATX-gamma isoform. THC was also co-crystallized with...

competitor with IC50 values of 11 and 18 nM, respectively. The inhibitor is significantly less active towards other kinases, including JAK3 (IC50 = 0.16 μM)...

inhibitor of G6PDHTooltip glucose-6-phosphate dehydrogenase (Ki = 17 μM; IC50 = 18.7 μM), and is able to lower NADPHTooltip nicotinamide adenine dinucleotide...

crenolanib is toxic at IC50 concentrations of 7 nM and 8 nM, respectively. Crenolanib has been shown to inhibit PDGFRα with an IC50 of 0.4 ng/mL in porcine...

It exhibits strong potency in lowering huntingtin protein levels, with an IC50 of ≤ 0.1 μM. The drug is an orally bioavailable small molecule that specifically...

PcTX1. PcTX1 specifically inhibits ASICa and has an IC50 value in the nanomolar range- a smaller IC50 than all other known ASIC inhibitors which have been...

Bretisilocin is also a serotonin reuptake inhibitor to a much weaker extent (IC50 = 418.9 nM). Additional values have also been published. Bretisilocin is...

profile in the tissue in question, such as the calculation of the drug's EC50, IC50, and Hill coefficient.[citation needed] Examples of important contributions...

improve selectivity. While the IC50 values of philanthotoxins varies between analogues and receptor subunit composition, the IC50 value of PhTX-433 at the iGluR...

memantine. In patch-clamp measurements memantine has an IC50 of (2.3+0.3) μM while amantadine has an IC50 of (71.0+11.1) μM. The binding site with the highest...

Fluorenol is a weak dopamine reuptake inhibitor with an IC50 of 9 μM, notably 59% weaker than modafinil (IC50 = 3.70 μM), potentially making it even less liable...

selective inhibitor of the enzyme fatty-acid amide hydrolase (FAAH), with an IC50 of 70 nM. It is described as a covalently binding but slowly reversible selective...

species such as Aβ38 and Aβ37. The compound demonstrates high potency with an IC50 below 10 nM for gamma-secretase modulation of APP cleavage, and importantly...

effects on cancer cell lines, with more than a five-fold difference in the IC50 values in some cell lines. Euphol treatment had a higher selective cytotoxicity...

Cepharanoline is an isolate of Stephania that has antiplasmodial activity with an IC50 of 0.2 μM. Aun Chea, Sok-Siya Bun, Nadine Azas, Monique Gasquet, Sothavireak...

3-BHPPN), is a synthetic, nonsteroidal, and highly selective agonist of ERβ (IC50 = 15 nM) that is used widely in scientific research to study the function...

Against rat NMDAR Compound IC50 (nM) Ki (nM) (+)-MK-801 4.1 2.5 2-Cl-Diphenidine 14.6 9.3 Diphenidine 28.6 18.2 2-MeO-Diphenidine 56.5 36.0 Phencyclidine...

a potent inhibitor of 3β-hydroxysteroid dehydrogenase (3β-HSD) 1 and 2 (IC50 = 0.02 and 0.16 μM, respectively). On the basis of this finding, it has been...

serotonin 5-HT2B receptor (IC50 = 410 nM). It is far less potent as an antagonist of the dopamine D1, D3, and D5 receptors (IC50 = 3,200–8,300 nM) and of...

doi:10.1111/bph.14832. PMC 6965684. PMID 31418454. TABLE 1 Summary of pIC50 (negative logarithm of the molar concentration of these compounds at which...

moderately potent but highly selective blocker of the TRPM4 ion channel, with an IC50 of 1.5 μM. It is protective against glutamate mediated neuronal excitotoxicity...

doi:10.1111/bph.14832. PMC 6965684. PMID 31418454. TABLE 1 Summary of pIC50 (negative logarithm of the molar concentration of these compounds at which...

marketed. It is selective for the GABAB receptor over the GABAA receptor (IC50 = 1.70 μM and > 100 μM, respectively). The drug is a GABA analogue and is...

8-triazaspiro[4.5]decan-8-yl)ethyl)-2-naphthamide: 75-fold selective versus PLD1, IC50 = 20 nM. GRCh38: Ensembl release 89: ENSG00000129219 – Ensembl, May 2017...

fruit) is the most potent known inhibitor of NADH dehydrogenase (ubiquinone) (IC50=1.2 nM, stronger than rotenone). Despite more than 50 years of study of complex...

Cobicistat shows potent, selective inhibition of the CYP3A isozyme family (IC50 0.15 μM) compared to some CYP1A and CYP2C isozymes. As cobicistat was discovered...

published lethal dose (LDLo) EC50 (half maximal effective concentration) IC50 (half maximal inhibitory concentration) Draize test Indicative limit value...

with an IC50 value of 0.03 μg/ml. The chief reason for this activity are believed to be the monoterpenes 1,8-cineole and α-pinene which have IC50 values...

the in vitro ACAT inhibitory activity of these analogs was modest (e.g., IC50 values of 2–50 mM), they exhibited significant activity in a cholesterol-fed...

binding affinity of Ki 0.92 μM and an IC50 value of 1.26 μM which is about 100 times less potent than diazepam (IC50 value of 0.012 μM). The LD50 of pure...

frog oocytes, of the nAChR cloned from avian DNA: MLA was found to have an IC50 of ~8 × 10−8M at α3β2 and ~7 × 10−7M at α4β2 receptor sub-types. Although...

for the glutamate receptor mGluR3. It has only moderate potency with an IC50 of 450 nM, but is highly selective over the closely related subtype mGluR2...

Pravadoline (WIN 48,098) is an anti-inflammatory and analgesic drug with an IC50 of 4.9 μM and a Ki of 2511 nM at CB1, related in structure to nonsteroidal...

be much more active resulting in compound 60 (irindalone) (Fig. 15), with IC50 values of 3.4, 400, and 26 nM for 5HT2, DA, and α1 receptors, respectively...

works by directly blocking the epithelial sodium channel (ENaC) with an IC50 around 0.1 μM, indicating potent blockade. Antagonism of ENaC thereby inhibits...

potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). Aminorex released NE (IC50 = 26.4 nM), DA (IC50 = 44.8 nM) and 5-HT (IC50 = 193 nM)...

vitro studies show that yangonin inhibits MAO-A with an IC50 of 1.29 μM and MAO-B with an IC50 of 0.085 μM, indicating strong activity, particularly against...

progesterone, and these concentrations are still well below the aforementioned IC50 values for inhibition of 5α-reductase types 1 and 2. As with endogenous progesterone...

concentration of 0.95 mg/L, copper(II) chloride was found to cause a 50% inhibition (IC50) of the metabolic activity of denitrifying microbes. Copper(I) chloride A...

(EC50) 45%a (Emax) 5-HT2C 55 (Ki) 22a (EC50) 81%a (Emax) SERT 830 (Ki) 394 (IC50) Notes: The smaller the value, the more avidly the drug interacts with the...

mixture of amitifadine (DOV-21,947) and its (–)-enantiomer, DOV-102,677. Its IC50 values for SERT, NET, and DAT are Ki 14 nM, 20 nM, and 78 nM, respectively...

selective inhibitor of serine/threonine-protein kinase 33 (STK33), with a IC50 of 9.2 nM. In animal studies it causes production of abnormal sperm with...

of potency NE (IC50 = 28.8 nM)> DA (IC50 = 262 nM)> 5-HT (IC50 = 2575 nM). [...] Chlorphentermine was a very potent 5-HT releaser (IC50 = 18.2 nM), a weaker...

>100,000 (IC50) Rat NETTooltip Norepinephrine transporter 10,000 (IC50) 3,560 Rat Canine DATTooltip Dopamine transporter 1,000–1,400 (IC50) 3,330 Rat...

TRPV5 and TRPV6, with an IC50 in the micromolar range ZINC17988990 is a potent and selective inhibitor of TRPV5, with an IC50 of 177nM and good selectivity...

derivative drug which acts as a competitive antagonist of the AMPA receptor (IC50 = 11 nM). It was investigated as an anticonvulsant for the treatment of epilepsy...

variety of additional effects such as inhibition of other protein kinases (IC50 values of 80, 120, 135, 270, 2600 and 2800 nM for S6K1, MSK1, PKA, ROCKII...

which initiates apoptosis. MG132 also inhibits NF-κB activation with an IC50 of 3 μM and prevents β-secretase cleavage. There are several inhibitors that...

manner (IC50 = 44 μM) by inhibiting the hydrolysis of peptide substrates. At the same time it acts as a competitive inhibitor against ERAP1 (IC50 = 73 μM)...

silent antagonist 12 α2A Agonist 1130 α2B Agonist 480 α2C Agonist 550 NR1/NR2B subunit containing NMDA receptor antagonist; ifenprodil site IC50 – 2.0...

treatment of various cancers. Entinostat inhibits class I HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM, respectively. Syndax pharmaceuticals currently holds...

{\displaystyle K_{\mathrm {M} }} V max {\displaystyle V_{\max }} Vmax calculator (ic50.tk/kmvmax.html) based on the C programming language and the non-linear least-squares...

affinity was measured at the CB1 and CB2 receptors and it was found to have an IC50 of 591 nM at CB1 and 968 nM at CB2, making it 2.3 times and 9.4 times weaker...

Transporter Ki[nM] IC50 [nM] SERT 40.2 47.3 NET 558.4 531.3...

57 (IC50) 415 (IC50) 67 (IC50) 97 (IC50) 53 (IC50) Human/rat Glycopyrrolate 0.37 1.38 1.31 0.41 1.30 Human Hexahydrodifenidol 11 200 16 76 (IC50) 83 Human/rat...

Varenicline's Binding Affinity Table Target EC50 (μM) IC50 (nM) Ki (nM) Emax (%) Action α4β2 1.30 ± 0.18 2.8 ± 1.2 0.09 20 ± 6 Partial Agonist α4β4 0.37...

oral test in 2001. Draize test EC50 (half maximal effective concentration) IC50 (half maximal inhibitory concentration) EID50 Egg Infective Dosage ELD50...

binding assay, Patch clamp) Metrics Efficacy Intrinsic activity Potency (EC50, IC50, ED50, LD50, TD50) Therapeutic index Affinity Pharmacokinetics Metrics Loading...

inhibit NR2A and NR2B subunit-containing NMDA receptors with respective IC50 values of 5.62 and 4.57 μM. As such, levomilnacipran is an NMDA receptor...

lead Dual-flashlight plot High-content screening High throughput biology IC50 / EC50 Laboratory automation Reverse pharmacology Synthetic genetic array...

oxidase A (MAO-A), whereas it was inactive at monoamine oxidase B (MAO-B) (IC50 > 100,000 nM). 3,4-DMA fails to produce stimulus generalization to dextroamphetamine...

small-molecule partial agonist of TrkB (EC50 for TrkB activation = 200–500 pM; IC50 for inhibition of BDNF binding to TrkB = 47 nM; IA = ~85%), the main receptor...

description of the binding of a substance, in the same way that EC50 and IC50 describe the biological activities of substances. Experimentally, the concentration...

stereospecific, as both L- and D-GsMTx-4 can block MSCs. Published KD value and IC50 values are listed here. GsMTx-4 might play a role in the treatment of volume-activated...

channel blockers. At lower membrane potentials, it is possible to get an IC50 in rats of 0.28nM, which shows that NPTX-8 is one of the most potent polyamine...

trimebutine also exhibits antagonistic effects in sodium channels with IC50 equal 8.4 μM and inhibits glutamate release. Oral bioavailability of trimebutine...

receptors (Ki = 12 nM vs Ki >1000 nM), where it acts as a full agonist (IC50 = 0.5 μM, Emax = 130% vs DAMGO). Herkinorin is a semi-synthetic compound...

shows significant antitumor properties in vitro (IC50=480nM against mouse B16 melanoma cells and IC50=500nM against P388 leukemia cells). It is an antineoplastic...

acts as a potent and selective inhibitor of the enzyme Rho kinase, with an IC50 of 0.6 nM at ROCK1 and 1.1 nM at ROCK2. It has vasodilatory effects and has...

human VEGFR-2, with an IC50 of 25 nmol/L and Ki of 26 nmol/L. In addition, it inhibits VEGFR-1 (IC50 = 380 nmol/L) and VEGFR-3 (IC50 = 10 nmol/L). BMS-540215...

a neurotransmitter. Tests have described tolserine as having an average IC50 value of 8.13 nM and an estimated Ki of 4.69 nM, which represents a more...

norepinephrine reuptake inhibitor (IC50 = 1.7 μM), but is substantially weaker as a dopamine reuptake inhibitor (IC50 = >10 μM). Like bupropion, hydroxybupropion...

class that acts as a norepinephrine–dopamine reuptake inhibitor (NDRI) with IC50 inhibition values of 0.0978 and 0.0467 μM, respectively (97 nM and 46 nM)...

inhibitor for Src-family kinases. It strongly inhibits the kinases Lck (IC50=4 nM), Fyn (5 nM) and Hck (5 nM), shows weaker inhibition of epidermal growth...

other racetams, nefiracetam shows high affinity for the GABAA receptor (IC50 = 8.5 nM), where it is presumed to be an agonist. It was able to potently...

Igmesine (JO-1,784) is a sigma receptor agonist (IC50 = 39 nM (rat brain)). It has neuroprotective and antidepressant-like effects in animal studies, as...

2012 due to inadequate efficacy. The selective sPLA2 inhibitor varespladib (IC50 value 0.009 μM in chromogenic assay, mole fraction 7.3X10-6) was studied...

potent and selective sirtuin 2 (SIRT2) inhibitor. It inhibits SIRT2 with an IC50 of 140nM, and is selective over SIRT1, SIRT3 and SIRT5. It is used in research...

receptor agonist (Ki > 5 μM; EC50 > 5 μM) Farnesoid X receptor antagonist (IC50 = 5–50 μM) Pregnane X receptor agonist (EC50 = 2.4 μM ((Z)-isomer)) Guggulsterone...

1-methylnaphthyl PP1 (MN-PP1), which inhibited hole-modified yeast kinases with IC50 values in low nanomolar concentrations. The BET (Bromodomains and Extra Terminal)...

Stimulant Cocaine 304 779 478 SNDRI Stimulant Cocaine 313±17 (IC50) 292±34 (IC50) 211±19 (IC50) SNDRI Stimulant Desipramine 17.6 0.83 3,190 SNRI TCA Desmethylcitalopram...

guvacine isolated from the A. catechu are effective antagonists of GABA, with IC50 values 122712 μM and 871 μM, respectively (Johnston et al., 1975; Lodge et...

nM, respectively), but has ~2-fold lower affinity than JJC8-016 at hERG (IC50 = 0.13 and 0.06 μM, respectively). Ku TC, Cao J, Won SJ, Guo J, Camacho-Hernandez...

α2δ VDCC subunit with similar affinity as gabapentin and pregabalin (e.g., IC50 = 71 nM for L-isoleucine), and are present in human cerebrospinal fluid at...

Angeles, California, USA first identified bisantrene to also be a potent (IC50 = 142nM) inhibitor of the Fat Mass and Obesity (FTO) associated protein,...

estradiol). It also has weak affinity for the androgen receptor in vitro (IC50 = 277 nM relative to 15 nM for dihydrotestosterone), but doesn't appear to...

Monoamine transport inhibition, IC50 (μM) NET 2.02 (1.5–2.7) DAT 2.90 (2.5–3.4) SERT 6.22 (4.3–9.0)...

potent in vitro cytotoxicity against HCT-116 human colon carcinoma with an IC50 value of 11 ng mL-1. This compound also displayed potent and highly selective...

widely among individual plants and populations. Notes: In brackets is the IC50/EC50 value depending on whether it is an inhibitory or inductive action being...

alkaloids. A standardised ethanolic extract of dried M. tortuosum had an IC50 for SERT of 4.3 μg/ml and for PDE4 inhibition of 8.5 μg/ml. Kanna inhibits...

attracted research interest because it is an inhibitor of pancreatic lipase (IC50 0.4 μg/mL) with in vitro activity comparable to that of the obesity drug...

time-dependent inhibition and their potency therefore cannot be characterised by an IC50 value. This is because the amount of active enzyme at a given concentration...

binding assay, Patch clamp) Metrics Efficacy Intrinsic activity Potency (EC50, IC50, ED50, LD50, TD50) Therapeutic index Affinity Pharmacokinetics Metrics Loading...

inhibition of the targeted activity of BTK, while having a much greater IC50 or otherwise virtually no inhibition on the kinase activities of ITK, EGFR...

doi:10.1111/bph.14832. PMC 6965684. PMID 31418454. TABLE 1 Summary of pIC50 (negative logarithm of the molar concentration of these compounds at which...

transmembrane alpha-helical segments (S1-S6). Grayanotoxin has a binding affinity (IC50) of approximately 10 μM and binds the group II receptor site located on segment...

when administered as tablets to 40% as an oral solution. Candesartan has an IC50 of 15 μg/kg. The active form of candesartan is not used directly in clinical...

IC50 of ibuprofen Enzyme IC50 [μM] COX-1 13 COX-2 370...

replaced with an oxazole ring inhibited VDR-meditated transcription with IC50 of 660 nM. Other novel analogues which are more potent than GWO742 with reduced...

d-LSD: IC50: [3H]5-HT: 10 [nM]. d-[3H]LSD: 8 [nM]. [...] d-Isolysergic acid amide. IC50: [3H]5-HT: 100 [nM]. d-[3H]LSD: 200 [nM]. [...] l-LSD. IC50: [3H]5-HT:...

uptake into mitochondria. It is still relatively selective for SIRT2 with an IC50 of 62nM at SIRT2 vs 530nM at SIRT3, but this still makes it one of the most...

has been shown to inhibit COX-1 (but not COX-2) with a 3-18 times lower IC50 compared to aspirin, a range that may be relevant for typical doses. Calcitriol...

1.38 Phenibut 9.6 >100 4-F-phenibut 1.70 >100 Baclofen 0.13 >100   (R)-Baclofen 0.13 >100   (S)-Baclofen 74.0 >100 Values are IC50 (μM) in rat brain....

half-maximal inhibitory concentration of 5.2 μM. For comparison, amphetamine has an IC50 of 11 μM and 4-methylthioamphetamine (4-MTA) has a value of 0.2 μM. The chemical...

even at very high concentrations (100 μM). NM-2AI has high affinity (2.4 μM IC50) as a norepinephrine reuptake inhibitor but also has affinity as a TAAR1...

marketed as a cough suppressant. It binds to the sigma-1 receptor with an IC50 value of 190 nM. It also has local anesthetic action, and in large doses...

extracts. Clavaric acid is a reversible farnesyltransferase inhibitor with an IC50 of 1.3 μM. Lingham RB, Silverman KC, Jayasuriya H, Kim BM, Amo SE, Wilson...

act as a potent and weakly selective serotonin releasing agent (SSRA) with IC50 values of 82 nM, 1,848 nM, and 849 nM for inhibiting the reuptake of serotonin...

inhibitor of the enzyme 15-hydroxyprostaglandin dehydrogenase (15-PGDH), with an IC50 of 56 nM. It increases levels of prostaglandin E2 and stimulates tissue regeneration...

PFKFB3 inhibitor (3PO was inactive in a kinase PFKFB3 inhibition assay (IC50 > 100 μM)) (see the corresponding discussion in § Small molecule inhibitors...

transporters, though it does possess low affinity for the sigma receptor (IC50 = 286 nM). Blonanserin has a relatively high affinity towards the 5-HT6 receptor...

shown to possess the highest inhibitory activity against cyclooxygenase (IC50 = 24 μg/mL), among other citrus studied. Flavedo extract of ripe Lumia inhibited...

negative allosteric modulator of the α7-nicotinic acetylcholine receptor (IC50 < 1 μM). Moreover, (2S,6S)-HNK was tested and found to increase the function...

serine and cysteine proteases, human leukocyte elastase and cathepsin B (IC50 > 30 μM). Its development was halted in phase Ib clinical trials because...

EPPTB is 272-fold less potent at the hTAAR1 (IC50 = 7,487 nM) and 165-fold less potent at the rTAAR1 (IC50 = 4,539 nM) in vitro. EPPTB seems to not be...

hepatocytes and is considered to be a potential contributor for the low IC50 for rosuvastatin in hepatocytes. Of the marketed statins, cerivastatin was...

breast cancer. Norethisterone is a very weak inhibitor of CYP2C9 and CYP3A4 (IC50 = 46 μM and 51 μM, respectively), but these actions require very high concentrations...

sensitive to piperaquine in vitro; i.e. piperaquine appears to have the same IC50 in sensitive parasites and resistant parasites. The mechanism by which parasites...

Perampanel did not affect NMDA receptor currents. The extent of block (IC50, 0.56 μM) was similar at all agonist concentrations, demonstrating a noncompetitive...

doi:10.1111/bph.14832. PMC 6965684. PMID 31418454. TABLE 1 Summary of pIC50 (negative logarithm of the molar concentration of these compounds at which...

after inhibition of telomerase activity in vitro.[medical citation needed] IC50 values ranged from 50 to 200nM for 10 different pancreatic cell lines. The...

potency as GABAA receptor positive allosteric modulators (e.g., affinity (IC50 = 50 nM or improved by 6-fold) have been developed and reported. Lirequinil...

Rheb an attractive approach. However, since HY-124798 has a relatively weak IC50 of 2.1μM, and Rheb also has other targets in addition to mTORC1, it remains...

proliferation and T cell activation. Ursolic acid is a weak aromatase inhibitor (IC50 = 32 μM), and has been shown to increase the amount of muscle and brown fat...

androgen receptors (mARs) and found to act as a potent antagonist of ZIP9 (IC50 = 66.3 nM), whereas it does not appear to interact with GPRC6A. The affinity...

5-methoxytryptoline are the most active monoamine oxidase inhibitors (MAOIs) with IC50 values of 500 nM and 1,500 nM, respectively. Tryptolines are also potent...

doi:10.1111/bph.14832. PMC 6965684. PMID 31418454. TABLE 1 Summary of pIC50 (negative logarithm of the molar concentration of these compounds at which...

workload and improving left ventricular function. The IC50 for SGLT2 is less than one-thousandth of the IC50 for SGLT1 (1.1 versus 1390 nmol/L), so that the...

calcium channel (IC50 = 88nM[2]). However, sensitivity of the drug on the channel depends on the species and the tissue. For example, the IC50 for block of...

nausea, dizziness, and drowsiness. It binds to the sigma-1 receptor with an IC50 value of 25 nM. "Caramiphen". drugs.com. Retrieved 26 September 2012. "Caramiphen...

(MDA) and 3,4-methylenedioxy-N-methylamphetamine (MDMA). 6-Methyl-MDA has IC50 values of 783 nM, 28,300 nM, and 4,602 nM for inhibiting the reuptake of...

nucleoside 5-prime monophosphate. AMG-579 Balipodect (TAK-063): IC50 = 300 pM Compound 96: IC50 = 700 pM, high selectivity against all other members of the...

determine the shape and function of the GABAA receptors, at which it has an IC50 of 4.1nM. Difludiazepam has subsequently been sold as a designer drug, and...

deacetylase (HDAC) inhibitor, with half maximal inhibitory concentrations (IC50) of 62 nM, 570 nM and 550 nM, against HDAC1, HDAC2 and HDAC3, respectively...

the α2δ VGCC subunit with similar affinity as the gabapentinoids (e.g., IC50=71 nM for L-isoleucine), and are present in human cerebrospinal fluid at...

dividing the EC50 or the IC50 of the eutomer by the same measurement of the distomer. Whether one chooses to use the EC50 or IC50 depends on the drug in...

Finasteride mainly inhibits the 5α-R2 (IC50=69 nM) and 5α-R3 (IC50=17.4 nM) with little inhibition of 5α-R1 (IC50=360 nM). As mentioned above, finasteride...

nanomolar) 121 161 2250 IC50 (nM) 20 23 1600 NET Ki (nM) 788 206 >10000 IC50 (nM) 51 39 980 SERT Ki (nM) >10000 >10000 >6700 IC50 (nM) — >10000 >10000 GPCR...

inhibits the cytochrome P450 enzymes CYP2C9 (IC50 = 130.95 μM), CYP2C19 (IC50 = 10.05 μM), and CYP3A4 (IC50 = 78.59 μM), indicating potential drug interaction...

1,100–1,718 (Ki) 6,700–11,000 (IC50) ND (EC50) DATTooltip Dopamine transporter 7,200–>10,000 (Ki) 99,000–117,000 (IC50) ND (EC50) Notes: The smaller the...

inhibitor through high-throughput screening. An isobutyl analog (table 2) showed IC50=0.7 μM submicromolar activity against NS5B. In the development, 5-phenyl...

of CDC2-like kinases (CLKs), primarily targeting CLK2 with high potency (IC50 of 1.4 nM). It is being developed as a potential treatment for certain cancers...

inhibition of noradrenaline uptake (Egawa et al., 1983), although weak (IC50 = 10-6-10-7 M), coexist. {{cite book}}: |journal= ignored (help) Kondo Y...

tamoxifen, has been found to act as a potent competitive aromatase inhibitor (IC50 = 90 nM), and may also be involved in the antiestrogenic activity of tamoxifen...

It has a good selectivity against CYP450 enzymes (CYP1A2 IC50 = 1.8 µM, other isoforms IC50 > 10 µM). It has a brain:plasma ratio of 37, t1/2 of 1.1 and...

of serotonin, norepinephrine, dopamine) and of GABA and glutamate, with IC50 values of 0.05–0.10 μg/mL for all compounds, with the exception of glutamate...

study interactions as opposed to actual functional reuptake inhibition (IC50). Trimipramine is extensively metabolized, so its metabolites may contribute...

receptors, including the 5-HT7 and 5-HT1A receptors, with high affinity (IC50 ≤ 2 nM) and selectivity, and displays agonist activity. It also shows lower...

although it is known to be a phosphodiesterase inhibitor. It is a potent (IC50 = 36nM) inhibitor of phosphodiesterase-II.[citation needed] It inhibits PDE-3...

particles from beef heart, presumable by interfering with NADH oxidase activity (IC50 1.5 μM and 2.5 μM, respectively). First total synthesis of circumdatin H...

Lasofoxifene selectively binds to both ERα and ERβ with high affinity. Its IC50 for ERα (1.5 nM) is similar to that of estradiol (4.8 nM) and is at least...

electrostatic properties, causing altered pharmacological effects. Table 1: IC50 values of four subgroups of hainantoxins HNTX-I, HNTX-III, HNTX-IV, and HNTX-V...

norepinephrine, and dopamine transporters are weak. According to the article, the IC50 values are 240μM (5-HT, human platelets), 474 μM (5-HT, rat brain synaptosomes)...

together occur in about 40% of AML cases. The compound shows high potency with IC50 values in the nanomolar range and has demonstrated encouraging activity in...

the IC50 value which gives the concentration of the compound at which it causes 50% of its inhibitory effect e.g. on enzymes in cells. The IC50 values...

endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF) with IC50 of 0.2, 2, 4, and 7 nM for human endothelial cells, PDGF receptor beta (PDGFR-β)...

acts as a potent sirtuin 2 (SIRT2) inhibitor. It inhibits SIRT2 with an IC50 of 28 nM, though its activity at other SIRT subtypes has not been well characterized...

Studies on acute toxicity in mice have determined a median lethal dose (IC50) for injection of 2.0 mg\kg. However, no specific lethal or save dose has...

Human enzyme and GPCR binding Inhibited enzyme IC50 (nM) Entry note HDAC1 16,000 HDAC2 12,000 HDAC3 9,000 HDAC4 2,000,000 Lower bound HDAC5 2,000,000 Lower...

inhibits acetylcholinesterase (AChE) and ascorbic acid biosynthesis. The IC50 of lycorine was found to vary between the different species it can be found...

Human 5-HT2A 6.3–69 Human 5-HT2B 200 Human 5-HT2C 8.9–39 Human 5-HT3 8.1 70 (IC50) Human 5-HT4L 10000+ Human 5-HT5A 670 Human 5-HT6 ND ND ND 5-HT7 265 Human...

some activity against the malarial pathogen Plasmodium falciparum with an IC50 value of 1 to 2 microgram/millilitre (as did almost everything tested), though...

determine the concentration that results in half maximal binding or activity (IC50 or EC50 value respectively). Orthogonal testing: confirmed hits are assayed...

selective norepinephrine reuptake inhibitor (IC50 = 1,700 nM) with no apparent inhibition of dopamine reuptake (IC50 > 10,000 nM). Normally, activity with racemic...

FEP scans identified diaminotriazoles that inhibit STAT5 phosphorylation (IC50 < 10 nM) and show cell-active potency against hyperproliferative models,...

(ER)-positive metastatic breast cancer. The drug is a silent antagonist of the ERα (IC50 = 4.1 nM) as well as a selective estrogen receptor degrader (SERD). It is...

for SERT, NET, and DAT of amitifadine are 99 nM, 262 nM, and 213 nM. The IC50 values for serotonin, norepinephrine and dopamine uptake are 12, 23 and 96 nM...

Receptor: GABAA. Receptor ligand: [3H]muscimolA. Compound: nefiracetam. IC50: 8.5 nMB. Refs.: 222. [...] From Table 1 it is, however, evident that the...

κ-opioid receptor (KOR) (Ki = 140 nM), and the sigma σ1 receptor (Ki = 42 nM; IC50 = 19 nM), whereas it has only low affinity for the δ-opioid receptor (Ki...

the rat and mouse, respectively. At the human ERβ and ERα, WAY-166818 has IC50 values of 29 nM and 1227 nM (25-fold difference), respectively. The compound...

the first selective SIRT2 inhibitors developed, and inhibits SIRT2 with an IC50 of 3.5μM, making it less potent than other more recently developed compounds...

antagonist for both AMPA receptors, which have an IC50 value of 400 nM, and kainate receptors, which have an IC50 value of 4 μM. It also noncompetitively inhibits...

methicillin resistance more effectively than EGCG at low concentrations (IC50 ~50 μM). It also disrupts staphylococcal virulence by reducing coagulase...

affinities. ɑ p <0.05 versus Ki of (±)—threo-methylphenidate. b p <0.05 versus IC50 of (±)—threo-methylphenidate. c p <0.05 versus its corresponding Ki. Additional...

depression. DPI-3290 acts as an agonist at both μ- and δ-opioid receptor, with an IC50 of 6.2nM at μ and 1.0nM at δ. AZD2327 BW373U86 DPI-221 DPI-287 US Patent...

inhibits 5α-R2 at a mean inhibitory concentration IC50 of 69 nM, but is less effective with 5α-R1 with an IC50 of 360 nM. Finasteride decreases mean serum level...

that MAOB does not contribute to DA degradation [39]. KDS2010 is a potent (IC50 = 7.6 nM), and selective MAOB inhibitor named shows no known off-target effect...

estradiol from estrogen receptors, particularly ERβ, with 4-MBC showing an IC50 of 35.3 μM for ERβ binding. The compound stimulates MCF-7 breast cancer cell...

Half-maximal inhibitory concentration) Rat DATTooltip Dopamine transporter 29,000 (IC50) Rat VDCCTooltip Voltage-dependent calcium channel >10,000 Rat Notes: Values...

and 1D receptors has been seen. It is also a serotonin reuptake inhibitor (IC50 = 1.4 nM) and has been reported to act as a 5-HT2A receptor antagonist as...

(Ki) 45,000 (IC50) IA (EC50) DATTooltip Dopamine transporter >30,000 (Ki) 626,000 (IC50) IA (EC50) MAO-ATooltip Monoamine oxidase A ND (IC50) MAO-BTooltip...

titration – process of finding the correct dose of a drug Effective dose EC50 IC50 LD50 Hormesis Trevor A, Katzung B, Masters S, Knuidering-Hall M (2013). "Chapter...

enzyme isolated from HeLa cells with a half maximal inhibitory concentration (IC50) of 79 nM. BI 99179 showed acute efficacy in rat models. Increased hypothalamic...

to avoid the electrostatic clash. That's why the IC50 value for thrombin is >1000μM while the IC50 value for FXa is 0.16μM. Rivaroxaban binding to FXa...

pocket. These include dovitinib and brivanib. The table below provides the IC50 (nanomolar) of small-molecule compounds targeting FGFRs. FGFR1 mutation in...

to inhibit the reuptake of serotonin, dopamine, and norepinephrine with IC50 values of 322 nM, 1,997 nM, and 980 nM, respectively. These values are very...

inhibition of human 5α-reductase type I over 5α-reductase type II, with IC50 values of 0.9 nM and 154 nM, respectively. The drug was under investigation...

preceding actions, the drug is a monoamine oxidase A (MAO-A) inhibitor, with an IC50 of 945 nM. It produces anxiolytic-like and antiobsessional-like effects in...

bonds, and therefore it reduces the metabolism. The Cl atom also reduces the IC50 value of the medication, so the medication has better activity. The carbon-fluorine...

inhibitory effect on PMAT activity when used at higher than normal dosages (IC50 test values used in trials were 3–4 fold higher than typical prescriptive...

molecular motif yielded SERT inhibitors with nanomolar and subnanomolar IC50 values. Indalpine is the generic name of the drug and its INNTooltip International...

receptors (subtype M1) and as an agonist at sigma receptors (subtype σ1) with an IC50 of 9 nM. Its anticholinergic properties can theoretically relax the pulmonary...

[3H]Nisoxetine binding 609 16628 6576 2.27 NMDA-induced current 768 2 0.020 95 All values are IC50 (nM), except NMDA-induced current, which is IC50 (μM)....

concentration of 60 nM. It is also a weak dopamine reuptake inhibitor (DRI), with an IC50 of 1,490 nM at the dopamine transporter (DAT). Harmane shows weak affinity...

Orlistat Esterastin Valilactone Panclicin D Ebelactone Vibralactone Structure IC50 value 6.9 × 10−2 μg/ml 1.2 × 10−1 μg/ml 2.0 × 10−1 μg/ml 1.4 × 10−4 μg/ml...

49nM. It is also a weak antagonist at the related receptor GPR55, with an IC50 of 6350nM, but has no significant affinity for GPR18. PSB-SB-487 Rempel V...

pharmacodynamics. To compare inhibitors, the parameter of choice is IC50; by measuring IC50 for different JAKs, determining selectivity is possible. In the...

channels, Gomora's team found that ethosuximide blocked the channels with an IC50 of 12 ± 2 mmol/L and that of N-desmethylmethsuximide (the active metabolite...

agonist of the δ-opioid receptor with far lower potency (Ki = not reported, IC50 = 184 nM, and Imax = 68% for (±)-alazocine against the mouse receptor transfected...

found to act as a serotonin–norepinephrine reuptake inhibitor (SNRI), with pIC50 values of 5.86 for the serotonin transporter (SERT) and 5.68 for the norepinephrine...

mechanism of action. Linopirdine blocks the KCNQ2\3 heteromer M current with an IC50 of 2.4 micromolar disinhibiting acetylcholine release, and increasing hippocampal...

a weak serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI) with IC50 values of 5,289 nM, 8,869 nM, and 6,844 nM, respectively, as well as a weak...

to specifically act on PDE2 by inhibiting cGMP-activation of PDE2 with an IC50 value of ~1μM and an at least 50-fold selectivity over other PDEs. The core...

with an IC50 of 65 nM. N-indol-1-amide compound is a possible anti-tumor drug in combination with other anticancer treatment and has an IC50 value of...

transporter were 16 nM, 211 nM, and 638 nM, respectively. Conversely, its IC50 values for inhibition of dopamine, norepinephrine, and serotonin reuptake...

Ki (nM) SERT 0.8–1.1 NET 7,800 DAT 27,400 5-HT1A >1,000 5-HT2A >1,000 5-HT2C 2,500 α1 3,900 α2 >1,000 D2 >1,000 H1 2,000 mACh 1,240 hERG 2,600 (IC50)...

histone demethylase, BHC110/LSD1. Tranylcypromine inhibits this enzyme with an IC50 < 2 μM, thus acting as a small molecule inhibitor of histone demethylation...

NETTooltip Norepinephrine transporter ND (Ki) ND (IC50) ND (EC50) DATTooltip Dopamine transporter ND (Ki) ND (IC50) ND (EC50) Notes: The smaller the value, the...

It acts as a competitive inhibitor of 3β-hydroxysteroid dehydrogenase (IC50 = 1 μM), and thereby inhibiting the formation of progesterone, corticosteroids...

and inhibits IL-17 production by CD4 T cells stimulated with IL-15 with IC50 of 20 to 60 nM. Y-320 also inhibits the production of IFN-γ and TNF-α by...

doi:10.1111/bph.14832. PMC 6965684. PMID 31418454. TABLE 1 Summary of pIC50 (negative logarithm of the molar concentration of these compounds at which...

acts as a potent and selective inhibitor of the enzyme Rho kinase, with an IC50 of 14.5 nM at ROCK1 and 6.2 nM at ROCK2. It has been investigated for applications...

A small shift in the steady-state inactivation curve has been reported. IC50 is 0.25 μM. HLTx inhibits both delayed rectifier and A-type potassium channels...

inhibited the uptake of [3H]-norepinephrine with an IC50 = 5.8 μM; l-synephrine was less potent (IC50 = 13.5 μM). d-Synephrine also competitively inhibited...

voltage-gated potassium channel Kv1.1. Pi4 reversibly blocks this channel with an IC50 of 3.0 ± 2.2 nM. A Pi4 peptide, synthesized with a different C-terminus than...

selective antagonist for the TRPV2 receptor. It is moderately potent with an IC50 of 460nM, but is highly selective for TRPV2 over the other subtypes of TRPV...

rat and human 5α-reductase with half-maximal inhibitory concentrations (IC50) of 15 and 16 nM, respectively, while finasteride had values of 30 and 52 nM...

, 2014), and it is also a 5-HT3A and 5-HT3AB antagonist with respective IC50 values of 0.66 and 2.7 µM (Thompson and Lummis, 2008). Though the studies...

moiety. Like aspirin, perilloxin inhibits the enzyme cyclooxygenase with an IC50 of 23.2 μM. Other chemotypes include eschscholzia ketone, perillene, and...

IC224 inhibits PDE1 (IC50 = 0.08 μM) with a selective ratio of 127 (ratio of IC50 value for the next most sensitive PDE and for IC50 value for PDE1). It...

activity via noncompetitive inhibition of the dual specificity kinase MEK with IC50 of 72 nM for MEK1 and 58 nM for MEK2. U0126 inhibited anchorage-independent...

norepinephrine. The respective EC50 values are 200 nM, 730 nM, and 37 nM, while the IC50 values are 770 nM, 6800 nM, and 420 nM. The drug shows some affinity for...

concentration) Rat 5-HT2C ND ND ND α1 460 (IC50) Rat D1 10000+ Mouse D2 378 560 (IC50) Mouse Rat H1 2.0–19 6.4 100 (IC50) Human Bovine Rat H2 ND ND ND H3 ND...

SNRIs at the human SERT and NET Compound SERT NET ~Ratio (5-HT : NE) Ki IC50 Ki IC50 Venlafaxine 7.8 145 1920 1420 ~1:2 Desvenlafaxine 40.2 47.3 558.4 531...

dextrallorphan was found to have a half maximal inhibitory concentration (IC50) for binding to the pituitary and brain receptor of 10,000 ± 1000 nM and...

Conversely, it is inactive as a dopamine and norepinephrine reuptake inhibitor (IC50 = >10,000 nM). Similarly to DMT, but in contrast to most other psychedelics...

Activities of dihydroergotamine at various sites Site Affinity (Ki/IC50 [nM]) Efficacy (Emax [%]) Action 5-HT1A 0.4–1.5 100% Agonist 5-HT1B 0.006–18 ?...

Cymserine and derivatives Profenamine Rivastigmine Tacrine (+)-ZINC-12613047: IC50 human BChE 13nM, high selectivity over AChE. Hybrid/bitopic ligands The nomenclatural...

Plasmodium falciparum (IC50 = 115 nM against K1 strain) and P. berghei (ED50 = 250 mg/kg in vivo). Its C14-epi analog shows higher potency (IC50 = 56 nM; ED50...

binding assay, Patch clamp) Metrics Efficacy Intrinsic activity Potency (EC50, IC50, ED50, LD50, TD50) Therapeutic index Affinity Pharmacokinetics Metrics Loading...

potent and selective sirtuin 2 (SIRT2) inhibitor. It inhibits SIRT2 with an IC50 of 15.5 nM, and is highly selective over SIRT1, SIRT3 and SIRT5, however...

Waglerin-1 inhibited the adult mouse endplate response to acetylcholine with an IC50 of 50 nanomolar. In striking contrast, transmission across neuromuscular...

3,026 NR2B 8,720 SERTTooltip Serotonin transporter 1,411–1,800 (Ki) 383 (IC50) DATTooltip Dopamine transporter IA Notes: The smaller the value, the more...

assay using hA3-CHO-cells indicated that PSB-10 acts as an inverse agonist (IC50 = 4 nM). It has been shown to produce antiinflammatory effects in animal...

was found to possess anticancer activity ... Alpha-hederin also, in sub-IC50 cytotoxic concentrations, was shown to enhance the cytotoxicity of 5-fluorouracil...

efficiency for a compound is defined as its potency, via measured values of pIC50 or pEC50, minus its value of log P. In the context of pharmacokinetics (how...

be cytotoxic against 25 different human cancer cell lines with an average IC50 value of 9.4 μg/mL, ranging from 3.5 (NEC) to 45 (A549) μg/mL. Torreyanic...

irreversible inhibition of selenoenzymes, such as thioredoxin reductase (IC50 = 9 nM). Although it has many functions, thioredoxin reductase restores vitamins...

Transporter Ki [nM] IC50 [nM] SERT 82 27 NET 2480 535 DAT 7647 ND...

PI3K-α with elevated kinase activity at concentrations equivalent to the IC50 for wild-type PI3K-α. PI3K-β, -δ and -γ isoforms were inhibited by gedatolisib...

suppresses the growth and proliferation of MCF-7 cancer cells. The results of IC50 determination (Liu et al.) of compounds of Melilotus officinalis (Linn.)...

binding to H1 histamine receptors, and dopaminergic (D2) receptors. The IC50 (half-maximal inhibitory concentration) of cinnarizine for smooth muscle...

(IC50Tooltip half-maximal inhibitory concentration = 2.5 nM) and 17,20-lyase (IC50 = 15 nM) (approximately 6-fold more selective for inhibition of 17α-hydroxylase...

(IC50Tooltip half-maximal inhibitory concentration = 69 nM) over 17α-hydroxylase (IC50 = 670 nM), which results in less interference with corticosteroid production...

painful stimuli such as heat. Depending on the pharmacological assay, the IC50 is in the nanomolar to low micromolar range. In addition to its effects on...

5-Methyl-MDA acts as a selective serotonin releasing agent (SSRA) with IC50 values of 107nM, 11,600nM, and 1,494nM for serotonin, dopamine, and norepinephrine...

line MDA-MB231. MTT assays conducted three days after treatment showed an IC50 value of 94.63 + 1.63 μg/ml. A guaianolide, lactucin-8-0-methylacrylate,...

patients receiving lopinavir/ritonavir found lopinavir CSF levels above the IC50 in 77% of samples. A 2014 study indicates that lopinavir is effective against...

concentration ranges for a selection of related compounds and the midpoints (IC50) of the calibration curves are calculated and compared. The figure then provides...

drug binds to the site. Values at the mAChRsTooltip muscarinic acetylcholine receptors and hERGTooltip Human Ether-à-go-go-Related Gene are IC50 (nM)....

to H-460 human lung and Neuro-2a mouse neuroblastoma cell lines with an IC50 value of 15 μM for both cell lines. This compound also displayed low micromolar...

depression, DOV-102,677 is being developed for the treatment of alcoholism. IC50 values for the SERT, NET and DAT are 129 nM, 103 nM, and 133 nM. DOV-102...

responsible for the conversion of 4-androstene-3,17-dione to testosterone, with IC50 of 1.4 μM. Umbelliferone is the parent compound for a large number of natural...

Transporter EC50 [nM] IC50 [nM] SERTTooltip Serotonin transporter 211 1194 NETTooltip Norepinephrine transporter 19 290 DATTooltip Dopamine transporter...

acetylcholine receptors 700–8900 (IC50) 1300–29600 (IC50) Rat VDSCsTooltip Voltage-dependent sodium channels 50000+ (IC50) ND Rat Values are Ki (nM), unless...

receptor activity and inhibits the reuptake of serotonin (IC50 = 31uM) and norepinephrine (IC50 = 63uM) in rat brain synaptosomes.1,2 30C-NBOMe exhibits...

(both with bicyclo[3.1.0]hexane skeleton) ML337: selective NAM, IC50 = 450 nM for mGluR3, IC50 >30μM for mGluR2 MNI-137: inhibitor VU-0650786: NAM compound...

Cheng–Prusoff equation to calculate the absolute inhibition constant Ki (IC50). In 1974, Cheng became an assistant professor in pharmacology at the State...

Type Affinity (nM) F3 Human IC50 23 RT HIV-1 IC50 562000 D1/1A Human IC50 1630 166±8 D1/1A Human Ki 231 124±6 D2 Human IC50 450 1470±270 D2 Human Ki 1130...

rimonabant. Guineesine is also a monoamine oxidase inhibitor (MAOI) in vitro (IC50 = 139.2 μM). Liu W, Jiang Z, Chen J, Zhang X, Ma Y (May 2009). "荜茇三氯甲烷部位化学成分研究"...

amyloid β in guiena pig brain at 1.83 mg/kg, sc. Another study showed, that IC50 values for cell-free enzyme assay (amyloid β1-40), whole-cell assay (amyloid...

1,300–4,574 (Ki) 10,000–11,000 (IC50) ND (EC50) DATTooltip Dopamine transporter 5,031–5,400 (Ki) 53,000–65,000 (IC50) ND (EC50) Notes: The smaller the...

activities of minocycline include: PARP1 inhibition Ki = 13.8 nM Neuroprotection IC50 = 10 nM Microglia full inhibition = 20 nM Suppression of the mouse's locomotor...

IC50 was determined by an automated cell culture growth inhibition assay which shows IC50 ranging from 2-8 mM, depending on the cell type. The IC50 was...

Norepinephrine transporter 13,000 (Ki) 11,000 (IC50) IA (EC50) DATTooltip Dopamine transporter >26,000 (Ki) >100,000 (IC50) IA (EC50) Notes: The smaller the value...

activity Neuropeptide VF (NPVF) (RFRP-3) – agonist of the NPFF1 receptor (IC50 = 0.7 nM) NPSF and NPVF, originally referred to as the RFamide-related peptides...

uptake Drug Uptake Inhibition at DAT IC50 (nM) Uptake Inhibition at NET IC50 (nM) Uptake Inhibition at SERT IC50 (nM) Mephedrone (4-MMC) 769 ± 106 319...

and 5-HT2A receptor activity of substituted tryptamines [...] d Value is IC50 for uptake inhibition in nM. Reyes-Parada M, Iturriaga-Vasquez P, Cassels...

stronger affinity for NMDA receptors. Kaitocephalin's IC50 for NMDA receptors is around 75 nM, while its IC50 for AMPA receptors is 200-600 nM. It is also a...

analog (PAL-424) caused the compound to become a DAT uptake inhibitor with an IC50 value of 1013 nM. Increasing the size even further to butyl (PAL-90) rendered...

binding affinity to αvβ6-integrin (IC50 = 0.047 nM). Its affinity to other RGD-binding integrins is much lower (IC50 for αvβ3, αvβ8, and α5β1 are 2.7,...

highly irritant, with a wide range of half-maximal inhibitory concentration (IC50) values. The median lethal dose (LD50) of phorbol esters for male mice was...

integrated within CDD Vault to generate, QC, and analyze results such as IC50, pIC50, EC50. AI Artificial intelligence in pharmacy Web application within...

transporter >10,000 (Ki) ND (IC50) DATTooltip Dopamine transporter >10,000 (Ki) ND (IC50) MAO-ATooltip Monoamine oxidase A 352 (Ki) 540 (IC50) MAO-BTooltip Monoamine...

NETTooltip Norepinephrine transporter 30–58 13 (IC50) Human DATTooltip Dopamine transporter >10,000 4,600 (IC50) Human 5-HT1A 276 Human 5-HT2A 11–27 Human...

those found in Bougainvillea spectabilis (Nyctaginaceae) leaves (with an IC50 of 7.23 μM), typically used in folk medicine. Xanthine dehydrogenase Sodium...

The most potent compound in the study was claimed to be 16. This had a DAT IC50 of 1.75 nM. The chemical name of this compound is 1-[3-[N...

Compd DAT (Ki) DA (IC50) NET (Ki) (IC50) D-TMP 161 23 206 39 L-TMP 2250 1600 >10K 980 DL-TMP 121 20 788 51...

uptake 1,424 (IC50) Inhibitor Rat [3H]NIS binding 16,628 (IC50) Inhibitor Rat [3H]DA uptake 347 (IC50) Inhibitor Rat [3H]CFT binding 1,547 (IC50) Inhibitor...

same time. Another factor that supports this theory is the estimated IC50. The IC50 for inhibition of activation is approximately 400-fold smaller than...

Compound pIC50 R1 R2 R3 ATP 3.6 O C C-NH2 1A 3.5 C C-NH2 1B 8.6 C-NH2 1C 9.1 Cangrelor 9.4...

SNDRI). For another related SNDRI agent see PC71812205. The racemic agent had IC50's of 11, 14, 190nM S~N>D. Artaiz I, Zazpe A, Innerárity A, Del Olmo E, Díaz...

d-LSD: IC50: [3H]5-HT: 10 [nM]. d-[3H]LSD: 8 [nM]. [...] d-Isolysergic acid amide. IC50: [3H]5-HT: 100 [nM]. d-[3H]LSD: 200 [nM]. [...] l-LSD. IC50: [3H]5-HT:...

transporter 6,500–>10,000 (Ki) 3,900 (IC50) 4,166 (EC50) ND (Emax) DATTooltip Dopamine transporter >10,000–22,000 (Ki) 52,000 (IC50) >10,000 (EC50) 5.4% (Emax)...

active metabolite, desmethylketamir (norketamir), which has an affinity (IC50) for the PCP site of the NMDA receptor of about 470 μM. Ketamir-2 showed...

which benzoctamine carries out its effects, studies have shown it to have an IC50 value of 115 mM at the serotonin receptor. Benzoctamine can be injected directly...

stage 3. IC50 values in patent for compound 225: hSERT=7nM, hNET= 23nM, hDAT=167nM. Although in the earlier patent (277 on scheme 36) IC50 values (nM)...

inhibitory concentration) (rat) MAO-BTooltip Monoamine oxidase B >100,000 (IC50) (rat) Notes: The smaller the value, the more avidly the drug binds to the...

inhibits PfPDE1, a P. falciparum cGMP-specific phosphodiesterase, with an IC50 value of 3.8 μM. Xanthines such as caffeine and theobromine are cAMP-phosphodiesterase...

NETTooltip Norepinephrine transporter ND (Ki) 5,400 (IC50) DATTooltip Dopamine transporter ND (Ki) 65,000 (IC50) VMATTooltip Vesicular monoamine transporter 10%...

(50–500 μM) and likely not clinically relevant. Although one study found an IC50 for dopamine transport of 3.56 μM, relative to 28.66 nM for mesocarb; neither...

~900 (IC50) 992–1,190 >20,000 (IC50) 2,980 ((−)) (IC50) Human Rat NETTooltip Norepinephrine transporter 14,600 785 1,080 (−) (IC50) 860 (IC50) Human...

doi:10.1111/bph.14832. PMC 6965684. PMID 31418454. TABLE 1 Summary of pIC50 (negative logarithm of the molar concentration of these compounds at which...

dramatically weaker as an inhibitor of acetylcholinesterase (AChE), with an IC50 of only 6300 nM, while it is a potent inhibitor of two enzymes monoacylglycerol...

It is reported to have bioactivity against Plasmodium falciparum with an IC50 = 2.3 μg/mL (4.7 μM). Pure codinaeopsin was reported to be isolated with...

However, formebolone was found to be a very weak inhibitor of 11β-HSD type 2 (IC50 > 10 μM), although this specific isoenzyme of 11β-HSD is responsible for...

inhibit replication of SARS-CoV-2 in monkey kidney cell culture with an IC50 of 2.2–2.8 μM. However, doses much higher than the maximum approved or safely...

RAD51, which is a central gene molecule of homologous recombination, with IC50 ranging from 5 to 30 μM. RAD51 is a eukaryote gene, encoding RAD51 protein...

celogentin C is the most potent (IC50 0.8×10−6 M), and it is more potent than the anti-mitotic agent vinblastine (IC50 3.0×10−6). Moroidin has the same...

Cynaropicrin has shown variable efficacy on different cancer cell lines. The IC50 lies between 0.068 and 8.7 μg/ml, with outliers of 30.22 and 116.96 μg/ml...

Cheng–Prusoff equation to calculate the absolute inhibition constant Ki (IC50). In the 1980s, while the AIDS epidemic was spreading and found to be caused...

the drug is a lower-potency dopamine reuptake inhibitor (DRI), with an IC50 at the dopamine transporter (DAT) of 660 nM. It has also been found to induce...

7.60) with the best expressing a half-maximal inhibitory concentration (IC50) of 140 nM in the greenhouse at 3 kg/ha (2.7 lb/acre). Thanks to an x-ray...

acts as a potent and selective antagonist for the TRPA1 receptor, with an IC50 of 17nM, vs ~3μM at the related TRPV1 and TRPM channels. It has antiinflammatory...