Graphical representation of the IC50 determination of the inhibition of an enzyme's activity by a small molecule ("drug"). Four different concentrations of the small molecule (ranging from 30 to 300 μM) were tested.
Half maximal inhibitory concentration (IC50) is a measure of the potency of a substance in inhibiting a specific biological or biochemical function. IC50 is a quantitative measure that indicates how much of a particular inhibitory substance (e.g. drug) is needed to inhibit, in vitro, a given biological process or biological component by 50%.[1] The biological component could be an enzyme, cell, cell receptor or microorganism. IC50 values are typically expressed as molar concentration.
IC50 is commonly used as a measure of antagonist drug potency in pharmacological research. IC50 is comparable to other measures of potency, such as EC50 for excitatory drugs. EC50 represents the dose or plasma concentration required for obtaining 50% of a maximum effect in vivo.[1]
IC50 can be determined with functional assays or with competition binding assays.
Sometimes, IC50 values are converted to the pIC50 scale.
Due to the minus sign, higher values of pIC50 indicate exponentially more potent inhibitors. pIC50 is usually given in terms of molar concentration (mol/L, or M), thus requiring IC50 in units of M.[2]
The IC50 terminology is also used for some behavioral measures in vivo, such as the two bottle fluid consumption test. When animals decrease consumption from the drug-laced water bottle, the concentration of the drug that results in a 50% decrease in consumption is considered the IC50 for fluid consumption of that drug.[3]
^ abHoetelmans RM. "IC50 versus EC50". PK-PD relationships for anti-retroviral drugs. Amsterdam: Slotervaart Hospital. Archived from the original on 2017-05-28 – via U.S. Food and Drug Administration.
^Stewart MJ, Watson ID (July 1983). "Standard units for expressing drug concentrations in biological fluids". British Journal of Clinical Pharmacology. 16 (1): 3–7. doi:10.1111/j.1365-2125.1983.tb02136.x. PMC 1427960. PMID 6882621.
^Robinson SF, Marks MJ, Collins AC (April 1996). "Inbred mouse strains vary in oral self-selection of nicotine". Psychopharmacology. 124 (4): 332–9. doi:10.1007/bf02247438. PMID 8739548. S2CID 19172675.
inhibitory concentration (IC50) is a measure of the potency of a substance in inhibiting a specific biological or biochemical function. IC50 is a quantitative...
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...
Tesofensine has IC50 of 8.0, 3.2 and 11.0nM at the DAT, NAT and 5HTT. More recently, though, the following data was submitted: IC50 (nM) NE 1.7, SER...
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...
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...
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...
(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...
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...
bupropion 1 23.8 0.6 11.2 2.5 Half-life 11 h 19 h 15 h 31 h 22 h Inhibition IC50 (μM) in human cells, unless noted otherwise (Lesser values indicate greater...
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...
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...
It antagonises these receptors with the following IC50 values: 5-HT3, IC50 = 18 μM σ receptors, IC50 = 145 μM The pharmacokinetics of lamotrigine follow...
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...
neurotransmitter release at glutamatergic synapses in hippocampus and cortex with IC50 of 980 μM, a brain concentration seen in classical phenylketonuria, whereas...
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)...
androgen receptor with a very high affinity with an IC50 of 0.28 nM. Reference drug bicalutamide had an IC50 of 3.1 nM. Saceda-Corralo D, Domínguez-Santas M...
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)...
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...
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...
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...
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...
drug binds to the site. Values at the mAChRsTooltip muscarinic acetylcholine receptors and hERGTooltip Human Ether-à-go-go-Related Gene are IC50 (nM)....
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...
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