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Assay Detail

CHEMBL2039549

Review assay metadata, readout intent, target linkage, and publication context from the same page.

ADMET
Inhibition of human recombinant CYP2C8 incubated for 15 mins prior to substrate addition measured after 30 mins by spectrophotometry
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 2C8 (CHEMBL3721)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Novel Series of CRTH2 (DP2) Receptor Antagonists Devoid of Carboxylic Acids.
Crosignani S, Jorand-Lebrun C, Campbell G, Prêtre A, Grippi-Vallotton T, Quattropani A, Bouscary-Desforges G, Bombrun A, Missotten M, Humbert Y, Frémaux C, Pâquet M, El Harkani K, Bradshaw CG, Cleva C, Abla N, Daff H, Schott O, Pittet PA, Arrighi JF, Gaudet M, Johnson Z.
ACS Med Chem Lett (2011) 2 : 938 -942
PubMed 24900284 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.79 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2036213 1 7.37
CHEMBL2036225 1 7.30
CHEMBL2036220 1 7.27
CHEMBL2036222 1 7.10
CHEMBL2036210 1 7.07
CHEMBL2036223 1 6.66
CHEMBL2036017 1 6.50
CHEMBL2036030 1 6.33
CHEMBL2036203 1 6.24
CHEMBL2036217 1 6.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2036213 IC50 = 43.0 nM 7.37
CHEMBL2036225 IC50 = 50.0 nM 7.30
CHEMBL2036220 IC50 = 54.0 nM 7.27
CHEMBL2036222 IC50 = 79.0 nM 7.10
CHEMBL2036210 IC50 = 86.0 nM 7.07
CHEMBL2036223 IC50 = 220.0 nM 6.66
CHEMBL2036017 IC50 = 320.0 nM 6.50
CHEMBL2036030 IC50 = 470.0 nM 6.33
CHEMBL2036203 IC50 = 570.0 nM 6.24
CHEMBL2036217 IC50 = 970.0 nM 6.01