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Assay Detail

CHEMBL2061657

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

ADMET
Inhibition of CYP2C9
9
Total Activities
9
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 2C9 (CHEMBL3397)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel 1,2,4-thiadiazole derivatives as potent, orally active agonists of sphingosine 1-phosphate receptor subtype 1 (S1P(1)).
Ren F, Deng G, Wang H, Luan L, Meng Q, Xu Q, Xu H, Xu X, Zhang H, Zhao B, Li C, Guo TB, Yang J, Zhang W, Zhao Y, Jia Q, Lu H, Xiang JN, Elliott JD, Lin X.
J Med Chem (2012) 55 : 4286 -4296
PubMed 22500954 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.40 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2059521 1 5.80
CHEMBL2059520 1 5.40
CHEMBL2059527 1 5.40
CHEMBL2059517 1 5.30
CHEMBL2059519 1 5.10
CHEMBL2059515 1 -
CHEMBL2059516 1 -
CHEMBL2057282 1 -
CHEMBL2057285 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2059521 IC50 = 1584.89 nM 5.80
CHEMBL2059520 IC50 = 3981.07 nM 5.40
CHEMBL2059527 IC50 = 3981.07 nM 5.40
CHEMBL2059517 IC50 = 5011.87 nM 5.30
CHEMBL2059519 IC50 = 7943.28 nM 5.10
CHEMBL2059515 IC50 > 10000.0 nM -
CHEMBL2059516 IC50 > 10000.0 nM -
CHEMBL2057282 IC50 > 10000.0 nM -
CHEMBL2057285 IC50 > 10000.0 nM -