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Assay Detail

CHEMBL4370357

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

ADMET
Inhibition of CYP2C9 in human liver microsomes
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cytochrome P450 2C9 (CHEMBL3397)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tricyclic Indazoles-A Novel Class of Selective Estrogen Receptor Degrader Antagonists.
Scott JS, Bailey A, Buttar D, Carbajo RJ, Curwen J, Davey PRJ, Davies RDM, Degorce SL, Donald C, Gangl E, Greenwood R, Groombridge SD, Johnson T, Lamont S, Lawson M, Lister A, Morrow CJ, Moss TA, Pink JH, Polanski R.
J Med Chem (2019) 62 : 1593 -1608
PubMed 30640465 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.39 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4448852 1 5.60
CHEMBL4436187 1 5.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4448852 IC50 = 2500.0 nM 5.60
CHEMBL4436187 IC50 = 6600.0 nM 5.18