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Assay Detail

CHEMBL971595

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

ADMET
Inhibition of human recombinant CYP2C9 expressed in baculovirus-infected insect microsomes
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel aldosterone synthase inhibitors with extended carbocyclic skeleton by a combined ligand-based and structure-based drug design approach.
Lucas S, Heim R, Negri M, Antes I, Ries C, Schewe KE, Bisi A, Gobbi S, Hartmann RW.
J Med Chem (2008) 51 : 6138 -6149
PubMed 18763754 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.85 7.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL494713 1 7.19
CHEMBL1109 SULFAPHENAZOLE 4.0 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL494713 IC50 = 64.0 nM 7.19
CHEMBL1109 SULFAPHENAZOLE IC50 = 318.0 nM 6.50