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Assay Detail

CHEMBL972103

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

ADMET
Binding affinity to CYP2C9
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Modeling and synthesis of novel tight-binding inhibitors of cytochrome P450 2C9.
Peng CC, Rushmore T, Crouch GJ, Jones JP.
Bioorg Med Chem (2008) 16 : 4064 -4074
PubMed 18255300 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 6.46 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL456432 1 8.38
CHEMBL388590 BENZBROMARONE 4.0 1 7.72
CHEMBL458566 1 7.64
CHEMBL458567 1 7.39
CHEMBL457087 1 7.35
CHEMBL250251 1 7.00
CHEMBL465715 1 6.18
CHEMBL465664 1 5.85
CHEMBL459249 1 5.51
CHEMBL464669 1 5.31
CHEMBL465716 1 5.23
CHEMBL465908 1 5.19
CHEMBL445600 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL456432 Ki = 4.2 nM 8.38
CHEMBL388590 BENZBROMARONE Ki = 19.0 nM 7.72
CHEMBL458566 Ki = 23.0 nM 7.64
CHEMBL458567 Ki = 41.0 nM 7.39
CHEMBL457087 Ki = 44.34 nM 7.35
CHEMBL250251 Ki = 101.0 nM 7.00
CHEMBL465715 Ki = 656.0 nM 6.18
CHEMBL465664 Ki = 1420.0 nM 5.85
CHEMBL459249 Ki = 3120.0 nM 5.51
CHEMBL464669 Ki = 4870.0 nM 5.31
CHEMBL465716 Ki = 5930.0 nM 5.23
CHEMBL465908 Ki = 6480.0 nM 5.19
CHEMBL445600 Ki = 6740.0 nM 5.17