Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3603197

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

Binding
Inhibition of human microsomal CYP1B1-dependent ethoxyresorufin-O-deethylase activity by spectrofluorimetric analysis in presence of NADPH regenerating solution
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cytochrome P450 1B1 (CHEMBL4878)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A Ligand-Based Drug Design. Discovery of 4-Trifluoromethyl-7,8-pyranocoumarin as a Selective Inhibitor of Human Cytochrome P450 1A2.
Liu J, Pham PT, Skripnikova EV, Zheng S, Lovings LJ, Wang Y, Goyal N, Bellow SM, Mensah LM, Chatters AJ, Bratton MR, Wiese TE, Zhao M, Wang G, Foroozesh M.
J Med Chem (2015) 58 : 6481 -6493
PubMed 26222195 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 5.78 8.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2347912 1 8.25
CHEMBL283196 ALPHA-NAPHTHOFLAVONE 1 7.80
CHEMBL2347756 1 7.28
CHEMBL3601434 1 7.00
CHEMBL3601435 1 6.92
CHEMBL3601433 1 6.75
CHEMBL3601436 1 6.32
CHEMBL3601441 1 5.33
CHEMBL3601437 1 5.30
CHEMBL50703 1 5.13
CHEMBL3601439 1 4.92
CHEMBL3601440 1 4.69
CHEMBL3601438 1 4.67
CHEMBL3601508 1 4.65
CHEMBL3601511 1 4.52
CHEMBL3601509 1 4.33
CHEMBL3601510 1 4.33
CHEMBL405845 FURAFYLLINE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2347912 Ki = 5.6 nM 8.25
CHEMBL283196 ALPHA-NAPHTHOFLAVONE Ki = 16.0 nM 7.80
CHEMBL2347756 Ki = 53.0 nM 7.28
CHEMBL3601434 Ki = 100.0 nM 7.00
CHEMBL3601435 Ki = 120.0 nM 6.92
CHEMBL3601433 Ki = 180.0 nM 6.75
CHEMBL3601436 Ki = 480.0 nM 6.32
CHEMBL3601441 Ki = 4620.0 nM 5.33
CHEMBL3601437 Ki = 5040.0 nM 5.30
CHEMBL50703 Ki = 7460.0 nM 5.13
CHEMBL3601439 Ki = 12000.0 nM 4.92
CHEMBL3601440 Ki = 20400.0 nM 4.69
CHEMBL3601438 Ki = 21200.0 nM 4.67
CHEMBL3601508 Ki = 22600.0 nM 4.65
CHEMBL3601511 Ki = 30100.0 nM 4.52
CHEMBL3601509 Ki = 46800.0 nM 4.33
CHEMBL3601510 Ki = 46600.0 nM 4.33
CHEMBL405845 FURAFYLLINE Ki > 200000.0 nM -