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Assay Detail

CHEMBL664422

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ADMET
Inhibition of ethoxyresorufin O-deethylation (EROD) in bicistronic bacterial membranes epressing human cytochrome P450 1A1
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cytochrome P450 1A1 (CHEMBL2231)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and discovery of novel trans-stilbene analogues as potent and selective human cytochrome P450 1B1 inhibitors.
Kim S, Ko H, Park JE, Jung S, Lee SK, Chun YJ.
J Med Chem (2002) 45 : 160 -164
PubMed 11754588 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.07 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42428 1 7.21
CHEMBL43741 1 6.85
CHEMBL46909 1 6.52
CHEMBL43740 1 6.21
CHEMBL44509 (E)-3,4,3',5'-TETRAMETHOXYSTILBENE 1 6.12
CHEMBL296411 TRISMETHOXYRESVERATROL 1 6.08
CHEMBL441035 1 6.04
CHEMBL43395 1 6.01
CHEMBL43013 1 5.96
CHEMBL42427 1 5.82
CHEMBL43396 1 5.18
CHEMBL43065 OXYRESVERATROL 1 4.82
CHEMBL44156 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42428 IC50 = 61.0 nM 7.21
CHEMBL43741 IC50 = 140.0 nM 6.85
CHEMBL46909 IC50 = 300.0 nM 6.52
CHEMBL43740 IC50 = 610.0 nM 6.21
CHEMBL44509 (E)-3,4,3',5'-TETRAMETHOXYSTILBENE IC50 = 750.0 nM 6.12
CHEMBL296411 TRISMETHOXYRESVERATROL IC50 = 830.0 nM 6.08
CHEMBL441035 IC50 = 920.0 nM 6.04
CHEMBL43395 IC50 = 980.0 nM 6.01
CHEMBL43013 IC50 = 1100.0 nM 5.96
CHEMBL42427 IC50 = 1500.0 nM 5.82
CHEMBL43396 IC50 = 6600.0 nM 5.18
CHEMBL43065 OXYRESVERATROL IC50 = 15000.0 nM 4.82
CHEMBL44156 IC50 = 300000.0 nM -