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Assay Detail

CHEMBL3224673

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

Binding
Inhibition of human CYP1B1 expressed in Escherichia coli assessed as changes in ethoxyresorufin O-deethylation activity after 3 mins by spectrofluorometer analysis
14
Total Activities
14
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

trans-Stilbenoids: potent and selective inhibitors for human cytochrome P450 1B1
Chun Y, Lim C, Ohk SO, Lee JM, Lee JH, Choi S, Kim S
Medchemcomm (2011) 2 : 402 -405
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.60 7.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3220148 1 7.11
CHEMBL3220143 1 7.01
CHEMBL3220149 1 6.83
CHEMBL3132926 1 6.72
CHEMBL3220146 1 6.72
CHEMBL3220145 1 6.65
CHEMBL46909 1 6.52
CHEMBL3220147 1 6.52
CHEMBL2043279 1 6.47
CHEMBL3220144 1 6.46
CHEMBL3132932 1 6.46
CHEMBL3220150 1 6.38
CHEMBL3219852 1 6.31
CHEMBL242396 1 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3220148 IC50 = 78.4 nM 7.11
CHEMBL3220143 IC50 = 98.2 nM 7.01
CHEMBL3220149 IC50 = 148.0 nM 6.83
CHEMBL3132926 IC50 = 190.0 nM 6.72
CHEMBL3220146 IC50 = 192.0 nM 6.72
CHEMBL3220145 IC50 = 222.0 nM 6.65
CHEMBL46909 IC50 = 300.0 nM 6.52
CHEMBL3220147 IC50 = 301.0 nM 6.52
CHEMBL2043279 IC50 = 336.0 nM 6.47
CHEMBL3220144 IC50 = 350.0 nM 6.46
CHEMBL3132932 IC50 = 350.0 nM 6.46
CHEMBL3220150 IC50 = 420.0 nM 6.38
CHEMBL3219852 IC50 = 493.0 nM 6.31
CHEMBL242396 IC50 = 666.0 nM 6.18