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Assay Detail

CHEMBL5377828

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

ADMET
Inhibition of recombinant CYP1B1 (unknown origin) using 7-ethoxyresorufin as substrate preincubated for 5 mins followed by NADPH addition incubated for 35 mins by EROD assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and Synthesis of Novel Near-Infrared Fluorescence Probes Based on an Open Conformation of a Cytochrome P450 1B1 Complex for Molecular Imaging of Colorectal Tumors.
Chen D, Li R, Shao Q, Wu Z, Cui J, Meng Q, Li S.
J Med Chem (2023) 66 : 16032 -16050
PubMed 38031326 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 8.02 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5422312 1 9.17
CHEMBL5405256 1 8.84
CHEMBL5400922 1 8.69
CHEMBL5412492 1 8.61
CHEMBL5421843 1 8.47
CHEMBL5429019 1 8.35
CHEMBL283196 ALPHA-NAPHTHOFLAVONE 1 8.30
CHEMBL5426998 1 7.95
CHEMBL5435493 1 7.75
CHEMBL5418796 1 7.59
CHEMBL5396845 1 7.54
CHEMBL5426732 1 7.09
CHEMBL5404201 1 7.02
CHEMBL5411203 1 6.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5422312 IC50 = 0.67 nM 9.17
CHEMBL5405256 IC50 = 1.44 nM 8.84
CHEMBL5400922 IC50 = 2.03 nM 8.69
CHEMBL5412492 IC50 = 2.47 nM 8.61
CHEMBL5421843 IC50 = 3.37 nM 8.47
CHEMBL5429019 IC50 = 4.43 nM 8.35
CHEMBL283196 ALPHA-NAPHTHOFLAVONE IC50 = 4.97 nM 8.30
CHEMBL5426998 IC50 = 11.31 nM 7.95
CHEMBL5435493 IC50 = 17.93 nM 7.75
CHEMBL5418796 IC50 = 25.88 nM 7.59
CHEMBL5396845 IC50 = 28.73 nM 7.54
CHEMBL5426732 IC50 = 81.67 nM 7.09
CHEMBL5404201 IC50 = 95.05 nM 7.02
CHEMBL5411203 IC50 = 112.63 nM 6.95