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Assay Detail

CHEMBL5377830

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

ADMET
Inhibition of recombinant CYP1A2 (unknown origin) using 7-ethoxyresorufin as substrate preincubated for 5 mins followed by NADPH addition incubated for 50 mins by EROD assay
10
Total Activities
10
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 1A2 (CHEMBL3356)
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 10 6.34 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL283196 ALPHA-NAPHTHOFLAVONE 1 8.12
CHEMBL5435493 1 6.29
CHEMBL5418796 1 6.28
CHEMBL5396845 1 5.83
CHEMBL5426998 1 5.80
CHEMBL5426732 1 5.73
CHEMBL5422312 1 -
CHEMBL5421843 1 -
CHEMBL5429019 1 -
CHEMBL5405256 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL283196 ALPHA-NAPHTHOFLAVONE IC50 = 7.67 nM 8.12
CHEMBL5435493 IC50 = 513.9 nM 6.29
CHEMBL5418796 IC50 = 524.57 nM 6.28
CHEMBL5396845 IC50 = 1463.33 nM 5.83
CHEMBL5426998 IC50 = 1598.33 nM 5.80
CHEMBL5426732 IC50 = 1844.33 nM 5.73
CHEMBL5422312 IC50 > 2000.0 nM -
CHEMBL5421843 IC50 > 2000.0 nM -
CHEMBL5429019 IC50 > 2000.0 nM -
CHEMBL5405256 IC50 > 2000.0 nM -