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Assay Detail

CHEMBL5522601

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

ADMET
Inhibition of human recombinant CYP1A1 using 7-ethoxyresorufin as substrate preincubated with enzyme for 5 mins followed by fluorescent substrate and NADPH addition and measured after 15 mins by EROD assay
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 Autocuration

Target

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

Publication

Design of Novel 2-Phenylquinazolin-4-amines as Selective CYP1B1 Inhibitors for Overcoming Paclitaxel Resistance in A549 Cells.
Yang M, Yang F, Huang X, Cai J, Zhang Y, Jia J, Qiu D.
J Med Chem (2024) 67 : 5883 -5901
PubMed 38509663 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.45 8.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5566974 1 8.79
CHEMBL5557701 1 8.24
CHEMBL5560596 1 7.91
CHEMBL5560837 1 7.58
CHEMBL5565554 1 7.56
CHEMBL5563177 1 7.55
CHEMBL5561280 1 7.48
CHEMBL5561334 1 7.43
CHEMBL5568160 1 7.07
CHEMBL283196 ALPHA-NAPHTHOFLAVONE 1 7.06
CHEMBL5555246 1 6.99
CHEMBL5560888 1 6.61
CHEMBL5560939 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5566974 IC50 = 1.63 nM 8.79
CHEMBL5557701 IC50 = 5.74 nM 8.24
CHEMBL5560596 IC50 = 12.35 nM 7.91
CHEMBL5560837 IC50 = 26.48 nM 7.58
CHEMBL5565554 IC50 = 27.41 nM 7.56
CHEMBL5563177 IC50 = 28.13 nM 7.55
CHEMBL5561280 IC50 = 33.16 nM 7.48
CHEMBL5561334 IC50 = 36.69 nM 7.43
CHEMBL5568160 IC50 = 85.83 nM 7.07
CHEMBL283196 ALPHA-NAPHTHOFLAVONE IC50 = 86.67 nM 7.06
CHEMBL5555246 IC50 = 103.58 nM 6.99
CHEMBL5560888 IC50 = 247.8 nM 6.61
CHEMBL5560939 IC50 = 262.8 nM 6.58