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Assay Detail

CHEMBL3423816

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

ADMET
Inhibition of human CYP1A1 assessed as reduction in 7-ethoxyresorufin O-deethylation activity by fluorescence based EROD assay
29
Total Activities
29
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 and Synthesis of New α-Naphthoflavones as Cytochrome P450 (CYP) 1B1 Inhibitors To Overcome Docetaxel-Resistance Associated with CYP1B1 Overexpression.
Cui J, Meng Q, Zhang X, Cui Q, Zhou W, Li S.
J Med Chem (2015) 58 : 3534 -3547
PubMed 25799264 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.64 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3422338 1 8.74
CHEMBL3422257 1 8.32
CHEMBL3422258 1 8.23
CHEMBL3422337 1 8.19
CHEMBL3422335 1 8.01
CHEMBL3422341 1 7.94
CHEMBL3421639 1 7.94
CHEMBL3422350 1 7.93
CHEMBL3422346 1 7.92
CHEMBL283196 ALPHA-NAPHTHOFLAVONE 1 7.92
CHEMBL3422340 1 7.89
CHEMBL3422354 1 7.87
CHEMBL3422339 1 7.73
CHEMBL3422336 1 7.72
CHEMBL3422358 1 7.70
CHEMBL3422342 1 7.65
CHEMBL3422353 1 7.57
CHEMBL3422348 1 7.56
CHEMBL3422347 1 7.50
CHEMBL3422351 1 7.48
CHEMBL3421640 1 7.44
CHEMBL3422355 1 7.41
CHEMBL3422352 1 7.34
CHEMBL3422349 1 7.17
CHEMBL3422343 1 7.17
CHEMBL3422357 1 7.15
CHEMBL3422345 1 6.94
CHEMBL3422356 1 6.72
CHEMBL3422344 1 6.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3422338 IC50 = 1.8 nM 8.74
CHEMBL3422257 IC50 = 4.8 nM 8.32
CHEMBL3422258 IC50 = 5.9 nM 8.23
CHEMBL3422337 IC50 = 6.4 nM 8.19
CHEMBL3422335 IC50 = 9.8 nM 8.01
CHEMBL3422341 IC50 = 11.5 nM 7.94
CHEMBL3421639 IC50 = 11.5 nM 7.94
CHEMBL3422350 IC50 = 11.8 nM 7.93
CHEMBL3422346 IC50 = 12.1 nM 7.92
CHEMBL283196 ALPHA-NAPHTHOFLAVONE IC50 = 11.9 nM 7.92
CHEMBL3422340 IC50 = 12.9 nM 7.89
CHEMBL3422354 IC50 = 13.6 nM 7.87
CHEMBL3422339 IC50 = 18.8 nM 7.73
CHEMBL3422336 IC50 = 19.2 nM 7.72
CHEMBL3422358 IC50 = 20.16 nM 7.70
CHEMBL3422342 IC50 = 22.5 nM 7.65
CHEMBL3422353 IC50 = 26.9 nM 7.57
CHEMBL3422348 IC50 = 27.5 nM 7.56
CHEMBL3422347 IC50 = 31.6 nM 7.50
CHEMBL3422351 IC50 = 32.9 nM 7.48
CHEMBL3421640 IC50 = 36.16 nM 7.44
CHEMBL3422355 IC50 = 39.4 nM 7.41
CHEMBL3422352 IC50 = 46.0 nM 7.34
CHEMBL3422349 IC50 = 66.9 nM 7.17
CHEMBL3422343 IC50 = 67.8 nM 7.17
CHEMBL3422357 IC50 = 70.24 nM 7.15
CHEMBL3422345 IC50 = 113.7 nM 6.94
CHEMBL3422356 IC50 = 192.0 nM 6.72
CHEMBL3422344 IC50 = 535.1 nM 6.27