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Assay Detail

CHEMBL4257981

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

Binding
Inhibition of human recombinant CYP1A1 expressed in adherent HEK293 cells assessed as protection of cells against CYP1A1-mediated sensitivity to to B[a]P-induced cytotoxicity by measuring B[a]P- EC50 by MTT assay (Rvb = 0.8 +/- 0.1 uM)
3
Total Activities
3
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 1A1 (CHEMBL2231)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of karanjin isolated from the Indian beech tree as a potent CYP1 enzyme inhibitor with cellular efficacy <i>via</i> screening of a natural product repository.
Joshi P, Sonawane VR, Williams IS, McCann GJP, Gatchie L, Sharma R, Satti N, Chaudhuri B, Bharate SB.
Medchemcomm (2018) 9 : 371 -382
PubMed 30108931 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 5.16 5.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL283196 ALPHA-NAPHTHOFLAVONE 1 5.75
CHEMBL4282750 1 4.87
CHEMBL140796 ISOPIMPINELLIN 1 4.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL283196 ALPHA-NAPHTHOFLAVONE EC50 = 1800.0 nM 5.75
CHEMBL4282750 EC50 = 13500.0 nM 4.87
CHEMBL140796 ISOPIMPINELLIN EC50 = 13800.0 nM 4.86