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Assay Detail

CHEMBL4181979

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

Binding
Inhibition of recombinant human CYP1B1 expressed in HEK293 cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring cisplatin EC50 by MTT assay (Rvb = 65.01 +/- 7.01 uM)
4
Total Activities
4
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 1B1 (CHEMBL4878)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

(E)-3-(3,4,5-Trimethoxyphenyl)-1-(pyridin-4-yl)prop-2-en-1-one, a heterocyclic chalcone is a potent and selective CYP1A1 inhibitor and cancer chemopreventive agent.
Horley NJ, Beresford KJM, Kaduskar S, Joshi P, McCann GJP, Ruparelia KC, Williams IS, Gatchie L, Sonawane VR, Bharate SB, Chaudhuri B.
Bioorg Med Chem Lett (2017) 27 : 5409 -5414
PubMed 29138024 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.00 5.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2237710 1 5.00
CHEMBL4214111 1 5.00
CHEMBL4209004 1 5.00
CHEMBL4212722 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2237710 EC50 = 10000.0 nM 5.00
CHEMBL4214111 EC50 = 10000.0 nM 5.00
CHEMBL4209004 EC50 = 10000.0 nM 5.00
CHEMBL4212722 EC50 = 10000.0 nM 5.00