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Assay Detail

CHEMBL4009463

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

Binding
Inhibition of human CYP1B1 expressed in HEK293 cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring cisplatin EC50 at 0.018 uM by MTT assay (Rvb = 61 +/- 8 uM)
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 1B1 (CHEMBL4878)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and characterization of novel CYP1B1 inhibitors based on heterocyclic chalcones: Overcoming cisplatin resistance in CYP1B1-overexpressing lines.
Horley NJ, Beresford KJ, Chawla T, McCann GJ, Ruparelia KC, Gatchie L, Sonawane VR, Williams IS, Tan HL, Joshi P, Bharate SS, Kumar V, Bharate SB, Chaudhuri B.
Eur J Med Chem (2017) 129 : 159 -174
PubMed 28222316 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 5.08 5.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4092737 1 5.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4092737 EC50 = 8300.0 nM 5.08