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Assay Detail

CHEMBL4683864

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

Binding
Potentiation of amphotericin-induced cytotoxicity against human DU-145 cells over expressing CYP1B1 assessed as reversal of CYP1B1 mediated drug resistance at 1 uM after 48 hrs by MTT assay (Rvb = 43.25 +/- 1.7 nM)
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type DU-145
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design and synthesis of α-naphthoflavone chimera derivatives able to eliminate cytochrome P450 (CYP)1B1-mediated drug resistance via targeted CYP1B1 degradation.
Zhou L,Chen W,Cao C,Shi Y,Ye W,Hu J,Wang L,Zhou W
Eur J Med Chem (2020) 189 : 112028 -112028
PubMed 31945665 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.55 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4763775 1 7.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4763775 IC50 = 28.25 nM 7.55