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Assay Detail

CHEMBL695434

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Functional
Concentration that reduces the difference in reversal of DOX accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%.
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Breast cancer cell line
Confidence 1 — Organism
Curated By Intermediate

Target

Breast cancer cell line (CHEMBL614788)
Type CELL-LINE
Organism Homo sapiens

Publication

C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump.
Leonessa F, Kim JH, Ghiorghis A, Kulawiec RJ, Hammer C, Talebian A, Clarke R.
J Med Chem (2002) 45 : 390 -398
PubMed 11784143 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 5.89 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL160 CYCLOSPORINE 4.0 1 6.30
CHEMBL131172 1 6.22
CHEMBL419965 1 6.22
CHEMBL338904 1 6.16
CHEMBL6966 VERAPAMIL 4.0 1 5.62
CHEMBL129251 1 4.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL160 CYCLOSPORINE EC50 = 500.0 nM 6.30
CHEMBL131172 EC50 = 600.0 nM 6.22
CHEMBL419965 EC50 = 600.0 nM 6.22
CHEMBL338904 EC50 = 700.0 nM 6.16
CHEMBL6966 VERAPAMIL EC50 = 2400.0 nM 5.62
CHEMBL129251 EC50 = 14700.0 nM 4.83