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Assay Detail

CHEMBL4825980

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

Binding
Inhibition of paclitaxel stimulated- P-gp ATPase activity (unknown origin)
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

ATP-dependent translocase ABCB1 (CHEMBL4302)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Encequidar, First-in-Class Intestine Specific P-glycoprotein Inhibitor.
Smolinski MP, Urgaonkar S, Pitzonka L, Cutler M, Lee G, Suh KH, Lau JYN.
J Med Chem (2021) 64 : 3677 -3693
PubMed 33729781 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.97 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4594298 ENCEQUIDAR 3.0 1 9.22
CHEMBL396298 ELACRIDAR 2.0 1 8.31
CHEMBL348475 TARIQUIDAR 3.0 1 7.49
CHEMBL160 CYCLOSPORINE 4.0 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4594298 ENCEQUIDAR IC50 = 0.6 nM 9.22
CHEMBL396298 ELACRIDAR IC50 = 4.9 nM 8.31
CHEMBL348475 TARIQUIDAR IC50 = 32.7 nM 7.49
CHEMBL160 CYCLOSPORINE IC50 = 141.3 nM 6.85