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Assay Detail

CHEMBL4826013

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

Binding
Inhibition of P-gp in MDCK-MDR1 cells assessed as reduction in basal to apical transport of paclitaxel measured after 120 mins by LC-MS/MS analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Canis lupus familiaris
Cell Type MDCK-MDR1
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 1 7.46 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4594298 ENCEQUIDAR 3.0 1 7.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4594298 ENCEQUIDAR IC50 = 35.0 nM 7.46