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Assay Detail

CHEMBL1767592

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

Binding
Inhibition of human Pgp overexpressed in human MDCK2-MDR1 cells assessed as inhibition of R123 efflux after 60 mins
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MDCK-II
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Radiosynthesis and in vivo evaluation of 1-[18F]fluoroelacridar as a positron emission tomography tracer for P-glycoprotein and breast cancer resistance protein.
Dörner B, Kuntner C, Bankstahl JP, Wanek T, Bankstahl M, Stanek J, Müllauer J, Bauer F, Mairinger S, Löscher W, Miller DW, Chiba P, Müller M, Erker T, Langer O.
Bioorg Med Chem (2011) 19 : 2190 -2198
PubMed 21419632 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.91 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL396298 ELACRIDAR 2.0 1 6.40
CHEMBL1765143 1 6.22
CHEMBL1765142 1 5.85
CHEMBL1765141 1 5.80
CHEMBL1765140 1 5.77
CHEMBL1765139 1 5.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL396298 ELACRIDAR IC50 = 400.0 nM 6.40
CHEMBL1765143 IC50 = 600.0 nM 6.22
CHEMBL1765142 IC50 = 1400.0 nM 5.85
CHEMBL1765141 IC50 = 1600.0 nM 5.80
CHEMBL1765140 IC50 = 1700.0 nM 5.77
CHEMBL1765139 IC50 = 3800.0 nM 5.42