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Assay Detail

CHEMBL1035255

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

Binding
Inhibition of MRP1-mediated transport of [3H]LTC4 expressed in human HeLa T5 cells by liquid scintillation counting
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HeLa
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Multidrug resistance-associated protein 1 (CHEMBL3004)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Aromatic 2-(thio)ureidocarboxylic acids as a new family of modulators of multidrug resistance-associated protein 1: synthesis, biological evaluation, and structure-activity relationships.
Häcker HG, Leyers S, Wiendlocha J, Gütschow M, Wiese M.
J Med Chem (2009) 52 : 4586 -4595
PubMed 19580319 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.93 6.10
Ki 1 6.22 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL15177 MK-571 1 6.22
CHEMBL116734 1 6.10
CHEMBL172119 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL15177 MK-571 Ki = 600.0 nM 6.22
CHEMBL116734 IC50 = 800.0 nM 6.10
CHEMBL172119 IC50 = 1800.0 nM 5.75