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Assay Detail

CHEMBL875065

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

Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

C-C chemokine receptor type 2 (CHEMBL4015)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
Berkhout TA, Blaney FE, Bridges AM, Cooper DG, Forbes IT, Gribble AD, Groot PH, Hardy A, Ife RJ, Kaur R, Moores KE, Shillito H, Willetts J, Witherington J.
J Med Chem (2003) 46 : 4070 -4086
PubMed 12954060 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.18 7.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL432713 1 7.78
CHEMBL41275 1 7.56
CHEMBL134074 1 7.23
CHEMBL131243 1 6.82
CHEMBL337246 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL432713 Ki = 16.6 nM 7.78
CHEMBL41275 Ki = 27.54 nM 7.56
CHEMBL134074 Ki = 58.88 nM 7.23
CHEMBL131243 Ki = 151.36 nM 6.82
CHEMBL337246 Ki = 316.23 nM 6.50