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Assay Detail

CHEMBL905928

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Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Alpha-aminothiazole-gamma-aminobutanoic amides as potent, small molecule CCR2 receptor antagonists.
Zhou C, Guo L, Parsons WH, Mills SG, MacCoss M, Vicario PP, Zweerink H, Cascieri MA, Springer MS, Yang L.
Bioorg Med Chem Lett (2007) 17 : 309 -314
PubMed 17092717 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.45 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL438304 1 9.22
CHEMBL388487 1 9.15
CHEMBL397996 1 9.15
CHEMBL230281 1 8.74
CHEMBL397948 1 8.28
CHEMBL388867 1 7.57
CHEMBL398150 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL438304 IC50 = 0.6 nM 9.22
CHEMBL388487 IC50 = 0.7 nM 9.15
CHEMBL397996 IC50 = 0.7 nM 9.15
CHEMBL230281 IC50 = 1.8 nM 8.74
CHEMBL397948 IC50 = 5.3 nM 8.28
CHEMBL388867 IC50 = 27.0 nM 7.57
CHEMBL398150 IC50 = 87.0 nM 7.06