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Assay Detail

CHEMBL1104429

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

Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albumin
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

gamma-Lactams as glycinamide replacements in cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists.
Cherney RJ, Mo R, Meyer DT, Voss ME, Yang MG, Santella JB, Duncia JV, Lo YC, Yang G, Miller PB, Scherle PA, Zhao Q, Mandlekar S, Cvijic ME, Barrish JC, Decicco CP, Carter PH.
Bioorg Med Chem Lett (2010) 20 : 2425 -2430
PubMed 20346664 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 9.10 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1091605 1 9.30
CHEMBL1091604 1 8.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1091605 IC50 = 0.5 nM 9.30
CHEMBL1091604 IC50 = 1.3 nM 8.89