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Assay Detail

CHEMBL3243550

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

Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Alkylsulfone-containing trisubstituted cyclohexanes as potent and bioavailable chemokine receptor 2 (CCR2) antagonists.
Cherney RJ, Mo R, Yang MG, Xiao Z, Zhao Q, Mandlekar S, Cvijic ME, Charo IF, Barrish JC, Decicco CP, Carter PH.
Bioorg Med Chem Lett (2014) 24 : 1843 -1845
PubMed 24613378 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 8.90 9.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3233186 1 9.47
CHEMBL3233187 1 9.30
CHEMBL3233181 1 9.15
CHEMBL3233188 1 9.02
CHEMBL1091605 1 9.00
CHEMBL3233185 1 8.96
CHEMBL3233180 1 8.92
CHEMBL3233184 1 8.92
CHEMBL3233189 1 8.92
CHEMBL3233190 1 8.89
CHEMBL3233178 1 8.74
CHEMBL3233179 1 8.66
CHEMBL3233183 1 8.30
CHEMBL3233182 1 8.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3233186 IC50 = 0.34 nM 9.47
CHEMBL3233187 IC50 = 0.5 nM 9.30
CHEMBL3233181 IC50 = 0.7 nM 9.15
CHEMBL3233188 IC50 = 0.96 nM 9.02
CHEMBL1091605 IC50 = 1.0 nM 9.00
CHEMBL3233185 IC50 = 1.1 nM 8.96
CHEMBL3233180 IC50 = 1.2 nM 8.92
CHEMBL3233184 IC50 = 1.2 nM 8.92
CHEMBL3233189 IC50 = 1.2 nM 8.92
CHEMBL3233190 IC50 = 1.3 nM 8.89
CHEMBL3233178 IC50 = 1.8 nM 8.74
CHEMBL3233179 IC50 = 2.2 nM 8.66
CHEMBL3233183 IC50 = 5.0 nM 8.30
CHEMBL3233182 IC50 = 5.2 nM 8.28