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Assay Detail

CHEMBL3243169

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

Binding
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
5
Total Activities
5
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 5 9.30 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3233186 1 9.70
CHEMBL3233188 1 9.70
CHEMBL1091605 1 9.30
CHEMBL3233184 1 9.22
CHEMBL3233178 1 8.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3233186 IC50 = 0.2 nM 9.70
CHEMBL3233188 IC50 = 0.2 nM 9.70
CHEMBL1091605 IC50 = 0.5 nM 9.30
CHEMBL3233184 IC50 = 0.6 nM 9.22
CHEMBL3233178 IC50 = 2.6 nM 8.59