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Assay Detail

CHEMBL1693612

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

Functional
Antagonist activity at CCR2 in human PBMC cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery, optimization, and pharmacological characterization of novel heteroaroylphenylureas antagonists of C-C chemokine ligand 2 function.
Laborde E, Macsata RW, Meng F, Peterson BT, Robinson L, Schow SR, Simon RJ, Xu H, Baba K, Inagaki H, Ishiwata Y, Jomori T, Matsumoto Y, Miyachi A, Nakamura T, Okamoto M, Handel TM, Bernard CC.
J Med Chem (2011) 54 : 1667 -1681
PubMed 21341682 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.70 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1688889 1 6.70
CHEMBL1688888 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1688889 IC50 = 200.0 nM 6.70
CHEMBL1688888 IC50 - -