Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4339737

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

Binding
Inhibition of CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 10 mins by calcein-AM dye based fluorescence assay
1
Total Activities
1
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

Use of a Conformational-Switching Mechanism to Modulate Exposed Polarity: Discovery of CCR2 Antagonist BMS-741672.
Yang MG, Xiao Z, Cherney RJ, Tebben AJ, Batt DG, Brown GD, Chen J, Cvijic ME, Dabros M, Duncia JV, Galella M, Gardner DS, Khandelwal P, Ko SS, Malley MF, Mo R, Pang J, Rose AV, Santella JB, Shi H, Srivastava A, Traeger SC, Wang B, Xu S, Zhao R, Barrish JC, Mandlekar S, Zhao Q, Carter PH.
ACS Med Chem Lett (2019) 10 : 300 -305
PubMed 30891130 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 9.17 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4442783 1 9.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4442783 IC50 = 0.67 nM 9.17