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Assay Detail

CHEMBL834068

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Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type THP-1
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Small molecule antagonists of the CCR2b receptor. Part 2: Discovery process and initial structure-activity relationships of diamine derivatives.
Moree WJ, Kataoka K, Ramirez-Weinhouse MM, Shiota T, Imai M, Sudo M, Tsutsumi T, Endo N, Muroga Y, Hada T, Tanaka H, Morita T, Greene J, Barnum D, Saunders J, Kato Y, Myers PL, Tarby CM.
Bioorg Med Chem Lett (2004) 14 : 5413 -5416
PubMed 15454236 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.67 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL255408 1 7.70
CHEMBL435499 1 7.40
CHEMBL2096789 1 6.44
CHEMBL181432 1 6.21
CHEMBL2448120 1 6.20
CHEMBL2096788 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL255408 EC50 = 20.0 nM 7.70
CHEMBL435499 EC50 = 40.0 nM 7.40
CHEMBL2096789 EC50 = 360.0 nM 6.44
CHEMBL181432 EC50 = 610.0 nM 6.21
CHEMBL2448120 EC50 = 630.0 nM 6.20
CHEMBL2096788 EC50 = 810.0 nM 6.09