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

CHEMBL904898

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

Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytes
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Alpha-aminothiazole-gamma-aminobutanoic amides as potent, small molecule CCR2 receptor antagonists.
Zhou C, Guo L, Parsons WH, Mills SG, MacCoss M, Vicario PP, Zweerink H, Cascieri MA, Springer MS, Yang L.
Bioorg Med Chem Lett (2007) 17 : 309 -314
PubMed 17092717 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 8.08 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL230281 1 9.37
CHEMBL389771 1 9.10
CHEMBL229316 1 8.89
CHEMBL397749 1 8.89
CHEMBL397948 1 8.85
CHEMBL388487 1 8.77
CHEMBL397996 1 8.74
CHEMBL230790 1 8.74
CHEMBL437552 1 8.64
CHEMBL387583 1 8.59
CHEMBL438304 1 8.52
CHEMBL230166 1 8.52
CHEMBL388486 1 8.52
CHEMBL230684 1 8.46
CHEMBL397997 1 8.46
CHEMBL230794 1 8.41
CHEMBL397747 1 8.40
CHEMBL389888 1 8.28
CHEMBL388868 1 8.24
CHEMBL388867 1 8.19
CHEMBL396517 1 8.14
CHEMBL395721 1 8.13
CHEMBL230727 1 8.04
CHEMBL231340 1 7.89
CHEMBL231252 1 7.89
CHEMBL389773 1 7.88
CHEMBL230507 1 7.88
CHEMBL231149 1 7.85
CHEMBL438514 1 7.84
CHEMBL397750 1 7.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL230281 IC50 = 0.43 nM 9.37
CHEMBL389771 IC50 = 0.8 nM 9.10
CHEMBL397749 IC50 = 1.3 nM 8.89
CHEMBL229316 IC50 = 1.3 nM 8.89
CHEMBL397948 IC50 = 1.4 nM 8.85
CHEMBL388487 IC50 = 1.7 nM 8.77
CHEMBL397996 IC50 = 1.8 nM 8.74
CHEMBL230790 IC50 = 1.8 nM 8.74
CHEMBL437552 IC50 = 2.3 nM 8.64
CHEMBL387583 IC50 = 2.6 nM 8.59
CHEMBL388486 IC50 = 3.0 nM 8.52
CHEMBL230166 IC50 = 3.0 nM 8.52
CHEMBL438304 IC50 = 3.0 nM 8.52
CHEMBL230684 IC50 = 3.5 nM 8.46
CHEMBL397997 IC50 = 3.5 nM 8.46
CHEMBL230794 IC50 = 3.9 nM 8.41
CHEMBL397747 IC50 = 4.0 nM 8.40
CHEMBL389888 IC50 = 5.2 nM 8.28
CHEMBL388868 IC50 = 5.8 nM 8.24
CHEMBL388867 IC50 = 6.5 nM 8.19
CHEMBL396517 IC50 = 7.3 nM 8.14
CHEMBL395721 IC50 = 7.4 nM 8.13
CHEMBL230727 IC50 = 9.1 nM 8.04
CHEMBL231252 IC50 = 13.0 nM 7.89
CHEMBL231340 IC50 = 13.0 nM 7.89
CHEMBL389773 IC50 = 13.3 nM 7.88
CHEMBL230507 IC50 = 13.3 nM 7.88
CHEMBL231149 IC50 = 14.0 nM 7.85
CHEMBL438514 IC50 = 14.5 nM 7.84
CHEMBL397750 IC50 = 14.3 nM 7.84
CHEMBL230165 IC50 = 16.0 nM 7.80
CHEMBL388869 IC50 = 17.0 nM 7.77
CHEMBL396101 IC50 = 18.0 nM 7.75
CHEMBL438128 IC50 = 19.0 nM 7.72
CHEMBL230624 IC50 = 20.0 nM 7.70
CHEMBL395289 IC50 = 23.0 nM 7.64
CHEMBL229536 IC50 = 28.6 nM 7.54
CHEMBL398150 IC50 = 30.0 nM 7.52
CHEMBL230791 IC50 = 32.7 nM 7.49
CHEMBL230824 IC50 = 36.0 nM 7.44
CHEMBL397717 IC50 = 36.0 nM 7.44
CHEMBL388949 IC50 = 42.0 nM 7.38
CHEMBL231150 IC50 = 74.0 nM 7.13
CHEMBL427110 IC50 = 182.7 nM 6.74
CHEMBL230828 IC50 = 229.0 nM 6.64