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Assay Detail

CHEMBL889104

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

Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
28
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

3-Amino-1-alkyl-cyclopentane carboxamides as small molecule antagonists of the human and murine CC chemokine receptor 2.
Butora G, Jiao R, Parsons WH, Vicario PP, Jin H, Ayala JM, Cascieri MA, Yang L.
Bioorg Med Chem Lett (2007) 17 : 3636 -3641
PubMed 17482462 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.89 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL437359 1 8.72
CHEMBL230933 1 8.51
CHEMBL230932 1 8.48
CHEMBL231246 1 8.46
CHEMBL231039 1 8.41
CHEMBL230722 1 8.40
CHEMBL231038 1 8.30
CHEMBL436796 1 8.26
CHEMBL231142 4 8.20
CHEMBL266017 1 8.19
CHEMBL230721 1 8.12
CHEMBL398000 1 8.10
CHEMBL389610 1 8.07
CHEMBL230617 1 8.05
CHEMBL388007 1 8.00
CHEMBL230832 1 7.89
CHEMBL230831 1 7.81
CHEMBL387587 1 7.80
CHEMBL230405 1 7.72
CHEMBL230078 1 7.70
CHEMBL230616 1 7.70
CHEMBL231143 1 7.57
CHEMBL388675 1 7.55
CHEMBL231247 1 7.17
CHEMBL398001 1 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL437359 IC50 = 1.9 nM 8.72
CHEMBL230933 IC50 = 3.1 nM 8.51
CHEMBL230932 IC50 = 3.3 nM 8.48
CHEMBL231246 IC50 = 3.5 nM 8.46
CHEMBL231039 IC50 = 3.9 nM 8.41
CHEMBL230722 IC50 = 4.0 nM 8.40
CHEMBL231038 IC50 = 5.0 nM 8.30
CHEMBL436796 IC50 = 5.5 nM 8.26
CHEMBL231142 IC50 = 6.3 nM 8.20
CHEMBL266017 IC50 = 6.5 nM 8.19
CHEMBL230721 IC50 = 7.6 nM 8.12
CHEMBL398000 IC50 = 8.0 nM 8.10
CHEMBL389610 IC50 = 8.5 nM 8.07
CHEMBL230617 IC50 = 9.0 nM 8.05
CHEMBL388007 IC50 = 10.0 nM 8.00
CHEMBL230832 IC50 = 13.0 nM 7.89
CHEMBL230831 IC50 = 15.5 nM 7.81
CHEMBL387587 IC50 = 16.0 nM 7.80
CHEMBL230405 IC50 = 19.0 nM 7.72
CHEMBL230078 IC50 = 20.0 nM 7.70
CHEMBL230616 IC50 = 20.0 nM 7.70
CHEMBL231143 IC50 = 27.0 nM 7.57
CHEMBL388675 IC50 = 28.0 nM 7.55
CHEMBL231142 IC50 = 32.0 nM 7.50
CHEMBL231247 IC50 = 67.0 nM 7.17
CHEMBL231142 IC50 = 135.0 nM 6.87
CHEMBL231142 IC50 = 229.0 nM 6.64
CHEMBL398001 IC50 = 231.0 nM 6.64