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Assay Detail

CHEMBL929486

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

Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCs
20
Total Activities
20
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

Discovery of disubstituted cyclohexanes as a new class of CC chemokine receptor 2 antagonists.
Cherney RJ, Mo R, Meyer DT, Nelson DJ, Lo YC, Yang G, Scherle PA, Mandlekar S, Wasserman ZR, Jezak H, Solomon KA, Tebben AJ, Carter PH, Decicco CP.
J Med Chem (2008) 51 : 721 -724
PubMed 18232650 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.48 8.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273083 1 8.29
CHEMBL271828 1 8.05
CHEMBL270906 1 7.68
CHEMBL270959 1 7.64
CHEMBL411726 1 7.43
CHEMBL272168 1 7.19
CHEMBL429425 1 7.06
CHEMBL271537 1 6.44
CHEMBL271752 1 6.40
CHEMBL270957 1 6.28
CHEMBL269898 1 6.27
CHEMBL411935 1 6.26
CHEMBL273079 1 6.10
CHEMBL408172 1 6.01
CHEMBL409712 1 5.92
CHEMBL406925 1 5.66
CHEMBL272860 1 5.52
CHEMBL272167 1 5.38
CHEMBL272407 1 5.11
CHEMBL407145 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL273083 IC50 = 5.1 nM 8.29
CHEMBL271828 IC50 = 9.0 nM 8.05
CHEMBL270906 IC50 = 21.0 nM 7.68
CHEMBL270959 IC50 = 23.0 nM 7.64
CHEMBL411726 IC50 = 37.0 nM 7.43
CHEMBL272168 IC50 = 64.0 nM 7.19
CHEMBL429425 IC50 = 87.0 nM 7.06
CHEMBL271537 IC50 = 360.0 nM 6.44
CHEMBL271752 IC50 = 400.0 nM 6.40
CHEMBL270957 IC50 = 530.0 nM 6.28
CHEMBL269898 IC50 = 540.0 nM 6.27
CHEMBL411935 IC50 = 550.0 nM 6.26
CHEMBL273079 IC50 = 790.0 nM 6.10
CHEMBL408172 IC50 = 970.0 nM 6.01
CHEMBL409712 IC50 = 1190.0 nM 5.92
CHEMBL406925 IC50 = 2170.0 nM 5.66
CHEMBL272860 IC50 = 3010.0 nM 5.52
CHEMBL272167 IC50 = 4130.0 nM 5.38
CHEMBL272407 IC50 = 7860.0 nM 5.11
CHEMBL407145 IC50 = 12000.0 nM 4.92