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Assay Detail

CHEMBL928514

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Functional
Antagonist activity at human CCR2b receptor
94
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

QSAR studies on CCR2 antagonists with chiral sensitive hologram descriptors.
Nair PC, Srikanth K, Sobhia ME.
Bioorg Med Chem Lett (2008) 18 : 1323 -1330
PubMed 18258426 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 94 7.31 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL230281 2 9.37
CHEMBL397996 2 8.74
CHEMBL437359 2 8.72
CHEMBL230933 2 8.51
CHEMBL231246 2 8.46
CHEMBL397997 2 8.46
CHEMBL231039 2 8.41
CHEMBL230722 2 8.40
CHEMBL230721 2 8.12
CHEMBL398000 2 8.10
CHEMBL230617 2 8.05
CHEMBL230832 2 7.89
CHEMBL389773 2 7.88
CHEMBL230507 2 7.88
CHEMBL252412 2 7.85
CHEMBL397750 2 7.84
CHEMBL387587 2 7.80
CHEMBL230405 2 7.72
CHEMBL230616 2 7.70
CHEMBL400517 2 7.60
CHEMBL252611 2 7.55
CHEMBL388675 2 7.55
CHEMBL398150 2 7.52
CHEMBL211775 2 7.41
CHEMBL388949 2 7.38
CHEMBL231247 2 7.17
CHEMBL215654 2 7.01
CHEMBL252815 2 6.90
CHEMBL409162 2 6.76
CHEMBL210606 2 6.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL230281 IC50 = 0.4266 nM 9.37
CHEMBL230281 IC50 = 0.43 nM 9.37
CHEMBL397996 IC50 = 1.8 nM 8.74
CHEMBL397996 IC50 = 1.82 nM 8.74
CHEMBL437359 IC50 = 1.9 nM 8.72
CHEMBL437359 IC50 = 1.905 nM 8.72
CHEMBL230933 IC50 = 3.1 nM 8.51
CHEMBL230933 IC50 = 3.09 nM 8.51
CHEMBL231246 IC50 = 3.467 nM 8.46
CHEMBL397997 IC50 = 3.5 nM 8.46
CHEMBL231246 IC50 = 3.5 nM 8.46
CHEMBL397997 IC50 = 3.467 nM 8.46
CHEMBL231039 IC50 = 3.9 nM 8.41
CHEMBL231039 IC50 = 3.89 nM 8.41
CHEMBL230722 IC50 = 3.981 nM 8.40
CHEMBL230722 IC50 = 4.0 nM 8.40
CHEMBL230721 IC50 = 7.586 nM 8.12
CHEMBL230721 IC50 = 7.6 nM 8.12
CHEMBL398000 IC50 = 8.0 nM 8.10
CHEMBL398000 IC50 = 7.943 nM 8.10
CHEMBL230617 IC50 = 8.913 nM 8.05
CHEMBL230617 IC50 = 9.0 nM 8.05
CHEMBL230832 IC50 = 13.0 nM 7.89
CHEMBL230832 IC50 = 12.88 nM 7.89
CHEMBL389773 IC50 = 13.18 nM 7.88
CHEMBL230507 IC50 = 13.18 nM 7.88
CHEMBL230507 IC50 = 13.3 nM 7.88
CHEMBL389773 IC50 = 13.3 nM 7.88
CHEMBL252412 IC50 = 14.0 nM 7.85
CHEMBL252412 IC50 = 14.13 nM 7.85
CHEMBL397750 IC50 = 14.45 nM 7.84
CHEMBL397750 IC50 = 14.3 nM 7.84
CHEMBL387587 IC50 = 15.85 nM 7.80
CHEMBL387587 IC50 = 16.0 nM 7.80
CHEMBL230405 IC50 = 19.05 nM 7.72
CHEMBL230405 IC50 = 19.0 nM 7.72
CHEMBL230616 IC50 = 19.95 nM 7.70
CHEMBL230616 IC50 = 20.0 nM 7.70
CHEMBL400517 IC50 = 25.0 nM 7.60
CHEMBL400517 IC50 = 25.12 nM 7.60
CHEMBL252611 IC50 = 28.18 nM 7.55
CHEMBL252611 IC50 = 28.0 nM 7.55
CHEMBL388675 IC50 = 28.18 nM 7.55
CHEMBL388675 IC50 = 28.0 nM 7.55
CHEMBL398150 IC50 = 30.2 nM 7.52
CHEMBL398150 IC50 = 30.0 nM 7.52
CHEMBL211775 IC50 = 39.0 nM 7.41
CHEMBL211775 IC50 = 38.9 nM 7.41
CHEMBL388949 IC50 = 41.69 nM 7.38
CHEMBL388949 IC50 = 42.0 nM 7.38