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Assay Detail

CHEMBL960972

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

Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
38
Total Activities
29
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 Autocuration

Target

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

Publication

Design, synthesis, and structure-activity relationship of novel CCR2 antagonists.
Kothandaraman S, Donnely KL, Butora G, Jiao R, Pasternak A, Morriello GJ, Goble SD, Zhou C, Mills SG, Maccoss M, Vicario PP, Ayala JM, Demartino JA, Struthers M, Cascieri MA, Yang L.
Bioorg Med Chem Lett (2009) 19 : 1830 -1834
PubMed 19237282 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 7.41 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL494191 4 8.92
CHEMBL522688 4 8.52
CHEMBL495368 1 8.34
CHEMBL492569 1 8.26
CHEMBL492564 3 8.22
CHEMBL495151 1 8.15
CHEMBL494540 1 8.11
CHEMBL494580 2 8.07
CHEMBL521697 1 7.66
CHEMBL495149 1 7.55
CHEMBL41275 1 7.55
CHEMBL523054 1 7.52
CHEMBL495165 1 7.44
CHEMBL494542 1 7.29
CHEMBL494770 1 7.25
CHEMBL493780 1 7.19
CHEMBL494019 1 7.11
CHEMBL494591 1 7.07
CHEMBL494541 1 6.91
CHEMBL523857 1 6.81
CHEMBL494399 1 6.76
CHEMBL523696 1 6.73
CHEMBL493575 1 6.71
CHEMBL492376 1 6.64
CHEMBL523861 1 6.62
CHEMBL493779 1 6.44
CHEMBL524030 1 6.38
CHEMBL493843 1 6.20
CHEMBL523503 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL494191 IC50 = 1.2 nM 8.92
CHEMBL494191 IC50 = 1.5 nM 8.82
CHEMBL522688 IC50 = 3.0 nM 8.52
CHEMBL522688 IC50 = 3.0 nM 8.52
CHEMBL494191 IC50 = 4.0 nM 8.40
CHEMBL495368 IC50 = 4.6 nM 8.34
CHEMBL492569 IC50 = 5.5 nM 8.26
CHEMBL522688 IC50 = 5.6 nM 8.25
CHEMBL492564 IC50 = 6.0 nM 8.22
CHEMBL495151 IC50 = 7.0 nM 8.15
CHEMBL494540 IC50 = 7.8 nM 8.11
CHEMBL494580 IC50 = 8.6 nM 8.07
CHEMBL492564 IC50 = 14.3 nM 7.84
CHEMBL521697 IC50 = 22.0 nM 7.66
CHEMBL495149 IC50 = 28.0 nM 7.55
CHEMBL41275 IC50 = 28.0 nM 7.55
CHEMBL523054 IC50 = 30.0 nM 7.52
CHEMBL495165 IC50 = 36.0 nM 7.44
CHEMBL494191 IC50 = 42.0 nM 7.38
CHEMBL494542 IC50 = 51.0 nM 7.29
CHEMBL494770 IC50 = 56.0 nM 7.25
CHEMBL493780 IC50 = 64.0 nM 7.19
CHEMBL494019 IC50 = 77.0 nM 7.11
CHEMBL494591 IC50 = 85.0 nM 7.07
CHEMBL494541 IC50 = 123.0 nM 6.91
CHEMBL522688 IC50 = 141.0 nM 6.85
CHEMBL523857 IC50 = 156.0 nM 6.81
CHEMBL494399 IC50 = 175.0 nM 6.76
CHEMBL523696 IC50 = 187.0 nM 6.73
CHEMBL493575 IC50 = 193.0 nM 6.71
CHEMBL492376 IC50 = 230.0 nM 6.64
CHEMBL523861 IC50 = 239.0 nM 6.62
CHEMBL492564 IC50 = 259.0 nM 6.59
CHEMBL493779 IC50 = 362.0 nM 6.44
CHEMBL524030 IC50 = 419.0 nM 6.38
CHEMBL494580 IC50 = 469.0 nM 6.33
CHEMBL493843 IC50 = 631.0 nM 6.20
CHEMBL523503 IC50 = 765.0 nM 6.12