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Assay Detail

CHEMBL1108763

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

Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293-EBNA
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists.
Lim JW, Oh Y, Kim JH, Oak MH, Na Y, Lee JO, Lee SW, Cho H, Park WK, Choi G, Kang J.
Bioorg Med Chem Lett (2010) 20 : 2099 -2102
PubMed 20223662 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 5.69 6.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1092929 1 6.24
CHEMBL337246 1 6.21
CHEMBL1093469 1 6.00
CHEMBL1089965 1 6.00
CHEMBL1092238 1 5.95
CHEMBL1089881 1 5.95
CHEMBL1090548 1 5.93
CHEMBL495202 1 5.92
CHEMBL1088874 1 5.88
CHEMBL1092921 1 5.85
CHEMBL1092293 1 5.76
CHEMBL1092294 1 5.76
CHEMBL1093802 1 5.73
CHEMBL1089629 1 5.66
CHEMBL1090206 1 5.54
CHEMBL1089793 1 5.52
CHEMBL1088875 1 5.50
CHEMBL255408 1 5.50
CHEMBL1093153 1 5.46
CHEMBL1092343 1 5.45
CHEMBL1093470 1 5.35
CHEMBL1092920 1 5.18
CHEMBL1089849 1 5.12
CHEMBL1092656 1 5.08
CHEMBL254355 1 -
CHEMBL1093154 1 -
CHEMBL273083 1 -
CHEMBL1088810 1 -
CHEMBL1090148 1 -
CHEMBL1091171 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1092929 IC50 = 580.0 nM 6.24
CHEMBL337246 IC50 = 610.0 nM 6.21
CHEMBL1093469 IC50 = 990.0 nM 6.00
CHEMBL1089965 IC50 = 1000.0 nM 6.00
CHEMBL1092238 IC50 = 1120.0 nM 5.95
CHEMBL1089881 IC50 = 1130.0 nM 5.95
CHEMBL1090548 IC50 = 1180.0 nM 5.93
CHEMBL495202 IC50 = 1200.0 nM 5.92
CHEMBL1088874 IC50 = 1310.0 nM 5.88
CHEMBL1092921 IC50 = 1410.0 nM 5.85
CHEMBL1092293 IC50 = 1740.0 nM 5.76
CHEMBL1092294 IC50 = 1730.0 nM 5.76
CHEMBL1093802 IC50 = 1880.0 nM 5.73
CHEMBL1089629 IC50 = 2210.0 nM 5.66
CHEMBL1090206 IC50 = 2880.0 nM 5.54
CHEMBL1089793 IC50 = 3040.0 nM 5.52
CHEMBL1088875 IC50 = 3160.0 nM 5.50
CHEMBL255408 IC50 = 3200.0 nM 5.50
CHEMBL1093153 IC50 = 3460.0 nM 5.46
CHEMBL1092343 IC50 = 3520.0 nM 5.45
CHEMBL1093470 IC50 = 4440.0 nM 5.35
CHEMBL1092920 IC50 = 6600.0 nM 5.18
CHEMBL1089849 IC50 = 7520.0 nM 5.12
CHEMBL1092656 IC50 = 8330.0 nM 5.08
CHEMBL254355 IC50 = 2400.0 nM -
CHEMBL1093154 IC50 > 10000.0 nM -
CHEMBL273083 IC50 = 5100.0 nM -
CHEMBL1088810 IC50 > 10000.0 nM -
CHEMBL1090148 IC50 > 10000.0 nM -
CHEMBL1091171 IC50 > 10000.0 nM -
CHEMBL1091172 IC50 > 10000.0 nM -