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Assay Detail

CHEMBL864277

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

Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

4-Amino-2-alkyl-butyramides as small molecule CCR2 antagonists with favorable pharmacokinetic properties.
Butora G, Morriello GJ, Kothandaraman S, Guiadeen D, Pasternak A, Parsons WH, MacCoss M, Vicario PP, Cascieri MA, Yang L.
Bioorg Med Chem Lett (2006) 16 : 4715 -4722
PubMed 16870431 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.31 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL441856 1 8.40
CHEMBL215020 1 8.05
CHEMBL378195 1 7.92
CHEMBL213058 1 7.89
CHEMBL385540 1 7.82
CHEMBL380190 1 7.43
CHEMBL215394 1 7.43
CHEMBL215654 1 7.42
CHEMBL214641 1 7.38
CHEMBL215093 1 7.33
CHEMBL214825 1 7.32
CHEMBL215689 1 7.14
CHEMBL214647 1 7.14
CHEMBL214747 1 7.14
CHEMBL212972 1 7.10
CHEMBL215391 1 7.07
CHEMBL409162 1 7.03
CHEMBL215759 1 6.89
CHEMBL215271 1 6.67
CHEMBL212939 1 6.63
CHEMBL377819 1 6.33
CHEMBL386711 1 -
CHEMBL215976 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL441856 IC50 = 4.0 nM 8.40
CHEMBL215020 IC50 = 9.0 nM 8.05
CHEMBL378195 IC50 = 12.0 nM 7.92
CHEMBL213058 IC50 = 13.0 nM 7.89
CHEMBL385540 IC50 = 15.0 nM 7.82
CHEMBL380190 IC50 = 37.0 nM 7.43
CHEMBL215394 IC50 = 37.0 nM 7.43
CHEMBL215654 IC50 = 38.0 nM 7.42
CHEMBL214641 IC50 = 42.0 nM 7.38
CHEMBL215093 IC50 = 47.0 nM 7.33
CHEMBL214825 IC50 = 48.0 nM 7.32
CHEMBL215689 IC50 = 72.0 nM 7.14
CHEMBL214647 IC50 = 72.0 nM 7.14
CHEMBL214747 IC50 = 73.0 nM 7.14
CHEMBL212972 IC50 = 80.0 nM 7.10
CHEMBL215391 IC50 = 86.0 nM 7.07
CHEMBL409162 IC50 = 93.0 nM 7.03
CHEMBL215759 IC50 = 129.0 nM 6.89
CHEMBL215271 IC50 = 216.0 nM 6.67
CHEMBL212939 IC50 = 232.0 nM 6.63
CHEMBL377819 IC50 = 462.0 nM 6.33
CHEMBL386711 IC50 - -
CHEMBL215976 IC50 - -