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Assay Detail

CHEMBL2340873

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

Binding
Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type THP-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-C chemokine receptor type 1 (CHEMBL2413)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Spirocyclic compounds, potent CCR1 antagonists.
Hossain N, Ivanova S, Bergare J, Eriksson T.
Bioorg Med Chem Lett (2013) 23 : 1883 -1886
PubMed 23414842 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.15 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2332935 1 8.70
CHEMBL2332936 1 8.59
CHEMBL2332942 1 7.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2332935 IC50 = 2.0 nM 8.70
CHEMBL2332936 IC50 = 2.6 nM 8.59
CHEMBL2332942 IC50 = 68.0 nM 7.17