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Assay Detail

CHEMBL950882

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Functional
Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

Novel pyrrolidine ureas as C-C chemokine receptor 1 (CCR1) antagonists.
Merritt JR, Liu J, Quadros E, Morris ML, Liu R, Zhang R, Jacob B, Postelnek J, Hicks CM, Chen W, Kimble EF, Rogers WL, O'Brien L, White N, Desai H, Bansal S, King G, Ohlmeyer MJ, Appell KC, Webb ML.
J Med Chem (2009) 52 : 1295 -1301
PubMed 19183043 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.71 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL232656 BX 471 FREE BASE 2.0 1 8.82
CHEMBL475748 1 8.22
CHEMBL473734 1 7.80
CHEMBL514611 1 7.66
CHEMBL473532 1 7.66
CHEMBL473531 1 7.46
CHEMBL517290 1 6.36
CHEMBL461590 1 -
CHEMBL516495 1 -
CHEMBL462441 1 -
CHEMBL462442 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL232656 BX 471 FREE BASE IC50 = 1.5 nM 8.82
CHEMBL475748 IC50 = 6.0 nM 8.22
CHEMBL473734 IC50 = 16.0 nM 7.80
CHEMBL514611 IC50 = 22.0 nM 7.66
CHEMBL473532 IC50 = 22.0 nM 7.66
CHEMBL473531 IC50 = 35.0 nM 7.46
CHEMBL517290 IC50 = 440.0 nM 6.36
CHEMBL461590 IC50 - -
CHEMBL516495 IC50 - -
CHEMBL462441 IC50 - -
CHEMBL462442 IC50 - -