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Assay Detail

CHEMBL950881

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

Binding
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
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 29 6.33 8.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL232656 BX 471 FREE BASE 2.0 1 8.26
CHEMBL475748 1 7.96
CHEMBL473532 1 7.64
CHEMBL473734 1 7.30
CHEMBL473531 1 6.92
CHEMBL514611 1 6.85
CHEMBL454942 1 6.57
CHEMBL455162 1 6.57
CHEMBL517290 1 6.54
CHEMBL454940 1 6.27
CHEMBL461590 1 6.17
CHEMBL516495 1 6.16
CHEMBL462441 1 6.14
CHEMBL517261 1 5.89
CHEMBL462442 1 5.53
CHEMBL509457 1 5.44
CHEMBL460535 1 5.40
CHEMBL517262 1 5.33
CHEMBL462644 1 5.24
CHEMBL462650 1 4.37
CHEMBL454941 1 -
CHEMBL462611 1 -
CHEMBL517141 1 -
CHEMBL462435 1 -
CHEMBL462612 1 -
CHEMBL515927 1 -
CHEMBL472912 1 -
CHEMBL472711 1 -
CHEMBL460534 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL232656 BX 471 FREE BASE IC50 = 5.5 nM 8.26
CHEMBL475748 IC50 = 11.0 nM 7.96
CHEMBL473532 IC50 = 23.0 nM 7.64
CHEMBL473734 IC50 = 50.0 nM 7.30
CHEMBL473531 IC50 = 120.0 nM 6.92
CHEMBL514611 IC50 = 140.0 nM 6.85
CHEMBL454942 IC50 = 270.0 nM 6.57
CHEMBL455162 IC50 = 270.0 nM 6.57
CHEMBL517290 IC50 = 290.0 nM 6.54
CHEMBL454940 IC50 = 540.0 nM 6.27
CHEMBL461590 IC50 = 680.0 nM 6.17
CHEMBL516495 IC50 = 700.0 nM 6.16
CHEMBL462441 IC50 = 720.0 nM 6.14
CHEMBL517261 IC50 = 1300.0 nM 5.89
CHEMBL462442 IC50 = 2950.0 nM 5.53
CHEMBL509457 IC50 = 3600.0 nM 5.44
CHEMBL460535 IC50 = 4000.0 nM 5.40
CHEMBL517262 IC50 = 4700.0 nM 5.33
CHEMBL462644 IC50 = 5700.0 nM 5.24
CHEMBL462650 IC50 = 43000.0 nM 4.37
CHEMBL454941 IC50 > 75000.0 nM -
CHEMBL462611 IC50 > 100000.0 nM -
CHEMBL517141 IC50 > 77000.0 nM -
CHEMBL462435 IC50 > 13000.0 nM -
CHEMBL462612 IC50 > 100000.0 nM -
CHEMBL515927 IC50 > 28000.0 nM -
CHEMBL472912 IC50 > 100000.0 nM -
CHEMBL472711 IC50 > 28000.0 nM -
CHEMBL460534 IC50 > 100000.0 nM -