Assay Detail

CHEMBL3366559

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Binding

Antagonist activity at CCR1 receptor in human whole blood assessed as blocked of MIP-1alpha-mediated CD11b upregulation preincubated for 1 hr

ChEMBL ↗

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Target

C-C chemokine receptor type 1 (CHEMBL2413) ↗

Open DB target context

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C-C chemokine receptor type 1 (CHEMBL2413) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target C-C chemokine receptor type 1

CHEMBL2413

Anchored from Assay target.

Protein identity C-C chemokine receptor type 1

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Tissue	Blood
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

C-C chemokine receptor type 1 (CHEMBL2413) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis.

Santella JB, Gardner DS, Duncia JV, Wu H, Dhar M, Cavallaro C, Tebben AJ, Carter PH, Barrish JC, Yarde M, Briceno SW, Cvijic ME, Grafstrom RR, Liu R, Patel SR, Watson AJ, Yang G, Rose AV, Vickery RD, Caceres-Cortes J, Caporuscio C, Camac DM, Khan JA, An Y, Foster WR, Davies P, Hynes J.
J Med Chem (2014) 57 : 7550 -7564
PubMed 25101488 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	7.60	7.60

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3334824	BMS-817399	2.0	1	7.60

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3334824	BMS-817399	IC50	=	25.0	nM	7.60