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BioAssay: AID 645526

Displacement of [125I]MCP1 from CCR2 in human PBMC at 1 uM after 30 mins by gamma counter

We report the identification of 13 (INCB3284) as a potent human CCR2 (hCCR2) antagonist. INCB3284 exhibited an IC50 of 3.7 nM in antagonism of monocyte chemoattractant protein-1 binding to hCCR2, an IC50 of 4.7 nM in antagonism of chemotaxis activity, an IC50 of 84 muM in inhibition of the hERG potassium current, a free fraction of 58% in protein binding, high selectivity over other chemokine more ..
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 Tested Compounds
 Tested Compounds
All(12)
 
 
Unspecified(12)
 
 
 Tested Substances
 Tested Substances
All(12)
 
 
Unspecified(12)
 
 
 Related BioAssays
 Related BioAssays
AID: 645526
Data Source: ChEMBL (802974)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-08-24

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=C-C chemokine receptor type 2; Short=C-C CKR-2; Short=CC-CKR-2; Short=CCR-2; Short=CCR2; AltName: Full=Monocyte chemoattractant protein 1 receptor; Short=MCP-1-R; AltName: CD_antigen=CD192
Description ..   
Comment ..   

Gene:CCR2     Conserved Domain     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist.

Abstract: We report the identification of 13 (INCB3284) as a potent human CCR2 (hCCR2) antagonist. INCB3284 exhibited an IC50 of 3.7 nM in antagonism of monocyte chemoattractant protein-1 binding to hCCR2, an IC50 of 4.7 nM in antagonism of chemotaxis activity, an IC50 of 84 muM in inhibition of the hERG potassium current, a free fraction of 58% in protein binding, high selectivity over other chemokine receptors and G-protein-coupled receptors, and acceptable oral bioavailability in rodents and primates. In human clinical trials, INCB3284 exhibited a pharmacokinetic profile suitable for once-a-day dosing (T 1/2 = 15 h).
(PMID: 24900329)
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Inhibition activity commentInhibition activity commentString
2Inhibition standard flagInhibition standard flagInteger
3Inhibition qualifierInhibition qualifierString
4Inhibition published valueInhibition published valueFloat%
5Inhibition standard valueInhibition standard valueFloat%

Data Table (Concise)
Data Table ( Complete ):     View All Data
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