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BioAssay: AID 630066

Inhibition of TEK relative to control

Imidazo[1,5-a]quinoxalines were synthesized that function as irreversible Bruton's tyrosine kinase (BTK) inhibitors. The syntheses and SAR of this series of compounds are presented as well as the X-ray crystal structure of the lead compound 36 in complex with a gate-keeper variant of ITK enzyme. The lead compound showed good in vivo efficacy in preclinical RA models. ..more
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
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Unspecified(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 630066
Data Source: ChEMBL (787514)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-08-23

Data Table ( Complete ):           View All Data
Tested Compound:
Description:
Title: Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis.

Abstract: Imidazo[1,5-a]quinoxalines were synthesized that function as irreversible Bruton's tyrosine kinase (BTK) inhibitors. The syntheses and SAR of this series of compounds are presented as well as the X-ray crystal structure of the lead compound 36 in complex with a gate-keeper variant of ITK enzyme. The lead compound showed good in vivo efficacy in preclinical RA models.
(PMID: 21958547)
Comment
Putative Target:

ChEMBL Target ID: 12913
Target Type: SINGLE PROTEIN
Pref Name: Tyrosine-protein kinase TIE-2
Synonyms: Angiopoietin-1 receptor;CD_antigen=CD202b;Endothelial tyrosine kinase;hTIE2;p140 TEK;Tunica interna endothelial cell kinase;Tyrosine kinase with Ig and EGF homology domains-2;Tyrosine-protein kinase receptor TEK;Tyrosine-protein kinase receptor TIE-2;
Gene Name: TEK;TIE2 ;VMCM;VMCM1;
Protein Accession: Q02763;
Protein GI: 218511853;
Organism: Homo sapiens
Tax ID: 9606
Target Classification: enzyme kinase protein kinase tk tie
Confidence: Homologous single protein target assigned
Relationship Type: Homologous protein target assigned
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
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)
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