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BioAssay: AID 630061

Inhibition of RSK1 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
All(1)
 
 
Unspecified(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 630061
Data Source: ChEMBL (787509)
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: 10929
Target Type: SINGLE PROTEIN
Pref Name: Ribosomal protein S6 kinase alpha 1
Synonyms: 90 kDa ribosomal protein S6 kinase 1;MAP kinase-activated protein kinase 1a;MAPK-activated protein kinase 1a;MAPKAP kinase 1a;MAPKAPK-1a;p90-RSK 1;p90RSK1;p90S6K;Ribosomal protein S6 kinase alpha-1;Ribosomal S6 kinase 1;RSK-1;S6K-alpha-1;
Gene Name: MAPKAPK1A ;RPS6KA1;RSK1;
Protein Accession: Q15418;
Protein GI: 20178306;
Organism: Homo sapiens
Tax ID: 9606
Target Classification 1: enzyme kinase protein kinase agc rsk rsk
Target Classification 2: enzyme kinase protein kinase camk rskb rskb
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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