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BioAssay: AID 780006

Inhibition of ROCK1 (unknown origin) at 30 uM

Structure-activity relationships of 6-(benzoylamino)benzoxaborole analogs were investigated for the inhibition of TNF-alpha, IL-1beta, and IL-6 from lipopolysaccharide stimulated peripheral blood mononuclear cells. Compound 1q showed potent activity against all three cytokines with IC50 values between 0.19 and 0.50muM, inhibited LPS-induced TNF-alpha and IL-6 elevation in mice and improved collagen-induced arthritis in mice. Compound 1q (AN4161) is considered to be a promising lead for novel anti-inflammatory agent with an excellent pharmacokinetic profile. ..more
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Inactive(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Inactive(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 780006
Data Source: ChEMBL (990575)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2014-05-03
Modify Date: 2014-08-25

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Rho-associated protein kinase 1; AltName: Full=Renal carcinoma antigen NY-REN-35; AltName: Full=Rho-associated, coiled-coil-containing protein kinase 1; AltName: Full=Rho-associated, coiled-coil-containing protein kinase I; Short=ROCK-I; AltName: Full=p160 ROCK-1; Short=p160ROCK
Description ..   
Protein Family: Catalytic domain of the Serine/Threonine Kinase, Rho-associated coiled-coil containing protein kinase 1
Comment ..   

Gene:ROCK1     Related Protein 3D Structures     More BioActivity Data..
Tested Compound:
Description:
Title: Discovery and structure-activity relationships of 6-(benzoylamino)benzoxaboroles as orally active anti-inflammatory agents.

Abstract: Structure-activity relationships of 6-(benzoylamino)benzoxaborole analogs were investigated for the inhibition of TNF-alpha, IL-1beta, and IL-6 from lipopolysaccharide stimulated peripheral blood mononuclear cells. Compound 1q showed potent activity against all three cytokines with IC50 values between 0.19 and 0.50muM, inhibited LPS-induced TNF-alpha and IL-6 elevation in mice and improved collagen-induced arthritis in mice. Compound 1q (AN4161) is considered to be a promising lead for novel anti-inflammatory agent with an excellent pharmacokinetic profile.
(PMID: 24075731)
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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