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BioAssay: AID 268013

Protein binding in rat plasma at 10 uM at pH 7.4

We have screened molecules for inhibition of MetAP2 as a novel approach toward antiangiogenesis and anticancer therapy using affinity selection/mass spectrometry (ASMS) employing MetAP2 loaded with Mn(2+) as the active site metal. After a series of anthranilic acid sulfonamides with micromolar affinities was identified, chemistry efforts were initiated. The micromolar hits were quickly improved to potent nanomolar inhibitors by chemical modifications guided by insights from X-ray crystallography. ..more
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 Tested Compounds
 Tested Compounds
All(5)
 
 
Unspecified(5)
 
 
 Tested Substances
 Tested Substances
All(5)
 
 
Unspecified(5)
 
 
 Related BioAssays
 Related BioAssays
AID: 268013
Data Source: ChEMBL (374368)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-24
Modify Date: 2014-05-22

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Tested Compounds:
Description:
Title: Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.

Abstract: We have screened molecules for inhibition of MetAP2 as a novel approach toward antiangiogenesis and anticancer therapy using affinity selection/mass spectrometry (ASMS) employing MetAP2 loaded with Mn(2+) as the active site metal. After a series of anthranilic acid sulfonamides with micromolar affinities was identified, chemistry efforts were initiated. The micromolar hits were quickly improved to potent nanomolar inhibitors by chemical modifications guided by insights from X-ray crystallography.
(PMID: 16632353)
Comment
Putative Target:

ChEMBL Target ID: 102352
Target Type: TISSUE
Pref Name: Plasma
Organism: Rattus norvegicus
Tax ID: 10116
Confidence: Target assigned is non-molecular
Relationship Type: Non-molecular target assigned
Categorized Comment - additional comments and annotations
From ChEMBL:
Assay Type: ADME
Assay Data Source: Scientific Literature
Assay Tissue: Plasma
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1PPB activity commentPPB activity commentString
2PPB standard flagPPB standard flagInteger
3PPB qualifierPPB qualifierString
4PPB published valuePPB published valueFloat%
5PPB standard valuePPB standard valueFloat%

Data Table (Concise)
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