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BioAssay: AID 146705

Tested for inhibition of Nucleoside Triphosphate Diphosphohydrolase (NTPDase) from bovine spleen.

To elucidate the physiological role played by nucleoside triphosphate diphosphohydrolase (NTPDase; EC 3.6.1.5), adenine nucleotide analogues, modified on the purine ring, have been synthesized and tested as potential inhibitors. Resistance of ATP analogues to hydrolysis and their potency as NTPDase inhibitors were evaluated. For this purpose, a particulate fraction isolated from bovine spleen was more ..
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 Tested Compounds
 Tested Compounds
All(10)
 
 
Active(9)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(10)
 
 
Active(9)
 
 
Unspecified(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 146705
Data Source: ChEMBL (143949)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-24
Modify Date: 2014-05-20

Data Table ( Complete ):           Active    All
BioActive Compounds: 9
Description:
Title: Novel inhibitors of nucleoside triphosphate diphosphohydrolases: chemical synthesis and biochemical and pharmacological characterizations.

Abstract: To elucidate the physiological role played by nucleoside triphosphate diphosphohydrolase (NTPDase; EC 3.6.1.5), adenine nucleotide analogues, modified on the purine ring, have been synthesized and tested as potential inhibitors. Resistance of ATP analogues to hydrolysis and their potency as NTPDase inhibitors were evaluated. For this purpose, a particulate fraction isolated from bovine spleen was used as the enzyme source. Among the synthesized analogues, 8-thiobutyladenosine 5'-triphosphate (8-BuS-ATP) was found to be the most effective nonhydrolyzable competitive inhibitor, with an estimated K(i) of 10 microM. This nonhydrolyzable analogue did not exert any P2X-receptor-mediated effect on endothelium-denuded blood vessels, from the guinea pig mesenteric bed. In agreement with this observation, infusion of the analogue did not cause any significant blood pressure variations of the precontracted vessel. Because in previous studies on isolated turkey erythrocytes and rat astrocytes 8-BuS-ATP was not able to trigger any P2Y(1)-receptor-mediated effect, it therefore appears that this NTPDase inhibitor does not interfere with purinergic receptors.
(PMID: 10841802)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Putative Target:

ChEMBL Target ID: 11227
Target Type: SINGLE PROTEIN
Pref Name: Ectonucleoside triphosphate diphosphohydrolase 1
Synonyms: CD_antigen=CD39;Ecto-apyrase;Ecto-ATP diphosphohydrolase 1;Ecto-ATPase 1;Ecto-ATPDase 1;Ectonucleoside triphosphate diphosphohydrolase 1;Lymphoid cell activation antigen;NTPDase 1;
Gene Name: CD39;ENTPD1;
Protein Accession: O18956;
Protein GI: 14547940;
Organism: Bos taurus
Tax ID: 9913
Target Classification: enzyme
Confidence: Homologous single protein target assigned
Relationship Type: Homologous protein target assigned
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: biochemical format

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Km*Km PubChem standard valueFloatμM
2Km activity commentKm activity commentString
3Km standard flagKm standard flagInteger
4Km qualifierKm qualifierString
5Km published valueKm published valueFloatμM
6Km standard valueKm standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
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