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BioAssay: AID 365828

Activation of human recombinant CA2 at 10 uM by stopped-flow CO2 hydration method

An activation study of the human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms hCA III (cytosolic) and IV (membrane-associated) with a series of natural and non-natural amino acids and aromatic/heterocyclic amines is reported. hCA III was efficiently activated by d-His, serotonin, pyridyl-alkylamines, and aminoethyl-piperazine/morpholine (K(A)s of 91nM-1.12microM), whereas the best hCA IV more ..
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 Tested Compounds
 Tested Compounds
All(18)
 
 
Active(15)
 
 
Unspecified(3)
 
 
 Tested Substances
 Tested Substances
All(18)
 
 
Active(15)
 
 
Unspecified(3)
 
 
AID: 365828
Data Source: ChEMBL (513857)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2014-05-25

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Carbonic anhydrase 2; AltName: Full=Carbonate dehydratase II; AltName: Full=Carbonic anhydrase C; Short=CAC; AltName: Full=Carbonic anhydrase II; Short=CA-II
Description ..   
Protein Family: alpha_CA_I_II_III_XIII
Comment ..   

Gene:CA2     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 15
Description:
Title: Carbonic anhydrase activators: Activation of the human cytosolic isozyme III and membrane-associated isoform IV with amino acids and amines.

Abstract: An activation study of the human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms hCA III (cytosolic) and IV (membrane-associated) with a series of natural and non-natural amino acids and aromatic/heterocyclic amines is reported. hCA III was efficiently activated by d-His, serotonin, pyridyl-alkylamines, and aminoethyl-piperazine/morpholine (K(A)s of 91nM-1.12microM), whereas the best hCA IV activators were 4-amino-phenylalanine, serotonin, and 4-(2-aminoethyl)-morpholine (K(A)s of 79nM-3.14microM). Precise steric and electronic requirements are needed to be present in the molecules of effective CA III/IV activators, in order to assure an adequate fit within the enzyme active site for the formation of the enzyme-activator complex, and for efficient proton transfer processes between the active site and the reaction medium. The activation profiles of CA III and IV are distinct from those of all other mammalian CA isoforms investigated so far for their interaction with amino acids and amines.
(PMID: 18627905)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: biochemical format

Target Type: Target is a single protein chain

Protein Target Class: enzyme lyase

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Ka activity commentKa activity commentString
2Ka standard flagKa standard flagInteger
3Ka qualifierKa qualifierString
4Ka published valueKa published valueFloatμM
5Ka standard valueKa standard valueFloatnM

Data Table (Concise)
Data Table ( Complete ):     View Active Data    View All Data
Classification
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