Bookmark and Share
BioAssay: AID 365827

Activation of human recombinant CA1 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 ..
_
   
 Tested Compounds
 Tested Compounds
All(18)
 
 
Active(17)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(18)
 
 
Active(17)
 
 
Unspecified(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 365827
Data Source: ChEMBL (513856)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2013-11-21

Data Table ( Complete ):           Active    All
Target
Sequence: RecName: Full=Carbonic anhydrase 1; AltName: Full=Carbonate dehydratase I; AltName: Full=Carbonic anhydrase B; Short=CAB; AltName: Full=Carbonic anhydrase I; Short=CA-I
Description ..   
Protein Family: alpha_CA_I_II_III_XIII
Comment ..   

Gene:CA1     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 17
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
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 10193

ChEMBL Target Type: Target is a single protein chain

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)
Classification
PageFrom: