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BioAssay: AID 730373

Inhibition of human cytosolic carbonic anhydrase-2 preincubated for 15 mins by stopped flow CO2 hydration assay

Several beta-carbonic anhydrases (CAs, EC 4.2.1.1) are present in all land plants examined thus far. Here we report the first detailed biochemical characterization of one such isoform, FbiCA 1, from the C4 plant Flaveria bidentis, which was cloned, purified and characterized as recombinant protein. FbiCA 1 has an interesting CO2 hydrase catalytic activity (kcat of 1.2#10(5) and kcat/Km of more ..
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 Tested Compounds
 Tested Compounds
All(33)
 
 
Active(5)
 
 
Unspecified(28)
 
 
 Tested Substances
 Tested Substances
All(36)
 
 
Active(5)
 
 
Unspecified(31)
 
 
AID: 730373
Data Source: ChEMBL (942941)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-11-07
Modify Date: 2014-05-27

Data Table ( Complete ):           Active    All
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: 5
Description:
Title: Kinetic and anion inhibition studies of a beta-carbonic anhydrase (FbiCA 1) from the C4 plant Flaveria bidentis.

Abstract: Several beta-carbonic anhydrases (CAs, EC 4.2.1.1) are present in all land plants examined thus far. Here we report the first detailed biochemical characterization of one such isoform, FbiCA 1, from the C4 plant Flaveria bidentis, which was cloned, purified and characterized as recombinant protein. FbiCA 1 has an interesting CO2 hydrase catalytic activity (kcat of 1.2#10(5) and kcat/Km of 7.5#10(6)M(-1)#s(-1)) and was moderately inhibited by most simple/complex inorganic anions. Potent FbiCA 1 inhibitors were also detected, such as trithiocarbonate, diethyldithiocarbamate, sulfamide, sulfamic acid, phenylboronic acid and phenylarsonic acid (KIs in the range of 4-60muM). Such inhibitors may be used as tools to better understand the role of various beta-CA isoforms in photosynthesis.
(PMID: 23414801)
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
Show more
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Ki*Ki PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6Ki activity commentKi activity commentString
7Ki standard flagKi standard flagInteger
8Ki qualifierKi qualifierString
9Ki published valueKi published valueFloatmM
10Ki standard valueKi standard valueFloatnM
11Ki data validityKi data validityString
12Ki binding domainsKi binding domainsString
13Ki activity commentKi activity commentString
14Ki standard flagKi standard flagInteger
15Ki qualifierKi qualifierString
16Ki published valueKi published valueFloatnM
17Ki standard valueKi standard valueFloatnM
18Ki data validityKi data validityString
19Ki binding domainsKi binding domainsString

* Activity Concentration.

Data Table (Concise)
Classification
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