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BioAssay: AID 238688

Inhibitory activity against human carbonic anhydrase V expressed in Escherichia coli

The inhibition of the newly discovered cytosolic carbonic anhydrase (CA, EC 4.2.1.1) isozyme XIII of murine origin (mCA XIII) has been investigated with a series of anions, such as the physiological ones (bicarbonate, chloride), or the metal complexing anions (cyanate, cyanide, azide, hydrogen sulfide, etc), nitrate, nitrite, sulfate, sulfamate, sulfamide as well as with phenylboronic and more ..
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 Tested Compounds
 Tested Compounds
All(18)
 
 
Active(12)
 
 
Unspecified(6)
 
 
 Tested Substances
 Tested Substances
All(18)
 
 
Active(12)
 
 
Unspecified(6)
 
 
 Related BioAssays
 Related BioAssays
AID: 238688
Data Source: ChEMBL (302782)
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 ):           View Active Data    View All Data
BioActive Compounds: 12
Description:
Title: Carbonic anhydrase inhibitors. Inhibition of the newly isolated murine isozyme XIII with anions.

Abstract: The inhibition of the newly discovered cytosolic carbonic anhydrase (CA, EC 4.2.1.1) isozyme XIII of murine origin (mCA XIII) has been investigated with a series of anions, such as the physiological ones (bicarbonate, chloride), or the metal complexing anions (cyanate, cyanide, azide, hydrogen sulfide, etc), nitrate, nitrite, sulfate, sulfamate, sulfamide as well as with phenylboronic and phenylarsonic acids. The best mCA XIII inhibitors were cyanate, thiocyanate, cyanide and sulfamide, with K(I)-s in the range of 0.25microM-0.74 mM, whereas fluoride, iodide, azide, carbonate and hydrogen sulfide were less effective (K(I)-s in the range of 3.0-5.5mM). The least effective inhibitors were sulfate, chloride and bicarbonate (K(I)-s in the range of 138-267 mM). The affinity of mCA XIII for anions is very different from that of the other cytosolic isozymes (hCA I and II) or the mitochondrial isozyme hCA V. This resistance to inhibition by the physiological anions bicarbonate and chloride suggests an evolutionary adaptation of CA XIII to the presence of high concentrations of such anions (e.g., in the reproductive tract of both female and male), and the possible participation of this isozyme (similarly to CA II, CA IV and CA V) in metabolons with proteins involved in the anion exchange and transport, such as the anion exchangers (AE1-3) or the sodium bicarbonate co-transporter (NBC1 and NBC3) proteins, which remain to be identified.
(PMID: 15454240)
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: 104979
Target Type: PROTEIN FAMILY
Pref Name: Carbonic anhydrase V
Synonyms: CA-VA;Carbonate dehydratase VA;Carbonic anhydrase 5A; mitochondrial;Carbonic anhydrase VA;CA-VB;Carbonate dehydratase VB;Carbonic anhydrase 5B; mitochondrial;Carbonic anhydrase VB;
Gene Name: CA5;CA5A;CA5B;
Protein Accession: P35218;Q9Y2D0;
Protein GI: 461680;8928041;
Organism: Homo sapiens
Tax ID: 9606
Target Classification: enzyme lyase
Confidence: Multiple homologous protein targets may be assigned
Relationship Type: Homologous protein target assigned
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

Result Definitions
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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 activity commentKi activity commentString
13Ki standard flagKi standard flagInteger
14Ki qualifierKi qualifierString
15Ki published valueKi published valueFloatnM
16Ki standard valueKi standard valueFloatnM
17Ki data validityKi data validityString

* Activity Concentration.

Data Table (Concise)
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