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BioAssay: AID 624194

Antagonists at Human 5-Hydroxytryptamine receptor 5-ht5a

This assay details affinity data for antagonists at human 5-Hydroxytryptamine receptor 5-ht5a, as described in the published literature. Where possible the data described are at transfected receptors expressed in cell lines and the ligands described are those that are potent, selective, endogenous, or those used as prescription medications. ..more
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 Tested Compounds
 Tested Compounds
All(11)
 
 
Active(11)
 
 
 Tested Substances
 Tested Substances
All(11)
 
 
Active(11)
 
 
 Related BioAssays
 Related BioAssays
AID: 624194
Data Source: IUPHAR-DB (10_Antagonist_Human)
Depositor Category: Literature, Extracted
Deposit Date: 2012-05-24

Data Table ( Complete ):           Active    All
Target
BioActive Compounds: 11
Description:
This assay details affinity data for antagonists at human 5-Hydroxytryptamine receptor 5-ht5a, as described in the published literature. Where possible the data described are at transfected receptors expressed in cell lines and the ligands described are those that are potent, selective, endogenous, or those used as prescription medications.
Protocol
The International Union of Basic and Clinical Pharmacology Database (IUPHAR-DB) uses expert subcommittees to collate peer-reviewed information from the published literature regarding individual receptors or ion channels, and describes the pharmacology, genetics, function and anatomy of each receptor. Its pages provide a richly curated overview of the biology of each receptor and can be found by following the external link to the IUPHAR-DB website.
Comment
The data collected focuses on ligands at human receptors. Data are provided at rat or mouse receptors where there are significant species differences, or where data are not yet available at human receptors.

Information on individual experimental protocols can be found in the primary references listed for each ligand.

Affinity data are expressed as pKi [-log(Ki)], pKd [-log(Kd)], pIC50 [-log(IC50)], pEC50 [-log(EC50)], pKB [-log(KB)] or as a micromolar concentration range. In most cases the original concentration can be found in the primary reference.
Result Definitions
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TIDNameDescriptionAnnotationHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1pKi_minThe negative logarithm to base 10 of the equilibrium dissociation constant (Ki) for the ligand, determined in inhibition studies.

This column contains the minimum pKi value, where several measurements have been published.
Float
2pKi_maxThe negative logarithm to base 10 of the equilibrium dissociation constant (Ki) for the ligand, determined in inhibition studies.

This column contains the maximum pKi value, where several measurements have been published.
Float
3pKd_minThe negative logarithm to base 10 of the equilibrium dissociation constant (Kd) for the ligand, determined directly in a binding assay using a labelled ligand.

This column contains the minimum pKd value, where several measurements have been published.
Float
4pKd_maxThe negative logarithm to base 10 of the equilibrium dissociation constant (Kd) for the ligand, determined directly in a binding assay using a labelled ligand.

This column contains the maximum pKd value, where several measurements have been published.
Float
5pIC50_minThe negative logarithm to base 10 of the IC50. The IC50 is used in two ways:
1) the concentration of an antagonist that reduces the response to an agonist by 50%;
2) the concentration of an unlabeled agonist or antagonist that inhibits the binding of a radioligand by 50%.

This column contains the minimum pIC50 value, where several measurements have been published.
Float
6pIC50_maxThe negative logarithm to base 10 of the IC50. The IC50 is used in two ways:
1) the concentration of an antagonist that reduces the response to an agonist by 50%;
2) the concentration of an unlabeled agonist or antagonist that inhibits the binding of a radioligand by 50%.

This column contains the maximum pIC50 value, where several measurements have been published.
Float
7pEC50_minThe negative logarithm to base 10 of the EC50. The EC50 is the concentration of an agonist that produces 50% of the maximal possible effect of that agonist.

This column contains the minimum pEC50 value, where several measurements have been published.
Float
8pEC50_maxThe negative logarithm to base 10 of the EC50. The EC50 is the concentration of an agonist that produces 50% of the maximal possible effect of that agonist.

This column contains the maximum pEC50 value, where several measurements have been published.
Float
9pKB_minThe negative logarithm to base 10 of the equilibrium dissociation constant (KB) of a ligand (traditionally, a competitive antagonist), determined by means of a functional assay.

This column contains the minimum pKB value, where several measurements have been published.
Float
10pKB_maxThe negative logarithm to base 10 of the equilibrium dissociation constant (KB) of a ligand (traditionally, a competitive antagonist), determined by means of a functional assay.

This column contains the maximum pKB value, where several measurements have been published.
Float
11Concentration range (muM)Where affinity data are not available, the concentration range of the ligand used for the study is displayed (in muM).String
12ActionThe specific action of the ligand at the target, for example, full, partial or inverse agonist.String
13Reference (PubMed ID)The primary reference from which the data was obtained.PMIDString

Data Table (Concise)
Classification
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