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BioAssay: AID 478696

Binding affinity to adrenergic alpha2A receptor

The example of St. John's wort offers convincing evidence for the concept that modern methods of pharmacological and phytochemical research are effective in advancing the development of traditional herbal remedies. As a consequence of these efforts, it is known today that several compounds from different structural groups and with different mechanisms of action seem to be responsible for the more ..
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 Tested Compounds
 Tested Compounds
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Active(1)
 
 
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AID: 478696
Data Source: ChEMBL (629559)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-09-27
Modify Date: 2014-08-23

Data Table ( Complete ):           View Active Data    View All Data
BioActive Compound: 1
Description:
Title: Lessons learned from herbal medicinal products: the example of St. John's Wort (perpendicular).

Abstract: The example of St. John's wort offers convincing evidence for the concept that modern methods of pharmacological and phytochemical research are effective in advancing the development of traditional herbal remedies. As a consequence of these efforts, it is known today that several compounds from different structural groups and with different mechanisms of action seem to be responsible for the observed antidepressant efficacy of St. John's Wort. Co-effectors in the extract improve the bioavailability of active constituents such as hypericin (1) (pharmacokinetic synergy). Unwanted side effects are preventable without remarkable loss of activity when the responsible constituent(s) are carefully removed during the extraction process, as demonstrated for hyperforin (3), which is responsible for the induction of cytochrome P450 (CYP)-metabolizing enzymes (CYP3A4, in particular). On the basis of our findings, it is likely that positive interactions between single compounds occur more frequently in traditionally used herbal preparations than is known presently.
(PMID: 20408551)
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: 52
Target Type: SINGLE PROTEIN
Pref Name: Alpha-2a adrenergic receptor
Synonyms: Alpha-2 adrenergic receptor subtype C10;Alpha-2A adrenergic receptor;Alpha-2A adrenoceptor;Alpha-2A adrenoreceptor;Alpha-2AAR;
Gene Name: ADRA2A;ADRA2R ;ADRAR;
Protein Accession: P08913;
Protein GI: 1351829;
Organism: Homo sapiens
Tax ID: 9606
Target Classification: membrane receptor 7tm1 smallmol monoamine receptor adrenergic receptor
Confidence: Homologous single protein target assigned
Relationship Type: Homologous protein target assigned
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
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 valueFloatnM
10Ki standard valueKi standard valueFloatnM

* Activity Concentration.

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