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BioAssay: AID 254633

Concentration required to stimulate binding of [35S]GTP-gamma-S, with G alpha i1; not determined

Heterotrimeric G proteins play a pivotal role in the communication of cells with the environment. G proteins are stimulated by cell surface receptors (GPCR) that catalyze the exchange of GDP, bound to Galpha subunit, with GTP and can per se be the target of drugs. Based on the structure of two nonpeptidic modulators of Gi proteins, a series of new molecules characterized by a long hydrophobic more ..
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Inconclusive(1)
 
 
 Tested Substances
 Tested Substances
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Inconclusive(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 254633
Data Source: ChEMBL (321109)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-24
Modify Date: 2014-05-21

Data Table ( Complete ):           All
Target
Sequence: RecName: Full=Guanine nucleotide-binding protein G(i) subunit alpha-1; AltName: Full=Adenylate cyclase-inhibiting G alpha protein
Description ..   
Protein Family: Alpha subunit of G proteins (guanine nucleotide binding)
Comment ..   

Gene:GNAI1     Related Protein 3D Structures     More BioActivity Data..
Tested Compound:
Description:
Title: Design, synthesis, and preliminary pharmacological evaluation of a set of small molecules that directly activate gi proteins.

Abstract: Heterotrimeric G proteins play a pivotal role in the communication of cells with the environment. G proteins are stimulated by cell surface receptors (GPCR) that catalyze the exchange of GDP, bound to Galpha subunit, with GTP and can per se be the target of drugs. Based on the structure of two nonpeptidic modulators of Gi proteins, a series of new molecules characterized by a long hydrophobic chain and at least two nitrogen atoms protonated at physiological pH was designed. The compounds were tested for their ability to stimulate binding of GTPgammaS to recombinant Gi proteins. Gi activation properties were also evaluated by inhibition of adenylyl cyclase activity in intact lymphocytes. Most compounds were able to stimulate GTPgammaS binding and to inhibit cAMP production at micromolar doses. Among the active compounds, 34 showed good efficacy and was the most potent compound studied, particularly on alpha(o) subtype; its regioisomer, 36, was the most efficacious one. Compound 7 showed also an interesting profile as it showed selectivity toward the alpha(o) subtype, in both efficacy and potency. Some of the compounds synthesized and found to be active may be useful leads to develop more potent and selective Gi protein modulators.
(PMID: 16190775)
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: biochemical format

Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1EC50 activity commentEC50 activity commentString
2EC50 standard flagEC50 standard flagInteger
3EC50 qualifierEC50 qualifierString
4EC50 published valueEC50 published valueFloatμM
5EC50 standard valueEC50 standard valueFloat

Data Table (Concise)
Classification
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