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BioAssay: AID 297178

Activation of olfactory CNG A2A41b channel expressed in HEK293 cells assessed as effect on half maximal current

Cyclic nucleotide-gated (CNG) channels, key players in olfactory and visual signal transduction, generate electrical responses to odorant- and light-induced changes in cyclic nucleotide concentration. Previous work suggests that substitutions are tolerated solely at the C8 position on the purine ring of cGMP. Our studies with C8, 2'-OH, and 2-NH2-modified cGMP derivatives support this assertion. more ..
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 Tested Compounds
 Tested Compounds
All(17)
 
 
Active(14)
 
 
Inactive(1)
 
 
Unspecified(2)
 
 
 Tested Substances
 Tested Substances
All(17)
 
 
Active(14)
 
 
Inactive(1)
 
 
Unspecified(2)
 
 
 Related BioAssays
 Related BioAssays
AID: 297178
Data Source: ChEMBL (445204)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-25
Modify Date: 2014-05-23

Data Table ( Complete ):           View Active Data    View All Data
BioActive Compounds: 14
Description:
Title: Novel N7- and N1-substituted cGMP derivatives are potent activators of cyclic nucleotide-gated channels.

Abstract: Cyclic nucleotide-gated (CNG) channels, key players in olfactory and visual signal transduction, generate electrical responses to odorant- and light-induced changes in cyclic nucleotide concentration. Previous work suggests that substitutions are tolerated solely at the C8 position on the purine ring of cGMP. Our studies with C8, 2'-OH, and 2-NH2-modified cGMP derivatives support this assertion. To gain further insight into determinants important for CNG channel binding and activation, we targeted previously unexplored positions. Modifications at N7 of 8-SH-cGMP (6) are well tolerated by olfactory and retinal rod CNG channels. Toleration of a very large substituent, a 3400 molecular weight PEG, at either N7 or C8 argues for broad accommodation at these positions in the binding site. Modification at N1 of cGMP reduces the apparent affinity for the channel; however, when combined with 8-parachlorophenylthio derivatization, the resulting cGMP analogue is more potent than cGMP itself. These studies establish the N7 and N1 positions of cGMP as targets for modification in the design of novel CNG channel agonists.
(PMID: 17665892)
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: 22226
Target Type: UNCHECKED
Pref Name: Unchecked
Confidence: Default value - Target unknown or has yet to be assigned
Relationship Type: Default value - Target has yet to be curated
Categorized Comment - additional comments and annotations
From ChEMBL:
Assay Type: Binding
Assay Data Source: Scientific Literature
BAO: Assay Format: cell-based format
Assay Cell Type: HEK293
Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Activity activity commentActivity activity commentString
2Activity standard flagActivity standard flagInteger
3Activity qualifierActivity qualifierString
4Activity published valueActivity published valueFloat
5Activity standard valueActivity standard valueFloat
6K1/2 activity commentK1/2 activity commentString
7K1/2 standard flagK1/2 standard flagInteger
8K1/2 qualifierK1/2 qualifierString
9K1/2 published valueK1/2 published valueFloatμM
10K1/2 standard valueK1/2 standard valueFloatnM

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