In the course of a high throughput screening, a series of pyrazole compounds were identified with luteinizing hormone receptor (LH-R) agonist activity. A focused pyrazole library was produced by solid-phase synthesis and key pyrazole regioisomers were obtained selectively in solution. Evaluation of those compounds in a cAMP assay in CHO cells transfected with h-LH receptor allowed us to propose a more ..
Related BioAssays
Related BioAssays
Target
BioActive Compound: 1
Description:
Title: Identification, synthesis, and biological evaluation of novel pyrazoles as low molecular weight luteinizing hormone receptor agonists.
Abstract: In the course of a high throughput screening, a series of pyrazole compounds were identified with luteinizing hormone receptor (LH-R) agonist activity. A focused pyrazole library was produced by solid-phase synthesis and key pyrazole regioisomers were obtained selectively in solution. Evaluation of those compounds in a cAMP assay in CHO cells transfected with h-LH receptor allowed us to propose a structure-activity relationship model for this series and led to the identification of the first low molecular weight molecule with in vitro activity in a Leydig cells assay (ED(50)=1.31 microM) and in vivo in a model of testosterone induction in rats (significant effect at 32 mpk ip).
(PMID: 17321742)
Abstract: In the course of a high throughput screening, a series of pyrazole compounds were identified with luteinizing hormone receptor (LH-R) agonist activity. A focused pyrazole library was produced by solid-phase synthesis and key pyrazole regioisomers were obtained selectively in solution. Evaluation of those compounds in a cAMP assay in CHO cells transfected with h-LH receptor allowed us to propose a structure-activity relationship model for this series and led to the identification of the first low molecular weight molecule with in vitro activity in a Leydig cells assay (ED(50)=1.31 microM) and in vivo in a model of testosterone induction in rats (significant effect at 32 mpk ip).
(PMID: 17321742)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
Categorized Comment
ChEMBL Assay Type: Binding
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Target ID: 10956
ChEMBL target type: Target is a single protein chain
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Target ID: 10956
ChEMBL target type: Target is a single protein chain
Result Definitions
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| TID | Name | Description | Histogram | Type | Unit | |
|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||
| 1 | ED50* | ED50 PubChem standard value |  | Float | μM | |
| 2 | ED50 activity comment | ED50 activity comment | String | |||
| 3 | ED50 standard flag | ED50 standard flag | | Integer | ||
| 4 | ED50 qualifier | ED50 qualifier | String | |||
| 5 | ED50 published value | ED50 published value | | Float | nM | |
| 6 | ED50 standard value | ED50 standard value | | Float | nM | |
| 7 | Efficacy activity comment | Efficacy activity comment | String | |||
| 8 | Efficacy standard flag | Efficacy standard flag | | Integer | ||
| 9 | Efficacy qualifier | Efficacy qualifier | String | |||
| 10 | Efficacy published value | Efficacy published value | | Float | % | |
| 11 | Efficacy standard value | Efficacy standard value | | Float | % |
* Activity Concentration.
Data Table (Concise)
Classification
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