A series of 23 N-(Pyridin-3-yl)benzamides was synthesized and evaluated for their potential to inhibit human steroid-11##-hydroxylase (CYP11B1) and human aldosterone synthase (CYP11B2). The most potent and selective CYP11B2 inhibitors (IC(50) values 53-166 nM) were further evaluated for their potential to inhibit human CYP17 and CYP19, and no inhibition was observed. Clear evidence was shown for N-(Pyridin-3-yl)benzamides to be a highly selective class of CYP11B2 inhibitors in vitro. ..more
Related BioAssays
Related BioAssays
Target
| Sequence: RecName: Full=Cytochrome P450 19A1; AltName: Full=Aromatase; AltName: Full=CYPXIX; AltName: Full=Cytochrome P-450AROM; AltName: Full=Estrogen synthase Description ..   Protein Family: Cytochrome P450 Comment .. Gene:CYP19A1 Related Protein 3D Structures |
BioActive Compound: 1
Description:
Title: N-(Pyridin-3-yl)benzamides as selective inhibitors of human aldosterone synthase (CYP11B2).
Abstract: A series of 23 N-(Pyridin-3-yl)benzamides was synthesized and evaluated for their potential to inhibit human steroid-11##-hydroxylase (CYP11B1) and human aldosterone synthase (CYP11B2). The most potent and selective CYP11B2 inhibitors (IC(50) values 53-166 nM) were further evaluated for their potential to inhibit human CYP17 and CYP19, and no inhibition was observed. Clear evidence was shown for N-(Pyridin-3-yl)benzamides to be a highly selective class of CYP11B2 inhibitors in vitro.
(PMID: 21129965)
Abstract: A series of 23 N-(Pyridin-3-yl)benzamides was synthesized and evaluated for their potential to inhibit human steroid-11##-hydroxylase (CYP11B1) and human aldosterone synthase (CYP11B2). The most potent and selective CYP11B2 inhibitors (IC(50) values 53-166 nM) were further evaluated for their potential to inhibit human CYP17 and CYP19, and no inhibition was observed. Clear evidence was shown for N-(Pyridin-3-yl)benzamides to be a highly selective class of CYP11B2 inhibitors in vitro.
(PMID: 21129965)
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: 65
ChEMBL target type: Target is a single protein chain
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Target ID: 65
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 | IC50* | IC50 PubChem standard value |  | Float | μM | |
| 2 | BEI | Binding Efficiency Index(nM) | | Float | ||
| 3 | SEI | Surface Efficiency Index(nM) | | Float | ||
| 4 | IC50 activity comment | IC50 activity comment | String | |||
| 5 | IC50 standard flag | IC50 standard flag | | Integer | ||
| 6 | IC50 qualifier | IC50 qualifier | String | |||
| 7 | IC50 published value | IC50 published value | | Float | nM | |
| 8 | IC50 standard value | IC50 standard value | | Float | nM | |
| 9 | IC50 binding domains | IC50 binding domains | String |
* Activity Concentration.
Data Table (Concise)
Classification
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