We previously disclosed tricylic, 6-carboxylic acid-bearing 4-quinolones as GSK-3## inhibitors. Herein we discuss the optimization of this series to yield a series of more potent 6-nitrile analogs with insignificant anti-microbial activity. Finally, kinase profiling indicated that members of this class were highly specific GSK-3 inhibitors. ..more
Tested Compounds:
Description:
Title: 6-Position optimization of tricyclic 4-quinolone-based inhibitors of glycogen synthase kinase-3##: discovery of nitrile derivatives with picomolar potency.
Abstract: We previously disclosed tricylic, 6-carboxylic acid-bearing 4-quinolones as GSK-3## inhibitors. Herein we discuss the optimization of this series to yield a series of more potent 6-nitrile analogs with insignificant anti-microbial activity. Finally, kinase profiling indicated that members of this class were highly specific GSK-3 inhibitors.
(PMID: 22202172)
Abstract: We previously disclosed tricylic, 6-carboxylic acid-bearing 4-quinolones as GSK-3## inhibitors. Herein we discuss the optimization of this series to yield a series of more potent 6-nitrile analogs with insignificant anti-microbial activity. Finally, kinase profiling indicated that members of this class were highly specific GSK-3 inhibitors.
(PMID: 22202172)
Comment
Putative Target:
ChEMBL Target ID: 22226
Target Type: UNCHECKED
Pref Name: Unchecked
Confidence: Multiple direct protein targets may be assigned
Relationship Type: Direct protein target assigned
ChEMBL Target ID: 22226
Target Type: UNCHECKED
Pref Name: Unchecked
Confidence: Multiple direct protein targets may be assigned
Relationship Type: Direct protein target assigned
Categorized Comment
ChEMBL Assay Type: Binding
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Target ID: 22226
ChEMBL target type: NULL
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Target ID: 22226
ChEMBL target type: NULL
Result Definitions
| TID | Name | Description | Histogram | Type | Unit | |
|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||
| 1 | Inhibition activity comment | Inhibition activity comment | String | |||
| 2 | Inhibition standard flag | Inhibition standard flag |  | Integer | ||
| 3 | Inhibition qualifier | Inhibition qualifier | String | |||
| 4 | Inhibition published value | Inhibition published value | | Float | % | |
| 5 | Inhibition standard value | Inhibition standard value | | Float | % |
Data Table (Concise)
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