Fourteen new 9,10-secosteroids designated as astrogorgols A-N (1-14) were isolated from a Chinese gorgonian Astrogorgia sp. together with eight known analogues. The structural patterns were characterized by the presence of a sterol-based 9,10-seco nucleus containing a 3-hydroxy-10-methylphenyl ring. Astrogorgol N (14) possessing a 1,4-dien-3-one unit in ring A was biogenetically considered as an more ..
Target
| Sequence: RecName: Full=Tyrosine-protein kinase receptor UFO; AltName: Full=AXL oncogene; Flags: Precursor Description ..   Protein Family: Catalytic domain of the Protein Tyrosine Kinase, Axl Comment .. Gene:AXL Related Protein 3D Structures |
BioActive Compounds: 5
Description:
Title: 9,10-secosteroids, protein kinase inhibitors from the Chinese gorgonian Astrogorgia sp.
Abstract: Fourteen new 9,10-secosteroids designated as astrogorgols A-N (1-14) were isolated from a Chinese gorgonian Astrogorgia sp. together with eight known analogues. The structural patterns were characterized by the presence of a sterol-based 9,10-seco nucleus containing a 3-hydroxy-10-methylphenyl ring. Astrogorgol N (14) possessing a 1,4-dien-3-one unit in ring A was biogenetically considered as an intermediate to generate diverse 9,10-secosteroids. Five compounds showed significant inhibitory activities against human tumor related protein kinases, including ALK, AXL, FAK, IGF-1R, MET wt, SRC, and VEGF-R2.
(PMID: 21982797)
Abstract: Fourteen new 9,10-secosteroids designated as astrogorgols A-N (1-14) were isolated from a Chinese gorgonian Astrogorgia sp. together with eight known analogues. The structural patterns were characterized by the presence of a sterol-based 9,10-seco nucleus containing a 3-hydroxy-10-methylphenyl ring. Astrogorgol N (14) possessing a 1,4-dien-3-one unit in ring A was biogenetically considered as an intermediate to generate diverse 9,10-secosteroids. Five compounds showed significant inhibitory activities against human tumor related protein kinases, including ALK, AXL, FAK, IGF-1R, MET wt, SRC, and VEGF-R2.
(PMID: 21982797)
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: 100410
ChEMBL target type: Target is a single protein chain
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Target ID: 100410
ChEMBL target type: Target is a single protein chain
Result Definitions
| 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 |
* Activity Concentration.
Data Table (Concise)
Classification
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