Synonyms: BMS-794833 | BMS794833
Compound class:
Synthetic organic
Comment: Metatinib (BMS794833) is a MET, VEGFR2, and MER tyrosine kinase inhibitor [1]. The crystal structure of MER/BMS794833 has resolved its binding mode. The compound simultaneously occupies MER's ATP-binding pocket and its allosteric back pocket, and it inhibits MER TK activity in an ATP competitive manner. BMS817378 is a prodrug of BMS794833, and is the code used in clinical trials.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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No information available. |
Summary of Clinical Use |
The BMS794833 prodrug, BMS817378, has entered early stage clinical evaluation, to determine potential anti-tumour efficacy. |
Clinical Trials | |||||
Clinical Trial ID | Title | Type | Source | Comment | References |
NCT00792558 | Ascending Multiple-Dose Study of BMS-817378 in Subjects With Advanced Cancers | Phase 1 Interventional | Bristol-Myers Squibb | Note that the active metabolite of BMS817378 is BMS794833. |