Synonyms: ASTX-660 | ASTX660 | compound 27 [PMID: 30091600]
Compound class:
Synthetic organic
Comment: Tolinapant (ASTX660) is a non-peptidomimetic inhibitor of cIAP1/2 and XIAP, that was discovered using fragment-based drug design [1,5]. It is a Smac mimetic that induces TNFα-mediated necroptosis (inflammatory cell death) in cancer cells [4]. ASTX660 was designed for anticancer potential, and is active in in vitro and in vivo cancer models [2].
![]() 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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Classification ![]() |
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Compound class | Synthetic organic |
IUPAC Name ![]() |
1-[6-[(4-fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-2H-pyrrolo[3,2-b]pyridin-1-yl]-2-[(2R,5R)-5-methyl-2-[[(3R)-3-methylmorpholin-4-yl]methyl]piperazin-1-yl]ethanone |
International Nonproprietary Names ![]() |
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INN number | INN |
11623 | tolinapant |
Synonyms ![]() |
ASTX-660 | ASTX660 | compound 27 [PMID: 30091600] |
Database Links ![]() |
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BindingDB Ligand | 50450046 |
CAS Registry No. | 1799328-86-1 (source: WHO INN record) |
ChEMBL Ligand | CHEMBL4173974 |
GtoPdb PubChem SID | 483123252 |
PubChem CID | 118169620 |
Search Google for chemical match using the InChIKey | YCXOHEXZVKOGEV-DNRQZRRGSA-N |
Search Google for chemicals with the same backbone | YCXOHEXZVKOGEV |
Search PubMed clinical trials | tolinapant |
Search PubMed titles | tolinapant |
Search PubMed titles/abstracts | tolinapant |
UniChem Compound Search for chemical match using the InChIKey | YCXOHEXZVKOGEV-DNRQZRRGSA-N |
UniChem Connectivity Search for chemical match using the InChIKey | YCXOHEXZVKOGEV-DNRQZRRGSA-N |