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thalidomide is an approved drug (FDA (1998), EMA (2008))
Compound class: Synthetic organic
Comment: Thalidomide is principally an immunomodulatory drug. It inhibits synthesis of TNFα. Mechanistically, thalidomide binds to cereblon, and this complex recruits substrate proteins for degradation by the ubiquitin system. The lymphoid transcription factors Ikaros (IKZF1) and Aiolos (IKZF3) have been identified as substrates for thalidomide-bound cereblon. More recently another transcription factor, PLZF (ZBTB16), has been reported as a potential thalidomide/cereblon substrate . Knockdown of Plfz induces skeletal abnormalities in chicken limbs, so thalidomide-targeted degradation of PLZF would be predicted to exhibit similar teratogenic effects.
SARS-CoV-2 and COVID-19: Thalidomide + low-dose glucocorticoid is being evaluated for efficacy in severe COVID-19 pneumonia (preprint available here https://www.preprints.org/manuscript/202002.0395/v1). An alternative approach is examining the combination of thalidomide + celecoxib (which targets NF-κB to suppress production of inflammatory cytokines; see preprint DOI: 10.13140/RG.2.2.26979.91689).
Ligand Activity Visualisation Charts
These 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.✖
|Compound class||Synthetic organic|
|Ligand families/groups||PROTACs, molecular glues and other degraders|
|Approved drug?||Yes (FDA (1998), EMA (2008))|
|WHO Essential Medicine||WHO Essential Medicines List (EML) (22nd List, 2021). Access PDF version.
Click to view more information about the WHO Model Lists of Essential Medicines.
|International Nonproprietary Names|
|CAS Registry No.||50-35-1|
|GtoPdb PubChem SID||178103899|
|Search Google for chemical match using the InChIKey||UEJJHQNACJXSKW-UHFFFAOYSA-N|
|Search Google for chemicals with the same backbone||UEJJHQNACJXSKW|
|Search PubMed clinical trials||thalidomide|
|Search PubMed titles||thalidomide|
|Search PubMed titles/abstracts||thalidomide|
|UniChem Compound Search for chemical match using the InChIKey||UEJJHQNACJXSKW-UHFFFAOYSA-N|
|UniChem Connectivity Search for chemical match using the InChIKey||UEJJHQNACJXSKW-UHFFFAOYSA-N|
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Cat. No. 0652