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Compound class: Synthetic organic
Comment: Indisulam is an anticancer sulfonamide that is in clinical development. This compound belongs to the family of carbonic anhydrase inhibitors. It also behaves as a type of molecular glue that targets certain proteins for ubiquitination and proteasomal degradation [1,3], by bringing them into the proximity the CUL4-DDB1-DDA1-DCAF15 E3 ubiquitin ligase complex.
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.✖
1. Han T, Goralski M, Gaskill N, Capota E, Kim J, Ting TC, Xie Y, Williams NS, Nijhawan D. (2017)
Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15.
Science, 356 (6336). [PMID:28302793]
2. Sethi KK, Vullo D, Verma SM, Tanç M, Carta F, Supuran CT. (2013)
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
Bioorg Med Chem, 21 (19): 5973-82. [PMID:23965175]
3. Uehara T, Minoshima Y, Sagane K, Sugi NH, Mitsuhashi KO, Yamamoto N, Kamiyama H, Takahashi K, Kotake Y, Uesugi M et al.. (2017)
Selective degradation of splicing factor CAPERα by anticancer sulfonamides.
Nat Chem Biol, 13 (6): 675-680. [PMID:28437394]