Synonyms: compound 13 [PMID:12656598] | SP4206 [3]
Compound class:
Synthetic organic
Comment: SP-4206 is a small molecule protein-protein interaction inhibitor. It binds IL-2 and prevents its interaction with the IL-2 receptor α [1-2]. The X-ray structure of SP-4206 bound to a dynamic hot spot on IL-2 is presented with PDB identifier 1PY2 [4].
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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References |
1. Arkin MR, Wells JA. (2004)
Small-molecule inhibitors of protein-protein interactions: progressing towards the dream. Nat Rev Drug Discov, 3 (4): 301-17. [PMID:15060526] |
2. Braisted AC, Oslob JD, Delano WL, Hyde J, McDowell RS, Waal N, Yu C, Arkin MR, Raimundo BC. (2003)
Discovery of a potent small molecule IL-2 inhibitor through fragment assembly. J Am Chem Soc, 125 (13): 3714-5. [PMID:12656598] |
3. Thanos CD, DeLano WL, Wells JA. (2006)
Hot-spot mimicry of a cytokine receptor by a small molecule. Proc Natl Acad Sci USA, 103 (42): 15422-7. [PMID:17032757] |
4. Thanos CD, Randal M, Wells JA. (2003)
Potent small-molecule binding to a dynamic hot spot on IL-2. J Am Chem Soc, 125 (50): 15280-1. [PMID:14664558] |