irigenol [Ligand Id: 11564] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1438439
  • RTP Type S/Receptor-type tyrosine-protein phosphatase S in Human [ChEMBL: CHEMBL2396508] [GtoPdb: 1866] [UniProtKB: Q13332]
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  • regulator of G-protein signaling 17/Regulator of G-protein signaling 17 in Human [ChEMBL: CHEMBL4295974] [GtoPdb: 2801] [UniProtKB: Q9UGC6]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
RTP Type S/Receptor-type tyrosine-protein phosphatase S in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2396508] [GtoPdb: 1866] [UniProtKB: Q13332]
ChEMBL Inhibition of recombinant human PTP-sigma (residues 1367 to 1948) using para-nitrophenylphosphate as substrate for 60 mins by fluorescence analysis B 6.3 pIC50 500 nM IC50 Bioorg Med Chem Lett (2016) 26: 87-93 [PMID:26602279]
regulator of G-protein signaling 17/Regulator of G-protein signaling 17 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295974] [GtoPdb: 2801] [UniProtKB: Q9UGC6]
ChEMBL Binding affinity to RGS17 (unknown origin) by ITC assay B 6.15 pKd 714 nM Kd US-20160264616-A1. Therapeutic compounds and methods (2016)
ChEMBL Inhibition of RGS17 (unknown origin) C117A mutant interaction with biotinylated Galphao after 30 mins in presence of AMF and GDP by AlphaScreen assay B 4.09 pIC50 81800 nM IC50 J Nat Prod (2017) 80: 1992-2000 [PMID:28621943]
ChEMBL Inhibition of wild type GST-tagged RGS17 (unknown origin) interaction with biotinylated Galphao after 30 mins in presence of AMF and GDP by AlphaScreen assay B 4.33 pIC50 47200 nM IC50 J Nat Prod (2017) 80: 1992-2000 [PMID:28621943]
GtoPdb - - 4.33 pIC50 47200 nM IC50 J Nat Prod (2017) 80: 1992-2000 [PMID:28621943]
ChEMBL Inhibition of RGS17 (unknown origin) in presence of and ATP Galpha-o by Malachite green steady-state GTPase assay B 4.45 pIC50 35510 nM IC50 US-20160264616-A1. Therapeutic compounds and methods (2016)
ChEMBL Inhibition of RGS17 (unknown origin) GAP activity in presence of GTP by malachite green dye based assay B 4.46 pIC50 35000 nM IC50 J Nat Prod (2017) 80: 1992-2000 [PMID:28621943]
ChEMBL Inhibition of RGS17 (unknown origin) assessed as reduction in RGS17 interaction with 6x-his-tagged biotinylated Galpha-o interaction by Alpha-screen assay B 6.37 pIC50 423.2 nM IC50 US-20160264616-A1. Therapeutic compounds and methods (2016)

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]