Ro31-8220 [Ligand Id: 5259] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL6291 (Ro-318220) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| chymotrypsinogen B1/Beta-chymotrypsin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4796] [GtoPdb: 3272] [UniProtKB: P17538] | ||||||||
| ChEMBL | Inhibitory activity against Chymotrypsinogen from Thermus flavus | B | 4.7 | pIC50 | 20000 | nM | IC50 | J Med Chem (2003) 46: 1478-1483 [PMID:12672248] |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
| ChEMBL | Inhibition of His-tagged human GSK3b expressed in Sf21 cells | B | 7.42 | pIC50 | 38 | nM | IC50 | Biochem J (2000) 351: 95-105 [PMID:10998351] |
| ChEMBL | Inhibition of GSK3-beta | B | 8.52 | pIC50 | 3 | nM | IC50 | Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249] |
| ChEMBL | Inhibition of human GSK3-beta | B | 8.55 | pIC50 | 2.8 | nM | IC50 | Eur J Med Chem (2009) 44: 2361-2371 [PMID:18929433] |
| ChEMBL | Inhibition of human GSK3-beta | B | 8.55 | pIC50 | 2.8 | nM | IC50 | Eur J Med Chem (2009) 44: 2361-2371 [PMID:18929433] |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3669] [GtoPdb: 2030] [UniProtKB: P18266] | ||||||||
| ChEMBL | Inhibition of Wistar rat GSK-3beta using RRAAEELDSRAGS(P)PQL as substrate after 15 mins in presence of [gamma-32P]-ATP by scintillation counting method | B | 8.17 | pIC50 | 6.8 | nM | IC50 | Bioorg Med Chem (2018) 26: 4209-4224 [PMID:30026041] |
| homeodomain interacting protein kinase 1/Homeodomain-interacting protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5427] [GtoPdb: 2033] [UniProtKB: Q86Z02] | ||||||||
| ChEMBL | Inhibition of human HIPK1 using MBP as substrate by [gamma-33P]-ATP assay | B | 6.21 | pIC50 | 621 | nM | IC50 | Eur J Med Chem (2019) 161: 456-467 [PMID:30384048] |
| Malate dehydrogenase in Thermus thermophilus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4255] [UniProtKB: P10584] | ||||||||
| ChEMBL | Inhibitory activity against malate dehydrogenase (MDH) from Thermus flavus | B | 4.35 | pIC50 | 45000 | nM | IC50 | J Med Chem (2003) 46: 1478-1483 [PMID:12672248] |
| mitogen-activated protein kinase kinase kinase 8/Mitogen-activated protein kinase kinase kinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4899] [GtoPdb: 2083] [UniProtKB: P41279] | ||||||||
| ChEMBL | Inhibition of human COT1 using MEK1 as substrate by [gamma-33P]-ATP assay | B | 5 | pIC50 | 9950 | nM | IC50 | Eur J Med Chem (2019) 161: 456-467 [PMID:30384048] |
| mitogen-activated protein kinase kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5749] [GtoPdb: 2085] [UniProtKB: Q92918] | ||||||||
| ChEMBL | Inhibition of human HPK1 using MBP as substrate by [gamma-33P]-ATP assay | B | 7.28 | pIC50 | 52.9 | nM | IC50 | Eur J Med Chem (2019) 161: 456-467 [PMID:30384048] |
| NAD-dependent deacetylase HST2 in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5933] [UniProtKB: P53686] | ||||||||
| ChEMBL | Inhibition of yeast Hst2 by fluorimetric assay | B | 4.7 | pIC50 | 20000 | nM | IC50 | Bioorg Med Chem (2009) 17: 7031-7041 [PMID:19734050] |
| sirtuin 1/NAD-dependent deacetylase sirtuin 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4506] [GtoPdb: 2707] [UniProtKB: Q96EB6] | ||||||||
| ChEMBL | Inhibition of human full length SIRT1 expressed in DE3 cells by fluorimetric assay | B | 4.6 | pIC50 | 25000 | nM | IC50 | Bioorg Med Chem (2009) 17: 7031-7041 [PMID:19734050] |
| ChEMBL | Inhibition of human SIRT1 by radioactive deacetylase assay | B | 5.29 | pIC50 | 5100 | nM | IC50 | J Med Chem (2006) 49: 7307-7316 [PMID:17149860] |
| ChEMBL | Inhibition of human SIRT1 | B | 5.46 | pIC50 | 3500 | nM | IC50 | J Med Chem (2006) 49: 7307-7316 [PMID:17149860] |
| ChEMBL | Inhibition of human SIRT1 by fluorescent deacetylase assay | B | 5.46 | pIC50 | 3500 | nM | IC50 | J Med Chem (2006) 49: 7307-7316 [PMID:17149860] |
| ChEMBL | Inhibition of human recombinant N-terminally GST-tagged Sirt1 expressed in Escherichia coli using ZMAL as substrate after 4 hrs by homogeneous fluorescent deacetylase assay | B | 5.46 | pIC50 | 3500 | nM | IC50 | Bioorg Med Chem (2011) 19: 3669-3677 [PMID:21315612] |
| sirtuin 2/NAD-dependent deacetylase sirtuin 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6] | ||||||||
| ChEMBL | Inhibition of human recombinant SIRT2 by radioactive deacetylase assay | B | 5.96 | pIC50 | 1100 | nM | IC50 | J Med Chem (2006) 49: 7307-7316 [PMID:17149860] |
| ChEMBL | Inhibition of human recombinant SIRT2 | B | 6.1 | pIC50 | 800 | nM | IC50 | J Med Chem (2006) 49: 7307-7316 [PMID:17149860] |
| ChEMBL | Inhibition of human recombinant SIRT2 by fluorescent deacetylase assay | B | 6.1 | pIC50 | 800 | nM | IC50 | J Med Chem (2006) 49: 7307-7316 [PMID:17149860] |
| ChEMBL | Inhibition of human N-terminally His6-tagged Sirt2 using ZMAL as substrate after 4 hrs by homogeneous fluorescent deacetylase assay | B | 6.1 | pIC50 | 800 | nM | IC50 | Bioorg Med Chem (2011) 19: 3669-3677 [PMID:21315612] |
| sirtuin 3/NAD-dependent deacetylase sirtuin 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4461] [GtoPdb: 2709] [UniProtKB: Q9NTG7] | ||||||||
| ChEMBL | Inhibition of human C-terminally His6-tagged Sirt3 using ZMAL as substrate after 4 hrs by homogeneous fluorescent deacetylase assay | B | 5.43 | pIC50 | 3700 | nM | IC50 | Bioorg Med Chem (2011) 19: 3669-3677 [PMID:21315612] |
| protein kinase C alpha/Protein kinase C alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252] | ||||||||
| ChEMBL | Inhibition of Protein kinase C alpha | B | 7.48 | pIC50 | 33 | nM | IC50 | J Med Chem (2003) 46: 1478-1483 [PMID:12672248] |
| ChEMBL | Inhibition of His-tagged human PKCalpha expressed in Escherichia coli | B | 7.48 | pIC50 | 33 | nM | IC50 | Biochem J (2000) 351: 95-105 [PMID:10998351] |
| ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443] | ||||||||
| ChEMBL | Inhibition of His-tagged human S6K1 expressed in Escherichia coli | B | 7.82 | pIC50 | 15 | nM | IC50 | Biochem J (2000) 351: 95-105 [PMID:10998351] |
| ribosomal protein S6 kinase A2/Ribosomal protein S6 kinase alpha 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3906] [GtoPdb: 1529] [UniProtKB: Q15349] | ||||||||
| ChEMBL | Inhibition of N-terminal His6 tagged full-length human recombinant active RSK2 using S6 peptide after 20 mins by fluorescence assay | B | 8 | pIC50 | 10 | nM | IC50 | Medchemcomm (2016) 7: 292-296 |
| ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812] | ||||||||
| ChEMBL | Inhibition of RSK2 after 60 mins | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2011) 54: 3564-3574 [PMID:21488662] |
| ribosomal protein S6 kinase A5/Ribosomal protein S6 kinase alpha 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4237] [GtoPdb: 1523] [UniProtKB: O75582] | ||||||||
| ChEMBL | Inhibition of His-tagged human MSK1 expressed in Sf9 cells | B | 8.1 | pIC50 | 8 | nM | IC50 | Biochem J (2000) 351: 95-105 [PMID:10998351] |
| serine/threonine kinase 10/Serine/threonine-protein kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3981] [GtoPdb: 2211] [UniProtKB: O94804] | ||||||||
| ChEMBL | Inhibition of STK10 (unknown origin) expressed in Sf9 cells assessed as transfer of radiolabelled phosphate group from ATP by reaction biology method | B | 7 | pIC50 | 99 | nM | IC50 | J Med Chem (2021) 64: 13259-13278 [PMID:34463505] |
| Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309] | ||||||||
| ChEMBL | Binding affinity to non phosphorylated PIM1 | B | 8.1 | pKd | 8 | nM | Kd | J Med Chem (2005) 48: 7604-7614 [PMID:16302800] |
| VRK serine/threonine kinase 1/Serine/threonine-protein kinase VRK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293199] [GtoPdb: 2275] [UniProtKB: Q99986] | ||||||||
| ChEMBL | Inhibition of human VRK1 using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK as substrate by [gamma-33P]-ATP assay | B | 6.13 | pIC50 | 743 | nM | IC50 | Eur J Med Chem (2019) 161: 456-467 [PMID:30384048] |
| VRK serine/threonine kinase 2/Serine/threonine-protein kinase VRK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1649059] [GtoPdb: 2276] [UniProtKB: Q86Y07] | ||||||||
| ChEMBL | Inhibition of human VRK2 using casein as substrate by [gamma-33P]-ATP assay | B | 4.79 | pIC50 | 16400 | nM | IC50 | Eur J Med Chem (2019) 161: 456-467 [PMID:30384048] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
