SB-415286 [Ligand Id: 8019] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL322970 (SB-415286)
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  • glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840]
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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094127] [GtoPdb: 1961] [UniProtKB: O95067P06493P14635Q8WWL7]
ChEMBL Inhibition of CDK1/cyclinB B 6.05 pIC50 900 nM IC50 Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248P24941P78396]
ChEMBL Inhibition of Cyclin-dependent kinase 2-cyclin A B 6.42 pIC50 380 nM IC50 J Med Chem (2003) 46: 3333-3341 [PMID:12852764]
glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840]
ChEMBL Inhibitory concentration was determined against human glycogen synthase kinase-3 alpha B 6.98 pIC50 104 nM IC50 Bioorg Med Chem Lett (2001) 11: 635-639 [PMID:11266159]
ChEMBL Inhibition of GSK3alpha B 7.11 pIC50 78 nM IC50 Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249]
GtoPdb - - 7.42 pIC50 38 nM IC50 Chem Biol (2000) 7: 793-803 [PMID:11033082]
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 GSK3-beta assessed as NADH level after 10 mins by pyruvate kinase/lactate dehydrogenase coupled spectrophotometric assay B 7.62 pKi 24 nM Ki Bioorg Med Chem Lett (2010) 20: 1661-1664 [PMID:20138514]
ChEMBL Inhibitory activity against human glycogen synthase kinase-3beta (GSK3-beta) at 100 uM ATP B 6.42 pIC50 380 nM IC50 J Med Chem (2003) 46: 3333-3341 [PMID:12852764]
ChEMBL Inhibition of recombinant GSK3-beta B 6.98 pIC50 104 nM IC50 J Med Chem (2008) 51: 2062-2077 [PMID:18324764]
ChEMBL Inhibition of GSK3-beta by luminescent assay B 7.05 pIC50 90 nM IC50 J Nat Prod (2011) 74: 99-101 [PMID:21126094]
ChEMBL Inhibition of human GSK3-beta B 7.11 pIC50 78 nM IC50 Eur J Med Chem (2009) 44: 2361-2371 [PMID:18929433]
ChEMBL Inhibition of human recombinant GSK3-beta assessed as [gamma33]ATP transfer to biotinylated CREB-peptide substrate after 1 hr by scintillation counting B 7.11 pIC50 77 nM IC50 Bioorg Med Chem Lett (2010) 20: 1693-1696 [PMID:20138512]
ChEMBL Inhibition of human full length GSK3beta expressed in baculovirus in Sf9 insect cells using YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE as substrate by ADP-Glo kinase assay B 7.27 pIC50 54 nM IC50 Eur J Med Chem (2021) 222: 113554-113554 [PMID:34098466]
ChEMBL Inhibition of human recombinant GSK3beta using GSM as substrate incubated for 30 mins by luminescence based assay B 7.3 pIC50 50 nM IC50 ACS Med Chem Lett (2019) 10: 469-474 [PMID:30996781]
GtoPdb - - 7.42 pIC50 ~38 nM IC50 Chem Biol (2000) 7: 793-803 [PMID:11033082]
ChEMBL Stimulation of glycogen synthase in CHO cells expressing human insulin receptor F 4.34 pEC50 45600 nM EC50 J Med Chem (2003) 46: 3333-3341 [PMID:12852764]
ChEMBL Induced beta-casein protein expression in the CHO-hIR cell line F 4.51 pEC50 30620 nM EC50 J Med Chem (2003) 46: 3333-3341 [PMID:12852764]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 6.3 pIC50 501.19 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]

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]