SB 216763 [Ligand Id: 8015] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL102714 (SB-216763)
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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 6.26 pIC50 550 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 human CDK2/Cyclin A by ELISA B 6.57 pIC50 269 nM IC50 J Med Chem (2010) 53: 994-1003 [PMID:20030405]
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802P24385]
ChEMBL Inhibition of human CDK4/cyclin D1 by ELISA B 4.49 pIC50 32000 nM IC50 J Med Chem (2010) 53: 994-1003 [PMID:20030405]
glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840]
ChEMBL Inhibition of GSK3alpha B 7.47 pIC50 34 nM IC50 Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249]
GtoPdb - - 8.05 pIC50 9 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 after 30 mins by luminescence assay B 7.04 pIC50 92 nM IC50 Bioorg Med Chem (2010) 18: 6785-6795 [PMID:20708937]
ChEMBL Competitive inhibition of human recombinant full length GSK3beta using YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE as substrate preincubated with enzyme for 10 mins followed by substrate and 25 uM ATP addition measured after 60 mins by ADP-Glo luminescence assay B 7.05 pIC50 89 nM IC50 Eur J Med Chem (2019) 175: 309-329 [PMID:31096153]
ChEMBL Inhibition of human GSK3-beta by scintillation counting B 7.3 pIC50 50 nM IC50 J Med Chem (2009) 52: 1853-1863 [PMID:19338355]
ChEMBL Inhibition of human recombinant GSK3-beta B 7.32 pIC50 48 nM IC50 J Med Chem (2010) 53: 994-1003 [PMID:20030405]
ChEMBL Inhibition of human GSK3-beta B 7.47 pIC50 34 nM IC50 Eur J Med Chem (2009) 44: 2361-2371 [PMID:18929433]
ChEMBL Inhibition of GSK3beta (unknown origin) B 7.47 pIC50 34 nM IC50 Eur J Med Chem (2021) 210: 112949-112949 [PMID:33097303]
ChEMBL Inhibition of GSK3beta (unknown origin) B 7.47 pIC50 34 nM IC50 Eur J Med Chem (2017) 125: 464-477 [PMID:27689729]
ChEMBL Inhibition of GSK3beta (unknown origin) expressed in Sf9 cells using GS1 as substrate and [gamma32]ATP after 30 min by scinitllation counting B 7.47 pIC50 33.88 nM IC50 Med Chem Res (2007) 16: 461-467
ChEMBL Inhibition of human recombinant N-terminal His-tagged GSK3beta expressed in Escherichia coli using RRRPASVPPSPSLS RHS(pS)HQRR as substrate incubated for 30 mins in presence of ATP by Kinase-Glo reagent based luminescence assay B 7.54 pIC50 29 nM IC50 Eur J Med Chem (2021) 223: 113663-113663 [PMID:34198150]
ChEMBL Inhibition of recombinant human N-terminal His6-tagged GSK3beta H350L mutant expressed in baculovirus infected Sf21 cells using prephosphorylated polypeptide as substrate incubated for 1 min followed by substrate addition and measured after 30 mins by Kinase-Glo luminescence assay B 7.7 pIC50 20 nM IC50 Bioorg Med Chem (2021) 30: 115940-115940 [PMID:33340937]
ChEMBL Inhibition of recombinant human N-terminal His6-tagged GSK-3beta H350L mutant expressed in baculovirus infected Sf21 cells using GSM as substrate incubated for 30 mins in presence of ATP by kinase-glo luminescence assay B 7.7 pIC50 19.8 nM IC50 Eur J Med Chem (2020) 207: 112751-112751 [PMID:32950908]
ChEMBL Inhibition of GSK3beta (unknown origin) pre-incubated for 30 mins followed by ULight-GS (Ser641/pSer657) peptide substrate addition and measured after 1 hr by TR-FRET assay B 7.94 pIC50 11.4 nM IC50 J Med Chem (2018) 61: 7640-7656 [PMID:30078314]
ChEMBL Inhibition of GSK3beta (unknown origin) pre-incubated for 30 mins followed by ULight-GS (Ser641/pSer657) peptide substrate addition and measured after 1 hr by TR-FRET assay B 7.94 pIC50 11.4 nM IC50 Eur J Med Chem (2019) 163: 394-402 [PMID:30530190]
ChEMBL Inhibition of GSK3beta (unknown origin) B 8.05 pIC50 9 nM IC50 Bioorg Med Chem Lett (2014) 24: 1532-1537 [PMID:24560539]
ChEMBL Inhibition of GSK3beta B 8.05 pIC50 9 nM IC50 J Med Chem (2012) 55: 9107-9119 [PMID:22489897]
GtoPdb - - 8.05 pIC50 ~9 nM IC50 Chem Biol (2000) 7: 793-803 [PMID:11033082]
ChEMBL Inhibition of recombinant human GSK3beta using YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE as substrate measured after 60 mins by ADP-Glo luminescence assay B 8.08 pIC50 8.35 nM IC50 Bioorg Med Chem (2019) 27: 1804-1817 [PMID:30902399]
ChEMBL Inhibition of Glycogen synthase kinase-3 beta B 8.15 pIC50 7 nM IC50 Bioorg Med Chem Lett (2003) 13: 3049-3053 [PMID:12941331]
ChEMBL Effective concentration of compound against glycogen synthase kinase-3 in HEK293 cells F 6.7 pEC50 200 nM EC50 Bioorg Med Chem Lett (2004) 14: 3245-3250 [PMID:15149684]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 4.8 pIC50 15848.93 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 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 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 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 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]