SB 216763 [Ligand Id: 8015] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL102714 (SB-216763) |
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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 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] | ||||||||
| ChEMBL | Inhibition of CDK1 (unknown origin) | B | 6.26 | pIC50 | 550 | nM | IC50 | J Med Chem (2022) 65: 6356-6389 [PMID:35235745] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094127] [GtoPdb: 1961] [UniProtKB: O95067, P06493, P14635, Q8WWL7] | ||||||||
| 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: P20248, P24941, P78396] | ||||||||
| 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: P11802, P24385] | ||||||||
| 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] |
| ChEMBL | Inhibition of recombinant human GSK-3 alpha expressed in baculovirus infected Sf9 insect cells using GS-2 peptide after 30 mins in presence of [33P]gamma-ATP by microbeta scintillation counting analysis | B | 7.47 | pIC50 | 34 | nM | IC50 | J Med Chem (2016) 59: 1041-1051 [PMID:26751161] |
| 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 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 human GSK3-beta | B | 7.47 | pIC50 | 34 | nM | IC50 | Eur J Med Chem (2009) 44: 2361-2371 [PMID:18929433] |
| ChEMBL | Inhibition of GSK3-beta (unknown origin) | B | 7.47 | pIC50 | 34 | nM | IC50 | J Med Chem (2023) 66: 4231-4252 [PMID:36950863] |
| ChEMBL | Displacement of FL-KRREILSRRP[ps]ERYR-NH2 from human recombinant N-terminal His6-tagged GSK-3-beta (14 to 306 residues) H355L mutant expressed in baculovirus-infected Sf21 cells incubated for 20 hrs by fluorescence based analysis | B | 7.47 | pIC50 | 34 | nM | IC50 | J Med Chem (2023) 66: 7534-7552 [PMID:37235865] |
| 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 (636 to 661 residues) assessed as reduction in human muscle glycogen synthase type 1 fragment phosphorylation using YRRAAVPPSPSLSRHSSPHQ(pS)EDE as substrate in presence of ATP incubated for 60 mins by ADP-Glo kinase assay | B | 8.08 | pIC50 | 8.4 | nM | IC50 | Bioorg Med Chem Lett (2023) 87: 129283-129283 [PMID:37054760] |
| 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] |
| ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418] | ||||||||
| ChEMBL | Inhibition of RSK1 (unknown origin) | B | 7 | pIC50 | 100 | nM | IC50 | Eur J Med Chem (2023) 251: 115229-115229 [PMID:36898330] |
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]
