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ChEMBL ligand: CHEMBL322970 (SB-415286) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | 6.05 | 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: P20248, P24941, P78396] | ||||||||
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]