Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL322970 (SB-415286) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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: 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 | Inhibition of GSK-3beta (unknown origin) | B | 7.47 | pIC50 | 34 | nM | IC50 | J Med Chem (2021) 64: 26-41 [PMID:33346659] |
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 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]