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ChEMBL ligand: CHEMBL336961 (Azakenpaullone) |
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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 human cyclin-dependent kinase 1-cyclin B | B | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 413-416 [PMID:14698171] |
ChEMBL | Inhibition of CDK1/cyclinB | B | 5.7 | pIC50 | 2000 | nM | IC50 | Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249] |
ChEMBL | Inhibition of CDK1/Cyclin B (unknown origin) in presence of gamma32P-ATP by scintillation counter analysis | B | 5.7 | pIC50 | 2000 | nM | IC50 | Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899] |
GtoPdb | CDK1/cyclin B complex in assay | - | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 413-6 [PMID:14698171] |
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635] | ||||||||
ChEMBL | Inhibition of GST-tagged CDK1/cyclin B (unknown origin) expressed in Escherichia coli | B | 5.7 | pIC50 | 2000 | nM | IC50 | Eur J Med Chem (2017) 142: 244-265 [PMID:28803677] |
GtoPdb | CDK1/cyclin B complex in assay | - | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 413-6 [PMID:14698171] |
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 CDK2/Cyclin A (unknown origin) | B | 5.7 | pIC50 | 2000 | nM | IC50 | Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899] |
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078] | ||||||||
ChEMBL | Inhibition of human Cyclin-dependent kinase 5-p35nck5a | B | 5.38 | pIC50 | 4200 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 413-416 [PMID:14698171] |
ChEMBL | Inhibition of recombinant CDK5/p25 expressed in Escherichia coli | B | 5.38 | pIC50 | 4200 | nM | IC50 | J Med Chem (2008) 51: 2196-2207 [PMID:18345612] |
ChEMBL | Inhibition of CDK5/p25 (unknown origin) | B | 5.38 | pIC50 | 4200 | nM | IC50 | Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899] |
GtoPdb | CDK5/p25 complex in assay | - | 5.38 | pIC50 | 4200 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 413-6 [PMID:14698171] |
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
ChEMBL | Binding affinity to human C-terminal his tagged GSK3beta (26 to 383 residues) expressed in Escherichia coli at 50 uM by radiometric analysis | B | 7.46 | pKd | 34.9 | nM | Kd | J Med Chem (2023) 66: 4009-4024 [PMID:36883902] |
ChEMBL | Inhibition of human C-terminal his tagged GSK3beta (26 to 383 residues) expressed in Escherichia coli using GYSI(YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE) as peptide substrate incubated for 1 hr in presence of ATP by cook activity assay | B | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2023) 66: 4009-4024 [PMID:36883902] |
GtoPdb | - | - | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 413-6 [PMID:14698171] |
ChEMBL | Inhibition of human glycogen synthase kinase-3 beta | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 413-416 [PMID:14698171] |
ChEMBL | Inhibition of GSK3-beta | B | 7.74 | pIC50 | 18 | nM | IC50 | Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249] |
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3669] [GtoPdb: 2030] [UniProtKB: P18266] | ||||||||
ChEMBL | Inhibition of rat GSK3beta expressed in Sf9 cells incubated for 30 mins using GS-1 peptide substrate and [gamma-32P]ATP by scintillation counting method | B | 7.74 | pIC50 | 18 | nM | IC50 | Eur J Med Chem (2017) 142: 244-265 [PMID:28803677] |
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]