bisindolylmaleimide IV [Ligand Id: 5937] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL266487 (Ro-31-6233)
  • calcium/calmodulin-dependent protein kinase II delta subunit/CaM kinase II delta in Human [ChEMBL: CHEMBL2801] [GtoPdb: 1558] [UniProtKB: Q13557]
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  • protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase alpha-catalytic subunit in Rat [ChEMBL: CHEMBL3390] [GtoPdb: 1476] [UniProtKB: P27791]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • sirtuin 2/NAD-dependent deacetylase sirtuin 2 in Human [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6]
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  • protein kinase C alpha/Protein kinase C alpha in Human [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
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  • protein kinase C beta/Protein kinase C beta in Human [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
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  • protein kinase C epsilon/Protein kinase C epsilon in Human [ChEMBL: CHEMBL3582] [GtoPdb: 1486] [UniProtKB: Q02156]
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  • protein kinase C gamma/Protein kinase C gamma in Rat [ChEMBL: CHEMBL3604] [GtoPdb: 1484] [UniProtKB: P63319]
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  • Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
calcium/calmodulin-dependent protein kinase II delta subunit/CaM kinase II delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2801] [GtoPdb: 1558] [UniProtKB: Q13557]
ChEMBL Inhibition of CaMK2delta B 5.92 pIC50 1190 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 2395-2398 [PMID:18334295]
protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase alpha-catalytic subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3390] [GtoPdb: 1476] [UniProtKB: P27791]
ChEMBL Inhibition of rat brain protein kinase A(PKA) in 10%DMSO B 4.93 pIC50 11800 nM IC50 J. Med. Chem. (1992) 35: 177-184 [PMID:1732526]
ChEMBL Inhibition of rat brain protein kinase A(PKA) in 1%DMSO B 5.51 pIC50 3100 nM IC50 J. Med. Chem. (1992) 35: 177-184 [PMID:1732526]
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094127] [GtoPdb: 1961] [UniProtKB: O95067P06493P14635Q8WWL7]
ChEMBL Inhibitory concentration was determined by measuring phosphorylation of H1 histone using active human Cell division cycle 2-cyclin B complex B 4.74 pIC50 18000 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 1019-1022 [PMID:9871700]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094126] [GtoPdb: 1973] [UniProtKB: O96020P24864P24941]
ChEMBL Inhibitory activity against Cyclin E-cyclin-dependent kinase 2 by measuring phosphorylation of RbING substrate B 4.93 pIC50 11690 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 3841-3846 [PMID:14552792]
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802P24385]
ChEMBL Inhibitory activity against Cyclin D1-cyclin-dependent kinase 4 by measuring phosphorylation of RbING substrate B 5.24 pIC50 5810 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 3841-3846 [PMID:14552792]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibitory activity against recombinant tyrosine kinase EGF-R (EGF-R ICD) B 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (1994) 37: 1015-1027 [PMID:8151612]
sirtuin 2/NAD-dependent deacetylase sirtuin 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6]
ChEMBL Inhibition of human recombinant SIRT2 B 5.33 pIC50 4700 nM IC50 J. Med. Chem. (2006) 49: 7307-7316 [PMID:17149860]
protein kinase C alpha/Protein kinase C alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
ChEMBL Inhibitory concentration against recombinant human Protein kinase C alpha B 5.8 pIC50 1599 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 5171-5174 [PMID:15380221]
protein kinase C beta/Protein kinase C beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
ChEMBL Inhibitory concentration against recombinant human Protein kinase C beta 1 B 6.52 pIC50 304 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 5171-5174 [PMID:15380221]
GtoPdb PKCβ2 isoform - 6.67 pIC50 212 nM IC50 Bioorg Med Chem Lett (2004) 14: 5171-4 [PMID:15380221]
ChEMBL Inhibitory concentration against recombinant human Protein kinase C beta 2 B 6.67 pIC50 212 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 5171-5174 [PMID:15380221]
protein kinase C epsilon/Protein kinase C epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3582] [GtoPdb: 1486] [UniProtKB: Q02156]
ChEMBL Inhibitory concentration against recombinant human Protein kinase C epsilon B 5.12 pIC50 7516 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 5171-5174 [PMID:15380221]
protein kinase C gamma/Protein kinase C gamma in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3604] [GtoPdb: 1484] [UniProtKB: P63319]
ChEMBL Inhibition of rat brain protein kinase C (PKC) with ATP and histone as substrates B 6.26 pIC50 550 nM IC50 J. Med. Chem. (1992) 35: 177-184 [PMID:1732526]
Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
ChEMBL Binding affinity to non phosphorylated PIM1 B 7.57 pKd 27 nM Kd J. Med. Chem. (2005) 48: 7604-7614 [PMID:16302800]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]