BIX 02565 [Ligand Id: 8039] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1933288
  • CDC like kinase 2/Dual specificity protein kinase CLK2 in Human [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760]
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  • CDC like kinase 1/Dual specificty protein kinase CLK1 in Human [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
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  • fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802]
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  • leucine rich repeat kinase 2/Leucine-rich repeat serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL1075104] [GtoPdb: 2059] [UniProtKB: Q5S007]
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  • platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
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  • protein kinase D1/Protein kinase C mu in Human [ChEMBL: CHEMBL3863] [GtoPdb: 1489] [UniProtKB: Q15139]
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  • protein kinase D3/Protein kinase C nu in Human [ChEMBL: CHEMBL2595] [GtoPdb: 2174] [UniProtKB: O94806]
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  • ribosomal protein S6 kinase A2/Ribosomal protein S6 kinase alpha 2 in Human [ChEMBL: CHEMBL3906] [GtoPdb: 1529] [UniProtKB: Q15349]
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  • ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha 3 in Human [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812]
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  • protein kinase D2/Serine/threonine-protein kinase D2 in Human [ChEMBL: CHEMBL4900] [GtoPdb: 2173] [UniProtKB: Q9BZL6]
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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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  • ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CDC like kinase 2/Dual specificity protein kinase CLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760]
ChEMBL Inhibition of human CLK2 B 6.95 pIC50 112 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 738-742 [PMID:22056746]
CDC like kinase 1/Dual specificty protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
ChEMBL Inhibition of human CLK1 B 6.29 pIC50 512 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 738-742 [PMID:22056746]
fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802]
ChEMBL Inhibition of human FGFR2 B 6.49 pIC50 320 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 738-742 [PMID:22056746]
leucine rich repeat kinase 2/Leucine-rich repeat serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075104] [GtoPdb: 2059] [UniProtKB: Q5S007]
ChEMBL Inhibition of human LRRK2 B 7.8 pIC50 16 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 738-742 [PMID:22056746]
platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
ChEMBL Inhibition of human PDGFRa B 6.02 pIC50 956 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 738-742 [PMID:22056746]
protein kinase D1/Protein kinase C mu in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3863] [GtoPdb: 1489] [UniProtKB: Q15139]
ChEMBL Inhibition of human PRKD1 B 7.46 pIC50 35 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 738-742 [PMID:22056746]
protein kinase D3/Protein kinase C nu in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2595] [GtoPdb: 2174] [UniProtKB: O94806]
ChEMBL Inhibition of human PRKD3 B 6.66 pIC50 219 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 738-742 [PMID:22056746]
ribosomal protein S6 kinase A2/Ribosomal protein S6 kinase alpha 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3906] [GtoPdb: 1529] [UniProtKB: Q15349]
ChEMBL Kinase Glo Plus Assay: Human RSK2 protein, purchased from Invitrogen, is used to measure kinase activity utilizing Kinase Glo Plus (Promega) a homogeneous assay technology, which uses a luciferin-luciferase based ATP detection reagent to quantify residual ATP. The assay is performed using 0.75 nM His-RSK2, 0.75 .mu.M ATP and 1.0 uM S6 Kinase/RSK Substrate Peptide 1 (Upstate, catalog #12-124), in assay buffer consisting of 25 mM HEPES, pH 7.5, 10 mM MgCl2, 5 mM MnCl2, 50 mM KCl, 0.2% BSA, 0.01% CHAPS, 100 uM Na3VO4, 0.5 mM DTT, and 1% DMSO. Solutions of test compounds at various concentrations are prepared by 1:3 fold serial dilution of a 1 mM solution of compound in DMSO. The DMSO solutions are further diluted with assay buffer to a final concentration of DMSO of 5%. The assay is performed in a 384 well, white, non-binding plate (Corning, catalogue #3574). Solutions of test compounds (10 uL) are transferred to a dry assay plate, followed by addition of 20 uL kinase. B 8.96 pIC50 1.1 nM IC50 US-9150577-B2. Heterocyclic compounds containing an indole core (2015)
ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812]
ChEMBL Inhibition of human RSK2-mediated CREB phosphorylation in HLR-CREB cells by cell based assay B 7.7 pIC50 20 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 738-742 [PMID:22056746]
GtoPdb - - 8.96 pIC50 1.1 nM IC50 Bioorg Med Chem Lett (2012) 22: 738-42 [PMID:22056746]
ChEMBL Inhibition of human RSK2 B 9 pIC50 1 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 738-742 [PMID:22056746]
protein kinase D2/Serine/threonine-protein kinase D2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4900] [GtoPdb: 2173] [UniProtKB: Q9BZL6]
ChEMBL Inhibition of human PRKD2 B 6.86 pIC50 139 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 738-742 [PMID:22056746]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Inhibition of human FLT3 B 6.15 pIC50 714 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 738-742 [PMID:22056746]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Inhibition of human RET B 6.79 pIC50 161 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 738-742 [PMID:22056746]

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]