BIX 02565 [Ligand Id: 8039] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1933288 |
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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 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]
