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 |
|---|---|---|---|---|---|---|---|---|
| A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
| ChEMBL | Selectivity interaction (Enzyme panel (receptors, ion channels, other enzymes)) EUB0000679a ADORA2A | B | 5.85 | pIC50 | 1420 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
| ChEMBL | Selectivity interaction (Enzyme panel (receptors, ion channels, other enzymes)) EUB0000679a ADRA1A | B | 6.04 | pIC50 | 914 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| ChEMBL | Selectivity interaction (Enzyme panel (receptors, ion channels, other enzymes)) EUB0000679a ADRA1B | B | 7.28 | pIC50 | 52 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
| ChEMBL | Selectivity interaction (Enzyme panel (receptors, ion channels, other enzymes)) EUB0000679a ADRB2 | B | 5.74 | pIC50 | 1820 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| CDC like kinase 1/Dual specificity 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] |
| ChEMBL | Selectivity interaction (SelectScreen (Invitrogen)) EUB0000679a CLK1 | B | 6.29 | pIC50 | 512 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Selectivity interaction (SelectScreen (Invitrogen)) EUB0000679a CLK2 | B | 6.95 | pIC50 | 112 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Selectivity interaction (SelectScreen (Invitrogen)) EUB0000679a FGFR2 | B | 6.49 | pIC50 | 320 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Selectivity interaction (SelectScreen (Invitrogen)) EUB0000679a LRRK2 | B | 7.8 | pIC50 | 16 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| Nischarin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3923] [UniProtKB: Q9Y2I1] | ||||||||
| ChEMBL | Selectivity interaction (Enzyme panel (receptors, ion channels, other enzymes)) EUB0000679a NISCH | B | 7.01 | pIC50 | 97 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Selectivity interaction (SelectScreen (Invitrogen)) EUB0000679a PDGFRA | B | 6.02 | pIC50 | 956 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Selectivity interaction (SelectScreen (Invitrogen)) EUB0000679a PRKD1 | B | 7.46 | pIC50 | 35 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Selectivity interaction (SelectScreen (Invitrogen)) EUB0000679a PRKD3 | B | 6.66 | pIC50 | 219 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Affinity Phenotypic Cellular interaction (Steady Glo Luciferase assay (Promega; inhibition of transcription factor CREB (cAMP Response Element Binding) phosphorylation by RSK2 in HLR-CREB cell line)) EUB0000679a RPS6KA3 | B | 7.7 | pIC50 | 20 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Affinity Biochemical interaction (Kinase Glo Plus assay (Promega; 0.75 µM ATP)) EUB0000679a RPS6KA3 | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Inhibition of human RSK2 in MCF7 cells | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2023) 251: 115229-115229 [PMID:36898330] |
| 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] |
| ChEMBL | Selectivity interaction (SelectScreen (Invitrogen)) EUB0000679a PRKD2 | B | 6.86 | pIC50 | 139 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Selectivity interaction (SelectScreen (Invitrogen)) EUB0000679a FLT3 | B | 6.15 | pIC50 | 714 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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 | Selectivity interaction (SelectScreen (Invitrogen)) EUB0000679a RET | B | 6.79 | pIC50 | 161 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
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]
