Syk inhibitor [Ligand Id: 6046] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL104279 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Fc fragment of IgE receptor II/Immunoglobulin epsilon Fc receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2940] [GtoPdb: 2935] [UniProtKB: P06734] | ||||||||
| ChEMBL | Effect on IgE/Fcepsilon RI triggered rat basophil cell (RBL-2H3) degranulation assessed by measuring the amount of 5-HT release | F | 6.5 | pEC50 | 313 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 3111-3114 [PMID:12941345] |
| neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629] | ||||||||
| ChEMBL | Inhibition of GAL4 fused TrkA (unknown origin) expressed in PC12 cells transfected with pFA2-Elk plasmid and pFR-luciferase plasmid measured for 18 hrs by luciferase reporter gene assay | B | 7.43 | pIC50 | 36.73 | nM | IC50 | Eur J Med Chem (2016) 121: 541-552 [PMID:27318978] |
| ChEMBL | Inhibition of GAL4 fused TrkA (unknown origin) expressed in PC12 cells transfected with pFA2-Elk plasmid and pFR-luciferase plasmid measured for 18 hrs by luciferase reporter gene assay | B | 7.44 | pIC50 | 36.7 | nM | IC50 | Eur J Med Chem (2016) 121: 541-552 [PMID:27318978] |
| ChEMBL | Inhibition of TrkA (unknown origin) | B | 8.38 | pIC50 | 4.17 | nM | IC50 | Eur J Med Chem (2016) 121: 541-552 [PMID:27318978] |
| neurotrophic receptor tyrosine kinase 2/Neurotrophic tyrosine kinase receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620] | ||||||||
| ChEMBL | Inhibition of TrkB (unknown origin) | B | 8.12 | pIC50 | 7.62 | nM | IC50 | Eur J Med Chem (2016) 121: 541-552 [PMID:27318978] |
| neurotrophic receptor tyrosine kinase 3/NT-3 growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5608] [GtoPdb: 1819] [UniProtKB: Q16288] | ||||||||
| ChEMBL | Inhibition of TrkC (unknown origin) | B | 8.16 | pIC50 | 6.86 | nM | IC50 | Eur J Med Chem (2016) 121: 541-552 [PMID:27318978] |
| spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405] | ||||||||
| GtoPdb | Assayed using N-Flag tagged catalytic domain of human SYK (Ala340-Asn635) | - | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 3111-4 [PMID:12941345] |
| ChEMBL | Inhibitory activity against human Syk protein tyrosine kinase expressed in yeast Klyveromyces lactis | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 3111-3114 [PMID:12941345] |
| ChEMBL | Inhibition of SYK | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2012) 55: 3614-3643 [PMID:22257213] |
| spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4364] [GtoPdb: 2230] [UniProtKB: Q64725] | ||||||||
| ChEMBL | Inhibition of SYK in rat RBL2H3 cells assessed as reduction in DNP-BSA-stimulated Fcepsilon receptor 1-mediated 5-HT release | B | 6.5 | pEC50 | 313 | nM | EC50 | J Med Chem (2012) 55: 3614-3643 [PMID:22257213] |
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]
