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 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]
