GNE-8505 [Ligand Id: 9990] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3715238 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| mitogen-activated protein kinase 8/c-Jun N-terminal kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983] | ||||||||
| ChEMBL | Inhibition of recombinant full length His-tagged human JNK1alpha1 expressed in baculovirus expression system by FRET assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 8083-8102 [PMID:28929759] |
| mitogen-activated protein kinase 9/c-Jun N-terminal kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4179] [GtoPdb: 1497] [UniProtKB: P45984] | ||||||||
| ChEMBL | Inhibition of recombinant full length His-tagged human JNK2 (473 to end residues) expressed in baculovirus expression system at by FRET assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 8083-8102 [PMID:28929759] |
| mitogen-activated protein kinase 10/c-Jun N-terminal kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2637] [GtoPdb: 1498] [UniProtKB: P53779] | ||||||||
| ChEMBL | Inhibition of recombinant full length GST-tagged human JNK3 expressed in baculovirus expression system by FRET assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 8083-8102 [PMID:28929759] |
| EPH receptor A7/Ephrin type-A receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4602] [GtoPdb: 1827] [UniProtKB: Q15375] | ||||||||
| ChEMBL | Inhibition of recombinant GST-tagged human EphA7 cytoplasmic domain expressed in baculovirus expression system by FRET assay | B | 6.18 | pIC50 | 665 | nM | IC50 | J Med Chem (2017) 60: 8083-8102 [PMID:28929759] |
| colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333] | ||||||||
| ChEMBL | Inhibition of recombinant His-tagged human CSF1R cytoplasmic domain (538 to 910 residues) expressed in baculovirus expression system by FRET assay | B | 5.91 | pIC50 | 1220 | nM | IC50 | J Med Chem (2017) 60: 8083-8102 [PMID:28929759] |
| mitogen-activated protein kinase kinase kinase 10/Mitogen-activated protein kinase kinase kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2873] [GtoPdb: 2070] [UniProtKB: Q02779] | ||||||||
| ChEMBL | Inhibition of recombinant human full length GST-tagged MLK2 expressed in baculovirus expression system by FRET assay | B | 5.29 | pIC50 | 5150 | nM | IC50 | J Med Chem (2017) 60: 8083-8102 [PMID:28929759] |
| mitogen-activated protein kinase kinase kinase 11/Mitogen-activated protein kinase kinase kinase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2708] [GtoPdb: 2071] [UniProtKB: Q16584] | ||||||||
| ChEMBL | Inhibition of recombinant human full length GST-tagged MLK3 expressed in baculovirus expression system by FRET assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 8083-8102 [PMID:28929759] |
| mitogen-activated protein kinase kinase kinase 12/Mitogen-activated protein kinase kinase kinase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1908389] [GtoPdb: 2072] [UniProtKB: Q12852] | ||||||||
| ChEMBL | Binding affinity to full length wild type human DLK (M1 to P859 residues) expressed in mammalian cells by KINOMEscan assay | B | 8.29 | pKd | 5.1 | nM | Kd | J Med Chem (2017) 60: 8083-8102 [PMID:28929759] |
| ChEMBL | Binding affinity to N-terminally GST-tagged wild type human DLK (1 to 520 residues) expressed in sf21 insect cells using N-terminally His-tagged MKK4 K131M as substrate after 60 mins in presence of ATP by TR-FRET assay | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2017) 60: 8083-8102 [PMID:28929759] |
| ChEMBL | Inhibition of N-terminally GST-tagged human DLK catalytic domain (1 to 520 amino acids) using N-terminal His-tagged MKK4 K131M substrate incubated for 60 mins by TR-FRET assay | B | 9.77 | pKi | 0.17 | nM | Ki | WO-2014111496-A1. 3-substituted pyrazoles and use as dlk inhibitors (2014) |
| GtoPdb | In a TR-FRET assay measuring inhibition of a N-terminally GST-tagged DLK catalytic domain (amino acids 1-520) construct interaction with MKK4 substrate. | - | 9.77 | pKi | 0.17 | nM | Ki | WO2014111496. 3-substituted pyrazoles and use as dlk inhibitors. (2017) |
| ChEMBL | Inhibition of doxycycline inducible human DLK transfected in HEK293 cells assessed as JNK phosphorylation after 5.5 hrs by Hoechst-33342 staining-based assay | B | 6.84 | pIC50 | 144 | nM | IC50 | J Med Chem (2017) 60: 8083-8102 [PMID:28929759] |
| mitogen-activated protein kinase kinase kinase 12/Mitogen-activated protein kinase kinase kinase 12 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295854] [GtoPdb: 2072] [UniProtKB: Q60700] | ||||||||
| ChEMBL | Inhibition of DLK in CD-1 mouse DRG neuron assessed as axonal protection pre-incubated for 2 hrs before NGF deprivation for 16 to 20 hrs by Campenot chamber based fluorescence assay | B | 6.34 | pEC50 | 457 | nM | EC50 | J Med Chem (2017) 60: 8083-8102 [PMID:28929759] |
| mitogen-activated protein kinase kinase kinase 13/Mitogen-activated protein kinase kinase kinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163124] [GtoPdb: 2073] [UniProtKB: O43283] | ||||||||
| ChEMBL | Binding affinity to full length wild type human LZK (M1 to W966 residues) expressed in mammalian cells by KINOMEscan assay | B | 6.92 | pKd | 120 | nM | Kd | J Med Chem (2017) 60: 8083-8102 [PMID:28929759] |
| mitogen-activated protein kinase kinase kinase 9/Mitogen-activated protein kinase kinase kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2872] [GtoPdb: 2084] [UniProtKB: P80192] | ||||||||
| ChEMBL | Inhibition of recombinant human GST-tagged MLK1 expressed in baculovirus expression system by FRET assay | B | 5.46 | pIC50 | 3500 | nM | IC50 | J Med Chem (2017) 60: 8083-8102 [PMID:28929759] |
| DM1 protein kinase/Myotonin-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5320] [GtoPdb: 1505] [UniProtKB: Q09013] | ||||||||
| ChEMBL | Inhibition of full length recombinant human DMPK expressed in baculovirus expression system by FRET assay | B | 5.86 | pIC50 | 1380 | nM | IC50 | J Med Chem (2017) 60: 8083-8102 [PMID:28929759] |
| 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 recombinant His-tagged human TrkA cytoplasmic domain (441 to 796 residues) expressed in baculovirus expression system by FRET assay | B | 6.42 | pIC50 | 383 | nM | IC50 | J Med Chem (2017) 60: 8083-8102 [PMID:28929759] |
| 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 recombinant His-tagged human FLT3 cytoplasmic domain expressed in baculovirus expression system by FRET assay | B | 6.62 | pIC50 | 238 | nM | IC50 | J Med Chem (2017) 60: 8083-8102 [PMID:28929759] |
| AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530] | ||||||||
| ChEMBL | Inhibition of recombinant His-tagged human AXL (473 to end residues) cytoplasmic domain expressed in insect cells by FRET assay | B | 6.35 | pIC50 | 448 | nM | IC50 | J Med Chem (2017) 60: 8083-8102 [PMID:28929759] |
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]
