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 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]
