CEP-1347 [Ligand Id: 8173] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL290352 (Cep-1347, CEP-1347, KT-1575, KT-7515, KT7515)
  • mitogen-activated protein kinase kinase kinase 10/Mitogen-activated protein kinase kinase kinase 10 in Human [ChEMBL: CHEMBL2873] [GtoPdb: 2070] [UniProtKB: Q02779]
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  • mitogen-activated protein kinase kinase kinase 11/Mitogen-activated protein kinase kinase kinase 11 in Human [ChEMBL: CHEMBL2708] [GtoPdb: 2071] [UniProtKB: Q16584]
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  • mitogen-activated protein kinase kinase kinase 9/Mitogen-activated protein kinase kinase kinase 9 in Human [ChEMBL: CHEMBL2872] [GtoPdb: 2084] [UniProtKB: P80192]
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  • neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
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  • fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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  • fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
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  • mitogen-activated protein kinase kinase kinase 12 in Human [GtoPdb: 2072] [UniProtKB: Q12852]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 Mixed lineage kinase 2(MLK2) B 7.29 pIC50 51 nM IC50 Bioorg Med Chem Lett (2002) 12: 147-150 [PMID:11755341]
ChEMBL Inhibition of recombinant GST-tagged full length human MLK2 KD/LZ expressed in baculovirus using myelin basic protein as substrate preincubated for 15 mins measured after 30 mins in presence of [gamma-32P]ATP by scintillation counting B 7.29 pIC50 51 nM IC50 J Med Chem (2018) 61: 8078-8087 [PMID:29863360]
ChEMBL Inhibition of MLK2 (unknown origin) after 20 mins in presence of [33P]-ATP B 8.7 pIC50 2 nM IC50 J Med Chem (2013) 56: 8032-8048 [PMID:24044867]
GtoPdb - - 8.7 pIC50 2 nM IC50 J Med Chem (2013) 56: 8032-48 [PMID:24044867];
J Biol Chem (2001) 276: 25302-8 [PMID:11325962]
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 GST-fused human MLK3 B 7.19 pIC50 64 nM IC50 J Med Chem (2008) 51: 5680-5689 [PMID:18714982]
ChEMBL Inhibition of Mixed lineage kinase 3 (MLK3) B 7.64 pIC50 23.1 nM IC50 Bioorg Med Chem Lett (2002) 12: 147-150 [PMID:11755341]
ChEMBL Inhibition of recombinant GST-tagged full length human MLK3 KD expressed in baculovirus using myelin basic protein as substrate preincubated for 15 mins measured after 30 mins in presence of [gamma-32P]ATP by scintillation counting B 7.64 pIC50 23 nM IC50 J Med Chem (2018) 61: 8078-8087 [PMID:29863360]
GtoPdb - - 8.22 pIC50 6 nM IC50 J Med Chem (2013) 56: 8032-48 [PMID:24044867];
J Biol Chem (2001) 276: 25302-8 [PMID:11325962]
ChEMBL Inhibition of MLK3 (unknown origin) after 20 mins in presence of [33P]-ATP B 8.22 pIC50 6 nM IC50 J Med Chem (2013) 56: 8032-8048 [PMID:24044867]
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 GST-fused human MLK1 expressed in CHO cells assessed as MKK4 phosphorylation B 7.14 pIC50 72 nM IC50 J Med Chem (2008) 51: 5680-5689 [PMID:18714982]
ChEMBL Inhibition of Mixed lineage kinase 1 (MLK1) B 7.42 pIC50 38 nM IC50 Bioorg Med Chem Lett (2002) 12: 147-150 [PMID:11755341]
ChEMBL Inhibition of GST-fused human MLK1 B 7.42 pIC50 38 nM IC50 J Med Chem (2008) 51: 5680-5689 [PMID:18714982]
ChEMBL Inhibition of recombinant GST-tagged human MLK1 KD (1 to 500 residues) expressed in baculovirus using myelin basic protein as substrate preincubated for 15 mins measured after 30 mins in presence of [gamma-32P]ATP by scintillation counting B 7.42 pIC50 38 nM IC50 J Med Chem (2018) 61: 8078-8087 [PMID:29863360]
GtoPdb - - 9 pIC50 1 nM IC50 J Med Chem (2013) 56: 8032-48 [PMID:24044867];
J Biol Chem (2001) 276: 25302-8 [PMID:11325962];
J Med Chem (2018) 61: 8078-8087 [PMID:29863360]
ChEMBL Inhibition of MLK1 (unknown origin) after 20 mins in presence of [33P]-ATP B 9 pIC50 <1 nM IC50 J Med Chem (2013) 56: 8032-8048 [PMID:24044867]
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 NGF high affinity receptor tyrosine kinase TrkA B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2002) 12: 147-150 [PMID:11755341]
Protein delta homolog 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5671] [UniProtKB: P80370]
ChEMBL Inhibition of human DLK expressed in baculovirus insect cell system B 6.94 pIC50 114 nM IC50 J Med Chem (2008) 51: 5680-5689 [PMID:18714982]
ChEMBL Inhibition of DLK (unknown origin) using myelin basic protein as substrate preincubated for 15 mins measured after 30 mins in presence of [gamma-32P]ATP by scintillation counting B 6.94 pIC50 114 nM IC50 J Med Chem (2018) 61: 8078-8087 [PMID:29863360]
fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
ChEMBL Inhibition of human VEGFR1 expressed in baculovirus insect cell system B 6.68 pIC50 209 nM IC50 J Med Chem (2008) 51: 5680-5689 [PMID:18714982]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL Inhibition of human VEGFR2 expressed in baculovirus insect cell system B 7.37 pIC50 43 nM IC50 J Med Chem (2008) 51: 5680-5689 [PMID:18714982]
fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
ChEMBL Inhibition of human VEGFR3 expressed in baculovirus insect cell system B 7.41 pIC50 39 nM IC50 J Med Chem (2008) 51: 5680-5689 [PMID:18714982]
mitogen-activated protein kinase kinase kinase 12 in Human [GtoPdb: 2072] [UniProtKB: Q12852]
GtoPdb - - 6.94 pIC50 114 nM IC50 J Med Chem (2018) 61: 8078-8087 [PMID:29863360]

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]