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 recombinant GST-tagged MLK2 (unknown origin) expressed in Baculovirus infected Sf21 cells incubated for 1 hr by affinity chromatography method B 7.29 pIC50 51 nM IC50 Eur J Med Chem (2023) 257: 115511-115511 [PMID:37247505]
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 recombinant GST-tagged MLK3 (unknown origin) expressed in Baculovirus infected Sf21 cells incubated for 1 hr by affinity chromatography method B 4.64 pIC50 23000 nM IC50 Eur J Med Chem (2023) 257: 115511-115511 [PMID:37247505]
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]
ChEMBL Inhibition of N-terminal GST-tagged recombinant MLK3 (unknown origin) expressed in insect cells incubated for 15 mins in presence of [gamma-32P]ATP by scintillation counter analysis B 7.64 pIC50 23 nM IC50 Bioorg Med Chem Lett (2024) 101: 129652-129652 [PMID:38346577]
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]
ChEMBL Inhibition of recombinant GST-tagged MLK1 (unknown origin) expressed in Baculovirus infected Sf21 cells incubated for 1 hr by affinity chromatography method B 7.42 pIC50 38 nM IC50 Eur J Med Chem (2023) 257: 115511-115511 [PMID:37247505]
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 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]