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ChEMBL ligand: CHEMBL290352 (Cep-1347, CEP-1347, KT-1575, KT-7515, KT7515) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]