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ChEMBL ligand: CHEMBL416056 ((+)-K-252A, K-252A) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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calcium/calmodulin dependent protein kinase kinase 2/CaM-kinase kinase beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5284] [GtoPdb: 1957] [UniProtKB: Q96RR4] | ||||||||
ChEMBL | Inhibition of CaM-KKbeta | B | 8.74 | pKi | 1.8 | nM | Ki | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094126] [GtoPdb: 1973] [UniProtKB: O96020, P24864, P24941] | ||||||||
ChEMBL | Inhibitory activity against Cyclin E-cyclin-dependent kinase 2 by measuring phosphorylation of RbING substrate | B | 6.59 | pIC50 | 260 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 3841-3846 [PMID:14552792] |
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802, P24385] | ||||||||
ChEMBL | Inhibitory activity against Cyclin D1-cyclin-dependent kinase 4 by measuring phosphorylation of RbING substrate | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 3841-3846 [PMID:14552792] |
death associated protein kinase 3/Death-associated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2468] [GtoPdb: 2004] [UniProtKB: O43293] | ||||||||
ChEMBL | Inhibition of DLK | B | 6.44 | pIC50 | 360 | nM | IC50 | J Med Chem (2007) 50: 433-441 [PMID:17266195] |
eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525] | ||||||||
ChEMBL | Inhibition of human recombinant PKR autophosphorylation using poly[I:C] after 10 mins by luminescent assay | B | 7 | pIC50 | <100 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4108-4114 [PMID:21632247] |
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 GST-MLK2 | B | 7.35 | pIC50 | 45 | nM | IC50 | J Med Chem (2007) 50: 433-441 [PMID:17266195] |
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-MLK3 expressed in baculovirus | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2007) 50: 433-441 [PMID:17266195] |
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-MLK1 expressed in baculovirus | B | 7.66 | pIC50 | 22 | nM | IC50 | J Med Chem (2007) 50: 433-441 [PMID:17266195] |
myosin light chain kinase/Myosin light chain kinase, smooth muscle in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2428] [GtoPdb: 1552] [UniProtKB: Q15746] | ||||||||
ChEMBL | Inhibition of human myosin light chain kinase | B | 7.77 | pKi | 17 | nM | Ki | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
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 TrkA | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2007) 50: 433-441 [PMID:17266195] |
GtoPdb | - | - | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2007) 50: 433-41 [PMID:17266195] |
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 VEGFR2 | B | 7.37 | pIC50 | 43 | nM | IC50 | J Med Chem (2007) 50: 433-441 [PMID:17266195] |
M1 receptor in Human [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
GtoPdb | - | - | 5.1 | pKd | - | - | - | Mol Pharmacol (2000) 58: 194-207 [PMID:10860942] |
large tumor suppressor kinase 1 in Human [GtoPdb: 1515] [UniProtKB: O95835] | ||||||||
GtoPdb | - | - | 7.17 | pKd | 67.6 | nM | Kd | Science (2017) 358: [PMID:29191878] |
ChEMBL data shown on this page come from version 32:
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]