K-252a | Ligand Activity Charts | IUPHAR/BPS Guide to PHARMACOLOGY

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K-252a
Ligand Activity Charts

K-252a [Ligand Id: 336] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL416056 ((+)-K-252A, K-252A)
calcium/calmodulin dependent protein kinase kinase 2/CaM-kinase kinase beta in Human [ChEMBL: CHEMBL5284] [GtoPdb: 1957] [UniProtKB: Q96RR4] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E in Human [ChEMBL: CHEMBL2094126] [GtoPdb: 1973] [UniProtKB: O96020, P24864, P24941] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802, P24385] There should be some charts here, you may need to enable JavaScript!
death associated protein kinase 3/Death-associated protein kinase 3 in Human [ChEMBL: CHEMBL2468] [GtoPdb: 2004] [UniProtKB: O43293] There should be some charts here, you may need to enable JavaScript!
eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase kinase 10/Mitogen-activated protein kinase kinase kinase 10 in Human [ChEMBL: CHEMBL2873] [GtoPdb: 2070] [UniProtKB: Q02779] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase kinase 11/Mitogen-activated protein kinase kinase kinase 11 in Human [ChEMBL: CHEMBL2708] [GtoPdb: 2071] [UniProtKB: Q16584] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase kinase 9/Mitogen-activated protein kinase kinase kinase 9 in Human [ChEMBL: CHEMBL2872] [GtoPdb: 2084] [UniProtKB: P80192] There should be some charts here, you may need to enable JavaScript!
myosin light chain kinase/Myosin light chain kinase, smooth muscle in Human [ChEMBL: CHEMBL2428] [GtoPdb: 1552] [UniProtKB: Q15746] There should be some charts here, you may need to enable JavaScript!
neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629] There should be some charts here, you may need to enable JavaScript!
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] There should be some charts here, you may need to enable JavaScript!
M₁ receptor in Human [GtoPdb: 13] [UniProtKB: P11229] There should be some charts here, you may need to enable JavaScript!
large tumor suppressor kinase 1 in Human [GtoPdb: 1515] [UniProtKB: O95835] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
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]