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 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]