compound 1a [PMID: 24900749] [Ligand Id: 8128] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2409175
  • casein kinase 2, alpha prime polypeptide subunit/casein kinase 2, beta polypeptide subunit/casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II in Human [ChEMBL: CHEMBL2095191] [GtoPdb: 155015511549] [UniProtKB: P19784P67870P68400]
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  • casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II alpha in Human [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400]
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  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • dual specificity tyrosine phosphorylation regulated kinase 3/Dual-specificity tyrosine-phosphorylation regulated kinase 3 in Human [ChEMBL: CHEMBL4575] [GtoPdb: 2012] [UniProtKB: O43781]
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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
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  • homeodomain interacting protein kinase 2/Homeodomain-interacting protein kinase 2 in Human [ChEMBL: CHEMBL4576] [GtoPdb: 2034] [UniProtKB: Q9H2X6]
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  • Pim-3 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM3 in Human [ChEMBL: CHEMBL5407] [GtoPdb: 2160] [UniProtKB: Q86V86]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
casein kinase 2, alpha prime polypeptide subunit/casein kinase 2, beta polypeptide subunit/casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2095191] [GtoPdb: 155015511549] [UniProtKB: P19784P67870P68400]
GtoPdb - - 8 pIC50 10 nM IC50 ACS Med Chem Lett (2013) 4: 800-5 [PMID:24900749]
ChEMBL Inhibition of CK2 in human DLD1 HA-myr-AKT1 cells assessed as suppression of AKTser129 phosphorylation after 3 to 24 hrs by Western blot analysis B 8.7 pIC50 2 nM IC50 ACS Med. Chem. Lett. (2016) 7: 300-305 [PMID:26985319]
casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400]
GtoPdb - - 8 pIC50 10 nM IC50 ACS Med Chem Lett (2013) 4: 800-5 [PMID:24900749]
ChEMBL Inhibition of N-terminal His6X-tagged recombinant human full length casein kinase-2alpha expressed in SF21 cells using BODIPY-FL-RRRDDDSDDD-CONH2 as substrate preincubated for 20 mins measured after 90 mins by mobility shift assay B 8.52 pIC50 <3 nM IC50 ACS Med. Chem. Lett. (2013) 4: 800-805 [PMID:24900749]
ChEMBL Inhibition of full length N-terminal 6xHis-tagged recombinant human CK2alpha expressed in fall armyworm Sf21 cells using BODIPY-FL-RRRDDDSDDD-CONH2 as substrate after 90 mins by mobility shift assay B 8.52 pIC50 <3 nM IC50 ACS Med. Chem. Lett. (2016) 7: 300-305 [PMID:26985319]
ChEMBL Inhibition of recombinant human full length N-terminal His6-tagged CK2alpha expressed in Sf21 insect cells using CK2tide as substrate treated for 20 mins measured after 90 mins in presence of MgCl2 by caliper mobility shift assay B 8.52 pIC50 <3 nM IC50 Bioorg Med Chem Lett (2018) 28: 1336-1341 [PMID:29559278]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibition of CDK2 (unknown origin) B 5.14 pIC50 7200 nM IC50 ACS Med. Chem. Lett. (2013) 4: 800-805 [PMID:24900749]
dual specificity tyrosine phosphorylation regulated kinase 3/Dual-specificity tyrosine-phosphorylation regulated kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4575] [GtoPdb: 2012] [UniProtKB: O43781]
GtoPdb - - 7.15 pIC50 70 nM IC50 ACS Med Chem Lett (2013) 4: 800-5 [PMID:24900749]
ChEMBL Inhibition of Dyrk-3 (unknown origin) B 7.15 pIC50 70 nM IC50 ACS Med. Chem. Lett. (2013) 4: 800-805 [PMID:24900749]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL Inhibition of GSK3beta (unknown origin) B 5.59 pIC50 2600 nM IC50 ACS Med. Chem. Lett. (2013) 4: 800-805 [PMID:24900749]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Binding affinity to human ERG expressed in CHO cells by IonWorks assay B 4.68 pIC50 21000 nM IC50 ACS Med. Chem. Lett. (2013) 4: 800-805 [PMID:24900749]
homeodomain interacting protein kinase 2/Homeodomain-interacting protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4576] [GtoPdb: 2034] [UniProtKB: Q9H2X6]
ChEMBL Inhibition of Hipk-2 (unknown origin) B 7.4 pIC50 40 nM IC50 ACS Med. Chem. Lett. (2013) 4: 800-805 [PMID:24900749]
GtoPdb - - 7.4 pIC50 40 nM IC50 ACS Med Chem Lett (2013) 4: 800-5 [PMID:24900749]
Pim-3 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5407] [GtoPdb: 2160] [UniProtKB: Q86V86]
GtoPdb - - 6.82 pIC50 150 nM IC50 ACS Med Chem Lett (2013) 4: 800-5 [PMID:24900749]
ChEMBL Inhibition of PIM3 (unknown origin) B 6.82 pIC50 150 nM IC50 ACS Med. Chem. Lett. (2013) 4: 800-805 [PMID:24900749]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]