compound 77 [PMID: 24793884] [Ligand Id: 8217] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3261517
  • casein kinase 1 alpha 1/Casein kinase I alpha in Human [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729]
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  • casein kinase 1 delta/Casein kinase I delta in Human [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
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  • 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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  • cell division cycle 7/CDC7/DBF4 (Cell division cycle 7-related protein kinase/Activator of S phase kinase) in Human [ChEMBL: CHEMBL2111377] [GtoPdb: 1960] [UniProtKB: O00311Q9UBU7]
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  • Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
casein kinase 1 alpha 1/Casein kinase I alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729]
ChEMBL Inhibition of CK1alpha (unknown origin) by TR-FRET assay B 6.26 pIC50 545 nM IC50 Eur J Med Chem (2014) 80: 364-382 [PMID:24793884]
casein kinase 1 delta/Casein kinase I delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
ChEMBL Inhibition of CK1delta (unknown origin) by TR-FRET assay B 6.98 pIC50 104 nM IC50 Eur J Med Chem (2014) 80: 364-382 [PMID:24793884]
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]
ChEMBL Inhibition of CK2 (unknown origin) by homogeneous time-resolved fluorescence assay B 4.19 pIC50 65000 nM IC50 Eur J Med Chem (2014) 80: 364-382 [PMID:24793884]
cell division cycle 7/CDC7/DBF4 (Cell division cycle 7-related protein kinase/Activator of S phase kinase) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111377] [GtoPdb: 1960] [UniProtKB: O00311Q9UBU7]
ChEMBL Inhibition of Cdc7/Dbf4 in human HCT116 cells assessed as reduction of MCM2 phosphorylation after 14 hrs B 6.06 pIC50 862 nM IC50 Eur J Med Chem (2014) 80: 364-382 [PMID:24793884]
ChEMBL Inhibition of Cdc7/Dbf4 (unknown origin)-mediated phosphorylation of MCM2 by protein-A luminescent proximity homogenous assay B 8.17 pIC50 6.81 nM IC50 Eur J Med Chem (2014) 80: 364-382 [PMID:24793884]
GtoPdb - - 8.17 pIC50 6.81 nM IC50 Eur J Med Chem (2014) 80: 364-82 [PMID:24793884]
cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563P50750]
ChEMBL Inhibition of CDK9/Cyclin-T1 (unknown origin) by homogeneous time-resolved fluorescence assay B 6.14 pIC50 729 nM IC50 Eur J Med Chem (2014) 80: 364-382 [PMID:24793884]
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493P14635]
ChEMBL Inhibition of CDK1/Cyclin-B (unknown origin) by homogeneous time-resolved fluorescence assay B 4.3 pIC50 >50000 nM IC50 Eur J Med Chem (2014) 80: 364-382 [PMID:24793884]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864P24941]
ChEMBL Inhibition of CDK2/Cyclin-E (unknown origin) using maltose binding protein as substrate by HTRF assay B 4.97 pIC50 10600 nM IC50 Eur J Med Chem (2014) 80: 364-382 [PMID:24793884]
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802P24385]
ChEMBL Inhibition of CDK4/Cyclin-D1 (unknown origin) by homogeneous time-resolved fluorescence assay B 4.3 pIC50 >50000 nM IC50 Eur J Med Chem (2014) 80: 364-382 [PMID:24793884]
Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
ChEMBL Inhibition of Pim1 (unknown origin) by homogeneous time-resolved fluorescence assay B 6 pIC50 >1000 nM IC50 Eur J Med Chem (2014) 80: 364-382 [PMID:24793884]

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]