compound 74 [PMID: 24793884] [Ligand Id: 8219] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL3261514
  • casein kinase 1 alpha 1/Casein kinase I alpha in Human [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729]
There should be some charts here, you may need to enable JavaScript!
  • casein kinase 1 delta/Casein kinase I delta in Human [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
There should be some charts here, you may need to enable JavaScript!
  • 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: 1550, 1551, 1549] [UniProtKB: P19784, P67870, P68400]
There should be some charts here, you may need to enable JavaScript!
  • 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: O00311, Q9UBU7]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
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
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 6.16 pIC50 694 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 7.08 pIC50 84 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: 1550, 1551, 1549] [UniProtKB: P19784, P67870, P68400]
ChEMBL Inhibition of CK2 (unknown origin) by homogeneous time-resolved fluorescence assay B 4.54 pIC50 29100 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: O00311, Q9UBU7]
ChEMBL Inhibition of Cdc7/Dbf4 in human HCT116 cells assessed as reduction of MCM2 phosphorylation after 14 hrs B 6.3 pIC50 501 nM IC50 Eur. J. Med. Chem. (2014) 80: 364-382 [PMID:24793884]
ChEMBL Inhibition of Cdc7/Dbf4 (unknown origin) using 54 uM of ATP as substrate by AlphaScreen assay B 7.07 pIC50 86 nM IC50 Eur. J. Med. Chem. (2014) 80: 364-382 [PMID:24793884]
ChEMBL Inhibition of Cdc7/Dbf4 (unknown origin) using 0.074 uM of ATP as substrate by AlphaScreen assay B 7.19 pIC50 64 nM IC50 Eur. J. Med. Chem. (2014) 80: 364-382 [PMID:24793884]
ChEMBL Inhibition of Cdc7/Dbf4 (unknown origin) using 0.037 uM of ATP as substrate by AlphaScreen assay B 7.2 pIC50 63 nM IC50 Eur. J. Med. Chem. (2014) 80: 364-382 [PMID:24793884]
ChEMBL Inhibition of Cdc7/Dbf4 (unknown origin) using 27 uM of ATP as substrate by AlphaScreen assay B 7.36 pIC50 44 nM IC50 Eur. J. Med. Chem. (2014) 80: 364-382 [PMID:24793884]
ChEMBL Inhibition of Cdc7/Dbf4 (unknown origin) using 0.025 uM of ATP as substrate by AlphaScreen assay B 7.4 pIC50 40 nM IC50 Eur. J. Med. Chem. (2014) 80: 364-382 [PMID:24793884]
ChEMBL Inhibition of Cdc7/Dbf4 (unknown origin) using 0.222 uM of ATP as substrate by AlphaScreen assay B 7.46 pIC50 35 nM IC50 Eur. J. Med. Chem. (2014) 80: 364-382 [PMID:24793884]
ChEMBL Inhibition of Cdc7/Dbf4 (unknown origin) using 0.111 uM of ATP as substrate by AlphaScreen assay B 7.54 pIC50 29 nM IC50 Eur. J. Med. Chem. (2014) 80: 364-382 [PMID:24793884]
ChEMBL Inhibition of Cdc7/Dbf4 (unknown origin) using 18 uM of ATP as substrate by AlphaScreen assay B 7.64 pIC50 23 nM IC50 Eur. J. Med. Chem. (2014) 80: 364-382 [PMID:24793884]
ChEMBL Inhibition of Cdc7/Dbf4 (unknown origin) using 0.333 uM of ATP as substrate by AlphaScreen assay B 7.7 pIC50 20 nM IC50 Eur. J. Med. Chem. (2014) 80: 364-382 [PMID:24793884]
ChEMBL Inhibition of Cdc7/Dbf4 (unknown origin) using 9 uM of ATP as substrate by AlphaScreen assay B 7.74 pIC50 18 nM IC50 Eur. J. Med. Chem. (2014) 80: 364-382 [PMID:24793884]
ChEMBL Inhibition of Cdc7/Dbf4 (unknown origin) using 0.012 uM of ATP as substrate by AlphaScreen assay B 7.77 pIC50 17 nM IC50 Eur. J. Med. Chem. (2014) 80: 364-382 [PMID:24793884]
ChEMBL Inhibition of Cdc7/Dbf4 (unknown origin) using 0.667 uM of ATP as substrate by AlphaScreen assay B 7.85 pIC50 14 nM IC50 Eur. J. Med. Chem. (2014) 80: 364-382 [PMID:24793884]
ChEMBL Inhibition of Cdc7/Dbf4 (unknown origin) using 6 uM of ATP as substrate by AlphaScreen assay B 7.89 pIC50 13 nM IC50 Eur. J. Med. Chem. (2014) 80: 364-382 [PMID:24793884]
ChEMBL Inhibition of Cdc7/Dbf4 (unknown origin) using 1 uM of ATP as substrate by AlphaScreen assay B 8 pIC50 10 nM IC50 Eur. J. Med. Chem. (2014) 80: 364-382 [PMID:24793884]
ChEMBL Inhibition of Cdc7/Dbf4 (unknown origin) using 2 uM of ATP as substrate by AlphaScreen assay B 8 pIC50 10 nM IC50 Eur. J. Med. Chem. (2014) 80: 364-382 [PMID:24793884]
GtoPdb - - 8.42 pIC50 3.77 nM IC50 Eur J Med Chem (2014) 80: 364-82 [PMID:24793884]
ChEMBL Inhibition of Cdc7/Dbf4 (unknown origin)-mediated phosphorylation of MCM2 by protein-A luminescent proximity homogenous assay B 8.42 pIC50 3.77 nM IC50 Eur. J. Med. Chem. (2014) 80: 364-382 [PMID:24793884]
cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563, P50750]
ChEMBL Inhibition of CDK9/Cyclin-T1 (unknown origin) by homogeneous time-resolved fluorescence assay B 6.13 pIC50 749 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: P06493, P14635]
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: P24864, P24941]
ChEMBL Inhibition of CDK2/Cyclin-E (unknown origin) using maltose binding protein as substrate by HTRF assay B 5.74 pIC50 1820 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: P11802, P24385]
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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]