compound 1a [PMID: 24900749] [Ligand Id: 8128] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2409175 |
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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: 1550, 1551, 1549] [UniProtKB: P19784, P67870, P68400] | ||||||||
| 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 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]
