DMAT [Ligand Id: 9323] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL376505 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| casein kinase 2, alpha 1 polypeptide subunit/casein kinase 2, beta polypeptide subunit/Casein kinase 2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3988629] [GtoPdb: 1549, 1551] [UniProtKB: P19139, P67874] | ||||||||
| ChEMBL | Inhibition of rat liver CK2 after 10 mins in presence of [gamma-33P]-ATP | B | 6.85 | pIC50 | 140 | nM | IC50 | US-20130225674-A1. Use of dibenzofuranone derivatives to inhibit kinases (2013) |
| 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 | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2004) 47: 6239-6247 [PMID:15566294] |
| ChEMBL | Inhibition of CK2 (unknown origin) | B | 7.4 | pKi | 40 | nM | Ki | Med Chem Res (2012) 21: 269-283 |
| ChEMBL | Inhibition of CK2 V66A, I174A mutant | B | 5.24 | pIC50 | 5790 | nM | IC50 | J Med Chem (2004) 47: 6239-6247 [PMID:15566294] |
| ChEMBL | Inhibition of CK2 I174A mutant | B | 5.48 | pIC50 | 3300 | nM | IC50 | J Med Chem (2004) 47: 6239-6247 [PMID:15566294] |
| ChEMBL | Inhibition of CK2 V66A mutant | B | 5.75 | pIC50 | 1780 | nM | IC50 | J Med Chem (2004) 47: 6239-6247 [PMID:15566294] |
| ChEMBL | Inhibition of CK2 | B | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (2004) 47: 6239-6247 [PMID:15566294] |
| casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400] | ||||||||
| ChEMBL | Inhibition of CK2alpha in human PLC1 cells using (Arg)3(Glu)3Thr(Glu)3 as substrate after 24 hrs in presence of [32P]gammaGTP | B | 5.35 | pKi | 4500 | nM | Ki | Eur J Med Chem (2019) 181: 111581-111581 [PMID:31400711] |
| ChEMBL | Inhibition of human CK2 alpha catalytic subunit expressed in Escherichia coli BL21 (DE3) assessed as [33P]gamma-ATP incorporation into RRRADDSDDDDD substrate after 15 mins by scintillation counting | B | 6.86 | pKi | 139 | nM | Ki | Eur J Med Chem (2012) 47: 345-350 [PMID:22115617] |
| ChEMBL | Inhibition of human CK2 alpha catalytic subunit expressed in Escherichia coli BE21 (DE3) assessed as [33P]gamma-ATP incorporation into P2B substrate after 15 mins by scintillation counting | B | 7.01 | pKi | 97 | nM | Ki | Eur J Med Chem (2012) 47: 345-350 [PMID:22115617] |
| ChEMBL | Binding affinity to CK2alpha (unknown origin) | B | 7.4 | pKi | 40 | nM | Ki | Eur J Med Chem (2014) 84: 364-374 [PMID:25036794] |
| casein kinase 2, alpha prime polypeptide subunit/Casein kinase II alpha (prime) in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4070] [GtoPdb: 1550] [UniProtKB: P19784] | ||||||||
| ChEMBL | Inhibition of human CK2 alpha' catalytic subunit expressed in Escherichia coli BE21 (DE3) assessed as [33P]gamma-ATP incorporation into RRRADDSDDDDD substrate after 15 mins by scintillation counting | B | 6.88 | pKi | 133 | nM | Ki | Eur J Med Chem (2012) 47: 345-350 [PMID:22115617] |
| ChEMBL | Inhibition of human CK2 alpha' catalytic subunit expressed in Escherichia coli BL21 (DE3) assessed as [33P]gamma-ATP incorporation into P2B substrate after 15 mins by scintillation counting | B | 6.95 | pKi | 112 | nM | Ki | Eur J Med Chem (2012) 47: 345-350 [PMID:22115617] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248, P24941, P78396] | ||||||||
| ChEMBL | Inhibition of CDK2/Cyclin A | B | 5.62 | pIC50 | 2380 | nM | IC50 | J Med Chem (2004) 47: 6239-6247 [PMID:15566294] |
| mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750] | ||||||||
| ChEMBL | Inhibition of MKK1 | B | 4.98 | pIC50 | 10500 | nM | IC50 | J Med Chem (2004) 47: 6239-6247 [PMID:15566294] |
| dual specificity tyrosine phosphorylation regulated kinase 1A/Dual-specificity tyrosine-phosphorylation regulated kinase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627] | ||||||||
| ChEMBL | Inhibition of DYRK1A (unknown origin) | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2018) 61: 9791-9810 [PMID:29985601] |
| ChEMBL | Inhibition of DYRK1A | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2004) 47: 6239-6247 [PMID:15566294] |
| ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418] | ||||||||
| ChEMBL | Inhibition of MAPKAPK1a | B | 4.99 | pIC50 | 10280 | nM | IC50 | J Med Chem (2004) 47: 6239-6247 [PMID:15566294] |
| serum/glucocorticoid regulated kinase 1/Serine/threonine-protein kinase Sgk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2343] [GtoPdb: 1534] [UniProtKB: O00141] | ||||||||
| ChEMBL | Inhibition of SGK | B | 5.45 | pIC50 | 3570 | nM | IC50 | J Med Chem (2004) 47: 6239-6247 [PMID:15566294] |
| Casein kinase 2 in Rat [GtoPdb: 1548] | ||||||||
| GtoPdb | - | - | 7.4 | pKi | 40 | nM | Ki | |
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]
