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 phosphorylation using RRRADDSDDDDD as substrate in presence of [32p]-ATP | B | 6.52 | pKi | 300 | nM | Ki | J Med Chem (2023) 66: 2257-2281 [PMID:36745746] |
| ChEMBL | Inhibition of rat liver CK2 phosphorylation using RRRADDSDDDDD as substrate in presence of [32p]-ATP | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (2023) 66: 2257-2281 [PMID:36745746] |
| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
