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ChEMBL ligand: CHEMBL177820 (4,5,6,7-Tetrabromobenzotriazole) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | 6.4 | pKi | 400 | 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 | 5.8 | pIC50 | 1600 | nM | IC50 | J Med Chem (2023) 66: 2257-2281 [PMID:36745746] |
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 | Competitive inhibition of human CK2 assessed as competitive with respect to ATP | B | 5.57 | pKi | 2700 | nM | Ki | Bioorg Med Chem (2014) 22: 4553-4565 [PMID:25131958] |
ChEMBL | Inhibition of human CK2 assessed as residual activity by KinaseProfiler assay | B | 5.91 | pIC50 | 1240 | nM | IC50 | Bioorg Med Chem (2014) 22: 4553-4565 [PMID:25131958] |
ChEMBL | Inhibition of CK2 (unknown origin) using E-peptide as substrate incubated for 10 mins prior to testing by capillary electrophoretic analysis | B | 6 | pIC50 | 1000 | nM | IC50 | US-20130225674-A1. Use of dibenzofuranone derivatives to inhibit kinases (2013) |
ChEMBL | Inhibition of CK2 (unknown origin) | B | 6.05 | pIC50 | 900 | nM | IC50 | Eur J Med Chem (2015) 96: 396-404 [PMID:25912672] |
ChEMBL | Inhibition of human recombinant CK2 expressed in Escherichia coli BL21(DE3) using RRRDDDSDDD as substrate after 15 mins by capillary electrophoretic analysis | B | 7.22 | pIC50 | 60 | nM | IC50 | Eur J Med Chem (2013) 65: 205-222 [PMID:23711832] |
ChEMBL | Inhibition of human recombinant CK2a1/CK2b holoenzyme expressed in Escherichia coli BL21(DE3) pre-incubated for 10 mins before substrate addition by capillary electrophoresis based assay | B | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (2015) 58: 265-277 [PMID:25272055] |
casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400] | ||||||||
ChEMBL | Inhibitory constant against Zea mays CK2alpha | B | 6.4 | pKi | 400 | nM | Ki | Biochem J (2003) 374: 639-646 [PMID:12816539] |
ChEMBL | Binding affinity to CK2alpha (unknown origin) | B | 6.4 | pKi | 400 | nM | Ki | Eur J Med Chem (2014) 84: 364-374 [PMID:25036794] |
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 | 6.52 | pKi | 300 | nM | Ki | Eur J Med Chem (2019) 181: 111581-111581 [PMID:31400711] |
ChEMBL | Inhibition of recombinant full length human His-tagged CK2alpha1 expressed in baculovirus expression system using ser/thr-11 peptide as substrate measured after 1 hr by Z'-Lyte assay | B | 5.83 | pIC50 | 1480 | nM | IC50 | Medchemcomm (2018) 9: 1472-1490 [PMID:30288222] |
ChEMBL | Inhibition of GST-fused human recombinant CK2alpha expressed in Escherichia coli HMS174 (DE3) | B | 6.05 | pIC50 | 900 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2920-2923 [PMID:19414254] |
ChEMBL | Inhibition of human recombinant casein kinase 2 subunit alpha expressed in Escherichia coli BL21 (DE3) assessed as [32P] incorporation by liquid scintillation counting | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem (2009) 17: 1573-1578 [PMID:19168362] |
ChEMBL | Inhibition of Zea mays CK2alpha | B | 6.3 | pIC50 | 500 | nM | IC50 | Biochem J (2003) 374: 639-646 [PMID:12816539] |
ChEMBL | Inhibition of human CK2alpha using RRRDDDSDDD peptide substrate by P81 filter-binding assay | B | 6.49 | pIC50 | 320 | nM | IC50 | Eur J Med Chem (2014) 84: 364-374 [PMID:25036794] |
casein kinase 2, beta polypeptide subunit/casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II alpha/beta in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038477] [GtoPdb: 1551, 1549] [UniProtKB: P67870, P68400] | ||||||||
ChEMBL | Binding affinity to recombinant human CK2alpha/beta expressed in Escherichia coli by surface plasmon resonance analysis | B | 6.1 | pKd | 790 | nM | Kd | Bioorg Med Chem (2018) 26: 3953-3957 [PMID:29934219] |
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 | 5.36 | pIC50 | 4360 | nM | IC50 | J Med Chem (2018) 61: 9791-9810 [PMID:29985601] |
ChEMBL | Inhibition of DYRK1a | B | 6 | pIC50 | <1000 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
NS3 in Hepatitis C virus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293269] [UniProtKB: A3EZJ3] | ||||||||
ChEMBL | Inhibitory concentration against hepatitis C virus helicase | B | 4.7 | pIC50 | 20000 | nM | IC50 | J Med Chem (2005) 48: 1-20 [PMID:15633995] |
Casein kinase 2 in Rat [GtoPdb: 1548] | ||||||||
GtoPdb | - | - | 6.4 | pKi | 400 | nM | Ki | Biochem J (2003) 374: 639-46 [PMID:12816539] |
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]