TBBt [Ligand Id: 9372] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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 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]
