Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T51565 | Target Info | |||
| Target Name | Casein kinase II alpha (CSNK2A1) | ||||
| Synonyms |
Protein kinase CK2; Casein kinase II subunit alpha; CK2A1; CK II alpha; CK II
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| Target Type | Clinical trial Target | ||||
| Gene Name | CSNK2A1 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 24 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
aloisine A
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Investigative | Compound Info | ||
| Synonyms |
ALOISINE A; 4-(7-butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl)phenol; 496864-16-5; RP107; 6-PHENYL[5H]PYRROLO[2,3-B]PYRAZINE; CHEMBL75680; 7-n-Butyl-6-(4-hydroxyphenyl)[5H]pyrrolo[2,3-b]pyrazine; RP-107; ALH; 4-{7-butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl}phenol; 1ung; SCHEMBL80147; BDBM7377; GTPL5924; AC1NS169; 4-(7-Butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl)-phenol; CHEBI:93641; CTK8D4068; DTXSID30416115; HMS3229A14; RM-39; BCP26893; ZINC2540737; ACT06534; IN1539; HSCI1_000219; MFCD04973541; AKOS005145972; CCG-206814; DB07364; RTC-063070; AJ-39131
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4-[(1,3-Dimethylpyrazolo[4,3-e][1,2,4]triazin-5-yl)amino]benzenesulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3237855; BDBM50004342
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
N-[4-(1,4-Diazepan-1-ylsulfonyl)phenyl]-1,3-dimethylpyrazolo[4,3-e][1,2,4]triazin-5-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3237852; BDBM50004350
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
Methyl 5-(3-chloro-4-fluoroanilino)pyrimido[4,5-c]quinoline-8-carboxylate
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL4970671; CHEMBL3700567; BDBM165639; US9062043, Table 20b, Compound 8
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
4-[(1,3-Dimethylpyrazolo[4,3-e][1,2,4]triazin-5-yl)amino]-N-(2-morpholin-4-ylethyl)benzenesulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3237857; BDBM50004344
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
Methyl 5-(3-methoxyanilino)benzo[c][2,6]naphthyridine-8-carboxylate
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL4972158; CHEMBL3700411; BDBM165345; US9062043, Table 20b, Compound 7; US9062043, Table 13, Compound 11
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
N-(2-Aminoethyl)-4-[(1,3-dimethylpyrazolo[4,3-e][1,2,4]triazin-5-yl)amino]benzenesulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3237854; BDBM50004340
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
1,3-Dimethyl-N-(4-pyrrolidin-1-ylsulfonylphenyl)pyrazolo[4,3-e][1,2,4]triazin-5-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3233061; BDBM50004351
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
4-[(1,3-Dimethylpyrazolo[4,3-e][1,2,4]triazin-5-yl)amino]-N-(1-hydroxy-3-methylbutan-2-yl)benzenesulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3237856; BDBM50004343
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
N-Phenyl-7-(1H-1,2,4-triazol-5-yl)thieno[3,2-c]quinolin-4-amine
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL1930346; CHEMBL3700566; BDBM165627; US9062043, Table 20, Compound 8
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| Activity |
IC50 = 50000 nM
|
[3] | |||
| Compound Name |
4-[2-(Dimethylamino)ethylamino]thieno[3,2-c]quinoline-7-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2689471; CHEMBL3700382; BDBM165217; US9062043, Table 11, Compound 6; US9062043, Table 14, Compound 6; US9062043, Table 20, Compound 6
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| Activity |
IC50 = 50000 nM
|
[3] | |||
| Compound Name |
N-(2,3-Dihydroxypropyl)-4-[(1,3-dimethylpyrazolo[4,3-e][1,2,4]triazin-5-yl)amino]benzenesulfonamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3237858; BDBM50004345
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
4-[(1,3-Dimethylpyrazolo[4,3-e][1,2,4]triazin-5-yl)amino]-N-(2-hydroxyethyl)benzenesulfonamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3237851; BDBM50004349
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|
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
4-[5-(4-Methoxybenzoylamino)-thiazole-2-yl]benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2087026; SCHEMBL12525990; BDBM50420566; 4-[5-[(4-methoxybenzoyl)amino]-1,3-thiazol-2-yl]benzoic acid
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| Activity |
IC50 = 50000 nM
|
[4] | |||
| Compound Name |
1,3-Dimethyl-N-[4-(4-methylpiperazin-1-yl)sulfonylphenyl]pyrazolo[4,3-e][1,2,4]triazin-5-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3237848; BDBM50004346
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
5-[2-(Dimethylamino)ethylamino]benzo[c][2,6]naphthyridine-8-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
SCHEMBL4975734; CHEMBL1652698; BDBM165336; US9062043, Table 13, Compound 2; US9062043, Table 20b, Compound 2
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
4-[5-(4-Methoxybenzoylamino)-1,3,4-oxadiazole-2-yl]benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2087024; SCHEMBL12525970; BDBM50420564; 4-[5-[(4-methoxybenzoyl)amino]-1,3,4-oxadiazol-2-yl]benzoic acid
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| Activity |
IC50 = 74000 nM
|
[4] | |||
| Compound Name |
N-(4-Methyl-3-sulfamoylphenyl)-5-nitro-1H-indazole-3-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3823680; BDBM50185767; ZINC40079601; AKOS008121094; MCULE-4295326590
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| Activity |
IC50 = 79300 nM
|
[5] | |||
| Compound Name |
4-{1-[(Benzyloxy)methyl]-1H-indol-3-yl}-3-(3,4,5-trimethoxyphenyl)-1,5-dihydro-2H-pyrrole-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL453336; SCHEMBL13961687; BDBM50243977; 3-[1-(phenylmethoxymethyl)indol-3-yl]-4-(3,4,5-trimethoxyphenyl)-1,2-dihydropyrrol-5-one
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| Activity |
IC50 = 93000 nM
|
[6] | |||
| Compound Name |
N-Methyl-4-(2-(piperidin-4-yl)-5-(3-(trifluoromethyl)phenyl)-1H-imidazol-4-yl)pyrimidin-2-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL489344; SCHEMBL4936886; BDBM50260228; N-methyl-4-[2-piperidin-4-yl-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyrimidin-2-amine
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
4-(4-(4-Fluorophenyl)-2-(4-methylcyclohexyl)-1H-imidazol-5-yl)pyridine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL523938; BDBM50260229
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
Chembl4276946
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Investigative | Compound Info | ||
| Synonyms |
GTPL9965; compound 3a [Pipionne et al, 2018]; 1-[5-amino-4-(3,4-dichlorophenyl)-3-methyl-1H-pyrazol-1-yl]ethan-1-one
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
5-(1H-Indol-3-yl)-3-(3,4,5-trimethoxyphenyl)-1H-pyrazin-2-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3358966
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| Activity |
IC50 ~ 100000 nM
|
[9] | |||
| Compound Name |
N-(3-Cyclopropaneamidophenyl)-1H-indazole-3-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3823185; BDBM50185765; ZINC31136924; AKOS034195488; MCULE-5094795701; Z333267120
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| Activity |
IC50 = 102600 nM
|
[5] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 4 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
N-(4-Fluoro-1H-indazol-3-yl)-2,3-dihydro-1-benzofuran-5-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3823658; BDBM50185756; ZINC58157881; AKOS034698850; MCULE-9760043685; Z915601596
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| Activity |
IC50 > 200000 nM
|
[5] | |||
| Compound Name |
5-Nitro-N-phenyl-1H-indazole-3-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3822582; 1h-indazole-3-carboxamide,5-nitro-n-phenyl-; SCHEMBL5945664; BDBM50185768; ZINC28026601; AKOS034167134; MCULE-5141312660; Z317165714
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| Activity |
IC50 > 200000 nM
|
[5] | |||
| Compound Name |
N-(2-Methyl-1H-indol-5-yl)-1H-indazole-3-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3823750; BDBM50185758; ZINC32828573; AKOS034254887; MCULE-2771188480; Z372876602
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| Activity |
IC50 > 200000 nM
|
[5] | |||
| Compound Name |
N-[3-(5-Ethyl-1,3,4-oxadiazol-2-yl)phenyl]-1H-indazole-3-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3823560; BDBM50185760; AKOS033236398; ZINC175379852; Z1286533456
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| Activity |
IC50 > 200000 nM
|
[5] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8. | ||||
| REF 2 | Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines. Eur J Med Chem. 2014 May 6;78:217-24. | ||||
| REF 3 | US patent application no. 9062043B2, Fused tricyclic compounds as serine-threonine protein kinase and PARP modulators | ||||
| REF 4 | Structure-based design of novel potent protein kinase CK2 (CK2) inhibitors with phenyl-azole scaffolds. J Med Chem. 2012 Mar 22;55(6):2899-903. | ||||
| REF 5 | Enriching screening libraries with bioactive fragment space. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3594-7. | ||||
| REF 6 | Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors. J Med Chem. 2008 Jul 10;51(13):3814-24. | ||||
| REF 7 | Hepatitis C virus NS5A is a direct substrate of casein kinase I-alpha, a cellular kinase identified by inhibitor affinity chromatography using specific NS5A hyperphosphorylation inhibitors. J Biol Chem. 2007 Feb 23;282(8):5536-44. | ||||
| REF 8 | N-Acetyl-3-aminopyrazoles block the non-canonical NF-kB cascade by selectively inhibiting NIK. Medchemcomm. 2018 Apr 12;9(6):963-968. | ||||
| REF 9 | Optimization of potent DFG-in inhibitors of platelet derived growth factor receptor (PDGF-R) guided by water thermodynamics. J Med Chem. 2015 Jan 8;58(1):170-82. | ||||
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