Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T71374 | Target Info | |||
| Target Name | Polo-like kinase 4 (PLK4) | ||||
| Synonyms |
Serine/threonine-protein kinase Sak; Serine/threonine-protein kinase PLK4; Serine/threonine-protein kinase 18; STK18; SAK; PLK-4
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| Target Type | Literature-reported Target | ||||
| Gene Name | PLK4 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 3 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
N-Cyclopropyl-2-methyl-4-(2-phenoxy-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)pyrazolo[1,5-a][1,3,5]triazin-8-yl)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3819210; CFI-401980; SCHEMBL15739891; BDBM50183019
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| Activity |
IC50 ~ 50000 nM
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[1] | |||
| Compound Name |
(2'R,3R)-2'-(1H-Indazol-6-yl)spiro[1H-indole-3,1'-cyclopropane]-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3353339; SCHEMBL9946247; BDBM50044661
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| 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
|
[3] | |||
| References | Top | ||||
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| REF 1 | Discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazin-8-yl)benzamides as novel, highly potent and selective, orally bioavailable inhibitors of Tyrosine Threonine Kinase, TTK. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3562-6. | ||||
| REF 2 | The Discovery of Polo-Like Kinase 4 Inhibitors: Design and Optimization of Spiro[cyclopropane-1,3'[3H]indol]-2'(1'H)-ones as Orally Bioavailable Antitumor Agents. J Med Chem. 2015 Jan 8;58(1):130-46. | ||||
| REF 3 | 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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