Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T23995 | Target Info | |||
| Target Name | Protein kinase C theta (PRKCQ) | ||||
| Synonyms |
Protein kinase C theta type; PRKCT; NPKC-theta
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| Target Type | Clinical trial Target | ||||
| Gene Name | PRKCQ | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 6 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
8-Bromo-4-(3-chloro-4-fluoroanilino)-6-[(1-methylimidazol-4-yl)methylamino]quinoline-3-carbonitrile
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Investigative | Compound Info | ||
| Synonyms |
Cyanoquinoline, 44; BMCL193485 Compound 3a; CHEMBL230761; SCHEMBL2278592; BDBM21933
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-(3-(8-(Pyridin-4-ylmethylamino)imidazo[1,2-a]pyrazin-6-yl)phenyl)-3-(3-(trifluoromethyl)phenyl)urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1081198; SCHEMBL5480112; BDBM50312153
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| Activity |
IC50 = 50000 nM
|
[2] | |||
| Compound Name |
9-(Oxetan-3-ylamino)-3,5-dihydro-1H-[1,2,4]triazino[3,4-c][1,4]benzoxazin-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3356446; BDBM50053778
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
N-(2-Oxo-3,5-dihydro-1H-[1,2,4]triazino[3,4-c][1,4]benzoxazin-9-yl)-2-piperidin-4-ylacetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3356460; BDBM50049447
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
9-(Azetidin-3-ylamino)-1-phenyl-3,5-dihydro-1H-[1,2,4]triazino[3,4-c][1,4]benzoxazin-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3356463; BDBM50049431
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
Xanthohumol
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Investigative | Compound Info | ||
| Synonyms |
UNII-T4467YT1NT; T4467YT1NT; 2',4,4'-trihydroxy-6'-methoxy-3'-prenylchalcone; XANTHOHUMO; 2',4,4'-Trihydroxy-3'-prenyl-6'-methoxychalcone; SCHEMBL143683; CHEMBL253896; MEGxp0_000104; ACon1_001634; DTXSID00893171; Xanthohumol(Random Configuration); HMS3886H19; BCP18498; ZINC5158937; 0397AC; BDBM50384998; LMPK12120294; MFCD00210576; s7889; AKOS016010098; CCG-268086; DB15359; MCULE-7307777782; SMP2_000278; NCGC00180304-01; AC-31276; BS-17392; SC-11144; W2672; C16417; Q408088; BRD-K77390737-001-01-6; Q27166535; Xanthohumol, primary pharmaceutical reference standard; Xanthohumol from hop (Humulus lupulus), >=96% (HPLC)
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| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 1 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
3,5-Dihydro[1,2,4]triazino[3,4-C][1,4]benzoxazin-2(1h)-One
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1968515; (1,2,4)Triazino(3,4-c)(1,4)benzoxazin-2(1H)-one, 3,5-dihydro-; 3,5-Dihydro-(1,2,4)triazino(3,4-c)(1,4)benzoxazin-2(1H)-one; Kinome_3625; 3,5-dihydro-1H-[1,2,4]triazino[3,4-c][1,4]benzoxazin-2-one; SCHEMBL15798857; DTXSID60161121; BDBM50049435; ZINC19926414; Q27453440
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| Activity |
IC50 = 453000 nM
|
[3] | |||
| References | Top | ||||
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| REF 1 | Inhibitors of tumor progression loci-2 (Tpl2) kinase and tumor necrosis factor alpha (TNF-alpha) production: selectivity and in vivo antiinflammatory activity of novel 8-substituted-4-anilino-6-aminoquinoline-3-carbonitriles. J Med Chem. 2007 Sep 20;50(19):4728-45. | ||||
| REF 2 | Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6991-5. | ||||
| REF 3 | Discovery of selective and orally bioavailable protein kinase C (PKC) inhibitors from a fragment hit. J Med Chem. 2015 Jan 8;58(1):222-36. | ||||
| REF 4 | Inverse Virtual Screening allows the discovery of the biological activity of natural compounds. Bioorg Med Chem. 2012 Jun 1;20(11):3596-602. | ||||
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