Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T64682 | Target Info | |||
| Target Name | Serine/threonine-protein kinase Sgk1 (SGK1) | ||||
| Synonyms |
Serum/glucocorticoid-regulated kinase 1; SGK1
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| Target Type | Clinical trial Target | ||||
| Gene Name | SGK1 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 24 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
A-432411
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Investigative | Compound Info | ||
| Synonyms |
43A; (3Z)-6-(4-HYDROXY-3-METHOXYPHENYL)-3-(1H-PYRROL-2-YLMETHYLENE)-1,3-DIHYDRO-2H-INDOL-2-ONE; 2ayp; indolinone analog 13; A-432411; CHEMBL202930; SCHEMBL6674605; BDBM14649; DB07078; 29690-EP2311842A2; 29690-EP2289868A1; 29690-EP2289894A2; (3Z)-6-(4-hydroxy-3-methoxyphenyl)-3-(1H-pyrrol-2-ylmethylidene)-1H-indol-2-one; (3Z)-6-(4-hydroxy-3-methoxyphenyl)-3-(1H-pyrrol-2-ylmethylidene)-2,3-dihydro-1H-indol-2-one
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
Ro-4396686
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL5809947; CHEMBL606964
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| Activity |
IC50 ~ 125000 nM
|
[2] | |||
| Compound Name |
1-[1-({4-[3-Phenyl-7-(2H-1,2,3,4-tetrazol-5-yl)quinoxalin-2-yl]phenyl}methyl)piperidin-4-yl]-2,3-dihydro-1H-1,3-benzodiazol-2-one
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Investigative | Compound Info | ||
| Synonyms |
quinoxaline 16d; CHEMBL408151; SCHEMBL5257848; BDBM15165
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
9-Phenyl-8-(4-((4-(5-(pyridin-2-yl)-1H-1,2,4-triazol-3-yl)piperidin-1-yl)methyl)phenyl)-[1,2,4]triazolo[3,4-f][1,6]naphthyridine-3-thiol
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL502854; SCHEMBL2279829; BDBM50256716
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
3-((4-Methylpiperazin-1-yl)methyl)-9-phenyl-8-(4-((4-(5-(pyridin-2-yl)-1H-1,2,4-triazol-3-yl)piperidin-1-yl)methyl)phenyl)-[1,2,4]triazolo[3,4-f][1,6]naphthyridine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL446779; SCHEMBL2276290; BDBM50256721
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
N-Methyl-6-phenyl-7-[4-({4-[5-(pyridin-2-yl)-4H-1,2,4-triazol-3-yl]piperidin-1-yl}methyl)phenyl]pyrido[2,3-d]pyrimidin-2-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL252857; Pyridopyrimidine, 14d; SCHEMBL3889646; BDBM24880
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| Activity |
IC50 ~ 50000 nM
|
[5] | |||
| Compound Name |
3-(5-Chloro-2-{[1-(dimethylamino)propan-2-yl]oxy}phenyl)-1-(5-cyanopyrazin-2-yl)urea
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Investigative | Compound Info | ||
| Synonyms |
urea-based inhibitor 2d; A-690002; CHEMBL425904; SCHEMBL5865729; BDBM14829; 1-[5-chloro-2-[1-(dimethylamino)propan-2-yloxy]phenyl]-3-(5-cyanopyrazin-2-yl)urea; (+/-)1-[5-Chloro-2-(2-dimethylamino-1-methyl-ethyloxy)-phenyl]-3-(5-cyano-pyrazin-2-yl)-urea
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| Activity |
IC50 ~ 50000 nM
|
[6] | |||
| Compound Name |
2-((9-Phenyl-8-(4-((4-(5-(pyridin-2-yl)-1H-1,2,4-triazol-3-yl)piperidin-1-yl)methyl)phenyl)-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-yl)methylamino)ethanol
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL442919; SCHEMBL2280576; BDBM50256722
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
3-(Chloromethyl)-9-phenyl-8-(4-((4-(5-(pyridin-2-yl)-1H-1,2,4-triazol-3-yl)piperidin-1-yl)methyl)phenyl)-[1,2,4]triazolo[3,4-f][1,6]naphthyridine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL508861; BDBM50256720
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| Activity |
IC50 ~ 50000 nM
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[4] | |||
| Compound Name |
1-(9-Phenyl-8-(4-((4-(5-(pyridin-2-yl)-1H-1,2,4-triazol-3-yl)piperidin-1-yl)methyl)phenyl)-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-yl)urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL509747; BDBM50256717
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
1-[1-({4-[3-Phenyl-6-(2H-1,2,3,4-tetrazol-5-yl)quinoxalin-2-yl]phenyl}methyl)piperidin-4-yl]-2,3-dihydro-1H-1,3-benzodiazol-2-one
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Investigative | Compound Info | ||
| Synonyms |
quinoxaline 16c; CHEMBL271091; SCHEMBL5308842; SCHEMBL14500992; BDBM15164
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
3-{5-Chloro-2-[(3-methyloxetan-3-yl)methoxy]phenyl}-1-(5-cyanopyrazin-2-yl)urea
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Investigative | Compound Info | ||
| Synonyms |
urea-based inhibitor 2e; A-641397; CHEMBL192161; BDBM14830; (+/-)1-[5-Chloro-2-(3-methyl-oxetan-3-ylmethoxy)-phenyl]-3-(5-cyano-pyrazin-2-yl)-urea
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| Activity |
IC50 ~ 50000 nM
|
[6] | |||
| Compound Name |
2-(4-{[4-(2-Oxo-2,3-dihydro-1H-1,3-benzodiazol-1-yl)piperidin-1-yl]methyl}phenyl)-3-phenylquinoxaline-6-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
quinoxaline 16a; CHEMBL272292; SCHEMBL5306880; BDBM15162
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
9-Phenyl-8-(4-((4-(5-(pyridin-2-yl)-1H-1,2,4-triazol-3-yl)piperidin-1-yl)methyl)phenyl)-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL499555; SCHEMBL2281158; BDBM50256714
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
1,2,4-Triazolo[3,4-f][1,6]naphthyridine, 9-phenyl-8-[4-[[4-[5-(2-pyridinyl)-1H-1,2,4-triazol-3-yl]-1-piperidinyl]methyl]phenyl]-
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL447328; SCHEMBL2278984; BDBM50256718; ZINC43202641
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
2-[9-(4-Amino-3-methoxyphenyl)-6-oxo-5,11-dihydrobenzo[b][1,4]benzodiazepin-3-yl]-N-(4-morpholin-4-ylphenyl)acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL395080; BDBM50218700
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| Activity |
IC50 ~ 50000 nM
|
[7] | |||
| Compound Name |
Merck-22-6
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL258696; SCHEMBL5310814; CTK5B2993; DTXSID50437084; SYN1118; C40H43N7O2; BDBM50373459; ZINC29049547; NCGC00345840-01; NCGC00345840-02
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
3-(4-((4-(2-Oxo-2,3-dihydro-1H-benzo[D]imidazol-1-YL)piperidin-1-YL)methyl)phenyl)-2-phenylquinoxaline-6-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
quinoxaline 16b; CHEMBL273160; SCHEMBL5311901; BDBM15163; FD7287
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
3-Methyl-9-phenyl-8-(4-((4-(5-(pyridin-2-yl)-1H-1,2,4-triazol-3-yl)piperidin-1-yl)methyl)phenyl)-[1,2,4]triazolo[3,4-f][1,6]naphthyridine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL445464; SCHEMBL2281488; BDBM50256719
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
(3Z)-6-(4-Hydroxy-3-methoxyphenyl)-3-{1H-pyrrolo[2,3-b]pyridin-3-ylmethylidene}-2,3-dihydro-1H-indol-2-one
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Investigative | Compound Info | ||
| Synonyms |
indolinone analog 28; CHEMBL383316; SCHEMBL6671445; BDBM14664; (3Z)-6-(4-hydroxy-3-methoxyphenyl)-3-(1H-pyrrolo[2,3-b]pyridin-3-ylmethylidene)-1H-indol-2-one
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
N-[2-(Diethylamino)ethyl]-2-[4-[[4-(2-oxo-3H-benzimidazol-1-yl)piperidin-1-yl]methyl]phenyl]-3-phenylquinoxaline-6-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL270444; SCHEMBL5315812; BDBM50374520
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
9-Phenyl-8-(4-((4-(5-(pyridin-2-yl)-1H-1,2,4-triazol-3-yl)piperidin-1-yl)methyl)phenyl)-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-ol
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL506077; SCHEMBL2283492; BDBM50256715
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
N-(4-Methoxyphenyl)-2-[4-(4-nitrophenyl)-1,3-thiazol-2-yl]acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2070409; CBKinase1_007666; CBKinase1_020066; ZINC5063718; BDBM50390256; AKOS001145721; MCULE-5864202536; SR-01000280197; SR-01000280197-1; BRD-K21663961-001-01-0; N-(4-methoxyphenyl)-2-[4-(4-nitrophenyl)thiazol-2-yl]acetamide
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| Activity |
IC50 = 60000 nM
|
[8] | |||
| Compound Name |
(+)-(1R,3R)-1-(3-Hydroxy-cyclopentyl)-3-(4-methoxy-phenyl)-7-phenylamino-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1952210; Ro-4383596; SCHEMBL5772118; BDBM50363957; 7-anilino-1-[(1R,3R)-3-hydroxycyclopentyl]-3-(4-methoxyphenyl)-4H-pyrimido[4,5-d]pyrimidin-2-one
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| Activity |
IC50 ~ 125000 nM
|
[9] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 1 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
2-[4-(3-Phenylquinoxalin-2-yl)phenyl]propan-2-amine
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Investigative | Compound Info | ||
| Synonyms |
Akt-I-1,2; alpha,alpha-Dimethyl-4-(3-phenyl-2-quinoxalinyl)benzenemethanamine; 2,3-diphenylquinoxaline 1; CHEMBL362455; SCHEMBL4605370; BDBM15148; DTXSID00431315; BCPP000420; ZINC14957904; BCP9000267; NCGC00345823-01; NCGC00345823-02; DB-070790; FT-0747552; 382D488
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| Activity |
IC50 > 250000 nM
|
[10] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2-ones as novel checkpoint 1 inhibitors. Bioorg Med Chem Lett. 2006 Jan 15;16(2):421-6. | ||||
| REF 2 | Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3. | ||||
| REF 3 | Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity. Bioorg Med Chem Lett. 2008 Jan 1;18(1):49-53. | ||||
| REF 4 | Allosteric inhibitors of Akt1 and Akt2: discovery of [1,2,4]triazolo[3,4-f][1,6]naphthyridines with potent and balanced activity. Bioorg Med Chem Lett. 2009 Feb 1;19(3):834-6. | ||||
| REF 5 | Development of pyridopyrimidines as potent Akt1/2 inhibitors. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1274-9. | ||||
| REF 6 | 1-(5-Chloro-2-alkoxyphenyl)-3-(5-cyanopyrazin-2-yl)ureas [correction of cyanopyrazi] as potent and selective inhibitors of Chk1 kinase: synthesis, preliminary SAR, and biological activities. J Med Chem. 2005 May 5;48(9):3118-21. | ||||
| REF 7 | Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors. J Med Chem. 2007 Aug 23;50(17):4162-76. | ||||
| REF 8 | Identification of a novel serum and glucocorticoid regulated kinase-1 (SGK1) ligand from virtual screening. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5675-8. | ||||
| REF 9 | RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation. Bioorg Med Chem. 2005 Aug 15;13(16):4835-41. | ||||
| REF 10 | 2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites. J Med Chem. 2014 Sep 25;57(18):7485-98. | ||||
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