Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T71266 | Target Info | |||
| Target Name | RAC-gamma serine/threonine-protein kinase (AKT3) | ||||
| Synonyms |
STK-2; RAC-PK-gamma; Protein kinase B gamma; Protein kinase Akt-3; PKBG; PKB gamma
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| Target Type | Successful Target | ||||
| Gene Name | AKT3 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 16 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
1-(1-{[4-(3-Phenylquinoxalin-2-yl)phenyl]methyl}piperidin-4-yl)-2,3-dihydro-1H-1,3-benzodiazol-2-one
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Investigative | Compound Info | ||
| Synonyms |
2,3-diphenylquinoxaline 5; CHEMBL260397; SCHEMBL5348455; BDBM15149; VU0449279-1; 3-[1-[[4-(3-phenylquinoxalin-2-yl)phenyl]methyl]piperidin-4-yl]-1H-benzimidazol-2-one
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-{1-[(4-{5-[(4-Hydroxyphenyl)methyl]-6-oxo-3-phenyl-1,6-dihydropyrazin-2-yl}phenyl)methyl]piperidin-4-yl}-2,3-dihydro-1H-1,3-benzodiazol-2-one
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Investigative | Compound Info | ||
| Synonyms |
pyrazinone 14d; CHEMBL3143723; BDBM15157
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-[1-({4-[7-(2-Methyl-2H-1,2,3,4-tetrazol-5-yl)-3-phenylquinoxalin-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 16f; CHEMBL180058; SCHEMBL5363861; BDBM15167
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-(1-{[4-(6-Oxo-3-phenyl-1,6-dihydropyrazin-2-yl)phenyl]methyl}piperidin-4-yl)-2,3-dihydro-1H-1,3-benzodiazol-2-one
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Investigative | Compound Info | ||
| Synonyms |
pyrazinone 14a; CHEMBL577792; SCHEMBL3980604; BDBM15151
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| 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
|
[2] | |||
| Compound Name |
1-{1-[(4-{6-[(4-Hydroxyphenyl)methyl]-5-oxo-3-phenyl-4,5-dihydropyrazin-2-yl}phenyl)methyl]piperidin-4-yl}-2,3-dihydro-1H-1,3-benzodiazol-2-one
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|
Investigative | Compound Info | ||
| Synonyms |
pyrazinone 13d; CHEMBL178133; BDBM15156
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-(1-{[4-(6-Methyl-5-oxo-3-phenyl-4,5-dihydropyrazin-2-yl)phenyl]methyl}piperidin-4-yl)-2,3-dihydro-1H-1,3-benzodiazol-2-one
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|
Investigative | Compound Info | ||
| Synonyms |
pyrazinone 13b; CHEMBL178397; SCHEMBL3978936; BDBM15152
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-[1-({4-[6-(2-Methyl-2H-1,2,3,4-tetrazol-5-yl)-3-phenylquinoxalin-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 16e; CHEMBL181419; SCHEMBL5260840; SCHEMBL5330758; BDBM15166
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-(1-{[4-(6-Benzyl-5-oxo-3-phenyl-4,5-dihydropyrazin-2-yl)phenyl]methyl}piperidin-4-yl)-2,3-dihydro-1H-1,3-benzodiazol-2-one
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Investigative | Compound Info | ||
| Synonyms |
pyrazinone 13c; CHEMBL180580; SCHEMBL3980608; BDBM15154
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-(1-{[4-(5-Oxo-3-phenyl-4,5-dihydropyrazin-2-yl)phenyl]methyl}piperidin-4-yl)-2,3-dihydro-1H-1,3-benzodiazol-2-one
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|
Investigative | Compound Info | ||
| Synonyms |
pyrazinone 13a; CHEMBL440560; SCHEMBL2436521; BDBM15150
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-[1-({4-[6-(Butan-2-yl)-5-oxo-3-phenyl-4,5-dihydropyrazin-2-yl]phenyl}methyl)piperidin-4-yl]-2,3-dihydro-1H-1,3-benzodiazol-2-one
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Investigative | Compound Info | ||
| Synonyms |
pyrazinone 13e; CHEMBL428861; SCHEMBL2435312; BDBM15158
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-[1-({4-[5-(Butan-2-yl)-6-oxo-3-phenyl-1,6-dihydropyrazin-2-yl]phenyl}methyl)piperidin-4-yl]-2,3-dihydro-1H-1,3-benzodiazol-2-one
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Investigative | Compound Info | ||
| Synonyms |
pyrazinone 14e; SCHEMBL2439485; SCHEMBL3979847; CHEMBL3143721; BDBM15159
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-[1-({4-[6-(2-Methylpropyl)-5-oxo-3-phenyl-4,5-dihydropyrazin-2-yl]phenyl}methyl)piperidin-4-yl]-2,3-dihydro-1H-1,3-benzodiazol-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL362016; pyrazinone 13f; SCHEMBL2437301; SCHEMBL2439564; BDBM15160
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| 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 ~ 50000 nM
|
[3] | |||
| Compound Name |
N-[[4-[2-(2-Aminopyridin-3-yl)-6-phenylimidazo[4,5-b]pyridin-3-yl]phenyl]methyl]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2177830; SCHEMBL2175106; BDBM50397779
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| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
N-[[4-[2-(2-Aminopyridin-3-yl)-6-cyclopentylimidazo[4,5-b]pyridin-3-yl]phenyl]methyl]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2177826; SCHEMBL2176642; BDBM50397785
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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, 3 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
N-[6-[[(2R)-6-Amino-1-[[6-[[(2R)-1-[[(2R)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-6-oxohexyl]amino]-1-oxohexan-2-yl]amino]-6-oxohexyl]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1077598; BDBM50311402
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| Activity |
IC50 = 360000 nM
|
[5] | |||
| Compound Name |
4-[[6-[[(2R)-6-Amino-1-[[6-[[(2R)-1-[[(2R)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-6-oxohexyl]amino]-1-oxohexan-2-yl]amino]-6-oxohexyl]carbamoylamino]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1077600; BDBM50311404
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| Activity |
IC50 = 900000 nM
|
[5] | |||
| Compound Name |
6-{[(2S,3S,4R,5R)-5-(6-Amino-9H-purin-9-yl)-3,4-dihydroxyoxolan-2-yl]formamido}hexanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL495766; BDBM27223; ARC-1031; ARC-1031, 3
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| Activity |
IC50 > 1000000 nM
|
[6] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors. Bioorg Med Chem Lett. 2005 Feb 1;15(3):761-4. | ||||
| REF 2 | 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 3 | Rapid assembly of diverse and potent allosteric Akt inhibitors. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2211-4. | ||||
| REF 4 | Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors. J Med Chem. 2012 Jun 14;55(11):5291-310. | ||||
| REF 5 | Effect of the structure of adenosine mimic of bisubstrate-analog inhibitors on their activity towards basophilic protein kinases. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6098-101. | ||||
| REF 6 | Structural analysis of ARC-type inhibitor (ARC-1034) binding to protein kinase A catalytic subunit and rational design of bisubstrate analogue inhi... J Med Chem. 2009 Jan 22;52(2):308-21. | ||||
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