Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T94621 | Target Info | |||
| Target Name | RAC-beta serine/threonine-protein kinase (AKT2) | ||||
| Synonyms |
RAC-PK-beta; Protein kinase B beta; Protein kinase Akt-2; PKB beta
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| Target Type | Literature-reported Target | ||||
| Gene Name | AKT2 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 30 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
6-(4-{[4-(1H-1,3-Benzodiazol-2-yl)piperidin-1-yl]methyl}phenyl)-5-phenylpyridine-3-carbonitrile
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|
Investigative | Compound Info | ||
| Synonyms |
cyanopyridine 7e; CHEMBL369094; SCHEMBL1938245; BDBM15176; 6-[4-[[4-(1H-benzimidazol-2-yl)piperidin-1-yl]methyl]phenyl]-5-phenylpyridine-3-carbonitrile
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| 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 |
6-(4-{[4-(6-Methyl-1H-1,3-benzodiazol-2-yl)piperidin-1-yl]methyl}phenyl)-5-phenylpyridine-3-carbonitrile
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|
Investigative | Compound Info | ||
| Synonyms |
cyanopyridine 7d; CHEMBL181927; SCHEMBL1939361; BDBM15175
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
({4-[3-Phenyl-5-(1H-1,2,3,4-tetrazol-5-yl)pyridin-2-yl]phenyl}methyl)({[4-(1,2,3-thiadiazol-4-yl)phenyl]methyl})amine
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Investigative | Compound Info | ||
| Synonyms |
tetrazolylypyridine 8b; CHEMBL425155; SCHEMBL1652607; BDBM15180
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
2-[1-({4-[3-Phenyl-5-(1H-1,2,3,4-tetrazol-5-yl)pyridin-2-yl]phenyl}methyl)piperidin-4-yl]-1H-1,3-benzodiazole
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Investigative | Compound Info | ||
| Synonyms |
tetrazolylypyridine 8e; CHEMBL178872; SCHEMBL1939708; BDBM15183; 2-[1-[[4-[3-phenyl-5-(2H-tetrazol-5-yl)pyridin-2-yl]phenyl]methyl]piperidin-4-yl]-1H-benzimidazole
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-(1-{[4-(2-Phenylquinolin-3-yl)phenyl]methyl}piperidin-4-yl)-2,3-dihydro-1H-1,3-benzodiazol-2-one
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Investigative | Compound Info | ||
| Synonyms |
quinoline 6; CHEMBL178349; SCHEMBL5401310; BDBM15171; 3-[1-[[4-(2-phenylquinolin-3-yl)phenyl]methyl]piperidin-4-yl]-1H-benzimidazol-2-one
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
6-Fluoro-2-[1-({4-[3-phenyl-5-(1H-1,2,3,4-tetrazol-5-yl)pyridin-2-yl]phenyl}methyl)piperidin-4-yl]-1H-1,3-benzodiazole
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Investigative | Compound Info | ||
| Synonyms |
tetrazolylypyridine 8c; CHEMBL181730; SCHEMBL1941284; BDBM15181
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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
|
[2] | |||
| Compound Name |
6-(4-{[4-(2-Oxo-2,3-Dihydro-1H-benzimidazol-1-yl)piperidin-1-yl]methyl}phenyl)-5-phenylnicotinonitrile
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|
Investigative | Compound Info | ||
| Synonyms |
cyanopyridine 7a; CHEMBL255212; SCHEMBL1938575; BDBM15172; 6-[4-[[4-(2-oxo-3H-benzimidazol-1-yl)piperidin-1-yl]methyl]phenyl]-5-phenylpyridine-3-carbonitrile
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-[1-({4-[3-Phenyl-5-(1H-1,2,3,4-tetrazol-5-yl)pyridin-2-yl]phenyl}methyl)piperidin-4-yl]-1H-1,3-benzodiazole
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|
Investigative | Compound Info | ||
| Synonyms |
tetrazolylypyridine 8f; CHEMBL178445; SCHEMBL1939613; BDBM15184; 1-[1-[[4-[3-phenyl-5-(2H-tetrazol-5-yl)pyridin-2-yl]phenyl]methyl]piperidin-4-yl]benzimidazole
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
6-(4-{[4-(2-Methyl-1H-1,3-benzodiazol-1-yl)piperidin-1-yl]methyl}phenyl)-5-phenylpyridine-3-carbonitrile
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Investigative | Compound Info | ||
| Synonyms |
cyanopyridine 7g; CHEMBL425338; SCHEMBL1940089; BDBM15178; 6-[4-[[4-(2-methylbenzimidazol-1-yl)piperidin-1-yl]methyl]phenyl]-5-phenylpyridine-3-carbonitrile
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
2-Methyl-1-[1-({4-[3-phenyl-5-(1H-1,2,3,4-tetrazol-5-yl)pyridin-2-yl]phenyl}methyl)piperidin-4-yl]-1H-1,3-benzodiazole
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Investigative | Compound Info | ||
| Synonyms |
tetrazolylypyridine 8g; CHEMBL369532; SCHEMBL1938164; BDBM15185
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
5-Phenyl-6-[4-[[[4-(thiadiazol-4-yl)phenyl]methylamino]methyl]phenyl]pyridine-3-carbonitrile
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|
Investigative | Compound Info | ||
| Synonyms |
cyanopyridine 7b; CHEMBL360333; SCHEMBL1653331; BDBM15173; 5-phenyl-6-[4({[4-(1,2,3-thiadiazol-4-yl)benzyl]amino}methyl)phenyl]nicotinonitrile; 5-phenyl-6-[4-({[4-(1,2,3-thiadiazol-4-yl)benzyl]amino}methyl)phenyl]nicotinonitrile
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
6-(4-{[4-(6-Fluoro-1H-benzimidazol-2-yl)piperidin-1-yl]methyl}phenyl)-5-phenylnicotinonitrile
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|
Investigative | Compound Info | ||
| Synonyms |
cyanopyridine 7c; CHEMBL368010; SCHEMBL1939898; BDBM15174
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|
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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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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| 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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|
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
1-(1-{[4-(3-Phenylquinolin-2-yl)phenyl]methyl}piperidin-4-yl)-2,3-dihydro-1H-1,3-benzodiazol-2-one
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|
Investigative | Compound Info | ||
| Synonyms |
quinoline 5; CHEMBL359864; SCHEMBL5351640; BDBM15170; 3-[1-[[4-(3-phenylquinolin-2-yl)phenyl]methyl]piperidin-4-yl]-1H-benzimidazol-2-one
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
6-(4-{[4-(1H-1,3-Benzodiazol-1-yl)piperidin-1-yl]methyl}phenyl)-5-phenylpyridine-3-carbonitrile
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|
Investigative | Compound Info | ||
| Synonyms |
cyanopyridine 7f; CHEMBL361391; SCHEMBL1938617; BDBM15177; 6-[4-[[4-(benzimidazol-1-yl)piperidin-1-yl]methyl]phenyl]-5-phenylpyridine-3-carbonitrile
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
6-Methyl-2-[1-({4-[3-phenyl-5-(1H-1,2,3,4-tetrazol-5-yl)pyridin-2-yl]phenyl}methyl)piperidin-4-yl]-1H-1,3-benzodiazole
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|
Investigative | Compound Info | ||
| Synonyms |
tetrazolylypyridine 8d; CHEMBL367601; SCHEMBL1938150; BDBM15182
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
1-[1-({4-[3-Phenyl-5-(1H-1,2,3,4-tetrazol-5-yl)pyridin-2-yl]phenyl}methyl)piperidin-4-yl]-2,3-dihydro-1H-1,3-benzodiazol-2-one
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|
Investigative | Compound Info | ||
| Synonyms |
tetrazolylypyridine 8a; CHEMBL270847; SCHEMBL1940025; BDBM15179
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|
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| 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 = 51000 nM
|
[3] | |||
| Compound Name |
6-(Piperidin-1-yl)-9H-purine
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Investigative | Compound Info | ||
| Synonyms |
6-piperidin-1-yl-7H-purine; 6-Piperidino-1-purine; MLS000104087; 6-(piperidin-1-yl)-7H-purine; 6-Piperidino-9H-purine; SMR000015510; 6-piperidylpurine; 6-piperidino-7H-purine; Oprea1_148697; Oprea1_788909; 6-(1-piperidinyl)-7H-purine; CHEMBL264666; IFLab1_000330; SCHEMBL3287249; SCHEMBL8939237; 6-(piperidin-1-yl)-1h-purine; BDBM37924; cid_3129049; CTK4E1115; 9H-Purine,6-(1-piperidinyl)-; DTXSID60389606; HMS1412O22; HMS2250I03; NSC20104; NSC-20104; STK844789; ZINC13151697; AKOS001428034; MCULE-6161586311; IDI1_008549; FT-0633920; ST50008286; Z277468448
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| Activity |
IC50 = 59000 nM
|
[4] | |||
| Compound Name |
6-(1,9-Diazaspiro[5.5]undecan-9-Yl)-9h-Purine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2420909; BDBM50439464; 9-(9H-purin-6-yl)-1,9-diazaspiro[5.5]undecane; Q27465376; SIJ
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| Activity |
IC50 = 66000 nM
|
[5] | |||
| Compound Name |
3,5-Dimethyl-4-phenyl-1H-pyrazole
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL540487; Phenyldimethylpyrazol; SCHEMBL873114; ZINC3091263; BDBM50414214; AKOS004902401; F2198-8628
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| Activity |
IC50 = 72000 nM
|
[6] | |||
| Compound Name |
3-Methyl-4-phenyl-1H-pyrazole
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Investigative | Compound Info | ||
| Synonyms |
3-Methyl-4-phenylpyrazole; 5-methyl-4-phenyl-1H-pyrazole; 3-Methyl-4-phenylpyrazol; CHEMBL228114; MFCD00051752; ACMC-1BRBB; Maybridge1_003313; 5-methyl-4-phenylpyrazole; pyrazole-based inhibitor 1; SCHEMBL105178; 3-methyl-4-phenyl-1H-pyrazol; 4-Phenyl-5-methyl-1H-pyrazole; BDBM16211; CTK3J4384; HMS550O13; DTXSID90160349; 1H-Pyrazole,3-methyl-4-phenyl-; 3-Methyl-4-phenyl-1H-pyrazole #; ALBB-006850; KS-00000NO5; ZINC4692749; 6627AA; ANW-72592; SBB048410; STK504166; AKOS000265029; AKOS015899729; AS06545; CM10492; CS-W016200; MCULE-1577784164; 3-METHYL-4-PHENYL-2H-PYRAZOLE; AK-33201; CD 09292; DB-063215; 3-Methyl-4-phenyl-1H-pyrazole, AldrichCPR; FT-0616095; ST50824692; Y-8098; 12T-0222; J-512860; J-640176; J-800178; Q27460932
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| Activity |
IC50 = 80000 nM
|
[7] | |||
| Compound Name |
7-Azaindole
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Investigative | Compound Info | ||
| Synonyms |
1H-Pyrrolo[2,3-b]pyridine; 1,7-Diazaindene; 7H-Pyrrolo[2,3-b]pyridine; 7-Aza-1-pyrindine; 1,7-Dideazapurine; 1H-PYRROLO(2,3-b)PYRIDINE; MFCD00005606; pyrrolo[2,3-b]pyridine; 7-aza-indole; UNII-QX4465NR9T; 7H-Pyrrolo(2,3-b)pyridine; 7-Azaindole, 98%; 1 h-pyrrolo[2,3:b]pyridine; QX4465NR9T; Pyrrolo(2,3-b)pyridine; WLN: T56 BM INJ; EINECS 205-981-0; NSC 67063; 7-azaindol; 7-aza indole; pyrrolo[b]pyridine; zlchem 221; PubChem7679; ACMC-20lk5f; ACMC-1CKM0; pyrrolo[2,3-b]-pyridine; NCIOpen2_000707; SCHEMBL17837; KSC202K2D; 1-H-pyrrolo[2,3-b]pyridine; 1H-pyrrolo(2,3-b)-pyridine; CHEMBL389685; DTXSID3075046; BDBM16223; CTK1A2521; CTK2J8336; ZLC0029; WT674; ACN-S002680; ACT02468; ALBB-006259; BCP26852; CS-B0516; KS-000002OI; NSC67063; NSC77951; STR01850; ANW-26142; BBL008683; HTS000456; MFCD00075874; NSC-67063; NSC-77951; SBB004295; SC1771; STK503791; ZINC15442276; AKOS000446848; AC-1215; AS07114; CM14215; LS21042; MCULE-6621126582; PB32078; PS-4533; QC-3424; NCGC00188278-01; AK-26735; BR-26735; SC-03043; SY001940; AB0005988; DB-016106; AM20070247; FT-0604377; P1117; ST51044413; EN300-25796; A-9500; C-8859; Z-9562; 38720-EP2272517A1; 38720-EP2292615A1; 38720-EP2295433A2; 38720-EP2303879A1; 38720-EP2311837A1; 72278-EP2272517A1; 72278-EP2308867A2; 72278-EP2308870A2; 271A636; 271-63-6 7-azaindole; Q27287542; F0001-0881
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| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
(3S,5E)-1-Methyl-3-(pyridin-2-ylmethyl)-5-(pyridin-2-ylmethylidene)piperidin-4-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2338335; BDBM50431025
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
(3R,5E)-1-Methyl-3-(pyridin-2-ylmethyl)-5-(pyridin-2-ylmethylidene)piperidin-4-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2338334; BDBM50431026
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
1-(8-Methyl-7H-purin-6-yl)piperidin-4-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL265194; BDBM50376073
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| Activity |
IC50 = 110000 nM
|
[4] | |||
| Compound Name |
4-Phenyl-1H-pyrazole
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Investigative | Compound Info | ||
| Synonyms |
4-Phenylpyrazole; 1H-Pyrazole, 4-phenyl-; Pyrazole, 4-phenyl-; 4-(C6H5)-pyrazole; CHEMBL390066; MFCD00462204; 4-Phenyl-1H-pyrazole #; pyrazole-based inhibitor 5; SCHEMBL82741; JMC514968 Compound 35; BDBM16215; CTK0H9678; DTXSID80144491; ABLOCK AB-12-2432; BCP09906; KS-00000P6I; ZINC3164652; AKOS005198822; AB06118; AS06546; CM10493; CS-W022231; MCULE-5589155043; NCGC00333584-01; AK-30224; BS-13375; SY028300; AB0134942; DB-058747; FT-0646841; EN300-07023; K-0273; AB01329407-02; J-515933; Z56940955
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| Activity |
IC50 = 135000 nM
|
[7] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 2 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
|
[9] | |||
| Compound Name |
3-Methyl-4-phenyl-1H-pyrazol-5-amine
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Investigative | Compound Info | ||
| Synonyms |
5-Methyl-4-phenyl-2H-pyrazol-3-ylamine; 5-amino-3-methyl-4-phenylpyrazole; 5-methyl-4-phenyl-1H-pyrazol-3-amine; 3-Amino-5-Methyl-4-Phenylpyrazole; 5-methyl-4-phenyl-2H-pyrazol-3-amine; UNII-OC0W48DG01; OC0W48DG01; 1H-Pyrazol-3-amine,5-methyl-4-phenyl-; 1H-Pyrazol-5-amine,3-methyl-4-phenyl-; 3-methyl-4-phenylpyrazole-5-ylamine; Pyrazole, 5-amino-3-methyl-4-phenyl-; 1H-Pyrazol-3-amine, 5-methyl-4-phenyl-; Maybridge3_005336; Oprea1_166909; MLS000718547; SCHEMBL544723; Pyrazole, 3(OR 5)-amino-5(OR 3)-methyl-4-phenyl-; CHEMBL1609052; CTK4G7923; CTK5B1468; DTXSID80975823; HMS1446C12; HMS2678A07; ALBB-006621; KS-00003KC6; ZINC8743937; BBL007578; CCG-48710; KM0404; MFCD00831955; SBB010561; STK161389; AKOS000265012; AKOS015898914; FS-1252; MCULE-5899288516; SB21940; IDI1_016723; 3-Amino-5-methyl-4-phenyl-1H-pyrazole; 3-Methyl-4-phenyl-1H-pyrazole-5-amine; 5-Methyl-4-phenyl-1H-pyrazol-3-ylamine; SMR000290815; ST037469; AB0131798; DB-053614; A5753; BB 0219097; FT-0640686; V6864; EN300-41461; AB00583018-02; SR-01000530901; 5-Methyl-4-phenyl-1,2-dihydro-3H-pyrazol-3-imine; SR-01000530901-1; SR-01000530901-2; 5-Methyl-4-phenyl-2H-pyrazol-3-ylamine, AldrichCPR; Q27285561; F0912-0735
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| Activity |
IC50 = 660000 nM
|
[6] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors. Bioorg Med Chem Lett. 2005 Feb 15;15(4):905-9. | ||||
| REF 2 | Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors. Bioorg Med Chem Lett. 2005 Feb 1;15(3):761-4. | ||||
| REF 3 | 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 4 | Identification of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidines as selective inhibitors of protein kinase B through fragment elaboration. J Med Chem. 2008 Apr 10;51(7):2147-57. | ||||
| REF 5 | Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases. Bioorg Med Chem. 2013 Sep 15;21(18):5707-24. | ||||
| REF 6 | The Fragment Network: A Chemistry Recommendation Engine Built Using a Graph Database. J Med Chem. 2017 Jul 27;60(14):6440-6450. | ||||
| REF 7 | Identification of inhibitors of protein kinase B using fragment-based lead discovery. J Med Chem. 2007 May 17;50(10):2293-6. | ||||
| REF 8 | Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties. J Med Chem. 2013 May 9;56(9):3456-66. | ||||
| REF 9 | 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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