Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T03279 | Target Info | |||
| Target Name | Ribosomal protein S6 kinase alpha-3 (RSK3) | ||||
| Synonyms |
pp90RSK2; p90RSK3; p90-RSK 3; S6K-alpha-3; Ribosomal S6 kinase 2; RSK2; RSK-2; MAPKAPK1B; MAPKAPK-1b; MAPKAP kinase 1b; MAPK-activated protein kinase 1b; MAP kinase-activated protein kinase 1b; Insulin-stimulated protein kinase 1; ISPK1; ISPK-1; 90 kDa ribosomal protein S6 kinase 3
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| Target Type | Patented-recorded Target | ||||
| Gene Name | RPS6KA3 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 26 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
2-[(Z)-[6-(4-Fluoro-3-nitrophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910602; NSC-747112
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| Activity |
IC50 = 53750 nM
|
[1] | |||
| Compound Name |
2-[(Z)-[6-(4-Bromo-3-nitrophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1909651; NSC-747420
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| Activity |
IC50 = 56730 nM
|
[1] | |||
| Compound Name |
N-Methyl-4-(2-(piperidin-4-yl)-5-(3-(trifluoromethyl)phenyl)-1H-imidazol-4-yl)pyrimidin-2-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL489344; SCHEMBL4936886; BDBM50260228; N-methyl-4-[2-piperidin-4-yl-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyrimidin-2-amine
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| Activity |
IC50 = 76000 nM
|
[2] | |||
| Compound Name |
2-[(E)-[6-(2,5-Dichlorothiophen-3-yl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
NSC-732181; CHEMBL1910757; NSC732181
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| Activity |
IC50 = 79000 nM
|
[1] | |||
| Compound Name |
2-[(E)-[6-(2,4-Dichloro-5-nitrophenyl)-2-ethylimidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910758
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| Activity |
IC50 = 83000 nM
|
[1] | |||
| Compound Name |
2-[(E)-[2-Chloro-6-(4-fluorophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910373; NSC-747109
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| Activity |
IC50 = 86000 nM
|
[1] | |||
| Compound Name |
2-[(E)-[6-(4-Chloro-3-nitrophenyl)-2-methylimidazo[2,1-b][1,3,4]thiadiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
NSC-734178; CHEMBL1910759; NSC734178
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| Activity |
IC50 = 94000 nM
|
[1] | |||
| Compound Name |
2-[(E)-[6-(2,4-Dichloro-5-nitrophenyl)-2,3-dimethylimidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
NSC-722877; CHEMBL1910760; NSC722877
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| Activity |
IC50 = 98500 nM
|
[1] | |||
| Compound Name |
2-[(Z)-[6-(4-Fluorophenyl)-2-methylimidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910605; NSC-747107
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(E)-[6-(2,5-Dichlorothiophen-3-yl)-2-methylimidazo[2,1-b][1,3,4]thiadiazol-5-yl]methylideneamino]guanidine;hydrochloride
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910376
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(Z)-[6-(4-Fluorophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910597; NSC-747111
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(E)-(2-Chloro-6-phenylimidazo[2,1-b][1,3]thiazol-5-yl)methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910372; NSC-747418
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(Z)-[6-(2-Fluoro-3-nitrophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910603; NSC-747421
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
N-[(E)-[2-(2,5-Dichlorothiophen-3-yl)imidazo[2,1-b][1,3]benzothiazol-1-yl]methylideneamino]-4,5-dihydro-1H-imidazol-2-amine;hydrobromide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910617; NSC-745851
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(Z)-[6-(2,5-Dimethoxy-4-nitrophenyl)-2-methylimidazo[2,1-b][1,3,4]thiadiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910595; NSC-745253
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(E)-(3-Methyl-6-pyridin-3-ylimidazo[2,1-b][1,3]thiazol-5-yl)methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
NSC-728902; CHEMBL1910762; NSC728902
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| Activity |
IC50 = 100000 nM
|
[1] | |||
| Compound Name |
2-[(Z)-[6-[3-(Trifluoromethyl)phenyl]imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910604; NSC-747417
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(Z)-[6-(2,4,5-Trifluorophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910601; NSC-747419
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
N-[(E)-[2-(2,5-Dichlorothiophen-3-yl)imidazo[1,2-a]pyridin-3-yl]methylideneamino]-4,5-dihydro-1H-imidazol-2-amine;hydrobromide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910624; NSC-745852
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(E)-[2-(2,5-Dichlorothiophen-3-yl)imidazo[1,2-a]pyridin-3-yl]methylideneamino]guanidine;hydrochloride
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910622; NSC-745257
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(E)-(2,3-Dimethyl-6-pyridin-3-ylimidazo[2,1-b][1,3]thiazol-5-yl)methylideneamino]guanidine;hydrochloride
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|
Investigative | Compound Info | ||
| Synonyms |
NSC-726886; CHEMBL1910761; NSC726886
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|
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| Activity |
IC50 = 100000 nM
|
[1] | |||
| Compound Name |
N-[(E)-[2-Chloro-6-(2,5-dichlorothiophen-3-yl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]-4,5-dihydro-1H-imidazol-2-amine;hydrobromide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910609; NSC-745850
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(Z)-[6-(2,6-Difluorophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910599; NSC-747413
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(Z)-[6-(2-Fluorophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910598; NSC-747415
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
N-[(E)-[6-(4-Chloro-3-nitrophenyl)-2-methylimidazo[2,1-b][1,3,4]thiadiazol-5-yl]methylideneamino]-4,5-dihydro-1H-imidazol-2-amine;hydrobromide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910610; NSC-745258
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(Z)-[6-(3,4-Difluorophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methylideneamino]guanidine;hydrochloride
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1910600; NSC-747414
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 2 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
3-(4-Amino-5-p-tolyl-7H-pyrrolo[2,3-d]pyrimidin-7-yl)propan-1-ol
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL473965; SCHEMBL12200845; BDBM50248766; 3-(4-Amino-5-(p-tolyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)propan-1-ol; 3-[4-amino-5-(4-methylphenyl)pyrrolo[2,3-d]pyrimidin-7-yl]propan-1-ol
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| Activity |
IC50 = 430000 nM
|
[3] | |||
| Compound Name |
1-[4-Amino-7-(3-hydroxypropyl)-5-(4-methylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-2-fluoroethanone
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL515414; RSK2 kinase inhibitor; FMK (covalent); RSK inhibitor Fmk; FMK;RSK2 kinase inhibitor; GTPL9358; SCHEMBL12200837; KS-00001DWT; DTXSID40349344; EX-A846; HMS3741I07; BCP10804; ZINC6718642; 3681AH; BDBM50248765; HY-52101A; MFCD22417081; AKOS027325130; CS-0648; QC-8903; NCGC00386649-02; DS-016104; fluoromethylketone-pyrrolopyrimidine scaffold; FT-0700368; A11423; W-5913; J-690355
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| Activity |
IC50 = 3400000 nM
|
[3] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. Eur J Med Chem. 2011 Sep;46(9):4311-23. | ||||
| REF 2 | Hepatitis C virus NS5A is a direct substrate of casein kinase I-alpha, a cellular kinase identified by inhibitor affinity chromatography using specific NS5A hyperphosphorylation inhibitors. J Biol Chem. 2007 Feb 23;282(8):5536-44. | ||||
| REF 3 | Structural bioinformatics-based design of selective, irreversible kinase inhibitors. Science. 2005 May 27;308(5726):1318-21. | ||||
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