Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T94479 | Target Info | |||
| Target Name | Ribosomal protein S6 kinase beta-1 (S6K1) | ||||
| Synonyms |
p70-S6K 1; p70 ribosomal S6 kinase alpha; p70 S6KA; p70 S6K-alpha; p70 S6 kinase alpha; Serine/threonine-protein kinase 14A; STK14A; S6K-beta-1; S6K; Ribosomal protein S6 kinase I; P70S6K1; P70-S6K; 70 kDa ribosomal protein S6 kinase 1
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| Target Type | Clinical trial Target | ||||
| Gene Name | RPS6KB1 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 18 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
8-chloro-quinoline-3-carbonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL436817; Cyanoquinoline, 11; SCHEMBL6071997; BDBM21898; CHEBI:94979; BRD-K00088062-001-01-3; 4-[(3-Chloro-4-fluorophenyl)amino]-6-[(1H-imidazole-5-ylmethyl)amino]-8-chloro-3-quinolinecarbonitrile
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-(3-(1H-Indazol-5-yl)ureido)-5-(tert-butyl)thiophene-3-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
S6K-18; CHEMBL1641799; C17H18N4O3S; 2-(3-(1H-INDAZOL-5-YL)UREIDO)-5-TERT-BUTYLTHIOPHENE-3-CARBOXYLIC ACID; SYN1132; S6K18; BCP21624; EX-A1859; BDBM50333474; ZINC66263052; NCGC00263196-01; NCGC00263196-02; AS-16271; 2-(3-1H-indazol-5-ylureido)-5-tert-butylthiophene-3-carboxylic acid
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| Activity |
IC50 = 52000 nM
|
[2] | |||
| Compound Name |
5-[3-(Aminomethyl)piperidin-1-yl]quinazoline-8-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3947957; SCHEMBL15073448; BDBM181303; US9139568, 56
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| Activity |
IC50 = 56000 nM
|
[3] | |||
| Compound Name |
N-[2-(Dimethylamino)ethyl]-5-ethyl-2-(1H-indazol-5-ylcarbamoylamino)thiophene-3-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1641792; BDBM50333481; 2-(3-1H-indazol-5-ylureido)-N-(2-(dimethylamino)ethyl)-5-ethylthiophene-3-carboxamide
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| Activity |
IC50 = 62000 nM
|
[2] | |||
| Compound Name |
4(3H)-Pyrimidinone,2-[(4-fluorophenyl)amino]-5-[5-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]-2-pyridinyl]-3-methyl-
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Investigative | Compound Info | ||
| Synonyms |
pyrimidone, 62; CHEMBL447602; SCHEMBL13511902; BDBM24772; ZINC43202030
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| Activity |
IC50 = 65000 nM
|
[4] | |||
| Compound Name |
5-Cyclopropyl-N-[2-(dimethylamino)ethyl]-2-(1H-indazol-5-ylcarbamoylamino)thiophene-3-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1641793; BDBM50333480; 2-(3-1H-indazol-5-ylureido)-5-cyclopropyl-N-(2-(dimethylamino)ethyl)thiophene-3-carboxamide
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| Activity |
IC50 = 70000 nM
|
[2] | |||
| 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 = 83100 nM
|
[1] | |||
| Compound Name |
6-[4-[2-(Azetidin-1-yl)-1-(3,4-dichlorophenyl)ethyl]piperazin-1-yl]-5-(6-piperazin-1-ylpyridin-3-yl)pyrimidin-4-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3921032; SCHEMBL14787840; BDBM224456; US9321760, 133
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
COC(=O)Cn1cc(cn1)-c1c(N)ncnc1N1CCN(CC1)C(CN1CCC1)c1cccc(c1)C#N
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3965499; SCHEMBL16680953; BDBM224453; US9321760, 130
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
5-[4-(5-Chloro-2-methylphenyl)piperazin-1-yl]quinazoline-8-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3969122; SCHEMBL15060158; BDBM181358; US9139568, 111
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
Aminopyrimidine amide, 13b
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL272888; SCHEMBL2943385; BDBM26369
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| Activity |
IC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
5-[4-(3,4-Dichlorophenyl)piperazin-1-yl]quinazoline-8-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3911505; SCHEMBL15059364; BDBM181357; US9139568, 110
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| 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
|
[7] | |||
| 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
|
[7] | |||
| Compound Name |
6-[4-[2-(Azetidin-1-yl)-1-(5,6,7,8-tetrahydronaphthalen-2-yl)ethyl]piperazin-1-yl]-5-(6-piperazin-1-ylpyridin-3-yl)pyrimidin-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3987086; SCHEMBL14787842; BDBM224438; US9321760, 115
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
8-Bromo-4-[(3-chloro-4-fluorophenyl)amino]-6-[(1H-1,2,3-triazol-4-ylmethyl)amino]quinoline-3-carbonitrile
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|
Investigative | Compound Info | ||
| Synonyms |
Cyanoquinoline, 51; BMCL193485 Compound 8; CHEMBL230232; SCHEMBL4961707; BDBM21925; 8-bromo-4-(3-chloro-4-fluoroanilino)-6-(2H-triazol-4-ylmethylamino)quinoline-3-carbonitrile
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
5-Tert-butyl-N-[(2-fluorophenyl)methyl]-2-(1H-indazol-5-ylcarbamoylamino)thiophene-3-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1641805; BDBM50333469; 2-(3-1H-indazol-5-ylureido)-5-tert-butyl-N-(2-fluorobenzyl)thiophene-3-carboxamide
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| Activity |
IC50 = 191000 nM
|
[2] | |||
| Compound Name |
N-[2-(Dimethylamino)ethyl]-5-[(1R)-1-hydroxyethyl]-2-(1H-indazol-5-ylcarbamoylamino)thiophene-3-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1641796; BDBM50333477; (R)-2-(3-1H-indazol-5-ylureido)-N-(2-(dimethylamino)ethyl)-5-(1-hydroxyethyl)thiophene-3-carboxamide
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| Activity |
IC50 = 196000 nM
|
[2] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 5 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
2-(3-1H-Indazol-5-ylureido)-N-benzyl-5-tert-butylthiophene-3-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1641804; BDBM50333470
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|
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| Activity |
IC50 = 201000 nM
|
[2] | |||
| Compound Name |
1-(5-Tert-butyl-3-(morpholine-4-carbonyl)thiophen-2-yl)-3-(1H-indazol-5-yl)urea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1641803; BDBM50333471
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|
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| Activity |
IC50 = 207000 nM
|
[2] | |||
| Compound Name |
N-[2-(Dimethylamino)ethyl]-2-(1H-indazol-5-ylcarbamoylamino)-5-methylthiophene-3-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1641794; BDBM50333479; 2-(3-1H-indazol-5-ylureido)-N-(2-(dimethylamino)ethyl)-5-methylthiophene-3-carboxamide
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|
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| Activity |
IC50 = 223000 nM
|
[2] | |||
| Compound Name |
N-[2-(Dimethylamino)ethyl]-5-[(1S)-1-hydroxyethyl]-2-(1H-indazol-5-ylcarbamoylamino)thiophene-3-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1641797; BDBM50333476; (S)-2-(3-1H-indazol-5-ylureido)-N-(2-(dimethylamino)ethyl)-5-(1-hydroxyethyl)thiophene-3-carboxamide
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| Activity |
IC50 = 379000 nM
|
[2] | |||
| Compound Name |
N-[2-(Dimethylamino)ethyl]-2-(1H-indazol-5-ylcarbamoylamino)-5-phenylthiophene-3-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1641795; BDBM50333478; 2-(3-1H-indazol-5-ylureido)-N-(2-(dimethylamino)ethyl)-5-phenylthiophene-3-carboxamide
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| Activity |
IC50 = 1900000 nM
|
[2] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| 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 | Potent and selective thiophene urea-templated inhibitors of S6K. Bioorg Med Chem Lett. 2011 Jan 15;21(2):849-52. | ||||
| REF 3 | US patent application no. 9139568B2, Heterocyclic carboxamides as modulators of kinase activity | ||||
| REF 4 | Design, synthesis, and biological evaluation of potent c-Met inhibitors. J Med Chem. 2008 Sep 25;51(18):5766-79. | ||||
| REF 5 | US patent application no. 9321760B2, Aminopyrimidine derivatives for use as modulators of kinase activity | ||||
| REF 6 | Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation. J Med Chem. 2008 Mar 27;51(6):1681-94. | ||||
| REF 7 | Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties. J Med Chem. 2013 May 9;56(9):3456-66. | ||||
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