Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T83202 | Target Info | |||
| Target Name | Ribosomal protein S6 kinase alpha-1 (RSK1) | ||||
| Synonyms |
p90S6K; p90RSK1; p90-RSK 1; S6K-alpha-1; Ribosomal S6 kinase 1; RSK-1; MAPKAPK1A; MAPKAPK-1a; MAPKAP kinase 1a; MAPK-activated protein kinase 1a; MAP kinase-activated protein kinase 1a; 90 kDa ribosomal protein S6 kinase 1
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| Target Type | Patented-recorded Target | ||||
| Gene Name | RPS6KA1 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 11 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
3-{[2-(3-Thienyl)pyridin-4-yl]amino}-4-{[(1R)-1-phenylethyl]amino}cyclobut-3-ene-1,2-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL481248; BDBM50259638
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
CID 46179972
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1163016; BDBM50378568
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
Methyl 4-(6-(4-(methoxycarbonylamino)phenyl)-4-morpholino-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate
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Investigative | Compound Info | ||
| Synonyms |
WYE-354; WYE 354; pyrazolo pyrimidine, 19; cc-506; MLS006011008; SCHEMBL300431; CHEMBL561708; GTPL9361; WYE354; BDBM35587; DTXSID00657912; C24H29N7O5; HMS3654N09; BCP02898; ZINC43013490; CCG-264882; CS-0183; SB19260; NCGC00242484-01; NCGC00242484-02; NCGC00242484-09; AC-28454; AS-55957; HY-12034; SMR004702806; BCP0726000260; DB-059456; FT-0675866; S1266; SW219671-1; X7422; W-5702; J-001552; J-514253; BRD-K77008974-001-01-6; Q27166532; mTOR Kinase Inhibitor II, WYE-354 - CAS 1062169-56-5
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
Methyl 4-(6-(4-aminophenyl)-4-morpholino-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1095626; SCHEMBL3984085; BDBM50316252; methyl 4-[6-(4-aminophenyl)-4-morpholin-4-ylpyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carboxylate
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
4-(4-Methyl-1H-indol-5-ylamino)-5-(3-(4-methylpiperazin-1-ylsulfonyl)styryl)nicotinonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1080994; SCHEMBL2934634; BDBM50311953
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| Activity |
IC50 ~ 50000 nM
|
[5] | |||
| Compound Name |
4-(4-Methyl-1H-indol-5-ylamino)-2-(3-oxo-3-(pyrrolidin-1-yl)prop-1-enyl)thieno[2,3-b]pyridine-5-carbonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL477817; SCHEMBL5520662; SCHEMBL5520668; BDBM50263132
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| Activity |
IC50 ~ 50000 nM
|
[6] | |||
| Compound Name |
3-[[2-(2-Fluorophenyl)pyridin-4-yl]amino]-4-[[(1R)-1-phenylethyl]amino]cyclobut-3-ene-1,2-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL468125; 3-{[2-(2-Fluorophenyl)pyridin-4-yl]amino}-4-{[(1R)-1-phenylethyl]amino}cyclobut-3-ene-1,2-dione; SCHEMBL4371574; BDBM50259601
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
3-{[2-(2-Furyl)pyridin-4-yl]amino}-4-{[(1R)-1-phenylethyl]amino}cyclobut-3-ene-1,2-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL519113; SCHEMBL4366875; BDBM50259637; 3-[[2-(furan-2-yl)pyridin-4-yl]amino]-4-[[(1R)-1-phenylethyl]amino]cyclobut-3-ene-1,2-dione
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
Tert-Butyl 4-(6-(4-aminophenyl)-4-morpholino-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1095627; SCHEMBL3991434; BDBM50316253
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
6-Methyl-4-(4-methyl-1H-indol-5-ylamino)-5-(3-(4-methylpiperazin-1-ylsulfonyl)styryl)nicotinonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1080995; SCHEMBL2934911; BDBM50311954
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| Activity |
IC50 ~ 50000 nM
|
[5] | |||
| 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 = 63000 nM
|
[7] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2). Bioorg Med Chem. 2009 May 1;17(9):3342-51. | ||||
| REF 2 | Novel synthesis and structural characterization of a high-affinity paramagnetic kinase probe for the identification of non-ATP site binders by nuclear magnetic resonance. J Med Chem. 2010 Feb 11;53(3):1238-49. | ||||
| REF 3 | ATP-competitive inhibitors of the mammalian target of rapamycin: design and synthesis of highly potent and selective pyrazolopyrimidines. J Med Chem. 2009 Aug 27;52(16):5013-6. | ||||
| REF 4 | Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent. J Med Chem. 2009 Dec 24;52(24):8010-24. | ||||
| REF 5 | Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6575-7. | ||||
| REF 6 | 2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4420-3. | ||||
| REF 7 | 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. | ||||
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