Target Information
| Target General Information | Top | |||||
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| Target ID |
T45597
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| Target Name |
Ribosomal protein S6 kinase (S6K)
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| Synonyms |
Ribosomal s6 kinase
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| Gene Name |
NO-GeName
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
| BioChemical Class |
Kinase
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| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 4 Clinical Trial Drugs | + | ||||
| 1 | LY-2584702 | Drug Info | Phase 1 | Solid tumour/cancer | [2], [3] | |
| 2 | LY2780301 | Drug Info | Phase 1 | Solid tumour/cancer | [4] | |
| 3 | LYS-6KAKT1 | Drug Info | Phase 1 | Solid tumour/cancer | [5] | |
| 4 | XL418 | Drug Info | Phase 1 | Solid tumour/cancer | [6] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Modulator | [+] 4 Modulator drugs | + | ||||
| 1 | LY-2584702 | Drug Info | [7] | |||
| 2 | LY2780301 | Drug Info | [8] | |||
| 3 | LYS-6KAKT1 | Drug Info | [1] | |||
| 4 | XL418 | Drug Info | [9] | |||
| Activator | [+] 1 Activator drugs | + | ||||
| 1 | PMID27410995-Compound-Figure3k | Drug Info | [10] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
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| Co-Targets | ||||||
| References | Top | |||||
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| REF 1 | DOI: 10.1016/S1359-6349(10)71767-5 | |||||
| REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8248). | |||||
| REF 3 | ClinicalTrials.gov (NCT01241461) A Study of LY2584702 in Solid Tumors. U.S. National Institutes of Health. | |||||
| REF 4 | ClinicalTrials.gov (NCT01115751) A Study in Patients With Advanced or Metastatic Cancer. U.S. National Institutes of Health. | |||||
| REF 5 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034531) | |||||
| REF 6 | ClinicalTrials.gov (NCT00460278) Study of XL418 in Adults With Solid Tumors. U.S. National Institutes of Health. | |||||
| REF 7 | A phase Ib trial of LY2584702 tosylate, a p70 S6 inhibitor, in combination with erlotinib or everolimus in patients with solid tumours.Eur J Cancer.2014 Mar;50(5):876-84. | |||||
| REF 8 | A first-in-human phase I trial of LY2780301, a dual p70 S6 kinase and Akt Inhibitor, in patients with advanced or metastatic cancer. Invest New Drugs. 2015 Jun;33(3):710-9. | |||||
| REF 9 | Targeting the phosphoinositide 3-kinase (PI3K) pathway in cancer | |||||
| REF 10 | Ribosomal S6 kinase (RSK) modulators: a patent review.Expert Opin Ther Pat. 2016 Sep;26(9):1061-78. | |||||
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