Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T78874
(Former ID: TTDR01081)
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| Target Name |
Protein kinase (PK)
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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) | [+] 7 Clinical Trial Drugs | + | ||||
| 1 | MGCD516 | Drug Info | Phase 2/3 | Solid tumour/cancer | [2] | |
| 2 | ENMD-2076 | Drug Info | Phase 2 | Acute myeloid leukaemia | [3], [4] | |
| 3 | LY2801653 | Drug Info | Phase 2 | Solid tumour/cancer | [5] | |
| 4 | MGCD265 | Drug Info | Phase 2 | Non-small-cell lung cancer | [6] | |
| 5 | RV-568 | Drug Info | Phase 2 | Asthma | [7] | |
| 6 | LX-7101 | Drug Info | Phase 1/2 | Glaucoma/ocular hypertension | [8] | |
| 7 | TG02 | Drug Info | Phase 1/2 | Anaplastic astrocytoma | [9], [10] | |
| Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
| 1 | Cyclocreatine | Drug Info | Discontinued in Phase 1 | Virus infection | [11], [12] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 8 Inhibitor drugs | + | ||||
| 1 | MGCD516 | Drug Info | [9] | |||
| 2 | ENMD-2076 | Drug Info | [9] | |||
| 3 | LY2801653 | Drug Info | [9] | |||
| 4 | MGCD265 | Drug Info | [9] | |||
| 5 | RV-568 | Drug Info | [1] | |||
| 6 | LX-7101 | Drug Info | [13] | |||
| 7 | TG02 | Drug Info | [10] | |||
| 8 | Cyclocreatine | Drug Info | [14] | |||
| Drug Property Profile of Target | Top | |
|---|---|---|
| (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 | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Investigational p38 inhibitors for the treatment of chronic obstructive pulmonary disease. Expert Opin Investig Drugs. 2015 Mar;24(3):383-92. | |||||
| REF 2 | ClinicalTrials.gov (NCT04887870) Study of Sitravatinib With or Without Other Anticancer Therapies Receiving Clinical Benefit From Parent Study. U.S. National Institutes of Health. | |||||
| REF 3 | 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: 7885). | |||||
| REF 4 | ENMD-2076 is an orally active kinase inhibitor with antiangiogenic and antiproliferative mechanisms of action. Mol Cancer Ther. 2011 Jan;10(1):126-37. | |||||
| REF 5 | ClinicalTrials.gov (NCT01285037) A Study of LY2801653 in Advanced Cancer. U.S. National Institutes of Health. | |||||
| REF 6 | ClinicalTrials.gov (NCT02544633) Phase 2 Study of MGCD265 in Patients With Non-Small Cell Lung Cancer With Activating Genetic Alterations in MET. | |||||
| REF 7 | ClinicalTrials.gov (NCT01475292) A Study to Investigate How Safe and Well Tolerated RV568 is in Patients With Chronic Obstructive Pulmonary Disease (COPD). U.S. National Institutes of Health. | |||||
| REF 8 | ClinicalTrials.gov (NCT01528111) Study to Evaluate the Safety, Tolerability, and Efficacy of LX7101 in Subjects With Primary Open-angle Glaucoma or Ocular Hypertension. U.S. National Institutes of Health. | |||||
| REF 9 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 10 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 11 | 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: 5491). | |||||
| REF 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002859) | |||||
| REF 13 | Design, synthesis and biological characterization of selective LIMK inhibitors. Bioorg Med Chem Lett. 2015 Sep 15;25(18):4005-10. | |||||
| REF 14 | Direct determination of creatine kinase equilibrium constants with creatine or cyclocreatine substrate. Biochim Biophys Acta. 1989 Oct 19;998(3):317-20. | |||||
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