Target Information
| Target General Information | Top | |||||
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| Target ID |
T43415
(Former ID: TTDC00316)
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| Target Name |
Tyrosine-protein kinase (PTK)
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| Synonyms |
Protein-tyrosine kinase; PTK
Click to Show/Hide
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| Gene Name |
NO-GeName
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Rheumatoid arthritis [ICD-11: FA20] | |||||
| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 5 Clinical Trial Drugs | + | ||||
| 1 | ASP-015K | Drug Info | Phase 3 | Psoriasis vulgaris | [2], [3] | |
| 2 | Masitinib | Drug Info | Phase 3 | Amyotrophic lateral sclerosis | [4] | |
| 3 | ATI-502 | Drug Info | Phase 2 | Atopic dermatitis | [5] | |
| 4 | KD019 | Drug Info | Phase 2 | Non-small-cell lung cancer | [6] | |
| 5 | LEO 124249 | Drug Info | Phase 2 | Asthma | [5], [7] | |
| Discontinued Drug(s) | [+] 4 Discontinued Drugs | + | ||||
| 1 | SDZ-LAP-977 | Drug Info | Discontinued in Phase 2 | Psoriasis vulgaris | [8] | |
| 2 | PN-355 | Drug Info | Discontinued in Phase 1 | Human immunodeficiency virus-1 infection | [9] | |
| 3 | AP-23588 | Drug Info | Terminated | Osteoporosis | [10] | |
| 4 | CLX-0301 | Drug Info | Terminated | Diabetic complication | [11] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 15 Inhibitor drugs | + | ||||
| 1 | ASP-015K | Drug Info | [7] | |||
| 2 | Masitinib | Drug Info | [12] | |||
| 3 | ATI-502 | Drug Info | [5] | |||
| 4 | KD019 | Drug Info | [12], [13] | |||
| 5 | LEO 124249 | Drug Info | [5] | |||
| 6 | Aminotriazolopyridine derivative 1 | Drug Info | [14] | |||
| 7 | Imidazo[4,5-c]pyridine derivative 1 | Drug Info | [14] | |||
| 8 | PMID27774822-Compound-Figure10CompoundA | Drug Info | [15] | |||
| 9 | PMID27774822-Compound-Figure10Example1 | Drug Info | [15] | |||
| 10 | Ruxolitinib derivative 1 | Drug Info | [14] | |||
| 11 | Tetra-cyclic compound 1 | Drug Info | [14] | |||
| 12 | SDZ-LAP-977 | Drug Info | [16] | |||
| 13 | PN-355 | Drug Info | [17] | |||
| 14 | AP-23588 | Drug Info | [18] | |||
| 15 | CLX-0301 | Drug Info | [19] | |||
| 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 | ||||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89. | |||||
| 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: 8315). | |||||
| REF 3 | ClinicalTrials.gov (NCT02308163) A Study to Evaluate Safety and Efficacy of ASP015K in Patients With Rheumatoid Arthritis (RA) Who Had an Inadequate Response to DMARDs. U.S. National Institutes of Health. | |||||
| REF 4 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 5 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 6 | ClinicalTrials.gov (NCT01487174) KD019 Versus Erlotinib in Subjects With Stage IIIB/IV Non Small Cell Lung Cancer With Progression After First- or Second-Line Chemotherapy. U.S. National Institutes of Health. | |||||
| REF 7 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 8 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004738) | |||||
| REF 9 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005490) | |||||
| REF 10 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017871) | |||||
| REF 11 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013358) | |||||
| REF 12 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 13 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 14 | Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 1.Expert Opin Ther Pat. 2017 Feb;27(2):127-143. | |||||
| REF 15 | Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 2.Expert Opin Ther Pat. 2017 Feb;27(2):145-161. | |||||
| REF 16 | Structure-activity relationship studies on a novel class of antiproliferative agents derived from Lavendustin A. Part I: Ring A modifications. Bioorg Med Chem. 2008 Aug 15;16(16):7552-60. | |||||
| REF 17 | WO patent application no. 2005,0502,03, Biological materials and uses thereof. | |||||
| REF 18 | Foye's Principles of Medicinal Chemistry, Thomas L. Lemke, David A. Williams. 2008. Page(950). | |||||
| REF 19 | CLX-0901 (Calyx Therapeutics). Curr Opin Investig Drugs. 2001 May;2(5):650-3. | |||||
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