Target Information
| Target General Information | Top | |||||
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| Target ID |
T78932
(Former ID: TTDNC00412)
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| Target Name |
TYK2 tyrosine kinase (TYK2)
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| Synonyms |
Non-receptor tyrosine-protein kinase TYK2
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| Gene Name |
TYK2
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Psoriasis [ICD-11: EA90] | |||||
| Function |
Probably involved in intracellular signal transduction by being involved in the initiation of type I IFN signaling. Phosphorylates the interferon-alpha/beta receptor alpha chain.
Click to Show/Hide
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| BioChemical Class |
Kinase
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| UniProt ID | ||||||
| EC Number |
EC 2.7.10.2
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| Sequence |
MPLRHWGMARGSKPVGDGAQPMAAMGGLKVLLHWAGPGGGEPWVTFSESSLTAEEVCIHI
AHKVGITPPCFNLFALFDAQAQVWLPPNHILEIPRDASLMLYFRIRFYFRNWHGMNPREP AVYRCGPPGTEASSDQTAQGMQLLDPASFEYLFEQGKHEFVNDVASLWELSTEEEIHHFK NESLGMAFLHLCHLALRHGIPLEEVAKKTSFKDCIPRSFRRHIRQHSALTRLRLRNVFRR FLRDFQPGRLSQQMVMVKYLATLERLAPRFGTERVPVCHLRLLAQAEGEPCYIRDSGVAP TDPGPESAAGPPTHEVLVTGTGGIQWWPVEEEVNKEEGSSGSSGRNPQASLFGKKAKAHK AVGQPADRPREPLWAYFCDFRDITHVVLKEHCVSIHRQDNKCLELSLPSRAAALSFVSLV DGYFRLTADSSHYLCHEVAPPRLVMSIRDGIHGPLLEPFVQAKLRPEDGLYLIHWSTSHP YRLILTVAQRSQAPDGMQSLRLRKFPIEQQDGAFVLEGWGRSFPSVRELGAALQGCLLRA GDDCFSLRRCCLPQPGETSNLIIMRGARASPRTLNLSQLSFHRVDQKEITQLSHLGQGTR TNVYEGRLRVEGSGDPEEGKMDDEDPLVPGRDRGQELRVVLKVLDPSHHDIALAFYETAS LMSQVSHTHLAFVHGVCVRGPENIMVTEYVEHGPLDVWLRRERGHVPMAWKMVVAQQLAS ALSYLENKNLVHGNVCGRNILLARLGLAEGTSPFIKLSDPGVGLGALSREERVERIPWLA PECLPGGANSLSTAMDKWGFGATLLEICFDGEAPLQSRSPSEKEHFYQRQHRLPEPSCPQ LATLTSQCLTYEPTQRPSFRTILRDLTRLQPHNLADVLTVNPDSPASDPTVFHKRYLKKI RDLGEGHFGKVSLYCYDPTNDGTGEMVAVKALKADCGPQHRSGWKQEIDILRTLYHEHII KYKGCCEDQGEKSLQLVMEYVPLGSLRDYLPRHSIGLAQLLLFAQQICEGMAYLHAQHYI HRDLAARNVLLDNDRLVKIGDFGLAKAVPEGHEYYRVREDGDSPVFWYAPECLKEYKFYY ASDVWSFGVTLYELLTHCDSSQSPPTKFLELIGIAQGQMTVLRLTELLERGERLPRPDKC PCEVYHLMKNCWETEASFRPTFENLIPILKTVHEKYQGQAPSVFSVC Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 4 Clinical Trial Drugs | + | ||||
| 1 | BMS-986165 | Drug Info | Phase 3 | Plaque psoriasis | [1], [2] | |
| 2 | PF-06700841 | Drug Info | Phase 2 | Asthma | [1] | |
| 3 | PF-06826647 | Drug Info | Phase 2 | Plaque psoriasis | [3] | |
| 4 | PF-06826647 | Drug Info | Phase 1 | Plaque psoriasis | [1] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 40 Inhibitor drugs | + | ||||
| 1 | BMS-986165 | Drug Info | [1] | |||
| 2 | PF-06700841 | Drug Info | [1] | |||
| 3 | PF-06826647 | Drug Info | [4] | |||
| 4 | PF-06826647 | Drug Info | [1] | |||
| 5 | Aminooxazole carboxamide derivative 1 | Drug Info | [5] | |||
| 6 | Aminopyridine derivative 1 | Drug Info | [5] | |||
| 7 | Aminopyrimidine derivative 5 | Drug Info | [5] | |||
| 8 | Aminotriazolopyridine derivative 1 | Drug Info | [6] | |||
| 9 | Benzimidazole derivative 7 | Drug Info | [6] | |||
| 10 | Bis-aminopyrimidine derivative 1 | Drug Info | [6] | |||
| 11 | Bis-aminopyrimidine derivative 2 | Drug Info | [6] | |||
| 12 | Bis-aminopyrimidine derivative 3 | Drug Info | [6] | |||
| 13 | Bis-aminopyrimidine derivative 4 | Drug Info | [6] | |||
| 14 | Bis-aminopyrimidine derivative 5 | Drug Info | [6] | |||
| 15 | Imidazopyridine derivative 3 | Drug Info | [5] | |||
| 16 | Imidazo[4,5-c]pyridine derivative 1 | Drug Info | [6] | |||
| 17 | Imidazo[4,5-c]pyridine derivative 2 | Drug Info | [6] | |||
| 18 | N-methylmethanesulfonamide derivative 1 | Drug Info | [5] | |||
| 19 | PMID27774822-Compound-Figure11Example5 | Drug Info | [5] | |||
| 20 | PMID27774822-Compound-Figure3CompoundI-165 | Drug Info | [5] | |||
| 21 | PMID27774822-Compound-Figure9Example15 | Drug Info | [5] | |||
| 22 | PMID27774824-Compound-Figure11Example1up | Drug Info | [6] | |||
| 23 | PMID27774824-Compound-Figure3Example18 | Drug Info | [6] | |||
| 24 | PMID27774824-Compound-Figure6Example12 | Drug Info | [6] | |||
| 25 | PMID27774824-Compound-Figure9Example2down | Drug Info | [6] | |||
| 26 | PMID27774824-Compound-Figure9Example2up | Drug Info | [6] | |||
| 27 | Pyrazolopyridine derivative 3 | Drug Info | [5] | |||
| 28 | Pyrazolopyridine derivative 5 | Drug Info | [5] | |||
| 29 | Pyrazolo[4,3-c]pyridine derivative 2 | Drug Info | [6] | |||
| 30 | Pyrrole derivative 7 | Drug Info | [5] | |||
| 31 | Pyrrolo-pyridone derivative 3 | Drug Info | [5] | |||
| 32 | Pyrrolo[2,3-d]pyrimidine derivative 6 | Drug Info | [5] | |||
| 33 | Pyrrolo[2,3-d]pyrimidine derivative 7 | Drug Info | [5] | |||
| 34 | Pyrrolo[2,3-d]pyrimidine derivative 8 | Drug Info | [5] | |||
| 35 | Thiazolopyridine derivative 1 | Drug Info | [5] | |||
| 36 | Tricyclic compound 11 | Drug Info | [5] | |||
| 37 | Tricyclic heterocycle derivative 1 | Drug Info | [5] | |||
| 38 | Tricyclic heterocycle derivative 5 | Drug Info | [5] | |||
| 39 | Tricyclic pyrrolopyridine compound 1 | Drug Info | [5] | |||
| 40 | CMP-6 | Drug Info | [7] | |||
| 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 | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
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| Target-interacting Proteins | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 8 KEGG Pathways | + | ||||
| 1 | Osteoclast differentiation | |||||
| 2 | Jak-STAT signaling pathway | |||||
| 3 | Toxoplasmosis | |||||
| 4 | Hepatitis C | |||||
| 5 | Measles | |||||
| 6 | Influenza A | |||||
| 7 | Herpes simplex infection | |||||
| 8 | Epstein-Barr virus infection | |||||
| PID Pathway | [+] 5 PID Pathways | + | ||||
| 1 | IL27-mediated signaling events | |||||
| 2 | Signaling events mediated by PTP1B | |||||
| 3 | IL12-mediated signaling events | |||||
| 4 | IL6-mediated signaling events | |||||
| 5 | IL23-mediated signaling events | |||||
| Reactome | [+] 5 Reactome Pathways | + | ||||
| 1 | Interleukin-6 signaling | |||||
| 2 | MAPK3 (ERK1) activation | |||||
| 3 | MAPK1 (ERK2) activation | |||||
| 4 | Interferon alpha/beta signaling | |||||
| 5 | Regulation of IFNA signaling | |||||
| WikiPathways | [+] 7 WikiPathways | + | ||||
| 1 | Interferon type I signaling pathways | |||||
| 2 | IL-4 Signaling Pathway | |||||
| 3 | IL-6 signaling pathway | |||||
| 4 | Oncostatin M Signaling Pathway | |||||
| 5 | Interleukin-11 Signaling Pathway | |||||
| 6 | Type III interferon signaling | |||||
| 7 | Interferon alpha/beta signaling | |||||
| References | Top | |||||
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| REF 1 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 2 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 3 | ClinicalTrials.gov (NCT03210961) A First in Human Study to Evaluate Safety, Tolerability, and Pharmacology of PF-06826647 in Healthy Subjects and Subjects With Plaque Psoriasis. U.S. National Institutes of Health. | |||||
| REF 4 | Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases. J Med Chem. 2020 Nov 25;63(22):13561-13577. | |||||
| REF 5 | 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 6 | 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 7 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8. | |||||
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