ID: ALA3940537
Cas Number: 1438284-00-4
PubChem CID: 76072368
Max Phase: Preclinical
Molecular Formula: C23H27N5O4S
Molecular Weight: 469.57
Molecule Type: Small molecule
Associated Items:
Canonical SMILES: Cc1cnc(Nc2ccc(N3CCOCC3)cc2)nc1-c1cc2c(o1)CCN(S(C)(=O)=O)C2
Standard InChI: InChI=1S/C23H27N5O4S/c1-16-14-24-23(25-18-3-5-19(6-4-18)27-9-11-31-12-10-27)26-22(16)21-13-17-15-28(33(2,29)30)8-7-20(17)32-21/h3-6,13-14H,7-12,15H2,1-2H3,(H,24,25,26)
Standard InChI Key: YDZHOVOPBMIATL-UHFFFAOYSA-N
Molfile:
RDKit 2D
33 37 0 0 0 0 0 0 0 0999 V2000
3.8507 -9.9755 0.0000 O 0 0 0 0 0 0 0 0 0 0 0 0
4.6431 -9.7650 0.0000 S 0 0 0 0 0 0 0 0 0 0 0 0
4.0646 -9.1840 0.0000 O 0 0 0 0 0 0 0 0 0 0 0 0
10.0672 -8.2421 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
9.2500 -8.2421 0.0000 N 0 0 0 0 0 0 0 0 0 0 0 0
8.8414 -8.9512 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
9.2500 -9.6603 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
10.0672 -9.6603 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
10.4758 -8.9512 0.0000 N 0 0 0 0 0 0 0 0 0 0 0 0
10.4758 -7.5371 0.0000 N 0 0 0 0 0 0 0 0 0 0 0 0
11.2930 -7.5371 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
11.7016 -8.2421 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
12.5188 -8.2421 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
12.9274 -7.5371 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
12.5188 -6.8280 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
11.7016 -6.8280 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
15.3790 -7.5371 0.0000 O 0 0 0 0 0 0 0 0 0 0 0 0
14.9704 -6.8280 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
14.1532 -6.8280 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
13.7446 -7.5371 0.0000 N 0 0 0 0 0 0 0 0 0 0 0 0
14.1532 -8.2421 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
14.9704 -8.2421 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
6.0578 -9.7684 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
6.7669 -9.3598 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
6.7669 -8.5426 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
6.0578 -8.1340 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
5.3528 -8.5426 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
5.3528 -9.3598 0.0000 N 0 0 0 0 0 0 0 0 0 0 0 0
7.5441 -8.2920 0.0000 O 0 0 0 0 0 0 0 0 0 0 0 0
7.5441 -9.6144 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
8.0243 -8.9512 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
8.8414 -10.3693 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
4.6430 -10.5855 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
2 1 2 0
3 2 2 0
4 5 1 0
5 6 2 0
6 7 1 0
7 8 2 0
8 9 1 0
4 9 2 0
4 10 1 0
11 12 1 0
12 13 2 0
13 14 1 0
14 15 2 0
15 16 1 0
11 16 2 0
17 18 1 0
18 19 1 0
19 20 1 0
20 21 1 0
21 22 1 0
17 22 1 0
14 20 1 0
10 11 1 0
23 24 1 0
24 25 2 0
25 26 1 0
26 27 1 0
27 28 1 0
23 28 1 0
30 31 2 0
29 31 1 0
24 30 1 0
25 29 1 0
28 2 1 0
6 31 1 0
7 32 1 0
2 33 1 0
M END| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Natural Product: No | Oral: No | Chemical Probe: No | Parenteral: No |
| Molecule Type: Small molecule | Topical: No | First In Class: No | Black Box: No |
| Chirality: No | Availability: No | Prodrug: No |
| MESH ID | MESH Heading | EFO IDs | EFO Terms | Max Phase for Indication | References |
|---|
| Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
|---|
| Molecular Weight: 469.57 | Molecular Weight (Monoisotopic): 469.1784 | AlogP: 2.94 | #Rotatable Bonds: 5 |
| Polar Surface Area: 100.80 | Molecular Species: NEUTRAL | HBA: 8 | HBD: 1 |
| #RO5 Violations: ┄ | HBA (Lipinski): 9 | HBD (Lipinski): 1 | #RO5 Violations (Lipinski): ┄ |
| CX Acidic pKa: ┄ | CX Basic pKa: 2.30 | CX LogP: 2.06 | CX LogD: 2.06 |
| Aromatic Rings: 3 | Heavy Atoms: 33 | QED Weighted: 0.61 | Np Likeness Score: -1.53 |
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| 2. Changelian, Paul S PS and 58 more authors. 2003-10-31 Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. [PMID:14593182] |
| 3. Côté, Bernard B and 19 more authors. 2007-12-15 Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. [PMID:18029174] |
| 4. Changelian, Paul S PS and 13 more authors. 2008-02-15 The specificity of JAK3 kinase inhibitors. [PMID:18094329] |
| 5. Gozgit, Joseph M JM and 11 more authors. 2008-11-21 Effects of the JAK2 inhibitor, AZ960, on Pim/BAD/BCL-xL survival signaling in the human JAK2 V617F cell line SET-2. [PMID:18775810] |
| 6. Jiang, Jian-kang and 12 more authors. 2008-12-25 Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550). [PMID:19053756] |
| 7. Pardanani, A A and 5 more authors. 2009-08 CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients. [PMID:19295546] |
| 8. Hall, Matthew D and 8 more authors. 2009-05-28 Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. [PMID:19397322] |
| 9. Zarrinkar, Patrick P PP and 15 more authors. 2009-10-01 AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). [PMID:19654408] |
| 10. Ledeboer, Mark W MW and 20 more authors. 2009-12-01 2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2. [PMID:19857967] |
| 11. Fridman, Jordan S JS and 21 more authors. 2010-05-01 Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. [PMID:20363976] |
| 12. Flanagan, Mark E ME and 22 more authors. 2010-12-23 Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection. [PMID:21105711] |
| 13. Malerich, Jeremiah P JP and 6 more authors. 2010-12-15 Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3. [PMID:21106455] |
| 14. Ioannidis, Stephanos S and 20 more authors. 2011-01-13 Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway. [PMID:21138246] |
| 15. William, Anthony D AD and 18 more authors. 2011-07-14 Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymphoma. [PMID:21604762] |
| 16. Purandare, A V AV and 28 more authors. 2012-02 Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2. [PMID:22015772] |
| 17. Weinberg, Linda R LR and 13 more authors. 2011-12-15 2,7-Pyrrolo[2,1-f][1,2,4]triazines as JAK2 inhibitors: modification of target structure to minimize reactive metabolite formation. [PMID:22041060] |
| 18. William, Anthony D AD and 16 more authors. 2012-01-12 Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase-3 (FLT3) for the treatment of cancer. [PMID:22148278] |
| 19. William, Anthony D AD and 16 more authors. 2012-03-22 Discovery of the macrocycle (9E)-15-(2-(pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a potent inhibitor of janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) for the treatment of rheumatoid arthritis. [PMID:22339472] |
| 20. Kulagowski, Janusz J JJ and 29 more authors. 2012-06-28 Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors. [PMID:22591402] |
| 21. Chen, Huifen H and 14 more authors. 2012-06-14 Discovery of selective LRRK2 inhibitors guided by computational analysis and molecular modeling. [PMID:22591441] |
| 22. Dugan, Benjamin J BJ and 18 more authors. 2012-06-14 A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of Janus kinase 2 for use in anticancer therapy: discovery of CEP-33779. [PMID:22594690] |
| 23. Nakaya, Y Y and 11 more authors. 2011-07 Efficacy of NS-018, a potent and selective JAK2/Src inhibitor, in primary cells and mouse models of myeloproliferative neoplasms. [PMID:22829185] |
| 24. Hanan, Emily J EJ and 22 more authors. 2012-11-26 Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors. [PMID:23061660] |
| 25. Soth, Michael M and 38 more authors. 2013-01-10 3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models. [PMID:23214979] |
| 26. Ma, L L and 22 more authors. 2013-04-12 Discovery and characterization of LY2784544, a small-molecule tyrosine kinase inhibitor of JAK2V617F. [PMID:23584399] |
| 27. Cirstea, D D and 15 more authors. 2013-12 Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. [PMID:23807770] |
| 28. Liang, Jun J and 31 more authors. 2013-09 Lead identification of novel and selective TYK2 inhibitors. [PMID:23867602] |
| 29. Van Rompaey, Luc L and 16 more authors. 2013-10-01 Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. [PMID:24006460] |
| 30. Kim, Mi Kyoung MK, Shin, Heerim H, Cho, Seo Young SY and Chong, Youhoon Y. 2014-02-01 Linear propargylic alcohol functionality attached to the indazole-7-carboxamide as a JAK1-specific linear probe group. [PMID:24398382] |
| 31. McDonnell, Mark E ME and 6 more authors. 2014-02-15 Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors. [PMID:24461299] |
| 32. Haidle, Andrew M AM and 14 more authors. 2014-04-15 Thiophene carboxamide inhibitors of JAK2 as potential treatments for myleoproliferative neoplasms. [PMID:24666646] |
| 33. Currie, Kevin S KS and 16 more authors. 2014-05-08 Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase. [PMID:24779514] |
| 34. Works, Melissa G MG and 11 more authors. 2014-10-01 Inhibition of TYK2 and JAK1 ameliorates imiquimod-induced psoriasis-like dermatitis by inhibiting IL-22 and the IL-23/IL-17 axis. [PMID:25156366] |
| 35. Coffey, Greg G and 8 more authors. 2014-12 The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. [PMID:25253883] |
| 36. Menet, Christel J CJ and 18 more authors. 2014-11-26 Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634. [PMID:25369270] |
| 37. Tanimoto, Atsuo A and 10 more authors. 2015-01 Pharmacological properties of JTE-052: a novel potent JAK inhibitor that suppresses various inflammatory responses in vitro and in vivo. [PMID:25387665] |
| 38. Ye, Qing Q and 14 more authors. 2015-03-01 Synthesis and biological evaluation of 3-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-4-(indol-3-yl)-maleimides as potent, selective GSK-3β inhibitors and neuroprotective agents. [PMID:25662701] |
| 39. Lawrence, Harshani R HR and 10 more authors. 2015-03-26 Development of novel ACK1/TNK2 inhibitors using a fragment-based approach. [PMID:25699576] |
| 40. Yamagishi, Hiroaki H and 10 more authors. 2015-08-01 Discovery of 3,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2(1H)-one derivatives as novel JAK inhibitors. [PMID:26059596] |
| 41. Tan, Li L and 18 more authors. 2015-08-27 Development of Selective Covalent Janus Kinase 3 Inhibitors. [PMID:26258521] |
| 42. Wan, Honghe H and 34 more authors. 2015-08-13 Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms. [PMID:26288683] |
| 43. Simov, Vladimir V and 15 more authors. 2016-04-01 Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors. [PMID:26927423] |
| 44. Wang, Tingfang T and 6 more authors. 2016-06-15 Design, synthesis and evaluation of pyrrolo[2,3-d]pyrimidine-phenylamide hybrids as potent Janus kinase 2 inhibitors. [PMID:27130359] |
| 45. Liang, Xuewu X and 6 more authors. 2016-06-15 Design, synthesis and preliminary biological evaluation of 4-aminopyrazole derivatives as novel and potent JAKs inhibitors. [PMID:27137359] |
| 46. Valenciano, Ana L AL, Ramsey, Aaron C AC, Santos, Webster L WL and Mackey, Zachary B ZB. 2016-10-01 Discovery and antiparasitic activity of AZ960 as a Trypanosoma brucei ERK8 inhibitor. [PMID:27519462] |
| 47. Lee, Sun-Mi SM and 11 more authors. 2016-11-01 The discovery of 2,5-isomers of triazole-pyrrolopyrimidine as selective Janus kinase 2 (JAK2) inhibitors versus JAK1 and JAK3. [PMID:27555284] |
| 48. Ito, Misato M and 11 more authors. 2017-01 A novel JAK inhibitor, peficitinib, demonstrates potent efficacy in a rat adjuvant-induced arthritis model. [PMID:28117214] |
| 49. Liu, Zhiqing and 6 more authors. 2017-06-08 Drug Discovery Targeting Bromodomain-Containing Protein 4. [PMID:28195723] |
| 50. Puleo, David E DE and 7 more authors. 2017-06-08 Identification and Characterization of JAK2 Pseudokinase Domain Small Molecule Binders. [PMID:28626521] |
| 51. Liang, Jun J and 32 more authors. 2017-09-15 Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model. [PMID:28830649] |
| 52. Klaeger, Susan S and 47 more authors. 2017-12-01 The target landscape of clinical kinase drugs. [PMID:29191878] |
| 53. Vazquez, Michael L ML and 34 more authors. 2018-02-08 Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases. [PMID:29298069] |
| 54. Chough, Chieyeon C and 5 more authors. 2018-05-01 Development of selective inhibitors for the treatment of rheumatoid arthritis: (R)-3-(3-(Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)pyrrolidin-1-yl)-3-oxopropanenitrile as a JAK1-selective inhibitor. [PMID:29452839] |
| 55. Huang, Yahui Y and 5 more authors. 2018-07-26 Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections. [PMID:29940115] |
| 56. Drilon, Alexander A and 21 more authors. 2018-10 Repotrectinib (TPX-0005) Is a Next-Generation ROS1/TRK/ALK Inhibitor That Potently Inhibits ROS1/TRK/ALK Solvent- Front Mutations. [PMID:30093503] |
| 57. Hamaguchi, Hisao H and 9 more authors. 2018-10-01 Discovery and structural characterization of peficitinib (ASP015K) as a novel and potent JAK inhibitor. [PMID:30145050] |
| 58. Chu-Farseeva, Yu-Yi YY and 6 more authors. 2018-10-05 Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat. [PMID:30243158] |
| 59. Barker, Michael D MD and 11 more authors. 2018-11-15 Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease. [PMID:30249354] |
| 60. Narayan, Satya S and 7 more authors. 2019-01-01 ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. [PMID:30384048] |
| 61. Elsayed, Mohamed S A MSA and 9 more authors. 2018-12-13 Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series. [PMID:30460842] |
| 62. Yin, Yuan Y and 5 more authors. 2019-04-15 Discovery of novel selective Janus kinase 2 (JAK2) inhibitors bearing a 1H-pyrazolo[3,4-d]pyrimidin-4-amino scaffold. [PMID:30846405] |
| 63. Yu, Ru-Nan RN and 6 more authors. 2019-04-15 Structure-based design and synthesis of pyrimidine-4,6-diamine derivatives as Janus kinase 3 inhibitors. [PMID:30853331] |
| 64. Spergel, Steven H SH and 24 more authors. 2019-03-14 Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis. [PMID:30891131] |
| 65. Liang, Xuewu X and 11 more authors. 2019-04-25 Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies. [PMID:30901208] |
| 66. Zak, Mark M and 28 more authors. 2019-06-15 Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling. [PMID:30981576] |
| 67. Wang, Wanqi W and 16 more authors. 2019-06-15 Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2. [PMID:30981578] |
| 68. Yuan, Ting T and 8 more authors. 2019-09-15 Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade. [PMID:31207462] |
| 69. Moslin, Ryan R and 28 more authors. 2019-07-17 Identification of N-Methyl Nicotinamide and N-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2). [PMID:31314518] |
| 70. Wrobleski, Stephen T ST and 31 more authors. 2019-07-18 Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165. [PMID:31318208] |
| 71. Collier, Philip N PN and 16 more authors. 2019-08-08 Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase Cθ (PKCθ) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis. [PMID:31417666] |
| 72. Yang, Tao and 13 more authors. 2019-11-27 Discovery of Potent and Orally Effective Dual Janus Kinase 2/FLT3 Inhibitors for the Treatment of Acute Myelogenous Leukemia and Myeloproliferative Neoplasms. [PMID:31670517] |
| 73. Ren, Jing and 11 more authors. 2020-01-15 Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors. [PMID:31843459] |
| 74. Shu, Lei and 9 more authors. 2020-04-01 Design, synthesis, and pharmacological evaluation of 4- or 6-phenyl-pyrimidine derivatives as novel and selective Janus kinase 3 inhibitors. [PMID:32097841] |
| 75. Ma, Xiangyu and 6 more authors. 2020-04-15 Discovery and optimization of 2-aminopyridine derivatives as novel and selective JAK2 inhibitors. [PMID:32122740] |
| 76. Su, Qibin and 26 more authors. 2020-05-14 Discovery of (2R)-N-[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1H-indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 Inhibitor. [PMID:32297743] |
| 77. Gerstenberger, Brian S and 23 more authors. 2020-11-25 Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases. [PMID:32787094] |
| 78. Yang, Tao and 13 more authors. 2020-12-10 N-(Pyrimidin-2-yl)-1,2,3,4-tetrahydroisoquinolin-6-amine Derivatives as Selective Janus Kinase 2 Inhibitors for the Treatment of Myeloproliferative Neoplasms. [PMID:33256400] |
| 79. Davis, Ryan R and 10 more authors. 2021-02-25 Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof. [PMID:33570945] |
| 80. Zhang, Chufeng and 9 more authors. 2021-02-25 Discovery of 3-(4-(2-((1H-Indol-5-yl)amino)-5-fluoropyrimidin-4-yl)-1H-pyrazol-1-yl)propanenitrile Derivatives as Selective TYK2 Inhibitors for the Treatment of Inflammatory Bowel Disease. [PMID:33593051] |
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