3-(2-(2-((4-Morpholinophenyl)amino)pyrimidin-4-yl)-6,7-dihydrofuro[3,2-c]pyridin-5(4H)-yl)-3-oxopropanenitrile

ID: ALA3948663

PubChem CID: 72202399

Max Phase: Preclinical

Molecular Formula: C24H24N6O3

Molecular Weight: 444.50

Molecule Type: Small molecule

This compound is available for customization.

Associated Items:

Bioactivity Summary Target Summary Assay Summary

Names and Identifiers

Canonical SMILES: N#CCC(=O)N1CCc2oc(-c3ccnc(Nc4ccc(N5CCOCC5)cc4)n3)cc2C1

Standard InChI: InChI=1S/C24H24N6O3/c25-8-5-23(31)30-10-7-21-17(16-30)15-22(33-21)20-6-9-26-24(28-20)27-18-1-3-19(4-2-18)29-11-13-32-14-12-29/h1-4,6,9,15H,5,7,10-14,16H2,(H,26,27,28)

Standard InChI Key: GGDYPNFYGKVTEZ-UHFFFAOYSA-N

Molfile:

     RDKit          2D

 33 37  0  0  0  0  0  0  0  0999 V2000
   11.9885   -5.7430    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   11.1713   -5.7430    0.0000 N   0  0  0  0  0  0  0  0  0  0  0  0
   10.7627   -6.4480    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   11.1713   -7.1571    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   11.9885   -7.1571    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   12.3971   -6.4480    0.0000 N   0  0  0  0  0  0  0  0  0  0  0  0
   12.3971   -5.0339    0.0000 N   0  0  0  0  0  0  0  0  0  0  0  0
   13.2142   -5.0339    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   13.6228   -5.7430    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   14.4400   -5.7430    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   14.8486   -5.0339    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   14.4400   -4.3290    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   13.6228   -4.3290    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   17.3002   -5.0339    0.0000 O   0  0  0  0  0  0  0  0  0  0  0  0
   16.8916   -4.3290    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   16.0744   -4.3290    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   15.6658   -5.0339    0.0000 N   0  0  0  0  0  0  0  0  0  0  0  0
   16.0744   -5.7430    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
   16.8916   -5.7430    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
    7.9790   -7.2652    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
    8.6881   -6.8566    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
    8.6881   -6.0394    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
    7.9790   -5.6308    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
    7.2741   -6.0394    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
    7.2741   -6.8566    0.0000 N   0  0  0  0  0  0  0  0  0  0  0  0
    9.4653   -5.7889    0.0000 O   0  0  0  0  0  0  0  0  0  0  0  0
    9.4653   -7.1113    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
    9.9455   -6.4480    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
    6.5660   -7.2646    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
    5.8586   -6.8554    0.0000 O   0  0  0  0  0  0  0  0  0  0  0  0
    6.5653   -8.0818    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
    5.8573   -8.4898    0.0000 C   0  0  0  0  0  0  0  0  0  0  0  0
    5.1499   -8.8975    0.0000 N   0  0  0  0  0  0  0  0  0  0  0  0
  1  2  1  0
  2  3  2  0
  3  4  1  0
  4  5  2  0
  5  6  1  0
  1  6  2  0
  1  7  1  0
  8  9  1  0
  9 10  2  0
 10 11  1  0
 11 12  2  0
 12 13  1  0
  8 13  2  0
 14 15  1  0
 15 16  1  0
 16 17  1  0
 17 18  1  0
 18 19  1  0
 14 19  1  0
 11 17  1  0
  7  8  1  0
 20 21  1  0
 21 22  2  0
 22 23  1  0
 23 24  1  0
 24 25  1  0
 20 25  1  0
 27 28  2  0
 26 28  1  0
 21 27  1  0
 22 26  1  0
  3 28  1  0
 25 29  1  0
 29 30  2  0
 29 31  1  0
 31 32  1  0
 32 33  3  0
M  END

Associated Targets(Human)

JAK2 Tclin Tyrosine-protein kinase JAK2 (12915 Activities)

Discover Target: JAK2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

JAK3 Tclin Tyrosine-protein kinase JAK3 (8349 Activities)

Discover Target: JAK3

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

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

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

Calculated Properties

Molecular Weight: 444.50	Molecular Weight (Monoisotopic): 444.1910	AlogP: 3.12	#Rotatable Bonds: 5
Polar Surface Area: 107.52	Molecular Species: NEUTRAL	HBA: 8	HBD: 1
#RO5 Violations: ┄	HBA (Lipinski): 9	HBD (Lipinski): 1	#RO5 Violations (Lipinski): ┄
CX Acidic pKa: 9.14	CX Basic pKa: 2.30	CX LogP: 2.00	CX LogD: 1.99
Aromatic Rings: 3	Heavy Atoms: 33	QED Weighted: 0.64	Np Likeness Score: -1.57

References

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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]

3-(2-(2-((4-Morpholinophenyl)amino)pyrimidin-4-yl)-6,7-dihydrofuro[3,2-c]pyridin-5(4H)-yl)-3-oxopropanenitrile

Names and Identifiers

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Associated Targets(non-human)

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References

Source