The Ligandable Human Proteome

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Tyrosine-protein kinase JAK2

Protein kinase domain

IndexLigand NameStructurePDB codeCompound Potency nM
1dqxCrystal Structure of JAK2 complexed with a potent quinoxaline ATP site inhibitor3krr0.48
21k3JAK2 kinase (JH1 domain) in complex with compound 94jia0.6
3jzhJanus Kinase 2 Inhibitors3jy91
46tpco-crystal structure of Jak2 with thienopyridine 193tjd1
550vCRYSTAL STRUCTURE OF JANUS KINASE 2 IN COMPLEX WITH N,N-DICYCLOPROPYL-10-ETHYL-7-[(3-METHOXYPROPYL)AMINO] -3-METHYL-3,5,8,10-TETRAAZATRICYCLO[7.3.0.0,6] DODECA-1(9),2(6),4,7,11-PENTAENE-11-CARBOXAMIDE5cf81.1
6l0iStructure determination of Aurora Kinase in complex with inhibitor2w1i1.2
7j2iStructure of Janus kinase 2 with a pyrrolotriazine inhibitor3q321.8
8467Discovery of VX-509 (Decernotinib): A Potent and Selective Janus kinase (JAK) 3 Inhibitor for the Treatment of Autoimmune Diseases4yth2
9o19Aminoalkylpyrimidine Inhibitor Complexes with JAK24bbf2.2
104okCRYSTAL STRUCTURE OF JANUS KINASE 2 IN COMPLEX WITH A 9H-CARBAZOLE-1-CARBOXAMIDE INHIBITOR4zim2.4
1150wCRYSTAL STRUCTURE OF JANUS KINASE 2 IN COMPLEX WITH N,N-DICYCLOPROPYL-7-[(DIMETHYL-1,3-THIAZOL-2-YL)AMINO]-10-ETHYL-3-METHYL-3,5,8,10-TETRAAZATRICYCLO[7.3.0.02,6] DODECA-1(9),2(6),4,7,11-PENTAENE-11-CARBOXAMIDE5cf52.5
12az5Inhibitors of Jak2 Kinase domain2xa43
133o4Aminoalkylpyrimidine Inhibitor Complexes with JAK24bbe3.6
14lmmInhibitors of Jak2 Kinase domain4c614
157gyDesign and Synthesis of a pan-JAK Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin5tq44.2
160nvJAK2 kinase (JH1 domain) triple mutant in complex with compound 124e6q4.4
1717pCrystals structure of Jak2 with a 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitor3rvg5
184hzDiscovery of VX-509 (Decernotinib): A Potent and Selective Janus kinase (JAK) 3 Inhibitor for the Treatment of Autoimmune Diseases4ytf7
19953Pyrrole-3-carboxamides as potent and selective JAK2 inhibitors4d0x8
2050oCRYSTAL STRUCTURE OF JANUS KINASE 2 IN COMPLEX WITH N,N-DICYCLOPROPYL-10-[(2S)-2,3-DIHYDROXYPROPYL]-3-METHYL-7-(METHYLAMINO)-3,5,8,10-TETRAAZATRICYCLO [7.3.0.02,6]DODECA-1(9),2(6),4,7,11-PENTAENE-11-CARBOXAMIDE5cf68.2
211p62-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK23iok11
2215vJAK2 kinase (JH1 domain) in complex with compound 84hge11.9
23vjkDiscovery of VX-509 (Decernotinib): A Potent and Selective Janus kinase (JAK) 3 Inhibitor for the Treatment of Autoimmune Disease4yti13
241p52-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK23io717
257gtDesign and Synthesis of a pan-JAK Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin5tq721.2
26mi1Crystal structures of JAK1 and JAK2 inhibitor complexes3fup21.7
27bjgPyrrole-3-carboxamides as potent and selective JAK2 inhibitors4d1s22
287gsDesign and Synthesis of a pan-JAK Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin5tq823.1
290x5JAK2 kinase (JH1 domain) in complex with 2,6-DICHLORO-N-{2-[(CYCLOPROPYLCARBONYL)AMINO]PYRIDIN-4-YL}BENZAMIDE4gmy28
300tpCo-crystal structure of jak2 with thienopyridine 83tjc31
31skeJAK2 JH1 in complex with JNJ-77066215usy31
3250yCRYSTAL STRUCTURE OF JANUS KINASE 2 IN COMPLEX WITH N,N-DICYCLOPROPYL-10-ETHYL-7-[(3-METHOXYPROPYL)AMINO] -3-METHYL-3,5,8,10-TETRAAZATRICYCLO[7.3.0.0,6] DODECA-1(9),2(6),4,7,11-PENTAENE-11-CARBOXAMIDE5cf440
33nvbCrystal structure of Jak2 complexed with a potent 2,8-diaryl-quinoxaline inhibitor3lpb42
347gxDesign and Synthesis of a pan-JAK Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin5tq558.8
350x2JAK2 kinase (JH1 domain) with 2,6-DICHLORO-N-(2-OXO-2,5-DIHYDROPYRIDIN-4-YL)BENZAMIDE4gfm60
36skeJAK2 JH2 in complex with JNJ-77066215usz106
377gvDesign and Synthesis of a pan-JAK Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin5tq6123.6
389zsIdentification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model5wev150
39046Structural basis of Jak2 inhibition by the type II inhibtor NVP-BBT5943ugc947
4035rJAK2 JH2 in complex with AT92835ut01323
412hbTriazolopyridine compounds as selective JAK1 inhibitors: from hit identification to GLPG06344p7e1.75e+004
42dqxJAK2 JH2 in complex with NVP-BSK8055ut44.2e+004