The Ligandable Human Proteome

Tyrosine-protein kinase JAK2

Index	Ligand Name	Structure	PDB code	ligand desolvation
1	mi1	Crystal structures of JAK1 and JAK2 inhibitor complexes	3fup	94.84
2	d7d	Crystal Structure of JAK2 in complex with compound 25	6bbv	94.19
3	0nv	JAK2 kinase (JH1 domain) triple mutant in complex with compound 12	4e6q	91.69
4	0x2	JAK2 kinase (JH1 domain) with 2,6-DICHLORO-N-(2-OXO-2,5-DIHYDROPYRIDIN-4-YL)BENZAMIDE	4gfm	91.53
5	15v	JAK2 kinase (JH1 domain) in complex with compound 8	4hge	90.54
6	1p6	2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2	3iok	90.38
7	7gv	Design 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 Skin	5tq6	90.25
8	046	Structural basis of Jak2 inhibition by the type II inhibtor NVP-BBT594	3ugc	89.31
9	1p5	2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2	3io7	88.81
10	953	Pyrrole-3-carboxamides as potent and selective JAK2 inhibitors	4d0x	88.72
11	jzh	Janus Kinase 2 Inhibitors	3jy9	88.25
12	7gy	Design 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 Skin	5tq4	88
13	vjk	Discovery of VX-509 (Decernotinib): A Potent and Selective Janus kinase (JAK) 3 Inhibitor for the Treatment of Autoimmune Disease	4yti	87.22
14	4hz	Discovery of VX-509 (Decernotinib): A Potent and Selective Janus kinase (JAK) 3 Inhibitor for the Treatment of Autoimmune Diseases	4ytf	87.03
15	9t6	Crystal structure of JAK2 in complex with peficitinib	6aaj	86.45
16	az5	Inhibitors of Jak2 Kinase domain	2xa4	86.39
17	0tp	Co-crystal structure of jak2 with thienopyridine 8	3tjc	86.36
18	50y	CRYSTAL 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-CARBOXAMIDE	5cf4	85.98
19	467	Discovery of VX-509 (Decernotinib): A Potent and Selective Janus kinase (JAK) 3 Inhibitor for the Treatment of Autoimmune Diseases	4yth	85.71
20	6tp	co-crystal structure of Jak2 with thienopyridine 19	3tjd	85.11
21	50o	CRYSTAL 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-CARBOXAMIDE	5cf6	84.79
22	ekt	Crystal Structure of JAK2-V617F pseudokinase domain in complex with Compound 2	6g3c	84.67
23	j2i	Structure of Janus kinase 2 with a pyrrolotriazine inhibitor	3q32	83.96
24	50v	CRYSTAL 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-CARBOXAMIDE	5cf8	83.67
25	nvb	Crystal structure of Jak2 complexed with a potent 2,8-diaryl-quinoxaline inhibitor	3lpb	82.52
26	584	JAK2 Pseudokinase in complex with BI-D1870	5wik	81.69
27	50w	CRYSTAL 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-CARBOXAMIDE	5cf5	81.06
28	7gx	Design 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 Skin	5tq5	80.64
29	7gt	Design 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 Skin	5tq7	80.39
30	lmm	Inhibitors of Jak2 Kinase domain	4c61	80.34
31	2hb	Triazolopyridine compounds as selective JAK1 inhibitors: from hit identification to GLPG0634	4p7e	80.28
32	dqx	Crystal Structure of JAK2 complexed with a potent quinoxaline ATP site inhibitor	3krr	79.8
33	ske	JAK2 JH1 in complex with JNJ-7706621 (Crystal Form 2)	6drw	79.21
34	o19	Aminoalkylpyrimidine Inhibitor Complexes with JAK2	4bbf	78.8
35	ydj	JAK2 Pseudokinase in complex with AZD7762	5wil	78.5
36	7dz	JAK2 JH2 in complex with BI-D1870	5ut1	77.98
37	1m3	JAK2 kinase (JH1 domain) in complex with TG101209	4ji9	77.93
38	3o4	Aminoalkylpyrimidine Inhibitor Complexes with JAK2	4bbe	77.41
39	xww	Inhibitors of Jak2 Kinase domain	4c62	76.7
40	5bs	JAK2 JH2 in complex with XMU-MP-1	6brw	75.68
41	ske	JAK2 Pseudokinase in complex with JNJ7706621	5win	75.11
42	2hb	JAK2 JH2 in complex with GLPG0634	5ut5	74.78
43	bjg	Pyrrole-3-carboxamides as potent and selective JAK2 inhibitors	4d1s	74.75
44	ske	JAK2 JH2 in complex with JNJ-7706621	5usz	74.23
45	17p	Crystals structure of Jak2 with a 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitor	3rvg	74.16
46	0x5	JAK2 kinase (JH1 domain) in complex with 2,6-DICHLORO-N-{2-[(CYCLOPROPYLCARBONYL)AMINO]PYRIDIN-4-YL}BENZAMIDE	4gmy	73.47
47	ik1	JAK2 JH2 in complex with IKK-2 Inhibitor VI	5ut3	73.08
48	4ok	CRYSTAL STRUCTURE OF JANUS KINASE 2 IN COMPLEX WITH A 9H-CARBAZOLE-1-CARBOXAMIDE INHIBITOR	4zim	72.94
49	9zs	Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model	5wev	72.01
50	ske	JAK2 JH1 in complex with JNJ-7706621	5usy	71.25
51	3yt	JAK2 JH2 in complex with PRT062607	5ut2	71.12
52	l0i	Structure determination of Aurora Kinase in complex with inhibitor	2w1i	70.94
53	7gs	Design 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 Skin	5tq8	70.72
54	4sp	JAK2 JH2 in complex with NU6102	6bss	69.84
55	35r	JAK2 Pseudokinase in complex with AT9283	5wim	69.54
56	dqx	JAK2 JH2 in complex with NVP-BSK805	5ut4	68.34
57	35r	JAK2 JH2 in complex with AT9283	5ut0	65.05
58	1k3	JAK2 kinase (JH1 domain) in complex with compound 9	4jia	64.66
59	aqg	JAK2 Pseudokinase in complex with NU6140	5wij	64.38