ruxolitinib Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	4190	941678-49-5

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: ruxolitinib jakafi INCB 018424 ruxolitinib phosphate jakavi

a kinase inhibitor, inhibits Janus Associated Kinases (JAKs) JAK1 and JAK2 which mediate the signaling of a number of cytokines and growth factors that are important for hematopoiesis and immune function. Although some small studies have suggested possibility of benefit from ruxolitinib in patients with COVID-19, it is not recommended the use of JAK inhibitors other than baricitinib for the treatment of COVID-19. Molecular weight: 306.37 Formula: C17H18N6 CLOGP: 2.22 LIPINSKI: 0 HAC: 6 HDO: 1 TPSA: 83.18 ALOGS: -3.42 ROTB: 4 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Nov. 16, 2011	FDA	INCYTE CORP

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Platelet count decreased	392.83	18.58	297	14992	99727	46571046
Platelet count increased	383.46	18.58	154	15135	14720	46656053
Haemoglobin decreased	356.60	18.58	312	14977	128637	46542136
Splenomegaly	352.67	18.58	129	15160	9559	46661214
Myelofibrosis	244.34	18.58	61	15228	1198	46669575
Blood count abnormal	236.67	18.58	116	15173	17762	46653011
Anaemia	201.33	18.58	325	14964	255454	46415319
Weight increased	178.15	18.58	243	15046	164230	46506543
Product dose omission issue	157.37	18.58	232	15057	168288	46502485
Death	154.52	18.58	339	14950	335209	46335564
Contusion	153.14	18.58	165	15124	87322	46583451
White blood cell count increased	148.60	18.58	120	15169	44099	46626674
Red blood cell count decreased	112.69	18.58	90	15199	32533	46638240
Acute myeloid leukaemia	97.33	18.58	62	15227	15716	46655057
Increased appetite	85.73	18.58	46	15243	8481	46662292
Thrombocytopenia	78.37	18.58	145	15144	126436	46544337
Primary myelofibrosis	75.44	18.58	14	15275	58	46670715
Flatulence	73.75	18.58	67	15222	28811	46641962
Dizziness	64.84	18.58	251	15038	340163	46330610
Fatigue	62.98	18.58	376	14913	608321	46062452
Drug hypersensitivity	55.98	18.58	7	15282	243818	46426955
Night sweats	50.41	18.58	53	15236	27197	46643576
Haematocrit decreased	49.13	18.58	59	15230	34998	46635775
Febrile neutropenia	47.13	18.58	99	15190	94528	46576245
Abdominal distension	41.58	18.58	81	15208	73270	46597503
Bone pain	39.96	18.58	62	15227	46828	46623945
Transfusion	38.36	18.58	33	15256	13198	46657575
Drug ineffective	38.08	18.58	106	15183	677732	45993041
Graft versus host disease in liver	36.40	18.58	11	15278	447	46670326
Graft versus host disease	35.99	18.58	24	15265	6564	46664209
Graft versus host disease in gastrointestinal tract	35.07	18.58	17	15272	2533	46668240
Epistaxis	34.02	18.58	69	15220	64236	46606537
Platelet count abnormal	33.73	18.58	17	15272	2755	46668018
Therapeutic response unexpected	33.67	18.58	33	15256	15583	46655190
Fungal endocarditis	33.07	18.58	9	15280	250	46670523
Muscle spasms	32.19	18.58	101	15188	123012	46547761
White blood cell count decreased	32.08	18.58	95	15194	112136	46558637
Splenectomy	31.94	18.58	10	15279	458	46670315
Eye infection bacterial	29.50	18.58	7	15282	110	46670663
Spleen disorder	28.79	18.58	11	15278	917	46669856
Infective aneurysm	28.40	18.58	9	15280	429	46670344
Gout	28.30	18.58	26	15263	11330	46659443
Product use in unapproved indication	28.29	18.58	79	15210	90194	46580579
Leukaemia	28.23	18.58	16	15273	3279	46667494
Iron overload	27.16	18.58	10	15279	752	46670021
Bronchopulmonary aspergillosis	26.54	18.58	21	15268	7475	46663298
Blast cell count increased	25.84	18.58	8	15281	353	46670420
Toxicity to various agents	25.83	18.58	19	15270	211747	46459026
Haemorrhage	25.67	18.58	56	15233	54813	46615960
Headache	24.75	18.58	252	15037	478100	46192673
Second primary malignancy	24.51	18.58	19	15270	6565	46664208
Cytomegalovirus infection reactivation	23.89	18.58	11	15278	1461	46669312
Pancytopenia	23.35	18.58	71	15218	84987	46585786
Overdose	23.20	18.58	3	15286	101976	46568797
Chronic graft versus host disease	22.72	18.58	13	15276	2712	46668061
JC virus infection	22.62	18.58	11	15278	1651	46669122
Drug interaction	22.55	18.58	20	15269	203074	46467699
Herpes zoster	21.86	18.58	60	15229	67812	46602961
Condition aggravated	21.82	18.58	29	15260	245023	46425750
Adenocarcinoma metastatic	21.67	18.58	5	15284	69	46670704
Blood lactate dehydrogenase increased	21.64	18.58	30	15259	20470	46650303
Asthenia	21.19	18.58	174	15115	310901	46359872
Acute leukaemia	20.03	18.58	9	15280	1129	46669644
Leukocytosis	20.01	18.58	31	15258	23367	46647406
Encopresis	19.75	18.58	5	15284	104	46670669
Encephalitis fungal	19.67	18.58	4	15285	29	46670744
Aspergillus infection	19.59	18.58	17	15272	6873	46663900
Epstein-Barr virus infection reactivation	19.48	18.58	6	15283	260	46670513
Red blood cell count increased	19.03	18.58	11	15278	2339	46668434
Promyelocyte count increased	19.00	18.58	3	15286	3	46670770
Graft versus host disease in skin	18.96	18.58	11	15278	2356	46668417

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Myelofibrosis	386.07	16.56	103	17117	1468	29933790
Splenomegaly	385.33	16.56	177	17043	13303	29921955
Platelet count decreased	330.15	16.56	353	16867	105776	29829482
Death	246.64	16.56	594	16626	356689	29578569
Haemoglobin decreased	224.82	16.56	301	16919	113797	29821461
Anaemia	204.89	16.56	400	16820	207592	29727666
Platelet count increased	186.55	16.56	94	17126	8648	29926610
White blood cell count increased	161.51	16.56	153	17067	39520	29895738
Blood count abnormal	153.32	16.56	91	17129	11561	29923697
Acute myeloid leukaemia	141.95	16.56	102	17118	17904	29917354
Product dose omission issue	126.91	16.56	205	17015	91426	29843832
Febrile neutropenia	123.06	16.56	220	17000	106473	29828785
Second primary malignancy	122.99	16.56	64	17156	6292	29928966
Contusion	81.28	16.56	95	17125	31185	29904073
Red blood cell count decreased	80.45	16.56	87	17133	26234	29909024
Fatigue	68.93	16.56	364	16856	320309	29614949
Blast cell count increased	65.03	16.56	24	17196	1025	29934233
Night sweats	64.77	16.56	59	17161	14469	29920789
Iron overload	60.37	16.56	24	17196	1257	29934001
Acute leukaemia	59.52	16.56	23	17197	1116	29934142
Toxicity to various agents	52.87	16.56	18	17202	177165	29758093
Drug interaction	50.37	16.56	26	17194	199542	29735716
Nocardiosis	48.09	16.56	28	17192	3427	29931831
Weight increased	47.24	16.56	121	17099	74792	29860466
Thrombocytopenia	46.97	16.56	179	17041	136865	29798393
Graft versus host disease	46.77	16.56	42	17178	10108	29925150
Epistaxis	45.95	16.56	97	17123	52884	29882374
Completed suicide	45.44	16.56	3	17217	99489	29835769
Graft versus host disease in gastrointestinal tract	43.06	16.56	25	17195	3044	29932214
Transfusion	42.79	16.56	35	17185	7426	29927832
Leukocytosis	42.54	16.56	57	17163	21445	29913813
Flatulence	42.05	16.56	52	17168	18077	29917181
Blast cells present	40.93	16.56	11	17209	161	29935097
Platelet count abnormal	40.69	16.56	22	17198	2335	29932923
Haematocrit decreased	40.10	16.56	67	17153	30632	29904626
Early satiety	39.92	16.56	14	17206	515	29934743
Leukaemia	38.84	16.56	24	17196	3273	29931985
Pneumonia	38.44	16.56	325	16895	333981	29601277
Primary myelofibrosis	38.10	16.56	9	17211	75	29935183
Eye infection fungal	37.96	16.56	12	17208	318	29934940
Graft versus host disease in liver	34.48	16.56	15	17205	987	29934271
Blast cell crisis	32.56	16.56	8	17212	80	29935178
Overdose	32.18	16.56	5	17215	84332	29850926
Squamous cell carcinoma	31.51	16.56	34	17186	10216	29925042
Hypotension	31.05	16.56	42	17178	200523	29734735
Polycythaemia vera	29.64	16.56	9	17211	208	29935050
Thyroid gland abscess	29.05	16.56	7	17213	64	29935194
Necrotising retinitis	28.74	16.56	12	17208	713	29934545
Retinal ischaemia	28.67	16.56	10	17210	362	29934896
Splenectomy	27.72	16.56	10	17210	400	29934858
Adenovirus infection	26.55	16.56	21	17199	4247	29931011
Infectious thyroiditis	26.14	16.56	7	17213	101	29935157
Skin cancer	25.51	16.56	27	17193	7934	29927324
Increased appetite	25.40	16.56	23	17197	5594	29929664
Varicella zoster virus infection	25.19	16.56	13	17207	1255	29934003
Haemorrhage	24.56	16.56	70	17150	46009	29889249
Graft versus host disease in skin	24.37	16.56	18	17202	3289	29931969
Serum ferritin increased	24.07	16.56	22	17198	5415	29929843
Herpes zoster	23.85	16.56	53	17167	29890	29905368
Gout	22.88	16.56	38	17182	17277	29917981
Cardio-respiratory arrest	22.78	16.56	3	17217	57303	29877955
White blood cell count decreased	22.68	16.56	102	17118	83845	29851413
Product use in unapproved indication	22.56	16.56	93	17127	73600	29861658
Spleen disorder	22.22	16.56	11	17209	972	29934286
Haematocrit increased	21.80	16.56	13	17207	1663	29933595
Syncope	21.46	16.56	11	17209	84892	29850366
Therapeutic response unexpected	21.39	16.56	26	17194	8877	29926381
Procedural pneumothorax	21.35	16.56	5	17215	40	29935218
Plasma cell myeloma	20.78	16.56	3	17217	53459	29881799
Splenic infarction	20.77	16.56	13	17207	1812	29933446
Septic embolus	20.73	16.56	11	17209	1124	29934134
Seizure	20.44	16.56	16	17204	98459	29836799
Drug hypersensitivity	20.33	16.56	7	17213	68512	29866746
Cerebral artery embolism	19.99	16.56	10	17210	904	29934354
Myeloproliferative neoplasm	19.76	16.56	8	17212	439	29934819
Cytopenia	19.65	16.56	24	17196	8232	29927026
Scleroderma	19.12	16.56	11	17209	1316	29933942
Graft versus host disease in lung	18.72	16.56	8	17212	504	29934754
Haematoma	18.63	16.56	42	17178	23911	29911347
Tuberculosis	18.45	16.56	23	17197	8054	29927204
Red blood cell count increased	18.36	16.56	11	17209	1418	29933840
Microangiopathy	18.23	16.56	9	17211	791	29934467
Blood product transfusion dependent	18.03	16.56	7	17213	344	29934914
Enterocolitis infectious	17.64	16.56	10	17210	1164	29934094
Basophil count increased	17.63	16.56	7	17213	365	29934893
Acute graft versus host disease in intestine	17.52	16.56	13	17207	2392	29932866
Serum ferritin abnormal	17.26	16.56	6	17214	215	29935043
Chronic myelomonocytic leukaemia	16.82	16.56	8	17212	648	29934610
Bone marrow transplant	16.61	16.56	9	17211	959	29934299

Pharmacologic Action:

Source	Code	Description
ATC	L01EJ01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Janus-associated kinase (JAK) inhibitors
FDA MoA	N0000175076	Protein Kinase Inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
CHEBI has role	CHEBI:35610	cytostatic
CHEBI has role	CHEBI:76617	abl inhibitors

Drug Use (View source of the data)

Disease	Relation	SNOMED_ID	DOID
Myelofibrosis	indication	52967002	DOID:4971
Polycythemia vera	indication	109992005
Myeloproliferative disorder	indication	425333006
Coronavirus infection	off-label use	186747009

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	6.44	acidic
pKa2	4.6	Basic
pKa3	2.37	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 10MG BASE	JAKAFI	INCYTE CORP	N202192	Nov. 16, 2011	RX	TABLET	ORAL	Dec. 4, 2021	TREATMENT OF PATIENTS WITH POLYCYTHEMIA VERA WHO HAVE HAD AN INULLDEQUATE RESPONSE TO OR ARE INTOLERANT OF HYDROXYUREA
EQ 15MG BASE	JAKAFI	INCYTE CORP	N202192	Nov. 16, 2011	RX	TABLET	ORAL	Dec. 4, 2021	TREATMENT OF PATIENTS WITH POLYCYTHEMIA VERA WHO HAVE HAD AN INULLDEQUATE RESPONSE TO OR ARE INTOLERANT OF HYDROXYUREA
EQ 20MG BASE	JAKAFI	INCYTE CORP	N202192	Nov. 16, 2011	RX	TABLET	ORAL	Dec. 4, 2021	TREATMENT OF PATIENTS WITH POLYCYTHEMIA VERA WHO HAVE HAD AN INULLDEQUATE RESPONSE TO OR ARE INTOLERANT OF HYDROXYUREA
EQ 25MG BASE	JAKAFI	INCYTE CORP	N202192	Nov. 16, 2011	RX	TABLET	ORAL	Dec. 4, 2021	TREATMENT OF PATIENTS WITH POLYCYTHEMIA VERA WHO HAVE HAD AN INULLDEQUATE RESPONSE TO OR ARE INTOLERANT OF HYDROXYUREA
EQ 5MG BASE	JAKAFI	INCYTE CORP	N202192	Nov. 16, 2011	RX	TABLET	ORAL	Dec. 4, 2021	TREATMENT OF PATIENTS WITH POLYCYTHEMIA VERA WHO HAVE HAD AN INULLDEQUATE RESPONSE TO OR ARE INTOLERANT OF HYDROXYUREA
EQ 10MG BASE	JAKAFI	INCYTE CORP	N202192	Nov. 16, 2011	RX	TABLET	ORAL	May 24, 2022	TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE (GVHD) IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER
EQ 15MG BASE	JAKAFI	INCYTE CORP	N202192	Nov. 16, 2011	RX	TABLET	ORAL	May 24, 2022	TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE (GVHD) IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER
EQ 20MG BASE	JAKAFI	INCYTE CORP	N202192	Nov. 16, 2011	RX	TABLET	ORAL	May 24, 2022	TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE (GVHD) IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER
EQ 25MG BASE	JAKAFI	INCYTE CORP	N202192	Nov. 16, 2011	RX	TABLET	ORAL	May 24, 2022	TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE (GVHD) IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER
EQ 5MG BASE	JAKAFI	INCYTE CORP	N202192	Nov. 16, 2011	RX	TABLET	ORAL	May 24, 2022	TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE (GVHD) IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER
EQ 10MG BASE	JAKAFI	INCYTE CORP	N202192	Nov. 16, 2011	RX	TABLET	ORAL	May 24, 2026	TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE (GVHD) IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER
EQ 15MG BASE	JAKAFI	INCYTE CORP	N202192	Nov. 16, 2011	RX	TABLET	ORAL	May 24, 2026	TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE (GVHD) IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER
EQ 20MG BASE	JAKAFI	INCYTE CORP	N202192	Nov. 16, 2011	RX	TABLET	ORAL	May 24, 2026	TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE (GVHD) IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER
EQ 25MG BASE	JAKAFI	INCYTE CORP	N202192	Nov. 16, 2011	RX	TABLET	ORAL	May 24, 2026	TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE (GVHD) IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER
EQ 5MG BASE	JAKAFI	INCYTE CORP	N202192	Nov. 16, 2011	RX	TABLET	ORAL	May 24, 2026	TREATMENT OF STEROID-REFRACTORY ACUTE GRAFT-VERSUS-HOST DISEASE (GVHD) IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Tyrosine-protein kinase JAK2	Kinase	O60674	JAK2_HUMAN	INHIBITOR	Kd	10.44		CHEMBL	CHEMBL
Tyrosine-protein kinase JAK1	Kinase	P23458	JAK1_HUMAN	INHIBITOR	Ki	10.05		CHEMBL	CHEMBL
Phosphatidylinositol 4-kinase beta	Kinase	Q9UBF8	PI4KB_HUMAN		Kd	5.47		CHEMBL
Serine/threonine-protein kinase DCLK1	Kinase	O15075	DCLK1_HUMAN		Kd	7.17		CHEMBL
Calcium/calmodulin-dependent protein kinase type 1	Kinase	Q14012	KCC1A_HUMAN		Kd	6.33		CHEMBL
SRSF protein kinase 1	Kinase	Q96SB4	SRPK1_HUMAN		Kd	5.68		CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 2	Kinase	Q92630	DYRK2_HUMAN		Kd	5.43		CHEMBL
Serine/threonine-protein kinase RIO3	Kinase	O14730	RIOK3_HUMAN		Kd	5.70		CHEMBL
Serine/threonine-protein kinase Nek3	Kinase	P51956	NEK3_HUMAN		Kd	5.96		CHEMBL
Dual specificity mitogen-activated protein kinase kinase 3	Kinase	P46734	MP2K3_HUMAN		Kd	6.33		CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit beta	Kinase	Q13554	KCC2B_HUMAN		Kd	6.51		CHEMBL
Death-associated protein kinase 2	Kinase	Q9UIK4	DAPK2_HUMAN		Kd	7.01		CHEMBL
Ribosomal protein S6 kinase alpha-6	Kinase	Q9UK32	KS6A6_HUMAN		Kd	6.82		CHEMBL
Ribosomal protein S6 kinase alpha-1	Kinase	Q15418	KS6A1_HUMAN		Kd	6.92		CHEMBL
Cyclin-G-associated kinase	Kinase	O14976	GAK_HUMAN		Kd	7		CHEMBL
Serine/threonine-protein kinase SBK1	Kinase	Q52WX2	SBK1_HUMAN		Kd	5.89		CHEMBL
Mitogen-activated protein kinase kinase kinase 15	Kinase	Q6ZN16	M3K15_HUMAN		Kd	5.96		CHEMBL
Microtubule-associated serine/threonine-protein kinase 1	Kinase	Q9Y2H9	MAST1_HUMAN		Kd	6.28		CHEMBL
JAK2/TYK2	Kinase	O60674 P29597	JAK2_HUMAN TYK2_HUMAN		IC50	6.09		CHEMBL
JAK1/JAK2/TYK2	Kinase	O60674 P23458 P29597	JAK1_HUMAN JAK2_HUMAN TYK2_HUMAN		IC50	6.53		CHEMBL
JAK1/TYK2	Kinase	P23458 P29597	JAK1_HUMAN TYK2_HUMAN		IC50	6.71		CHEMBL
Homeodomain-interacting protein kinase 3	Kinase	Q9H422	HIPK3_HUMAN		Kd	5.92		CHEMBL
Homeodomain-interacting protein kinase 2	Kinase	Q9H2X6	HIPK2_HUMAN		Kd	6		CHEMBL
Maternal embryonic leucine zipper kinase	Kinase	Q14680	MELK_HUMAN		Kd	5.66		CHEMBL
Serine/threonine-protein kinase PLK1	Kinase	P53350	PLK1_HUMAN		Kd	6.89		CHEMBL
Serine/threonine-protein kinase TBK1	Kinase	Q9UHD2	TBK1_HUMAN		Kd	5.77		CHEMBL
Serine/threonine-protein kinase Nek7	Kinase	Q8TDX7	NEK7_HUMAN		Kd	5.31		CHEMBL
Serine/threonine-protein kinase/endoribonuclease IRE1	Kinase	O75460	ERN1_HUMAN		Kd	5.60		CHEMBL
Serine/threonine-protein kinase B-raf	Kinase	P15056	BRAF_HUMAN		Kd	5.66		CHEMBL
Serine/threonine-protein kinase OSR1	Kinase	O95747	OXSR1_HUMAN		Kd	5.57		CHEMBL
STE20/SPS1-related proline-alanine-rich protein kinase	Kinase	Q9UEW8	STK39_HUMAN		Kd	5.72		CHEMBL
Mitogen-activated protein kinase kinase kinase 7	Kinase	O43318	M3K7_HUMAN		Kd	6.14		CHEMBL
Dual specificity protein kinase CLK2	Kinase	P49760	CLK2_HUMAN		Kd	6.34		CHEMBL
G protein-coupled receptor kinase 7	Kinase	Q8WTQ7	GRK7_HUMAN		Kd	6.27		CHEMBL
Homeodomain-interacting protein kinase 1	Kinase	Q86Z02	HIPK1_HUMAN		Kd	5.92		CHEMBL
JAK3/JAK1	Kinase	P23458 P52333	JAK1_HUMAN JAK3_HUMAN		IC50	7.64		CHEMBL
Dual specificity protein kinase TTK	Kinase	P33981	TTK_HUMAN		Kd	6.32		CHEMBL
JAK2/JAK1	Kinase	O60674 P23458	JAK1_HUMAN JAK2_HUMAN		IC50	7.51		CHEMBL
Ephrin type-A receptor 3	Kinase	P29320	EPHA3_HUMAN		Kd	5.21		CHEMBL
Serine/threonine-protein kinase 16	Kinase	O75716	STK16_HUMAN		Kd	6.31		CHEMBL
Serine/threonine-protein kinase 17B	Kinase	O94768	ST17B_HUMAN		Kd	5.46		CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit gamma	Kinase	Q13555	KCC2G_HUMAN		Kd	7		CHEMBL
Serine/threonine-protein kinase PLK4	Kinase	O00444	PLK4_HUMAN		Kd	6.70		CHEMBL
AP2-associated protein kinase 1	Kinase	Q2M2I8	AAK1_HUMAN		Kd	6.92		CHEMBL
Serine/threonine-protein kinase MARK2	Kinase	Q7KZI7	MARK2_HUMAN		Kd	6.18		CHEMBL
Protein kinase C epsilon type	Kinase	Q02156	KPCE_HUMAN		Kd	6.28		CHEMBL
Tyrosine-protein kinase JAK3	Kinase	P52333	JAK3_HUMAN		Kd	8.70		CHEMBL
Ribosomal protein S6 kinase alpha-5	Kinase	O75582	KS6A5_HUMAN		Kd	6.85		CHEMBL
Casein kinase II subunit alpha'	Kinase	P19784	CSK22_HUMAN		Kd	5.48		CHEMBL
Serine/threonine-protein kinase TAO1	Kinase	Q7L7X3	TAOK1_HUMAN		Kd	5.89		CHEMBL
Aurora kinase C	Kinase	Q9UQB9	AURKC_HUMAN		Kd	5.06		CHEMBL
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform	Kinase	P15735	PHKG2_HUMAN		Kd	6		CHEMBL
High affinity nerve growth factor receptor	Kinase	P04629	NTRK1_HUMAN		Kd	5.82		CHEMBL
Rho-associated protein kinase 1	Kinase	Q13464	ROCK1_HUMAN		Kd	7.22		CHEMBL
Ankyrin repeat and protein kinase domain-containing protein 1	Kinase	Q8NFD2	ANKK1_HUMAN		Kd	6.41		CHEMBL
Serine/threonine-protein kinase 25	Kinase	O00506	STK25_HUMAN		Kd	5.20		CHEMBL
Myosin light chain kinase, smooth muscle	Kinase	Q15746	MYLK_HUMAN		Kd	6.44		CHEMBL
Serine/threonine-protein kinase DCLK2	Kinase	Q8N568	DCLK2_HUMAN		Kd	6.12		CHEMBL
Leucine-rich repeat serine/threonine-protein kinase 2	Kinase	Q5S007	LRRK2_HUMAN		Kd	7.05		CHEMBL
Serine/threonine-protein kinase PAK 6	Kinase	Q9NQU5	PAK6_HUMAN		Kd	5.54		CHEMBL
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN		Kd	5.20		CHEMBL
BMP-2-inducible protein kinase	Kinase	Q9NSY1	BMP2K_HUMAN		Kd	6.68		CHEMBL
Serine/threonine-protein kinase PAK 7	Kinase	Q9P286	PAK5_HUMAN		Kd	5.89		CHEMBL
Serine/threonine-protein kinase 17A	Kinase	Q9UEE5	ST17A_HUMAN		Kd	5.21		CHEMBL
Ribosomal protein S6 kinase alpha-4	Kinase	O75676	KS6A4_HUMAN		Kd	6.47		CHEMBL
Dual specificity protein kinase CLK4	Kinase	Q9HAZ1	CLK4_HUMAN		Kd	5.77		CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 2	Kinase	Q9HBH9	MKNK2_HUMAN		Kd	6.70		CHEMBL
Bone morphogenetic protein receptor type-1B	Kinase	O00238	BMR1B_HUMAN		Kd	5.74		CHEMBL
Non-receptor tyrosine-protein kinase TYK2	Kinase	P29597	TYK2_HUMAN		Ki	9.30		CHEMBL
Interleukin-1 receptor-associated kinase 1	Kinase	P51617	IRAK1_HUMAN		Kd	6.54		CHEMBL
Calcium/calmodulin-dependent protein kinase type 1D	Kinase	Q8IU85	KCC1D_HUMAN		Kd	6.92		CHEMBL
Calcium/calmodulin-dependent protein kinase type 1G	Kinase	Q96NX5	KCC1G_HUMAN		Kd	5.66		CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit beta	Kinase	O14920	IKKB_HUMAN		Kd	5.64		CHEMBL
Serine/threonine-protein kinase TAO2	Kinase	Q9UL54	TAOK2_HUMAN		Kd	6.51		CHEMBL
Ribosomal protein S6 kinase alpha-2	Kinase	Q15349	KS6A2_HUMAN		Kd	6.82		CHEMBL
Serine/threonine-protein kinase ULK2	Kinase	Q8IYT8	ULK2_HUMAN		Kd	6.72		CHEMBL
Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform	Kinase	Q16816	PHKG1_HUMAN		Kd	5.24		CHEMBL
Activated CDC42 kinase 1	Kinase	Q07912	ACK1_HUMAN		Kd	5.59		CHEMBL
Casein kinase II subunit alpha	Kinase	P68400	CSK21_HUMAN		Kd	5.38		CHEMBL
NT-3 growth factor receptor	Kinase	Q16288	NTRK3_HUMAN		Kd	6.48		CHEMBL
Rhodopsin kinase	Kinase	Q15835	RK_HUMAN		Kd	6.14		CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit alpha	Kinase	Q9UQM7	KCC2A_HUMAN		Kd	7.34		CHEMBL
G protein-coupled receptor kinase 4	Kinase	P32298	GRK4_HUMAN		Kd	5.21		CHEMBL
Mitogen-activated protein kinase kinase kinase 2	Kinase	Q9Y2U5	M3K2_HUMAN		Kd	7.39		CHEMBL
Serine/threonine-protein kinase ULK3	Kinase	Q6PHR2	ULK3_HUMAN		Kd	5.62		CHEMBL
Serine/threonine-protein kinase 26	Kinase	Q9P289	STK26_HUMAN		Kd	5.51		CHEMBL
Serine/threonine-protein kinase PLK2	Kinase	Q9NYY3	PLK2_HUMAN		Kd	5.82		CHEMBL
Bone morphogenetic protein receptor type-2	Kinase	Q13873	BMPR2_HUMAN		Kd	6.03		CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit epsilon	Kinase	Q14164	IKKE_HUMAN		Kd	5.92		CHEMBL
Peripheral plasma membrane protein CASK	Kinase	O14936	CSKP_HUMAN		Kd	5.82		CHEMBL
Ephrin type-B receptor 6	Kinase	O15197	EPHB6_HUMAN		Kd	5.51		CHEMBL
Mitogen-activated protein kinase 8	Kinase	P45983	MK08_HUMAN		Kd	5.32		CHEMBL
Serine/threonine-protein kinase TAO3	Kinase	Q9H2K8	TAOK3_HUMAN		Kd	6.23		CHEMBL
Casein kinase I isoform alpha	Kinase	P48729	KC1A_HUMAN		Kd	5.74		CHEMBL
Mitogen-activated protein kinase kinase kinase 1	Kinase	Q13233	M3K1_HUMAN		Kd	5.38		CHEMBL
Cyclin-dependent kinase 7	Kinase	P50613	CDK7_HUMAN		Kd	5.48		CHEMBL
Serine/threonine-protein kinase SIK3	Kinase	Q9Y2K2	SIK3_HUMAN		Kd	5.89		CHEMBL
Rho-associated protein kinase 2	Kinase	O75116	ROCK2_HUMAN		Kd	7.28		CHEMBL
Death-associated protein kinase 1	Kinase	P53355	DAPK1_HUMAN		Kd	7.14		CHEMBL
Uncharacterized serine/threonine-protein kinase SBK3	Kinase	P0C264	SBK3_HUMAN		Kd	5.24		CHEMBL
Death-associated protein kinase 3	Kinase	O43293	DAPK3_HUMAN		Kd	7.05		CHEMBL
Serine/threonine-protein kinase PAK 4	Kinase	O96013	PAK4_HUMAN		Kd	5.80		CHEMBL
Serine/threonine-protein kinase DCLK3	Kinase	Q9C098	DCLK3_HUMAN		Kd	6.59		CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 1A	Kinase	Q13627	DYR1A_HUMAN		Kd	6.04		CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN		Kd	6.72		CHEMBL
Myotonin-protein kinase	Kinase	Q09013	DMPK_HUMAN		Kd	5.46		CHEMBL
Leukocyte tyrosine kinase receptor	Kinase	P29376	LTK_HUMAN		Kd	6.36		CHEMBL
Mitogen-activated protein kinase kinase kinase 19	Kinase	Q56UN5	M3K19_HUMAN		Kd	6.57		CHEMBL
Serine/threonine-protein kinase PLK3	Kinase	Q9H4B4	PLK3_HUMAN		Kd	6.15		CHEMBL
BDNF/NT-3 growth factors receptor	Kinase	Q16620	NTRK2_HUMAN		Kd	6.44		CHEMBL
NUAK family SNF1-like kinase 2	Kinase	Q9H093	NUAK2_HUMAN		Kd	6.49		CHEMBL
Dual specificity mitogen-activated protein kinase kinase 2	Kinase	P36507	MP2K2_HUMAN		Kd	5.40		CHEMBL
Dual specificity mitogen-activated protein kinase kinase 4	Kinase	P45985	MP2K4_HUMAN		Kd	5.74		CHEMBL
SRSF protein kinase 3	Kinase	Q9UPE1	SRPK3_HUMAN		Kd	5.48		CHEMBL
Serine/threonine-protein kinase VRK2	Kinase	Q86Y07	VRK2_HUMAN		Kd	5.40		CHEMBL
ALK tyrosine kinase receptor	Kinase	Q9UM73	ALK_HUMAN		Kd	5.82		CHEMBL
Mitogen-activated protein kinase kinase kinase 3	Kinase	Q99759	M3K3_HUMAN		Kd	6.82		CHEMBL
Serine/threonine-protein kinase RIO1	Kinase	Q9BRS2	RIOK1_HUMAN		Kd	5.60		CHEMBL
Serine/threonine-protein kinase RIO2	Kinase	Q9BVS4	RIOK2_HUMAN		Kd	5.92		CHEMBL
Serine/threonine-protein kinase ULK1	Kinase	O75385	ULK1_HUMAN		Kd	6.52		CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit delta	Kinase	Q13557	KCC2D_HUMAN		Kd	7.05		CHEMBL
cGMP-dependent protein kinase 2	Kinase	Q13237	KGP2_HUMAN		Kd	6.16		CHEMBL
Receptor-interacting serine/threonine-protein kinase 4	Kinase	P57078	RIPK4_HUMAN		Kd	5.68		CHEMBL
Dual specificity mitogen-activated protein kinase kinase 1	Kinase	Q02750	MP2K1_HUMAN		Kd	5.72		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2	Kinase	Q12851	M4K2_HUMAN		Kd	5.70		CHEMBL
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN		Kd	5.96		CHEMBL
Serine/threonine-protein kinase PknB	Kinase		PKNB_MYCTU		Kd	5.38		CHEMBL

External reference:

ID	Source
4031235	VUID
N0000184017	NUI
D09959	KEGG_DRUG
1092939-17-7	SECONDARY_CAS_RN
4031235	VANDF
C3247913	UMLSCUI
CHEBI:66917	CHEBI
RXT	PDB_CHEM_ID
CHEMBL1795071	ChEMBL_ID
CHEMBL1789941	ChEMBL_ID
5688	IUPHAR_LIGAND_ID
C540383	MESH_SUPPLEMENTAL_RECORD_UI
9287	INN_ID
DB08877	DRUGBANK_ID
82S8X8XX8H	UNII
25126798	PUBCHEM_CID
1193325	RXNORM
186162	MMSL
28206	MMSL
d07812	MMSL
014040	NDDF
014041	NDDF
702806008	SNOMEDCT_US
703779004	SNOMEDCT_US
734494005	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
JAKAFI	HUMAN PRESCRIPTION DRUG LABEL	1	50881-005	TABLET	5 mg	ORAL	NDA	28 sections
JAKAFI	HUMAN PRESCRIPTION DRUG LABEL	1	50881-010	TABLET	10 mg	ORAL	NDA	28 sections
JAKAFI	HUMAN PRESCRIPTION DRUG LABEL	1	50881-015	TABLET	15 mg	ORAL	NDA	28 sections
JAKAFI	HUMAN PRESCRIPTION DRUG LABEL	1	50881-020	TABLET	20 mg	ORAL	NDA	28 sections
JAKAFI	HUMAN PRESCRIPTION DRUG LABEL	1	50881-025	TABLET	25 mg	ORAL	NDA	28 sections