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

Stem definition	Drug id	CAS RN
angiogenesis inhibitors	4903	656247-17-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: BIBF1120 nibtedanib nintedanib nintedanib esylate intedanib BIBF 1120 ofev nintedanib ethanesulfonate vargatef	Molecular weight: 539.64 Formula: C31H33N5O4 CLOGP: 3.08 LIPINSKI: 1 HAC: 9 HDO: 2 TPSA: 94.22 ALOGS: -4.24 ROTB: 8 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

None

ADMET properties:

Property	Value	Reference
Vd (Volume of distribution)	15 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	19.90 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.02 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	9.50 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
July 3, 2015	PMDA	Boehringer Ingelheim
Oct. 15, 2014	FDA	BOEHRINGER INGELHEIM
Nov. 20, 2014	EMA	Boehringer Ingelheim International GmbH

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
Diarrhoea	640.38	26.41	620	7535	558982	46118925
Idiopathic pulmonary fibrosis	586.69	26.41	115	8040	1373	46676534
Malignant neoplasm progression	211.66	26.41	135	8020	64791	46613116
Nausea	191.66	26.41	388	7767	687066	45990841
Decreased appetite	149.21	26.41	176	7979	193660	46484247
Vomiting	147.91	26.41	274	7881	452520	46225387
Drug ineffective	73.08	26.41	15	8140	677823	46000084
Death	68.26	26.41	168	7987	335380	46342527
Weight decreased	65.06	26.41	125	8030	210724	46467183
Dyspnoea	57.04	26.41	208	7947	515340	46162567
Liver disorder	46.70	26.41	44	8111	37202	46640705
Stomatitis	41.10	26.41	55	8100	68242	46609665
Non-small cell lung cancer	38.51	26.41	16	8139	3128	46674779
Interstitial lung disease	38.04	26.41	47	8108	53902	46624005
Flatulence	37.90	26.41	35	8120	28843	46649064
Constipation	36.12	26.41	88	8067	174009	46503898
Gamma-glutamyltransferase increased	33.26	26.41	34	8121	31706	46646201
Intestinal haemorrhage	32.05	26.41	14	8141	3094	46674813
Pulmonary embolism	30.52	26.41	62	8093	108523	46569384
Large intestine perforation	30.32	26.41	18	8137	7562	46670345
White blood cell count decreased	30.27	26.41	63	8092	112168	46565739
Neutrophil count decreased	29.27	26.41	37	8118	43389	46634518
Skin reaction	28.88	26.41	20	8135	10926	46666981
Mucosal infection	28.43	26.41	6	8149	105	46677802
Aspartate aminotransferase increased	28.39	26.41	50	8105	78650	46599257
Oxygen saturation decreased	27.65	26.41	46	8109	69118	46608789
Liver function test increased	26.77	26.41	26	8129	22800	46655107
Alanine aminotransferase increased	26.64	26.41	52	8103	88399	46589508
Febrile neutropenia	26.54	26.41	54	8101	94573	46583334

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
Idiopathic pulmonary fibrosis	2259.91	22.31	484	12094	3585	29936315
Diarrhoea	1038.25	22.31	952	11626	333151	29606749
Malignant neoplasm progression	436.79	22.31	307	12271	71980	29867920
Decreased appetite	232.06	22.31	299	12279	149611	29790289
Death	172.75	22.31	427	12151	356856	29583044
Weight decreased	142.86	22.31	239	12339	150682	29789218
Pneumothorax	134.21	22.31	84	12494	16109	29923791
Lung transplant	124.99	22.31	42	12536	1874	29938026
Dyspnoea	106.08	22.31	343	12235	332952	29606948
Nausea	102.12	22.31	314	12264	296643	29643257
Abnormal loss of weight	74.70	22.31	35	12543	3767	29936133
Cough	70.73	22.31	160	12418	125482	29814418
Liver disorder	65.05	22.31	71	12507	29651	29910249
Respiratory failure	57.52	22.31	129	12449	100513	29839387
Productive cough	54.45	22.31	65	12513	29888	29910012
Pulmonary embolism	47.84	22.31	103	12475	78032	29861868
Hepatic enzyme increased	45.63	22.31	63	12515	33431	29906469
Drug ineffective	40.77	22.31	50	12528	340337	29599563
Pulmonary fibrosis	38.35	22.31	40	12538	15850	29924050
Pneumonia	36.32	22.31	252	12326	334054	29605846
Abdominal pain upper	35.48	22.31	80	12498	62471	29877429
Pneumonia bacterial	34.81	22.31	30	12548	9373	29930527
Chronic respiratory failure	32.85	22.31	14	12564	1204	29938696
Drug interaction	32.53	22.31	22	12556	199546	29740354
Dysgeusia	31.32	22.31	45	12533	24756	29915144
Lung neoplasm malignant	31.10	22.31	35	12543	15097	29924803
Completed suicide	30.94	22.31	3	12575	99489	29840411
Polyneuropathy	30.77	22.31	31	12547	11792	29928108
Faeces soft	30.57	22.31	16	12562	2183	29937717
Abdominal discomfort	29.46	22.31	64	12514	48727	29891173
Hepatic function abnormal	28.80	22.31	58	12520	41887	29898013
Mesenteric vein thrombosis	28.35	22.31	10	12568	516	29939384
Toxicity to various agents	28.25	22.31	20	12558	177163	29762737
Pulmonary hypertension	27.72	22.31	37	12541	18999	29920901
Pulmonary function test decreased	27.55	22.31	19	12559	4276	29935624
Acute kidney injury	27.04	22.31	46	12532	273796	29666104
Vomiting	25.75	22.31	169	12409	219649	29720251
Gastrointestinal disorder	25.71	22.31	44	12534	28093	29911807
Fatigue	25.49	22.31	225	12353	320448	29619452
Pneumomediastinum	24.81	22.31	13	12565	1778	29938122
Splenic vein thrombosis	24.54	22.31	8	12570	324	29939576
Hypotension	24.43	22.31	29	12549	200536	29739364
General physical health deterioration	23.87	22.31	94	12484	99850	29840050
Epistaxis	23.85	22.31	62	12516	52919	29886981
Constipation	22.91	22.31	101	12477	112805	29827095
Non-small cell lung cancer	22.76	22.31	16	12562	3714	29936186
Overdose	22.73	22.31	4	12574	84333	29855567

Pharmacologic Action:

Source	Code	Description
ATC	L01EX09	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Other protein kinase inhibitors
FDA MoA	N0000175076	Protein Kinase Inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors
CHEBI has role	CHEBI:35610	cytostatic
CHEBI has role	CHEBI:38637	tyrosine kinase inhibitors
CHEBI has role	CHEBI:48422	angiostatic agents
CHEBI has role	CHEBI:63457	fibroblast growth factor receptor antagonists
CHEBI has role	CHEBI:65207	vegfr inhibitors

Drug Use (View source of the data)

Disease	Relation	SNOMED_ID	DOID
Interstitial fibrosis	indication	125565008
Non-small cell lung cancer	indication	254637007	DOID:3908
Idiopathic pulmonary fibrosis	indication	700250006	DOID:0050156

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.97	acidic
pKa2	7.77	Basic
pKa3	3.25	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 100MG BASE	OFEV	BOEHRINGER INGELHEIM	N205832	Oct. 15, 2014	RX	CAPSULE	ORAL	Oct. 15, 2021	TREATMENT OF IDIOPATHIC PULMONULLRY FIBROSIS
EQ 150MG BASE	OFEV	BOEHRINGER INGELHEIM	N205832	Oct. 15, 2014	RX	CAPSULE	ORAL	Oct. 15, 2021	TREATMENT OF IDIOPATHIC PULMONULLRY FIBROSIS
EQ 100MG BASE	OFEV	BOEHRINGER INGELHEIM	N205832	Oct. 15, 2014	RX	CAPSULE	ORAL	Sept. 6, 2022	SLOW THE RATE OF DECLINE IN PULMONULLRY FUNCTION IN PATIENTS WITH SYSTEMIC SCLEROSIS-ASSOCIATED INTERSTITIAL LUNG DISEASE
EQ 150MG BASE	OFEV	BOEHRINGER INGELHEIM	N205832	Oct. 15, 2014	RX	CAPSULE	ORAL	Sept. 6, 2022	SLOW THE RATE OF DECLINE IN PULMONULLRY FUNCTION IN PATIENTS WITH SYSTEMIC SCLEROSIS-ASSOCIATED INTERSTITIAL LUNG DISEASE
EQ 100MG BASE	OFEV	BOEHRINGER INGELHEIM	N205832	Oct. 15, 2014	RX	CAPSULE	ORAL	March 9, 2023	TREATMENT FOR CHRONIC FIBROSING INTERSTITIAL LUNG DISEASES WITH A PROGRESSIVE PHENOTYPE
EQ 150MG BASE	OFEV	BOEHRINGER INGELHEIM	N205832	Oct. 15, 2014	RX	CAPSULE	ORAL	March 9, 2023	TREATMENT FOR CHRONIC FIBROSING INTERSTITIAL LUNG DISEASES WITH A PROGRESSIVE PHENOTYPE
EQ 100MG BASE	OFEV	BOEHRINGER INGELHEIM	N205832	Oct. 15, 2014	RX	CAPSULE	ORAL	Sept. 6, 2026	INDICATED TO SLOW THE RATE OF DECLINE IN PULMONULLRY FUNCTION IN PATIENTS WITH SYSTEMIC SCLEROSIS-ASSOCIATED INTERSTITIAL LUNG DISEASE (SSC-ILD)
EQ 150MG BASE	OFEV	BOEHRINGER INGELHEIM	N205832	Oct. 15, 2014	RX	CAPSULE	ORAL	Sept. 6, 2026	INDICATED TO SLOW THE RATE OF DECLINE IN PULMONULLRY FUNCTION IN PATIENTS WITH SYSTEMIC SCLEROSIS-ASSOCIATED INTERSTITIAL LUNG DISEASE (SSC-ILD)

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Platelet-derived growth factor receptor beta	Kinase	P09619	PGFRB_HUMAN	INHIBITOR	Kd	7.82		CHEMBL	CHEMBL
Fibroblast growth factor receptor 2	Kinase	P21802	FGFR2_HUMAN	INHIBITOR	Kd	6.46		CHEMBL	CHEMBL
Fibroblast growth factor receptor 1	Kinase	P11362	FGFR1_HUMAN	INHIBITOR	IC50	7.42		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Fibroblast growth factor receptor 4	Kinase	P22455	FGFR4_HUMAN	INHIBITOR	Kd	5.74		CHEMBL	CHEMBL
Platelet-derived growth factor receptor alpha	Kinase	P16234	PGFRA_HUMAN	INHIBITOR	IC50	7.74		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Fibroblast growth factor receptor 3	Kinase	P22607	FGFR3_HUMAN	INHIBITOR	Kd	7.03		CHEMBL	CHEMBL
Vascular endothelial growth factor receptor 1	Kinase	P17948	VGFR1_HUMAN	INHIBITOR	IC50	6.98		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Vascular endothelial growth factor receptor 3	Kinase	P35916	VGFR3_HUMAN	INHIBITOR	IC50	8.30		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN	INHIBITOR	IC50	8.30		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Proto-oncogene tyrosine-protein kinase Src	Kinase	P12931	SRC_HUMAN		Kd	6.24		CHEMBL
Calcium/calmodulin-dependent protein kinase type 1	Kinase	Q14012	KCC1A_HUMAN		Kd	5.23		CHEMBL
Serine/threonine-protein kinase 35	Kinase	Q8TDR2	STK35_HUMAN		Kd	6.09		CHEMBL
Calcium/calmodulin-dependent protein kinase type IV	Kinase	Q16566	KCC4_HUMAN		Kd	5.43		CHEMBL
Insulin receptor	Kinase	P06213	INSR_HUMAN	AGONIST	Kd	7.62		CHEMBL
SRSF protein kinase 1	Kinase	Q96SB4	SRPK1_HUMAN		Kd	7.43		CHEMBL
Serine/threonine-protein kinase RIO3	Kinase	O14730	RIOK3_HUMAN		Kd	7.44		CHEMBL
Hepatocyte growth factor receptor	Kinase	P08581	MET_HUMAN		Kd	6.70		CHEMBL
Casein kinase I isoform epsilon	Kinase	P49674	KC1E_HUMAN		Kd	6.64		CHEMBL
Myosin-IIIb	Kinase	Q8WXR4	MYO3B_HUMAN		Kd	5.57		CHEMBL
Dual specificity mitogen-activated protein kinase kinase 3	Kinase	P46734	MP2K3_HUMAN		Kd	5.68		CHEMBL
Serine/threonine-protein kinase PAK 3	Kinase	O75914	PAK3_HUMAN		Kd	6.68		CHEMBL
Ephrin type-B receptor 4	Kinase	P54760	EPHB4_HUMAN		Kd	5.96		CHEMBL
Tyrosine-protein kinase JAK2	Kinase	O60674	JAK2_HUMAN		Kd	7.85		CHEMBL
Ribosomal protein S6 kinase alpha-6	Kinase	Q9UK32	KS6A6_HUMAN		Kd	6.64		CHEMBL
MAP/microtubule affinity-regulating kinase 3	Kinase	P27448	MARK3_HUMAN		Kd	6.11		CHEMBL
Ribosomal protein S6 kinase alpha-1	Kinase	Q15418	KS6A1_HUMAN		Kd	6.74		CHEMBL
Serine/threonine-protein kinase SBK1	Kinase	Q52WX2	SBK1_HUMAN		Kd	6.96		CHEMBL
Mitogen-activated protein kinase kinase kinase 15	Kinase	Q6ZN16	M3K15_HUMAN		Kd	5.85		CHEMBL
Microtubule-associated serine/threonine-protein kinase 1	Kinase	Q9Y2H9	MAST1_HUMAN		Kd	5.34		CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5	Kinase	Q13163	MP2K5_HUMAN		Kd	8.74		CHEMBL
Tyrosine-protein kinase JAK1	Kinase	P23458	JAK1_HUMAN		Kd	8.32		CHEMBL
Casein kinase I isoform delta	Kinase	P48730	KC1D_HUMAN		Kd	5.89		CHEMBL
Tyrosine-protein kinase ITK/TSK	Kinase	Q08881	ITK_HUMAN		Kd	6.68		CHEMBL
Homeodomain-interacting protein kinase 3	Kinase	Q9H422	HIPK3_HUMAN		Kd	6.07		CHEMBL
Homeodomain-interacting protein kinase 2	Kinase	Q9H2X6	HIPK2_HUMAN		Kd	6.10		CHEMBL
Maternal embryonic leucine zipper kinase	Kinase	Q14680	MELK_HUMAN		Kd	8.31		CHEMBL
Wee1-like protein kinase	Kinase	P30291	WEE1_HUMAN		Kd	5.54		CHEMBL
Tyrosine-protein kinase BTK	Kinase	Q06187	BTK_HUMAN		Kd	6.51		CHEMBL
NUAK family SNF1-like kinase 1	Kinase	O60285	NUAK1_HUMAN		Kd	6.80		CHEMBL
Serine/threonine-protein kinase D1	Kinase	Q15139	KPCD1_HUMAN		Kd	6		CHEMBL
Mitogen-activated protein kinase kinase kinase 13	Kinase	O43283	M3K13_HUMAN		Kd	6.85		CHEMBL
Serine/threonine-protein kinase TBK1	Kinase	Q9UHD2	TBK1_HUMAN		Kd	6.82		CHEMBL
Serine/threonine-protein kinase ICK	Kinase	Q9UPZ9	ICK_HUMAN		Kd	5.77		CHEMBL
Ephrin type-A receptor 1	Kinase	P21709	EPHA1_HUMAN		Kd	5.92		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1	Kinase	Q92918	M4K1_HUMAN		Kd	7.46		CHEMBL
Serine/threonine-protein kinase/endoribonuclease IRE1	Kinase	O75460	ERN1_HUMAN		Kd	5.70		CHEMBL
MAP/microtubule affinity-regulating kinase 4	Kinase	Q96L34	MARK4_HUMAN		Kd	5.70		CHEMBL
Tyrosine-protein kinase Fgr	Kinase	P09769	FGR_HUMAN		Kd	6.52		CHEMBL
Serine/threonine-protein kinase OSR1	Kinase	O95747	OXSR1_HUMAN		Kd	5.89		CHEMBL
Serine/threonine-protein kinase D3	Kinase	O94806	KPCD3_HUMAN		Kd	6.19		CHEMBL
Serine/threonine-protein kinase Sgk3	Kinase	Q96BR1	SGK3_HUMAN		Kd	6		CHEMBL
STE20/SPS1-related proline-alanine-rich protein kinase	Kinase	Q9UEW8	STK39_HUMAN		Kd	6.28		CHEMBL
Mitogen-activated protein kinase kinase kinase 7	Kinase	O43318	M3K7_HUMAN		Kd	8.39		CHEMBL
Dual specificity protein kinase CLK2	Kinase	P49760	CLK2_HUMAN		Kd	6.12		CHEMBL
G protein-coupled receptor kinase 7	Kinase	Q8WTQ7	GRK7_HUMAN		Kd	5.92		CHEMBL
Tyrosine-protein kinase FRK	Kinase	P42685	FRK_HUMAN		Kd	5.57		CHEMBL
Myosin light chain kinase family member 4	Kinase	Q86YV6	MYLK4_HUMAN		Kd	6.36		CHEMBL
Homeodomain-interacting protein kinase 1	Kinase	Q86Z02	HIPK1_HUMAN		Kd	5.89		CHEMBL
Dual specificity protein kinase CLK1	Kinase	P49759	CLK1_HUMAN		Kd	8.06		CHEMBL
Dual specificity protein kinase TTK	Kinase	P33981	TTK_HUMAN		Kd	7.66		CHEMBL
Ephrin type-A receptor 2	Kinase	P29317	EPHA2_HUMAN		Kd	5.54		CHEMBL
Ephrin type-A receptor 3	Kinase	P29320	EPHA3_HUMAN		Kd	5.07		CHEMBL
Serine/threonine-protein kinase 10	Kinase	O94804	STK10_HUMAN		Kd	7.06		CHEMBL
Tyrosine-protein kinase Fer	Kinase	P16591	FER_HUMAN		Kd	7.14		CHEMBL
Serine/threonine-protein kinase 16	Kinase	O75716	STK16_HUMAN		Kd	7.74		CHEMBL
Serine/threonine-protein kinase 17B	Kinase	O94768	ST17B_HUMAN		Kd	6.17		CHEMBL
Serine/threonine-protein kinase PLK4	Kinase	O00444	PLK4_HUMAN		Kd	7.28		CHEMBL
AP2-associated protein kinase 1	Kinase	Q2M2I8	AAK1_HUMAN		Kd	7.20		CHEMBL
Serine/threonine-protein kinase MARK2	Kinase	Q7KZI7	MARK2_HUMAN		Kd	5.85		CHEMBL
Tyrosine-protein kinase JAK3	Kinase	P52333	JAK3_HUMAN		Kd	8.09		CHEMBL
Ribosomal protein S6 kinase alpha-5	Kinase	O75582	KS6A5_HUMAN		Kd	6.70		CHEMBL
Casein kinase II subunit alpha'	Kinase	P19784	CSK22_HUMAN		Kd	6.05		CHEMBL
Tyrosine-protein kinase Yes	Kinase	P07947	YES_HUMAN		Kd	7.10		CHEMBL
Serine/threonine-protein kinase N2	Kinase	Q16513	PKN2_HUMAN		Kd	5.85		CHEMBL
Tyrosine-protein kinase HCK	Kinase	P08631	HCK_HUMAN		Kd	5.28		CHEMBL
Aurora kinase C	Kinase	Q9UQB9	AURKC_HUMAN		Kd	6.72		CHEMBL
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform	Kinase	P15735	PHKG2_HUMAN		Kd	6.59		CHEMBL
High affinity nerve growth factor receptor	Kinase	P04629	NTRK1_HUMAN		Kd	8.35		CHEMBL
Ribosomal protein S6 kinase alpha-3	Kinase	P51812	KS6A3_HUMAN		Kd	7.19		CHEMBL
Homeodomain-interacting protein kinase 4	Kinase	Q8NE63	HIPK4_HUMAN		Kd	5.92		CHEMBL
Myosin light chain kinase, smooth muscle	Kinase	Q15746	MYLK_HUMAN		Kd	6.54		CHEMBL
Mitogen-activated protein kinase kinase kinase 10	Kinase	Q02779	M3K10_HUMAN		Kd	5.64		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 5	Kinase	Q9Y4K4	M4K5_HUMAN		Kd	6.41		CHEMBL
Misshapen-like kinase 1	Kinase	Q8N4C8	MINK1_HUMAN		Kd	7.09		CHEMBL
Leucine-rich repeat serine/threonine-protein kinase 2	Kinase	Q5S007	LRRK2_HUMAN		Kd	7.43		CHEMBL
Interleukin-1 receptor-associated kinase 4	Kinase	Q9NWZ3	IRAK4_HUMAN		Kd	6.09		CHEMBL
Insulin receptor-related protein	Kinase	P14616	INSRR_HUMAN		Kd	7.68		CHEMBL
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN		Kd	8.57		CHEMBL
BMP-2-inducible protein kinase	Kinase	Q9NSY1	BMP2K_HUMAN		Kd	8.66		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	6.96		CHEMBL
Mitogen-activated protein kinase kinase kinase 11	Kinase	Q16584	M3K11_HUMAN		Kd	6.15		CHEMBL
Insulin-like growth factor 1 receptor	Kinase	P08069	IGF1R_HUMAN		Kd	7.21		CHEMBL
Ephrin type-A receptor 6	Kinase	Q9UF33	EPHA6_HUMAN		Kd	6.03		CHEMBL
TRAF2 and NCK-interacting protein kinase	Kinase	Q9UKE5	TNIK_HUMAN		Kd	7.28		CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 2	Kinase	Q96RR4	KKCC2_HUMAN		Kd	6.04		CHEMBL
Ribosomal protein S6 kinase alpha-4	Kinase	O75676	KS6A4_HUMAN		Kd	6.21		CHEMBL
Aurora kinase B	Kinase	Q96GD4	AURKB_HUMAN		Kd	6.38		CHEMBL
STE20-like serine/threonine-protein kinase	Kinase	Q9H2G2	SLK_HUMAN		Kd	7.29		CHEMBL
Dual specificity protein kinase CLK4	Kinase	Q9HAZ1	CLK4_HUMAN		Kd	7.74		CHEMBL
Death-associated protein kinase 2	Kinase	Q9UIK4	DAPK2_HUMAN		Kd	5.49		CHEMBL
Non-receptor tyrosine-protein kinase TYK2	Kinase	P29597	TYK2_HUMAN		Kd	7.43		CHEMBL
Interleukin-1 receptor-associated kinase 1	Kinase	P51617	IRAK1_HUMAN		Kd	6.92		CHEMBL
Serine/threonine-protein kinase 4	Kinase	Q13043	STK4_HUMAN		Kd	8.05		CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 1	Kinase	Q8N5S9	KKCC1_HUMAN		Kd	6.20		CHEMBL
Calcium/calmodulin-dependent protein kinase type 1D	Kinase	Q8IU85	KCC1D_HUMAN		Kd	5.66		CHEMBL
Serine/threonine-protein kinase 3	Kinase	Q13188	STK3_HUMAN		Kd	7.42		CHEMBL
Calcium/calmodulin-dependent protein kinase type 1G	Kinase	Q96NX5	KCC1G_HUMAN		Kd	6.59		CHEMBL
5'-AMP-activated protein kinase catalytic subunit alpha-1	Kinase	Q13131	AAPK1_HUMAN		Kd	7.06		CHEMBL
Tyrosine-protein kinase Lyn	Kinase	P07948	LYN_HUMAN		Kd	6.03		CHEMBL
Ribosomal protein S6 kinase alpha-2	Kinase	Q15349	KS6A2_HUMAN		Kd	7.24		CHEMBL
Serine/threonine-protein kinase ULK2	Kinase	Q8IYT8	ULK2_HUMAN		Kd	6.42		CHEMBL
Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform	Kinase	Q16816	PHKG1_HUMAN		Kd	6.85		CHEMBL
Ephrin type-B receptor 1	Kinase	P54762	EPHB1_HUMAN		Kd	6.26		CHEMBL
Activated CDC42 kinase 1	Kinase	Q07912	ACK1_HUMAN		Kd	5.80		CHEMBL
Cyclin-dependent kinase 16	Kinase	Q00536	CDK16_HUMAN		Kd	7.68		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 3	Kinase	Q8IVH8	M4K3_HUMAN		Kd	6.54		CHEMBL
Focal adhesion kinase 1	Kinase	Q05397	FAK1_HUMAN		Kd	6.68		CHEMBL
Casein kinase II subunit alpha	Kinase	P68400	CSK21_HUMAN		Kd	5.12		CHEMBL
NT-3 growth factor receptor	Kinase	Q16288	NTRK3_HUMAN		Kd	7.49		CHEMBL
Serine/threonine-protein kinase STK11	Kinase	Q15831	STK11_HUMAN		Kd	7.74		CHEMBL
Rhodopsin kinase	Kinase	Q15835	RK_HUMAN		Kd	6		CHEMBL
Tyrosine-protein kinase ZAP-70	Kinase	P43403	ZAP70_HUMAN		Kd	5.46		CHEMBL
Activin receptor type-1	Kinase	Q04771	ACVR1_HUMAN		Kd	6.22		CHEMBL
Interleukin-1 receptor-associated kinase 3	Kinase	Q9Y616	IRAK3_HUMAN		Kd	5.28		CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit alpha	Kinase	Q9UQM7	KCC2A_HUMAN		Kd	5.44		CHEMBL
G protein-coupled receptor kinase 4	Kinase	P32298	GRK4_HUMAN		Kd	7.77		CHEMBL
Mitogen-activated protein kinase kinase kinase 2	Kinase	Q9Y2U5	M3K2_HUMAN		Kd	8.03		CHEMBL
Cyclin-dependent kinase 2	Kinase	P24941	CDK2_HUMAN		Kd	5.85		CHEMBL
Serine/threonine-protein kinase ULK3	Kinase	Q6PHR2	ULK3_HUMAN		Kd	7.22		CHEMBL
Abelson tyrosine-protein kinase 2	Kinase	P42684	ABL2_HUMAN		Kd	5.70		CHEMBL
Serine/threonine-protein kinase MARK1	Kinase	Q9P0L2	MARK1_HUMAN		Kd	5.85		CHEMBL
Serine/threonine-protein kinase 26	Kinase	Q9P289	STK26_HUMAN		Kd	7.31		CHEMBL
Bone morphogenetic protein receptor type-2	Kinase	Q13873	BMPR2_HUMAN		Kd	7.25		CHEMBL
Protein-tyrosine kinase 2-beta	Kinase	Q14289	FAK2_HUMAN		Kd	7.09		CHEMBL
Tyrosine-protein kinase Blk	Kinase	P51451	BLK_HUMAN		Kd	6.42		CHEMBL
Serine/threonine-protein kinase LATS2	Kinase	Q9NRM7	LATS2_HUMAN		Kd	6.42		CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit alpha	Kinase	O15111	IKKA_HUMAN		Kd	5.35		CHEMBL
Angiopoietin-1 receptor	Kinase	Q02763	TIE2_HUMAN		Kd	5.85		CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit epsilon	Kinase	Q14164	IKKE_HUMAN		Kd	6.77		CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 1B	Kinase	Q9Y463	DYR1B_HUMAN		Kd	5.80		CHEMBL
Serine/threonine-protein kinase PRP4 homolog	Kinase	Q13523	PRP4B_HUMAN		Kd	8.08		CHEMBL
Proto-oncogene tyrosine-protein kinase ROS	Kinase	P08922	ROS1_HUMAN		Kd	5.43		CHEMBL
Ephrin type-B receptor 6	Kinase	O15197	EPHB6_HUMAN		Kd	6.85		CHEMBL
Mitogen-activated protein kinase 8	Kinase	P45983	MK08_HUMAN		Kd	6.20		CHEMBL
Serine/threonine-protein kinase SIK2	Kinase	Q9H0K1	SIK2_HUMAN		Kd	6.55		CHEMBL
Cyclin-dependent kinase 7	Kinase	P50613	CDK7_HUMAN		Kd	6.52		CHEMBL
Serine/threonine-protein kinase 24	Kinase	Q9Y6E0	STK24_HUMAN		Kd	6.96		CHEMBL
5'-AMP-activated protein kinase catalytic subunit alpha-2	Kinase	P54646	AAPK2_HUMAN		Kd	7.08		CHEMBL
Tyrosine-protein kinase Fyn	Kinase	P06241	FYN_HUMAN		Kd	6.20		CHEMBL
Macrophage colony-stimulating factor 1 receptor	Kinase	P07333	CSF1R_HUMAN		Kd	7.32		CHEMBL
Uncharacterized serine/threonine-protein kinase SBK3	Kinase	P0C264	SBK3_HUMAN		Kd	5.70		CHEMBL
Discoidin domain-containing receptor 2	Kinase	Q16832	DDR2_HUMAN		Kd	7.38		CHEMBL
Cyclin-dependent kinase 17	Kinase	Q00537	CDK17_HUMAN		Kd	7.03		CHEMBL
Death-associated protein kinase 3	Kinase	O43293	DAPK3_HUMAN		Kd	5.68		CHEMBL
Serine/threonine-protein kinase receptor R3	Kinase	P37023	ACVL1_HUMAN		Kd	5.38		CHEMBL
Activin receptor type-1B	Kinase	P36896	ACV1B_HUMAN		Kd	5.31		CHEMBL
Tyrosine-protein kinase receptor Tie-1	Kinase	P35590	TIE1_HUMAN		Kd	5.66		CHEMBL
TGF-beta receptor type-1	Kinase	P36897	TGFR1_HUMAN		Kd	5.38		CHEMBL
Serine/threonine-protein kinase PAK 4	Kinase	O96013	PAK4_HUMAN		Kd	5.52		CHEMBL
Serine/threonine-protein kinase DCLK3	Kinase	Q9C098	DCLK3_HUMAN		Kd	6.11		CHEMBL
Cyclin-dependent kinase 14	Kinase	O94921	CDK14_HUMAN		Kd	6.33		CHEMBL
Eukaryotic translation initiation factor 2-alpha kinase 4	Kinase	Q9P2K8	E2AK4_HUMAN		Kd	5.70		CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN		Kd	8.02		CHEMBL
Epithelial discoidin domain-containing receptor 1	Kinase	Q08345	DDR1_HUMAN		Kd	7.92		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 4	Kinase	O95819	M4K4_HUMAN		Kd	6.82		CHEMBL
Cyclin-dependent kinase 18	Kinase	Q07002	CDK18_HUMAN		Kd	6.29		CHEMBL
Serine/threonine-protein kinase LATS1	Kinase	O95835	LATS1_HUMAN		Kd	6.38		CHEMBL
Serine/threonine-protein kinase PAK 2	Kinase	Q13177	PAK2_HUMAN		Kd	5.48		CHEMBL
Tyrosine-protein kinase receptor TYRO3	Kinase	Q06418	TYRO3_HUMAN		Kd	5.31		CHEMBL
Tyrosine-protein kinase Fes/Fps	Kinase	P07332	FES_HUMAN		Kd	5.92		CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN		Kd	8.21		CHEMBL
Myosin light chain kinase 2, skeletal/cardiac muscle	Kinase	Q9H1R3	MYLK2_HUMAN		Kd	5.40		CHEMBL
Mitogen-activated protein kinase kinase kinase 9	Kinase	P80192	M3K9_HUMAN		Kd	6.66		CHEMBL
Leukocyte tyrosine kinase receptor	Kinase	P29376	LTK_HUMAN		Kd	6.82		CHEMBL
Mitogen-activated protein kinase kinase kinase 19	Kinase	Q56UN5	M3K19_HUMAN		Kd	8.28		CHEMBL
Tyrosine-protein kinase receptor UFO	Kinase	P30530	UFO_HUMAN		Kd	7.92		CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 beta	Kinase	P78356	PI42B_HUMAN		Kd	7.77		CHEMBL
3-phosphoinositide-dependent protein kinase 1	Kinase	O15530	PDPK1_HUMAN		Kd	5.55		CHEMBL
Serine/threonine-protein kinase D2	Kinase	Q9BZL6	KPCD2_HUMAN		Kd	6.14		CHEMBL
BDNF/NT-3 growth factors receptor	Kinase	Q16620	NTRK2_HUMAN		Kd	7.72		CHEMBL
NUAK family SNF1-like kinase 2	Kinase	Q9H093	NUAK2_HUMAN		Kd	7.68		CHEMBL
SRSF protein kinase 2	Kinase	P78362	SRPK2_HUMAN		Kd	7.44		CHEMBL
Dual specificity mitogen-activated protein kinase kinase 2	Kinase	P36507	MP2K2_HUMAN		Kd	7.38		CHEMBL
Dual specificity mitogen-activated protein kinase kinase 4	Kinase	P45985	MP2K4_HUMAN		Kd	5.43		CHEMBL
SRSF protein kinase 3	Kinase	Q9UPE1	SRPK3_HUMAN		Kd	7.92		CHEMBL
Tyrosine-protein kinase TXK	Kinase	P42681	TXK_HUMAN		Kd	6.07		CHEMBL
ALK tyrosine kinase receptor	Kinase	Q9UM73	ALK_HUMAN		Kd	7.51		CHEMBL
Mitogen-activated protein kinase kinase kinase 12	Kinase	Q12852	M3K12_HUMAN		Kd	6.85		CHEMBL
Myosin light chain kinase 3	Kinase	Q32MK0	MYLK3_HUMAN		Kd	6.96		CHEMBL
Receptor-interacting serine/threonine-protein kinase 1	Kinase	Q13546	RIPK1_HUMAN		Kd	6.62		CHEMBL
Phosphatidylinositol 4-phosphate 5-kinase type-1 alpha	Kinase	Q99755	PI51A_HUMAN		Kd	7.31		CHEMBL
Mitogen-activated protein kinase kinase kinase 3	Kinase	Q99759	M3K3_HUMAN		Kd	7.47		CHEMBL
Serine/threonine-protein kinase RIO1	Kinase	Q9BRS2	RIOK1_HUMAN		Kd	7.64		CHEMBL
Cyclin-dependent kinase 4	Kinase	P11802	CDK4_HUMAN		Kd	6.80		CHEMBL
Ribosomal protein S6 kinase beta-1	Kinase	P23443	KS6B1_HUMAN		Kd	6.72		CHEMBL
Serine/threonine-protein kinase ULK1	Kinase	O75385	ULK1_HUMAN		Kd	6.47		CHEMBL
Serine/threonine-protein kinase 33	Kinase	Q9BYT3	STK33_HUMAN		Kd	5.96		CHEMBL
Testis-specific serine/threonine-protein kinase 1	Kinase	Q9BXA7	TSSK1_HUMAN		Kd	5.21		CHEMBL
Glycogen synthase kinase-3 beta	Kinase	P49841	GSK3B_HUMAN		Kd	7.08		CHEMBL
Serine/threonine-protein kinase Chk1	Kinase	O14757	CHK1_HUMAN		Kd	6.54		CHEMBL
Glycogen synthase kinase-3 alpha	Kinase	P49840	GSK3A_HUMAN		Kd	6.37		CHEMBL
cGMP-dependent protein kinase 1	Kinase	Q13976	KGP1_HUMAN		Kd	7.85		CHEMBL
Receptor-interacting serine/threonine-protein kinase 4	Kinase	P57078	RIPK4_HUMAN		Kd	6.36		CHEMBL
Serine/threonine-protein kinase N1	Kinase	Q16512	PKN1_HUMAN		Kd	6.13		CHEMBL
Serine/threonine-protein kinase SIK1	Kinase	P57059	SIK1_HUMAN		Kd	6.17		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2	Kinase	Q12851	M4K2_HUMAN		Kd	6.54		CHEMBL
Tyrosine-protein kinase Mer	Kinase	Q12866	MERTK_HUMAN		Kd	8.07		CHEMBL
Mitogen-activated protein kinase 7	Kinase	Q13164	MK07_HUMAN		Kd	5.60		CHEMBL
Non-receptor tyrosine-protein kinase TNK1	Kinase	Q13470	TNK1_HUMAN		Kd	6.68		CHEMBL
Mitogen-activated protein kinase 10	Kinase	P53779	MK10_HUMAN		Kd	6.57		CHEMBL
Dual specificity mitogen-activated protein kinase kinase 1	Kinase	Q02750	MP2K1_HUMAN		Kd	8		CHEMBL
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN		Kd	8		CHEMBL
Cyclin-dependent kinase-like 2	Kinase	Q92772	CDKL2_HUMAN		Kd	5.89		CHEMBL
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN		Kd	9.38		CHEMBL
Protein kinase C theta type	Kinase	Q04759	KPCT_HUMAN		Kd	5.26		CHEMBL
Serine/threonine-protein kinase DCLK1	Kinase	O15075	DCLK1_HUMAN		Kd	6.27		CHEMBL
Muscle, skeletal receptor tyrosine-protein kinase	Kinase	O15146	MUSK_HUMAN		Kd	6.23		CHEMBL
Serine/threonine-protein kinase PknB	Kinase		PKNB_MYCTU		Kd	8.44		CHEMBL
Calcium-dependent protein kinase 1	Kinase		CDPK1_PLAF7		Kd	5.92		CHEMBL
Vascular endothelial growth factor receptor 2	Kinase		VGFR2_MOUSE		IC50	7.89		CHEMBL

External reference:

ID	Source
D10396	KEGG_DRUG
4033814	VUID
N0000191096	NUI
656247-18-6	SECONDARY_CAS_RN
4033814	VANDF
C1879771	UMLSCUI
CHEBI:85164	CHEBI
XIN	PDB_CHEM_ID
CHEMBL502835	ChEMBL_ID
CHEMBL3039504	ChEMBL_ID
DB09079	DRUGBANK_ID
C530716	MESH_SUPPLEMENTAL_RECORD_UI
135423438	PUBCHEM_CID
5936	IUPHAR_LIGAND_ID
9229	INN_ID
G6HRD2P839	UNII
1592736	RXNORM
229920	MMSL
30617	MMSL
d08301	MMSL
015720	NDDF
015723	NDDF
712494002	SNOMEDCT_US
715613009	SNOMEDCT_US
863993005	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Ofev	HUMAN PRESCRIPTION DRUG LABEL	1	0597-0143	CAPSULE	100 mg	ORAL	NDA	31 sections
Ofev	HUMAN PRESCRIPTION DRUG LABEL	1	0597-0145	CAPSULE	150 mg	ORAL	NDA	31 sections