crizotinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	4187	877399-52-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: crizotinib xalkori PF 02341066 PF-02341066	Crizotinib is an inhibitor of receptor tyrosine kinases including ALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), ROS1 (c-ros), and Recepteur d'Origine Nantais (RON). Translocations can affect the ALK gene resulting in the expression of oncogenic fusion proteins. The formation of ALK fusion proteins results in activation and dysregulation of the gene's expression and signaling which can contribute to increased cell proliferation and survival in tumors expressing these proteins. Crizotinib demonstrated concentration-dependent inhibition of ALK, ROS1, and c-Met phosphorylation in cell-based assays using tumor cell lines and demonstrated antitumor activity in mice bearing tumor xenografts that expressed echinoderm microtubule-associated protein-like 4 (EML4)- or nucleophosmin (NPM)-ALK fusion proteins or c-Met. Molecular weight: 450.34 Formula: C21H22Cl2FN5O CLOGP: 4.34 LIPINSKI: 0 HAC: 6 HDO: 2 TPSA: 77.99 ALOGS: -4.87 ROTB: 5 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

crizotinib
xalkori
PF 02341066
PF-02341066

Crizotinib is an inhibitor of receptor tyrosine kinases including ALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), ROS1 (c-ros), and Recepteur d'Origine Nantais (RON). Translocations can affect the ALK gene resulting in the expression of oncogenic fusion proteins. The formation of ALK fusion proteins results in activation and dysregulation of the gene's expression and signaling which can contribute to increased cell proliferation and survival in tumors expressing these proteins. Crizotinib demonstrated concentration-dependent inhibition of ALK, ROS1, and c-Met phosphorylation in cell-based assays using tumor cell lines and demonstrated antitumor activity in mice bearing tumor xenografts that expressed echinoderm microtubule-associated protein-like 4 (EML4)- or nucleophosmin (NPM)-ALK fusion proteins or c-Met.

Molecular weight: 450.34
Formula: C21H22Cl2FN5O
CLOGP: 4.34
LIPINSKI: 0
HAC: 6
HDO: 2
TPSA: 77.99
ALOGS: -4.87
ROTB: 5

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.50	g	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution)	22.15 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	9.75 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.09 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	38.90 hours	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.01 mg/mL	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company	Orphan
Oct. 23, 2012	EMA
Aug. 26, 2011	FDA	PF PRISM CV

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
Neoplasm progression	885.69	25.14	297	9686	36131	63442908
Disease progression	836.09	25.14	399	9584	122359	63356680
Death	439.09	25.14	404	9579	373977	63105062
Photopsia	252.42	25.14	70	9913	4439	63474600
Visual impairment	235.24	25.14	153	9830	84293	63394746
Nausea	227.23	25.14	445	9538	854026	62625013
Vomiting	153.27	25.14	296	9687	559321	62919718
Pleural effusion	137.07	25.14	115	9868	93095	63385944
Renal abscess	118.46	25.14	27	9956	763	63478276
Oedema peripheral	118.10	25.14	147	9836	189364	63289675
Dysgeusia	116.27	25.14	79	9904	46631	63432408
Diarrhoea	106.58	25.14	298	9685	715068	62763971
Oesophagitis	102.10	25.14	49	9934	14959	63464080
Constipation	96.98	25.14	146	9837	224797	63254242
Vitreous floaters	81.94	25.14	32	9951	5934	63473105
Drug resistance	74.81	25.14	46	9937	22887	63456152
Interstitial lung disease	72.14	25.14	67	9916	61841	63417198
Pneumonitis	67.87	25.14	51	9932	35171	63443868
Metastases to central nervous system	60.63	25.14	33	9950	13072	63465967
Pericardial effusion	50.22	25.14	40	9943	30018	63449021
Acquired gene mutation	49.25	25.14	14	9969	969	63478070
Dysphagia	49.19	25.14	65	9918	88520	63390519
Transaminases increased	48.72	25.14	40	9943	31327	63447712
Oedema	48.70	25.14	68	9915	97554	63381485
Pulmonary embolism	43.56	25.14	71	9912	116613	63362426
Decreased appetite	43.49	25.14	111	9872	250941	63228098
Embolism	42.48	25.14	22	9961	7884	63471155
Vision blurred	39.96	25.14	60	9923	91864	63387175
Drug ineffective	39.51	25.14	65	9918	1044700	62434339
Bradycardia	38.00	25.14	52	9931	73175	63405864
Oesophageal pain	37.62	25.14	16	9967	3685	63475354
Renal cyst	37.03	25.14	22	9961	10280	63468759
Oesophageal ulcer	34.65	25.14	16	9967	4474	63474565
Hepatotoxicity	33.63	25.14	35	9948	37006	63442033
Alanine aminotransferase increased	33.24	25.14	59	9924	103711	63375328
Drug hypersensitivity	32.55	25.14	5	9978	310682	63168357
Malignant neoplasm progression	32.04	25.14	51	9932	82070	63396969
Multiple-drug resistance	29.55	25.14	15	9968	5155	63473884
Visual brightness	29.07	25.14	5	9978	30	63479009
Oesophageal candidiasis	28.26	25.14	15	9968	5648	63473391
Renal cyst infection	28.11	25.14	6	9977	124	63478915
Diplopia	26.31	25.14	25	9958	23703	63455336
Electrocardiogram QT prolonged	26.06	25.14	39	9944	59491	63419548
Hypersensitivity	25.92	25.14	7	9976	292678	63186361

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
Disease progression	746.06	25.24	389	6996	107688	34841858
Neoplasm progression	662.58	25.24	230	7155	23070	34926476
Death	408.64	25.24	456	6929	397593	34551953
Visual impairment	109.57	25.24	77	7308	35725	34913821
Nausea	104.23	25.24	224	7161	339684	34609862
Oedema peripheral	68.70	25.24	104	7281	119708	34829838
Photopsia	61.81	25.24	21	7364	1947	34947599
Interstitial lung disease	57.72	25.24	70	7315	65212	34884334
Acquired gene mutation	52.74	25.24	17	7368	1338	34948208
Dysgeusia	50.36	25.24	43	7342	26454	34923092
Constipation	49.58	25.24	97	7288	136885	34812661
Diarrhoea	48.61	25.24	186	7199	389726	34559820
Vomiting	47.70	25.24	137	7248	247484	34702062
Oedema	47.00	25.24	53	7332	45688	34903858
Pneumonitis	39.56	25.24	42	7343	33836	34915710
Oesophagitis	39.30	25.24	28	7357	13233	34936313
Pleural effusion	38.70	25.24	65	7320	81481	34868065
Drug resistance	37.33	25.24	36	7349	25891	34923655
Hypoalbuminaemia	36.76	25.24	26	7359	12148	34937398
Metastases to central nervous system	35.66	25.24	22	7363	8183	34941363
Decreased appetite	34.85	25.24	95	7290	166297	34783249
Second primary malignancy	31.40	25.24	20	7365	7866	34941680
Malignant neoplasm progression	25.53	25.24	57	7328	87989	34861557

FDA Adverse Event Reporting System (Geriatric)

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
Disease progression	1370.97	21.23	687	15304	183675	79544722
Neoplasm progression	1184.13	21.23	429	15562	51253	79677144
Death	703.01	21.23	703	15288	565811	79162586
Nausea	279.93	21.23	599	15392	956597	78771800
Visual impairment	279.26	21.23	193	15798	91938	79636459
Photopsia	270.74	21.23	81	15910	5255	79723142
Oedema peripheral	156.35	21.23	221	15770	252067	79476330
Vomiting	156.10	21.23	383	15608	665445	79062952
Pleural effusion	152.60	21.23	166	15825	145096	79583301
Dysgeusia	143.73	21.23	107	15884	57070	79671327
Constipation	135.66	21.23	220	15771	282830	79445567
Renal abscess	127.73	21.23	32	15959	1061	79727336
Interstitial lung disease	122.27	21.23	131	15860	112469	79615928
Diarrhoea	119.77	21.23	417	15574	880072	78848325
Oesophagitis	113.63	21.23	67	15924	24222	79704175
Acquired gene mutation	96.62	21.23	30	15961	2203	79726194
Drug resistance	95.04	21.23	74	15917	42139	79686258
Vitreous floaters	84.22	21.23	37	15954	7219	79721178
Metastases to central nervous system	81.42	21.23	47	15944	16328	79712069
Decreased appetite	73.54	21.23	191	15800	342227	79386170
Pneumonitis	68.11	21.23	72	15919	60788	79667609
Embolism	58.73	21.23	36	15955	13946	79714451
Transaminases increased	57.51	21.23	61	15930	51682	79676715
Hypoalbuminaemia	56.05	21.23	41	15950	21256	79707141
Pulmonary embolism	55.94	21.23	113	15878	171541	79556856
Oedema	55.83	21.23	92	15899	119488	79608909
Malignant neoplasm progression	50.98	21.23	95	15896	135895	79592502
Renal cyst	49.62	21.23	33	15958	14699	79713698
Oesophageal ulcer	48.50	21.23	25	15966	6950	79721447
Toxicity to various agents	47.35	21.23	13	15978	421527	79306870
Pericardial effusion	46.99	21.23	52	15939	46185	79682212
Hepatic function abnormal	46.54	21.23	65	15926	73042	79655355
Dysphagia	45.37	21.23	85	15906	122051	79606346
Vision blurred	44.82	21.23	78	15913	105820	79622577
Drug ineffective	44.70	21.23	94	15897	1080819	78647578
Second primary malignancy	40.90	21.23	29	15962	14321	79714076
Multiple-drug resistance	40.40	21.23	24	15967	8784	79719613
Drug hypersensitivity	40.22	21.23	6	15985	298910	79429487
Hepatotoxicity	39.35	21.23	50	15941	51302	79677095
Renal cyst infection	39.20	21.23	9	15982	204	79728193
Electrocardiogram QT prolonged	37.49	21.23	66	15925	90320	79638077
Sinus bradycardia	35.84	21.23	34	15957	25213	79703184
Alanine aminotransferase increased	35.12	21.23	91	15900	162479	79565918
Carcinoembryonic antigen increased	34.80	21.23	14	15977	2195	79726202
Renal impairment	32.74	21.23	87	15904	157696	79570701
Lung adenocarcinoma	32.39	21.23	20	15971	7844	79720553
Bradycardia	31.49	21.23	78	15913	135479	79592918
Aspartate aminotransferase increased	27.30	21.23	75	15916	138566	79589831
Oesophageal candidiasis	27.13	21.23	19	15972	9199	79719198
Dehydration	26.33	21.23	109	15882	248078	79480319
Diplopia	26.29	21.23	33	15958	33433	79694964
Rheumatoid arthritis	26.23	21.23	5	15986	208465	79519932
Hypersensitivity	24.43	21.23	11	15980	262228	79466169
Pain	24.39	21.23	67	15924	703735	79024662
Adenocarcinoma metastatic	24.36	21.23	6	15985	185	79728212
Arthralgia	24.14	21.23	49	15942	571754	79156643
Oesophageal pain	23.20	21.23	13	15978	4266	79724131
Visual field defect	22.86	21.23	17	15974	9028	79719369
Hypertension	22.45	21.23	20	15971	330972	79397425
Urticaria	22.14	21.23	5	15986	185196	79543201
Sinusitis	21.98	21.23	6	15985	195495	79532902

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01ED01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Anaplastic lymphoma kinase (ALK) inhibitors
FDA MoA	N0000020000	Receptor Tyrosine Kinase Inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000182139	Cytochrome P450 2B6 Inhibitors
FDA MoA	N0000185503	P-Glycoprotein Inhibitors
FDA MoA	N0000187061	Organic Cation Transporter 2 Inhibitors
FDA MoA	N0000190114	Cytochrome P450 3A Inhibitors
FDA MoA	N0000191265	Organic Cation Transporter 1 Inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:59163	biological marker
CHEBI has role	CHEBI:62434	ALK inhibitor

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Non-small cell lung cancer	indication	254637007	DOID:3908

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.74	Basic
pKa2	6.14	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
200MG	XALKORI	PF PRISM CV	N202570	Aug. 26, 2011	RX	CAPSULE	ORAL	7825137	May 12, 2027	METHOD OF REVERSING OR INHIBITING THE PROGRESS OF UNRESECTABLE, RECURRENT, OR REFRACTORY INFLAMMATORY MYOFIBROBLASTIC TUMOR (IMT) THAT IS ALK-POSITIVE IN ADULT AND PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER
200MG	XALKORI	PF PRISM CV	N202570	Aug. 26, 2011	RX	CAPSULE	ORAL	7825137	May 12, 2027	TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) THAT IS ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE
200MG	XALKORI	PF PRISM CV	N202570	Aug. 26, 2011	RX	CAPSULE	ORAL	7825137	May 12, 2027	TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER AND YOUNG ADULTS WITH RELAPSED OR REFRACTORY, SYSTEMIC ANAPLASTIC LARGE CELL LYMPHOMA (ALCL) THAT IS ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE
250MG	XALKORI	PF PRISM CV	N202570	Aug. 26, 2011	RX	CAPSULE	ORAL	7825137	May 12, 2027	METHOD OF REVERSING OR INHIBITING THE PROGRESS OF UNRESECTABLE, RECURRENT, OR REFRACTORY INFLAMMATORY MYOFIBROBLASTIC TUMOR (IMT) THAT IS ALK-POSITIVE IN ADULT AND PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER
250MG	XALKORI	PF PRISM CV	N202570	Aug. 26, 2011	RX	CAPSULE	ORAL	7825137	May 12, 2027	TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) THAT IS ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE
250MG	XALKORI	PF PRISM CV	N202570	Aug. 26, 2011	RX	CAPSULE	ORAL	7825137	May 12, 2027	TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER AND YOUNG ADULTS WITH RELAPSED OR REFRACTORY, SYSTEMIC ANAPLASTIC LARGE CELL LYMPHOMA (ALCL) THAT IS ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
200MG	XALKORI	PF PRISM CV	N202570	Aug. 26, 2011	RX	CAPSULE	ORAL	March 11, 2023	TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER WHOSE TUMORS ARE ROS-1 POSITIVE.
250MG	XALKORI	PF PRISM CV	N202570	Aug. 26, 2011	RX	CAPSULE	ORAL	March 11, 2023	TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER WHOSE TUMORS ARE ROS-1 POSITIVE.
200MG	XALKORI	PF PRISM CV	N202570	Aug. 26, 2011	RX	CAPSULE	ORAL	Jan. 14, 2024	TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER AND YOUNG ADULTS WITH RELAPSED OR REFRACTORY, SYSTEMIC ANAPLASTIC LARGE CELL LYMPHOMA (ALCL) THAT IS ALK-POSITIVE
250MG	XALKORI	PF PRISM CV	N202570	Aug. 26, 2011	RX	CAPSULE	ORAL	Jan. 14, 2024	TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER AND YOUNG ADULTS WITH RELAPSED OR REFRACTORY, SYSTEMIC ANAPLASTIC LARGE CELL LYMPHOMA (ALCL) THAT IS ALK-POSITIVE
200MG	XALKORI	PF PRISM CV	N202570	Aug. 26, 2011	RX	CAPSULE	ORAL	July 14, 2025	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH UNRESECTABLE, RECURRENT OR REFRACTORY INFLAMMATORY MYOFIBROBLASTIC TUMOR (IMT) THAT IS ANAPLASTIC LYMPHOMA KINASE (ALK) POSITIVE
250MG	XALKORI	PF PRISM CV	N202570	Aug. 26, 2011	RX	CAPSULE	ORAL	July 14, 2025	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH UNRESECTABLE, RECURRENT OR REFRACTORY INFLAMMATORY MYOFIBROBLASTIC TUMOR (IMT) THAT IS ANAPLASTIC LYMPHOMA KINASE (ALK) POSITIVE
200MG	XALKORI	PF PRISM CV	N202570	Aug. 26, 2011	RX	CAPSULE	ORAL	Jan. 14, 2028	TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER AND YOUNG ADULTS WITH RELAPSED OR REFRACTORY, SYSTEMIC ANAPLASTIC LARGE CELL LYMPHOMA (ALCL) THAT IS ALK-POSITIVE
250MG	XALKORI	PF PRISM CV	N202570	Aug. 26, 2011	RX	CAPSULE	ORAL	Jan. 14, 2028	TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER AND YOUNG ADULTS WITH RELAPSED OR REFRACTORY, SYSTEMIC ANAPLASTIC LARGE CELL LYMPHOMA (ALCL) THAT IS ALK-POSITIVE
200MG	XALKORI	PF PRISM CV	N202570	Aug. 26, 2011	RX	CAPSULE	ORAL	July 14, 2029	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH UNRESECTABLE, RECURRENT, OR REFRACTORY INFLAMMATORY MYOFIBROBLASTIC TUMOR (IMT) THAT IS ALK-POSITIVE
250MG	XALKORI	PF PRISM CV	N202570	Aug. 26, 2011	RX	CAPSULE	ORAL	July 14, 2029	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH UNRESECTABLE, RECURRENT, OR REFRACTORY INFLAMMATORY MYOFIBROBLASTIC TUMOR (IMT) THAT IS ALK-POSITIVE

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Hepatocyte growth factor receptor	Kinase	P08581	MET_HUMAN	INHIBITOR	Kd	9.26	CHEMBL	CHEMBL
ALK tyrosine kinase receptor	Kinase	Q9UM73	ALK_HUMAN	INHIBITOR	Ki	9.13	CHEMBL	CHEMBL
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN		Kd	8	CHEMBL
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN		Kd	6.10	CHEMBL
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN		Kd	5.57	CHEMBL
Breakpoint cluster region protein	Kinase	P11274	BCR_HUMAN		Kd	5.61	CHEMBL
Proto-oncogene tyrosine-protein kinase Src	Kinase	P12931	SRC_HUMAN		Kd	6.25	CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN		Kd	7.52	CHEMBL
Tyrosine-protein kinase Yes	Kinase	P07947	YES_HUMAN		Kd	6.11	CHEMBL
Tyrosine-protein kinase Fyn	Kinase	P06241	FYN_HUMAN		Kd	5.89	CHEMBL
Ephrin type-A receptor 2	Kinase	P29317	EPHA2_HUMAN		Kd	7	CHEMBL
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN		Kd	6.68	CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN		Kd	5.89	CHEMBL
Vascular endothelial growth factor receptor 1	Kinase	P17948	VGFR1_HUMAN		Kd	5.64	CHEMBL
Macrophage colony-stimulating factor 1 receptor	Kinase	P07333	CSF1R_HUMAN		Kd	6.68	CHEMBL
Insulin-like growth factor 1 receptor	Kinase	P08069	IGF1R_HUMAN		Kd	6.11	CHEMBL
Insulin receptor	Kinase	P06213	INSR_HUMAN	AGONIST	Kd	6.47	CHEMBL
Fibroblast growth factor receptor 3	Kinase	P22607	FGFR3_HUMAN		Kd	5.57	CHEMBL
Rho-associated protein kinase 1	Kinase	Q13464	ROCK1_HUMAN		Kd	5.43	CHEMBL
Focal adhesion kinase 1	Kinase	Q05397	FAK1_HUMAN		Kd	6.51	CHEMBL
Tyrosine-protein kinase JAK1	Kinase	P23458	JAK1_HUMAN		Kd	6.48	CHEMBL
High affinity nerve growth factor receptor	Kinase	P04629	NTRK1_HUMAN		Kd	7.02	CHEMBL
Tyrosine-protein kinase JAK2	Kinase	O60674	JAK2_HUMAN		Kd	6.54	CHEMBL
Rho-associated protein kinase 2	Kinase	O75116	ROCK2_HUMAN		Kd	5.48	CHEMBL
Tyrosine-protein kinase SYK	Kinase	P43405	KSYK_HUMAN		Kd	5.60	CHEMBL
Angiopoietin-1 receptor	Kinase	Q02763	TIE2_HUMAN		Kd	6.57	CHEMBL
Ephrin type-A receptor 8	Kinase	P29322	EPHA8_HUMAN		Kd	6.55	CHEMBL
AP2-associated protein kinase 1	Kinase	Q2M2I8	AAK1_HUMAN		Kd	5.64	CHEMBL
Tyrosine-protein kinase Lyn	Kinase	P07948	LYN_HUMAN		Kd	6.03	CHEMBL
Cytoplasmic tyrosine-protein kinase BMX	Kinase	P51813	BMX_HUMAN		Kd	5.44	CHEMBL
LIM domain kinase 1	Kinase	P53667	LIMK1_HUMAN		Kd	6.08	CHEMBL
5'-AMP-activated protein kinase catalytic subunit alpha-1	Kinase	Q13131	AAPK1_HUMAN		Kd	5.62	CHEMBL
Serine/threonine-protein kinase 10	Kinase	O94804	STK10_HUMAN		Kd	7.36	CHEMBL
Tyrosine-protein kinase Fer	Kinase	P16591	FER_HUMAN		Kd	6.57	CHEMBL
Serine/threonine-protein kinase PLK4	Kinase	O00444	PLK4_HUMAN		Kd	7.22	CHEMBL
Aurora kinase C	Kinase	Q9UQB9	AURKC_HUMAN		Kd	5.37	CHEMBL
Abelson tyrosine-protein kinase 2	Kinase	P42684	ABL2_HUMAN		Kd	6.34	CHEMBL
Ephrin type-A receptor 5	Kinase	P54756	EPHA5_HUMAN		Kd	6	CHEMBL
Ephrin type-A receptor 4	Kinase	P54764	EPHA4_HUMAN		Kd	6.44	CHEMBL
Ephrin type-A receptor 6	Kinase	Q9UF33	EPHA6_HUMAN		Kd	7.19	CHEMBL
Tyrosine-protein kinase Fgr	Kinase	P09769	FGR_HUMAN		Kd	6.17	CHEMBL
Aurora kinase A	Kinase	O14965	AURKA_HUMAN		Kd	6.59	CHEMBL
Ephrin type-A receptor 3	Kinase	P29320	EPHA3_HUMAN		Kd	6.15	CHEMBL
BMP-2-inducible protein kinase	Kinase	Q9NSY1	BMP2K_HUMAN		Kd	6.13	CHEMBL
Tyrosine-protein kinase FRK	Kinase	P42685	FRK_HUMAN		Kd	5.54	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 5	Kinase	Q9Y4K4	M4K5_HUMAN		Kd	7.10	CHEMBL
Receptor-interacting serine/threonine-protein kinase 2	Kinase	O43353	RIPK2_HUMAN		Kd	6.05	CHEMBL
Ephrin type-B receptor 1	Kinase	P54762	EPHB1_HUMAN		Kd	6.92	CHEMBL
Serine/threonine-protein kinase 4	Kinase	Q13043	STK4_HUMAN		Kd	6.24	CHEMBL
Activated CDC42 kinase 1	Kinase	Q07912	ACK1_HUMAN		Kd	6.12	CHEMBL
Ephrin type-A receptor 7	Kinase	Q15375	EPHA7_HUMAN		Kd	6.33	CHEMBL
STE20-like serine/threonine-protein kinase	Kinase	Q9H2G2	SLK_HUMAN		Kd	7.74	CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 2	Kinase	Q96RR4	KKCC2_HUMAN		Kd	5.82	CHEMBL
Epithelial discoidin domain-containing receptor 1	Kinase	Q08345	DDR1_HUMAN		Kd	6.29	CHEMBL
Ephrin type-B receptor 4	Kinase	P54760	EPHB4_HUMAN		Kd	6.24	CHEMBL
Activin receptor type-1B	Kinase	P36896	ACV1B_HUMAN		Kd	6.07	CHEMBL
Activin receptor type-1	Kinase	Q04771	ACVR1_HUMAN		Kd	6.36	CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit beta	Kinase	O14920	IKKB_HUMAN		Kd	5.26	CHEMBL
Tyrosine-protein kinase ITK/TSK	Kinase	Q08881	ITK_HUMAN		Kd	5.70	CHEMBL
Tyrosine-protein kinase ZAP-70	Kinase	P43403	ZAP70_HUMAN		Kd	5.38	CHEMBL
Tyrosine-protein kinase BTK	Kinase	Q06187	BTK_HUMAN		Kd	5.11	CHEMBL
Tyrosine-protein kinase receptor UFO	Kinase	P30530	UFO_HUMAN		Kd	8.11	CHEMBL
BDNF/NT-3 growth factors receptor	Kinase	Q16620	NTRK2_HUMAN		Kd	7.43	CHEMBL
Tyrosine-protein kinase receptor TYRO3	Kinase	Q06418	TYRO3_HUMAN		Kd	6.10	CHEMBL
Cyclin-dependent kinase 7	Kinase	P50613	CDK7_HUMAN		Kd	6.48	CHEMBL
Serine/threonine-protein kinase D1	Kinase	Q15139	KPCD1_HUMAN		Kd	6	CHEMBL
Ribosomal protein S6 kinase beta-1	Kinase	P23443	KS6B1_HUMAN		Kd	6.19	CHEMBL
Serine/threonine-protein kinase 3	Kinase	Q13188	STK3_HUMAN		Kd	6	CHEMBL
NUAK family SNF1-like kinase 2	Kinase	Q9H093	NUAK2_HUMAN		Kd	6.92	CHEMBL
Non-receptor tyrosine-protein kinase TNK1	Kinase	Q13470	TNK1_HUMAN		Kd	6.49	CHEMBL
Non-receptor tyrosine-protein kinase TYK2	Kinase	P29597	TYK2_HUMAN		Kd	6.68	CHEMBL
Phosphatidylinositol 4-phosphate 5-kinase type-1 alpha	Kinase	Q99755	PI51A_HUMAN		Kd	5.49	CHEMBL
Protein-tyrosine kinase 2-beta	Kinase	Q14289	FAK2_HUMAN		Kd	6.72	CHEMBL
Serine/threonine-protein kinase RIO1	Kinase	Q9BRS2	RIOK1_HUMAN		Kd	5.21	CHEMBL
Tyrosine-protein kinase receptor Tie-1	Kinase	P35590	TIE1_HUMAN		Kd	6.96	CHEMBL
NT-3 growth factor receptor	Kinase	Q16288	NTRK3_HUMAN		Kd	7.09	CHEMBL
Tyrosine-protein kinase TXK	Kinase	P42681	TXK_HUMAN		Kd	6.07	CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit epsilon	Kinase	Q14164	IKKE_HUMAN		Kd	6.15	CHEMBL
LIM domain kinase 2	Kinase	P53671	LIMK2_HUMAN		Kd	6.16	CHEMBL
Dual specificity mitogen-activated protein kinase kinase 3	Kinase	P46734	MP2K3_HUMAN		Kd	5.48	CHEMBL
Serine/threonine-protein kinase 26	Kinase	Q9P289	STK26_HUMAN		Kd	5.55	CHEMBL
Serine/threonine-protein kinase Nek7	Kinase	Q8TDX7	NEK7_HUMAN		Kd	5.24	CHEMBL
Insulin receptor-related protein	Kinase	P14616	INSRR_HUMAN		Kd	6.22	CHEMBL
Interleukin-1 receptor-associated kinase 3	Kinase	Q9Y616	IRAK3_HUMAN		Kd	7.51	CHEMBL
Serine/threonine-protein kinase RIO3	Kinase	O14730	RIOK3_HUMAN		Kd	5.40	CHEMBL
Serine/threonine-protein kinase SIK2	Kinase	Q9H0K1	SIK2_HUMAN		Kd	6.70	CHEMBL
SRSF protein kinase 1	Kinase	Q96SB4	SRPK1_HUMAN		Kd	5.74	CHEMBL
Serine/threonine-protein kinase TNNI3K	Kinase	Q59H18	TNI3K_HUMAN		Kd	6.96	CHEMBL
Ankyrin repeat and protein kinase domain-containing protein 1	Kinase	Q8NFD2	ANKK1_HUMAN		Kd	6.11	CHEMBL
Myotonin-protein kinase	Kinase	Q09013	DMPK_HUMAN		Kd	5.85	CHEMBL
Leukocyte tyrosine kinase receptor	Kinase	P29376	LTK_HUMAN		Kd	7.92	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1	Kinase	Q92918	M4K1_HUMAN		Kd	7.41	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 3	Kinase	Q8IVH8	M4K3_HUMAN		Kd	7.12	CHEMBL
Aurora kinase B	Kinase	Q96GD4	AURKB_HUMAN		Kd	7.12	CHEMBL
Tyrosine-protein kinase Blk	Kinase	P51451	BLK_HUMAN		Kd	6.96	CHEMBL
Tyrosine-protein kinase Mer	Kinase	Q12866	MERTK_HUMAN		Kd	8.44	CHEMBL
Cyclin-dependent kinase 11B	Kinase	P21127	CD11B_HUMAN		Kd	6.12	CHEMBL
Cyclin-dependent kinase 11A	Kinase	Q9UQ88	CD11A_HUMAN		Kd	6.38	CHEMBL
Muscle, skeletal receptor tyrosine-protein kinase	Kinase	O15146	MUSK_HUMAN		Kd	6.64	CHEMBL
Serine/threonine-protein kinase DCLK1	Kinase	O15075	DCLK1_HUMAN		Kd	6.48	CHEMBL
Serine/threonine-protein kinase DCLK2	Kinase	Q8N568	DCLK2_HUMAN		Kd	6.43	CHEMBL
Serine/threonine-protein kinase Nek9	Kinase	Q8TD19	NEK9_HUMAN		Kd	6.10	CHEMBL
AarF domain-containing protein kinase 4	Kinase	Q96D53	COQ8B_HUMAN		Kd	5.96	CHEMBL
Dual specificity testis-specific protein kinase 1	Kinase	Q15569	TESK1_HUMAN		Kd	6.42	CHEMBL
TGF-beta receptor type-1	Kinase	P36897	TGFR1_HUMAN		Kd	6	CHEMBL
Ephrin type-A receptor 1	Kinase	P21709	EPHA1_HUMAN		Kd	6.85	CHEMBL
Mitogen-activated protein kinase 6	Kinase	Q16659	MK06_HUMAN		Kd	5.47	CHEMBL
Mitogen-activated protein kinase 7	Kinase	Q13164	MK07_HUMAN		Kd	6.29	CHEMBL
Serine/threonine-protein kinase D2	Kinase	Q9BZL6	KPCD2_HUMAN		Kd	5.19	CHEMBL
Serine/threonine-protein kinase D3	Kinase	O94806	KPCD3_HUMAN		Kd	6.29	CHEMBL
Interferon-induced, double-stranded RNA-activated protein kinase	Kinase	P19525	E2AK2_HUMAN		Kd	5.96	CHEMBL
Receptor-interacting serine/threonine-protein kinase 1	Kinase	Q13546	RIPK1_HUMAN		Kd	5.80	CHEMBL
Tyrosine-protein kinase Fes/Fps	Kinase	P07332	FES_HUMAN		Kd	6.35	CHEMBL
Proto-oncogene tyrosine-protein kinase ROS	Kinase	P08922	ROS1_HUMAN		Kd	8.39	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2	Kinase	Q12851	M4K2_HUMAN		Kd	7.10	CHEMBL
Misshapen-like kinase 1	Kinase	Q8N4C8	MINK1_HUMAN		Kd	5.36	CHEMBL
Serine/threonine-protein kinase TBK1	Kinase	Q9UHD2	TBK1_HUMAN		Kd	6.16	CHEMBL
Interleukin-1 receptor-associated kinase 4	Kinase	Q9NWZ3	IRAK4_HUMAN		Kd	5.44	CHEMBL
Cyclin-dependent kinase-like 2	Kinase	Q92772	CDKL2_HUMAN		Kd	5.68	CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 2	Kinase	Q92630	DYRK2_HUMAN		Kd	5.40	CHEMBL
Ephrin type-B receptor 6	Kinase	O15197	EPHB6_HUMAN		Kd	8.22	CHEMBL
G protein-coupled receptor kinase 4	Kinase	P32298	GRK4_HUMAN		Kd	5.38	CHEMBL
Homeodomain-interacting protein kinase 4	Kinase	Q8NE63	HIPK4_HUMAN		Kd	5.44	CHEMBL
Interleukin-1 receptor-associated kinase 1	Kinase	P51617	IRAK1_HUMAN		Kd	7.31	CHEMBL
Mitogen-activated protein kinase kinase kinase 13	Kinase	O43283	M3K13_HUMAN		Kd	6.64	CHEMBL
Mitogen-activated protein kinase kinase kinase 2	Kinase	Q9Y2U5	M3K2_HUMAN		Kd	7.14	CHEMBL
Mitogen-activated protein kinase kinase kinase 3	Kinase	Q99759	M3K3_HUMAN		Kd	6.96	CHEMBL
Serine/threonine-protein kinase NIM1	Kinase	Q8IY84	NIM1_HUMAN		Kd	5.34	CHEMBL
SRSF protein kinase 3	Kinase	Q9UPE1	SRPK3_HUMAN		Kd	5.09	CHEMBL
Mitogen-activated protein kinase kinase kinase 7	Kinase	O43318	M3K7_HUMAN		Kd	5.74	CHEMBL
Serine/threonine-protein kinase TAO1	Kinase	Q7L7X3	TAOK1_HUMAN		Kd	5.92	CHEMBL
Serine/threonine-protein kinase TAO3	Kinase	Q9H2K8	TAOK3_HUMAN		Kd	6.31	CHEMBL
Serine/threonine-protein kinase ULK1	Kinase	O75385	ULK1_HUMAN		Kd	6	CHEMBL
Serine/threonine-protein kinase ULK2	Kinase	Q8IYT8	ULK2_HUMAN		Kd	5.80	CHEMBL
Serine/threonine-protein kinase ULK3	Kinase	Q6PHR2	ULK3_HUMAN		Kd	5.17	CHEMBL
Mitogen-activated protein kinase kinase kinase 19	Kinase	Q56UN5	M3K19_HUMAN		Kd	6.01	CHEMBL
Mitogen-activated protein kinase kinase kinase 15	Kinase	Q6ZN16	M3K15_HUMAN		Kd	5.55	CHEMBL
Receptor-interacting serine/threonine-protein kinase 4	Kinase	P57078	RIPK4_HUMAN		Kd	5.68	CHEMBL
Uncharacterized serine/threonine-protein kinase SBK3	Kinase	P0C264	SBK3_HUMAN		Kd	6.62	CHEMBL
Serine/threonine-protein kinase 35	Kinase	Q8TDR2	STK35_HUMAN		Kd	6.21	CHEMBL
Mitogen-activated protein kinase kinase kinase 1	Kinase	Q13233	M3K1_HUMAN		Kd	5.96	CHEMBL
Bone morphogenetic protein receptor type-1B	Kinase	O00238	BMR1B_HUMAN		Kd	6.64	CHEMBL
Serine/threonine-protein kinase SBK1	Kinase	Q52WX2	SBK1_HUMAN		Kd	5.89	CHEMBL
Peripheral plasma membrane protein CASK	Kinase	O14936	CSKP_HUMAN		Kd	6.85	CHEMBL
Mitogen-activated protein kinase kinase kinase 12	Kinase	Q12852	M3K12_HUMAN		Kd	6.77	CHEMBL
Serine/threonine-protein kinase TAO2	Kinase	Q9UL54	TAOK2_HUMAN		Kd	6.05	CHEMBL
Dual serine/threonine and tyrosine protein kinase	Kinase	Q6XUX3	DUSTY_HUMAN		Kd	6.35	CHEMBL
NPM/ALK (Nucleophosmin/ALK tyrosine kinase receptor)	Kinase	P06748 Q9UM73	NPM_HUMAN ALK_HUMAN		IC50	7.29	CHEMBL
Phosphatidylinositol 3,4,5-trisphosphate 5-phosphatase 2	Enzyme	O15357	SHIP2_HUMAN		IC50	5.26	CHEMBL
Receptor-interacting serine/threonine-protein kinase 3	Kinase	Q9Y572	RIPK3_HUMAN		Kd	5.17	CHEMBL
Mixed lineage kinase domain-like protein	Kinase	Q8NB16	MLKL_HUMAN		Kd	6.66	CHEMBL
Tyrosine-protein kinase JAK3	Kinase	P52333	JAK3_HUMAN		Kd	6.70	CHEMBL
Acyl-CoA dehydrogenase family member 11	Enzyme	Q709F0	ACD11_HUMAN		Kd	5.72	CHEMBL
Macrophage-stimulating protein receptor	Kinase	Q04912	RON_HUMAN		Kd	7.60	CHEMBL
Tyrosine-protein kinase ABL1	Kinase		ABL1_MOUSE		IC50	5.94	CHEMBL
Macrophage-stimulating protein receptor	Kinase		RON_MOUSE		IC50	7.10	CHEMBL
Angiopoietin-1 receptor	Kinase		TIE2_MOUSE		IC50	6.35	CHEMBL
ALK tyrosine kinase receptor	Kinase		ALK_MOUSE		IC50	7.10	CHEMBL

External reference:

ID	Source
4030983	VUID
N0000183253	NUI
D09731	KEGG_DRUG
4030983	VANDF
C2974289	UMLSCUI
CHEBI:64310	CHEBI
VGH	PDB_CHEM_ID
CHEMBL601719	ChEMBL_ID
D000077547	MESH_DESCRIPTOR_UI
DB08865	DRUGBANK_ID
4903	IUPHAR_LIGAND_ID
9301	INN_ID
53AH36668S	UNII
11626560	PUBCHEM_CID
1148495	RXNORM
185331	MMSL
28080	MMSL
d07800	MMSL
013917	NDDF
703637000	SNOMEDCT_US
703638005	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Xalkori	HUMAN PRESCRIPTION DRUG LABEL	1	0069-8140	CAPSULE	250 mg	ORAL	NDA	32 sections
Xalkori	HUMAN PRESCRIPTION DRUG LABEL	1	0069-8140	CAPSULE	250 mg	ORAL	NDA	32 sections
Xalkori	HUMAN PRESCRIPTION DRUG LABEL	1	0069-8141	CAPSULE	200 mg	ORAL	NDA	32 sections
Xalkori	HUMAN PRESCRIPTION DRUG LABEL	1	0069-8141	CAPSULE	200 mg	ORAL	NDA	32 sections