crizotinib 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: 4.29 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:

None

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

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
Disease progression	801.68	24.30	379	8810	90921	46585952
Neoplasm progression	728.15	24.30	251	8938	26432	46650441
Non-small cell lung cancer	445.58	24.30	107	9082	3037	46673836
Lung neoplasm malignant	411.41	24.30	143	9046	15346	46661527
Death	324.78	24.30	362	8827	335186	46341687
Photopsia	241.11	24.30	69	9120	3907	46672966
Visual impairment	224.67	24.30	148	9041	66541	46610332
Nausea	193.24	24.30	418	8771	687036	45989837
Vomiting	124.75	24.30	274	8915	452520	46224353
Pleural effusion	109.05	24.30	106	9083	82846	46594027
Dysgeusia	103.61	24.30	76	9113	40415	46636458
Renal abscess	101.75	24.30	24	9165	627	46676246
Constipation	89.10	24.30	138	9051	173959	46502914
Oedema peripheral	87.95	24.30	131	9058	159575	46517298
Oesophagitis	87.44	24.30	46	9143	13605	46663268
Diarrhoea	84.57	24.30	271	8918	559331	46117542
Vitreous floaters	76.71	24.30	31	9158	5014	46671859
Pneumonitis	65.22	24.30	50	9139	28370	46648503
Interstitial lung disease	59.94	24.30	63	9126	53886	46622987
Neoplasm malignant	57.58	24.30	43	9146	23456	46653417
Oedema	50.37	24.30	64	9125	67007	46609866
Drug ineffective	48.19	24.30	38	9151	677800	45999073
Lung adenocarcinoma	41.39	24.30	19	9170	4185	46672688
Dysphagia	39.03	24.30	61	9128	77251	46599622
Decreased appetite	38.68	24.30	104	9085	193732	46483141
Non-small cell lung cancer metastatic	38.49	24.30	11	9178	618	46676255
Embolism	37.22	24.30	21	9168	7117	46669756
Multiple-drug resistance	36.39	24.30	15	9174	2550	46674323
Transaminases increased	35.51	24.30	35	9154	27726	46649147
Drug resistance	34.34	24.30	28	9161	17340	46659533
Acquired gene mutation	34.25	24.30	10	9179	606	46676267
Pericardial effusion	34.16	24.30	33	9156	25510	46651363
Renal cyst	33.24	24.30	21	9168	8738	46668135
Drug hypersensitivity	31.78	24.30	5	9184	243820	46433053
Vision blurred	31.03	24.30	56	9133	79652	46597221
Metastases to central nervous system	30.80	24.30	22	9167	11199	46665674
Bradycardia	30.29	24.30	50	9139	66248	46610625
Oesophageal pain	29.85	24.30	13	9176	2530	46674343
Visual brightness	29.63	24.30	5	9184	20	46676853
Hepatotoxicity	29.18	24.30	30	9159	24979	46651894
Pulmonary embolism	27.67	24.30	64	9125	108521	46568352
Oesophageal ulcer	27.22	24.30	14	9175	3947	46672926
Bronchial carcinoma	24.90	24.30	8	9181	669	46676204
Alanine aminotransferase increased	24.61	24.30	54	9135	88397	46588476

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	765.21	26.09	368	6468	79506	29866136
Neoplasm progression	579.85	26.09	199	6637	17824	29927818
Non-small cell lung cancer	416.75	26.09	108	6728	3622	29942020
Death	346.83	26.09	413	6423	356870	29588772
Lung neoplasm malignant	299.57	26.09	117	6719	15015	29930627
Visual impairment	113.12	26.09	76	6760	30362	29915280
Nausea	84.40	26.09	199	6637	296758	29648884
Neoplasm malignant	72.24	26.09	47	6789	17767	29927875
Oedema peripheral	62.40	26.09	97	6739	105735	29839907
Photopsia	58.08	26.09	20	6816	1786	29943856
Interstitial lung disease	53.11	26.09	67	6769	60130	29885512
Lung adenocarcinoma	51.62	26.09	23	6813	4076	29941566
Diarrhoea	48.21	26.09	176	6660	333927	29611715
Drug ineffective	45.51	26.09	11	6825	340376	29605266
Constipation	44.90	26.09	87	6749	112819	29832823
Dysgeusia	43.96	26.09	40	6796	24761	29920881
Oesophagitis	41.69	26.09	28	6808	11143	29934499
Pneumonitis	38.65	26.09	39	6797	27415	29918227
Oedema	38.12	26.09	48	6788	42945	29902697
Lung adenocarcinoma stage IV	38.07	26.09	8	6828	103	29945539
Vomiting	32.57	26.09	117	6719	219701	29725941
Pleural effusion	31.78	26.09	59	6777	74007	29871635
Hypoalbuminaemia	30.32	26.09	23	6813	11069	29934573
Second primary malignancy	28.80	26.09	18	6818	6338	29939304
Non-small cell lung cancer stage IV	28.01	26.09	7	6829	201	29945441
Decreased appetite	26.76	26.09	85	6751	149825	29795817
Metastases to central nervous system	26.56	26.09	18	6818	7266	29938376

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
FDA EPC	N0000175605	Kinase Inhibitor
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors
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	cytostatic
CHEBI has role	CHEBI:59163	biological marker
CHEBI has role	CHEBI:62434	alk inhibitor

Drug Use (View source of the data)

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

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)

None

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 ANULLPLASTIC 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 ANULLPLASTIC LARGE CELL LYMPHOMA (ALCL) THAT IS 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 ANULLPLASTIC 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 ANULLPLASTIC LARGE CELL LYMPHOMA (ALCL) THAT IS ALK-POSITIVE

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
ALK tyrosine kinase receptor	Kinase	Q9UM73	ALK_HUMAN	INHIBITOR	Ki	9.13		CHEMBL	CHEMBL
Hepatocyte growth factor receptor	Kinase	P08581	MET_HUMAN	INHIBITOR	Kd	9.26		CHEMBL	CHEMBL
SRSF protein kinase 1	Kinase	Q96SB4	SRPK1_HUMAN		Kd	5.74		CHEMBL
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN		Kd	6.68		CHEMBL
Cyclin-dependent kinase-like 2	Kinase	Q92772	CDKL2_HUMAN		Kd	5.68		CHEMBL
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN		Kd	8		CHEMBL
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN		Kd	5.57		CHEMBL
Serine/threonine-protein kinase DCLK1	Kinase	O15075	DCLK1_HUMAN		Kd	6.48		CHEMBL
Muscle, skeletal receptor tyrosine-protein kinase	Kinase	O15146	MUSK_HUMAN		Kd	6.64		CHEMBL
Vascular endothelial growth factor receptor 1	Kinase	P17948	VGFR1_HUMAN		Kd	5.64		CHEMBL
Proto-oncogene tyrosine-protein kinase Src	Kinase	P12931	SRC_HUMAN		Kd	6.25		CHEMBL
Fibroblast growth factor receptor 3	Kinase	P22607	FGFR3_HUMAN		Kd	5.57		CHEMBL
Serine/threonine-protein kinase 35	Kinase	Q8TDR2	STK35_HUMAN		Kd	6.21		CHEMBL
Insulin receptor	Kinase	P06213	INSR_HUMAN	AGONIST	Kd	6.47		CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 2	Kinase	Q92630	DYRK2_HUMAN		Kd	5.40		CHEMBL
Serine/threonine-protein kinase RIO3	Kinase	O14730	RIOK3_HUMAN		Kd	5.40		CHEMBL
Dual specificity mitogen-activated protein kinase kinase 3	Kinase	P46734	MP2K3_HUMAN		Kd	5.48		CHEMBL
Receptor-interacting serine/threonine-protein kinase 2	Kinase	O43353	RIPK2_HUMAN		Kd	6.05		CHEMBL
Ephrin type-B receptor 4	Kinase	P54760	EPHB4_HUMAN		Kd	6.24		CHEMBL
Tyrosine-protein kinase JAK2	Kinase	O60674	JAK2_HUMAN		Kd	6.54		CHEMBL
Serine/threonine-protein kinase NIM1	Kinase	Q8IY84	NIM1_HUMAN		Kd	5.34		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	5.55		CHEMBL
Aurora kinase A	Kinase	O14965	AURKA_HUMAN		Kd	6.59		CHEMBL
Tyrosine-protein kinase JAK1	Kinase	P23458	JAK1_HUMAN		Kd	6.48		CHEMBL
Tyrosine-protein kinase ITK/TSK	Kinase	Q08881	ITK_HUMAN		Kd	5.70		CHEMBL
Tyrosine-protein kinase SYK	Kinase	P43405	KSYK_HUMAN		Kd	5.60		CHEMBL
Interferon-induced, double-stranded RNA-activated protein kinase	Kinase	P19525	E2AK2_HUMAN		Kd	5.96		CHEMBL
Tyrosine-protein kinase BTK	Kinase	Q06187	BTK_HUMAN		Kd	5.11		CHEMBL
Cyclin-dependent kinase 11B	Kinase	P21127	CD11B_HUMAN		Kd	6.12		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	6.64		CHEMBL
Serine/threonine-protein kinase TBK1	Kinase	Q9UHD2	TBK1_HUMAN		Kd	6.16		CHEMBL
Ephrin type-A receptor 1	Kinase	P21709	EPHA1_HUMAN		Kd	6.85		CHEMBL
Serine/threonine-protein kinase Nek7	Kinase	Q8TDX7	NEK7_HUMAN		Kd	5.24		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1	Kinase	Q92918	M4K1_HUMAN		Kd	7.41		CHEMBL
AarF domain-containing protein kinase 4	Kinase	Q96D53	COQ8B_HUMAN		Kd	5.96		CHEMBL
Tyrosine-protein kinase Fgr	Kinase	P09769	FGR_HUMAN		Kd	6.17		CHEMBL
Serine/threonine-protein kinase D3	Kinase	O94806	KPCD3_HUMAN		Kd	6.29		CHEMBL
Mitogen-activated protein kinase kinase kinase 7	Kinase	O43318	M3K7_HUMAN		Kd	5.74		CHEMBL
Tyrosine-protein kinase FRK	Kinase	P42685	FRK_HUMAN		Kd	5.54		CHEMBL
Ephrin type-A receptor 8	Kinase	P29322	EPHA8_HUMAN		Kd	6.55		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
AP2-associated protein kinase 1	Kinase	Q2M2I8	AAK1_HUMAN		Kd	5.64		CHEMBL
Tyrosine-protein kinase JAK3	Kinase	P52333	JAK3_HUMAN		Kd	6.70		CHEMBL
Tyrosine-protein kinase Yes	Kinase	P07947	YES_HUMAN		Kd	6.11		CHEMBL
Serine/threonine-protein kinase TAO1	Kinase	Q7L7X3	TAOK1_HUMAN		Kd	5.92		CHEMBL
Serine/threonine-protein kinase TNNI3K	Kinase	Q59H18	TNI3K_HUMAN		Kd	6.96		CHEMBL
Aurora kinase C	Kinase	Q9UQB9	AURKC_HUMAN		Kd	5.37		CHEMBL
High affinity nerve growth factor receptor	Kinase	P04629	NTRK1_HUMAN		Kd	7.02		CHEMBL
Rho-associated protein kinase 1	Kinase	Q13464	ROCK1_HUMAN		Kd	5.43		CHEMBL
Ankyrin repeat and protein kinase domain-containing protein 1	Kinase	Q8NFD2	ANKK1_HUMAN		Kd	6.11		CHEMBL
Homeodomain-interacting protein kinase 4	Kinase	Q8NE63	HIPK4_HUMAN		Kd	5.44		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 5	Kinase	Q9Y4K4	M4K5_HUMAN		Kd	7.10		CHEMBL
Serine/threonine-protein kinase DCLK2	Kinase	Q8N568	DCLK2_HUMAN		Kd	6.43		CHEMBL
Misshapen-like kinase 1	Kinase	Q8N4C8	MINK1_HUMAN		Kd	5.36		CHEMBL
Interleukin-1 receptor-associated kinase 4	Kinase	Q9NWZ3	IRAK4_HUMAN		Kd	5.44		CHEMBL
Insulin receptor-related protein	Kinase	P14616	INSRR_HUMAN		Kd	6.22		CHEMBL
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN		Kd	6.10		CHEMBL
BMP-2-inducible protein kinase	Kinase	Q9NSY1	BMP2K_HUMAN		Kd	6.13		CHEMBL
Insulin-like growth factor 1 receptor	Kinase	P08069	IGF1R_HUMAN		Kd	6.11		CHEMBL
Ephrin type-A receptor 6	Kinase	Q9UF33	EPHA6_HUMAN		Kd	7.19		CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 2	Kinase	Q96RR4	KKCC2_HUMAN		Kd	5.82		CHEMBL
Aurora kinase B	Kinase	Q96GD4	AURKB_HUMAN		Kd	7.12		CHEMBL
STE20-like serine/threonine-protein kinase	Kinase	Q9H2G2	SLK_HUMAN		Kd	7.74		CHEMBL
Bone morphogenetic protein receptor type-1B	Kinase	O00238	BMR1B_HUMAN		Kd	6.64		CHEMBL
Macrophage-stimulating protein receptor	Kinase	Q04912	RON_HUMAN		Kd	7.60		CHEMBL
Non-receptor tyrosine-protein kinase TYK2	Kinase	P29597	TYK2_HUMAN		Kd	6.68		CHEMBL
Interleukin-1 receptor-associated kinase 1	Kinase	P51617	IRAK1_HUMAN		Kd	7.31		CHEMBL
Serine/threonine-protein kinase 4	Kinase	Q13043	STK4_HUMAN		Kd	6.24		CHEMBL
Ephrin type-A receptor 7	Kinase	Q15375	EPHA7_HUMAN		Kd	6.33		CHEMBL
Serine/threonine-protein kinase 3	Kinase	Q13188	STK3_HUMAN		Kd	6		CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit beta	Kinase	O14920	IKKB_HUMAN		Kd	5.26		CHEMBL
Serine/threonine-protein kinase Nek9	Kinase	Q8TD19	NEK9_HUMAN		Kd	6.10		CHEMBL
Serine/threonine-protein kinase TAO2	Kinase	Q9UL54	TAOK2_HUMAN		Kd	6.05		CHEMBL
Tyrosine-protein kinase Lyn	Kinase	P07948	LYN_HUMAN		Kd	6.03		CHEMBL
5'-AMP-activated protein kinase catalytic subunit alpha-1	Kinase	Q13131	AAPK1_HUMAN		Kd	5.62		CHEMBL
Cytoplasmic tyrosine-protein kinase BMX	Kinase	P51813	BMX_HUMAN		Kd	5.44		CHEMBL
Ephrin type-A receptor 5	Kinase	P54756	EPHA5_HUMAN		Kd	6		CHEMBL
LIM domain kinase 1	Kinase	P53667	LIMK1_HUMAN		Kd	6.08		CHEMBL
NPM/ALK (Nucleophosmin/ALK tyrosine kinase receptor)	Kinase	P06748 Q9UM73	ALK_HUMAN NPM_HUMAN		IC50	7.29		CHEMBL
Serine/threonine-protein kinase ULK2	Kinase	Q8IYT8	ULK2_HUMAN		Kd	5.80		CHEMBL
Ephrin type-A receptor 4	Kinase	P54764	EPHA4_HUMAN		Kd	6.44		CHEMBL
Ephrin type-B receptor 1	Kinase	P54762	EPHB1_HUMAN		Kd	6.92		CHEMBL
Activated CDC42 kinase 1	Kinase	Q07912	ACK1_HUMAN		Kd	6.12		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 3	Kinase	Q8IVH8	M4K3_HUMAN		Kd	7.12		CHEMBL
Dual specificity testis-specific protein kinase 1	Kinase	Q15569	TESK1_HUMAN		Kd	6.42		CHEMBL
Focal adhesion kinase 1	Kinase	Q05397	FAK1_HUMAN		Kd	6.51		CHEMBL
NT-3 growth factor receptor	Kinase	Q16288	NTRK3_HUMAN		Kd	7.09		CHEMBL
Tyrosine-protein kinase ZAP-70	Kinase	P43403	ZAP70_HUMAN		Kd	5.38		CHEMBL
Activin receptor type-1	Kinase	Q04771	ACVR1_HUMAN		Kd	6.36		CHEMBL
Interleukin-1 receptor-associated kinase 3	Kinase	Q9Y616	IRAK3_HUMAN		Kd	7.51		CHEMBL
G protein-coupled receptor kinase 4	Kinase	P32298	GRK4_HUMAN		Kd	5.38		CHEMBL
Mitogen-activated protein kinase kinase kinase 2	Kinase	Q9Y2U5	M3K2_HUMAN		Kd	7.14		CHEMBL
Serine/threonine-protein kinase ULK3	Kinase	Q6PHR2	ULK3_HUMAN		Kd	5.17		CHEMBL
Abelson tyrosine-protein kinase 2	Kinase	P42684	ABL2_HUMAN		Kd	6.34		CHEMBL
Serine/threonine-protein kinase 26	Kinase	Q9P289	STK26_HUMAN		Kd	5.55		CHEMBL
Protein-tyrosine kinase 2-beta	Kinase	Q14289	FAK2_HUMAN		Kd	6.72		CHEMBL
Tyrosine-protein kinase Blk	Kinase	P51451	BLK_HUMAN		Kd	6.96		CHEMBL
Angiopoietin-1 receptor	Kinase	Q02763	TIE2_HUMAN		Kd	6.57		CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit epsilon	Kinase	Q14164	IKKE_HUMAN		Kd	6.15		CHEMBL
Peripheral plasma membrane protein CASK	Kinase	O14936	CSKP_HUMAN		Kd	6.85		CHEMBL
Dual serine/threonine and tyrosine protein kinase	Kinase	Q6XUX3	DUSTY_HUMAN		Kd	6.35		CHEMBL
Proto-oncogene tyrosine-protein kinase ROS	Kinase	P08922	ROS1_HUMAN		Kd	8.39		CHEMBL
Ephrin type-B receptor 6	Kinase	O15197	EPHB6_HUMAN		Kd	8.22		CHEMBL
Serine/threonine-protein kinase SIK2	Kinase	Q9H0K1	SIK2_HUMAN		Kd	6.70		CHEMBL
Serine/threonine-protein kinase TAO3	Kinase	Q9H2K8	TAOK3_HUMAN		Kd	6.31		CHEMBL
Mitogen-activated protein kinase kinase kinase 1	Kinase	Q13233	M3K1_HUMAN		Kd	5.96		CHEMBL
Cyclin-dependent kinase 7	Kinase	P50613	CDK7_HUMAN		Kd	6.48		CHEMBL
Rho-associated protein kinase 2	Kinase	O75116	ROCK2_HUMAN		Kd	5.48		CHEMBL
Tyrosine-protein kinase Fyn	Kinase	P06241	FYN_HUMAN		Kd	5.89		CHEMBL
Macrophage colony-stimulating factor 1 receptor	Kinase	P07333	CSF1R_HUMAN		Kd	6.68		CHEMBL
Uncharacterized serine/threonine-protein kinase SBK3	Kinase	P0C264	SBK3_HUMAN		Kd	6.62		CHEMBL
Activin receptor type-1B	Kinase	P36896	ACV1B_HUMAN		Kd	6.07		CHEMBL
Tyrosine-protein kinase receptor Tie-1	Kinase	P35590	TIE1_HUMAN		Kd	6.96		CHEMBL
TGF-beta receptor type-1	Kinase	P36897	TGFR1_HUMAN		Kd	6		CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN		Kd	5.89		CHEMBL
Myotonin-protein kinase	Kinase	Q09013	DMPK_HUMAN		Kd	5.85		CHEMBL
Epithelial discoidin domain-containing receptor 1	Kinase	Q08345	DDR1_HUMAN		Kd	6.29		CHEMBL
Tyrosine-protein kinase receptor TYRO3	Kinase	Q06418	TYRO3_HUMAN		Kd	6.10		CHEMBL
Tyrosine-protein kinase Fes/Fps	Kinase	P07332	FES_HUMAN		Kd	6.35		CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN		Kd	7.52		CHEMBL
Leukocyte tyrosine kinase receptor	Kinase	P29376	LTK_HUMAN		Kd	7.92		CHEMBL
Mitogen-activated protein kinase kinase kinase 19	Kinase	Q56UN5	M3K19_HUMAN		Kd	6.01		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
NUAK family SNF1-like kinase 2	Kinase	Q9H093	NUAK2_HUMAN		Kd	6.92		CHEMBL
SRSF protein kinase 3	Kinase	Q9UPE1	SRPK3_HUMAN		Kd	5.09		CHEMBL
Tyrosine-protein kinase TXK	Kinase	P42681	TXK_HUMAN		Kd	6.07		CHEMBL
LIM domain kinase 2	Kinase	P53671	LIMK2_HUMAN		Kd	6.16		CHEMBL
Mitogen-activated protein kinase kinase kinase 12	Kinase	Q12852	M3K12_HUMAN		Kd	6.77		CHEMBL
Receptor-interacting serine/threonine-protein kinase 1	Kinase	Q13546	RIPK1_HUMAN		Kd	5.80		CHEMBL
Phosphatidylinositol 4-phosphate 5-kinase type-1 alpha	Kinase	Q99755	PI51A_HUMAN		Kd	5.49		CHEMBL
Mitogen-activated protein kinase kinase kinase 3	Kinase	Q99759	M3K3_HUMAN		Kd	6.96		CHEMBL
Cyclin-dependent kinase 11A	Kinase	Q9UQ88	CD11A_HUMAN		Kd	6.38		CHEMBL
Serine/threonine-protein kinase RIO1	Kinase	Q9BRS2	RIOK1_HUMAN		Kd	5.21		CHEMBL
Ribosomal protein S6 kinase beta-1	Kinase	P23443	KS6B1_HUMAN		Kd	6.19		CHEMBL
Serine/threonine-protein kinase ULK1	Kinase	O75385	ULK1_HUMAN		Kd	6		CHEMBL
Receptor-interacting serine/threonine-protein kinase 4	Kinase	P57078	RIPK4_HUMAN		Kd	5.68		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2	Kinase	Q12851	M4K2_HUMAN		Kd	7.10		CHEMBL
Tyrosine-protein kinase Mer	Kinase	Q12866	MERTK_HUMAN		Kd	8.44		CHEMBL
Mitogen-activated protein kinase 7	Kinase	Q13164	MK07_HUMAN		Kd	6.29		CHEMBL
Ephrin type-A receptor 2	Kinase	P29317	EPHA2_HUMAN		Kd	7		CHEMBL
Non-receptor tyrosine-protein kinase TNK1	Kinase	Q13470	TNK1_HUMAN		Kd	6.49		CHEMBL
Ephrin type-A receptor 3	Kinase	P29320	EPHA3_HUMAN		Kd	6.15		CHEMBL
Angiopoietin-1 receptor	Kinase		TIE2_MOUSE		IC50	6.35		CHEMBL
Tyrosine-protein kinase ABL1	Kinase		ABL1_MOUSE		IC50	5.94		CHEMBL
Macrophage-stimulating protein receptor	Kinase		RON_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
DB08865	DRUGBANK_ID
D000077547	MESH_DESCRIPTOR_UI
11626560	PUBCHEM_CID
4903	IUPHAR_LIGAND_ID
9301	INN_ID
53AH36668S	UNII
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	0069-8141	CAPSULE	200 mg	ORAL	NDA	32 sections