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	1412.64	44.35	363	2567	16732	2338423
Neoplasm progression	900.92	44.35	198	2732	4470	2350685
Nausea	781.02	44.35	375	2555	111814	2243341
Death	658.33	44.35	303	2627	81165	2273990
Lung neoplasm malignant	646.96	44.35	140	2790	2902	2352253
Non-small cell lung cancer	636.39	44.35	106	2824	467	2354688
Vomiting	492.04	44.35	239	2691	71363	2283792
Diarrhoea	471.54	44.35	244	2686	83320	2271835
Visual impairment	408.22	44.35	128	2802	11627	2343528
Constipation	338.97	44.35	130	2800	21499	2333656
Photopsia	330.22	44.35	66	2864	899	2354256
Oedema peripheral	289.01	44.35	119	2811	23644	2331511
Pleural effusion	263.68	44.35	92	2838	11576	2343579
Dysgeusia	215.45	44.35	73	2857	8386	2346769
Fatigue	192.03	44.35	139	2791	84734	2270421
Decreased appetite	186.08	44.35	93	2837	28798	2326357
Interstitial lung disease	177.78	44.35	62	2868	7750	2347405
Oesophagitis	155.67	44.35	41	2889	1965	2353190
Pneumonitis	143.90	44.35	45	2885	3994	2351161
Pneumonia	134.95	44.35	91	2839	49205	2305950
Vitreous floaters	131.13	44.35	31	2899	948	2354207
Renal abscess	129.38	44.35	23	2907	156	2354999
Neoplasm malignant	125.77	44.35	43	2887	5050	2350105
Dyspnoea	125.41	44.35	105	2825	78628	2276527
Dysphagia	124.87	44.35	55	2875	12750	2342405
Oedema	116.47	44.35	49	2881	10154	2345001
Pulmonary embolism	112.60	44.35	57	2873	18026	2337129
Product use issue	111.35	44.35	50	2880	12119	2343036
Asthenia	110.43	44.35	79	2851	46847	2308308
Peripheral swelling	102.38	44.35	53	2877	17544	2337611
Dizziness	96.85	44.35	80	2850	58585	2296570
Vision blurred	96.46	44.35	48	2882	14620	2340535
Alanine aminotransferase increased	95.48	44.35	47	2883	13985	2341170
Neutropenia	95.00	44.35	54	2876	21494	2333661
Transaminases increased	91.30	44.35	33	2897	4554	2350601
Hepatic enzyme increased	85.58	44.35	39	2891	9763	2345392
Bradycardia	81.78	44.35	38	2892	9943	2345212
Pericardial effusion	80.37	44.35	29	2901	3980	2351175
Renal impairment	78.29	44.35	37	2893	10055	2345100
Pyrexia	75.79	44.35	67	2863	53641	2301514
Malaise	75.79	44.35	68	2862	55517	2299638
Cardiac failure	74.84	44.35	38	2892	12056	2343099
Aspartate aminotransferase increased	73.33	44.35	38	2892	12574	2342581
Renal cyst	72.81	44.35	20	2910	1122	2354033
Embolism	70.04	44.35	20	2910	1293	2353862
Hepatotoxicity	65.37	44.35	24	2906	3457	2351698
Swelling	61.50	44.35	37	2893	16313	2338842
Dyspepsia	61.09	44.35	31	2899	9813	2345342
Renal failure	59.47	44.35	37	2893	17312	2337843
Dehydration	57.99	44.35	40	2890	22255	2332900
Non-small cell lung cancer metastatic	56.94	44.35	11	2919	123	2355032
Multiple-drug resistance	56.13	44.35	12	2918	229	2354926
Lung adenocarcinoma	52.46	44.35	14	2916	703	2354452
Oesophageal ulcer	51.96	44.35	14	2916	729	2354426
Acute kidney injury	51.83	44.35	41	2889	28081	2327074
Deep vein thrombosis	50.52	44.35	30	2900	12902	2342253
Oesophageal pain	50.23	44.35	12	2918	383	2354772
Electrocardiogram QT prolonged	49.61	44.35	25	2905	7789	2347366
Oesophageal candidiasis	48.40	44.35	13	2917	669	2354486
Liver disorder	48.13	44.35	23	2907	6391	2348764
White blood cell count decreased	48.11	44.35	33	2897	18175	2336980
Cough	47.98	44.35	42	2888	33075	2322080
Blood creatinine increased	47.96	44.35	27	2903	10506	2344649
Second primary malignancy	47.77	44.35	14	2916	992	2354163
Diplopia	47.50	44.35	19	2911	3446	2351709
Weight decreased	45.19	44.35	38	2892	28333	2326822

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	1262.07	55.42	352	1998	16911	1727520
Death	707.64	55.42	353	1997	87090	1657341
Neoplasm progression	619.78	55.42	144	2206	3123	1741308
Non-small cell lung cancer	571.94	55.42	103	2247	559	1743872
Lung neoplasm malignant	441.08	55.42	109	2241	3070	1741361
Nausea	330.91	55.42	180	2170	51016	1693415
Diarrhoea	270.99	55.42	161	2189	53691	1690740
Visual impairment	213.53	55.42	72	2278	6146	1738285
Oedema peripheral	193.53	55.42	86	2264	15464	1728967
Constipation	173.96	55.42	79	2271	14921	1729510
Vomiting	159.62	55.42	102	2248	38213	1706218
Interstitial lung disease	137.87	55.42	59	2291	9637	1734794
Neoplasm malignant	136.07	55.42	47	2303	4292	1740139
Decreased appetite	123.19	55.42	73	2277	23798	1720633
Fatigue	122.64	55.42	97	2253	50684	1693747
Pneumonitis	102.11	55.42	37	2313	3878	1740553
Pulmonary embolism	100.40	55.42	52	2298	13007	1731424
Dysgeusia	96.45	55.42	38	2312	5011	1739420
Pleural effusion	93.39	55.42	47	2303	11063	1733368
Pneumonia	91.99	55.42	79	2271	46103	1698328
Dehydration	90.93	55.42	54	2296	17604	1726827
Photopsia	84.76	55.42	20	2330	452	1743979
Dyspnoea	83.82	55.42	79	2271	51980	1692451
Oedema	81.56	55.42	37	2313	6911	1737520
Lung adenocarcinoma	81.21	55.42	21	2329	699	1743732
Product use issue	77.13	55.42	38	2312	8533	1735898
Stomatitis	77.06	55.42	33	2317	5371	1739060
Renal impairment	74.90	55.42	42	2308	12272	1732159
Oesophagitis	71.48	55.42	23	2327	1678	1742753
Respiratory failure	65.96	55.42	41	2309	14464	1729967
Dizziness	64.65	55.42	57	2293	34304	1710127
Hypoalbuminaemia	62.40	55.42	20	2330	1440	1742991
Vision blurred	57.43	55.42	31	2319	8392	1736039
Blood creatinine increased	57.35	55.42	37	2313	13909	1730522
Dysphagia	57.27	55.42	33	2317	10135	1734296
Hepatic function abnormal	56.66	55.42	29	2321	7045	1737386
Anaemia	55.63	55.42	49	2301	29408	1715023

Pharmacologic Action:

Source	Code	Description
ATC	L01XE16	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Protein kinase inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agent
CHEBI has role	CHEBI:59163	biomarker
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000190114	Cytochrome P450 3A Inhibitors
FDA MoA	N0000020000	Receptor Tyrosine Kinase Inhibitors
FDA MoA	N0000182139	Cytochrome P450 2B6 Inhibitors
FDA MoA	N0000185503	P-Glycoprotein Inhibitors
FDA MoA	N0000191265	Organic Cation Transporter 1 Inhibitors
FDA MoA	N0000187061	Organic Cation Transporter 2 Inhibitors

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)

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	TREATMENT OF A CANCER MEDIATED BY AN ANAPLASTIC LYMPHOMA KINASE (ALK)
250MG	XALKORI	PF PRISM CV	N202570	Aug. 26, 2011	RX	CAPSULE	ORAL	7825137	May 12, 2027	TREATMENT OF A CANCER MEDIATED BY AN ANAPLASTIC LYMPHOMA KINASE (ALK)

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.

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
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
SRSF protein kinase 1	Kinase	Q96SB4	SRPK1_HUMAN		Kd	5.74		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
Ephrin type-A receptor 2	Kinase	P29317	EPHA2_HUMAN		Kd	7		CHEMBL
Ephrin type-A receptor 3	Kinase	P29320	EPHA3_HUMAN		Kd	6.15		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
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN		Kd	6.68		CHEMBL
Non-receptor tyrosine-protein kinase TNK1	Kinase	Q13470	TNK1_HUMAN		Kd	6.49		CHEMBL
Cyclin-dependent kinase-like 2	Kinase	Q92772	CDKL2_HUMAN		Kd	5.68		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
D000077547	MESH_DESCRIPTOR_UI
4030983	VUID
N0000183253	NUI
C2974289	UMLSCUI
D09731	KEGG_DRUG
53AH36668S	UNII
9301	INN_ID
703638005	SNOMEDCT_US
1148495	RXNORM
013917	NDDF
28080	MMSL
d07800	MMSL
4030983	VANDF
703637000	SNOMEDCT_US
11626560	PUBCHEM_CID
CHEBI:64310	CHEBI
CHEMBL601719	ChEMBL_ID
VGH	PDB_CHEM_ID
DB08865	DRUGBANK_ID
4903	IUPHAR_LIGAND_ID

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Xalkori	HUMAN PRESCRIPTION DRUG LABEL	1	0069-8140	CAPSULE	250 mg	ORAL	NDA	17 sections
Xalkori	HUMAN PRESCRIPTION DRUG LABEL	1	0069-8141	CAPSULE	200 mg	ORAL	NDA	17 sections