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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 4187 877399-52-5

Description:

MoleculeDescription

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:

PropertyValueReference
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:

DateAgencyCompanyOrphan
Oct. 23, 2012 EMA
Aug. 26, 2011 FDA PF PRISM CV

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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:

SourceCodeDescription
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)

DiseaseRelationSNOMED_IDDOID
Non-small cell lung cancer indication 254637007 DOID:3908

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.74 Basic
pKa2 6.14 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
ALK tyrosine kinase receptor Kinase INHIBITOR Ki 9.13 CHEMBL CHEMBL
Hepatocyte growth factor receptor Kinase INHIBITOR Kd 9.26 CHEMBL CHEMBL
Tyrosine-protein kinase ABL1 Kinase Kd 8 CHEMBL
Epidermal growth factor receptor Kinase Kd 5.57 CHEMBL
Serine/threonine-protein kinase DCLK1 Kinase Kd 6.48 CHEMBL
Muscle, skeletal receptor tyrosine-protein kinase Kinase Kd 6.64 CHEMBL
Vascular endothelial growth factor receptor 1 Kinase Kd 5.64 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase Kd 6.25 CHEMBL
Fibroblast growth factor receptor 3 Kinase Kd 5.57 CHEMBL
Serine/threonine-protein kinase 35 Kinase Kd 6.21 CHEMBL
Insulin receptor Kinase AGONIST Kd 6.47 CHEMBL
SRSF protein kinase 1 Kinase Kd 5.74 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 2 Kinase Kd 5.40 CHEMBL
Serine/threonine-protein kinase RIO3 Kinase Kd 5.40 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 3 Kinase Kd 5.48 CHEMBL
Receptor-interacting serine/threonine-protein kinase 2 Kinase Kd 6.05 CHEMBL
Ephrin type-B receptor 4 Kinase Kd 6.24 CHEMBL
Tyrosine-protein kinase JAK2 Kinase Kd 6.54 CHEMBL
Serine/threonine-protein kinase NIM1 Kinase Kd 5.34 CHEMBL
Serine/threonine-protein kinase SBK1 Kinase Kd 5.89 CHEMBL
Mitogen-activated protein kinase kinase kinase 15 Kinase Kd 5.55 CHEMBL
Aurora kinase A Kinase Kd 6.59 CHEMBL
Tyrosine-protein kinase JAK1 Kinase Kd 6.48 CHEMBL
Tyrosine-protein kinase ITK/TSK Kinase Kd 5.70 CHEMBL
Tyrosine-protein kinase SYK Kinase Kd 5.60 CHEMBL
Interferon-induced, double-stranded RNA-activated protein kinase Kinase Kd 5.96 CHEMBL
Tyrosine-protein kinase BTK Kinase Kd 5.11 CHEMBL
Cyclin-dependent kinase 11B Kinase Kd 6.12 CHEMBL
Serine/threonine-protein kinase D1 Kinase Kd 6 CHEMBL
Mitogen-activated protein kinase kinase kinase 13 Kinase Kd 6.64 CHEMBL
Serine/threonine-protein kinase TBK1 Kinase Kd 6.16 CHEMBL
Ephrin type-A receptor 1 Kinase Kd 6.85 CHEMBL
Serine/threonine-protein kinase Nek7 Kinase Kd 5.24 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1 Kinase Kd 7.41 CHEMBL
AarF domain-containing protein kinase 4 Kinase Kd 5.96 CHEMBL
Tyrosine-protein kinase Fgr Kinase Kd 6.17 CHEMBL
Serine/threonine-protein kinase D3 Kinase Kd 6.29 CHEMBL
Mitogen-activated protein kinase kinase kinase 7 Kinase Kd 5.74 CHEMBL
Tyrosine-protein kinase FRK Kinase Kd 5.54 CHEMBL
Ephrin type-A receptor 8 Kinase Kd 6.55 CHEMBL
Ephrin type-A receptor 2 Kinase Kd 7 CHEMBL
Ephrin type-A receptor 3 Kinase Kd 6.15 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 7.36 CHEMBL
Tyrosine-protein kinase Fer Kinase Kd 6.57 CHEMBL
Serine/threonine-protein kinase PLK4 Kinase Kd 7.22 CHEMBL
AP2-associated protein kinase 1 Kinase Kd 5.64 CHEMBL
Tyrosine-protein kinase JAK3 Kinase Kd 6.70 CHEMBL
Tyrosine-protein kinase Yes Kinase Kd 6.11 CHEMBL
Serine/threonine-protein kinase TAO1 Kinase Kd 5.92 CHEMBL
Serine/threonine-protein kinase TNNI3K Kinase Kd 6.96 CHEMBL
Aurora kinase C Kinase Kd 5.37 CHEMBL
High affinity nerve growth factor receptor Kinase Kd 7.02 CHEMBL
Rho-associated protein kinase 1 Kinase Kd 5.43 CHEMBL
Ankyrin repeat and protein kinase domain-containing protein 1 Kinase Kd 6.11 CHEMBL
Homeodomain-interacting protein kinase 4 Kinase Kd 5.44 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 5 Kinase Kd 7.10 CHEMBL
Serine/threonine-protein kinase DCLK2 Kinase Kd 6.43 CHEMBL
Misshapen-like kinase 1 Kinase Kd 5.36 CHEMBL
Interleukin-1 receptor-associated kinase 4 Kinase Kd 5.44 CHEMBL
Insulin receptor-related protein Kinase Kd 6.22 CHEMBL
Mast/stem cell growth factor receptor Kit Kinase Kd 6.10 CHEMBL
BMP-2-inducible protein kinase Kinase Kd 6.13 CHEMBL
Insulin-like growth factor 1 receptor Kinase Kd 6.11 CHEMBL
Ephrin type-A receptor 6 Kinase Kd 7.19 CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 2 Kinase Kd 5.82 CHEMBL
Aurora kinase B Kinase Kd 7.12 CHEMBL
STE20-like serine/threonine-protein kinase Kinase Kd 7.74 CHEMBL
Bone morphogenetic protein receptor type-1B Kinase Kd 6.64 CHEMBL
Macrophage-stimulating protein receptor Kinase Kd 7.60 CHEMBL
Non-receptor tyrosine-protein kinase TYK2 Kinase Kd 6.68 CHEMBL
Interleukin-1 receptor-associated kinase 1 Kinase Kd 7.31 CHEMBL
Serine/threonine-protein kinase 4 Kinase Kd 6.24 CHEMBL
Ephrin type-A receptor 7 Kinase Kd 6.33 CHEMBL
Serine/threonine-protein kinase 3 Kinase Kd 6 CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit beta Kinase Kd 5.26 CHEMBL
Serine/threonine-protein kinase Nek9 Kinase Kd 6.10 CHEMBL
Serine/threonine-protein kinase TAO2 Kinase Kd 6.05 CHEMBL
Tyrosine-protein kinase Lyn Kinase Kd 6.03 CHEMBL
5'-AMP-activated protein kinase catalytic subunit alpha-1 Kinase Kd 5.62 CHEMBL
Cytoplasmic tyrosine-protein kinase BMX Kinase Kd 5.44 CHEMBL
Ephrin type-A receptor 5 Kinase Kd 6 CHEMBL
LIM domain kinase 1 Kinase Kd 6.08 CHEMBL
NPM/ALK (Nucleophosmin/ALK tyrosine kinase receptor) Kinase IC50 7.29 CHEMBL
Serine/threonine-protein kinase ULK2 Kinase Kd 5.80 CHEMBL
Ephrin type-A receptor 4 Kinase Kd 6.44 CHEMBL
Ephrin type-B receptor 1 Kinase Kd 6.92 CHEMBL
Activated CDC42 kinase 1 Kinase Kd 6.12 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 3 Kinase Kd 7.12 CHEMBL
Dual specificity testis-specific protein kinase 1 Kinase Kd 6.42 CHEMBL
Focal adhesion kinase 1 Kinase Kd 6.51 CHEMBL
NT-3 growth factor receptor Kinase Kd 7.09 CHEMBL
Tyrosine-protein kinase ZAP-70 Kinase Kd 5.38 CHEMBL
Activin receptor type-1 Kinase Kd 6.36 CHEMBL
Interleukin-1 receptor-associated kinase 3 Kinase Kd 7.51 CHEMBL
G protein-coupled receptor kinase 4 Kinase Kd 5.38 CHEMBL
Mitogen-activated protein kinase kinase kinase 2 Kinase Kd 7.14 CHEMBL
Serine/threonine-protein kinase ULK3 Kinase Kd 5.17 CHEMBL
Abelson tyrosine-protein kinase 2 Kinase Kd 6.34 CHEMBL
Serine/threonine-protein kinase 26 Kinase Kd 5.55 CHEMBL
Protein-tyrosine kinase 2-beta Kinase Kd 6.72 CHEMBL
Tyrosine-protein kinase Blk Kinase Kd 6.96 CHEMBL
Angiopoietin-1 receptor Kinase Kd 6.57 CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit epsilon Kinase Kd 6.15 CHEMBL
Peripheral plasma membrane protein CASK Kinase Kd 6.85 CHEMBL
Dual serine/threonine and tyrosine protein kinase Kinase Kd 6.35 CHEMBL
Proto-oncogene tyrosine-protein kinase ROS Kinase Kd 8.39 CHEMBL
Ephrin type-B receptor 6 Kinase Kd 8.22 CHEMBL
Serine/threonine-protein kinase SIK2 Kinase Kd 6.70 CHEMBL
Serine/threonine-protein kinase TAO3 Kinase Kd 6.31 CHEMBL
Mitogen-activated protein kinase kinase kinase 1 Kinase Kd 5.96 CHEMBL
Cyclin-dependent kinase 7 Kinase Kd 6.48 CHEMBL
Rho-associated protein kinase 2 Kinase Kd 5.48 CHEMBL
Tyrosine-protein kinase Fyn Kinase Kd 5.89 CHEMBL
Macrophage colony-stimulating factor 1 receptor Kinase Kd 6.68 CHEMBL
Uncharacterized serine/threonine-protein kinase SBK3 Kinase Kd 6.62 CHEMBL
Activin receptor type-1B Kinase Kd 6.07 CHEMBL
Tyrosine-protein kinase receptor Tie-1 Kinase Kd 6.96 CHEMBL
TGF-beta receptor type-1 Kinase Kd 6 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase Kd 5.89 CHEMBL
Myotonin-protein kinase Kinase Kd 5.85 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase Kd 6.29 CHEMBL
Tyrosine-protein kinase receptor TYRO3 Kinase Kd 6.10 CHEMBL
Tyrosine-protein kinase Fes/Fps Kinase Kd 6.35 CHEMBL
Tyrosine-protein kinase Lck Kinase Kd 7.52 CHEMBL
Leukocyte tyrosine kinase receptor Kinase Kd 7.92 CHEMBL
Mitogen-activated protein kinase kinase kinase 19 Kinase Kd 6.01 CHEMBL
Tyrosine-protein kinase receptor UFO Kinase Kd 8.11 CHEMBL
BDNF/NT-3 growth factors receptor Kinase Kd 7.43 CHEMBL
NUAK family SNF1-like kinase 2 Kinase Kd 6.92 CHEMBL
SRSF protein kinase 3 Kinase Kd 5.09 CHEMBL
Tyrosine-protein kinase TXK Kinase Kd 6.07 CHEMBL
LIM domain kinase 2 Kinase Kd 6.16 CHEMBL
Mitogen-activated protein kinase kinase kinase 12 Kinase Kd 6.77 CHEMBL
Receptor-interacting serine/threonine-protein kinase 1 Kinase Kd 5.80 CHEMBL
Phosphatidylinositol 4-phosphate 5-kinase type-1 alpha Kinase Kd 5.49 CHEMBL
Mitogen-activated protein kinase kinase kinase 3 Kinase Kd 6.96 CHEMBL
Cyclin-dependent kinase 11A Kinase Kd 6.38 CHEMBL
Serine/threonine-protein kinase RIO1 Kinase Kd 5.21 CHEMBL
Ribosomal protein S6 kinase beta-1 Kinase Kd 6.19 CHEMBL
Serine/threonine-protein kinase ULK1 Kinase Kd 6 CHEMBL
Receptor-interacting serine/threonine-protein kinase 4 Kinase Kd 5.68 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2 Kinase Kd 7.10 CHEMBL
Tyrosine-protein kinase Mer Kinase Kd 8.44 CHEMBL
Mitogen-activated protein kinase 7 Kinase Kd 6.29 CHEMBL
Receptor-type tyrosine-protein kinase FLT3 Kinase Kd 6.68 CHEMBL
Non-receptor tyrosine-protein kinase TNK1 Kinase Kd 6.49 CHEMBL
Cyclin-dependent kinase-like 2 Kinase Kd 5.68 CHEMBL
Angiopoietin-1 receptor Kinase IC50 6.35 CHEMBL
Tyrosine-protein kinase ABL1 Kinase IC50 5.94 CHEMBL
Macrophage-stimulating protein receptor Kinase IC50 7.10 CHEMBL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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