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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 1932 641571-10-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • nilotinib hydrochloride hydrate
  • nilotinib
  • tasigna
  • nilotinib hydrochloride monohydrate
Nilotinib is an inhibitor of the BCR-ABL kinase. Nilotinib binds to and stabilizes the inactive conformation of the kinase domain of ABL protein. In vitro, nilotinib inhibited BCR-ABL mediated proliferation of murine leukemic cell lines and human cell lines derived from patients with Ph+ CML. Under the conditions of the assays, nilotinib was able to overcome imatinib resistance resulting from BCR-ABL kinase mutations, in 32 out of 33 mutations tested. In vivo, nilotinib reduced the tumor size in a murine BCR-ABL xenograft model.
  • Molecular weight: 529.53
  • Formula: C28H22F3N7O
  • CLOGP: 5.69
  • LIPINSKI: 2
  • HAC: 8
  • HDO: 2
  • TPSA: 97.62
  • ALOGS: -5.42
  • ROTB: 7

  • 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 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 4 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 21.58 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 30 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Oct. 29, 2007 FDA NOVARTIS

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
Cytogenetic analysis abnormal 479.23 15.45 96 19443 480 46666043
Chronic myeloid leukaemia 471.62 15.45 124 19415 2334 46664189
Peripheral arterial occlusive disease 333.93 15.45 104 19435 3648 46662875
Electrocardiogram QT prolonged 305.01 15.45 216 19323 51109 46615414
Blast crisis in myelogenous leukaemia 212.41 15.45 48 19491 460 46666063
Second primary malignancy 199.15 15.45 82 19457 6502 46660021
Rash 174.24 15.45 428 19111 356084 46310439
Chronic myeloid leukaemia transformation 174.17 15.45 32 19507 90 46666433
Lipase increased 165.64 15.45 78 19461 8525 46657998
Pleural effusion 122.67 15.45 162 19377 82790 46583733
Drug resistance 121.69 15.45 81 19458 17287 46649236
Peripheral artery stenosis 117.18 15.45 30 19509 505 46666018
Intermittent claudication 115.29 15.45 39 19500 1781 46664742
Bone pain 104.67 15.45 113 19426 46777 46619746
Philadelphia chromosome positive 102.29 15.45 24 19515 275 46666248
Blood bilirubin increased 95.55 15.45 93 19446 34091 46632432
Malignant neoplasm progression 94.72 15.45 126 19413 64800 46601723
Myocardial infarction 88.98 15.45 152 19387 97376 46569147
Off label use 86.35 15.45 26 19513 379815 46286708
Thrombocytopenia 73.48 15.45 163 19376 126418 46540105
Chronic myeloid leukaemia recurrent 72.92 15.45 17 19522 189 46666334
Pruritus 70.38 15.45 242 19297 242110 46424413
Platelet count decreased 68.72 15.45 138 19401 99886 46566637
Acute lymphocytic leukaemia recurrent 66.43 15.45 27 19512 2068 46664455
Rheumatoid arthritis 65.40 15.45 11 19528 240204 46426319
Pancreatitis 62.57 15.45 84 19455 43543 46622980
Angina pectoris 60.55 15.45 65 19474 26710 46639813
Myalgia 59.95 15.45 148 19391 122940 46543583
Normal newborn 59.74 15.45 35 19504 5966 46660557
White blood cell count increased 58.68 15.45 82 19457 44137 46622386
Labelled drug-food interaction medication error 58.38 15.45 11 19528 37 46666486
Arteriosclerosis 57.78 15.45 41 19498 9692 46656831
Peripheral vascular disorder 54.65 15.45 33 19506 5944 46660579
Platelet count increased 54.28 15.45 47 19492 14827 46651696
Acute myocardial infarction 51.26 15.45 65 19474 31859 46634664
Death 49.36 15.45 273 19266 335275 46331248
Therapeutic response delayed 47.92 15.45 15 19524 534 46665989
Alopecia 46.90 15.45 162 19377 162252 46504271
Pericardial effusion 45.83 15.45 55 19484 25488 46641035
Exposure via father 45.43 15.45 13 19526 338 46666185
Condition aggravated 43.86 15.45 24 19515 245028 46421495
Blast cell crisis 43.38 15.45 9 19530 55 46666468
Hyperbilirubinaemia 42.23 15.45 35 19504 10403 46656120
Drug hypersensitivity 42.03 15.45 25 19514 243800 46422723
Exposure via partner 40.91 15.45 10 19529 138 46666385
Splenomegaly 40.27 15.45 33 19506 9655 46656868
Pancytopenia 40.03 15.45 101 19438 84957 46581566
Blood glucose increased 39.79 15.45 91 19448 71922 46594601
Polymerase chain reaction positive 39.43 15.45 8 19531 43 46666480
Arterial disorder 37.47 15.45 15 19524 1104 46665419
Haematotoxicity 36.14 15.45 27 19512 6906 46659617
Carotid artery stenosis 36.14 15.45 24 19515 5096 46661427
Dry skin 36.13 15.45 63 19476 40953 46625570
Gastrointestinal stromal tumour 33.79 15.45 14 19525 1126 46665397
Xanthelasma 32.68 15.45 7 19532 51 46666472
Leukaemia recurrent 31.92 15.45 14 19525 1295 46665228
Thrombocytosis 31.85 15.45 22 19517 4980 46661543
Drug ineffective 31.31 15.45 162 19377 677676 45988847
Food interaction 31.16 15.45 11 19528 571 46665952
Anaemia 31.03 15.45 198 19341 255581 46410942
Toxicity to various agents 30.84 15.45 26 19513 211740 46454783
Basophil count increased 30.80 15.45 12 19527 822 46665701
Acute kidney injury 30.78 15.45 32 19507 235823 46430700
Myocardial ischaemia 30.68 15.45 32 19507 12717 46653806
Gene mutation identification test positive 30.53 15.45 8 19531 148 46666375
Amylase increased 30.12 15.45 22 19517 5437 46661086
Bone marrow failure 29.35 15.45 48 19491 29621 46636902
Cerebrovascular accident 29.31 15.45 101 19438 100938 46565585
Skin disorder 29.09 15.45 41 19498 22222 46644301
Abdominal pain upper 28.94 15.45 129 19410 145176 46521347
Hypotension 28.75 15.45 33 19506 232556 46433967
Joint swelling 28.64 15.45 17 19522 166056 46500467
Coronary artery disease 28.64 15.45 51 19488 33701 46632822
Palpitations 28.31 15.45 96 19443 95163 46571360
Concomitant disease progression 28.03 15.45 15 19524 2147 46664376
Arterial occlusive disease 27.97 15.45 20 19519 4784 46661739
Peripheral artery occlusion 27.21 15.45 12 19527 1125 46665398
Acute coronary syndrome 27.07 15.45 27 19512 10177 46656346
Peripheral ischaemia 26.59 15.45 19 19520 4540 46661983
Diabetes mellitus 26.26 15.45 62 19477 50003 46616520
Hypercholesterolaemia 26.07 15.45 28 19511 11502 46655021
Cytopenia 25.26 15.45 23 19516 7745 46658778
Pregnancy of partner 23.64 15.45 5 19534 34 46666489
Keratosis pilaris 23.64 15.45 5 19534 34 46666489
Neoplasm malignant 23.22 15.45 38 19501 23461 46643062
Overdose 23.06 15.45 7 19532 101972 46564551
Collateral circulation 22.41 15.45 4 19535 9 46666514
Concomitant disease aggravated 21.18 15.45 21 19518 7861 46658662
Pain in extremity 20.94 15.45 182 19357 258498 46408025
Haemolytic transfusion reaction 20.31 15.45 4 19535 18 46666505
Blast cell count increased 20.00 15.45 7 19532 354 46666169
Gamma-glutamyltransferase increased 19.65 15.45 42 19497 31698 46634825
Gangrene 19.52 15.45 16 19523 4679 46661844
Hyponatraemia 19.49 15.45 9 19530 101323 46565200
Therapeutic response decreased 19.01 15.45 50 19489 43095 46623428
Pancreatic enzymes increased 18.81 15.45 8 19531 687 46665836
Blood lactate dehydrogenase increased 18.72 15.45 32 19507 20468 46646055
Gene mutation 18.38 15.45 9 19530 1071 46665452
Abdominal pain 18.17 15.45 161 19378 229870 46436653
Urinary tract infection 18.03 15.45 41 19498 220225 46446298
Alanine aminotransferase increased 17.95 15.45 79 19460 88372 46578151
Fall 17.87 15.45 74 19465 329023 46337500
Muscle spasms 17.24 15.45 99 19440 123014 46543509
Arthropathy 17.11 15.45 7 19532 84693 46581830
Myelofibrosis 17.07 15.45 9 19530 1250 46665273
Oxygen saturation decreased 17.05 15.45 4 19535 69160 46597363
Growth disorder 17.05 15.45 3 19536 6 46666517
Chest pain 16.92 15.45 129 19410 176195 46490328
Hyperglycaemia 16.85 15.45 42 19497 35029 46631494
Hepatic infection 16.77 15.45 6 19533 324 46666199
Angiopathy 16.63 15.45 14 19525 4249 46662274
Dyspepsia 16.11 15.45 64 19475 68408 46598115
Delivery 15.73 15.45 7 19532 670 46665853
Thromboangiitis obliterans 15.72 15.45 3 19536 11 46666512
Leukocytosis 15.70 15.45 32 19507 23366 46643157
Systemic lupus erythematosus 15.61 15.45 4 19535 65176 46601347
Vertebral artery stenosis 15.58 15.45 4 19535 68 46666455
Musculoskeletal stiffness 15.56 15.45 11 19528 97982 46568541

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
Chronic myeloid leukaemia 545.79 14.69 157 20917 2420 29928984
Cytogenetic analysis abnormal 357.91 14.69 78 20996 339 29931065
Blast crisis in myelogenous leukaemia 354.77 14.69 81 20993 453 29930951
Electrocardiogram QT prolonged 349.94 14.69 250 20824 35585 29895819
Second primary malignancy 326.47 14.69 134 20940 6222 29925182
Peripheral arterial occlusive disease 321.16 14.69 125 20949 5043 29926361
Intermittent claudication 205.05 14.69 72 21002 2162 29929242
Angina pectoris 181.79 14.69 157 20917 29361 29902043
Pleural effusion 179.50 14.69 240 20834 73826 29857578
Rash 159.21 14.69 389 20685 191500 29739904
Lipase increased 158.45 14.69 90 20984 8586 29922818
Drug resistance 157.30 14.69 123 20951 20010 29911394
Chronic myeloid leukaemia transformation 134.51 14.69 30 21044 148 29931256
Myocardial infarction 126.36 14.69 275 20799 125350 29806054
Coronary artery stenosis 116.30 14.69 75 20999 8995 29922409
Death 115.57 14.69 526 20548 356757 29574647
Pancreatitis 90.93 14.69 120 20954 36370 29895034
Blood bilirubin increased 89.01 14.69 119 20955 36517 29894887
Off label use 87.75 14.69 33 21041 249257 29682147
Peripheral artery stenosis 83.85 14.69 29 21045 831 29930573
Arterial disorder 82.38 14.69 31 21043 1137 29930267
Chronic myeloid leukaemia recurrent 81.78 14.69 19 21055 116 29931288
Philadelphia chromosome positive 81.26 14.69 21 21053 210 29931194
Malignant neoplasm progression 80.35 14.69 165 20909 72122 29859282
Acute kidney injury 74.36 14.69 51 21023 273791 29657613
Drug intolerance 72.50 14.69 121 20953 45170 29886234
Toxicity to various agents 72.10 14.69 18 21056 177165 29754239
Peripheral vascular disorder 71.48 14.69 45 21029 5174 29926230
Platelet count decreased 67.20 14.69 195 20879 105934 29825470
White blood cell count increased 66.19 14.69 108 20966 39565 29891839
Coronary artery disease 65.58 14.69 122 20952 49590 29881814
Hypotension 63.42 14.69 31 21043 200534 29730870
Acute myocardial infarction 60.17 14.69 122 20952 52817 29878587
Concomitant disease aggravated 59.86 14.69 40 21034 5089 29926315
Abdominal pain upper 59.40 14.69 134 20940 62417 29868987
Myocardial ischaemia 56.08 14.69 65 21009 17252 29914152
Chest pain 55.19 14.69 195 20879 117432 29813972
Carotid artery stenosis 53.61 14.69 36 21038 4618 29926786
Blast cell crisis 51.27 14.69 12 21062 76 29931328
Gene mutation identification test positive 50.90 14.69 14 21060 181 29931223
Acute coronary syndrome 50.89 14.69 55 21019 13518 29917886
Arterial stenosis 50.15 14.69 22 21052 1203 29930201
Gastrointestinal stromal tumour 48.79 14.69 22 21052 1284 29930120
Concomitant disease progression 48.31 14.69 27 21047 2493 29928911
Splenomegaly 47.72 14.69 53 21021 13427 29917977
Pruritus 47.13 14.69 186 20888 118018 29813386
Peripheral artery occlusion 46.65 14.69 22 21052 1424 29929980
Thrombocytopenia 46.33 14.69 205 20869 136839 29794565
Exposure via father 45.99 14.69 12 21062 125 29931279
Gene mutation 44.49 14.69 18 21056 803 29930601
Bone pain 43.45 14.69 60 21014 18966 29912438
Polymerase chain reaction positive 39.84 14.69 10 21064 88 29931316
Arteriosclerosis 39.05 14.69 43 21031 10790 29920614
Overdose 37.44 14.69 7 21067 84330 29847074
Confusional state 36.64 14.69 25 21049 134809 29796595
Labelled drug-food interaction medication error 34.99 14.69 8 21066 45 29931359
Drug interaction 34.04 14.69 55 21019 199513 29731891
Myalgia 33.27 14.69 124 20950 76543 29854861
Peripheral ischaemia 32.04 14.69 28 21046 5306 29926098
Infarction 31.87 14.69 21 21053 2609 29928795
Amylase increased 31.79 14.69 29 21045 5812 29925592
Angina unstable 31.43 14.69 41 21033 12269 29919135
Fall 31.12 14.69 50 21024 181822 29749582
Hyperglycaemia 30.73 14.69 73 21001 35127 29896277
Blast cells present 29.90 14.69 9 21065 163 29931241
Pain in extremity 28.65 14.69 153 20921 110068 29821336
Blood glucose increased 27.94 14.69 101 20973 61429 29869975
Cerebral artery stenosis 27.86 14.69 10 21064 320 29931084
Paternal exposure during pregnancy 27.36 14.69 5 21069 6 29931398
Dehydration 27.28 14.69 28 21046 123511 29807893
Hypercholesterolaemia 27.13 14.69 30 21044 7562 29923842
Cerebral infarction 25.56 14.69 57 21017 26316 29905088
Condition aggravated 25.41 14.69 36 21038 137830 29793574
Chloroma 24.93 14.69 10 21064 436 29930968
Acute lymphocytic leukaemia 24.47 14.69 19 21055 3053 29928351
Pericardial effusion 24.31 14.69 49 21025 21095 29910309
Hallucination 24.21 14.69 3 21071 49056 29882348
Drug hypersensitivity 24.14 14.69 9 21065 68510 29862894
Ischaemia 23.74 14.69 22 21052 4499 29926905
Clonal evolution 23.73 14.69 7 21067 118 29931286
Somnolence 23.64 14.69 20 21054 96743 29834661
Tremor 23.23 14.69 12 21062 75351 29856053
Fatigue 22.14 14.69 332 20742 320341 29611063
Cerebrovascular accident 21.76 14.69 116 20958 83361 29848043
Arteritis 21.48 14.69 8 21066 285 29931119
Gangrene 21.46 14.69 21 21053 4593 29926811
Necrosis 21.21 14.69 22 21052 5157 29926247
Agitation 20.99 14.69 6 21068 54067 29877337
Carotid arteriosclerosis 20.82 14.69 11 21063 908 29930496
Loss of therapeutic response 20.69 14.69 6 21068 95 29931309
Gamma-glutamyltransferase increased 20.55 14.69 56 21018 29294 29902110
Abdominal pain 20.33 14.69 164 20910 135490 29795914
Cytopenia 20.30 14.69 27 21047 8229 29923175
Hyponatraemia 20.27 14.69 11 21063 67191 29864213
Leukaemia recurrent 20.23 14.69 13 21061 1548 29929856
Chest discomfort 20.08 14.69 74 21000 45406 29885998
Gelatinous transformation of the bone marrow 19.76 14.69 4 21070 11 29931393
Therapeutic response decreased 19.65 14.69 49 21025 24300 29907104
Product blister packaging issue 19.44 14.69 5 21069 49 29931355
Intentional overdose 19.38 14.69 3 21071 41478 29889926
Leukocytosis 19.20 14.69 45 21029 21457 29909947
Acne 18.95 14.69 28 21046 9408 29921996
Pancreatic toxicity 18.78 14.69 3 21071 0 29931404
Central nervous system leukaemia 18.59 14.69 7 21067 257 29931147
Atrial fibrillation 18.59 14.69 135 20939 107989 29823415
Acquired gene mutation 18.42 14.69 11 21063 1150 29930254
Diabetes mellitus 18.38 14.69 68 21006 41797 29889607
B-cell small lymphocytic lymphoma 18.35 14.69 6 21068 144 29931260
Muscle spasms 18.21 14.69 92 20982 64746 29866658
Arterial occlusive disease 18.07 14.69 18 21056 4022 29927382
Rectosigmoid cancer 17.82 14.69 6 21068 158 29931246
Hepatic infection 17.63 14.69 8 21066 474 29930930
Seizure 16.88 14.69 27 21047 98448 29832956
Coronary artery occlusion 16.76 14.69 29 21045 11128 29920276
Delirium 16.74 14.69 4 21070 40627 29890777
Neoplasm malignant 16.70 14.69 38 21036 17776 29913628
Basophil count increased 16.27 14.69 7 21067 365 29931039
Lethargy 16.06 14.69 4 21070 39515 29891889
Alopecia 15.77 14.69 39 21035 19236 29912168
Plasma cell myeloma 15.76 14.69 9 21065 53453 29877951
Nipple swelling 15.49 14.69 3 21071 6 29931398
Febrile neutropenia 14.99 14.69 33 21041 106660 29824744

Pharmacologic Action:

SourceCodeDescription
ATC L01EA03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
BCR-ABL tyrosine kinase inhibitors
FDA MoA N0000175076 Protein Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
CHEBI has role CHEBI:35610 cytostatic
CHEBI has role CHEBI:38637 tyrosine kinase inhibitors
CHEBI has role CHEBI:149553 anti-coronaviral agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Chronic phase chronic myeloid leukemia indication 413847001
Philadelphia Chromosome Positive Chronic Myelocytic Leukemia indication
Chronic Myelocytic Leukemia Accelerated Phase indication
Hypophosphatemia contraindication 4996001
Hypocalcemia contraindication 5291005
Hypercholesterolemia contraindication 13644009
Hyperkalemia contraindication 14140009
Hyperbilirubinemia contraindication 14783006 DOID:2741
Torsades de pointes contraindication 31722008
Hypertensive disorder contraindication 38341003 DOID:10763
Hypokalemia contraindication 43339004
Gastrectomy contraindication 53442002
Diabetes mellitus contraindication 73211009 DOID:9351
Pancreatitis contraindication 75694006 DOID:4989
Hyperglycemia contraindication 80394007 DOID:4195
Hyponatremia contraindication 89627008
Prolonged QT interval contraindication 111975006
Liver function tests abnormal contraindication 166603001
Hypomagnesemia contraindication 190855004
Disease of liver contraindication 235856003 DOID:409
Anemia contraindication 271737000 DOID:2355
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Neutropenic disorder contraindication 303011007 DOID:1227
Breastfeeding (mother) contraindication 413712001
Congenital long QT syndrome contraindication 442917000
Elevated Serum Lipase contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.89 acidic
pKa2 6.03 Basic
pKa3 3.97 Basic
pKa4 2.2 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 50MG BASE TASIGNULL NOVARTIS N022068 March 22, 2018 RX CAPSULE ORAL March 22, 2021 NEW PATIENT POPULATION
EQ 50MG BASE TASIGNULL NOVARTIS N022068 March 22, 2018 RX CAPSULE ORAL Sept. 22, 2021 PEDIATRIC EXCLUSIVITY
EQ 50MG BASE TASIGNULL NOVARTIS N022068 March 22, 2018 RX CAPSULE ORAL March 22, 2025 TREATMENT OF PEDIATRIC PATIENTS GREATER THAN OR EQUAL TO 1 YEAR OF AGE WITH CHRONIC PHASE PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA WITH RESISTANCE OR INTOLERANCE TO PRIOR TYROSINE-KINULLSE INHIBITOR THERAPY
EQ 50MG BASE TASIGNULL NOVARTIS N022068 March 22, 2018 RX CAPSULE ORAL March 22, 2025 TREATMENT OF PEDIATRIC PATIENTS GREATER THAN OR EQUAL TO 1 YEAR OF AGE WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA (PH+CML) IN CHRONIC PHASE
EQ 50MG BASE TASIGNULL NOVARTIS N022068 March 22, 2018 RX CAPSULE ORAL Sept. 22, 2025 PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Tyrosine-protein kinase ABL1 Kinase INHIBITOR Kd 8.44 CHEMBL CHEMBL
Cytoplasmic tyrosine-protein kinase BMX Kinase Ki 5.32 PDSP
Fibroblast growth factor receptor 2 Kinase Ki 5.14 PDSP
Fibroblast growth factor receptor 1 Kinase Ki 5.10 PDSP
Tyrosine-protein kinase JAK2 Kinase Ki 5.07 PDSP
Mitogen-activated protein kinase 10 Kinase Kd 5.70 CHEMBL
Receptor-type tyrosine-protein kinase FLT3 Kinase Kd 4.40 CHEMBL
Carbonic anhydrase 2 Enzyme Ki 8.39 CHEMBL
Mitogen-activated protein kinase 9 Kinase Kd 5.24 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase Kd 5.72 CHEMBL
Platelet-derived growth factor receptor alpha Kinase Kd 7.13 CHEMBL
Ephrin type-B receptor 4 Kinase Kd 6.14 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5 Kinase Kd 6.72 CHEMBL
Mitogen-activated protein kinase kinase kinase MLT Kinase Kd 7.96 CHEMBL
RAF proto-oncogene serine/threonine-protein kinase Kinase Kd 5.41 CHEMBL
Ephrin type-A receptor 1 Kinase Kd 6.23 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1 Kinase Kd 6.05 CHEMBL
Serine/threonine-protein kinase B-raf Kinase Kd 6.24 CHEMBL
Tyrosine-protein kinase Fgr Kinase Kd 6.49 CHEMBL
Tyrosine-protein kinase FRK Kinase Kd 7.07 CHEMBL
Dual specificity protein kinase CLK1 Kinase Kd 5.68 CHEMBL
Ephrin type-A receptor 8 Kinase Kd 7.43 CHEMBL
Ephrin type-A receptor 2 Kinase Kd 6.64 CHEMBL
Ephrin type-A receptor 3 Kinase Kd 6.96 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 5.17 CHEMBL
Tyrosine-protein kinase Yes Kinase Kd 5.96 CHEMBL
Tyrosine-protein kinase CSK Kinase Kd 5.62 CHEMBL
Serine/threonine-protein kinase TAO1 Kinase Kd 5.33 CHEMBL
Serine/threonine-protein kinase TNNI3K Kinase Kd 6.44 CHEMBL
Tyrosine-protein kinase HCK Kinase Kd 6.41 CHEMBL
Platelet-derived growth factor receptor beta Kinase Kd 7.80 CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma Kinase Kd 5.06 CHEMBL
Mast/stem cell growth factor receptor Kit Kinase Kd 7.77 CHEMBL
Ephrin type-A receptor 6 Kinase Kd 6.19 CHEMBL
Dual specificity protein kinase CLK4 Kinase Kd 5.15 CHEMBL
Tyrosine-protein kinase Lyn Kinase Kd 7 CHEMBL
Ephrin type-A receptor 5 Kinase Kd 5.72 CHEMBL
Ephrin type-A receptor 4 Kinase Kd 6.48 CHEMBL
Ephrin type-B receptor 1 Kinase Kd 5.89 CHEMBL
NT-3 growth factor receptor Kinase Kd 6.22 CHEMBL
Carbonic anhydrase 12 Enzyme Ki 6.52 CHEMBL
Serine/threonine-protein kinase MRCK beta Kinase Kd 6.04 CHEMBL
Abelson tyrosine-protein kinase 2 Kinase Kd 7.59 CHEMBL
Carbonic anhydrase 4 Enzyme Ki 6.35 CHEMBL
Tyrosine-protein kinase Blk Kinase Kd 6.30 CHEMBL
Angiopoietin-1 receptor Kinase Kd 6 CHEMBL
Ephrin type-B receptor 6 Kinase Kd 6.30 CHEMBL
Mitogen-activated protein kinase 8 Kinase Kd 6.35 CHEMBL
Serine/threonine-protein kinase TAO3 Kinase Kd 5.77 CHEMBL
Tyrosine-protein kinase Fyn Kinase Kd 5.80 CHEMBL
Macrophage colony-stimulating factor 1 receptor Kinase Kd 7.35 CHEMBL
Discoidin domain-containing receptor 2 Kinase Kd 8.22 CHEMBL
Tyrosine-protein kinase receptor Tie-1 Kinase Kd 6 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase Kd 6.06 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase Kd 8.96 CHEMBL
Tyrosine-protein kinase Lck Kinase Kd 7.33 CHEMBL
Carbonic anhydrase 3 Enzyme Ki 6.35 CHEMBL
BDNF/NT-3 growth factors receptor Kinase Kd 6.31 CHEMBL
Ephrin type-B receptor 2 Kinase Kd 6.19 CHEMBL
Mitogen-activated protein kinase 11 Kinase Kd 7.44 CHEMBL
Carbonic anhydrase 5A, mitochondrial Enzyme Ki 5.26 CHEMBL
Ephrin type-B receptor 3 Kinase Kd 6 CHEMBL
Carbonic anhydrase 14 Enzyme Ki 6.65 CHEMBL
Carbonic anhydrase 7 Enzyme Ki 7 CHEMBL
Carbonic anhydrase 9 Enzyme Ki 7.38 CHEMBL
Carbonic anhydrase 1 Enzyme Ki 7.53 CHEMBL
Carbonic anhydrase 5B, mitochondrial Enzyme Ki 4.83 CHEMBL
Carbonic anhydrase 6 Enzyme Ki 6.34 CHEMBL
Mitogen-activated protein kinase 14 Kinase Kd 6.34 CHEMBL
Insulin receptor Kinase Ki 5.39 PDSP
Bcr/Abl fusion protein Kinase IC50 9.48 CHEMBL
Carbonic anhydrase 13 Enzyme Ki 5.33 CHEMBL
Calcium-dependent protein kinase 1 Kinase Kd 6.10 CHEMBL
Carbonic anhydrase 15 Enzyme Ki 7.10 CHEMBL

External reference:

IDSource
4026964 VUID
N0000176124 NUI
D06413 KEGG_DRUG
923288-90-8 SECONDARY_CAS_RN
4026964 VANDF
C1721377 UMLSCUI
CHEBI:52172 CHEBI
NIL PDB_CHEM_ID
CHEMBL255863 ChEMBL_ID
CHEMBL1201740 ChEMBL_ID
DB04868 DRUGBANK_ID
C498826 MESH_SUPPLEMENTAL_RECORD_UI
5697 IUPHAR_LIGAND_ID
8654 INN_ID
F41401512X UNII
644241 PUBCHEM_CID
662281 RXNORM
127956 MMSL
24733 MMSL
d07057 MMSL
012401 NDDF
427941004 SNOMEDCT_US
428468009 SNOMEDCT_US
438943005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Tasigna HUMAN PRESCRIPTION DRUG LABEL 1 0078-0526 CAPSULE 200 mg ORAL NDA 32 sections
Tasigna HUMAN PRESCRIPTION DRUG LABEL 1 0078-0592 CAPSULE 150 mg ORAL NDA 32 sections
Tasigna HUMAN PRESCRIPTION DRUG LABEL 1 0078-0951 CAPSULE 50 mg ORAL NDA 32 sections