gilteritinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5306 1254053-43-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • gilteritinib fumarate
  • gilteritinib
  • xospata
  • ASP2215
Gilteritinib is a small molecule that inhibits multiple receptor tyrosine kinases, including FMS-like tyrosine kinase 3 (FLT3). Gilteritinib demonstrated the ability to inhibit FLT3 receptor signaling and proliferation in cells exogenously expressing FLT3 including FLT3-ITD, tyrosine kinase domain mutations (TKD) FLT3-D835Y and FLT3-ITD-D835Y, and it induced apoptosis in leukemic cells expressing FLT3-ITD.
  • Molecular weight: 552.72
  • Formula: C29H44N8O3
  • CLOGP: 2.48
  • LIPINSKI: 2
  • HAC: 11
  • HDO: 3
  • TPSA: 121.11
  • ALOGS: -4.39
  • ROTB: 9
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.12 g O

ADMET properties:

PropertyValueReference
S (Water solubility) 0.09 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.454 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 5.534 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 11.641 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 8.128 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 21.990 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 41.280 % High 1
herg hERG pIC50 5.016 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1.799 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 14.488 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 16.670 % High 1
kinase-safety-class AAK1,ABL1,ABL2,ACVR2A,ACVR2B,ACVRL1,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,BTK,CAMK1,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK14,CDK16,CDK19,CDK2,CDK3,CDK4,CDK5,CDK6,CDK7,CDK9,CHEK1,CHEK2,CLK1,CLK2,CLK4,CSF1R,CSK,CSNK2A2,DDR1,DYRK1A,DYRK1B,DYRK2,DYRK3,EGFR,EIF2AK3,EPHA2,EPHB1,EPHB4,ERBB2,ERBB4,FGFR1,FGFR4,FLT1,FLT3,FLT4,FYN,GAK,GRK1,GRK2,GSK3A,GSK3B,HASPIN,HIPK2,IGF1R,IKBKB,INSR,INSRR,IRAK1,IRAK3,IRAK4,ITK,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K19,MAP3K2,MAP3K21,MAP3K3,MAP3K7,MAP3K9,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK15,MAPK3,MAPK7,MAPK8,MAPK9,MARK1,MARK2,MARK3,MARK4,MELK,MET,MINK1,MKNK1,MKNK2,MST1R,MTOR,MYLK,NTRK1,NTRK2,NTRK3,NUAK1,PAK1,PAK2,PAK4,PAK5,PDGFRB,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CD,PIK3CG,PIM1,PIM2,PIM3,PLK1,PLK2,PLK3,PLK4,PRKAA1,PRKAA2,PRKACA,PRKCA,PRKCD,PRKCI,PRKCZ,PRKD1,PRKDC,PRKG1,PTK2,RET,RIPK1,RIPK3,ROCK1,ROCK2,RPS6KA1,SGK1,SIK2,SIK3,SRC,STK10,STK16,STK17A,STK3,STK33,STK4,SYK,TBK1,TEK,TGFBR1,TNIK,TNK1,TTK,TYRO3,UHMK1,ULK1,ULK2,YES1,ZAP70 179
kinase-selectivity-class AAK1,ABL2,ACVR2B,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,CAMK2A,CAMK2B,CAMK2D,CDK1,CDK16,CDK2,CDK4,CDK6,CDK7,CDK9,CHEK1,CLK2,CLK4,CSF1R,CSK,DDR1,DYRK1A,DYRK1B,DYRK3,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,ERBB4,FGFR1,FLT1,FLT3,FLT4,FYN,GAK,GSK3B,HIPK2,IGF1R,INSR,IRAK1,IRAK3,IRAK4,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP2K3,MAP2K6,MAP3K10,MAP3K11,MAP3K14,MAP3K19,MAP3K2,MAP3K21,MAP3K7,MAP3K9,MAP4K1,MAP4K3,MAP4K5,MAPK1,MAPK7,MARK1,MARK2,MARK3,MARK4,MELK,MET,MINK1,MKNK2,MST1R,MYLK,NTRK1,NTRK3,NUAK1,PAK2,PAK4,PAK5,PDGFRB,PDK1,PDK4,PDPK1,PIM3,PLK4,PRKAA1,PRKAA2,PRKCD,PTK2,RET,RIPK3,ROCK1,ROCK2,SIK2,SIK3,SRC,STK10,STK16,STK33,STK4,SYK,TEK,TNIK,TNK1,TTK,TYRO3,ULK1,ULK2,YES1 119
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 13.032 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 17.620 High 1
mh-clint Mouse hepatocyte intrinsic clearance 10.471 High 1
mppb Mouse plasma protein binding (% unbound) 16 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 70.795 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 30.100 % High 1
rat-kpuu-brain Rat brain Kpuu 0.013 % High 1
rh-clint Rat hepatocyte intrinsic clearance 4.027 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 32.470 % High 1
rppb Rat plasma protein binding (% unbound) 17.180 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 257.040 uM High 1

Approvals:

DateAgencyCompanyOrphan
Sept. 21, 2018 PMDA Astellas Pharma Inc
Nov. 28, 2018 FDA ASTELLAS
Oct. 24, 2019 EMA ASTELLAS PHARMA EUROPE BV

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
Febrile neutropenia 402.26 49.29 182 4289 158167 90465809
Myelosuppression 304.05 49.29 110 4361 53481 90570495
Acute myeloid leukaemia recurrent 248.00 49.29 48 4423 2009 90621967
Differentiation syndrome 197.58 49.29 37 4434 1294 90622682
Cytopenia 195.91 49.29 60 4411 17389 90606587
Hepatic function abnormal 193.28 49.29 76 4395 46212 90577764
Platelet count decreased 182.65 49.29 102 4369 136867 90487109
Neutrophil count decreased 170.74 49.29 79 4392 71453 90552523
Acute myeloid leukaemia 153.84 49.29 52 4419 20588 90603388
Blast cell count increased 146.72 49.29 25 4446 504 90623472
Electrocardiogram QT prolonged 124.63 49.29 64 4407 72392 90551584
Acute febrile neutrophilic dermatosis 104.29 49.29 26 4445 3519 90620457
Graft versus host disease 95.59 49.29 29 4442 8115 90615861
Pancytopenia 80.47 49.29 58 4413 120205 90503771
Left atrial hypertrophy 80.40 49.29 11 4460 44 90623932
Pneumonia adenoviral 77.67 49.29 13 4458 234 90623742
Product use issue 75.67 49.29 87 4384 329832 90294144
Septic shock 73.85 49.29 48 4423 84112 90539864
Adenoviral hepatitis 69.83 49.29 13 4458 439 90623537
Blood lactate dehydrogenase increased 69.20 49.29 31 4440 25901 90598075
Thrombocytopenia 67.26 49.29 66 4405 208659 90415317
Death 64.85 49.29 95 4376 456456 90167520
Sepsis 61.95 49.29 59 4412 179755 90444221
Pneumonia 58.54 49.29 109 4362 637950 89986026
Off label use 55.56 49.29 148 4323 1102104 89521872
Electrocardiogram PR shortened 55.28 49.29 11 4460 530 90623446
Acute graft versus host disease in skin 51.82 49.29 16 4455 4740 90619236
Bacteraemia 51.14 49.29 24 4447 22276 90601700
Atypical pneumonia 50.52 49.29 16 4455 5148 90618828

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
Myelosuppression 377.50 36.15 141 3783 40320 42577091
Acute myeloid leukaemia 208.66 36.15 78 3846 22178 42595233
Febrile neutropenia 199.57 36.15 152 3772 185551 42431860
Platelet count decreased 160.93 36.15 119 3805 138462 42478949
Acute myeloid leukaemia recurrent 138.87 36.15 37 3887 3475 42613936
Hepatic function abnormal 134.60 36.15 74 3850 51493 42565918
Differentiation syndrome 131.24 36.15 31 3893 1782 42615629
Cytopenia 113.42 36.15 47 3877 17450 42599961
Product use issue 107.45 36.15 74 3850 76677 42540734
Pneumonia 95.82 36.15 152 3772 421997 42195414
Blast cell count increased 79.19 36.15 19 3905 1166 42616245
Neutrophil count decreased 63.47 36.15 50 3874 63365 42554046
Liver disorder 59.59 36.15 40 3884 39604 42577807
Graft versus host disease 55.46 36.15 26 3898 12899 42604512
Infection 54.50 36.15 59 3865 112009 42505402
Electrocardiogram QT prolonged 48.36 36.15 38 3886 47907 42569504
Bacteraemia 46.83 36.15 29 3895 25011 42592400
Blood disorder 44.68 36.15 16 3908 4001 42613410
Graft versus host disease in skin 44.16 36.15 17 3907 5195 42612216
Underdose 43.60 36.15 24 3900 16642 42600769
Pyrexia 41.34 36.15 103 3821 393939 42223472
Sepsis 41.06 36.15 69 3855 199265 42418146
Thrombocytopenia 40.71 36.15 67 3857 190212 42427199
Off label use 37.66 36.15 136 3788 638199 41979212
Aspiration bone marrow abnormal 37.35 36.15 7 3917 128 42617283

FDA Adverse Event Reporting System (Geriatric)

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
Myelosuppression 727.35 37.58 271 8051 94069 110486908
Febrile neutropenia 566.75 37.58 330 7992 316437 110264540
Acute myeloid leukaemia recurrent 390.46 37.58 88 8234 5051 110575926
Platelet count decreased 379.42 37.58 228 8094 230215 110350762
Hepatic function abnormal 352.18 37.58 159 8163 89136 110491841
Acute myeloid leukaemia 350.61 37.58 125 8197 37985 110542992
Cytopenia 285.35 37.58 101 8221 30015 110550962
Differentiation syndrome 241.39 37.58 54 8268 2990 110577987
Neutrophil count decreased 228.35 37.58 131 8191 120810 110460167
Blast cell count increased 197.34 37.58 41 8281 1596 110579381
Graft versus host disease 193.12 37.58 67 8255 18739 110562238
Electrocardiogram QT prolonged 163.86 37.58 102 8220 108858 110472119
Pneumonia 163.45 37.58 259 8063 876455 109704522
Product use issue 139.83 37.58 143 8179 311552 110269425
Acute febrile neutrophilic dermatosis 106.58 37.58 31 8291 4905 110576072
Liver disorder 102.16 37.58 85 8237 142158 110438819
Sepsis 98.40 37.58 122 8200 327224 110253753
Bacteraemia 96.48 37.58 52 8270 42338 110538639
Blood lactate dehydrogenase increased 94.29 37.58 52 8270 44282 110536695
Thrombocytopenia 93.78 37.58 123 8199 348762 110232215
Pyrexia 93.45 37.58 207 8115 898058 109682919
Blood creatine phosphokinase increased 79.62 37.58 56 8266 73021 110507956
Pancytopenia 79.36 37.58 88 8234 209525 110371452
Graft versus host disease in skin 79.30 37.58 28 8294 8226 110572751
Left atrial hypertrophy 73.26 37.58 11 8311 58 110580919
Pneumonia fungal 70.06 37.58 30 8292 14724 110566253
Infection 69.74 37.58 109 8213 362091 110218886
Bronchopulmonary aspergillosis 68.97 37.58 37 8285 29826 110551151
Off label use 67.75 37.58 256 8066 1499929 109081048
Bone marrow failure 66.91 37.58 46 8276 57802 110523175
White blood cell count decreased 64.86 37.58 83 8239 229307 110351670
Neutropenia 64.29 37.58 107 8215 374513 110206464
Underdose 63.01 37.58 46 8276 63508 110517469
Septic shock 62.83 37.58 68 8254 157460 110423517
Anaemia 59.97 37.58 129 8193 546957 110034020
Pneumonia adenoviral 59.83 37.58 13 8309 627 110580350
Graft versus host disease in gastrointestinal tract 58.87 37.58 23 8299 8945 110572032
Acute graft versus host disease in skin 58.23 37.58 24 8298 10716 110570261
Electrocardiogram PR shortened 54.23 37.58 11 8311 379 110580598
Adenoviral hepatitis 53.91 37.58 13 8309 999 110579978
Pain 51.23 37.58 6 8316 954949 109626028
WT1 gene mutation 48.54 37.58 6 8316 3 110580974
Graft versus host disease in liver 46.73 37.58 14 8308 2451 110578526
Enterococcal bacteraemia 46.18 37.58 16 8306 4445 110576532
Death 43.38 37.58 133 8189 698736 109882241
Atypical pneumonia 40.70 37.58 17 8305 7845 110573132
Blast cells present 39.20 37.58 10 8312 968 110580009
Amylase increased 39.04 37.58 19 8303 12500 110568477
Fatigue 38.44 37.58 22 8300 1215936 109365041
Adenovirus infection 38.28 37.58 18 8304 10976 110570001
Dyspnoea 37.98 37.58 18 8304 1106854 109474123
Leukaemic infiltration extramedullary 37.71 37.58 8 8314 344 110580633
Chronic graft versus host disease 37.68 37.58 17 8305 9440 110571537

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EX13 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Other protein kinase inhibitors
MeSH PA D000092004 Tyrosine Kinase Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:62434 EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
CHEBI has role CHEBI:68495 apoptosis inducer
CHEBI has role CHEBI:231911 renoprotective agent

Related Drugs by ATC class:

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

DiseaseRelationSNOMED_IDDOID
Acute myeloid leukemia, disease indication 91861009




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.78 acidic
pKa2 8.76 Basic
pKa3 5.0 Basic
pKa4 4.38 Basic
pKa5 3.81 Basic
pKa6 0.35 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 40MG BASE XOSPATA ASTELLAS N211349 Nov. 28, 2018 RX TABLET ORAL 9487491 July 28, 2030 TREATMENT OF ACUTE MYELOID LEUKEMIA (AML)

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Receptor-type tyrosine-protein kinase FLT3 Kinase INHIBITOR IC50 8.30 SCIENTIFIC LITERATURE DRUG LABEL
Ribosyldihydronicotinamide dehydrogenase [quinone] Enzyme Kd 5.77 CHEMBL
Platelet-derived growth factor receptor beta Kinase Kd 6.29 CHEMBL
Epidermal growth factor receptor Kinase Kd 5.46 CHEMBL
ADP/ATP translocase 2 Enzyme Kd 6.35 CHEMBL
ADP/ATP translocase 3 Enzyme Kd 6.30 CHEMBL
Tyrosine-protein kinase Yes Kinase Kd 6.35 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase IC50 8.47 CHEMBL
Ribosomal protein S6 kinase alpha-3 Kinase Kd 5.58 CHEMBL
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform Kinase Kd 7.32 CHEMBL
Myosin light chain kinase, smooth muscle Kinase Kd 6.73 CHEMBL
Mitogen-activated protein kinase 8 Kinase Kd 6.13 CHEMBL
Tyrosine-protein kinase HCK Kinase Kd 5.80 CHEMBL
Mitogen-activated protein kinase 10 Kinase Kd 6.29 CHEMBL
High affinity nerve growth factor receptor Kinase INHIBITOR IC50 8.96 IUPHAR
Protein kinase C alpha type Kinase Kd 6.23 CHEMBL
Tyrosine-protein kinase SYK Kinase Kd 5.39 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit delta Kinase Kd 6.68 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit gamma Kinase Kd 6.77 CHEMBL
AP2-associated protein kinase 1 Kinase Kd 7.60 CHEMBL
Serine/threonine-protein kinase Nek2 Kinase Kd 6.61 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 6.83 CHEMBL
Tyrosine-protein kinase Fer Kinase Kd 6.73 CHEMBL
Serine/threonine-protein kinase PLK4 Kinase Kd 7.75 CHEMBL
Serine/threonine-protein kinase 16 Kinase Kd 6.53 CHEMBL
Aurora kinase A Kinase Kd 6.74 CHEMBL
ALK tyrosine kinase receptor Kinase IC50 8.82 CHEMBL
BMP-2-inducible protein kinase Kinase Kd 7.34 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 5 Kinase Kd 5.51 CHEMBL
Cyclin-G-associated kinase Kinase Kd 8.05 CHEMBL
Receptor-interacting serine/threonine-protein kinase 2 Kinase Kd 6.32 CHEMBL
Activated CDC42 kinase 1 Kinase Kd 5.50 CHEMBL
Ephrin type-A receptor 7 Kinase Kd 5.53 CHEMBL
STE20-like serine/threonine-protein kinase Kinase Kd 7.17 CHEMBL
Mitogen-activated protein kinase 9 Kinase Kd 6.37 CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 2 Kinase Kd 5.58 CHEMBL
Activin receptor type-1 Kinase Kd 7.41 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 1 Kinase Kd 5.56 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 2 Kinase Kd 6.30 CHEMBL
Tyrosine-protein kinase receptor UFO Kinase INHIBITOR IC50 9.10 IUPHAR
Non-receptor tyrosine-protein kinase TNK1 Kinase Kd 7.41 CHEMBL
Protein-tyrosine kinase 2-beta Kinase Kd 6.29 CHEMBL
Casein kinase II subunit alpha' Kinase Kd 6.02 CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit epsilon Kinase Kd 5.83 CHEMBL
Serine/threonine-protein kinase 26 Kinase Kd 5.94 CHEMBL
Interleukin-1 receptor-associated kinase 3 Kinase Kd 8.15 CHEMBL
Serine/threonine-protein kinase LATS1 Kinase Kd 6.66 CHEMBL
Leukocyte tyrosine kinase receptor Kinase INHIBITOR IC50 9.70 IUPHAR
Mitogen-activated protein kinase kinase kinase kinase 1 Kinase Kd 6.97 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 3 Kinase Kd 6.22 CHEMBL
Bone morphogenetic protein receptor type-1A Kinase Kd 6.92 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 4 Kinase Kd 6.70 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 6 Kinase Kd 5.72 CHEMBL
Tyrosine-protein kinase Mer Kinase INHIBITOR IC50 8.52 IUPHAR
Calcium/calmodulin-dependent protein kinase type IV Kinase Kd 6.38 CHEMBL
Mitogen-activated protein kinase kinase kinase 11 Kinase Kd 6.22 CHEMBL
Serine/threonine-protein kinase 24 Kinase Kd 6.64 CHEMBL
Citron Rho-interacting kinase Kinase Kd 5.63 CHEMBL
Mitogen-activated protein kinase 15 Kinase Kd 6.58 CHEMBL
Proto-oncogene tyrosine-protein kinase ROS Kinase IC50 8.72 CHEMBL
Ribosomal protein S6 kinase alpha-1 Kinase Kd 5.46 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2 Kinase Kd 6.61 CHEMBL
Interleukin-1 receptor-associated kinase 4 Kinase Kd 5.75 CHEMBL
Cyclin-dependent kinase 4 Kinase Kd 5.71 CHEMBL
Ephrin type-B receptor 6 Kinase Kd 6.62 CHEMBL
Mitogen-activated protein kinase kinase kinase 2 Kinase Kd 6.27 CHEMBL
Serine/threonine-protein kinase ULK3 Kinase Kd 8.22 CHEMBL
Bone morphogenetic protein receptor type-1B Kinase Kd 6.24 CHEMBL
Serine/threonine-protein kinase Nek3 Kinase Kd 5.55 CHEMBL
Serine/threonine-protein kinase TAO2 Kinase Kd 5.68 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5 Kinase Kd 5.69 CHEMBL
Receptor-interacting serine/threonine-protein kinase 3 Kinase Kd 5.88 CHEMBL
Mitotic checkpoint serine/threonine-protein kinase BUB1 Kinase Kd 6.72 CHEMBL
U5 small nuclear ribonucleoprotein 200 kDa helicase Enzyme Kd 5.86 CHEMBL
Cytochrome c1, heme protein, mitochondrial Enzyme Kd 6.70 CHEMBL
Macrophage-stimulating protein receptor Kinase Kd 6.09 CHEMBL
Elongation factor Tu, mitochondrial Enzyme Kd 6.33 CHEMBL
Actin-related protein 3 Structural Kd 5.26 CHEMBL
GTP-binding nuclear protein Ran Enzyme Kd 6.12 CHEMBL
Delta(24)-sterol reductase Enzyme Kd 6.37 CHEMBL
Rab-like protein 3 Enzyme Kd 5.32 CHEMBL
Uncharacterized protein FLJ45252 Unclassified Kd 7.96 CHEMBL
Uncharacterized aarF domain-containing protein kinase 1 Kinase Kd 6.82 CHEMBL
TP53-regulating kinase Kinase Kd 5.57 CHEMBL
Long-chain-fatty-acid--CoA ligase 5 Enzyme Kd 6.68 CHEMBL
Multifunctional protein ADE2 Enzyme Kd 5.26 CHEMBL

External reference:

IDSource
66D92MGC8M UNII
1254053-84-3 SECONDARY_CAS_RN
4038030 VANDF
C3896940 UMLSCUI
CHEBI:145372 CHEBI
C6F PDB_CHEM_ID
CHEMBL3301622 ChEMBL_ID
49803313 PUBCHEM_CID
DB12141 DRUGBANK_ID
CHEMBL3301603 ChEMBL_ID
D10709 KEGG_DRUG
10048 INN_ID
C000609080 MESH_SUPPLEMENTAL_RECORD_UI
8708 IUPHAR_LIGAND_ID
1217167001 SNOMEDCT_US
782974005 SNOMEDCT_US
782987004 SNOMEDCT_US
299484 MMSL
35657 MMSL
35755 MMSL
d09076 MMSL
017854 NDDF
017855 NDDF
2105806 RXNORM
66D92MGC8M INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Xospata HUMAN PRESCRIPTION DRUG LABEL 1 0469-1425 TABLET 40 mg ORAL NDA 28 sections