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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5280 901119-35-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tavlesse
  • fostamatinib
  • fostamatinib disodium
  • tavalisse
  • R935788
  • R788
Fostamatinib is a tyrosine kinase inhibitor with demonstrated activity against spleen tyrosine kinase (SYK). The major metabolite of fostamatinib, R406, inhibits signal transduction of Fc-activating receptors and B-cell receptor. The fostamatinib metabolite R406 reduces antibody-mediated destruction of platelets.
  • Molecular weight: 580.47
  • Formula: C23H26FN6O9P
  • CLOGP: 1.56
  • LIPINSKI: 2
  • HAC: 15
  • HDO: 4
  • TPSA: 186.72
  • ALOGS: -4.05
  • ROTB: 10
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.20 g O

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -1.340 High 0.92
caco2-efflux Caco-2 efflux ratio (BA/AB) 68.234 High 0.92
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 0.372 10^-6 cm/s High 0.92
dh-clint Dog hepatocyte intrinsic clearance 13.183 uL/min/10^6 cells High 0.92
dppb Dog plasma protein binding (% unbound) 1.280 % High 0.92
fcs-ppb Fetal calf serum protein binding (% unbound) 1.300 % High 0.92
herg hERG pIC50 4.535 pIC50 High 0.92
hh-clint Human hepatocyte intrinsic clearance 32.434 uL/min/10^6 cells High 0.92
hlm-clint Human liver microsomal intrinsic clearance 3.673 uL/min/mg protein High 0.92
hppb Human plasma protein binding (% unbound) 0.480 % High 0.92
kinase-safety-class AAK1,ABL1,ABL2,ACVR1B,ACVR2A,ACVR2B,ACVRL1,AKT2,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,CHUK,CLK1,CLK2,CLK4,CSF1R,CSK,CSNK1G1,CSNK1G2,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,MAP2K4,MAP2K6,MAP2K7,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K19,MAP3K2,MAP3K21,MAP3K3,MAP3K7,MAP3K9,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK12,MAPK3,MAPK7,MAPK8,MAPK9,MARK1,MARK2,MARK3,MARK4,MELK,MET,MINK1,MKNK2,MST1R,MTOR,NTRK1,NTRK2,NTRK3,NUAK1,PAK1,PAK2,PAK4,PAK5,PDGFRB,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM2,PIM3,PLK1,PLK2,PLK3,PLK4,PRKAA1,PRKAA2,PRKACA,PRKCD,PRKCI,PRKCZ,PRKD1,PRKDC,PTK2,PTK6,RET,RIPK1,RIPK3,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 182
kinase-selectivity-class AAK1,ABL2,ACVR2A,ACVR2B,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,CAMK2A,CAMK2B,CAMK2D,CDK1,CDK16,CDK2,CDK3,CDK4,CDK6,CDK7,CDK9,CHEK1,CLK2,CLK4,CSF1R,DDR1,DYRK1B,DYRK2,EGFR,EPHA2,EPHB4,ERBB2,ERBB4,FGFR1,FLT1,FLT3,FLT4,FYN,GAK,GRK2,GSK3A,GSK3B,IGF1R,IKBKB,INSR,IRAK1,IRAK3,IRAK4,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP2K3,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP3K9,MAP4K1,MAP4K3,MAP4K5,MAPK1,MAPK12,MAPK7,MAPK8,MARK1,MARK2,MARK4,MET,MINK1,MKNK2,MST1R,NTRK1,NTRK3,NUAK1,PAK1,PAK4,PAK5,PDGFRB,PDK1,PDK4,PIK3CA,PIK3CD,PIK3CG,PRKAA1,PRKAA2,PRKCD,PRKDC,PTK2,RET,RIPK3,SIK2,SIK3,SRC,STK10,STK16,STK33,SYK,TEK,TNIK,TTK,TYRO3,ULK1,ULK2,YES1,ZAP70 116
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 4.121 High 0.92
mh-clint Mouse hepatocyte intrinsic clearance 118.304 High 0.92
mppb Mouse plasma protein binding (% unbound) 1.440 High 0.92
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 0.484 High 0.92
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 1.590 % High 0.92
rh-clint Rat hepatocyte intrinsic clearance 102.329 uL/min/10^6 cells High 0.92
rh-fuinc Rat hepatocyte fraction unbound in incubation 56.920 % High 0.92
rppb Rat plasma protein binding (% unbound) 0.470 % High 0.92
solubility-dd Solubility at pH 7.4 in DMSO 924.698 uM High 0.92

Approvals:

DateAgencyCompanyOrphan
Jan. 9, 2020 EMA Instituto Grifols S.A.
April 17, 2018 FDA RIGEL PHARMS INC
Dec. 23, 2022 PMDA Kissei Pharmaceutical Co., Ltd.

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
Platelet count 164.16 43.94 18 1254 34 90627141
Platelet count decreased 163.80 43.94 64 1208 136905 90490270
Diarrhoea 84.88 43.94 83 1189 939107 89688068
Hepatic function abnormal 70.83 43.94 26 1246 46262 90580913
Product prescribing issue 68.61 43.94 17 1255 7962 90619213
Hospitalisation 65.21 43.94 33 1239 128067 90499108
Death 55.76 43.94 48 1224 456503 90170672
Platelet count increased 44.43 43.94 15 1257 20844 90606331

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
Platelet count 112.91 49.81 13 795 30 42620497
Platelet count decreased 110.47 49.81 53 755 138528 42481999
Death 55.26 49.81 55 753 471130 42149397

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
Platelet count decreased 130.76 37.29 63 1432 230380 110357424
Platelet count 107.37 37.29 13 1482 79 110587725
Hepatic function abnormal 94.74 37.29 38 1457 89257 110498547
Diarrhoea 82.57 37.29 88 1407 1139417 109448387
Death 66.96 37.29 63 1432 698806 109888998
Hypertension 60.65 37.29 52 1443 510032 110077772
Platelet count increased 57.04 37.29 19 1476 26315 110561489
Platelet count abnormal 47.54 37.29 12 1483 6270 110581534
Splenectomy 44.21 37.29 8 1487 862 110586942
Product prescribing issue 39.12 37.29 12 1483 12760 110575044

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC B02BX09 BLOOD AND BLOOD FORMING ORGANS
ANTIHEMORRHAGICS
VITAMIN K AND OTHER HEMOSTATICS
Other systemic hemostatics
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:33281 antimicrobial agent
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:35842 antirheumatic drug
CHEBI has role CHEBI:75835 anti-anaemic agent
CHEBI has role CHEBI:233423 antifibrotic agent

Related Drugs by ATC class:

B02BX Other systemic hemostatics 10 drugs
avatrombopagcarbazochromeconcizumabeltrombopagemicizumabetamsylatefitusiranlusutrombopagmarstacimab-hncqromiplostim

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

DiseaseRelationSNOMED_IDDOID
Immune thrombocytopenia indication 2897005 DOID:1587
Chronic idiopathic thrombocytopenic purpura indication 13172003




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 1.54 acidic
pKa2 6.59 acidic
pKa3 5.0 Basic
pKa4 4.34 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 100MG BASE TAVALISSE RIGEL PHARMS N209299 April 17, 2018 RX TABLET ORAL 9266912 Jan. 19, 2026 TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 150MG BASE TAVALISSE RIGEL PHARMS N209299 April 17, 2018 RX TABLET ORAL 9266912 Jan. 19, 2026 TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 100MG BASE TAVALISSE RIGEL PHARMS N209299 April 17, 2018 RX TABLET ORAL 7538108 March 28, 2026 TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 150MG BASE TAVALISSE RIGEL PHARMS N209299 April 17, 2018 RX TABLET ORAL 7538108 March 28, 2026 TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 100MG BASE TAVALISSE RIGEL PHARMS N209299 April 17, 2018 RX TABLET ORAL 7989448 June 12, 2026 TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 150MG BASE TAVALISSE RIGEL PHARMS N209299 April 17, 2018 RX TABLET ORAL 7989448 June 12, 2026 TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 100MG BASE TAVALISSE RIGEL PHARMS N209299 April 17, 2018 RX TABLET ORAL 8163902 June 17, 2026 TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 100MG BASE TAVALISSE RIGEL PHARMS N209299 April 17, 2018 RX TABLET ORAL 8912170 June 17, 2026 TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 100MG BASE TAVALISSE RIGEL PHARMS N209299 April 17, 2018 RX TABLET ORAL 9283238 June 17, 2026 TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 150MG BASE TAVALISSE RIGEL PHARMS N209299 April 17, 2018 RX TABLET ORAL 8163902 June 17, 2026 TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 150MG BASE TAVALISSE RIGEL PHARMS N209299 April 17, 2018 RX TABLET ORAL 8912170 June 17, 2026 TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 150MG BASE TAVALISSE RIGEL PHARMS N209299 April 17, 2018 RX TABLET ORAL 9283238 June 17, 2026 TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 100MG BASE TAVALISSE RIGEL PHARMS N209299 April 17, 2018 RX TABLET ORAL 8951504 July 27, 2032 TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 150MG BASE TAVALISSE RIGEL PHARMS N209299 April 17, 2018 RX TABLET ORAL 8951504 July 27, 2032 TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Tyrosine-protein kinase SYK Kinase INHIBITOR IC50 7.39 SCIENTIFIC LITERATURE DRUG LABEL
Macrophage-stimulating protein receptor Kinase Kd 6.33 CHEMBL
ATP-binding cassette sub-family G member 2 Transporter IC50 7.30 CHEMBL
Platelet-derived growth factor receptor beta Kinase Kd 8.48 CHEMBL
Tyrosine-protein kinase ABL1 Kinase Kd 6.77 CHEMBL
Mast/stem cell growth factor receptor Kit Kinase Kd 8.60 CHEMBL
Epidermal growth factor receptor Kinase Kd 7.21 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase Kd 8.08 CHEMBL
Tyrosine-protein kinase Lck Kinase Kd 7.52 CHEMBL
Tyrosine-protein kinase Yes Kinase Kd 7.46 CHEMBL
Tyrosine-protein kinase Fyn Kinase Kd 7.55 CHEMBL
Ephrin type-A receptor 2 Kinase Kd 6.85 CHEMBL
RAF proto-oncogene serine/threonine-protein kinase Kinase Kd 6.08 CHEMBL
Serine/threonine-protein kinase B-raf Kinase Kd 6.62 CHEMBL
Receptor-type tyrosine-protein kinase FLT3 Kinase Kd 9.43 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase INHIBITOR IC50 8.30 IUPHAR
Vascular endothelial growth factor receptor 1 Kinase Kd 7.80 CHEMBL
Vascular endothelial growth factor receptor 2 Kinase Kd 7.16 CHEMBL
Vascular endothelial growth factor receptor 3 Kinase Kd 8.04 CHEMBL
Macrophage colony-stimulating factor 1 receptor Kinase Kd 7.51 CHEMBL
Platelet-derived growth factor receptor alpha Kinase Kd 7.22 CHEMBL
Ribosomal protein S6 kinase alpha-3 Kinase Kd 5.10 CHEMBL
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform Kinase Kd 6.03 CHEMBL
Insulin-like growth factor 1 receptor Kinase Kd 5.89 CHEMBL
Myosin light chain kinase, smooth muscle Kinase Kd 5.19 CHEMBL
Insulin receptor Kinase Kd 5.96 CHEMBL
Death-associated protein kinase 3 Kinase Kd 7.89 CHEMBL
Calcium/calmodulin-dependent protein kinase type 1 Kinase Kd 6.64 CHEMBL
Mitogen-activated protein kinase 8 Kinase EC50 8 CHEMBL
Fibroblast growth factor receptor 3 Kinase Kd 7.25 CHEMBL
Rho-associated protein kinase 1 Kinase Kd 6.23 CHEMBL
Focal adhesion kinase 1 Kinase Kd 6.60 CHEMBL
Tyrosine-protein kinase HCK Kinase Kd 6.82 CHEMBL
Tyrosine-protein kinase JAK1 Kinase Kd 7.68 CHEMBL
Serine/threonine-protein kinase PLK1 Kinase Kd 6.08 CHEMBL
Receptor tyrosine-protein kinase erbB-4 Kinase Kd 6.22 CHEMBL
Mitogen-activated protein kinase 10 Kinase Kd 7.43 CHEMBL
Death-associated protein kinase 2 Kinase Kd 7.21 CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform Kinase Kd 5.38 CHEMBL
High affinity nerve growth factor receptor Kinase Kd 6.77 CHEMBL
Protein kinase C delta type Kinase Kd 5.39 CHEMBL
cAMP-dependent protein kinase catalytic subunit beta Kinase Kd 6.29 CHEMBL
Tyrosine-protein kinase JAK2 Kinase Kd 8.46 CHEMBL
Rho-associated protein kinase 2 Kinase Kd 6.25 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit delta Kinase Kd 5.52 CHEMBL
Tyrosine-protein kinase CSK Kinase Kd 6.80 CHEMBL
Angiopoietin-1 receptor Kinase Kd 6.51 CHEMBL
Ephrin type-A receptor 8 Kinase Kd 5.89 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit gamma Kinase Kd 6.04 CHEMBL
AP2-associated protein kinase 1 Kinase Kd 6.39 CHEMBL
Serine/threonine-protein kinase MARK2 Kinase Kd 6.55 CHEMBL
Hepatocyte growth factor receptor Kinase Kd 6.64 CHEMBL
Tyrosine-protein kinase Lyn Kinase Kd 7.58 CHEMBL
Cytoplasmic tyrosine-protein kinase BMX Kinase Kd 6.75 CHEMBL
Serine/threonine-protein kinase Nek2 Kinase Kd 6.58 CHEMBL
LIM domain kinase 1 Kinase Kd 6.21 CHEMBL
5'-AMP-activated protein kinase catalytic subunit alpha-1 Kinase Kd 6.52 CHEMBL
Fibroblast growth factor receptor 1 Kinase Kd 7.36 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit alpha Kinase Kd 5.96 CHEMBL
Serine/threonine-protein kinase 17B Kinase Kd 8.04 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 7.16 CHEMBL
Tyrosine-protein kinase Fer Kinase Kd 6.89 CHEMBL
Serine/threonine-protein kinase PLK4 Kinase Kd 8.38 CHEMBL
Aurora kinase C Kinase Kd 7.39 CHEMBL
Serine/threonine-protein kinase 16 Kinase Kd 8.77 CHEMBL
Dual specificity protein kinase TTK Kinase Kd 5.96 CHEMBL
Abelson tyrosine-protein kinase 2 Kinase Kd 6.14 CHEMBL
Ephrin type-A receptor 5 Kinase Kd 6.07 CHEMBL
Ephrin type-A receptor 4 Kinase Kd 6.82 CHEMBL
Fibroblast growth factor receptor 2 Kinase Kd 7.14 CHEMBL
Serine/threonine-protein kinase N1 Kinase Kd 6.18 CHEMBL
Serine/threonine-protein kinase 17A Kinase Kd 7.50 CHEMBL
Ephrin type-A receptor 6 Kinase Kd 6.92 CHEMBL
TRAF2 and NCK-interacting protein kinase Kinase Kd 5.89 CHEMBL
Mitogen-activated protein kinase 12 Kinase Kd 6.41 CHEMBL
Tyrosine-protein kinase Fgr Kinase Kd 7.48 CHEMBL
Aurora kinase A Kinase Kd 7.53 CHEMBL
ALK tyrosine kinase receptor Kinase Kd 6.62 CHEMBL
Serine/threonine-protein kinase 36 Kinase Kd 6.64 CHEMBL
Ephrin type-A receptor 3 Kinase Kd 6.44 CHEMBL
BMP-2-inducible protein kinase Kinase Kd 5.72 CHEMBL
Tyrosine-protein kinase FRK Kinase Kd 7.17 CHEMBL
Dual specificity protein kinase CLK1 Kinase Kd 5.92 CHEMBL
Dual specificity protein kinase CLK2 Kinase Kd 5.80 CHEMBL
Dual specificity protein kinase CLK3 Kinase Kd 5.72 CHEMBL
Mitogen-activated protein kinase kinase kinase 4 Kinase Kd 6.08 CHEMBL
Cyclin-G-associated kinase Kinase Kd 6.60 CHEMBL
Glycogen synthase kinase-3 beta Kinase Kd 6.92 CHEMBL
Receptor-interacting serine/threonine-protein kinase 2 Kinase Kd 6.01 CHEMBL
Ephrin type-B receptor 1 Kinase Kd 6.41 CHEMBL
Calcium/calmodulin-dependent protein kinase type 1D Kinase Kd 6.70 CHEMBL
Activated CDC42 kinase 1 Kinase Kd 7.16 CHEMBL
Ephrin type-A receptor 7 Kinase Kd 7.41 CHEMBL
Ribosomal protein S6 kinase alpha-5 Kinase Kd 6.82 CHEMBL
STE20-like serine/threonine-protein kinase Kinase Kd 7.48 CHEMBL
Dual specificity protein kinase CLK4 Kinase Kd 6.69 CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 2 Kinase Kd 6.89 CHEMBL
Mitogen-activated protein kinase 9 Kinase EC50 8 CHEMBL
MAP/microtubule affinity-regulating kinase 3 Kinase Kd 5.72 CHEMBL
Calcium/calmodulin-dependent protein kinase type 1G Kinase Kd 6.34 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase Kd 8.03 CHEMBL
Ephrin type-B receptor 4 Kinase Kd 6.22 CHEMBL
Testis-specific serine/threonine-protein kinase 1 Kinase Kd 6 CHEMBL
Activin receptor type-1B Kinase Kd 5.96 CHEMBL
Activin receptor type-1 Kinase Kd 5.32 CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit beta Kinase Kd 7.15 CHEMBL
3-phosphoinositide-dependent protein kinase 1 Kinase Kd 6.92 CHEMBL
TGF-beta receptor type-2 Kinase Kd 6.48 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 1 Kinase Kd 6.50 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 2 Kinase Kd 6.14 CHEMBL
Tyrosine-protein kinase ITK/TSK Kinase Kd 6.40 CHEMBL
Tyrosine-protein kinase ZAP-70 Kinase Kd 7.68 CHEMBL
Glycogen synthase kinase-3 alpha Kinase Kd 5.60 CHEMBL
Protein-tyrosine kinase 6 Kinase Kd 6.44 CHEMBL
Tyrosine-protein kinase BTK Kinase Kd 6.72 CHEMBL
Tyrosine-protein kinase Tec Kinase Kd 5.80 CHEMBL
Tyrosine-protein kinase receptor UFO Kinase Kd 7.09 CHEMBL
BDNF/NT-3 growth factors receptor Kinase Kd 6.05 CHEMBL
Tyrosine-protein kinase receptor TYRO3 Kinase Kd 5.72 CHEMBL
Ephrin type-B receptor 2 Kinase Kd 6.06 CHEMBL
Cyclin-dependent kinase 7 Kinase Kd 5.11 CHEMBL
Serine/threonine-protein kinase N2 Kinase Kd 5.58 CHEMBL
Serine/threonine-protein kinase DCLK3 Kinase Kd 6.22 CHEMBL
Serine/threonine-protein kinase 3 Kinase Kd 5.52 CHEMBL
NUAK family SNF1-like kinase 2 Kinase Kd 7.19 CHEMBL
Non-receptor tyrosine-protein kinase TNK1 Kinase Kd 7.60 CHEMBL
Non-receptor tyrosine-protein kinase TYK2 Kinase Kd 6.72 CHEMBL
Mitogen-activated protein kinase 13 Kinase Kd 6.16 CHEMBL
Serine/threonine-protein kinase Chk1 Kinase Kd 5.60 CHEMBL
Serine/threonine-protein kinase PAK 3 Kinase Kd 6.16 CHEMBL
Cyclin-dependent kinase 17 Kinase Kd 6.48 CHEMBL
Phosphatidylinositol 4-phosphate 5-kinase type-1 alpha Kinase Kd 5.72 CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 beta Kinase Kd 5.92 CHEMBL
Myosin light chain kinase family member 4 Kinase Kd 6.09 CHEMBL
Wee1-like protein kinase Kinase Kd 6.05 CHEMBL
Serine/threonine-protein kinase 25 Kinase Kd 5.04 CHEMBL
Protein-tyrosine kinase 2-beta Kinase Kd 7.54 CHEMBL
Serine/threonine-protein kinase RIO1 Kinase Kd 6.47 CHEMBL
Tyrosine-protein kinase receptor Tie-1 Kinase Kd 7.12 CHEMBL
Serine/threonine-protein kinase tousled-like 1 Kinase Kd 6.31 CHEMBL
Serine/threonine-protein kinase tousled-like 2 Kinase Kd 6.42 CHEMBL
NT-3 growth factor receptor Kinase Kd 6.24 CHEMBL
Tyrosine-protein kinase TXK Kinase Kd 6.85 CHEMBL
Casein kinase II subunit alpha Kinase Kd 7.19 CHEMBL
Casein kinase II subunit alpha' Kinase Kd 7.85 CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit epsilon Kinase Kd 7.89 CHEMBL
LIM domain kinase 2 Kinase Kd 5.85 CHEMBL
Serine/threonine-protein kinase STK11 Kinase Kd 5.47 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 3 Kinase Kd 7 CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 1 Kinase Kd 6.64 CHEMBL
Serine/threonine-protein kinase Nek7 Kinase Kd 7.96 CHEMBL
Eukaryotic translation initiation factor 2-alpha kinase 4 Kinase Kd 8.48 CHEMBL
Insulin receptor-related protein Kinase Kd 5.34 CHEMBL
Interleukin-1 receptor-associated kinase 3 Kinase Kd 7.96 CHEMBL
Serine/threonine-protein kinase RIO3 Kinase Kd 6.68 CHEMBL
Serine/threonine-protein kinase SIK2 Kinase Kd 7.11 CHEMBL
SRSF protein kinase 1 Kinase Kd 6.23 CHEMBL
Serine/threonine-protein kinase 33 Kinase Kd 6.01 CHEMBL
Serine/threonine-protein kinase TNNI3K Kinase Kd 6.51 CHEMBL
5'-AMP-activated protein kinase catalytic subunit alpha-2 Kinase Kd 6.12 CHEMBL
Ankyrin repeat and protein kinase domain-containing protein 1 Kinase Kd 6.48 CHEMBL
Discoidin domain-containing receptor 2 Kinase Kd 7.37 CHEMBL
Chaperone activity of bc1 complex-like, mitochondrial Kinase Kd 5.96 CHEMBL
Serine/threonine-protein kinase LATS1 Kinase Kd 5.67 CHEMBL
Serine/threonine-protein kinase LATS2 Kinase Kd 5.40 CHEMBL
Leukocyte tyrosine kinase receptor Kinase Kd 6.10 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1 Kinase Kd 5.85 CHEMBL
Serine/threonine-protein kinase PAK 6 Kinase Kd 6.51 CHEMBL
Serine/threonine-protein kinase PAK 7 Kinase Kd 7.16 CHEMBL
NUAK family SNF1-like kinase 1 Kinase Kd 7.12 CHEMBL
cAMP-dependent protein kinase catalytic subunit alpha Kinase Kd 6.22 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 3 Kinase Kd 5.62 CHEMBL
Aurora kinase B Kinase Kd 6.96 CHEMBL
Tyrosine-protein kinase Blk Kinase Kd 7.60 CHEMBL
Serine/threonine-protein kinase MARK1 Kinase Kd 6.57 CHEMBL
MAP/microtubule affinity-regulating kinase 4 Kinase Kd 7.05 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 4 Kinase Kd 6.70 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 6 Kinase Kd 6.32 CHEMBL
Tyrosine-protein kinase Mer Kinase Kd 6.77 CHEMBL
Mitogen-activated protein kinase kinase kinase 9 Kinase Kd 8.37 CHEMBL
Mitogen-activated protein kinase kinase kinase 10 Kinase Kd 8.42 CHEMBL
Mitogen-activated protein kinase kinase kinase 11 Kinase Kd 7.96 CHEMBL
Muscle, skeletal receptor tyrosine-protein kinase Kinase Kd 7 CHEMBL
Citron Rho-interacting kinase Kinase Kd 6.36 CHEMBL
Death-associated protein kinase 1 Kinase Kd 7.26 CHEMBL
Serine/threonine-protein kinase Nek5 Kinase Kd 7.89 CHEMBL
Serine/threonine-protein kinase Nek9 Kinase Kd 7.80 CHEMBL
Serine/threonine-protein kinase PAK 1 Kinase Kd 6.58 CHEMBL
Serine/threonine-protein kinase PAK 2 Kinase Kd 6.47 CHEMBL
Serine/threonine-protein kinase PAK 4 Kinase Kd 7.02 CHEMBL
AarF domain-containing protein kinase 4 Kinase Kd 7.19 CHEMBL
Serine/threonine-protein kinase SIK1 Kinase Kd 7.28 CHEMBL
Tyrosine-protein kinase Srms Kinase Kd 6.21 CHEMBL
Dual specificity testis-specific protein kinase 1 Kinase Kd 6.44 CHEMBL
TGF-beta receptor type-1 Kinase Kd 5.58 CHEMBL
Ephrin type-A receptor 1 Kinase Kd 7.17 CHEMBL
Serine/threonine-protein kinase PLK3 Kinase Kd 8.29 CHEMBL
Mitogen-activated protein kinase 15 Kinase Kd 6.19 CHEMBL
Serine/threonine-protein kinase D3 Kinase Kd 5.41 CHEMBL
cGMP-dependent protein kinase 2 Kinase Kd 5.44 CHEMBL
Interferon-induced, double-stranded RNA-activated protein kinase Kinase Kd 6.75 CHEMBL
Tyrosine-protein kinase Fes/Fps Kinase Kd 6.70 CHEMBL
Fibroblast growth factor receptor 4 Kinase Kd 6.46 CHEMBL
Proto-oncogene tyrosine-protein kinase ROS Kinase Kd 7.54 CHEMBL
Ribosomal protein S6 kinase alpha-1 Kinase Kd 6.31 CHEMBL
Ribosomal protein S6 kinase alpha-4 Kinase Kd 7.36 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2 Kinase Kd 6.17 CHEMBL
Serine/threonine-protein kinase TBK1 Kinase Kd 7.64 CHEMBL
Interleukin-1 receptor-associated kinase 4 Kinase Kd 6.85 CHEMBL
Cyclin-dependent kinase-like 2 Kinase Kd 5.23 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 1A Kinase Kd 6.58 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 2 Kinase Kd 6.33 CHEMBL
Ephrin type-B receptor 6 Kinase Kd 6.51 CHEMBL
Serine/threonine-protein kinase/endoribonuclease IRE1 Kinase Kd 5.80 CHEMBL
Rhodopsin kinase Kinase Kd 6.06 CHEMBL
G protein-coupled receptor kinase 4 Kinase Kd 6.35 CHEMBL
G protein-coupled receptor kinase 7 Kinase Kd 5.70 CHEMBL
Homeodomain-interacting protein kinase 2 Kinase Kd 5.32 CHEMBL
Homeodomain-interacting protein kinase 3 Kinase Kd 5.50 CHEMBL
Homeodomain-interacting protein kinase 4 Kinase Kd 5.55 CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit alpha Kinase Kd 6.92 CHEMBL
Interleukin-1 receptor-associated kinase 1 Kinase Kd 8.01 CHEMBL
Mitogen-activated protein kinase kinase kinase 2 Kinase Kd 7.03 CHEMBL
Mitogen-activated protein kinase kinase kinase 3 Kinase Kd 6.82 CHEMBL
Serine/threonine-protein kinase 38 Kinase Kd 5.03 CHEMBL
Serine/threonine-protein kinase NIM1 Kinase Kd 6.18 CHEMBL
Serine/threonine-protein kinase OSR1 Kinase Kd 5.51 CHEMBL
Serine/threonine-protein kinase RIO2 Kinase Kd 5.47 CHEMBL
SRSF protein kinase 3 Kinase Kd 6.40 CHEMBL
Mitogen-activated protein kinase kinase kinase 7 Kinase Kd 7.31 CHEMBL
Serine/threonine-protein kinase TAO1 Kinase Kd 6.31 CHEMBL
Tyrosine-protein kinase JAK3 Kinase Kd 7.44 CHEMBL
Serine/threonine-protein kinase ULK1 Kinase Kd 7.85 CHEMBL
Serine/threonine-protein kinase ULK2 Kinase Kd 7.72 CHEMBL
Serine/threonine-protein kinase ULK3 Kinase Kd 8.15 CHEMBL
Mitogen-activated protein kinase kinase kinase 19 Kinase Kd 7.17 CHEMBL
Homeodomain-interacting protein kinase 1 Kinase Kd 6.09 CHEMBL
Serine/threonine-protein kinase PLK2 Kinase Kd 7.47 CHEMBL
Receptor-interacting serine/threonine-protein kinase 4 Kinase Kd 6.66 CHEMBL
Uncharacterized serine/threonine-protein kinase SBK3 Kinase Kd 6.72 CHEMBL
Serine/threonine-protein kinase 35 Kinase Kd 5.85 CHEMBL
Phosphatidylinositol 4-kinase beta Kinase Kd 6.03 CHEMBL
Wee1-like protein kinase 2 Kinase Kd 5.03 CHEMBL
Bone morphogenetic protein receptor type-1B Kinase Kd 6.14 CHEMBL
Serine/threonine-protein kinase SBK1 Kinase Kd 7.03 CHEMBL
Serine/threonine-protein kinase 32A Kinase Kd 5.64 CHEMBL
Serine/threonine-protein kinase Nek3 Kinase Kd 6.77 CHEMBL
Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma Kinase Kd 6.89 CHEMBL
Serine/threonine-protein kinase TAO2 Kinase Kd 6.19 CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma Kinase Kd 6.92 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5 Kinase Kd 7.39 CHEMBL
Serine/threonine-protein kinase Nek11 Kinase Kd 6.77 CHEMBL
Leucine-rich repeat serine/threonine-protein kinase 2 Kinase Kd 7.57 CHEMBL
Serine/threonine-protein kinase Nek6 Kinase Kd 8.20 CHEMBL
Ferrochelatase, mitochondrial Enzyme Kd 5.51 CHEMBL
Serine/threonine-protein kinase Nek4 Kinase Kd 5.75 CHEMBL
Bromodomain testis-specific protein Nuclear other IC50 4.68 CHEMBL
Serine/threonine-protein kinase Nek1 Kinase Kd 6.77 CHEMBL
Myosin-10 Enzyme Kd 6.64 CHEMBL
Cyclin-dependent kinase-like 1 Kinase Kd 5.68 CHEMBL
Uncharacterized aarF domain-containing protein kinase 1 Kinase Kd 7.62 CHEMBL
Adenosine receptor A3 GPCR INHIBITOR IC50 7.09 SCIENTIFIC LITERATURE
Serine/threonine-protein kinase TAO3 Kinase Kd 5.34 CHEMBL
Serine/threonine-protein kinase PknB Kinase Kd 7.47 CHEMBL
Mast/stem cell growth factor receptor Kit Kinase EC50 7.34 CHEMBL

External reference:

IDSource
SQ8A3S5101 UNII
914295-16-2 SECONDARY_CAS_RN
4037543 VANDF
C2713632 UMLSCUI
CHEBI:750486 CHEBI
2RC PDB_CHEM_ID
CHEMBL2103830 ChEMBL_ID
11671467 PUBCHEM_CID
DB12010 DRUGBANK_ID
CHEMBL3989516 ChEMBL_ID
D09347 KEGG_DRUG
9022 INN_ID
C523665 MESH_SUPPLEMENTAL_RECORD_UI
7796 IUPHAR_LIGAND_ID
DB07159 DRUGBANK_ID
772033003 SNOMEDCT_US
772039004 SNOMEDCT_US
C4730994 UMLSCUI
CHEMBL475251 ChEMBL_ID
841290-80-0 SECONDARY_CAS_RN
276522 MMSL
d08782 MMSL
11213558 PUBCHEM_CID
017516 NDDF
017517 NDDF
5706 IUPHAR_LIGAND_ID
2044896 RXNORM
RC3A285J2G UNII
CHEBI:91348 CHEBI
RC3A285J2G INXIGHT DRUGS
SQ8A3S5101 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
TAVALISSE HUMAN PRESCRIPTION DRUG LABEL 1 71332-001 TABLET 100 mg ORAL NDA 28 sections
TAVALISSE HUMAN PRESCRIPTION DRUG LABEL 1 71332-001 TABLET 100 mg ORAL NDA 28 sections
TAVALISSE HUMAN PRESCRIPTION DRUG LABEL 1 71332-002 TABLET 150 mg ORAL NDA 28 sections
TAVALISSE HUMAN PRESCRIPTION DRUG LABEL 1 71332-002 TABLET 150 mg ORAL NDA 28 sections