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

Stem definitionDrug idCAS RN
5231 120685-11-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • midostaurin
  • CGP 41251
  • PKC 412
  • rydapt
Midostaurin is a small molecule that inhibits multiple receptor tyrosine kinases. In vitro biochemical or cellular assays have shown that midostaurin or its major human active metabolites CGP62221 and CGP52421 inhibit the activity of wild type FLT3, FLT3 mutant kinases (ITD and TKD), KIT (wild type and D816V mutant), PDGFR-alfa/beta, VEGFR2, as well as members of the serine/threonine kinase PKC (protein kinase C) family. Midostaurin demonstrated the ability to inhibit FLT3 receptor signaling and cell proliferation, and it induced apoptosis in leukemic cells expressing ITD and TKD mutant FLT3 receptors or overexpressing wild type FLT3 and PDGF receptors. Midostaurin also demonstrated the ability to inhibit KIT signaling, cell proliferation and histamine release and induce apoptosis in mast cells.
  • Molecular weight: 570.65
  • Formula: C35H30N4O4
  • CLOGP: 5.53
  • LIPINSKI: 2
  • HAC: 8
  • HDO: 1
  • TPSA: 77.73
  • ALOGS: -4.56
  • ROTB: 3
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.10 g O

ADMET properties:

PropertyValueReference
S (Water solubility) 0.00 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
kinase-safety-class AAK1,ABL1,ABL2,ACVR1B,ACVR2A,ACVR2B,ACVRL1,AKT2,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,BTK,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK14,CDK16,CDK19,CDK2,CDK3,CDK4,CDK5,CDK6,CDK7,CDK9,CHEK1,CHEK2,CHUK,CLK2,CLK4,CSF1R,CSK,DDR1,DYRK1A,DYRK1B,DYRK2,DYRK3,EGFR,EIF2AK3,EPHA2,EPHB1,EPHB3,EPHB4,ERBB2,ERBB4,FGFR1,FGFR4,FLT1,FLT3,FLT4,FYN,GAK,GRK1,GRK2,GSK3A,GSK3B,HASPIN,HIPK2,IGF1R,IKBKB,INSR,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,MAPKAPK2,MAPKAPK5,MARK1,MARK2,MARK3,MARK4,MELK,MET,MINK1,MKNK2,MST1R,MTOR,NTRK1,NTRK2,NTRK3,NUAK1,PAK1,PAK2,PAK4,PDGFRB,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM1,PIM2,PIM3,PLK1,PLK4,PRKAA1,PRKAA2,PRKACA,PRKCA,PRKCD,PRKCZ,PRKD1,PRKDC,PTK2,RET,RIPK1,RIPK3,ROCK1,ROCK2,RPS6KA1,SGK1,SIK2,SIK3,SRC,STK10,STK16,STK17A,STK33,STK4,SYK,TBK1,TEK,TGFBR1,TNIK,TNK1,TTK,TYRO3,UHMK1,ULK1,ULK2,YES1,ZAP70 176
kinase-selectivity-class ACVR2B,ALK,AURKC,AXL,BRAF,CAMK2D,CDK9,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,MAP4K1,MAPK7,MAPK8,PDK1,PIK3CD,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK 26
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Sept. 18, 2017 EMA Novartis Europharm Ltd
April 28, 2017 FDA NOVARTIS PHARMS CORP

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 189.06 32.82 92 2559 158257 90467539
Acute myeloid leukaemia recurrent 181.73 32.82 34 2617 2023 90623773
Death 75.61 32.82 79 2572 456472 90169324
Neutropenic colitis 67.22 32.82 17 2634 4126 90621670
Thrombocytopenia 59.50 32.82 49 2602 208676 90417120
Minimal residual disease 56.72 32.82 10 2641 424 90625372
Sepsis 55.01 32.82 44 2607 179770 90446026
Hyperbilirubinaemia 50.65 32.82 18 2633 13918 90611878
Abdominal wall wound 47.20 32.82 7 2644 97 90625699
Myeloblast percentage decreased 44.30 32.82 6 2645 41 90625755
Cytopenia 43.16 32.82 17 2634 17432 90608364
Neutropenia 42.68 32.82 42 2609 224862 90400934
Iron overload 42.38 32.82 9 2642 1016 90624780
Nausea 41.30 32.82 96 2555 1110220 89515576
Septic shock 40.24 32.82 27 2624 84133 90541663
Systemic mastocytosis 35.49 32.82 6 2645 198 90625598
Megacolon 35.49 32.82 9 2642 2205 90623591
Graft versus host disease 35.30 32.82 12 2639 8132 90617664
Enterococcal infection 32.90 32.82 12 2639 9979 90615817

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
Acute myeloid leukaemia recurrent 496.76 36.84 101 3255 3411 42614568
Febrile neutropenia 186.42 36.84 137 3219 185566 42432413
Bone marrow failure 183.76 36.84 76 3280 33017 42584962
Skin toxicity 165.92 36.84 47 3309 6502 42611477
Pancytopenia 155.60 36.84 103 3253 117640 42500339
Lymphadenopathy 109.24 36.84 53 3303 33312 42584667
Neutropenic colitis 82.02 36.84 25 3331 4445 42613534
Cytomegalovirus infection reactivation 80.43 36.84 31 3325 11147 42606832
Graft versus host disease 76.06 36.84 31 3325 12894 42605085
Thrombocytopenia 71.33 36.84 81 3275 190198 42427781
Drug intolerance 66.26 36.84 53 3303 80371 42537608
Tryptase increased 61.67 36.84 12 3344 318 42617661
Device related infection 59.71 36.84 30 3326 20249 42597730
Neutropenia 56.93 36.84 74 3282 199357 42418622
Myelosuppression 54.64 36.84 36 3320 40425 42577554
Pyrexia 48.78 36.84 100 3256 393942 42224037
Rash maculo-papular 44.96 36.84 31 3325 37472 42580507
Malignant neoplasm progression 43.66 36.84 48 3308 108352 42509627

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
Acute myeloid leukaemia recurrent 649.72 31.61 125 5420 5014 110578740
Febrile neutropenia 367.32 31.61 216 5329 316551 110267203
Bone marrow failure 212.43 31.61 87 5458 57761 110525993
Pancytopenia 201.21 31.61 127 5418 209486 110374268
Skin toxicity 163.87 31.61 48 5497 11735 110572019
Neutropenic colitis 158.23 31.61 43 5502 8022 110575732
Thrombocytopenia 129.53 31.61 120 5425 348765 110234989
Graft versus host disease 110.99 31.61 40 5505 18766 110564988
Neutropenia 107.55 31.61 112 5433 374508 110209246
Cytomegalovirus infection reactivation 104.47 31.61 38 5507 18295 110565459
Lymphadenopathy 93.60 31.61 51 5494 63784 110519970
Rash maculo-papular 81.21 31.61 49 5496 74173 110509581
Sepsis 76.65 31.61 88 5457 327258 110256496
Pyrexia 75.29 31.61 149 5396 898116 109685638
Septic shock 69.81 31.61 60 5485 157468 110426286
Tryptase increased 65.73 31.61 14 5531 929 110582825
Device related infection 59.08 31.61 32 5513 39487 110544267
Myelosuppression 56.77 31.61 43 5502 94297 110489457
Malignant neoplasm progression 55.03 31.61 55 5490 174512 110409242
Minimal residual disease 54.37 31.61 12 5533 941 110582813
Bacteraemia 54.28 31.61 31 5514 42359 110541395
Death 50.24 31.61 109 5436 698760 109884994
Diarrhoea 49.79 31.61 147 5398 1139358 109444396
Abdominal wall wound 43.84 31.61 7 5538 91 110583663
Cytopenia 41.19 31.61 23 5522 30093 110553661
Myeloblast percentage decreased 41.06 31.61 6 5539 41 110583713
Systemic mastocytosis 40.93 31.61 8 5537 345 110583409
Hyperbilirubinaemia 40.80 31.61 23 5522 30648 110553106
Anaemia 33.31 31.61 80 5465 547006 110036748

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EX10 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Other protein kinase inhibitors
FDA MoA N0000020000 Receptor Tyrosine Kinase Inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:37700 EC 2.7.11.13 (protein kinase C) inhibitor

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

DiseaseRelationSNOMED_IDDOID
Acute myeloid leukemia, disease indication 91861009
Mast cell leukemia indication 110002002
Aggressive systemic mastocytosis indication 716655008 DOID:4798




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.7 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
25MG RYDAPT NOVARTIS N207997 April 28, 2017 RX CAPSULE ORAL 7973031 Oct. 9, 2028 TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED ACUTE MYELOID LEUKEMIA (AML) WHO ARE FLT3 MUTATION-POSITIVE, IN COMBINATION WITH STANDARD CYTARABINE AND DAUNORUBICIN INDUCTION AND CYTARABINE CONSOLIDATION CHEMOTHERAPY
25MG RYDAPT NOVARTIS N207997 April 28, 2017 RX CAPSULE ORAL 8575146 Dec. 2, 2030 TREATMENT OF ADULT PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), OR MAST CELL LEUKEMIA (MCL)

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 Kd 7.96 IUPHAR DRUG LABEL
Dual specificity protein kinase CLK2 Kinase Kd 6.07 CHEMBL
Angiopoietin-1 receptor Kinase Kd 5.72 CHEMBL
cAMP-dependent protein kinase catalytic subunit beta Kinase Kd 6.62 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit gamma Kinase Kd 6.85 CHEMBL
AP2-associated protein kinase 1 Kinase Kd 7.32 CHEMBL
Serine/threonine-protein kinase MARK2 Kinase Kd 7 CHEMBL
Serine/threonine-protein kinase D3 Kinase Kd 5.50 CHEMBL
Dual specificity protein kinase CLK1 Kinase Kd 6.46 CHEMBL
Tyrosine-protein kinase JAK3 Kinase Kd 7.92 CHEMBL
Multidrug resistance protein 1 Transporter IC50 7.17 CHEMBL
ATP-binding cassette sub-family G member 2 Transporter IC50 5.35 CHEMBL
Platelet-derived growth factor receptor beta Kinase Kd 6.96 CHEMBL
Tyrosine-protein kinase ABL1 Kinase Kd 6.10 CHEMBL
Mast/stem cell growth factor receptor Kit Kinase Kd 8.11 CHEMBL
Epidermal growth factor receptor Kinase Kd 8.06 CHEMBL
Aspartyl/asparaginyl beta-hydroxylase Enzyme IC50 5.22 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase Kd 5.92 CHEMBL
Tyrosine-protein kinase Lck Kinase Kd 6.55 CHEMBL
Tyrosine-protein kinase Yes Kinase Kd 6.02 CHEMBL
Tyrosine-protein kinase Fyn Kinase Kd 5.68 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase Kd 7.70 CHEMBL
Vascular endothelial growth factor receptor 1 Kinase Kd 6.35 CHEMBL
Vascular endothelial growth factor receptor 2 Kinase IC50 6.60 CHEMBL
Vascular endothelial growth factor receptor 3 Kinase Kd 6.17 CHEMBL
Macrophage colony-stimulating factor 1 receptor Kinase IC50 6.85 CHEMBL
Platelet-derived growth factor receptor alpha Kinase Kd 6.75 CHEMBL
Ribosomal protein S6 kinase alpha-3 Kinase Kd 6.13 CHEMBL
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform Kinase Kd 6.05 CHEMBL
Serine/threonine-protein kinase pim-1 Kinase Kd 6.25 CHEMBL
Myosin light chain kinase, smooth muscle Kinase Kd 6.66 CHEMBL
Death-associated protein kinase 3 Kinase Kd 5.75 CHEMBL
Calcium/calmodulin-dependent protein kinase type 1 Kinase Kd 5.70 CHEMBL
Mitogen-activated protein kinase 8 Kinase Kd 5.36 CHEMBL
Fibroblast growth factor receptor 3 Kinase Kd 5.77 CHEMBL
Rho-associated protein kinase 1 Kinase Kd 5.11 CHEMBL
Tyrosine-protein kinase HCK Kinase Kd 6.14 CHEMBL
Tyrosine-protein kinase JAK1 Kinase Kd 6.17 CHEMBL
Receptor tyrosine-protein kinase erbB-4 Kinase Kd 5.51 CHEMBL
Mitogen-activated protein kinase 10 Kinase Kd 5.44 CHEMBL
Death-associated protein kinase 2 Kinase Kd 6.05 CHEMBL
High affinity nerve growth factor receptor Kinase Kd 6.42 CHEMBL
Protein kinase C delta type Kinase Kd 6.50 CHEMBL
Tyrosine-protein kinase JAK2 Kinase Kd 7.03 CHEMBL
Rho-associated protein kinase 2 Kinase Kd 5.64 CHEMBL
Protein kinase C alpha type Kinase Kd 6.14 CHEMBL
Tyrosine-protein kinase SYK Kinase Kd 7.06 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit delta Kinase Kd 7.44 CHEMBL
Hepatocyte growth factor receptor Kinase Kd 6.25 CHEMBL
Tyrosine-protein kinase Lyn Kinase Kd 5.38 CHEMBL
Ribosomal protein S6 kinase alpha-2 Kinase Kd 6.62 CHEMBL
5'-AMP-activated protein kinase catalytic subunit alpha-1 Kinase Kd 6.75 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit beta Kinase Kd 6.68 CHEMBL
Protein kinase C eta type Kinase Kd 6.54 CHEMBL
Fibroblast growth factor receptor 1 Kinase Kd 5.80 CHEMBL
Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform Kinase Kd 6.72 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit alpha Kinase Kd 7.70 CHEMBL
Serine/threonine-protein kinase 17B Kinase Kd 5.33 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 6.23 CHEMBL
Tyrosine-protein kinase Fer Kinase Kd 5.92 CHEMBL
Protein kinase C epsilon type Kinase Kd 6.27 CHEMBL
Serine/threonine-protein kinase PLK4 Kinase Kd 7.18 CHEMBL
Aurora kinase C Kinase Kd 6.77 CHEMBL
Serine/threonine-protein kinase 16 Kinase Kd 6.55 CHEMBL
Dual specificity protein kinase TTK Kinase Kd 6.46 CHEMBL
Fibroblast growth factor receptor 2 Kinase Kd 5.62 CHEMBL
Serine/threonine-protein kinase N1 Kinase Kd 8.03 CHEMBL
Protein kinase C theta type Kinase Kd 6.04 CHEMBL
Serine/threonine-protein kinase 17A Kinase Kd 5.72 CHEMBL
TRAF2 and NCK-interacting protein kinase Kinase Kd 5.80 CHEMBL
Tyrosine-protein kinase Fgr Kinase Kd 6.14 CHEMBL
Aurora kinase A Kinase IC50 7.10 CHEMBL
ALK tyrosine kinase receptor Kinase Kd 6.57 CHEMBL
RAC-alpha serine/threonine-protein kinase Kinase Kd 6.02 CHEMBL
BMP-2-inducible protein kinase Kinase Kd 6.66 CHEMBL
Serine/threonine-protein kinase pim-2 Kinase Kd 5.51 CHEMBL
Tyrosine-protein kinase FRK Kinase Kd 5.62 CHEMBL
Dual specificity protein kinase CLK3 Kinase Kd 5.44 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 5 Kinase Kd 5.96 CHEMBL
Cyclin-G-associated kinase Kinase Kd 6.42 CHEMBL
Glycogen synthase kinase-3 beta Kinase Kd 5.75 CHEMBL
Calcium/calmodulin-dependent protein kinase type 1D Kinase Kd 6.17 CHEMBL
Serine/threonine-protein kinase 4 Kinase Kd 7.77 CHEMBL
Activated CDC42 kinase 1 Kinase Kd 6.92 CHEMBL
Ribosomal protein S6 kinase alpha-5 Kinase Kd 6.62 CHEMBL
STE20-like serine/threonine-protein kinase Kinase Kd 6.66 CHEMBL
Dual specificity protein kinase CLK4 Kinase Kd 6.39 CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 2 Kinase Kd 6.02 CHEMBL
Mitogen-activated protein kinase 9 Kinase Kd 5.30 CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 2 Kinase Kd 7.14 CHEMBL
MAP/microtubule affinity-regulating kinase 3 Kinase Kd 7.68 CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 1 Kinase Kd 6.89 CHEMBL
Calcium/calmodulin-dependent protein kinase type 1G Kinase Kd 5.75 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase Kd 5.14 CHEMBL
Testis-specific serine/threonine-protein kinase 1 Kinase Kd 5.32 CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit beta Kinase Kd 5.20 CHEMBL
3-phosphoinositide-dependent protein kinase 1 Kinase Kd 6.96 CHEMBL
Tyrosine-protein kinase ZAP-70 Kinase Kd 5.59 CHEMBL
Glycogen synthase kinase-3 alpha Kinase Kd 5.60 CHEMBL
Tyrosine-protein kinase receptor UFO Kinase Kd 6.21 CHEMBL
BDNF/NT-3 growth factors receptor Kinase Kd 6.51 CHEMBL
Tyrosine-protein kinase receptor TYRO3 Kinase Kd 7.06 CHEMBL
Ribosomal protein S6 kinase beta-1 Kinase Kd 5.89 CHEMBL
Serine/threonine-protein kinase N2 Kinase Kd 7.82 CHEMBL
RAC-beta serine/threonine-protein kinase Kinase Kd 6.11 CHEMBL
Serine/threonine-protein kinase 3 Kinase Kd 7.40 CHEMBL
Ribosomal protein S6 kinase alpha-6 Kinase Kd 5.82 CHEMBL
NUAK family SNF1-like kinase 2 Kinase Kd 7.20 CHEMBL
Non-receptor tyrosine-protein kinase TNK1 Kinase Kd 7.08 CHEMBL
Non-receptor tyrosine-protein kinase TYK2 Kinase Kd 6.60 CHEMBL
Serine/threonine-protein kinase Chk1 Kinase Kd 5.89 CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Kinase Kd 5.96 CHEMBL
Serine/threonine-protein kinase PAK 3 Kinase Kd 6.75 CHEMBL
Phosphatidylinositol 4-phosphate 5-kinase type-1 alpha Kinase Kd 6.51 CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 beta Kinase Kd 6.57 CHEMBL
Myosin light chain kinase family member 4 Kinase Kd 6.19 CHEMBL
Wee1-like protein kinase Kinase Kd 5.34 CHEMBL
Serine/threonine-protein kinase 25 Kinase Kd 5.75 CHEMBL
Protein-tyrosine kinase 2-beta Kinase Kd 6.18 CHEMBL
Serine/threonine-protein kinase RIO1 Kinase Kd 5.92 CHEMBL
Tyrosine-protein kinase receptor Tie-1 Kinase Kd 5.85 CHEMBL
NT-3 growth factor receptor Kinase Kd 5.77 CHEMBL
Casein kinase II subunit alpha Kinase Kd 6.60 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 1B Kinase Kd 6.48 CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit epsilon Kinase Kd 6.80 CHEMBL
Serine/threonine-protein kinase STK11 Kinase Kd 6.46 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 3 Kinase Kd 5.28 CHEMBL
Maternal embryonic leucine zipper kinase Kinase Kd 6.55 CHEMBL
Eukaryotic translation initiation factor 2-alpha kinase 4 Kinase Kd 7.41 CHEMBL
Interleukin-1 receptor-associated kinase 3 Kinase Kd 6.75 CHEMBL
Serine/threonine-protein kinase RIO3 Kinase Kd 6.38 CHEMBL
Serine/threonine-protein kinase SIK2 Kinase Kd 6.25 CHEMBL
SRSF protein kinase 1 Kinase Kd 7.38 CHEMBL
SRSF protein kinase 2 Kinase Kd 6.48 CHEMBL
Serine/threonine-protein kinase 33 Kinase Kd 6.72 CHEMBL
5'-AMP-activated protein kinase catalytic subunit alpha-2 Kinase Kd 6.34 CHEMBL
Myotonin-protein kinase Kinase Kd 5.42 CHEMBL
RAC-gamma serine/threonine-protein kinase Kinase Kd 5.36 CHEMBL
Serine/threonine-protein kinase LATS1 Kinase Kd 5.96 CHEMBL
Serine/threonine-protein kinase LATS2 Kinase Kd 5.66 CHEMBL
Leukocyte tyrosine kinase receptor Kinase Kd 5.52 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1 Kinase Kd 5.68 CHEMBL
NUAK family SNF1-like kinase 1 Kinase Kd 7.39 CHEMBL
Serine/threonine-protein kinase pim-3 Kinase Kd 6.25 CHEMBL
cAMP-dependent protein kinase catalytic subunit alpha Kinase Kd 6.14 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 3 Kinase Kd 6.92 CHEMBL
Aurora kinase B Kinase Kd 7.21 CHEMBL
Tyrosine-protein kinase Blk Kinase Kd 6.30 CHEMBL
Serine/threonine-protein kinase BRSK1 Kinase Kd 5.92 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 4 Kinase Kd 6.19 CHEMBL
Serine/threonine-protein kinase MARK1 Kinase Kd 6.77 CHEMBL
MAP/microtubule affinity-regulating kinase 4 Kinase Kd 6.43 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 4 Kinase Kd 5.32 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 6 Kinase Kd 5.19 CHEMBL
Tyrosine-protein kinase Mer Kinase Kd 5.54 CHEMBL
Cyclin-dependent kinase 19 Kinase Kd 5.14 CHEMBL
Mitogen-activated protein kinase kinase kinase 9 Kinase Kd 7.82 CHEMBL
Mitogen-activated protein kinase kinase kinase 10 Kinase Kd 6.10 CHEMBL
Mitogen-activated protein kinase kinase kinase 11 Kinase Kd 7.77 CHEMBL
Death-associated protein kinase 1 Kinase Kd 5.33 CHEMBL
Serine/threonine-protein kinase PAK 1 Kinase Kd 5.70 CHEMBL
Serine/threonine-protein kinase PAK 2 Kinase Kd 5.68 CHEMBL
Serine/threonine-protein kinase BRSK2 Kinase Kd 6.19 CHEMBL
Serine/threonine-protein kinase SIK1 Kinase Kd 6.80 CHEMBL
Serine/threonine-protein kinase D2 Kinase Kd 5.20 CHEMBL
cGMP-dependent protein kinase 2 Kinase Kd 7.13 CHEMBL
Interferon-induced, double-stranded RNA-activated protein kinase Kinase Kd 5.16 CHEMBL
Proto-oncogene tyrosine-protein kinase ROS Kinase Kd 6.37 CHEMBL
Ribosomal protein S6 kinase alpha-1 Kinase Kd 6.59 CHEMBL
Ribosomal protein S6 kinase alpha-4 Kinase Kd 6.59 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2 Kinase Kd 5.60 CHEMBL
Misshapen-like kinase 1 Kinase Kd 6.77 CHEMBL
Serine/threonine-protein kinase TBK1 Kinase Kd 8.03 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 1A Kinase Kd 7 CHEMBL
Ephrin type-B receptor 6 Kinase Kd 5.51 CHEMBL
Serine/threonine-protein kinase/endoribonuclease IRE1 Kinase Kd 5.64 CHEMBL
Rhodopsin kinase Kinase Kd 7.07 CHEMBL
G protein-coupled receptor kinase 4 Kinase Kd 6.96 CHEMBL
G protein-coupled receptor kinase 7 Kinase Kd 7.32 CHEMBL
Homeodomain-interacting protein kinase 2 Kinase Kd 5.51 CHEMBL
Homeodomain-interacting protein kinase 3 Kinase Kd 5.64 CHEMBL
Homeodomain-interacting protein kinase 4 Kinase Kd 6.02 CHEMBL
Hormonally up-regulated neu tumor-associated kinase Kinase Kd 6.62 CHEMBL
Serine/threonine-protein kinase ICK Kinase Kd 5.23 CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit alpha Kinase Kd 5.42 CHEMBL
Mitogen-activated protein kinase kinase kinase 13 Kinase Kd 5.55 CHEMBL
Tyrosine-protein kinase CSK Kinase Kd 5.06 CHEMBL
Mitogen-activated protein kinase kinase kinase 3 Kinase Kd 6.68 CHEMBL
Microtubule-associated serine/threonine-protein kinase 1 Kinase Kd 6.72 CHEMBL
U4/U6 small nuclear ribonucleoprotein Prp4 Nuclear other Kd 7.26 CHEMBL
Serine/threonine-protein kinase RIO2 Kinase Kd 7.01 CHEMBL
SRSF protein kinase 3 Kinase Kd 7.10 CHEMBL
Mitogen-activated protein kinase kinase kinase 7 Kinase Kd 6.89 CHEMBL
Serine/threonine-protein kinase ULK3 Kinase Kd 5.89 CHEMBL
Mitogen-activated protein kinase kinase kinase 19 Kinase Kd 7.82 CHEMBL
Tankyrase-2 Enzyme Kd 6.92 CHEMBL
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta Kinase Kd 5.85 CHEMBL
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit gamma Kinase Kd 6.24 CHEMBL
Serine/threonine-protein kinase SIK3 Kinase Kd 7.01 CHEMBL
Serine/threonine-protein kinase 32A Kinase Kd 5.62 CHEMBL
Serine/threonine-protein kinase PRP4 homolog Kinase Kd 7.26 CHEMBL
Serine/threonine-protein kinase Sgk3 Kinase Kd 5.85 CHEMBL
Eukaryotic translation initiation factor 2-alpha kinase 1 Kinase Kd 5.69 CHEMBL
Myosin light chain kinase 3 Kinase Kd 5.64 CHEMBL
Leucine-rich repeat serine/threonine-protein kinase 2 Kinase Kd 6.75 CHEMBL
Dual serine/threonine and tyrosine protein kinase Kinase Kd 5.33 CHEMBL
cGMP-dependent protein kinase 1 Kinase Kd 6.60 CHEMBL
cAMP-dependent protein kinase catalytic subunit PRKX Kinase Kd 6.02 CHEMBL
5'-AMP-activated protein kinase subunit gamma-1 Kinase Kd 5.93 CHEMBL
Uncharacterized protein FLJ45252 Unclassified Kd 6.53 CHEMBL
5'-AMP-activated protein kinase subunit gamma-2 Kinase Kd 5.04 CHEMBL
Mitogen-activated protein kinase kinase kinase 2 Kinase Kd 6.85 CHEMBL
Tubulin alpha-1A chain Structural Kd 5.51 CHEMBL
Calcium-dependent protein kinase 1 Kinase Kd 6.02 CHEMBL

External reference:

IDSource
ID912S5VON UNII
4036652 VANDF
C0526371 UMLSCUI
CHEBI:63452 CHEBI
2K2 PDB_CHEM_ID
CHEMBL608533 ChEMBL_ID
9829523 PUBCHEM_CID
DB06595 DRUGBANK_ID
D05029 KEGG_DRUG
7677 INN_ID
C059539 MESH_SUPPLEMENTAL_RECORD_UI
5702 IUPHAR_LIGAND_ID
763613005 SNOMEDCT_US
763614004 SNOMEDCT_US
256612 MMSL
32671 MMSL
d08575 MMSL
017198 NDDF
1919083 RXNORM
ID912S5VON INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
RYDAPT HUMAN PRESCRIPTION DRUG LABEL 1 0078-0698 CAPSULE, LIQUID FILLED 25 mg ORAL NDA 28 sections