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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5347 936091-26-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fedratinib
  • fedratinib hydrochloride
  • SAR302503
  • SAR-302503
  • TG101348
  • TG-101348
  • FEDR
  • inrebic
Fedratinib is an oral kinase inhibitor with activity against wild type and mutationally activated Janus Associated Kinase 2 (JAK2) and FMS-like tyrosine kinase 3 (FLT3). Fedratinib is a JAK2-selective inhibitor with higher inhibitory activity for JAK2 over family members JAK1, JAK3 and TYK2. Abnormal activation of JAK2 is associated with myeloproliferative neoplasms (MPNs), including myelofibrosis and polycythemia vera.
  • Molecular weight: 524.68
  • Formula: C27H36N6O3S
  • CLOGP: 6.25
  • LIPINSKI: 2
  • HAC: 9
  • HDO: 3
  • TPSA: 108.48
  • ALOGS: -4.74
  • ROTB: 10
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.40 g O

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.676 Moderate 0.68
caco2-efflux Caco-2 efflux ratio (BA/AB) 11.668 Moderate 0.68
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 5.297 10^-6 cm/s Moderate 0.68
dh-clint Dog hepatocyte intrinsic clearance 21.380 uL/min/10^6 cells Moderate 0.68
dppb Dog plasma protein binding (% unbound) 15.490 % Moderate 0.68
fcs-ppb Fetal calf serum protein binding (% unbound) 33.180 % Moderate 0.68
herg hERG pIC50 5.612 pIC50 Moderate 0.68
hh-clint Human hepatocyte intrinsic clearance 9.290 uL/min/10^6 cells Moderate 0.68
hlm-clint Human liver microsomal intrinsic clearance 76.913 uL/min/mg protein Moderate 0.68
hppb Human plasma protein binding (% unbound) 10.490 % Moderate 0.68
kinase-safety-class AAK1,ABL1,ABL2,ACVR2A,ACVR2B,ACVRL1,AKT1,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,CDK8,CDK9,CHEK1,CHEK2,CHUK,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,MAP2K4,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K19,MAP3K2,MAP3K21,MAP3K3,MAP3K7,MAP3K9,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK12,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,PTK2,PTK6,RET,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 183
kinase-selectivity-class AAK1,ABL2,ACVR2A,ACVR2B,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,BTK,CAMK2A,CAMK2B,CAMK2D,CDK1,CDK16,CDK2,CDK3,CDK4,CDK6,CDK7,CDK9,CHEK1,CLK2,CLK4,CSF1R,DDR1,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,FGFR1,FGFR4,FLT1,FLT3,FLT4,FYN,GAK,GRK2,GSK3A,GSK3B,HIPK2,IGF1R,IKBKB,INSR,IRAK1,IRAK3,IRAK4,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP2K3,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K2,MAP3K21,MAP3K7,MAP3K9,MAP4K1,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK12,MAPK7,MAPK8,MARK1,MARK2,MARK3,MARK4,MELK,MET,MINK1,MST1R,MTOR,NTRK1,NTRK3,NUAK1,PAK1,PAK2,PAK4,PAK5,PDGFRB,PDK1,PDK4,PDPK1,PIK3CA,PLK1,PLK2,PLK3,PLK4,PRKAA1,PRKAA2,PRKACA,PRKCD,PRKCI,PRKCZ,PTK2,RET,RIPK1,RIPK3,ROCK1,ROCK2,SGK1,SIK2,SIK3,SRC,STK10,STK16,STK17A,STK33,STK4,SYK,TEK,TNIK,TNK1,TTK,TYRO3,ULK1,ULK2,YES1 134
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 14.421 Moderate 0.68
mh-clint Mouse hepatocyte intrinsic clearance 90.157 Moderate 0.68
mppb Mouse plasma protein binding (% unbound) 10.300 Moderate 0.68
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 37.154 Moderate 0.68
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 21.560 % Moderate 0.68
rh-clint Rat hepatocyte intrinsic clearance 83.176 uL/min/10^6 cells Moderate 0.68
rh-fuinc Rat hepatocyte fraction unbound in incubation 31.170 % Moderate 0.68
rppb Rat plasma protein binding (% unbound) 13.300 % Moderate 0.68
solubility-dd Solubility at pH 7.4 in DMSO 130.017 uM Moderate 0.68

Approvals:

DateAgencyCompanyOrphan
Feb. 8, 2021 EMA CELGENE EUROPE BV
Aug. 16, 2019 FDA IMPACT

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
Vitamin B1 decreased 91.33 38.18 13 710 525 90627199
Diarrhoea 78.64 38.18 62 661 939128 89688596
Vitamin B1 deficiency 60.94 38.18 9 714 470 90627254
Splenomegaly 40.56 38.18 11 712 12913 90614811

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
Vitamin B1 decreased 144.11 38.80 20 592 367 42620356
Vitamin B1 deficiency 126.38 38.80 18 594 400 42620323
Death 60.44 38.80 51 561 471134 42149589
Splenomegaly 51.33 38.80 16 596 17031 42603692

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
Vitamin B1 decreased 245.65 42.78 33 820 906 110587540
Vitamin B1 deficiency 170.11 42.78 24 829 946 110587500
Death 86.85 42.78 58 795 698811 109889635
Splenomegaly 78.37 42.78 21 832 24477 110563969
Diarrhoea 57.84 42.78 56 797 1139449 109448997

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EJ02 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Janus-associated kinase (JAK) inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:233423 antifibrotic agent

Related Drugs by ATC class:

L01EJ Janus-associated kinase (JAK) inhibitors 3 drugs
momelotinibpacritinibruxolitinib

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

DiseaseRelationSNOMED_IDDOID
Myelofibrosis indication 52967002 DOID:4971
Primary myelofibrosis indication 307651005
Post-polycythaemia vera myelofibrosis indication 871540009
Post-essential thrombocythaemia myelofibrosis indication 871541008




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.42 acidic
pKa2 8.9 Basic
pKa3 5.69 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 100MG BASE INREBIC BRISTOL-MYERS N212327 Aug. 16, 2019 RX CAPSULE ORAL 8138199 June 30, 2028 TREATMENT OF ADULT PATIENTS WITH INTERMEDIATE-2 OR HIGH-RISK PRIMARY OR SECONDARY MYELOFIBROSIS
EQ 100MG BASE INREBIC BRISTOL-MYERS N212327 Aug. 16, 2019 RX CAPSULE ORAL 10391094 June 4, 2032 TREATMENT OF ADULT PATIENTS WITH INTERMEDIATE-2 OR HIGH-RISK PRIMARY OR SECONDARY MYELOFIBROSIS
EQ 100MG BASE INREBIC BRISTOL-MYERS N212327 Aug. 16, 2019 RX CAPSULE ORAL 11400092 Sept. 24, 2039 TREATING ADULT PATIENTS WITH INTERMEDIATE-2 OR HIGH-RISK PRIMARY OR SECONDARY MYELOFIBROSIS, MONITORING THIAMINE LEVELS AND ADMINISTERING THIAMINE OR A THIAMINE EQUIVALENT

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 100MG BASE INREBIC BRISTOL-MYERS N212327 Aug. 16, 2019 RX CAPSULE ORAL Aug. 16, 2026 INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH INTERMEDIATE-2 OR HIGH-RISK PRIMARY OR SECONDARY (POST-POLYCYTHEMIA VERA OR POST-ESSENTIAL THROMBOCYTHEMIA) MYELOFIBROSIS (MF)

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Receptor-type tyrosine-protein kinase FLT3 Kinase INHIBITOR IC50 7.82 SCIENTIFIC LITERATURE DRUG LABEL
Tyrosine-protein kinase JAK2 Kinase INHIBITOR IC50 8.52 SCIENTIFIC LITERATURE DRUG LABEL
Focal adhesion kinase 1 Kinase Kd 7.38 CHEMBL
Tyrosine-protein kinase HCK Kinase Kd 5.68 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 5.54 CHEMBL
Ribosyldihydronicotinamide dehydrogenase [quinone] Enzyme Kd 5.37 CHEMBL
Platelet-derived growth factor receptor beta Kinase Kd 7.35 CHEMBL
Tyrosine-protein kinase ABL1 Kinase Kd 7.40 CHEMBL
Mast/stem cell growth factor receptor Kit Kinase Kd 7.34 CHEMBL
Epidermal growth factor receptor Kinase Kd 6.24 CHEMBL
Breakpoint cluster region protein Kinase Kd 5.76 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase Kd 7.12 CHEMBL
Tyrosine-protein kinase Lck Kinase Kd 7.14 CHEMBL
Tyrosine-protein kinase Yes Kinase Kd 6.92 CHEMBL
Tyrosine-protein kinase Fyn Kinase Kd 7.42 CHEMBL
Ephrin type-A receptor 2 Kinase Kd 5.36 CHEMBL
Serine/threonine-protein kinase B-raf Kinase Kd 5.03 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase IC50 7.32 CHEMBL
Vascular endothelial growth factor receptor 1 Kinase Kd 5.37 CHEMBL
Vascular endothelial growth factor receptor 2 Kinase Kd 5.28 CHEMBL
Vascular endothelial growth factor receptor 3 Kinase Kd 5.70 CHEMBL
Macrophage colony-stimulating factor 1 receptor Kinase Kd 6.21 CHEMBL
Platelet-derived growth factor receptor alpha Kinase Kd 5.57 CHEMBL
Ribosomal protein S6 kinase alpha-3 Kinase Kd 5.09 CHEMBL
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform Kinase Kd 5.80 CHEMBL
Insulin-like growth factor 1 receptor Kinase Kd 5.66 CHEMBL
Myosin light chain kinase, smooth muscle Kinase Kd 6.28 CHEMBL
Insulin receptor Kinase Kd 6.07 CHEMBL
Death-associated protein kinase 3 Kinase Kd 8.92 CHEMBL
Calcium/calmodulin-dependent protein kinase type 1 Kinase Kd 5.80 CHEMBL
Mitogen-activated protein kinase 8 Kinase Kd 6.58 CHEMBL
Fibroblast growth factor receptor 3 Kinase Kd 6.44 CHEMBL
Serine/threonine-protein kinase PLK1 Kinase Kd 6.55 CHEMBL
Receptor tyrosine-protein kinase erbB-4 Kinase Kd 5.70 CHEMBL
Mitogen-activated protein kinase 10 Kinase Kd 6.70 CHEMBL
Death-associated protein kinase 2 Kinase Kd 7.54 CHEMBL
High affinity nerve growth factor receptor Kinase Kd 6.08 CHEMBL
Rho-associated protein kinase 2 Kinase Kd 5.66 CHEMBL
Tyrosine-protein kinase SYK Kinase Kd 5.57 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit delta Kinase Kd 6.23 CHEMBL
Myosin light chain kinase 2, skeletal/cardiac muscle Kinase Kd 5.52 CHEMBL
Tyrosine-protein kinase CSK Kinase Kd 5.23 CHEMBL
Angiopoietin-1 receptor Kinase Kd 5.72 CHEMBL
Ephrin type-A receptor 8 Kinase Kd 5.11 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit gamma Kinase Kd 6.27 CHEMBL
AP2-associated protein kinase 1 Kinase Kd 7.46 CHEMBL
Serine/threonine-protein kinase MARK2 Kinase Kd 5.51 CHEMBL
Hepatocyte growth factor receptor Kinase Kd 5.36 CHEMBL
Tyrosine-protein kinase Lyn Kinase Kd 6.30 CHEMBL
Cytoplasmic tyrosine-protein kinase BMX Kinase Kd 5.92 CHEMBL
Serine/threonine-protein kinase Nek2 Kinase Kd 5.77 CHEMBL
LIM domain kinase 1 Kinase Kd 6.03 CHEMBL
Ribosomal protein S6 kinase alpha-2 Kinase Kd 5.64 CHEMBL
5'-AMP-activated protein kinase catalytic subunit alpha-1 Kinase Kd 5.62 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit beta Kinase Kd 5.17 CHEMBL
Fibroblast growth factor receptor 1 Kinase Kd 6.55 CHEMBL
Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform Kinase Kd 6.48 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit alpha Kinase Kd 6.52 CHEMBL
Serine/threonine-protein kinase 17B Kinase Kd 7.35 CHEMBL
Protein kinase C epsilon type Kinase Kd 5.09 CHEMBL
Serine/threonine-protein kinase PLK4 Kinase Kd 7.02 CHEMBL
Aurora kinase C Kinase Kd 6.46 CHEMBL
Serine/threonine-protein kinase 16 Kinase Kd 8.18 CHEMBL
Dual specificity protein kinase TTK Kinase Kd 6.35 CHEMBL
Abelson tyrosine-protein kinase 2 Kinase Kd 6.24 CHEMBL
Ephrin type-A receptor 4 Kinase Kd 5.40 CHEMBL
Fibroblast growth factor receptor 2 Kinase Kd 6.33 CHEMBL
Serine/threonine-protein kinase N1 Kinase Kd 5.96 CHEMBL
Serine/threonine-protein kinase 17A Kinase Kd 6.21 CHEMBL
Ephrin type-A receptor 6 Kinase Kd 5.41 CHEMBL
Tyrosine-protein kinase Fgr Kinase Kd 7.09 CHEMBL
Aurora kinase A Kinase Kd 5.36 CHEMBL
ALK tyrosine kinase receptor Kinase Kd 6.19 CHEMBL
Serine/threonine-protein kinase 36 Kinase Kd 6.06 CHEMBL
Ephrin type-A receptor 3 Kinase Kd 5.15 CHEMBL
BMP-2-inducible protein kinase Kinase Kd 7.50 CHEMBL
Tyrosine-protein kinase FRK Kinase Kd 6.70 CHEMBL
Dual specificity protein kinase CLK1 Kinase Kd 5.60 CHEMBL
Dual specificity protein kinase CLK2 Kinase Kd 5.64 CHEMBL
Mitogen-activated protein kinase kinase kinase 4 Kinase Kd 5.39 CHEMBL
Cyclin-G-associated kinase Kinase Kd 8.96 CHEMBL
Receptor-interacting serine/threonine-protein kinase 2 Kinase Kd 5.21 CHEMBL
Ephrin type-B receptor 1 Kinase Kd 5.77 CHEMBL
Calcium/calmodulin-dependent protein kinase type 1D Kinase Kd 6.34 CHEMBL
Cyclin-dependent kinase 16 Kinase Kd 5.51 CHEMBL
Activated CDC42 kinase 1 Kinase Kd 7.19 CHEMBL
Ephrin type-A receptor 7 Kinase Kd 5.19 CHEMBL
Ribosomal protein S6 kinase alpha-5 Kinase Kd 5.66 CHEMBL
STE20-like serine/threonine-protein kinase Kinase Kd 6.17 CHEMBL
Dual specificity protein kinase CLK4 Kinase Kd 5.70 CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 2 Kinase Kd 6.42 CHEMBL
Mitogen-activated protein kinase 9 Kinase Kd 6.62 CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 2 Kinase Kd 5.40 CHEMBL
MAP/microtubule affinity-regulating kinase 3 Kinase Kd 6.52 CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 1 Kinase Kd 5.75 CHEMBL
Calcium/calmodulin-dependent protein kinase type 1G Kinase Kd 5.50 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase Kd 5.72 CHEMBL
Ephrin type-B receptor 4 Kinase Kd 5.68 CHEMBL
Testis-specific serine/threonine-protein kinase 1 Kinase Kd 5.89 CHEMBL
Activin receptor type-1B Kinase Kd 5.17 CHEMBL
Serine/threonine-protein kinase receptor R3 Kinase Kd 5.62 CHEMBL
Activin receptor type-1 Kinase Kd 6.82 CHEMBL
Cyclin-dependent kinase 15 Kinase Kd 5.07 CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit beta Kinase Kd 6.44 CHEMBL
TGF-beta receptor type-2 Kinase Kd 5.96 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 1 Kinase Kd 5.29 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 2 Kinase Kd 5.51 CHEMBL
Tyrosine-protein kinase ITK/TSK Kinase Kd 6.31 CHEMBL
Tyrosine-protein kinase ZAP-70 Kinase Kd 5.42 CHEMBL
Cyclin-dependent kinase 9 Kinase Kd 5.06 CHEMBL
Protein-tyrosine kinase 6 Kinase Kd 5.92 CHEMBL
Tyrosine-protein kinase BTK Kinase Kd 6.07 CHEMBL
Tyrosine-protein kinase receptor UFO Kinase Kd 6.80 CHEMBL
BDNF/NT-3 growth factors receptor Kinase Kd 5.51 CHEMBL
Ephrin type-B receptor 2 Kinase Kd 5.41 CHEMBL
Cyclin-dependent kinase 7 Kinase Kd 6.92 CHEMBL
Ribosomal protein S6 kinase beta-1 Kinase Kd 5.70 CHEMBL
Serine/threonine-protein kinase DCLK3 Kinase Kd 7.89 CHEMBL
Ribosomal protein S6 kinase alpha-6 Kinase Kd 6.44 CHEMBL
NUAK family SNF1-like kinase 2 Kinase Kd 7.31 CHEMBL
Non-receptor tyrosine-protein kinase TNK1 Kinase Kd 6.44 CHEMBL
Serine/threonine-protein kinase Chk1 Kinase Kd 5.42 CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Kinase Kd 5.41 CHEMBL
Cyclin-dependent kinase 17 Kinase Kd 6.46 CHEMBL
Cyclin-dependent kinase 18 Kinase Kd 5.57 CHEMBL
Cyclin-dependent kinase 14 Kinase Kd 5.58 CHEMBL
Phosphatidylinositol 4-phosphate 5-kinase type-1 alpha Kinase Kd 7.18 CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 beta Kinase Kd 6.80 CHEMBL
Myosin light chain kinase family member 4 Kinase Kd 6.89 CHEMBL
Wee1-like protein kinase Kinase Kd 6.41 CHEMBL
Serine/threonine-protein kinase 25 Kinase Kd 5.14 CHEMBL
Mitogen-activated protein kinase kinase kinase MLT Kinase Kd 6.19 CHEMBL
Protein-tyrosine kinase 2-beta Kinase Kd 6.66 CHEMBL
Serine/threonine-protein kinase RIO1 Kinase Kd 7 CHEMBL
Tyrosine-protein kinase receptor Tie-1 Kinase Kd 6.16 CHEMBL
Serine/threonine-protein kinase tousled-like 1 Kinase Kd 5.89 CHEMBL
Serine/threonine-protein kinase tousled-like 2 Kinase Kd 5.70 CHEMBL
NT-3 growth factor receptor Kinase Kd 5.07 CHEMBL
Tyrosine-protein kinase TXK Kinase Kd 5.82 CHEMBL
Casein kinase II subunit alpha Kinase Kd 6.04 CHEMBL
Casein kinase II subunit alpha' Kinase Kd 6.92 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 1B Kinase Kd 5.02 CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit epsilon Kinase Kd 6.44 CHEMBL
LIM domain kinase 2 Kinase Kd 5.10 CHEMBL
Serine/threonine-protein kinase STK11 Kinase Kd 6.51 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 3 Kinase Kd 5.46 CHEMBL
Maternal embryonic leucine zipper kinase Kinase Kd 5.58 CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 1 Kinase Kd 5.14 CHEMBL
Serine/threonine-protein kinase 26 Kinase Kd 5.12 CHEMBL
Serine/threonine-protein kinase Nek7 Kinase Kd 6.80 CHEMBL
Eukaryotic translation initiation factor 2-alpha kinase 4 Kinase Kd 7 CHEMBL
Insulin receptor-related protein Kinase Kd 5.80 CHEMBL
Interleukin-1 receptor-associated kinase 3 Kinase Kd 6.92 CHEMBL
Serine/threonine-protein kinase RIO3 Kinase Kd 7.04 CHEMBL
Serine/threonine-protein kinase SIK2 Kinase Kd 7.01 CHEMBL
SRSF protein kinase 1 Kinase Kd 6.80 CHEMBL
SRSF protein kinase 2 Kinase Kd 7 CHEMBL
Serine/threonine-protein kinase 33 Kinase Kd 6.66 CHEMBL
Serine/threonine-protein kinase TNNI3K Kinase Kd 5.75 CHEMBL
5'-AMP-activated protein kinase catalytic subunit alpha-2 Kinase Kd 5.33 CHEMBL
Ankyrin repeat and protein kinase domain-containing protein 1 Kinase Kd 5.37 CHEMBL
Discoidin domain-containing receptor 2 Kinase Kd 6.02 CHEMBL
Myotonin-protein kinase Kinase Kd 6 CHEMBL
Chaperone activity of bc1 complex-like, mitochondrial Kinase Kd 5.16 CHEMBL
Serine/threonine-protein kinase LATS2 Kinase Kd 5.10 CHEMBL
Leukocyte tyrosine kinase receptor Kinase Kd 5.20 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1 Kinase Kd 5.89 CHEMBL
Serine/threonine-protein kinase PAK 6 Kinase Kd 5.16 CHEMBL
Serine/threonine-protein kinase PAK 7 Kinase Kd 5.92 CHEMBL
NUAK family SNF1-like kinase 1 Kinase Kd 7.47 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 3 Kinase Kd 5.75 CHEMBL
Aurora kinase B Kinase Kd 6.31 CHEMBL
Tyrosine-protein kinase Blk Kinase Kd 6.19 CHEMBL
Bone morphogenetic protein receptor type-2 Kinase Kd 5.54 CHEMBL
Serine/threonine-protein kinase MARK1 Kinase Kd 6.16 CHEMBL
MAP/microtubule affinity-regulating kinase 4 Kinase Kd 6.01 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 4 Kinase Kd 5 CHEMBL
Tyrosine-protein kinase Mer Kinase Kd 6.09 CHEMBL
Mitogen-activated protein kinase kinase kinase 9 Kinase Kd 5.50 CHEMBL
Mitogen-activated protein kinase kinase kinase 10 Kinase Kd 5.16 CHEMBL
Mitogen-activated protein kinase kinase kinase 11 Kinase Kd 5.51 CHEMBL
Muscle, skeletal receptor tyrosine-protein kinase Kinase Kd 6.10 CHEMBL
Citron Rho-interacting kinase Kinase Kd 6.85 CHEMBL
Death-associated protein kinase 1 Kinase Kd 7.80 CHEMBL
Serine/threonine-protein kinase DCLK1 Kinase Kd 6.72 CHEMBL
Serine/threonine-protein kinase DCLK2 Kinase Kd 6.06 CHEMBL
Serine/threonine-protein kinase Nek5 Kinase Kd 6.24 CHEMBL
Serine/threonine-protein kinase Nek9 Kinase Kd 6.82 CHEMBL
Serine/threonine-protein kinase PAK 1 Kinase Kd 5.51 CHEMBL
Serine/threonine-protein kinase PAK 2 Kinase Kd 5.22 CHEMBL
Serine/threonine-protein kinase PAK 4 Kinase Kd 5.42 CHEMBL
AarF domain-containing protein kinase 4 Kinase Kd 6.52 CHEMBL
Serine/threonine-protein kinase SIK1 Kinase Kd 7.41 CHEMBL
Tyrosine-protein kinase Srms Kinase Kd 5.30 CHEMBL
Dual specificity testis-specific protein kinase 1 Kinase Kd 5.50 CHEMBL
Ephrin type-A receptor 1 Kinase Kd 6.14 CHEMBL
Serine/threonine-protein kinase PLK3 Kinase Kd 5.80 CHEMBL
Mitogen-activated protein kinase 6 Kinase Kd 5.92 CHEMBL
Mitogen-activated protein kinase 7 Kinase Kd 7.18 CHEMBL
Mitogen-activated protein kinase 15 Kinase Kd 6.29 CHEMBL
Serine/threonine-protein kinase D3 Kinase Kd 5.02 CHEMBL
cGMP-dependent protein kinase 2 Kinase Kd 5.80 CHEMBL
Interferon-induced, double-stranded RNA-activated protein kinase Kinase Kd 5.96 CHEMBL
Receptor-interacting serine/threonine-protein kinase 1 Kinase Kd 5.28 CHEMBL
Tyrosine-protein kinase Fes/Fps Kinase Kd 6.28 CHEMBL
Fibroblast growth factor receptor 4 Kinase Kd 5.70 CHEMBL
Proto-oncogene tyrosine-protein kinase ROS Kinase Kd 6.22 CHEMBL
Ribosomal protein S6 kinase alpha-1 Kinase Kd 6.38 CHEMBL
Ribosomal protein S6 kinase alpha-4 Kinase Kd 6.85 CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Kinase Kd 5.12 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2 Kinase Kd 5.68 CHEMBL
Misshapen-like kinase 1 Kinase Kd 5.05 CHEMBL
Serine/threonine-protein kinase TBK1 Kinase Kd 7.04 CHEMBL
Interleukin-1 receptor-associated kinase 4 Kinase Kd 5.92 CHEMBL
Cyclin-dependent kinase 4 Kinase Kd 6.06 CHEMBL
Cyclin-dependent kinase-like 2 Kinase Kd 5.89 CHEMBL
Protein delta homolog 1 Membrane other Kd 5.20 CHEMBL
Ephrin type-B receptor 6 Kinase Kd 6.52 CHEMBL
Serine/threonine-protein kinase/endoribonuclease IRE1 Kinase Kd 5.92 CHEMBL
G protein-coupled receptor kinase 4 Kinase Kd 6.77 CHEMBL
G protein-coupled receptor kinase 7 Kinase Kd 5.58 CHEMBL
Homeodomain-interacting protein kinase 2 Kinase Kd 6 CHEMBL
Homeodomain-interacting protein kinase 3 Kinase Kd 5.89 CHEMBL
Homeodomain-interacting protein kinase 4 Kinase Kd 6.66 CHEMBL
Serine/threonine-protein kinase ICK Kinase Kd 5.72 CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit alpha Kinase Kd 6.08 CHEMBL
Interleukin-1 receptor-associated kinase 1 Kinase Kd 6.66 CHEMBL
Mitogen-activated protein kinase kinase kinase 13 Kinase Kd 6.23 CHEMBL
Mitogen-activated protein kinase kinase kinase 2 Kinase Kd 6.24 CHEMBL
Mitogen-activated protein kinase kinase kinase 3 Kinase Kd 5.89 CHEMBL
Serine/threonine-protein kinase 38 Kinase Kd 5.24 CHEMBL
Serine/threonine-protein kinase NIM1 Kinase Kd 5.36 CHEMBL
Serine/threonine-protein kinase RIO2 Kinase Kd 5.58 CHEMBL
SRSF protein kinase 3 Kinase Kd 6.77 CHEMBL
STE20/SPS1-related proline-alanine-rich protein kinase Kinase Kd 5.80 CHEMBL
Mitogen-activated protein kinase kinase kinase 7 Kinase Kd 5.51 CHEMBL
Serine/threonine-protein kinase TAO1 Kinase Kd 5.89 CHEMBL
Serine/threonine-protein kinase TAO3 Kinase Kd 5.72 CHEMBL
Serine/threonine-protein kinase ULK1 Kinase Kd 6.57 CHEMBL
Serine/threonine-protein kinase ULK2 Kinase Kd 7.10 CHEMBL
Serine/threonine-protein kinase ULK3 Kinase Kd 6.54 CHEMBL
Mitogen-activated protein kinase kinase kinase 19 Kinase Kd 7.72 CHEMBL
Homeodomain-interacting protein kinase 1 Kinase Kd 6.07 CHEMBL
Serine/threonine-protein kinase PLK2 Kinase Kd 5.62 CHEMBL
Receptor-interacting serine/threonine-protein kinase 4 Kinase Kd 5.01 CHEMBL
Uncharacterized serine/threonine-protein kinase SBK3 Kinase Kd 5.54 CHEMBL
Tyrosine-protein kinase Fer Kinase Kd 5.96 CHEMBL
Megakaryocyte-associated tyrosine-protein kinase Kinase Kd 5.77 CHEMBL
Phosphatidylinositol 4-kinase beta Kinase Kd 5.77 CHEMBL
Serine/threonine-protein kinase SIK3 Kinase Kd 5.72 CHEMBL
Wee1-like protein kinase 2 Kinase Kd 5.22 CHEMBL
Bone morphogenetic protein receptor type-1B Kinase Kd 6.39 CHEMBL
Serine/threonine-protein kinase SBK1 Kinase Kd 6.10 CHEMBL
Serine/threonine-protein kinase Nek3 Kinase Kd 6.19 CHEMBL
Peripheral plasma membrane protein CASK Kinase Kd 5.55 CHEMBL
Serine/threonine-protein kinase PRP4 homolog Kinase Kd 6.41 CHEMBL
Mitogen-activated protein kinase kinase kinase 12 Kinase Kd 5.20 CHEMBL
Serine/threonine-protein kinase Sgk3 Kinase Kd 5.60 CHEMBL
Eukaryotic translation initiation factor 2-alpha kinase 1 Kinase Kd 6 CHEMBL
Serine/threonine-protein kinase TAO2 Kinase Kd 6.12 CHEMBL
SNF-related serine/threonine-protein kinase Kinase Kd 6.64 CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma Kinase Kd 5.39 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5 Kinase Kd 6.44 CHEMBL
Serine/threonine-protein kinase Nek11 Kinase Kd 5.92 CHEMBL
Myosin light chain kinase 3 Kinase Kd 5.01 CHEMBL
Leucine-rich repeat serine/threonine-protein kinase 2 Kinase Kd 6.06 CHEMBL
Dual serine/threonine and tyrosine protein kinase Kinase Kd 5.77 CHEMBL
Bromodomain-containing protein 4 Nuclear other Kd 6.79 CHEMBL
Serine/threonine-protein kinase Nek6 Kinase Kd 6.92 CHEMBL
cGMP-dependent protein kinase 1 Kinase Kd 5.42 CHEMBL
Serine/threonine-protein kinase Nek4 Kinase Kd 5.80 CHEMBL
Bromodomain testis-specific protein Nuclear other IC50 6.47 CHEMBL
Serine/threonine-protein kinase Nek1 Kinase Kd 5.47 CHEMBL
Uncharacterized protein FLJ45252 Unclassified Kd 6.56 CHEMBL
Uncharacterized aarF domain-containing protein kinase 1 Kinase Kd 6.64 CHEMBL
Tyrosine-protein kinase JAK3 Kinase INHIBITOR IC50 5.99 SCIENTIFIC LITERATURE
Tyrosine-protein kinase JAK1 Kinase INHIBITOR IC50 6.97 SCIENTIFIC LITERATURE
Non-receptor tyrosine-protein kinase TYK2 Kinase INHIBITOR IC50 6.39 SCIENTIFIC LITERATURE
Cyclin-dependent kinase-like 5 Kinase Kd 5.14 CHEMBL
Rho-associated protein kinase 1 Kinase Kd 5.68 CHEMBL
Calcium-dependent protein kinase 1 Kinase Kd 5.92 CHEMBL
Serine/threonine-protein kinase PknB Kinase Kd 7 CHEMBL

External reference:

IDSource
6L1XP550I6 UNII
1374744-69-0 SECONDARY_CAS_RN
4038661 VANDF
C3886623 UMLSCUI
CHEBI:91408 CHEBI
2TA PDB_CHEM_ID
CHEMBL1287853 ChEMBL_ID
16722836 PUBCHEM_CID
DB12500 DRUGBANK_ID
CHEMBL4297216 ChEMBL_ID
D10630 KEGG_DRUG
9707 INN_ID
C528327 MESH_SUPPLEMENTAL_RECORD_UI
5716 IUPHAR_LIGAND_ID
789359000 SNOMEDCT_US
789368003 SNOMEDCT_US
895592002 SNOMEDCT_US
321679 MMSL
d09354 MMSL
018090 NDDF
2197490 RXNORM
6L1XP550I6 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Inrebic HUMAN PRESCRIPTION DRUG LABEL 1 59572-720 CAPSULE 100 mg ORAL NDA 31 sections