General
Preferred name
ixazomib
Synonyms
MLN2238 ()
MLN 2238 ()
Ixazomib (MLN2238) ()
MLN-2238 ()
MLN-9708 FREE BASE ()
P&D ID
PD003323
CAS
1072833-77-2
Tags
available
covalent binder
drug
nuisance
Approved by
FDA
PMDA
EMA
First approval
2015
Drug Status
approved
investigational
Max Phase
3.0
Drug indication
Neoplasm
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Ixazomib is the first approved oral proteasome inhibitor. Ixazomib reversibly inhibits 20S proteasome activity. Like , ixazomib primarily inhibits the chymotrypsin-like (β5) proteolytic site within the 20S proteasome, but its pharmacokinetics, pharmacodynamics, and antitumor activity are superior to those of bortezomib . (GtoPdb)
DESCRIPTION Ixazomib (MLN2238) is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (¦Â5) site of the 20S proteasome with an IC50 of 3.4 nM (Ki of 0.93 nM).
PRICE 110
DESCRIPTION Ixazomib (MLN2238) , a second generation, boron-containing peptide proteasome inhibitor (PI), inhibits the chymotrypsin-like proteolytic (??5) site of the 20S proteasome (IC50/Ki: 3.4/0.93 nM, in cell-free assays), also inhibits the caspase-like (??1) and trypsin-like (??2) proteolytic sites (IC50: 31/3500 nM).
DESCRIPTION inhibitor of 20S proteasome at the chymotrypsin-like proteolytic (beta-5) site (Informer Set)
DESCRIPTION Ixazomib (MLN2238) , a second generation, boron-containing peptide proteasome inhibitor (PI), inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome (IC50/Ki: 3.4/0.93 nM, in cell-free assays), also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites (IC50: 31/3500 nM). (TargetMol Bioactive Compound Library)
Cell lines
7
Organisms
0
Compound Sets
25
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
Cayman Chemical Bioactives
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CovalentInDB
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
Informer Set
MedChem Express Bioactive Compound Library
NCATS Inxight Approved Drugs
Nuisance compounds in cellular assays
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
External IDs
34
Properties
(calculated by RDKit )
Molecular Weight
360.08
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
4
Rotatable Bonds
7
Ring Count
1
Aromatic Ring Count
1
cLogP
1.27
TPSA
98.66
Fraction CSP3
0.43
Chiral centers
1.0
Largest ring
6.0
QED
0.55
Structural alerts
1
Protein disruption
Proteosome inhibition
Nuisance compounds
Custom attributes
(extracted from source data)
Target
PSMB5
Autophagy,Proteasome
Proteasome
20S proteasome
caspase-like (β1)
Compound status
clinical
Indication
multiple myeloma
MOA
Proteasome inhibitor
Pathway
Apoptosis
Autophagy
Proteases/Proteasome
Ubiquitination
Metabolic Enzyme/Protease
Source data