General
Preferred name
TAK-733
Synonyms
TAK733 ()
TAK 733 ()
Tak 733 ()
Rec-4881 ()
Mek inhibitor tak-733 ()
P&D ID
PD010918
CAS
1035555-63-5
Tags
available
drug candidate
Drug indication
Solid tumour/cancer
Metastatic melanoma
Drug Status
investigational
Max Phase
2.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
TAK-733 is a potent and selective MEK inhibitor with an allosteric binding mode, that was designed as a novel cancer chemotherapeutic .
(GtoPdb)
DESCRIPTION
TAK-733 is a potent and selective MEK allosteric site inhibitor with an IC50 of 3.2 nM.
PRICE
209
DESCRIPTION
TAK-733 is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity. MEK inhibitor TAK-733 selectively binds to and inhibits the activity of MEK1/2, preventing the activation of MEK1/2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK1/2 (MAP2K1/K2) are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK pathway and are often upregulated in a variety of tumor cell types. Check for active clinical trials or closed clinical trials using this agent.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
TAK-733 is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
2
Organisms
0
Compound Sets
15
AdooQ Bioactive Compound Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Clinical kinase drugs
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
28
Molecular Weight
504.01
Hydrogen Bond Acceptors
8
Hydrogen Bond Donors
3
Rotatable Bonds
5
Ring Count
3
Aromatic Ring Count
3
cLogP
1.07
TPSA
109.38
Fraction CSP3
0.24
Chiral centers
1.0
Largest ring
6.0
QED
0.45
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Targets
MAP2K1
Target
MEK
MEK1
MOA
MEK inhibitor
Pathway
MAPK
MAPK/ERK Pathway
Source data
