General
Preferred name
padnarsertib
Synonyms
KPT-9274 ()
KPT 9274 ()
PAK4-IN-1 ()
KPT 9274 ( ATG-019) ()
KPT9274 ()
P&D ID
PD060931
CAS
1643913-93-2
Tags
available
drug candidate
Drug indication
Solid tumour/cancer
non-Hodgkins lymphoma
Non-hodgkin lymphoma
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
Padnarsertib (KPT-9274) is an orally bioavailable, dual PAK4/Nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with IC50s of <100 nM and 120 nM, respectively[1][2][3].
PRICE
262
DESCRIPTION
KPT-9274 is a small molecule that has reported inhibitory activity against PAK4 and NAMPT . It is being developed by Karyopharm Therapeutics for anti-cancer efficacy in solid tumours and in B cell malignancies . KPT-9274 is suggested to act as an allosteric modulator of PAK4 that does not interfere with the enzyme's kinase activity (in contrast to the type 1 ATP-competitive PAK kinase inhibitor ). It produces dose-dependent antitumour effects in solid and haematologic cell lines at low nanomolar concentrations . KPT-9274 is claimed as example 728 in patent WO2015003166A1 .
The chemical structure of KPT-9274 is identical to that which was submitted to the WHO for the INN padnarsertib (proposed INN list 126, Jan 2022). (GtoPdb)
The chemical structure of KPT-9274 is identical to that which was submitted to the WHO for the INN padnarsertib (proposed INN list 126, Jan 2022). (GtoPdb)
DESCRIPTION
KPT9274 (PAK4-IN-1) is a non-competitive dual inhibitor of PAK4 and NAMPT(IC50= ~120 nM). It is an orally bioavailable small molecule.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
12
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugMAP
Guide to Pharmacology
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
16
Molecular Weight
610.22
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
2
Rotatable Bonds
7
Ring Count
6
Aromatic Ring Count
5
cLogP
7.08
TPSA
101.46
Fraction CSP3
0.17
Chiral centers
0.0
Largest ring
6.0
QED
0.19
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
NAMPT
PAK4
PAK
NAMPT,PAK
MOA
PAK inhibitor
Allosteric inhibitor that degrades PAK4
NAMPT inhibitor
Member status
member
Pathway
Cytoskeletal Signaling
Metabolism
Cell Cycle/DNA Damage
cytoskeleton
Metabolic Enzyme/Protease
Source data
