General
Preferred name
GW788388
Synonyms
GW 788388 ()
cpd 13d ()
GW-788388 ()
P&D ID
PD010684
CAS
452342-67-5
Tags
available
probe
drug candidate
Drug indication
Solid tumour/cancer
Probe info
Probe type
calculated probe
experimental probe
P&D approved
Probe selectivity
protein-selective
Probe targets
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
COMMENT The data for the probe was recorded some time ago. Today, kinase selectivity panels would typically be more comprehensive. Further selectivity testing should be considered. Aug 26 2021 - 9:45am
DESCRIPTION GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-¦Â type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
PRICE 84
MOA Inhibitor (Chemical Probes.org)
DESCRIPTION Potent ATP-competitive TGF-betaRI inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION Potent and selective inhibitor of TGF-betaRI (Tocriscreen Plus)
DESCRIPTION GW788388 is a selective inhibitor of TGF-beta type I receptor (TGF-βR1/ALK5; IC50 = 18 nM) with a much improved pharmacokinetic profile compared with SB431542. It inhibited both the TGF-beta type I and type II receptor kinase activities, but not that of the related bone morphogenic protein type II receptor. (BOC Sciences Bioactive Compounds)
DESCRIPTION GW788388 is a potent and selective inhibitor of ALK5, and it also inhibits TGF-(beta) type II receptor and activin type II receptor activities. (TargetMol Bioactive Compound Library)
Cell lines
1
Organisms
0
Compound Sets
15
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
Chemical Probes.org
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugMAP
High-quality chemical probes
MedChem Express Bioactive Compound Library
Probe Miner (suitable probes)
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
External IDs
22
Properties
(calculated by RDKit )
Molecular Weight
425.19
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
2
Rotatable Bonds
5
Ring Count
5
Aromatic Ring Count
4
cLogP
4.11
TPSA
92.79
Fraction CSP3
0.2
Chiral centers
0.0
Largest ring
6.0
QED
0.5
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target Type
Enzyme-Linked Receptors
Target
TGF-¦Â Receptor
TGF-??Receptor
LCK, MAPK14, TGFBR1
ALK5 inhibitor
TGFBR1
TGF-β Receptor
ALK5
Pathway
Angiogenesis
Stem Cells
Tyrosine Kinase/Adaptors
TGF-beta/Smad
Primary Target
TGF-? Receptors
MOA
Inhibitor
ALK tyrosine kinase receptor inhibitor
Target class
Protein kinase
Target subclass
TKL
Source data