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GW788388 | Inhibitor of TGFBR1
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
TGFBR1
  • IC50:18 nM
  • IC50:93 nM
Inhibitor
up to 1 uM, max 10 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - p38alpha: 7.2 uM

Potency Assay Off-Target:
In an in vitro panel of kinases, GW788388 only inhibited p38a >50% at 10 uM (panel included: P70S6K, ...
Selectivity Assessment Description:
In an in vitro panel of kinases, GW788388 only inhibited p38a >50% (IC50 of 7.28 µM) at 10 uM ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
In U2OS cells, GW788388 had no effect on BMP-induced Smad1/5 phosphorylation.

Potency
Cellular
In Vitro

TGFBR1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

In Vivo Validations

Sprague Dawley rat, various mice
Dose: 2 mg/kg, 4 mg/kg
Route of delivery: Intravenous, Oral
Plasma half life: 1.3 h (rat, IV)
Systemic clearance: 20 mL/min/kg (rat, IV)
Organ of interest (O): mouse liver, mouse kidney
Target engagement assay: In DMN-induced mouse models of liver disease and in chemically-induced mouse models of renal fibrosis, GW788388 inhibited TGF-beta-induced collagen IA1 mRNA expression. In db/db mouse model of diabetic retinopathy, GW788388 (2 mg/kg, oral) decreased TGF-beta-induced expression of extracellular matrix (ECM) mRNAs.

Reference: --

Chemical Information

Molecular Formula C25H23N5O2
SMILEs O=C(NC1CCOCC1)c1ccc(-c2cc(-c3c[nH]nc3-c3ccccn3)ccn2)cc1
InChI InChI=1S/C25H23N5O2/c31-25(29-20-9-13-32-14-10-20)18-6-4-17(5-7-18)23-15-19(8-12-27-23)21-16-28-30-24(21)22-3-1-2-11-26-22/h1-8,11-12,15-16,20H,9-10,13-14H2,(H,28,30)(H,29,31)
Molecular weight 425.19 Da
AlogP 0.0
HBond acceptors 7
HBond donors 2
Atoms 55

References

Publications

    Cross References

    canSARChEMBLBindingDBPubMed

    Vendors

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    Expert Reviews

    by SERP
    (on 26 Aug 2021 )
    Cellular Use Rating
    In Model Organisms
    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.
    by SERP
    (on 21 Sept 2021 )
    Cellular Use Rating
    The probe validation is a bit meagre and based on one assay from 2006. The assay, a fluorescence polarization displacement assay using rhodamine labelled ATP, is known to have a large variability (much...
    Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria