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VT103 | Inhibitor of TEAD1
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 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
TEAD1
  • ΔTm (°C):8.3
  • IC50:1.02 ± 0.09 nM
  • GI50:1-21 nM
Inhibitor
up to 3 uM

Selectivity

In Cell Selectivity Assessment

Potency: GI50

Potency Assay Off-Target:
Anti-proliferation activity in a panel of mesothelioma cell lines
Selectivity Assessment Description:
<strong>GI50 (nM)</strong> NCI-H226 1, NCI-H2373 2, Mero-48a 5, SDM103T2 2, NCI-H2052 10, ACC-MES ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Thermal Shift Assays (TSA)
Selectivity Assessment Description:
∆Tm (ºC) 4.1 TEAD2, 1.0 TEAD3, 1.9 TEAD4

Potency
Cellular
In Vitro

TEAD1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/1535-7163.MCT-20-0717

In Vivo Validations

Mouse
Dose: 10 mg/Kg
Route of delivery: Intravenous, Oral
Plasma half life: 13.2 h (IV)
Systemic clearance: 4.7 mL/min/kg (IV)

DOI Reference: 10.1158/1535-7163.MCT-20-0717

Negative Control Compounds

VT106

Orthogonal Probes def

VT104

Chemical Information

Molecular Formula C18H17F3N4O2S
SMILEs CNS(=O)(=O)c1ccc(Nc2ccc(C(F)(F)F)cc2)c(-c2cn(C)cn2)c1
InChI InChI=1S/C18H17F3N4O2S/c1-22-28(26,27)14-7-8-16(15(9-14)17-10-25(2)11-23-17)24-13-5-3-12(4-6-13)18(19,20)21/h3-11,22,24H,1-2H3
Molecular weight 410.10 Da
AlogP 0.0
HBond acceptors 6
HBond donors 2
Atoms 45

References

Publications

Cross References

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Expert Reviews

by SERP
(on 1 Oct 2021 )
Cellular Use Rating
In Model Organisms
SPR data or similar demonstrating the direct interaction between VT103 and TEAD1 (vs TEAD2-4) would be desirable. Also, CETSA in cells would be a useful addition, as well as some selectivity screens against...
by SERP
(on 5 Oct 2021 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 1 Nov 2021 )
Cellular Use Rating
In Model Organisms
This is a solid probe for TEAD1 that functions by inhibiting TEAD1 autopalmitoylation, and, thus, inhibiting interaction between TEAD1 and YAP-TAZ. In terms of probe validation, although selectivity over...
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