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VT104 | VT104 : Inhibitor of TEAD1, TEAD2, TEAD3, TEAD4
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 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:8.6 Celsius
  • IC 50:10.4 ± 0.8 nM
  • GI 50:16-98 nM
TEAD2
  • ΔTm:5.4 Celsius
    TEAD3
    • ΔTm:8.2 Celsius
      TEAD4
      • ΔTm:4.3 Celsius
        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 16, NCI-H2373 26, Mero-48a 98, SDM103T2 60, NCI-H2052 33, ACC ...

        Potency
        Cellular
        In Vitro

        TEAD1

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? Yes

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

        TEAD2

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? Yes

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

        TEAD3

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? Yes

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

        TEAD4

        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: 24.2 h (IV)
        Systemic clearance: 1.8 mL/min/kg (IV)

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

        Negative Control Compounds

        VT106

        Orthogonal Probes def

        VT103

        Chemical Information

        Molecular Formula C25H19F3N2O
        SMILEs C[C@H](NC(=O)c1ccc2c(-c3ccc(C(F)(F)F)cc3)cccc2c1)c1ccccn1
        InChI InChI=1S/C25H19F3N2O/c1-16(23-7-2-3-14-29-23)30-24(31)19-10-13-22-18(15-19)5-4-6-21(22)17-8-11-20(12-9-17)25(26,27)28/h2-16H,1H3,(H,30,31)/t16-/m0/s1
        Molecular weight 420.14 Da
        AlogP 0.0
        HBond acceptors 3
        HBond donors 1
        Atoms 50

        References

        Publications

        Cross References

        canSARChEMBLPubMed

        Vendors

        Note: This is not an exhaustive list and does not indicate endorsement by the portal.

        Expert Reviews

        by SERP
        (on 14 Sept 2021 )
        Cellular Use Rating
        In Model Organisms
        The Hippo pathway governs organ size and tissue homeostasis, regulating several fundamental cellular processes such as cell proliferation, migration, apoptosis and cell-fate decision. Yes-associated...
        by SERP
        (on 1 Oct 2021 )
        Cellular Use Rating
        In Model Organisms
        ( The reviewer did not leave any comments )
        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