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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 public 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