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PTPN1-Degrader-75 | PTPN1-Degrader-75 : Degrader (PROTAC) of PTPN1
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PTPN1
    • DC50:200 nM
    Degrader (PROTAC)
    up to 1 µM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Several PTP members including PTP1B, SHP1, SHP2, LYP, and CD45 were tested for their degradation eff ...

    Potency
    Cellular
    In Vitro

    PTPN1

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acs.jmedchem.4c00356

    Chemical Information

    Molecular Formula C61H92N4O11
    SMILEs CC1(C)CCC2(C(=O)NCCCCCCOCCOCCOCCOCCCCCC(=O)Nc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)CCC3(C)C(=CCC4C5(C)CCC(O)C(C)(C)C5CCC43C)C2C1
    InChI InChI=1S/C61H92N4O11/c1-56(2)27-29-61(30-28-59(6)42(43(61)40-56)19-21-47-58(5)25-24-48(66)57(3,4)46(58)23-26-60(47,59)7)55(72)62-31-12-8-9-13-32-73-34-36-75-38-39-76-37-35-74-33-14-10-11-18-49(67)63-44-17-15-16-41-51(44)54(71)65(53(41)70)45-20-22-50(68)64-52(45)69/h15-17,19,43,45-48,66H,8-14,18,20-40H2,1-7H3,(H,62,72)(H,63,67)(H,64,68,69)
    Molecular weight 1056.68 Da
    AlogP 9.4923
    HBond acceptors 15
    HBond donors 4
    Atoms 168

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    Expert Reviews

    by SERP
    (on 1 Sept 2024 )
    Cellular Use Rating
    PROTAC 75 has been characterised only in cell-based assays. It shows reasonable target degradation across a range of concentrations with no evidence of a Hook effect. There is evidence that the degradation...
    by SERP+
    (on 31 Oct 2024 )
    Cellular Use Rating
    Proteomic profiling would be necessary to fully evaluate this compounds' selectivity.
    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