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WLB-89462 | WLB-89462 : Modulator of TMEM97
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 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
TMEM97
    • Ki:13 ± 5 nM
    Modulator
    up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Highly selective vs both the σ1R (IC50 1777 nM) and a general panel of 180 different targets, compos ...

    Potency
    Cellular
    In Vitro

    TMEM97

    Mode of Action: Modulator

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acs.jmedchem.3c01060

    In Vivo Validations

    Rat
    Dose: 10 mg/Kg
    Route of delivery: Oral
    Cmax: 900 ng/mL
    Tmax: 0.8 h
    Area Under the Curve:: 2998 ng*h/mL
    Bioavailability: 51%

    DOI Reference: 10.1021/acs.jmedchem.3c01060

    Dose: 1 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 1.0 h
    Systemic clearance: 1.7 L/h/Kg
    Cmax: 2022 ng/mL
    Tmax: 0.3 h
    Area Under the Curve:: 593 ng*h/mL
    Volume of Distribution at Steady-State: 0.8 L/Kg

    DOI Reference: 10.1021/acs.jmedchem.3c01060

    Chemical Information

    Molecular Formula C21H29N5O3
    SMILEs CCc1ncc(-c2cc(C)no2)c(C2CCN(CC(=O)N3CCOCC3)CC2)n1
    InChI InChI=1S/C21H29N5O3/c1-3-19-22-13-17(18-12-15(2)24-29-18)21(23-19)16-4-6-25(7-5-16)14-20(27)26-8-10-28-11-9-26/h12-13,16H,3-11,14H2,1-2H3
    Molecular weight 399.23 Da
    AlogP 0.0
    HBond acceptors 8
    HBond donors --
    Atoms 58

    Vendors

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    Expert Reviews

    No SERP comments found for WLB-89462

    Probe WLB-89462 is in the process of SERP review.

    Please continue to check back for new reviews and commentary.