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RO-275 | RO-275 : Inhibitor of HCN1
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
HCN1
    • IC50:46 nM
    • IC50:49 nM
    • IC50:269 nM
    Inhibitor
    up to 1 uM

    Selectivity

    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    Selectivity within target family: 311/100/302-fold more selective over HCN2/3/4 Selectivity outside ...
    Selectivity Assessment Description:
    Used electrophysiological recordings of hippocampal neurons in brain slices from HCN1 KO mice and WT ...

    Potency
    Cellular
    In Vitro

    HCN1

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1016/j.chembiol.2023.11.004

    In Vivo Validations

    Rat
    Dose: 10 mg/kg
    Route of delivery: Oral
    Organ of interest (O): brain

    DOI Reference: 10.1016/j.chembiol.2023.11.004

    Chemical Information

    Molecular Formula C18H14ClN5O
    SMILEs Cc1c(C#Cc2nc(C(N)=O)n(-c3cccnc3)c2C)ccnc1Cl
    InChI InChI=1S/C18H14ClN5O/c1-11-13(7-9-22-16(11)19)5-6-15-12(2)24(18(23-15)17(20)25)14-4-3-8-21-10-14/h3-4,7-10H,1-2H3,(H2,20,25)
    Molecular weight 351.09 Da
    AlogP 2.4312400000000007
    HBond acceptors 6
    HBond donors 2
    Atoms 39

    References

    Publications

    Cross References

    Expert Reviews

    by SERP
    (on 9 Dec 2024 )
    Cellular Use Rating
    In Model Organisms
    RO-275 is a primary carboxamide derivative with potent HCN1 cation channel inhibitory activity (submicromolar concentrations), as shown in in vitro electrophysiology experiments. RO-275 is highly selective...
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