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GSK620 | GSK620 : BD2 selective inhibitor of BRD2, BRD3, BRD4, BRDT
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
BRD2
  • IC50:285 nM
  • IC50:318 nM
  • Kd:15 nM
    BRD3
    • IC50:72 nM
    • IC50:63 nM
    • Kd:12 nM
      BRD4
      • IC50:81 nM
      • IC50:63 nM
      • Kd:6 nM
      • Kd:50 nM
      • IC50:790 nM
      • IC50:63 nM
      BRDT
      • IC50:184 nM
      • IC50:200 nM
      • Kd:15 nM
        Inhibitor
        up to 10 uM

        Selectivity

        In Vitro Selectivity Assessment
        Selectivity Assessment Description:
        Selectivity within target family - BROMOScan (DiscoverX) (34 tested): selective for the BD2 domain o ...

        Potency
        Cellular
        In Vitro

        BRD2

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.1021/acs.jmedchem.0c00796

        BRD3

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.1021/acs.jmedchem.0c00796

        BRD4

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.1021/acs.jmedchem.0c00796

        BRDT

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.1021/acs.jmedchem.0c00796

        In Vivo Validations

        Rat
        Dose: 1 mg/Kg
        Route of delivery: Intravenous
        Plasma half life: 1.1 h
        Systemic clearance: 12 mL/min/kg
        Volume of Distribution at Steady-State: 0.8 L/Kg

        DOI Reference: 10.1021/acs.jmedchem.0c00796

        Dose: 3 mg/Kg
        Route of delivery: Oral
        Fb : 99.84%
        Bioavailability: 67%

        DOI Reference: 10.1021/acs.jmedchem.0c00796

        Dog
        Dose: 0.5 mg/Kg
        Route of delivery: Intravenous
        Plasma half life: 5.7 h
        Systemic clearance: 2 mL/min/kg
        Volume of Distribution at Steady-State: 1.0 L/kg

        DOI Reference: 10.1021/acs.jmedchem.0c00796

        Dose: 1.0 mg/Kg
        Route of delivery: Oral
        Fb : 99.62%
        Bioavailability: 57%

        DOI Reference: 10.1021/acs.jmedchem.0c00796

        Orthogonal Probes def

        GSK046
        GSK973
        ABBV-744

        Chemical Information

        Molecular Formula C18H19N3O3
        SMILEs CNC(=O)c1cc(C(=O)NC2CC2)cn(Cc2ccccc2)c1=O
        InChI InChI=1S/C18H19N3O3/c1-19-17(23)15-9-13(16(22)20-14-7-8-14)11-21(18(15)24)10-12-5-3-2-4-6-12/h2-6,9,11,14H,7-8,10H2,1H3,(H,19,23)(H,20,22)
        Molecular weight 325.14 Da
        AlogP 1.1483999999999992
        HBond acceptors 6
        HBond donors 2
        Atoms 43

        Vendors

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

        Expert Reviews

        by SERP
        (on 15 Feb 2022 )
        Cellular Use Rating
        In Model Organisms
        ( The reviewer did not leave any comments )
        by SERP
        (on 25 Feb 2022 )
        Cellular Use Rating
        In Model Organisms
        ...
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