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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 public comments)
        by SERP
        (on 25 Feb 2022)
        Cellular Use Rating
        In Model Organisms
        ...
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