Chemical Probes logo
GSK778 | GSK778 : BD1 selective inhibitor of BRD2, BRD3, BRD4, BRDT
RATINGS:
Cellular Use: (1 reviews)

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

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
BRD2
  • IC50:75 nM
  • Kd:13 nM
  • IC50:50 nM
  • IC50:100 nM
BRD3
  • IC50:41 nM
  • Kd:5 nM
    BRD4
    • IC50:41 nM
    • Kd:5.9 nM
      BRDT
      • IC50:143 nM
      • Kd:18 nM
        Inhibitor
        up to 1 uM

        Selectivity

        In Vitro Selectivity Assessment
        Selectivity Assessment Description:
        Selectivity within target family: Excellent selectivity against other BRD-containing proteins (Bromo ...

        Potency
        Cellular
        In Vitro

        BRD2

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.1021/acs.jmedchem.0c00566

        BRD3

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.1021/acs.jmedchem.0c00566

        BRD4

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.1021/acs.jmedchem.0c00566

        BRDT

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.1021/acs.jmedchem.0c00566

        In Vivo Validations

        Mouse
        Dose: 10 mg/Kg
        Route of delivery: Intraperitoneal
        Plasma half life: 0.9 h (predominant), 8.2 (terminal)
        Cmax: 2.40 uM
        Tmax: 0.25-0.50 h
        Area Under the Curve:: 3.34 uM*h

        DOI Reference: 10.1021/acs.jmedchem.0c00566

        Orthogonal Probes def

        ABBV-744
        GSK789

        Chemical Information

        Molecular Formula C30H33N5O3
        SMILEs COCc1nc2cnc3cc(-c4c(C)noc4C)c(OC[C@H]4CCNC4)cc3c2n1[C@H](C)c1ccccc1
        InChI InChI=1S/C30H33N5O3/c1-18-29(20(3)38-34-18)24-12-25-23(13-27(24)37-16-21-10-11-31-14-21)30-26(15-32-25)33-28(17-36-4)35(30)19(2)22-8-6-5-7-9-22/h5-9,12-13,15,19,21,31H,10-11,14,16-17H2,1-4H3/t19-,21+/m1/s1
        Molecular weight 511.26 Da
        AlogP 5.600340000000005
        HBond acceptors 8
        HBond donors 1
        Atoms 71

        Vendors

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

        Expert Reviews

        by SERP
        (on 25 Feb 2026 )
        Cellular Use Rating
        In Model Organisms
        A high-quality chemical probe for BD1 domains of BET proteins; can be paired with the BD2-selective probe GSK046 (from same chemical series) to compare BD1 vs BD2 inhibition. Can also be paired with GSK789,...
        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