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AZD5153 | AZD5153 : Bivalent inhibitor of BD1-BD2 of BRD4, BRD2, BRDT, BRD3
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
BRD4
  • Ki:5 nM
  • IC50:25 nM
  • IC50:12.6 nM
  • GI50:5 nM
BRD2
  • Ki:100 nM
    BRDT
    • Ki:100 nM
      BRD3
      • Ki:50 nM
        Bivalent BD1-BD2
        up to 1 uM

        Selectivity

        In Vitro Selectivity Assessment
        Potency Assay Off-Target:
        AZD5153 (10 μM) was tested for activity across 32 bromodomains in the Bromoscan panel showing inhere ...

        Potency
        Cellular
        In Vitro

        BRD4

        Mode of Action: Bivalent BD1-BD2

        Structure-Activity-Relationship data available? Yes

        DOI Reference: 10.1021/acs.jmedchem.6b00070

        BRD2

        Mode of Action: Bivalent BD1-BD2

        Structure-Activity-Relationship data available? Yes

        DOI Reference: 10.1021/acs.jmedchem.6b00070

        BRDT

        Mode of Action: Bivalent BD1-BD2

        Structure-Activity-Relationship data available? Yes

        DOI Reference: 10.1021/acs.jmedchem.6b00070

        BRD3

        Mode of Action: Bivalent BD1-BD2

        Structure-Activity-Relationship data available? Yes

        DOI Reference: 10.1021/acs.jmedchem.6b00070

        In Vivo Validations

        Rat
        Dose: unknown
        Route of delivery: Oral
        Systemic clearance: 4 mL/min/kg
        Bioavailability: 81%
        Volume of Distribution at Steady-State: 0.9 L/Kg

        DOI Reference: 10.1021/acs.jmedchem.6b00070

        Dog
        Dose: unknown
        Route of delivery: Oral
        Systemic clearance: 6 mL/min/kg
        Bioavailability: 55%
        Volume of Distribution at Steady-State: 0.4 L/Kg

        DOI Reference: 10.1021/acs.jmedchem.6b00070

        Orthogonal Probes def

        GSK-762 (i-BET-762)
        JQ1
        BIRABRESIB

        Chemical Information

        Molecular Formula C25H33N7O3
        SMILEs COc1nnc2ccc(N3CCC(c4ccc(OCCN5CCN(C)C(=O)[C@H]5C)cc4)CC3)nn12
        InChI InChI=1S/C25H33N7O3/c1-18-24(33)29(2)14-15-30(18)16-17-35-21-6-4-19(5-7-21)20-10-12-31(13-11-20)23-9-8-22-26-27-25(34-3)32(22)28-23/h4-9,18,20H,10-17H2,1-3H3/t18-/m1/s1
        Molecular weight 479.26 Da
        AlogP 0.0
        HBond acceptors 10
        HBond donors --
        Atoms 68

        References

        Publications

        Cross References

        canSARChEMBLBindingDBPDBPubMed

        Vendors

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

        Expert Reviews

        by SERP
        (on 17 Apr 2023 )
        Cellular Use Rating
        In Model Organisms
        AZD5153 is a high quality compound that has progressed to the clinical trial stage. The compound binds both bromodomains of the BET family members (BRD4 , BRD2, BRD3, BRDT) with comparable affinities,...
        by SERP
        (on 24 Apr 2023 )
        Cellular Use Rating
        In Model Organisms
        AZD5153 is a potent and well characterized BET inhibitor that binds both Bromo domains of BET proteins. Its comprehensive characterization makes it a great tool for studying the BET protein function in...
        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