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BI-5756 | BI-5756 : Inhibitor of CETP
RATINGS:
Cellular Use: (1 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
CETP
  • IC50:151 nM
  • IC50:18 nM
    Inhibitor
    1 µM

    Selectivity

    In Vitro Selectivity Assessment
    Selectivity Assessment Description:
    Selectivity is not considered to be crucial. Nonetheless, BI-5756 was tested on 104 targets in a sel ...

    Potency
    Cellular
    In Vitro

    CETP

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/jm500431d

    In Vivo Validations

    Mouse
    Dose: 10 uM/Kg
    Route of delivery: Oral
    Area Under the Curve:: 4.9 uM*h
    Bioavailability: 46%

    DOI Reference: 10.1021/jm500431d

    Dose: 1 uM/Kg
    Route of delivery: Intravenous
    Plasma half life: 6.5 h
    Systemic clearance: 14.6 mL/min/Kg
    Cmax: 387.8 nM
    Tmax: 0.8 h
    Volume of Distribution at Steady-State: 5.9 L/Kg

    DOI Reference: 10.1021/jm500431d

    Negative Control Compounds

    CANSAR577267
    Notes: BI-9313 shows 19-fold less activity on the TransF Assay and 29-fold less activity on the TF_ROAR assay.

    Orthogonal Probes def

    ANACETRAPIB

    Chemical Information

    Molecular Formula C27H32F3NO3
    SMILEs CC(C)c1nc2c(c3c1[C@@H](c1ccc(C(F)(F)F)cc1)OC31CCOCC1)[C@@H](O)CC(C)(C)C2
    InChI InChI=1S/C27H32F3NO3/c1-15(2)23-21-22(20-18(31-23)13-25(3,4)14-19(20)32)26(9-11-33-12-10-26)34-24(21)16-5-7-17(8-6-16)27(28,29)30/h5-8,15,19,24,32H,9-14H2,1-4H3/t19-,24+/m0/s1
    Molecular weight 475.23 Da
    AlogP 0.0
    HBond acceptors 4
    HBond donors 1
    Atoms 66

    Vendors

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

    Expert Reviews

    by SERP
    (on 30 Jun 2022 )
    In Model Organisms
    ( The reviewer did not leave any comments )
    by SERP
    (on 10 Aug 2022 )
    Cellular Use Rating
    In Model Organisms
    This compound is excellent upon evaluating the outcomes of the engagement of human CETP with a humanized mouse. This compound can be used against human CETP in other contexts but need to be evaluated collectively...
    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