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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

    BI-9313
    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 public 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