BI-5756

BI-5756 : Inhibitor of CETP

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(2 ratings)

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Probe BI-5756 is in the process of SERP review.

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Information

CETP

Inhibitor

1 µM

Probe Availability:

opnMe

In Vitro Validations

Uniprot ID: P11597

Target Class: Transporter

Target SubClass: BPI/LBP family

Potency: IC50

Potency Value: 151 nM

Potency Assay: Inhibition of the transfer of a fluorescence labelled lipid from donor vesicles to acceptor vesicles in the presence of human plasma

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Cholesteryl ester transfer protein, CETP, CETP_HUM ...

DOI Reference: 10.1021/jm500431d

Uniprot ID: P11597

Target Class: Transporter

Target SubClass: BPI/LBP family

Potency: IC50

Potency Value: 18 nM

Potency Assay: TF_ROAR assay, measuring the transfer of a neutral fluorescence labeled lipid from donor vesicles to acceptor vesicles by CETP

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Cholesteryl ester transfer protein, CETP, CETP_HUM ...

DOI Reference: 10.1021/jm500431d

In Cell Validations

No in Cell Validations available

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity is not considered to be crucial. Nonetheless, BI-5756 was tested on 104 targets in a selectivity panel and showed ≥1,000-fold selectivity for 93 targets (≤ 50% inhibition @ 10 µM). In 11 assays, the compound showed inhibition ≥ 51. It showed, for example, activity on Cannabinoid receptor CB1 (0.93 µM) and CB2 (0.66 µM). The negative control BI-9313 showed in 4 out of 44 targets inhibition with more than 50% @ 10 µM (e.g. PDE4D2 and CB1).

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SERP ratings and comments

SERP Ratings

In Model Organisms

(last updated: 30 Jun 2022 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

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 with other orthogonal methods.

(last updated: 10 Aug 2022 )