Venetoclax

Venetoclax : BH3 mimetic of BCL2

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(3 ratings)

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.

Information

BCL2

BH3 mimetic

Probe Availability:

In Vitro Validations

Uniprot ID: P10415

Target Class: Other

Target SubClass: Protein Phosphatase

Potency: Ki

Potency Value: <0.010 nM

Potency Assay: Time-resolved FRET competition binding assay

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

Target aliases:

Apoptosis regulator Bcl-2, BCL2, BCL2_HUMAN

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency end-point : Ki BCL-XL: 48 nM, BCL-W: 245 nM; MCL-1: >444 nM

Potency assay (off target): TR-FRET

Probe Selectivity in Vitro:

Not available

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 11 Apr 2017 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 12 Apr 2017 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Early studies with Venetoclax (ABT-199), a potent and selective orally-bioavailable B-cell lymphoma 2 small-molecule inhibitor, which has shown an remarkable response across a number of hematologic malignancies, with an acceptable safety profile. This drug has been approved by the US Food and Drug Administration and the European Medicines Agency for treatment of adult patients with 17p deleted relapsed/refractory chronic lymphocytic leukemia (del(17p) CLL) Venetoclax is sold under the brand names Venclexta and Venclyxto.

(last updated: 11 Nov 2020 )