BAY-6096

BAY-6096 : Antagonist of ADRA2B

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 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.

Probe BAY-6096 is in the process of SERP review.

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Information

ADRA2B

Antagonist

100 nM

Additional Data

SGC image SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: P18089

Target Class: GPCR

Target SubClass: Adrenergic receptor

Potency: Ki

Potency Value: 21 nM

Potency Assay: Radioactive binding assay for human ADRA2B

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

Target aliases:

Alpha-2B adrenergic receptor, ADRA2RL1, ADRA2L1, A ...

DOI Reference: 10.1021/acs.jmedchem.2c01690

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity within target family: Adrenergic receptor panel (IC50): ADRA1A (5.516 µM; 394- fold), ADRA1B (> 10 µM), ADRA1D (> 10 µM), ADRA2A (10 µM), ADRA2C (>11.83 µM), ADRB1 (> 10 µM), ADRB2 (> 10 µM), ADRB3 (> 10 µM). Selectivity outside target familyEurofins Panlabs panel (67 targets) at 10 µM: clean In-house kinase panel (22 kinases): human DDR2: IC50 = 1.4 µM, others IC50 > 20 µM

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

A highly potent, selective and aqueous soluble antagonist of alpha2B suitable for cell-based and in vivo studies (via the intravenous route).

(last updated: 12 Apr 2024 )

SERP+ Ratings

In Cell Rating

In Model Organisms

SERP+ Comments:

The compound demonstrates excellent potency and selectivity in cells with the only drawback being low permeability. It has demonstrated adequate pharmacokinetic data to be a good probe for in vivo use as well. However, there are still key pharmacokinetic data missing.

(last updated: 14 Oct 2025 )