(R)-9s

Antagonist of ADRA1D

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

ADRA1D

Antagonist

10 nM - 1 uM

DOI - 10.1021/acs.jmedchem.5b01528

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: P25100

Target Class: GPCR

Target SubClass: Alpha-Adrenergic Receptor

Potency: Ki

Potency Value: 1.9 nM

Potency Assay: Cell Free Activity Assay

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

Target aliases:

Alpha-1D adrenergic receptor, ADRA1A, ADRA1D, ADA1 ...

DOI Reference: 10.1021/acs.jmedchem.5b01528

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Binding to ADRA1A > 1700 fold, binding to ADRA1B > 750 fold

Probe Selectivity in Vitro:

unknown selectivity outside target family

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 18 Oct 2020 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

High quality probe with full supporting data and less active (distomer) negative control analogue. Whilst full selectivity data are still being generated, initial selectivity across GPCR and kinase panels is very good. Useful complement to other less selective alpha1D adrenergic R antagonists MBY7378 and SNAP8719.

(last updated: 18 Oct 2020 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 27 Oct 2020 )