A-192621

A-192621 : Antagonist of EDNRB

Structure

SERP Rating

In Cells

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In Model Organisms

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Probe A-192621 is in the process of SERP review.

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Information

EDNRB

Antagonist

0-300 nM
Reviewer recommended concentration: in some publications a dose of 30 mg/kg/d in mouse and rat has been used

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: P24530

Target Class: GPCR

Target SubClass: Endothelin Receptor

Potency: Ki

Potency Value: 8.8 nM

Potency Assay: 125I-labelled ET-1 saturation binding studies with EDNRB

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

Target aliases:

Endothelin receptor type B, ETRB, EDNRB, EDNRB_HUM ...

DOI Reference: 10.1042/CS103S107S

Uniprot ID: P24530

Target Class: GPCR

Target SubClass: Endothelin Receptor

Potency: IC50

Potency Value: 4.5 nM

Potency Assay: Inhibition of 125I labeled ET-3 binding to EDNRB

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

Target aliases:

Endothelin receptor type B, ETRB, EDNRB, EDNRB_HUM ...

DOI Reference: 10.1042/CS103S107S

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within target family: Surpasses criterion: > 600-fold selective against EDNRA (IC50 for EDNRA = 4.28 µM). Clean GPCR scan (43). Selectivity outside target family: Closest off targets: TSPO (72.1%), CCK (63.1%), Cl- channel (77.4%) @ 10 µM

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(last updated: 13 Feb 2022 )