ML154

ML154 : Antagonist of NPSR1

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe ML154 is in the process of SERP review.

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Information

NPSR1

Antagonist

up to 1 uM

Probe Availability:

MCULE

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): NCGC84 concentrations up to 10 μm did not affect intracellular Ca2+-level in cells expressing vasopressin V1b or purinergic receptors following the application of EC80 of their respective ligand. The NPSR has the closest protein sequence homology with the vasopressin V1b receptor (∼28%).

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

ML154 has demonstrated strong on-target cellular potency and encouraging selectivity for NPSR1 over vasopressin and purinergic receptors, but was apparently not evaluated for a broader cohort of off targets. Encouraging in vivo data at 1mg/kg i.p.

(last updated: 1 Feb 2023 )