ML5

ML5 : Antagonist of S1PR1

Structure

SERP Rating

Probe ML5 is in the process of SERP review.

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Information

S1PR1

Antagonist

up to 10 uM

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: P21453

Target Class: GPCR

Target SubClass: Sphingosine receptor

Potency: Ki

Potency Value: 77 nM

Potency Assay: GTP-γS binding assay using CHO cell membranes

PDB ID for probe-target interaction (3D structure): 3V2W, 3V2Y

Target aliases:

Sphingosine 1-phosphate receptor 1, EDG1, CHEDG1, ...

DOI Reference: 10.1038/nchembio804

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity within target family: Antagonistic effect of W146 was selective for S1P1 receptors, and 2a showed neither agonism nor antagonism at 10 μM in GTP-γS assays for S1P2, S1P3 and S1P5 receptors.

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