MRK-560

Inhibitor of PSEN1

Structure

SERP Rating

Probe MRK-560 is in the process of SERP review.

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Information

PSEN1

Inhibitor

up to 100 nM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: P49768

Target Class: Enzyme

Target SubClass: Gamma-Secretase complex

Potency: IC50

Potency Value: 0.65 nM

Potency Assay: CHAPSO-solubilized SH-SY5Y neuroblastoma P2 cell membranes

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

Target aliases:

Presenilin-1, PSNL1, PS1, AD3, PSEN1, PSN1_HUMAN, ...

DOI Reference: 10.1016/j.bmcl.2005.10.009

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): The compound was profiled in a large panel of off-targets

Probe Selectivity in Vitro:

All off-targets out of 171 enzymes and receptors are > 100-fold less potent. MRK-560 demonstrated activity in the SLC18A2 (Monoamine Transporter) assay with an IC50 of 213 nM. 6 other off-targets were found between 2 and 10 µM. Clean GPCR scan.

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SERP ratings and comments

No SERP comments found for MRK-560