ML075

ML075 : peptide competitive antagonist of NPY2R

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe ML075 is in the process of SERP review.

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Information

NPY2R

peptide competitive

up to 1 µM

Probe Availability:

MCULE

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity within target family: selective over Y1R, IC50 >35 uM Selectivity outside target family: The selectivity of SF-11 was assessed by the NIMH PDSP, in which the compounds were screened for binding to receptors (n = 35), ion channels (n = 2), and transporters (n = 3) typically found in the CNS at 10 uM. Only DAT and 5HT2B showed >50% binding, further radioligand displacement assay excluded them as off-targets (7093 and 4989 nM respectively).

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

The maximum inhibitory effect of this compound looks like 80% or around based on the literature, the users may need to take into account this point.

(last updated: 2 Feb 2023 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

In cells the compound shows an IC50>100 nM and is selective in a panel of 40 different receptors, ion channels, and transporters found in the CNS. The compound contains some PAINS feature, however the lack of activity at NY1R receptor suggests there is no assay interference. The half-life is very short and the low unbound fractions suggests sufficient exposure cannot be reached despite good brain penetration. We are assuming that concentration values in table 4 refer to total concentration. The compounds caused lethargy in mice which may interfere with the functional readouts.

(last updated: 14 Oct 2025 )