BAY-784

BAY-784 : Antagonist of GNRHR

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Probe BAY-784 is in the process of SERP review.

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Information

GNRHR

Antagonist

up to 1 uM
Reviewer recommended concentration: up to 10 µM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: P30968

Target Class: GPCR

Target SubClass: Hormone Receptor

Potency: IC50

Potency Value: 27 nM

Potency Assay: Tag Lite binding assay using human GnRHR

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

Target aliases:

, Gonadotropin-releasing hormone receptor, GRHR, G ...

DOI Reference: 10.1021/acs.jmedchem.0c01076

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within target family: Selectivity against a broad range of GPCR‘s. Clean GPCR scan except for weak activity on TMEM97 (Ki = 1107.9 nM). Eurofins-Panlabs radioligand binding assay: The closest off-target is CNR1 with IC = 3.44 µM at 3 µM. Selectivity outside target family: Eurofins-panlabs enzyme assay: The closest off-targets found at 10 µM are MAPK3 with IC50= 4.87 µM and MAPK14 with IC50 = 10.7 µM.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 5 Feb 2022 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Probe BAY-784 is an effective "partial antagonist" of GNRHR at two digit nanomolar, it can reduce the LH level ~up to 50% from base level in various testing model (cell, animal, human). For off-target screening, when tested at 1uM or 10uM against vast panels of kinase, GPCR, ion channel proteins (in vitro or in cell), no significant interference on these protein's activity or function was observed. The reason not giving a 4 star is because that in-situ or in cell chemical proteomics profiling is currently unavailable.

(last updated: 18 Feb 2022 )