UCSF924

UCSF924: Agonist of DRD4

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe UCSF924 is in the process of SERP review.

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Information

DRD4

Agonist

1 uM
Reviewer recommended concentration: Based on the Ki and EC50 values, the cellular concentration of 10-100nM can be recommended. .

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: P21917

Target Class: GPCR

Target SubClass: Dopamine receptor

Potency: Ki

Potency Value: 3.0 nM

Potency Assay: Radioligand binding assay (DRD4)

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

Target aliases:

D(4) dopamine receptor, DRD4, DRD4_HUMAN, Dopamine ...

DOI Reference: 10.1126/science.aan5468

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within target family: Tested D2-like family (DRD2 Ki > 10 µM , DRD3 Ki > 10 µM) > 3300-fold selectivity; No activity in panel of 320 non-olfactory GPCRs at 1 µM. Closest hits in the GPCR scan are HTR1A (Ki =223.0 nM), HTR2B (Ki =236.67 nM), HTR7 (Ki =2075.67 nM).

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

This compound not only has significant agonistic activity against D4D but also excellent subtype selectivity over other D4 receptors. Moreover, it was confirmed to penetrate to brain in mouse models. Therefore, it is one of the best chemical tools available to evaluate D4D activity in a variety of biological models.

(last updated: 8 Feb 2022 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

UCSF924 is a nanomolar DRD4 agonist with exceptional selectivity against other GPCRs in vitro. This compound provides an excellent chemical probe for cell-based DRD4 studies.

(last updated: 28 Feb 2022 )