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UCSF924 | UCSF924: Agonist of DRD4
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
DRD4
  • Ki:3.0 nM
  • EC50:0.2 nM
  • EC50:4.2 nM
Agonist
Based on the Ki and EC50 values, the cellular concentration of 10-100nM can be recommended. .
1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Selectivity within target family: Tested D2-like family (DRD2 Ki > 10 µM , DRD3 Ki > 10 µM) > 3300-f ...

Potency
Cellular
In Vitro

DRD4

Mode of Action: Agonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1126/science.aan5468

In Vivo Validations

Mouse
Dose: 10 mg/kg
Route of delivery: Intraperitoneal
Tmax: 0.5 h
Target engagement assay: Following a single i.p. administration of UCSF924 to male C57BL/6 mice at 10 mg/kg dose, plasma concentrations were quantifiable up to 12; Brain concentrations of UCSF924 were quantifiable up to 8 hr.

DOI Reference: 10.1126/science.aan5468

Negative Control Compounds

UCSF924NC
Notes: In vitro: Ki = 7500 nM; 2500 times less potent than the probe; Cell activity: EC50 not detectable (cAMP reporter assay)

Orthogonal Probes def

ABT-724

Chemical Information

Molecular Formula C20H22N2O2
SMILEs Cc1ccc2[nH]c(CNCCCOc3ccccc3)cc(=O)c2c1
InChI InChI=1S/C20H22N2O2/c1-15-8-9-19-18(12-15)20(23)13-16(22-19)14-21-10-5-11-24-17-6-3-2-4-7-17/h2-4,6-9,12-13,21H,5,10-11,14H2,1H3,(H,22,23)
Molecular weight 322.17 Da
AlogP 0.0
HBond acceptors 4
HBond donors 2
Atoms 46

Vendors

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Expert Reviews

by SERP
(on 8 Feb 2022 )
Cellular Use Rating
In Model Organisms
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,...
by SERP
(on 28 Feb 2022 )
Cellular Use Rating
In Model Organisms
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.
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. Read more about our evaluation criteria