Compound name
UCSF924
Protein family
GPCR
Target name
DRD4
Affinity biochemical (nM)
3
Affinity on-target cellular (nM)
4.2
CG-Set
GPCR set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000539a
SMILES
Cc1ccc2c(c1)C(C=C(CNCCCOc1ccccc1)N2)=O
InChIKey
RPHDOVLXDYWDGF-UHFFFAOYSA-N
NCBI gene ID
1815
UniProt ID
P21917
Mode of action
Agonist
Negative control
UCSF924NC
Affinity biochemical definition
Ki
Affinity biochemical assay type
Radioligand binding assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1126/science.aan5468
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/UCSF924
Affinity biochemical relation
=
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
Split luciferase based cAMP receptor assay (HEK293T cells)
Affinity on-target cellular relation
=
Selectivity platform
PRESTO-Tango GPCR-ome screening
Selectivity platform number of targets
320
Selectivity remarks
Screened at 1 µM (activity assay in HTLA cells), closest targets: Ki(DRD4 )= 4.9 nM, Ki(HTR1A) = 223 nM, Ki(HTR2B) = 236.67 nM, Ki(NMDA) = 1004 nM, Ki(HRH2) = 1909.67, Ki(SLC6A3) = 2116.67 nM; Screened against D2-like family: > 3300-fold selective (DRD2 Ki > 10 µM, DRD3 Ki >10 µM)
Selectivity Source Knowledge
https://doi.org/10.1126/science.aan5468
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/UCSF924
Selectivity Number of Off-targets
0