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(R)-ZINC-3573

2D structure
Target MRGPRX2 
Targeted domain TM5 (Asp184)
Mode of action Agonist
Control (S)-ZINC-3573
Recommended cellular usage concentration ≤ 1 µM
In vivo use No
Donated by UNC


Probe criteria


Selectivity within target family: > 30-fold Surpasses criterion: No off-target activity in concentration-response studies (tested 315 GPCRS in PRESTO-Tango GPCRome screening)
Closest hits in the PDSP scan are DRD2 (Ki =369.37 nM), TMEM97 (Ki =489.44 nM), HTR6 (Ki =748.23 nM) and SLC6A3 (Ki =1109.25 nM).
Selectivity outside target family Little activity for 97 representative kinases in DiscoverX KINOMEscan at 10 µM. Closest hits: BTK (Kd = 27 µM), MAPK8 (Kd = 19 µM) and MAPK10 Kd > 30 µM
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion: EC50 = 740 nM (PRESTO-Tango concentration response assay); EC50 = 1 µM (FLIPR assay); (R)-ZINC-3573 induces intracellular calcium release and degranulation in LAD2 mast cells.
Control compound (100 times less potent than the probe) (S)-ZINC-3573: EC50 ˃100 µM (PRESTO-Tango concentration response and FLIPR assay)
Closest hits in the PDSP scan are TMEM97 (Ki = 972.86 nM), HTR6 (Ki = 1092.22 nM), ADRA1B (Ki = 2293.6 nM) and others.