(R)-ZINC-3573
-ZINC-3573.6d5f77c0d756.svg)
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. |