Donated Chemical Probes

Target	P2RY14
Mode of action	Antagonist
Control	PPTN-NC
Recommended cellular usage concentration	100 nM
In vivo use	Yes
Donated by	MSD

Inhibitor/agonist potency: goal is < 100 nM (IC₅₀, K_d>/sub>)	Surpasses criterion: For P2RY14: IC₅₀ = 0.5 nM (FLIPR assay); K_i = 2.3 nM (Binding assay); K_i = 35 nM (Binding assay w/ 2% HSA)
Selectivity within target family: > 30-fold	Surpasses criterion: >10,000-fold selectivity over other P2RY* receptors Shows off-target activity in the PDSP scan: the closest hits are DRD3 (K_i = 884.3 nM), TMEM97 (K_i = 1120.99 nM) , SIGMAR1 (K_i = 1180.59 nM), ADRA2B (K_i = 2561.53 nM)
Selectivity outside target family	Closest off-targets (Panlabs): CYSLTR1 (h): IC₅₀ = 560 nM @ 1µM, HRH2 (h): IC₅₀ = 1390 nM @ 10 µM, SLC6A3 (Dopamine Transporter) (h): IC₅₀ = 2310 nM @ 10 µM KINOMEScan with 468 targets at 1 µM: clean
On target cell activity for cell-based targets: goal is < 1 µM IC₅₀/EC₅₀	Surpasses
Control compound (100 times less potent than the probe)	Surpasses criterion: P2RY14 potency > 4000x less; IC₅₀ = 4381 nM (FLIPR assay); K_i = 8614 nM (Binding assay); K_i > 100 µM (Binding assay w/ 2% HSA); Shows off-target activity in the PDSP scan: the closest hits are SIGMAR1 (K_i = 1168.69 nM), TMEM97 (K_i = 1704.51 nM) , ADRA2B (K_i = 1836.54 nM) KINOMEScan with 468 targets at 1 µM: clean