(R)-9s

2D structure
Target ADRA1D 
Mode of action Antagonist
Control (S)-9s
Recommended cellular usage concentration ≤ 1 µM
In vivo use yes
Synonyms TP-009
Donated by Takeda


Probe criteria


In vitro potency < 100 nM Ki = 1.6 (1.4 - 1.9) nM
Selectivity within target family: > 30-fold Binding to ADRA1A > 1700 fold, binding to ADRA1B > 750 fold
Selectivity outside target family KINOMEScan with 468 targets at 1 µM: Closest off-targets of primary data (% Ctrl) are TYRO3 (33), FYN (42), FGFR2 (43), NLK (44), EIF2AK4 (45), MAP3K4 (47).
Significant cell activity at 1 µM Inhibits phenylephrine-induced contractions in bladder strips taken from rats with bladder outlet obstruction, IC30 = 15 nM
Control compound (100 times less potent than the probe) (S)-9s with Ki = 130 (110 - 160) nM; Ki (ADRA1D/ADRA1A/ADRA1B): 130 / >2,700 / >1,200 nM
KINOMEScan with 468 targets at 1 µM: Closest off-targets of primary data (% Ctrl) are DYRK1B (37) and NEK3 (44).