BI-9627
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | pHi change assay: SLC9A1 IC50 = 6 nM |
| Selectivity within target family: > 30-fold | Solute carrier family 9 isoform selectivity: > 30-fold selective versus SLC9A2 (IC50 = 231 nM) and > 1000-fold versus SLC9A3 (IC50 > 16 µM) |
| Selectivity outside target family | Eurofins-Panlabs screen on 68 targets @ 10 µM did not give strong hits. Clean PDSP scan with the closest hit on SLC6A3 (pKi = 5.8) |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Human platelet swelling inhibition (hPSA) assay: IC50 = 31 nM; Rat PSA: IC50 = 138 nM |
| Control compound (100 times less potent than the probe) | pHi change assay: SLC9A1 IC50 > 10 µM; SLC9A2 and SLC9A3 IC50 > 10 µM; hPSA assay: IC50 > 10 µM; Clean PDSP scan with the closest hit on SLC6A3 (pKi = 6.1) |