Table 4. Rat IP1, GK Rat oGTT, BSEP, and Off-Target Activity Comparison of Key Compounds.
Cmpd | rat IP1a (EC50 nm ± SD) | GK rat oGTT MEDb (pl concc @ 3 h, dose) | Off-target Hitsd # | BSEPe (IC50 μM ± SEM) |
---|---|---|---|---|
14 | 1.2 ± 0.35 | 3.0 μm @ 10 mg/kg | 9 | 1.4 ± 0.1 |
16 | 2.3 ± 0.40 | 13.9 μm @ 30 mg/kg | 3 | 0.3 ± 0.04 |
AP5 | 0.49 ± 0.28 | 4.9 μm @ 10 mg/kg | 4 | 3.5 ± 0.2 |
29 | 5.2 ± 1.6 | 32 μm @ 30 mg/kg | 1 | 3.2 ± 0.4 |
Mean of at least two runs, % activation >370%.22
MED = maximum efficacious dose.
pl conc = plasma concentration.
>50% inhibition @ 10 μM; see Supporting Information for specific receptors.
Mean of three measurements.