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. 2018 Jun 14;9(7):685–690. doi: 10.1021/acsmedchemlett.8b00149

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
a

Mean of at least two runs, % activation >370%.22

b

MED = maximum efficacious dose.

c

pl conc = plasma concentration.

d

>50% inhibition @ 10 μM; see Supporting Information for specific receptors.

e

Mean of three measurements.