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. 2012 Nov 9;4(1):63–68. doi: 10.1021/ml300277t

Table 1. Pharmacological, Absorption, Metabolism, and Safety Properties of 5.

graphic file with name ml-2012-00277t_0007.jpg

	5 (R¹ = EtNH, R² = iPr)
MW 395.5, eLog D 3.40, TPSA 101
hTGR5 induced EC₅₀ (nM)	2.5
mTGR5 induced EC₅₀ (nM)	5620
rTGR5 induced EC₅₀ (nM)	3930
dTGR5 induced EC₅₀ (nM)	6
RRCK (P_app, 10^–6 cm/s)^a	20.2
RLM CLint (μL/min/mg)	>564
HLM CLint (μL/min/mg)	>317
CYP (pct inh at 3 μM)	1A2, 2D6, 2C9, 3A4 < 20%
[³H]-dofetilide (pct inh at 10 μM)	9%

^a

RRCK = modified Madin–Darby permeability assay.