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. Author manuscript; available in PMC: 2017 Jul 14.
Published in final edited form as: J Med Chem. 2016 Jul 1;59(13):6531–6546. doi: 10.1021/acs.jmedchem.6b00760

Table 4.

Solubility (in phosphase-buffered saline, pH= 6.5) and PK properties of the most potent and selective TgCDPK1 inhibitors dosed at 10 mg/kg PO to mice.

Solubility (μM) Tmax (min) Cmax (μM) AUCo->inf (μM.min) Half life (min) clearance (mL/min)
1 82 120 0.75 ±0.15 430 ±58 233 ±26 0.7
8 48 50 0.89 ±0.17 94 ±51 68 ±64 2.5
17 54 200 0.26 ±0.04 128 ± 53 223 ±182 1.8
29 17 30 0.88 ±0.23 67 ±60 50 ±73 110
31 >100 50 5.2 ±1.0 850 ± 411 114 ±115 0.2
32 >100 320 13 ±1 13700 ±1500 1190 ±510 0.2
33 >100 560 7.8 ±1.4 16600 ±4300 1110 ±400 0.3
34 6.2 40 0.39 ±0.16 31 ±8 40 ±5 6.7
35 8.0 30 3.9 ±1.1 3.9 ±1.1 41 ±21 21