Table 1Solubility experiments in various media with ML231 and analogs

EntryPubchem SIDPBS Solubility (μg/mL)aAssay Media Solubility (μg/mL)bConc. in Assay Media (μM)cAssay Media Solubility (μM)dCIT2 EC50 μMe (% resp)fAGP1 EC50 μM (% resp)MEP2 EC50 μM (% resp)LAP4 EC50 μM (% resp)RPL19A EC50 μM (% resp)
199300522 (ML231)0.050.070.244–63.8 (91.7%)> 100 (6.7%)> 100 (16.0%)> 100 (12.2%)> 100 (18.4%)
2960997812.14.114.7410–203.36 (94.7%)11.33 (39.2%)12.68 (77.2%)9.06 (59.1%)6.36 (69.9%)
3110923093NA0.993.214–100.77 (95.5%)0.72 (30.5%)0.68 (24.6%)> 100 (18.2%)0.51 (64.9%)
4993005413.26.123.43NA8.82 (97.7%)> 100 (5.8%)> 100 (4.4%)> 100 (8.1%)> 100 (18.2%)
a

Conditions: 1× PBS buffer, pH 7.4; Data collected by Sanford-Burnham

b

Conditions: SCD medium with 0.03% Pluronic F-6; Data collected by Sanford-Burnham

c

Concentration calc’d from assay media solubilityb data from Sanford Burnham and compound mol. wt

d

Conditions as in footnote b; Data collected by UNMCMD using Flow Cytometry, range shown

e

EC50 reported as greater than 100 for inactive compound. The actual EC50 for inactive compounds is not shown.

f

maximum % response compared to rapamycin. Compound scored inactive if % response was < 20%.

NA = data not available

From: Profiling a Selective Probe for RTG Branch of Yeast TORC1 Signaling Pathway

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