Table 1. Structure-activity relationship data for lithocholic acid derivatives.
Cpd. | R1 | R2 | R3 | R4 | R5 | Ki (μM)[a] |
---|---|---|---|---|---|---|
1 | 49±3.0 | |||||
2 | >200 | |||||
3 | >200 | |||||
4 | >200 | |||||
5 | 114±13 | |||||
6 | 138±20 | |||||
7 | 157±47 | |||||
8 | 114±14 | |||||
9 | 88±11 | |||||
10 | 25±4.0 | |||||
11 | >200 | |||||
12 | 5.1±1.4 | |||||
13 | >200 | |||||
14 | >200 | |||||
15 | >200 | |||||
16 | 186±27 |
Values are means ± standard error from at least three independent experiments