In vitro biological evaluation.
| ||||
|---|---|---|---|---|
| Compd | R | R1 | hTGR5 EC50 (nM) | mTGR5 EC50 (nM) |
| 18f |
|
2-F | 36.73 | — |
| 18g |
|
2-Cl | 1.44 | 119.6 |
| 18h |
|
4-OCH3 | 195.6 | — |
| 18i |
|
4-CH3 | 83.23 | — |
| 18j |
|
2,4-Di-Cl | 9.89 | 538.4 |
| 18k |
|
2,5-Di-Cl | 0.58 | 267.2 |
| 18l |
|
4-Phenyl | 895.1 | — |
| 18m |
|
2,5-Di-Cl | 9450 | — |
| 18n |
|
2,5-Di-Cl | >10 000 | — |
| 18o |
|
2,5-Di-Cl | >10 000 | — |
| 18p |
|
2,5-Di-Cl | >10 000 | — |
| 18q |
|
2,5-Di-Cl | >10 000 | — |
| 18r |
|
2,5-Di-Cl | >10 000 | — |
| 18s |
|
2,5-Di-Cl | >10 000 | — |
| 18t |
|
2,5-Di-Cl | >10 000 | — |
| 18u |
|
2,5-Di-Cl | >10 000 | — |
| INT-777 | 781 | 166 | ||