Fig. 1 | Signal Transduction and Targeted Therapy

Fig. 1

From: Drugging the intrinsically disordered transactivation domain of androgen receptor

Fig. 1The alternative text for this image may have been generated using AI.

Improving the potency of compounds. a Structures of compounds (1–10). b CLogPs and IC50s for blocking androgen-induced PSA-luciferase activities in LNCaP cells for compounds (1–8). c Dose response curves of inhibition of androgen-induced PSA-luciferase activity. d Chemical structures showing the route to BU130/BU170. e, f IC50s for pairs of compounds which differed only by the presence (right, red) or absence (left, blue) of the chlorohydrin group using the PSA-luciferase reporter in androgen-induced LNCaP cells. g Table showing the IC50s derived from the colony formation assays in LNCaP cells or (h) PC3 cells. i Dose response curves from the colony formation assay using LNCaP (solid lines) or PC3 (dashed lines) cells. Blue lines: compounds lacking the chlorohydrin functional group. Red lines: matched compounds with the chlorohydrin. n.s.: not significant. ND: not detected. N/A: not available. Error bars: mean ± SEM. See Supplementary Fig. 1

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