Table 1.
| Compound | Conformational Change |
Nuclear Accumulation |
Transcription IC50 (nM) |
DHT Binding IC50 (nM) |
|---|---|---|---|---|
| Chembridge 5107769 | X | 341 | 182 | |
| sanguinarine sulfate | X | 500 | 779 | |
| dihydrocelastrol | X* | X | 52 | 57 |
| gambogic acid | X* | X | 269 | 36 |
| thimerosal | X* | X | 347 | no effect |
| helenine | X* | X | 1010 | 6360 |
| radicicol | X | X | 3.4 | 10971 |
| Chembridge 5128773 | X | X | 834 | no effect |
| actinomycin D | X | 1.1 | no effect | |
| 17-AAG | X | 1.7 | no effect | |
| cucurbitacin I | X | 1.00 | 256 | |
| puromycin HCl | X | 19 | no effect | |
| AG 592 | X | 215 | no effect | |
| oxindole I | X | 224 | no effect | |
| xanthohumol | X | 276 | no effect | |
| sertaconazole nitrate | X | 554 | 1153 | |
| acrisorcin | X | 915 | 718 | |
| bromoconduritol | X | 1000 | 4600 | |
| cadmium acetate | X | 1102 | no effect | |
| 2,5-dihydroxycinnamic acid | X | 1142 | 10811 | |
| epigallocatechin-3-monogallate | X | 1432 | no effect | |
| oxiconazole nitrate | X | 1491 | 1534 | |
| mechlorethamine | x | 1560 | 7670 | |
| luffariellolide | x | 1563 | no effect | |
| madecassic acid | x | 1989 | no effect | |
| EGFR/ErbB-2 Inhibitor | x | 2426 | no effect | |
| Chembridge 5404078 | x | 2480 | no effect | |
| GSK-3b Inhibitor III | x | 2555 | no effect | |
| thapsigargicin | x | 2776 | no effect | |
| WR 216174 | x | 3108 | 12750 | |
| myoseverin | x | 4048 | no effect | |
| MDL-12,330A, HCl | x | 4412 | no effect | |
| xanthyletin | x | 5000 | no effect | |
| retusoquinone | x | 5616 | no effect | |
| mebendazole | x | 8473 | no effect | |
| glutethimide | x | 9795 | no effect | |
| catechin | x | 10000 | no effect | |
| Chembridge 5255637 | x | 10000 | no effect | |
| blasticidine S | x | 10000 | no effect | |
| epoxomicin | x | 10000 | no effect | |
| chlorpromazine HCl | x | 11950 | no effect | |
| ikarugamycin | x | 14304 | no effect | |
| heudelottin c | x | 16632 | no effect | |
| Chembridge 5213395 | x | 17000 | no effect |
*
indicates that positive result was obtained by cross-assay validation, as opposed to a result from the primary screen. Structures of all non-competitive inhibitors are shown in Supplementary Figure 1.