Table 2
From the following article
Chemical genetics reveals a complex functional ground state of neural stem cells
Phedias Diamandis, Jan Wildenhain, Ian D Clarke, Adrian G Sacher, Jeremy Graham, David S Bellows, Erick K M Ling, Ryan J Ward, Leanne G Jamieson, Mike Tyers & Peter B Dirks
Nature Chemical Biology 3, 268 - 273 (2007) Published online: 8 April 2007
doi:10.1038/nchembio873
Table 2. Highly potent and highly selective compounds identified by HTS of neurospheres
| Name | Action | Target | Selectivity | Neurosphere EC50 ( M) | Astrocyte EC50 (M) | Neurosphere selectivity | Ptch1+/-
neurosphere EC50 (M)b | Ptch1+/-
Trp53-
/-
neurosphere EC50 (M)b |
|---|---|---|---|---|---|---|---|---|
a Compounds listed represent confirmed hits with high selectivity for NPCs (neurosphere selectivity >5). | ||||||||
bPtch1+/-
and Ptch1+/-
Trp53-
/-
neurosphere cultures were derived from mouse cerebellar tumor samples. n.a., not applicable; n.d., not determined at highest tested dose (30 | ||||||||
| Controls | ||||||||
| Cycloheximide (1) | Inhibitor | Protein synthesis | 60S ribosome | 0.142 | 0.071 | 0.50 | 0.042 | 0.054 |
| Etoposide (2) | Inhibitor | Topoisomerase | Topo II | 0.340 | 0.433 | 1.28 | 0.208 | n.t. |
| Carboplatin (3) | Intercalator | DNA | n.a. | 0.489 | 2.453 | 5.08 | 0.196 | n.t. |
| Selected hitsa | ||||||||
( ) Butaclamol (4) | Antagonist | Dopamine receptor | D2 > D1 | 0.785 | 12.34 | 15.7 | 0.751 | 2.533 |
| (R)-(- )-Propylnorapomorphine (5) | Agonist | Dopamine receptor | D2 | 0.351 | 8.230 | 23.4 | 0.199 | n.t. |
| (R)-(- )-Apomorphine (6) | Agonist | Dopamine receptor | n.a. | 0.350 | 10.19 | 29.1 | 0.168 | 0.683 |
| cis-(Z)-Flupenthixol (7) | Antagonist | Dopamine receptor | n.a. | 0.199 | 1.182 | 5.93 | 0.187 | n.t. |
| p-F-HHSiD (8) | Antagonist | Acetylcholine receptor | M3 > M1 > M2 | 0.441 | 5.815 | 13.2 | 1.125 | 1.373 |
| Ifenprodil (9) | Antagonist | NMDA receptor | Polyamine site | 0.616 | 11.06 | 17.9 | 0.451 | 0.807 |
| Carbetapentane (10) | Agonist | Opioid receptor | Sigma 1 | 0.756 | 28.16 | 37.3 | 2.083 | 2.040 |
| Fenretinide (11) | Agonist | Retinoic acid receptor | n.a. | 0.334 | 2.399 | 7.18 | 0.204 | n.t. |
| WHI-P131 (12) | Antagonist | JAK3 | n.a. | 2.346 | n.d. | >10 | 1.525 | n.t. |
| SB 202190 (13) | Antagonist | p38 MAPK | n.a. | 8.063 | 64.8 | 8.04 | 3.006 | n.t. |
| PAPP (14) | Agonist | Serotonin receptor | 5-HT1A | 0.031 | 21.82 | 702 | 0.169 | 0.097 |
| Dihydrocapsaicin (15) | Agonist | Vanilloid receptor | VR1 | 0.218 | 41.83 | 192 | 0.020 | 0.651 |
| Cyclopamine (16) | Antagonist | Smoothened | n.t. | n.t. | n.a. | 1.00 | 13.44 | |
