Table 1.
LOPAC1280 screening top hit list
| % activity | ||||||
| Compounds | Pharmacol. class | Selectivity | R 1 | R 2 | Avrg. | Rank |
| Sanguinarine chloride | Ion Pump | Na+/K+ ATPase | 0.0 | 28.5 | 14.3 | 1 |
| Calcimycin | Intracellular Calcium | Ca2+ | 29.5 | 32.1 | 30.8 | 2 |
| Indirubin-3′-oxime | Phosphorylation | CDK | 26.3 | 47.0 | 36.7 | 3 |
| Podophyllotoxin | Cytoskeleton and ECM | 44.8 | 50.2 | 47.5 | 4 | |
| Mitoxantrone | DNA Metabolism | 46.0 | 51.3 | 48.6 | 5 | |
| Tyrphostin A9 | Phosphorylation | PDGFR | 43.5 | 54.5 | 49.0 | 6 |
| (S)-(+)-Camptothecin | Apoptosis | TopoI | 63.4 | 37.1 | 50.3 | 7 |
| Ammonium pyrrolidinedithiocarbamate | Nitric Oxide | NOS | 57.4 | 44.6 | 51.0 | 8 |
| IC 261 | Phosphorylation | CK-1delta/epsilon | 63.3 | 40.2 | 51.8 | 9 |
| Colchicine | Cytoskeleton and ECM | Tubulin | 43.5 | 60.9 | 52.2 | 10 |
| 7-Chloro-4-hydroxy-2-phenyl-1,8-naphthyridine | Adenosine | A1 | 55.1 | 52.1 | 53.6 | 11 |
| Tetraethylthiuram disulfide | Biochemistry | Alcohol Dehydrogenase | 63.9 | 43.4 | 53.7 | 12 |
| Brefeldin A from Penicillium brefeldianum | Cytoskeleton and ECM | Golgi apparatus | 64.6 | 44.6 | 54.6 | 13 |
| Taxol | Cytoskeleton and ECM | Tubulin | 51.9 | 57.6 | 54.7 | 14 |
| Emetine dihydrochloride hydrate | Apoptosis | 60.7 | 49.1 | 54.9 | 15 | |
| Idarubicin | DNA Metabolism | 44.1 | 69.6 | 56.8 | 16 | |
| Tomoxetine | Adrenoceptor | Reuptake | 57.6 | 59.0 | 58.3 | 17 |
| Dequalinium analog, C-14 linker | Phosphorylation | PKC-alpha | 70.9 | 46.7 | 58.8 | 18 |
| Dihydroouabain | Ion Pump | Na+/K+ Pump | 75.8 | 44.1 | 59.9 | 19 |
| Tyrphostin AG 538 | Phosphorylation | IGF-1 RTK | 65.2 | 54.8 | 60.0 | 20 |
| Diphenyleneiodonium chloride | Nitric Oxide | eNOS | 50.7 | 70.5 | 60.6 | 21 |
| Thapsigargin | Intracellular Calcium | 55.3 | 68.9 | 62.1 | 22 | |
| Tyrphostin 47 | Phosphorylation | EGFR | 66.6 | 61.5 | 64.1 | 23 |
| N-Oleoyldopamine | Neurotransmission | CB1 | 62.0 | 70.2 | 66.1 | 24 |
| 7-Cyclopentyl-5-(4-phenoxy)phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamine | Phosphorylation | Ick | 57.2 | 76.5 | 66.9 | 25 |
| U0126 | Phosphorylation | MEK1/MEK2 | 61.9 | 74.8 | 68.4 | 26 |
| SU 5416 | Phosphorylation | VEGFR PTK | 79.5 | 60.1 | 69.8 | 27 |
| Fluspirilene | Dopamine | D2/D1 | 75.4 | 70.5 | 73.0 | 28 |
| Propionylpromazine hydrochloride | Dopamine | D2 | 76.5 | 72.4 | 74.4 | 29 |
| U-99194A maleate | Dopamine | D3 | 73.5 | 77.7 | 75.6 | 30 |
| Wortmannin from Penicillium funiculosum |
Phosphorylation |
PI3K |
78.4 |
75.6 |
77.0 |
31 |
Compound name, pharmacological class and selectivity annotations are taken from the (LOPAC)1280 list. R 1/2 = screening replicate 1/2. % activity = relative sprout number per bead compared to negative control, < 80% in both replicates demarks a top hit. Top hit rate 2.4%.