Table 1. Performance of 16 hits and erbstatin analog in the EGFRB assay.
HTS % inhibition at 10 μM | IC50 or EC50 (nM) | |||||
---|---|---|---|---|---|---|
Compound name | Molecular target | Granule count | Nuclei count | Granule count | Nuclei count | |
Known EGFR inhibitors | BIBU 1361 | EGFR kinase | 98 | 3 | 38±7 | N.E. |
Tyrphostin AG 1478 | EGFR kinase | 94 | 12 | 65±8 | N.E. | |
PD 153035 | EGFR kinase | 97 | 12 | 91±20 | N.E. | |
Erlotinib | EGFR kinase | 98 | 36 | 210±30 | N.E. | |
Gefitinib | EGFR kinase | 91 | 5 | 380±40 | N.E. | |
Lapatinib | EGFR kinase | 91 | 0 | 590±30 | N.E. | |
GW 2974 | EGFR kinase | 89 | 18 | 1,300±500 | N.E. | |
GW 583340 | EGFR kinase | 94 | 26 | 2,000±400 | N.E. | |
Erbstatin analog | EGFR kinase | -24 | 2 | N.E. | N.E.* | |
Other confirmed granule formation inhibitors | ZM-306416 | VEGFR kinase | 97 | 21 | 670±200 | N.E. |
Camptothecin | Topoisomerase I | 81 | 40 | 720±100 | N.E.* | |
PKC 412 | Pan-kinase inhibitor | 68 | 35 | 1,300±700 | N.E.* | |
Aminopurvalanol A | CDKs | 62 | 40 | 910±400 | N.E.* | |
17-DMAG | Hsp90 | 92 | 33 | 29±3 | N.E. | |
Confirmed granule formation activators | Flurandrenolide | Corticosteroid | -165 | 7 | 23±20 | N.E. |
Beclomethasone | Corticosteroid | -116 | 16 | 42±7 | N.E. | |
Ebastine | H1 receptor | -110 | 6 | 1,500±300 | N.E. |
partial inhibition: a clear upper asymptote was not reached at the highest concentrations tested, or the upper asymptote did not reach 100% inhibition.
N.E.: no effect.