. Author manuscript; available in PMC: 2013 Apr 3.

Published in final edited form as: J Biomol Screen. 2012 May 9;17(7):885–899. doi: 10.1177/1087057112446174

Table 1. Performance of 16 hits and erbstatin analog in the EGFRB assay.

The average percentage inhibition at 10 μM compound concentration during the screen and the IC₅₀ or EC₅₀ values ±standard deviation calculated based on follow up dose response studies are summarized for both the granule count and nuclei count readouts.

			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.