Table 1. Primary hits identified in a PKD1 inhibitor screen of a targeted library.

Compound Name	Known target	% PKD1 Inhibition
Fasudil hydrochloride	ROCK	41%
SP 600125	JNK	74%
Ro 31-8220 Mesylate	PKC, MAPK, ERK2	72%
Arcyriaflavin A	Cyclin D1/CAMK II	75%
IKK-16	IκB kinase	67%
SB 218078	Check point Kinase I	85%
PD 407824	Check point Kinase I	57%
D 4476	casein kinase 1	45%
EO 1428	p38 MAPK	68%
H 89 Dihydrochloride	PKA	66%
Iressa	EGFR	45%
SU 5416	VEGFR	45%
1-NA-PP1	Src mutant	77%
Dorsomorphin dihydrochloride	AMPK	50%
BIO	GSK-3	47%
SD 208	TGF-βRI	74%
kb-NB142-70	PKD	88%

A targeted protein kinase inhibitor library of 80 compounds was screened for PKD1 inhibitory activity at 1 µM using an in vitro radiometric PKD1 kinase assay. Sixteen compounds were selected as primary hits based on their ability to inhibit PKD1 at or above 50% at 1 µM. The % PKD1 inhibition referred to the percent inhibition of the total kinase activity measured in the absence of inhibitors (DMSO). Kb-NB142-70, a previously validated PKD inhibitor, was used as a positive control. Experiments were performed with triplicate determinations at 1 µM for each compound.