Skip to main content
. 2017 Dec 8;9(1):44–66. doi: 10.1039/c7md00510e

Table 1. Hit rate for each member of the Nek family based upon screening data from large published screening sets with FLT3 values for comparison.

Compound set PKIS a PKIS2 b BMS c RBC d Ambit e GSK f Millipore g
No. of cmpds 368 645 21 851 178 72 577 158
Nek1 0.011 0.051 0.001 0.051 0.014
Nek2 0.005 0.057 0.003 0.006 0.056 0.059 0.006
Nek3 0.031 0.006 0.014 0
Nek4 0.012 0.039 0.014
Nek5 0.065 0.0286 0.014
Nek6 0 0.023 0.017 0 0.042 0.031 0
Nek7 0 0.035 0.0315 0 0.042 0.035 0
Nek8
Nek9 0.033 0.051 0.009 0.028 0.042 0.016
Nek10 0.059
Nek11 0.031 0.011 0.042 0.095
FLT3 0.14 0.23 0.15 0.41 0.036 0.14 0.3

aValues for PKIS calculated by the number of compounds that inhibited each Nek by ≥50% divided by the total number of compounds screened (Elkins et al., 2016).

bValues for PKIS2 calculated by the number of compounds that inhibited each Nek ≥50% divided by the total number of compounds screened (Drewry et al., 2017).

cValues from Bristol-Myers Squibb screening data (hit rate calculated based on <13% of control) (Posy et al., 2011).

dValues from Reaction Biology Corporation data (Anastassiasdis et al., 2011).

eValues calculated from reported ambit Kd values – number of compounds that inhibit each Nek ≥500 nM divided by the total number of compounds (Davis et al., 2011).

fValues from GlaxoSmithKline screening taken from Nc ≤ 1 (Bamborough et al., 2008).

gValues calculated using EMD millipore screening data. Number of compounds that inhibit each Nek ≥50% divided by total number of compounds screened (Gao et al., 2013).