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. 2013 Feb 22;8(2):e56770. doi: 10.1371/journal.pone.0056770

Table 2. High-throughput screening (Alphascreen®) system for inhibitors that block the interaction between the PLZF and HB-EGF- or AR-CTF.

Biotin-HB-EGF-CTF Biotin-AR-CTF
100 µM 10 µM 100 µM 10 µM
%Inhibition %Inhibition
No.7620 82.1 22.1 76.3 25.6
No.7632 81.7 12.6 74.9 40.5
No.7701 89.6 41.6 71.5 60.5
No.7702 86.7 34.4 77.9 46.3
No.7768 73 24.1 53.2 32.6
No.7787 82.1 10 82.2 14.9
No.7804 85.7 19.5 79.8 49.9
No.7826 82.3 14.5 82.6 30.7
No.7834 90.7 21.5 77.1 43.6
No.7887 93.9 28.4 90.9 39.5
No.7972 67.5 9.9 70.1 34.2
No.8016 71.4 33.1 75 30.4
Telmisartan * * 66.9 48.5
Camdesartan 78.1 12.6 84.1 23.2
Olmesartan * * 51.8 20.5
Losartan * * 68.4 12.9

Compounds: 9,000 → 12, Z’-factor: 0.73±0.091, S/B: 20.6,

*

not calculated.

Twelve candidate and four angiotensin II type 1 receptor blocker (ARB) based on efficacy for blocking binding of HB-EGF-CTF or AR-CTF to Zn5-8 of PLZF with Alphascreen system. Z’-factor showed to be 0.73 (0.5<Z’<1.0), suggesting the reliable data.