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.