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. 2009 Nov 18;4(12):2060–2069. doi: 10.1002/cmdc.200900262

Table 4.

Selectivity of hit compounds and mode of inhibition.[a]

Compd Mode of inhibiton Inhibitor constants [μm] IC50m] EC50m]
Ki Ki TryR hGR[b] Parasite[c] MRC-5[c]
1 linear mixed 1.6±0.2 3.2±0.3 1.7 >100 10.3 >50
2 NT[d] 1.1 NT 6.0 18.7
3 NT 1.2 NT >50 >50
4 linear mixed 3.0±0.2 4.3±0.3 4.2 74.2 25.6 >50
5 linear mixed 2.0±0.1 3.0±0.2 4.7 33.4 18.7 31.1
6 NT 7.2 NT 6.9 NT
7 NT 5.1 NT 16.5 NT
10 NT 5.8 NT 19.2 NT
12 NT 14.4 NT 32.1 43.7
19 NT 8.4 NT 14.5 NT
39 linear uncompetitive 4.6±0.3 (T[S]2) 29.4±1.7 (NADPH) 8.6 >100 1.22 1.62
40 linear uncompetitive 3.0±0.2 (T[S]2) 21.5±1.6 (NADPH) 12.8 10.0 1.43 3.2
41 NT 10.2 NT 8.1 NT
45 NT 13.0 NT 3.4 12.9

[a] MOI: Compounds 119 are from hit series 1 and 3945 from hit series 2. [b] hGR: human glutathione reductase. [c] Concentration giving 50% growth inhibition after 73 h exposure. [d] NT: not tested.