Table 1.

Binding parameters, inhibitory potencies and antiparasitic effects of selected TCCYP51 ligands

Compound	Spectral Response in TCCYP51			Effect on enzymatic activity (I/E2****)
	Type	Soret band maximum, nm	Kd, μM	TCCYP51	Mouse COX2
5	2	422	0.44±0.02	10
7	2	422	0.75±0.03	14
9	2	422	0.24±0.01	<1
12	2	422	0.29±0.01	9.1	2.1
13	2**	418	7.6±0.9	13	>10
14	2	422	0.54±0.02	10	10
15	2	422	0.37±0.05	8.5	1.7
16	1*	416	3.3±0.48	11	2.1
17	none	417	-	15	3.6
19	2**	420	0.56±0.08	7.7	<1
18	2**	420	0.26±0.04	4.2	<1
20	2***	422	2.31±0.09	6.3	2.4
21	2**	419	0.36±0.02	<1	<1
22	2**	419	0.15±0.01	<1	>40

^*weak type 1 response with only ~7% of P450 experiencing low to high spin transition;

^**modified type 2 response with the smaller shift in the Soret band maximum,

^***sigmoid curve, Hill coefficient 2.3±0.2 (see Figure 2);

^****inhibitory potencies of the compounds toward TCCYP51 (minimal final concentration required in the reconstituted reaction 1 μM⁹) and mouse COX2 (final concentration 0.1 μM) are compared as molar ratios Inhibitor/Enzyme which cause a two-fold decrease in the initial rate of catalysis.