. 2023 Jan 5;10:1089959. doi: 10.3389/fchem.2022.1089959

TABLE 3.

IC₅₀ values of diarylphosphonates desthiobiotin probes against a panel of serine proteases.


#	R¹	R²	Trypsin-3	β-tryptase	Thrombin	uPA ^a	CatG ^a	ChTryp ^a	NE ^a
#	R¹	R²	IC₅₀ (μM) ^b
42		H	>10	>10	>10	>10	3.23 ± 0.29	2.07 ± 0.85	>10
44		H	>10	>10	>10	>10	>10	>10	4.70 ± 0.20
45b		H	0.22 ± 0.02	0.80 ± 0.05	0.61 ± 0.17	>10	>10	>10	N.D. ^c
46b		Cl	0.07 ± 0.002	0.04 ± 0.006	0.04 ± 0.006	0.42 ± 0.05	>10	>10	N.D. ^c
47b		H	0.52 ± 0.24	2.49 ± 0.19	3.55 ± 0.17	4.62 ± 0.17	>10	>10	>10
49b		NHCOCH₃	0.09 ± 0.005	1.11 ± 0.05	1.18 ± 0.04	6.75 ± 0.52	4.47 ± 0.51	>10	>10
50b		H	0.03 ± 0.01	0.36 ± 0.07	3.52 ± 0.39	0.02 ± 0.0001	0.36 ± 0.004	1.64 ± 0.50	>10
52b		NHCOCH₃	0.01 ± 0.001	0.07 ± 0.003	0.76 ± 0.02	0.01 ± 0.003	0.05 ± 0.007	>10	>10
54b		Cl	0.008 ± 0.002	0.11 ± 0.009	0.20 ± 0.02	0.006 ± 0.0001	0.12 ± 0.01	5.60 ± 1.06	>10
55b		H	0.24 ± 0.01	0.37 ± 0.09	>10	2.22 ± 0.07	1.62 ± 0.09	>10	N.D. ^c
56b		NHCOCH₃	0.22 ± 0.004	0.39 ± 0.10	>10	5.19 ± 0.08	0.62 ± 0.009	>10	N.D. ^c
57b		Cl	0.18 ± 0.07	0.02 ± 0.0002	>10	0.16 ± 0.04	0.12 ± 0.04	>10	N.D. ^c
58b	Pro-Lys	H	0.16 ± 0.004	6.41 ± 0.15	0.16 ± 0.004	6.51 ± 1.15	2.90 ± 0.15	>10	N.D. ^c

^{^a}

Panel of serine proteases abbreviations: uPA, urokinase plasminogen activator; catG, cathepsin G; ChTryp, chymotrypsin; NE, neutrophil elastase.

^{^b}

Half maximal inhibitory concentration (IC₅₀) value is the concentration of inhibitor required to reduce the enzyme activity to 50% after a 15 min preincubation with the enzyme at 37°C and activity measurements as mentioned in the Experimental section. IC₅₀ are calculated from two independent experiments; when SD was higher than three times the average value, a third independent experiment was run (mean ± SD).

^{^c}

N.D., not determined.