Table 1.

Structures, X_I(50) values, calculated binding affinity (−logK_d), polar score that represents the contribution of hydrogen bonding to the calculated binding affinity, and the hydrophobic score that represents the contribution of the hydrophobic interactions to the calculated binding affinity for the 2-oxoamide inhibitors are shown.

Code	Molecular Structure	XI(50)	−logKd	Polar	Hydrophobic
AX074		0.003a	11.94	4.87	7.07
AX109		0.005b	10.11	2.98	7.13
AX007		0.009c	9.26	3.49	5.77
AX073		0.018a	8.24	3.17	5.07
AX063		0.019b	8.20	2.57	5.63
AX013		0.021d	7.84	3.17	4.67
GK165		0.023e	7.53	3.79	3.74
AX006		0.024f	7.21	4.08	3.13
AX021		0.027b	7.10	2.77	4.33
AX016		0.035d	7.19	2.76	4.43
AX008		0.068c	5.25	2.90	2.35

^aData taken from ref. 28.

^bData taken from ref. 27.

^cData taken from ref. 32.

^dData taken from ref. 31.

^eThe synthesis and the properties of inhibitor GK165 will be published elsewhere.

^fData taken from ref. 29.