Table 1 Inhibition constants (pM) reported for amprenavir, darunavir and tipranavir.

From: Fluorogenic Assay for Inhibitors of HIV-1 Protease with Sub-picomolar Affinity

Assay type

Amprenavir

Darunavir

Tipranavir

Reference

Enzymatic activity

100

8

88

8

(Unknown)

600

—

—

4

Enzymatic activity

—

—

8

5

(Unknown)

—

16

—

7

ITC (competitive displacement)

390

4.5

—

6

fluorescence (competitive displacement)

36

0.147

—

10

Enzymatic activity

57

—

—

16

Enzymatic activity

135 ± 6

10 ± 1

82 ± 6

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