Table 1.
The properties of the small molecule HIV-1 fusion inhibitors targeting gp41 pocket.
| Inhibitors | IC50 (μM) | CC50 | SI | Ref. | ||
|---|---|---|---|---|---|---|
| Inhibiting 6-HB formation | Inhibiting p24 production | Inhibiting Cell-cell fusion | ||||
| Computer modeling-based virtual screening | ||||||
| ADS-J1 | 0.73 | 8.29 | 4.95 | 292.16 | 35.24 | [51] |
| ADS-J2 | 3.18 | 30.76 | 21.85 | 289.94 | 9.43 | [51] |
| SB-D10 | 160 | >100 | [57] | |||
| SC-01 | 43 | >50 | [57] | |||
| ELISA- or FLISA-based high-throughput screening (HTS) assays | ||||||
| NB-2 | 1.04 | 6.74 | 2755 | [14] | ||
| NB-64 | 58.74 | 2.21 | 29.92 | >4000 | [14] | |
| A12 | 29.39-37.36 | 0.69-28.19 | 43.24 | 133.5-333.8 | [66] | |
| GLS-22 | 20.73 | 4.91 | 3.60 | 255.28 | [67] | |
| GLS-23 | 21.75 | 8.30 | 8.30 | 227.27 | [67] | |
| NB-293(11a) | 0.098 | 19.35 | 440 | [68] | ||
| 11b | 0.031 | 42.14 | 426 | [68] | ||
| NB-206 (11d) | 0.017 | 16.82 | 330 | [68] | ||
| 12l | 0.018-0.32 | 66.34 | 3686 | [70] | ||
| 12m | 0.014-0.99 | 27.85 | 1989 | [70] | ||
| 5f | 15.55 | 6.90 | 43.55 | 118.45 | [69] | |
| 5h | 12.89 | 16.79 | 45.92 | >320 | [69] | |
| Fluorescence resonance energy transfer (FRET) using metal ion | ||||||
| 11(6,11) | 8 | [73] | ||||
| Compound 1 | 3.2 | >500 | [80] | |||
| Fluorescence polarization assay | ||||||
| 5M038 | 19 | 38 | [82] | |||
| 5M041 | 18 | 18 | [82] | |||
| alpha-helical mimicry | ||||||
| Compound 1a | 13.18 | 15.70 | [83] | |||
| H2N-Asn-[Trp]-Trp-OH | 6 | [85] | ||||
| H2N-Trp-[Trp]-Leu-OH | 5 | [85] | ||||
| H2N-TyrMe-[Trp]-Trp-OH | 8 | [85] | ||||
| Structure-based combinatorial approach | ||||||
| C7-Mn34-Mn42-p30 | 0.3 | [86] | ||||