Screening target | Screening strategy | Screening library | Representative hit | IC50 | Bioactivity in cells | Reference |
---|---|---|---|---|---|---|
SENP1 | Benzodiazepine-based design | – | Compound 38 | 9.2 µM | Not tested | 42 |
SENP1 | Cleavage of fluorogenic substrate SUMO1-AMC | In-house compound library | GN6958 | 29.6 µM | Not tested | 43 |
SENP1 | Virtual screening | SPECS database | SI2 | 1.29 µM | Confirmed | 44 |
PfSENP1 | SUMO-procleavage assay with SDS-PAGE detection | Cysteine protease inhibitors library | JCP-666 | 17.9 µM | Not tested | 45 |
SENP1/2 | Virtual screening | DTP | NSC5068 | µM range | Confirmed | 46 |
SENP2 | Combination of virtual screening and FRET-based assay | Namiki-shoji library | 1,2,5-oxadiazoles | <10 µM | Not tested | 47 |
SENPs | Cleavage of fluorogenic AFC-based substrates | In-house compound library | VEA499 | µM range | No activity | 48 |
DTP, Developmental Therapeutics Program; FRET, fluorescence resonance energy transfer; IC50, half-maximum inhibitory concentration; PfSENP, SENP of Plasmodium falciparum; SENP, SUMO-specific protease; SUMO, small ubiquitin-like modifier.