Table 1b.
Compound Name | Compound Structure | Human Gene/Process | Viral Bait | Drug Status | Activity (nM) |
---|---|---|---|---|---|
| |||||
ABBV-74469 | BRD2/4 | E | Clinical Trial | BRD inhibitor KD = 2.1 | |
dBET6146 | BRD2/4 | E | Pre-clinical | Degrades BRD proteins IC50 < 10000 | |
MZ1147 | BRD2/4 | E | Pre-clinical | Degrades BRD proteins KD = 120–228 | |
CPI-0610148 | BRD2/4 | E | Clinical Trial | BRD2/4 inhibitor BRD2 IC50 = 25 BRD4 IC50 = 18 | |
Sapanisertib61,149 | LARP1 | N | Clinical Trial | mTOR inhibitor IC50 = 1 | |
Rapamycin61,150 | LARP1 FKBP15 FKBP7/10 | N Nsp2 Orf8 | Approved (Organ rejection) | mTOR inhibitor (with FKBP) IC50 = 2.0 | |
Zotatifin151 | EIF4E2/H | Nsp2 | Clinical Trial | EIF4a inhibitor IC50 = 1.5 | |
Verdinexor152 | NUPs RAE1 | Nsp4 Nsp9 Orf6 | Clinical Trial | XPO1 nuclear export inhibitor IC50 = 960 | |
Chloroquine153 | SIGMAR1 | Nsp6 | Approved (Malaria) | Sigma 1 binder Ki = 100 | |
Dabrafenib154 | NEK9 | Nsp9 | Approved (Cancer) | NEK9 inhibitor IC50 = 1 | |
WDB002 | CEP250 | Nsp13 | Clinical Trial | CEP250 inhibitor (with FKBP) Kd = 0.29 | |
Sanglifehrin A73 | IMPDH2 | Nsp14 | Pre-clinical | PPIA-IMPDH2 modulator PPIA KD = 0.2 IDPDH2 Binding EC50 = 11.5 (with PPIA) | |
FK-506155 | FKBP7 FKBP10 | Orf8 | Approved (Organ rejection) | FKBP binder | |
Pevonedistat68 | CUL2 | Orf10 | Clinical Trial | NEDD8-activating enzyme inhibitor IC50 = 4.7 | |
Ternatin 4156 | Translation | Pre-clinical | eEF1A inhibitor IC50 = 71 | ||
4E2RCat157 | Translation | Pre-clinical | eIF4E/G PPI inhibitor IC50 = 13500 | ||
Tomivosertib158,159 | Translation | Clinical Trial | MNK1/2 inhibitor IC50 = 2.4 | ||
Compound 2160 | Viral Transcription | Pre-clinical | Cyclophilin inhibitor KD = 24 | ||
Compound 10161 | Viral Transcription | Pre-clinical | PI4K-IIIβ inhibitor IC50 = 3.4 | ||
PS306130 | ER protein processing | Pre-clinical | Sec61 inhibitor IC50 = 20–500 | ||
IHVR-19029162,163 | ER protein processing | Clinical Trial | Antiviral activity IC50 = 1200 | ||
Captopril164 | Cell Entry | Approved (Hypertension) | ACE inhibitor Ki = 3 | ||
Lisinopril165 | Cell Entry | Approved (Hypertension) | ACE inhibitor Ki = 0.27 | ||
Camostat166,167 | Cell Entry | Approved (Pancreatitis) | Serine protease 1 inhibitor IC50 < 1000 | ||
Nafamostat166,168 | Cell Entry | Approved (Anticoagulant) | Serine protease 1 inhibitor IC50 = 100 | ||
Chloramphenicol169 | Mitochondrial ribosome | Approved (Bacterial infection) | Mitochondrial ribosome inhibitor IC50 = 7400 | ||
Tigecycline170 | Mitochondrial ribosome | Approved (Bacterial infection) | Mitochondrial ribosome inhibitor IC50 = 3300 | ||
Linezolid171 | Mitochondrial ribosome | Approved (Bacterial infection) | Mitochondrial ribosome inhibitor IC50 = 16000 |
These molecules derive from expert analysis of human protein interactors of SARS-Co-V2 and reagents and drugs that modulate them; not readily available from the chemoinformatically-searchable literature.