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[Preprint]. 2020 Mar 27:2020.03.22.002386. Originally published 2020 Mar 22. [Version 3] doi: 10.1101/2020.03.22.002386

Table 1b.

Expert-identifieda drugs and reagents that modulate SARS-CoV-2 interactors.

Compound Name Compound Structure Human Gene/Process Viral Bait Drug Status Activity (nM)

ABBV-74469 graphic file with name nihpp-2020.03.22.002386v3-t0041.jpg BRD2/4 E Clinical Trial BRD inhibitor KD = 2.1
dBET6146 graphic file with name nihpp-2020.03.22.002386v3-t0042.jpg BRD2/4 E Pre-clinical Degrades BRD proteins IC50 < 10000
MZ1147 graphic file with name nihpp-2020.03.22.002386v3-t0043.jpg BRD2/4 E Pre-clinical Degrades BRD proteins KD = 120–228
CPI-0610148 graphic file with name nihpp-2020.03.22.002386v3-t0044.jpg BRD2/4 E Clinical Trial BRD2/4 inhibitor BRD2 IC50 = 25 BRD4 IC50 = 18
Sapanisertib61,149 graphic file with name nihpp-2020.03.22.002386v3-t0045.jpg LARP1 N Clinical Trial mTOR inhibitor IC50 = 1
Rapamycin61,150 graphic file with name nihpp-2020.03.22.002386v3-t0046.jpg LARP1 FKBP15 FKBP7/10 N Nsp2 Orf8 Approved (Organ rejection) mTOR inhibitor (with FKBP) IC50 = 2.0
Zotatifin151 graphic file with name nihpp-2020.03.22.002386v3-t0047.jpg EIF4E2/H Nsp2 Clinical Trial EIF4a inhibitor IC50 = 1.5
Verdinexor152 graphic file with name nihpp-2020.03.22.002386v3-t0048.jpg NUPs RAE1 Nsp4 Nsp9 Orf6 Clinical Trial XPO1 nuclear export inhibitor IC50 = 960
Chloroquine153 graphic file with name nihpp-2020.03.22.002386v3-t0049.jpg SIGMAR1 Nsp6 Approved (Malaria) Sigma 1 binder Ki = 100
Dabrafenib154 graphic file with name nihpp-2020.03.22.002386v3-t0050.jpg NEK9 Nsp9 Approved (Cancer) NEK9 inhibitor IC50 = 1
WDB002 graphic file with name nihpp-2020.03.22.002386v3-t0051.jpg CEP250 Nsp13 Clinical Trial CEP250 inhibitor (with FKBP) Kd = 0.29
Sanglifehrin A73 graphic file with name nihpp-2020.03.22.002386v3-t0052.jpg IMPDH2 Nsp14 Pre-clinical PPIA-IMPDH2 modulator PPIA KD = 0.2 IDPDH2 Binding EC50 = 11.5 (with PPIA)
FK-506155 graphic file with name nihpp-2020.03.22.002386v3-t0053.jpg FKBP7 FKBP10 Orf8 Approved (Organ rejection) FKBP binder
Pevonedistat68 graphic file with name nihpp-2020.03.22.002386v3-t0054.jpg CUL2 Orf10 Clinical Trial NEDD8-activating enzyme inhibitor IC50 = 4.7
Ternatin 4156 graphic file with name nihpp-2020.03.22.002386v3-t0055.jpg Translation Pre-clinical eEF1A inhibitor IC50 = 71
4E2RCat157 graphic file with name nihpp-2020.03.22.002386v3-t0056.jpg Translation Pre-clinical eIF4E/G PPI inhibitor IC50 = 13500
Tomivosertib158,159 graphic file with name nihpp-2020.03.22.002386v3-t0057.jpg Translation Clinical Trial MNK1/2 inhibitor IC50 = 2.4
Compound 2160 graphic file with name nihpp-2020.03.22.002386v3-t0058.jpg Viral Transcription Pre-clinical Cyclophilin inhibitor KD = 24
Compound 10161 graphic file with name nihpp-2020.03.22.002386v3-t0059.jpg Viral Transcription Pre-clinical PI4K-IIIβ inhibitor IC50 = 3.4
PS306130 graphic file with name nihpp-2020.03.22.002386v3-t0060.jpg ER protein processing Pre-clinical Sec61 inhibitor IC50 = 20–500
IHVR-19029162,163 graphic file with name nihpp-2020.03.22.002386v3-t0061.jpg ER protein processing Clinical Trial Antiviral activity IC50 = 1200
Captopril164 graphic file with name nihpp-2020.03.22.002386v3-t0062.jpg Cell Entry Approved (Hypertension) ACE inhibitor Ki = 3
Lisinopril165 graphic file with name nihpp-2020.03.22.002386v3-t0063.jpg Cell Entry Approved (Hypertension) ACE inhibitor Ki = 0.27
Camostat166,167 graphic file with name nihpp-2020.03.22.002386v3-t0064.jpg Cell Entry Approved (Pancreatitis) Serine protease 1 inhibitor IC50 < 1000
Nafamostat166,168 graphic file with name nihpp-2020.03.22.002386v3-t0065.jpg Cell Entry Approved (Anticoagulant) Serine protease 1 inhibitor IC50 = 100
Chloramphenicol169 graphic file with name nihpp-2020.03.22.002386v3-t0066.jpg Mitochondrial ribosome Approved (Bacterial infection) Mitochondrial ribosome inhibitor IC50 = 7400
Tigecycline170 graphic file with name nihpp-2020.03.22.002386v3-t0067.jpg Mitochondrial ribosome Approved (Bacterial infection) Mitochondrial ribosome inhibitor IC50 = 3300
Linezolid171 graphic file with name nihpp-2020.03.22.002386v3-t0068.jpg Mitochondrial ribosome Approved (Bacterial infection) Mitochondrial ribosome inhibitor IC50 = 16000
a.

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.