Table 2.

Literature searched, and expert opinion derived small molecules, which modulate SARS-CoV-2 [131]

Data are taken from Gordon et al.

Classification	Compounds name	Targets	Status	Activity (nM) IC50	References
Drug repurposing	Valproic acid	HDAC2	Approved for CNS and cancer	62,000	[83–85]
	Silmitasertib	CSNK2A2	Approved for cancer	1	[79]
	Entacapone	COMT	Approved for Parkinson	151	[86, 87]
	Indomethacin	PTGES2	Approved for inflammation	750	[88]
	Metformin	NDUFs	Approved for diabetes	–	[89]
	Migalastat	GLA	Approved for fabry	40	[90]
	Mycophenolic acid	IMPDH2	Approved for organ rejection	20	[91]
	Midostaurin	MARK2/3	Approved for cancer	Kd = 100 for MARK1 Kd = 23 for MARK3	[92]
	Ruxolitinib	MARK2/3	Approved for Myelofibrosis	Kd = 660 for MARK1 Kd > 10,000 for MARK3	[93]
	Daunorubicin	ABCC1	Approved for cancer	Ki = 70	[94]
	S-verapamil	ABCC1	Approved for hypertension	Ki = 113	[95]
	Rapamycin	LARP1 FKBP15 FKBP7/10	Approved for organ rejection	2.0	[96, 97]
	Chloroquine	SIGMAR1	Approved for malaria	Ki = 100	[98]
	Dabrafenib	NEK9	Approved for malaria	1	[99]
Clinical and pre-clinical compounds	JQ1	BRD2/4	Pre-clinical	40–120	[77]
	RVX-208	BRD2/4	Clinical	50–1800	[77]
	TMCB	CSNK2A2	Pre-clinical	Ki = 21	[78, 80]
	Apicidin	HDAC2	Pre-clinical	120	[81]
	E-52862	SIGMAR1	Clinical	17	[100]
	PD-144418	SIGMAR1	Pre-clinical	Ki = 0.8	[101]
	RS-PPCC	SIGMAR1	Pre-clinical	Ki = 1.5	[102]
	PB28	SIGMAR1 TMEM97	Pre-clinical	15	[103]
	H-89	PRKACA	Pre-clinical	48	[104]
	Merimepodib	IMPDH2	Clinical	10	[105]
	XL413	DNMT1	Clinical	3.4	[106]
	CCT 365623	LOX	Pre-clinical	1500	[107]
	ZINC1775962367	DCTPP1	Pre-clinical	47	[108]
	ZINC4326719	DCTPP1	Pre-clinical	19	[109]
	ZINC4511851	DCTPP1	Pre-clinical	20	[110]
	ZINC95559591	MARK3, TBK1	Pre-clinical	12, 6	[111]
	AC-55541	F2RL1	Pre-clinical	pEC50 = 6.7	[112]
	AZ8838	F2RL1	Pre-clinical	344	[113]
	GB110	F2RL1	Pre-clinical	280	[114]
	AZ3451	F2RL1	Pre-clinical	pKd = 15	[113]
	ABBV-744	BRD2/4	clinical	Kd = 2.1	[115]
	dBET6	BRD2/4	Pre-clinical	< 10,000	[116]
	MZ1	BRD2/4	Pre-clinical	Kd = 120–228	[117]
	CPI-0610	BRD2/4	Clinical	25 for BRD2 18 for BRD4	[118]
	Sapanisertib	LARP1	Clinical	1	[97, 119]
	Zotatifin	EIF4E2/H	Clinical	1.5	[120]
	Verdinexor	NUPs RAE1	Clinical	960	[121]
	WDB002	CEP250	Clinical	Kd = 0.29	–
	Pevonedistat	CUL2	Clinical	4.7	[122]
	Sanglifehrin A	IMPDH2	Pre-clinical	Kd = 0.2	[123]
Pathway targets	Ternatin 4	Translation	Pre-clinical	7.1	[124]
	4E2RCat	Translation	Pre-clinical	13,500	[125]
	Tomivosertib	Translation	Clinical	2.4	[126, 127]
	Compound 2	Viral Transcription	Pre-clinical	24	[128]
	Compound 10	Viral Transcription	Pre-clinical	3.4	[129]
	PS3061	ER protein processing	Pre-clinical	20–500	[130]
	IHVR-19029	ER protein processing	Clinical	1200	[132, 133]
	Captopril	Cell entry	Approved for hypertension	Ki = 3	[134]
	Lisinopril	Cell entry	Approved for hypertension	Ki = 0.27	[135]
	Camostat	Cell entry	Approved for pancreatitis	< 10,000	[71, 136]
	Nafamostat	Cell entry	Approved for anticoagulant	100	[136, 137]
	Linezolid	Mitochondrial ribosome	Approved for bacterial infection	16,000	[138]
	Tigecycline	Mitochondrial ribosome	Approved for bacterial infection	3300	[139]

HDAC2 histone deacetylase 2, CSNK2A2 casein kinase 2 alpha 2, COMT catechol-O-methyltransferase, PTGES2 prostaglandin E synthase 2, NDUFS1 NADH–ubiquinone oxidoreductase 75 kDa subunit, GLA alpha-galactosidase A, IMPDH2 inosine-5′-monophosphate dehydrogenase 2, MARK2/3 MAP/microtubule affinity-regulating kinase 3, ABCC1 ATP-binding cassette subfamily C member 1, FKBP FK506-binding protein, LARP1 La Ribonucleoprotein 1, SIGMAR1 sigma non-opioid intracellular receptor 1, NEK9 NIMA: related kinase 9, BRD2 bromodomain containing 2, CSNK2A2 casein kinase 2 alpha 2, TMEM97 sigma-2 receptor, PRKACA protein kinase CAMP-activated catalytic subunit alpha, DNMT1 DNA (cytosine-5)-methyltransferase 1, DCTPP1 dCTP pyrophosphatase 1, F2RL1 F2R-like trypsin receptor 1, EIF4E2 eukaryotic translation initiation factor 4E family member 2, RAE1 ribonucleic acid export 1, CEP250 centrosomal protein 250, CUL2 cullin 2, LOX lysyl oxidase, NUPs nucleoporins