Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTPZG3C)

DTT Name	SARS-CoV 3C-like protease (3CLpro)
Synonyms	SARS-CoV 3C-like protease; SARS-CoV 3CLp; SARS-CoV 3CL-PRO; SARS-CoV 3CLpro
Gene Name	SARS-CoV rep
BioChemical Class	Coronaviruses polyprotein 1ab family
UniProt ID	R1AB_CVHSA (3241-3546)
TTD ID	T89826
EC Number	EC 3.4.22.-
Sequence	SGFRKMAFPSGKVEGCMVQVTCGTTTLNGLWLDDTVYCPRHVICTAEDMLNPNYEDLLIR KSNHSFLVQAGNVQLRVIGHSMQNCLLRLKVDTSNPKTPKYKFVRIQPGQTFSVLACYNG SPSGVYQCAMRPNHTIKGSFLNGSCGSVGFNIDYDCVSFCYMHHMELPTGVHAGTDLEGK FYGPFVDRQTAQAAGTDTTITLNVLAWLYAAVINGDRWFLNRFTTTLNDFNLVAMKYNYE PLTQDHVDILGPLSAQTGIAVLDMCAALKELLQNGMNGRTILGSTILEDEFTPFDVVRQC SGVTFQ
Function	Cleaves the C-terminus of replicase polyprotein at 11 sites. Recognizes substrates containing the core sequence [ILMVF]-Q-\|-[SGACN]. Also able to bind an ADP-ribose-1''-phosphate (ADRP). May cleave host ATP6V1G1 thereby modifying host vacuoles intracellular pH.

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA)

Jump to Detail Molecular Interaction Atlas of This DTT

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Lopinavir	DMITQS0	Human immunodeficiency virus infection	1C62	Approved	[2]
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8 Preclinical Drugs Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
GC376	DMR1CLY	Middle East Respiratory Syndrome (MERS)	1D64	Preclinical	[3]
GRL-001	DMVB1PD	Middle East Respiratory Syndrome (MERS)	1D64	Preclinical	[2]
Phenylisoserine derivatives SK80	DM16W8F	Severe acute respiratory syndrome (SARS)	1D65	Preclinical	[4]
PMID26868298-compound-N3	DMQFUCD	Middle East Respiratory Syndrome (MERS)	1D64	Preclinical	[2]
PMID27240464-compound-3f	DMPC29W	Middle East Respiratory Syndrome (MERS)	1D64	Preclinical	[5]
PMID28216367-compound-6d	DMPWUFT	Middle East Respiratory Syndrome (MERS)	1D64	Preclinical	[6]
PMID28624700-compound-3-31	DMYNCWK	Severe acute respiratory syndrome (SARS)	1D65	Preclinical	[1]
PMID30784880-compound-6-5	DMVB0P3	Severe acute respiratory syndrome (SARS)	1D65	Preclinical	[7]
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⏷ Show the Full List of 8 Preclinical Drugs

References

1	Discovery of Unsymmetrical Aromatic Disulfides as Novel Inhibitors of SARS-CoV Main Protease: Chemical Synthesis, Biological Evaluation, Molecular Docking and 3D-QSAR Study Eur J Med Chem. 2017 Sep 8;137:450-461.
2	Coronaviruses - drug discovery and therapeutic options. Nat Rev Drug Discov. 2016 May;15(5):327-47.
3	Reversal of the Progression of Fatal Coronavirus Infection in Cats by a Broad-Spectrum Coronavirus Protease Inhibitor. PLoS Pathog. 2016 Mar 30;12(3):e1005531.
4	Synthesis and Evaluation of Phenylisoserine Derivatives for the SARS-CoV 3CL Protease Inhibitor. Bioorg Med Chem Lett. 2017 Jun 15;27(12):2746-2751.
5	Identification, synthesis and evaluation of SARS-CoV and MERS-CoV 3C-like protease inhibitors. Bioorg Med Chem. 2016 Jul 1;24(13):3035-3042.
6	Identification and evaluation of potent Middle East respiratory syndrome coronavirus (MERS-CoV) 3CLPro inhibitors. Antiviral Res. 2017 May;141:101-106.
7	Chemical synthesis, crystal structure, versatile evaluation of their biological activities and molecular simulations of novel pyrithiobac derivatives. Eur J Med Chem. 2019 Apr 1;167:472-484.