PMC:7461420 / 78209-78870 JSONTXT

{"target":"https://pubannotation.org/docs/sourcedb/PMC/sourceid/7461420","sourcedb":"PMC","sourceid":"7461420","source_url":"https://www.ncbi.nlm.nih.gov/pmc/7461420","text":"Next, the same group studied the SARs for compound 158 further. This led to the discovery of compound 165 with high PLpro inhibitory activity of SARS‐CoV‐1 (IC50, 0.32 µM) and antiviral activity (EC50, 9.1 µM) in Vero cells. 199 The mode of action of 165 was found to be a noncovalent, competitive inhibition of PLpro. Unlike the previous series, the stereochemistry at the α‐methyl group did not make a significant difference in inhibition of PLpro. For example, both (S)‐ and (R)‐methyl inhibitors, 165 (IC50, 0.32 µM; EC50, 9.1 µM and 166 (IC50, 0.56 µM; EC50, 9.1 µM), respectively, shared equipotent inhibitory activity in enzymatic and cell‐based assays.","tracks":[{"project":"LitCovid-PD-FMA-UBERON","denotations":[{"id":"T277","span":{"begin":218,"end":223},"obj":"Body_part"},{"id":"T278","span":{"begin":643,"end":647},"obj":"Body_part"}],"attributes":[{"id":"A277","pred":"fma_id","subj":"T277","obj":"http://purl.org/sig/ont/fma/fma68646"},{"id":"A278","pred":"fma_id","subj":"T278","obj":"http://purl.org/sig/ont/fma/fma68646"},{"subj":"T277","pred":"source","obj":"LitCovid-PD-FMA-UBERON"},{"subj":"T278","pred":"source","obj":"LitCovid-PD-FMA-UBERON"}]},{"project":"LitCovid-PD-MONDO","denotations":[{"id":"T369","span":{"begin":145,"end":149},"obj":"Disease"}],"attributes":[{"id":"A369","pred":"mondo_id","subj":"T369","obj":"http://purl.obolibrary.org/obo/MONDO_0005091"},{"subj":"T369","pred":"source","obj":"LitCovid-PD-MONDO"}]},{"project":"LitCovid-PD-CLO","denotations":[{"id":"T925","span":{"begin":133,"end":141},"obj":"http://purl.obolibrary.org/obo/CLO_0001658"},{"id":"T926","span":{"begin":186,"end":194},"obj":"http://purl.obolibrary.org/obo/CLO_0001658"},{"id":"T927","span":{"begin":213,"end":217},"obj":"http://purl.obolibrary.org/obo/CLO_0009524"},{"id":"T928","span":{"begin":213,"end":217},"obj":"http://purl.obolibrary.org/obo/CLO_0050515"},{"id":"T929","span":{"begin":218,"end":223},"obj":"http://purl.obolibrary.org/obo/GO_0005623"},{"id":"T930","span":{"begin":272,"end":273},"obj":"http://purl.obolibrary.org/obo/CLO_0001020"},{"id":"T931","span":{"begin":403,"end":404},"obj":"http://purl.obolibrary.org/obo/CLO_0001020"},{"id":"T932","span":{"begin":617,"end":625},"obj":"http://purl.obolibrary.org/obo/CLO_0001658"},{"id":"T933","span":{"begin":643,"end":647},"obj":"http://purl.obolibrary.org/obo/GO_0005623"}],"attributes":[{"subj":"T925","pred":"source","obj":"LitCovid-PD-CLO"},{"subj":"T926","pred":"source","obj":"LitCovid-PD-CLO"},{"subj":"T927","pred":"source","obj":"LitCovid-PD-CLO"},{"subj":"T928","pred":"source","obj":"LitCovid-PD-CLO"},{"subj":"T929","pred":"source","obj":"LitCovid-PD-CLO"},{"subj":"T930","pred":"source","obj":"LitCovid-PD-CLO"},{"subj":"T931","pred":"source","obj":"LitCovid-PD-CLO"},{"subj":"T932","pred":"source","obj":"LitCovid-PD-CLO"},{"subj":"T933","pred":"source","obj":"LitCovid-PD-CLO"}]},{"project":"LitCovid-PD-CHEBI","denotations":[{"id":"T23665","span":{"begin":15,"end":20},"obj":"Chemical"},{"id":"T51563","span":{"begin":176,"end":185},"obj":"Chemical"},{"id":"T1863","span":{"begin":377,"end":389},"obj":"Chemical"},{"id":"T25019","span":{"begin":377,"end":383},"obj":"Chemical"},{"id":"T26688","span":{"begin":384,"end":389},"obj":"Chemical"},{"id":"T68003","span":{"begin":483,"end":489},"obj":"Chemical"},{"id":"T37926","span":{"begin":490,"end":500},"obj":"Chemical"}],"attributes":[{"id":"A91377","pred":"chebi_id","subj":"T23665","obj":"http://purl.obolibrary.org/obo/CHEBI_24433"},{"id":"A20289","pred":"chebi_id","subj":"T51563","obj":"http://purl.obolibrary.org/obo/CHEBI_22587"},{"id":"A64226","pred":"chebi_id","subj":"T1863","obj":"http://purl.obolibrary.org/obo/CHEBI_32875"},{"id":"A77559","pred":"chebi_id","subj":"T25019","obj":"http://purl.obolibrary.org/obo/CHEBI_29309"},{"id":"A37244","pred":"chebi_id","subj":"T26688","obj":"http://purl.obolibrary.org/obo/CHEBI_24433"},{"id":"A10315","pred":"chebi_id","subj":"T68003","obj":"http://purl.obolibrary.org/obo/CHEBI_32875"},{"id":"A19917","pred":"chebi_id","subj":"T68003","obj":"http://purl.obolibrary.org/obo/CHEBI_29309"},{"id":"A40177","pred":"chebi_id","subj":"T37926","obj":"http://purl.obolibrary.org/obo/CHEBI_35222"},{"subj":"T23665","pred":"source","obj":"LitCovid-PD-CHEBI"},{"subj":"T51563","pred":"source","obj":"LitCovid-PD-CHEBI"},{"subj":"T1863","pred":"source","obj":"LitCovid-PD-CHEBI"},{"subj":"T25019","pred":"source","obj":"LitCovid-PD-CHEBI"},{"subj":"T26688","pred":"source","obj":"LitCovid-PD-CHEBI"},{"subj":"T68003","pred":"source","obj":"LitCovid-PD-CHEBI"},{"subj":"T37926","pred":"source","obj":"LitCovid-PD-CHEBI"}]},{"project":"LitCovid-PubTator","denotations":[{"id":"2436","span":{"begin":145,"end":153},"obj":"Species"},{"id":"2437","span":{"begin":313,"end":318},"obj":"Chemical"}],"attributes":[{"id":"A2436","pred":"tao:has_database_id","subj":"2436","obj":"Tax:694009"},{"subj":"2436","pred":"source","obj":"LitCovid-PubTator"},{"subj":"2437","pred":"source","obj":"LitCovid-PubTator"}],"namespaces":[{"prefix":"Tax","uri":"https://www.ncbi.nlm.nih.gov/taxonomy/"},{"prefix":"MESH","uri":"https://id.nlm.nih.gov/mesh/"},{"prefix":"Gene","uri":"https://www.ncbi.nlm.nih.gov/gene/"},{"prefix":"CVCL","uri":"https://web.expasy.org/cellosaurus/CVCL_"}]},{"project":"LitCovid-sentences","denotations":[{"id":"T675","span":{"begin":0,"end":63},"obj":"Sentence"},{"id":"T676","span":{"begin":64,"end":224},"obj":"Sentence"},{"id":"T677","span":{"begin":225,"end":319},"obj":"Sentence"},{"id":"T678","span":{"begin":320,"end":451},"obj":"Sentence"},{"id":"T679","span":{"begin":452,"end":661},"obj":"Sentence"}],"namespaces":[{"prefix":"_base","uri":"http://pubannotation.org/ontology/tao.owl#"}],"attributes":[{"subj":"T675","pred":"source","obj":"LitCovid-sentences"},{"subj":"T676","pred":"source","obj":"LitCovid-sentences"},{"subj":"T677","pred":"source","obj":"LitCovid-sentences"},{"subj":"T678","pred":"source","obj":"LitCovid-sentences"},{"subj":"T679","pred":"source","obj":"LitCovid-sentences"}]}],"config":{"attribute types":[{"pred":"source","value type":"selection","values":[{"id":"LitCovid-PD-FMA-UBERON","color":"#ecb593","default":true},{"id":"LitCovid-PD-MONDO","color":"#9b93ec"},{"id":"LitCovid-PD-CLO","color":"#a5ec93"},{"id":"LitCovid-PD-CHEBI","color":"#ec93bf"},{"id":"LitCovid-PubTator","color":"#93d9ec"},{"id":"LitCovid-sentences","color":"#ece593"}]}]}}