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PMC:7461420 / 75889-81452 JSONTXT

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LitCovid-PD-FMA-UBERON

Id Subject Object Predicate Lexical cue fma_id
T272 246-254 Body_part denotes proteins http://purl.org/sig/ont/fma/fma67257
T273 447-451 Body_part denotes gene http://purl.org/sig/ont/fma/fma74402
T274 574-582 Body_part denotes cysteine http://purl.org/sig/ont/fma/fma82751
T275 1788-1793 Body_part denotes cells http://purl.org/sig/ont/fma/fma68646
T276 2248-2252 Body_part denotes cell http://purl.org/sig/ont/fma/fma68646
T277 2538-2543 Body_part denotes cells http://purl.org/sig/ont/fma/fma68646
T278 2963-2967 Body_part denotes cell http://purl.org/sig/ont/fma/fma68646
T279 3172-3176 Body_part denotes cell http://purl.org/sig/ont/fma/fma68646
T280 3444-3448 Body_part denotes cell http://purl.org/sig/ont/fma/fma68646
T281 5471-5479 Body_part denotes cysteine http://purl.org/sig/ont/fma/fma82751

LitCovid-PD-MONDO

Id Subject Object Predicate Lexical cue mondo_id
T363 890-894 Disease denotes SARS http://purl.obolibrary.org/obo/MONDO_0005091
T364 1018-1021 Disease denotes HTS http://purl.obolibrary.org/obo/MONDO_0011549
T365 1113-1117 Disease denotes SARS http://purl.obolibrary.org/obo/MONDO_0005091
T366 1836-1840 Disease denotes SARS http://purl.obolibrary.org/obo/MONDO_0005091
T367 1924-1928 Disease denotes SARS http://purl.obolibrary.org/obo/MONDO_0005091
T368 1934-1967 Disease denotes severe acute respiratory syndrome http://purl.obolibrary.org/obo/MONDO_0005091
T369 2465-2469 Disease denotes SARS http://purl.obolibrary.org/obo/MONDO_0005091
T370 3426-3430 Disease denotes SARS http://purl.obolibrary.org/obo/MONDO_0005091
T371 3545-3548 Disease denotes HTS http://purl.obolibrary.org/obo/MONDO_0011549
T372 3627-3631 Disease denotes SARS http://purl.obolibrary.org/obo/MONDO_0005091
T373 3818-3822 Disease denotes SARS http://purl.obolibrary.org/obo/MONDO_0005091
T374 3882-3886 Disease denotes SARS http://purl.obolibrary.org/obo/MONDO_0005091
T375 4111-4115 Disease denotes SARS http://purl.obolibrary.org/obo/MONDO_0005091
T376 4121-4154 Disease denotes severe acute respiratory syndrome http://purl.obolibrary.org/obo/MONDO_0005091
T377 4239-4243 Disease denotes SARS http://purl.obolibrary.org/obo/MONDO_0005091
T378 4472-4476 Disease denotes SARS http://purl.obolibrary.org/obo/MONDO_0005091
T379 4553-4557 Disease denotes SARS http://purl.obolibrary.org/obo/MONDO_0005091
T380 4675-4679 Disease denotes SARS http://purl.obolibrary.org/obo/MONDO_0005091
T381 4755-4759 Disease denotes SARS http://purl.obolibrary.org/obo/MONDO_0005091
T382 4969-4973 Disease denotes SARS http://purl.obolibrary.org/obo/MONDO_0005091
T383 5141-5145 Disease denotes SARS http://purl.obolibrary.org/obo/MONDO_0005091
T384 5250-5254 Disease denotes SARS http://purl.obolibrary.org/obo/MONDO_0005091
T385 5380-5384 Disease denotes SARS http://purl.obolibrary.org/obo/MONDO_0005091

LitCovid-PD-CLO

Id Subject Object Predicate Lexical cue
T901 447-451 http://purl.obolibrary.org/obo/OGG_0000000002 denotes gene
T902 572-573 http://purl.obolibrary.org/obo/CLO_0001020 denotes a
T903 600-606 http://purl.obolibrary.org/obo/CLO_0001658 denotes active
T904 621-622 http://purl.obolibrary.org/obo/CLO_0001020 denotes a
T905 692-693 http://purl.obolibrary.org/obo/CLO_0001020 denotes a
T906 721-722 http://purl.obolibrary.org/obo/CLO_0001020 denotes a
T907 992-994 http://purl.obolibrary.org/obo/CLO_0001313 denotes 36
T908 1025-1026 http://purl.obolibrary.org/obo/CLO_0001020 denotes a
T909 1122-1126 http://purl.obolibrary.org/obo/CLO_0001757 denotes 1 at
T910 1127-1128 http://purl.obolibrary.org/obo/CLO_0001020 denotes a
T911 1234-1235 http://purl.obolibrary.org/obo/CLO_0001020 denotes a
T912 1616-1624 http://purl.obolibrary.org/obo/CLO_0001658 denotes activity
T913 1661-1662 http://purl.obolibrary.org/obo/CLO_0001020 denotes a
T914 1698-1699 http://purl.obolibrary.org/obo/CLO_0001020 denotes a
T915 1771-1779 http://purl.obolibrary.org/obo/CLO_0001658 denotes activity
T916 1783-1787 http://purl.obolibrary.org/obo/CLO_0009524 denotes Vero
T917 1783-1787 http://purl.obolibrary.org/obo/CLO_0050515 denotes Vero
T918 1788-1793 http://purl.obolibrary.org/obo/GO_0005623 denotes cells
T919 1832-1834 http://purl.obolibrary.org/obo/CLO_0001313 denotes 36
T920 2155-2158 http://purl.obolibrary.org/obo/CLO_0001003 denotes 163
T921 2204-2207 http://purl.obolibrary.org/obo/CLO_0001003 denotes 163
T922 2248-2252 http://purl.obolibrary.org/obo/GO_0005623 denotes cell
T923 2270-2273 http://purl.obolibrary.org/obo/CLO_0001003 denotes 163
T924 2308-2318 http://purl.obolibrary.org/obo/CLO_0001658 denotes activities
T925 2453-2461 http://purl.obolibrary.org/obo/CLO_0001658 denotes activity
T926 2506-2514 http://purl.obolibrary.org/obo/CLO_0001658 denotes activity
T927 2533-2537 http://purl.obolibrary.org/obo/CLO_0009524 denotes Vero
T928 2533-2537 http://purl.obolibrary.org/obo/CLO_0050515 denotes Vero
T929 2538-2543 http://purl.obolibrary.org/obo/GO_0005623 denotes cells
T930 2592-2593 http://purl.obolibrary.org/obo/CLO_0001020 denotes a
T931 2723-2724 http://purl.obolibrary.org/obo/CLO_0001020 denotes a
T932 2937-2945 http://purl.obolibrary.org/obo/CLO_0001658 denotes activity
T933 2963-2967 http://purl.obolibrary.org/obo/GO_0005623 denotes cell
T934 3043-3051 http://purl.obolibrary.org/obo/CLO_0001658 denotes activity
T935 3096-3104 http://purl.obolibrary.org/obo/CLO_0001658 denotes activity
T936 3172-3176 http://purl.obolibrary.org/obo/GO_0005623 denotes cell
T937 3219-3221 http://purl.obolibrary.org/obo/CLO_0001313 denotes 36
T938 3253-3263 http://purl.obolibrary.org/obo/CLO_0001658 denotes activities
T939 3384-3392 http://purl.obolibrary.org/obo/CLO_0001658 denotes activity
T940 3435-3448 http://purl.obolibrary.org/obo/CLO_0001757 denotes 1 in the cell
T941 3552-3553 http://purl.obolibrary.org/obo/CLO_0001020 denotes a
T942 3620-3621 http://purl.obolibrary.org/obo/CLO_0001020 denotes a
T943 3865-3866 http://purl.obolibrary.org/obo/CLO_0001020 denotes a
T944 3929-3934 http://purl.obolibrary.org/obo/NCBITaxon_9606 denotes human
T945 4287-4288 http://purl.obolibrary.org/obo/CLO_0001020 denotes a
T946 4520-4521 http://purl.obolibrary.org/obo/CLO_0001020 denotes a
T947 4551-4552 http://purl.obolibrary.org/obo/CLO_0001020 denotes a
T948 5027-5030 http://purl.obolibrary.org/obo/CLO_0001180 denotes 203
T949 5081-5089 http://purl.obolibrary.org/obo/CLO_0001658 denotes activity
T950 5119-5120 http://purl.obolibrary.org/obo/CLO_0001021 denotes B
T951 5291-5292 http://purl.obolibrary.org/obo/CLO_0001020 denotes a
T952 5353-5355 http://purl.obolibrary.org/obo/CLO_0001000 denotes 35
T953 5378-5379 http://purl.obolibrary.org/obo/CLO_0001020 denotes a
T954 5459-5465 http://purl.obolibrary.org/obo/CLO_0001658 denotes active

LitCovid-PD-CHEBI

Id Subject Object Predicate Lexical cue chebi_id
T82062 23-33 Chemical denotes inhibitors http://purl.obolibrary.org/obo/CHEBI_35222
T21071 246-254 Chemical denotes proteins http://purl.obolibrary.org/obo/CHEBI_36080
T24059 425-435 Chemical denotes interferon http://purl.obolibrary.org/obo/CHEBI_52999
T54555 540-554 Chemical denotes antiviral drug http://purl.obolibrary.org/obo/CHEBI_36044
T42980 540-549 Chemical denotes antiviral http://purl.obolibrary.org/obo/CHEBI_22587
T18720 550-554 Chemical denotes drug http://purl.obolibrary.org/obo/CHEBI_23888
T6945 574-582 Chemical denotes cysteine http://purl.obolibrary.org/obo/CHEBI_15356
T3561 694-705 Chemical denotes nucleophile http://purl.obolibrary.org/obo/CHEBI_59740
T22358 731-735 Chemical denotes acid http://purl.obolibrary.org/obo/CHEBI_37527
T29111 736-740 Chemical denotes base http://purl.obolibrary.org/obo/CHEBI_22695
T41910 816-819 Chemical denotes Cys http://purl.obolibrary.org/obo/CHEBI_15356|http://purl.obolibrary.org/obo/CHEBI_17561|http://purl.obolibrary.org/obo/CHEBI_29950
T437 820-822 Chemical denotes SH http://purl.obolibrary.org/obo/CHEBI_29312|http://purl.obolibrary.org/obo/CHEBI_73651
T21797 907-917 Chemical denotes inhibitors http://purl.obolibrary.org/obo/CHEBI_35222
T17235 931-942 Chemical denotes naphthalene http://purl.obolibrary.org/obo/CHEBI_16482
T55336 957-971 Chemical denotes lead compounds http://purl.obolibrary.org/obo/CHEBI_33585
T442 1269-1278 Chemical denotes inhibitor http://purl.obolibrary.org/obo/CHEBI_35222
T41674 1311-1326 Chemical denotes racemic mixture http://purl.obolibrary.org/obo/CHEBI_60911
T43552 1319-1326 Chemical denotes mixture http://purl.obolibrary.org/obo/CHEBI_60004
T96618 1520-1526 Chemical denotes methyl http://purl.obolibrary.org/obo/CHEBI_32875|http://purl.obolibrary.org/obo/CHEBI_29309
T72348 1533-1545 Chemical denotes amino groups http://purl.obolibrary.org/obo/CHEBI_51142
T21234 1533-1538 Chemical denotes amino http://purl.obolibrary.org/obo/CHEBI_46882
T15943 1560-1566 Chemical denotes phenyl http://purl.obolibrary.org/obo/CHEBI_30396
T58369 1761-1770 Chemical denotes antiviral http://purl.obolibrary.org/obo/CHEBI_22587
T22446 1853-1863 Chemical denotes inhibitors http://purl.obolibrary.org/obo/CHEBI_35222
T452 1873-1884 Chemical denotes naphthalene http://purl.obolibrary.org/obo/CHEBI_16482
T453 2056-2061 Chemical denotes amide http://purl.obolibrary.org/obo/CHEBI_29337|http://purl.obolibrary.org/obo/CHEBI_32988
T59470 2062-2064 Chemical denotes NH http://purl.obolibrary.org/obo/CHEBI_29339|http://purl.obolibrary.org/obo/CHEBI_73424
T85501 2107-2116 Chemical denotes benzamide http://purl.obolibrary.org/obo/CHEBI_28179
T21639 2259-2268 Chemical denotes antiviral http://purl.obolibrary.org/obo/CHEBI_22587
T23665 2335-2340 Chemical denotes group http://purl.obolibrary.org/obo/CHEBI_24433
T51563 2496-2505 Chemical denotes antiviral http://purl.obolibrary.org/obo/CHEBI_22587
T1863 2697-2709 Chemical denotes methyl group http://purl.obolibrary.org/obo/CHEBI_32875
T25019 2697-2703 Chemical denotes methyl http://purl.obolibrary.org/obo/CHEBI_29309
T26688 2704-2709 Chemical denotes group http://purl.obolibrary.org/obo/CHEBI_24433
T68003 2803-2809 Chemical denotes methyl http://purl.obolibrary.org/obo/CHEBI_32875|http://purl.obolibrary.org/obo/CHEBI_29309
T37926 2810-2820 Chemical denotes inhibitors http://purl.obolibrary.org/obo/CHEBI_35222
T24619 3283-3289 Chemical denotes fluoro http://purl.obolibrary.org/obo/CHEBI_42645
T84377 3302-3311 Chemical denotes benzamide http://purl.obolibrary.org/obo/CHEBI_28179
T85927 3580-3589 Chemical denotes molecules http://purl.obolibrary.org/obo/CHEBI_25367
T90186 3694-3703 Chemical denotes inhibitor http://purl.obolibrary.org/obo/CHEBI_35222
T3146 4047-4057 Chemical denotes inhibitors http://purl.obolibrary.org/obo/CHEBI_35222
T97002 4195-4205 Chemical denotes thiopurine http://purl.obolibrary.org/obo/CHEBI_35666
T30860 4256-4266 Chemical denotes inhibitors http://purl.obolibrary.org/obo/CHEBI_35222
T25638 4327-4345 Chemical denotes thiocarbonyl group http://purl.obolibrary.org/obo/CHEBI_30256
T11104 4340-4345 Chemical denotes group http://purl.obolibrary.org/obo/CHEBI_24433
T92852 4413-4430 Chemical denotes anticancer agents http://purl.obolibrary.org/obo/CHEBI_35610
T477 4570-4579 Chemical denotes inhibitor http://purl.obolibrary.org/obo/CHEBI_35222
T95879 4628-4633 Chemical denotes group http://purl.obolibrary.org/obo/CHEBI_24433
T71817 4649-4665 Chemical denotes diarylheptanoids http://purl.obolibrary.org/obo/CHEBI_78802
T31826 4742-4751 Chemical denotes inhibitor http://purl.obolibrary.org/obo/CHEBI_35222
T66600 4819-4827 Chemical denotes carbonyl http://purl.obolibrary.org/obo/CHEBI_23019
T28022 4896-4905 Chemical denotes flavonoid http://purl.obolibrary.org/obo/CHEBI_47916|http://purl.obolibrary.org/obo/CHEBI_72544
T44605 5093-5104 Chemical denotes polyphenols http://purl.obolibrary.org/obo/CHEBI_26195
T3152 5329-5339 Chemical denotes Disulfiram http://purl.obolibrary.org/obo/CHEBI_4659
T19310 5397-5406 Chemical denotes inhibitor http://purl.obolibrary.org/obo/CHEBI_35222
T78735 5471-5479 Chemical denotes cysteine http://purl.obolibrary.org/obo/CHEBI_15356

LitCovid-PD-GO-BP

Id Subject Object Predicate Lexical cue
T68 144-161 http://purl.obolibrary.org/obo/GO_0019079 denotes viral replication
T69 144-161 http://purl.obolibrary.org/obo/GO_0019058 denotes viral replication
T70 325-342 http://purl.obolibrary.org/obo/GO_0019079 denotes viral replication
T71 325-342 http://purl.obolibrary.org/obo/GO_0019058 denotes viral replication
T72 387-403 http://purl.obolibrary.org/obo/GO_0016579 denotes deubiquitinating
T73 492-514 http://purl.obolibrary.org/obo/GO_0045087 denotes innate immune response
T74 499-514 http://purl.obolibrary.org/obo/GO_0006955 denotes immune response
T75 3958-3988 http://purl.obolibrary.org/obo/GO_0004843 denotes ubiquitin C‐terminal hydrolase

LitCovid-PubTator

Id Subject Object Predicate Lexical cue tao:has_database_id
2385 5-16 Species denotes Coronavirus Tax:11118
2390 49-53 Gene denotes Mpro Gene:8673700
2391 256-260 Gene denotes nsp1 Gene:10045
2392 261-265 Gene denotes nsp3 Gene:10044
2393 283-287 Gene denotes nsp3 Gene:10044
2404 574-591 Gene denotes cysteine protease Gene:1508
2405 652-658 Chemical denotes Cys112
2406 659-665 Chemical denotes His273
2407 666-672 Chemical denotes Asp287
2408 674-680 Chemical denotes Cys112
2409 711-717 Chemical denotes His273
2410 742-748 Chemical denotes Asp287
2411 755-761 Chemical denotes His273
2412 797-800 Chemical denotes His MESH:D006639
2413 816-819 Chemical denotes Cys MESH:D003545
2418 890-898 Species denotes SARS‐CoV Tax:694009
2419 1113-1121 Species denotes SARS‐CoV Tax:694009
2420 1345-1348 Species denotes SAR Tax:2698737
2421 931-942 Chemical denotes naphthalene MESH:C031721
2426 1902-1922 Gene denotes papain‐like protease
2427 1836-1844 Species denotes SARS‐CoV Tax:694009
2428 1924-1932 Species denotes SARS‐CoV Tax:694009
2429 1873-1884 Chemical denotes naphthalene MESH:C031721
2432 2056-2061 Chemical denotes amide MESH:D000577
2433 2107-2116 Chemical denotes benzamide MESH:C037689
2436 2465-2473 Species denotes SARS‐CoV Tax:694009
2437 2633-2638 Chemical denotes PLpro
2440 3426-3434 Species denotes SARS‐CoV Tax:694009
2441 3281-3311 Chemical denotes m‐fluoro‐substituted benzamide
2452 3958-3988 Gene denotes ubiquitin C‐terminal hydrolase Gene:7345
2453 3991-3998 Gene denotes hUCH‐L1 Gene:7345
2454 4005-4012 Gene denotes hUCH‐L3 Gene:7347
2455 3627-3635 Species denotes SARS‐CoV Tax:694009
2456 3664-3672 Species denotes MERS‐CoV Tax:1335626
2457 3764-3772 Species denotes MERS‐CoV Tax:1335626
2458 3818-3826 Species denotes SARS‐CoV Tax:694009
2459 3882-3890 Species denotes SARS‐CoV Tax:694009
2460 3903-3911 Species denotes MERS‐CoV Tax:1335626
2461 3929-3934 Species denotes human Tax:9606
2464 4089-4109 Gene denotes papain‐like protease
2465 4111-4119 Species denotes SARS‐CoV Tax:694009
2470 4239-4247 Species denotes SARS‐CoV Tax:694009
2471 4195-4205 Chemical denotes thiopurine
2472 4216-4229 Chemical denotes 6‐thioguanine MESH:D013866
2473 4395-4403 Disease denotes toxicity MESH:D064420
2480 4553-4561 Species denotes SARS‐CoV Tax:694009
2481 4675-4683 Species denotes SARS‐CoV Tax:694009
2482 4755-4763 Species denotes SARS‐CoV Tax:694009
2483 4969-4977 Species denotes SARS‐CoV Tax:694009
2484 4522-4532 Chemical denotes tanshinone MESH:C021751
2485 4896-4905 Chemical denotes flavonoid MESH:D005419
2492 5119-5132 Species denotes B. Papyrifera Tax:172644
2493 5141-5149 Species denotes SARS‐CoV Tax:694009
2494 5160-5168 Species denotes MERS‐CoV Tax:1335626
2495 5250-5258 Species denotes SARS‐CoV Tax:694009
2496 5271-5279 Species denotes MERS‐CoV Tax:1335626
2497 5093-5104 Chemical denotes polyphenols MESH:D059808
2501 5380-5388 Species denotes SARS‐CoV Tax:694009
2502 5329-5339 Chemical denotes Disulfiram MESH:D004221
2503 5471-5479 Chemical denotes cysteine MESH:D003545

LitCovid-sentences

Id Subject Object Predicate Lexical cue
T656 0-33 Sentence denotes 3.2 Coronavirus PLpro inhibitors
T657 34-162 Sentence denotes Along with the Mpro, papain‐like protease (PLpro) also cleaves polyproteins which is an important process for viral replication.
T658 163-267 Sentence denotes PLpro cleaves at the first three positions creating three nonstructural functional proteins (nsp1‐nsp3).
T659 268-351 Sentence denotes In particular, nsp3 is central for the generation of the viral replication complex.
T660 352-562 Sentence denotes The multifunctionality of PLpro in deubiquitinating, de‐ISGylation (ISG: interferon‐stimulated gene), 195 , 196 and in the evasion of the innate immune response make PLpro an attractive antiviral drug target.
T661 563-673 Sentence denotes PLpro is a cysteine protease and its active site contains a catalytic triad composing of Cys112‐His273‐Asp287.
T662 674-741 Sentence denotes Cys112 behaves as a nucleophile, and His273 is a general acid‐base.
T663 742-823 Sentence denotes Asp287 helps His273 to align perfectly, thus promoting His to deprotonate Cys‐SH.
T664 824-836 Sentence denotes Ghosh et al.
T665 837-952 Sentence denotes 197 contributed significantly to the development of SARS‐CoV‐1 PLpro inhibitors based on the naphthalene scaffold.
T666 953-1085 Sentence denotes Two lead compounds 157 and 158 (Figure 36) were identified by an HTS of a chemical library containing greater than 50 000 compounds.
T667 1086-1182 Sentence denotes They both inhibit PLpro of SARS‐CoV‐1 at a moderate potency (IC50 20.1 and 59 µM, respectively).
T668 1183-1333 Sentence denotes The (R)‐enantiomer of compound 157 was found to be a greater than twofold more potent inhibitor of PLpro when compared with its racemic mixture (157).
T669 1334-1572 Sentence denotes Subsequent SAR studies highlighted the 2‐naphthyl substitution as an important structural requirement rather than at the position 1 of the naphthyl ring in addition to the presence of o‐methyl and m‐amino groups, in the other phenyl ring.
T670 1573-1721 Sentence denotes Compound 159 displayed the best inhibitory activity of PLpro (IC50, 0.6 µM) and acts in a noncovalent reversible manner with a K i value of 0.49 µM.
T671 1722-1824 Sentence denotes 198 Compound 159 also showed moderate antiviral activity in Vero cells with an EC50 value of 14.5 µM.
T672 1825-1894 Sentence denotes Figure 36 SARS‐CoV‐1 PLpro inhibitors based on naphthalene scaffold.
T673 1895-2132 Sentence denotes PLpro, papain‐like protease; SARS‐CoV, severe acute respiratory syndrome coronavirus Compound 159 was further scrutinized by investigating the importance of the amide NH, and the effect of the substituent on the benzamide ring (160–164).
T674 2133-2319 Sentence denotes Among them, compounds 163 and 164 exhibited the most potent enzymatic (163: IC50, 0.46 µM; 164: IC50, 1.23 µM) and cell‐based antiviral (163: EC50, 6.0 µM; 164: EC50, 5.2 µM) activities.
T675 2320-2383 Sentence denotes Next, the same group studied the SARs for compound 158 further.
T676 2384-2544 Sentence denotes 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.
T677 2545-2639 Sentence denotes 199 The mode of action of 165 was found to be a noncovalent, competitive inhibition of PLpro.
T678 2640-2771 Sentence denotes Unlike the previous series, the stereochemistry at the α‐methyl group did not make a significant difference in inhibition of PLpro.
T679 2772-2981 Sentence denotes 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.
T680 2982-3052 Sentence denotes Further SARs of 159 and 165 were investigated to improve the activity.
T681 3053-3192 Sentence denotes However, no significant improvement in the activity was observed for the prepared compounds either in the enzymatic or cell‐based bioassay.
T682 3193-3264 Sentence denotes Compounds 167–169 (Figure 36) displayed the best inhibitory activities.
T683 3265-3407 Sentence denotes Especially, the m‐fluoro‐substituted benzamide derivative 168 (IC50, 0.15 µM; EC50, 5.4 µM) showed the best inhibition activity against PLpro.
T684 3408-3464 Sentence denotes It also inhibited SARS‐CoV‐1 in the cell‐based bioassay.
T685 3465-3544 Sentence denotes Both compounds 168 and 169 were metabolically more stable when compared to 167.
T686 3545-3704 Sentence denotes HTS of a chemical library of 25000 molecules identified 170 (Figure 37) as a dual SARS‐CoV‐1 PLpro (IC50, 10.9 µM) and MERS‐CoV PLpro (IC50, 6.2 µM) inhibitor.
T687 3705-3835 Sentence denotes 200 This compound acts via competitive inhibition against MERS‐CoV PLpro, yet via allosteric inhibition against SARS‐CoV‐1 PLpro.
T688 3836-4014 Sentence denotes This compound also exhibited a preference for SARS‐CoV‐1 PLpro and MERS‐CoV PLpro versus two human homologs of the PLpro, ubiquitin C‐terminal hydrolase, (hUCH‐L1) and (hUCH‐L3).
T689 4015-4081 Sentence denotes Figure 37 Broad spectral PLpro inhibitors from different sources.
T690 4082-4178 Sentence denotes PLpro, papain‐like protease; SARS‐CoV, severe acute respiratory syndrome coronavirus Chou et al.
T691 4179-4322 Sentence denotes 201 identified thiopurine (171) and 6‐thioguanine (172) as SARS‐CoV‐1 PLpro inhibitors by the screening of a library containing 160 compounds.
T692 4323-4381 Sentence denotes The thiocarbonyl group was important for PLpro inhibition.
T693 4382-4484 Sentence denotes However, the toxicity of these anticancer agents limits their therapeutic utility as anti‐SARS agents.
T694 4485-4505 Sentence denotes In 2012, Park et al.
T695 4506-4609 Sentence denotes 202 reported a tanshinone derivative 173 as a SARS‐CoV‐1 PLpro inhibitor with an IC50 value of 0.8 µM.
T696 4610-4692 Sentence denotes The same research group also described diarylheptanoids blocking SARS‐CoV‐1 PLpro.
T697 4693-4799 Sentence denotes In particular compound 174 performed as the best inhibitor of SARS‐CoV PLpro with an IC50 value of 4.1 µM.
T698 4800-4879 Sentence denotes An α,β‐unsaturated carbonyl functionality was crucial for effective inhibition.
T699 4880-5026 Sentence denotes The geranylated flavonoid 175 was another plant‐derived natural product, which displayed SARS‐CoV‐1 PLpro inhibition with an IC50 value of 5.0 µM.
T700 5027-5030 Sentence denotes 203
T701 5031-5051 Sentence denotes In 2017, Park et al.
T702 5052-5121 Sentence denotes 204 assessed the inhibitory activity of polyphenols isolated from B.
T703 5122-5175 Sentence denotes Papyrifera against SARS‐CoV PLpro and MERS‐CoV PLpro.
T704 5176-5328 Sentence denotes Two of them (176 and 177 Figure 37) displayed moderate inhibition at both SARS‐CoV‐1 PLpro and MERS‐CoV PLpro with a noncompetitive mechanism of action.
T705 5329-5563 Sentence denotes Disulfiram (151; Figure 35) was also reported as a SARS‐CoV‐1 PLpro inhibitor (IC50, 24.1 µM), 205 probably by reacting with the active site cysteine, thereby covalently modifying the enzyme target, as was reported for other targets.