WU-04
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.4
|
pKd |
30 |
|
⤷ |
pKd
7.4
(Kd 3.7x10-8 M)
[30]
Description: binding to SARS-CoV-2 Mpro
|
compound 19 [PMID: 35142215]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.4
|
pKd |
41 |
|
⤷ |
pKd
7.4
(Kd 3.8x10-8 M)
[41]
Description: Binding affinity
|
nirmatrelvir
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
9.6
|
pKi |
46 |
|
⤷ |
pKi
9.6
(Ki 2.71x10-10 M)
[46]
Description: Determined in vitro, in a TR-FRET enzyme assay
|
PF-00835231
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV |
Inhibition
|
8.4
|
pKi |
29 |
|
⤷ |
pKi
8.4
(Ki 4x10-9 M)
[29]
Description: Determined using an in vitro SARS-CoV-1 3CLpro FRET assay.
|
YH-53
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV |
Inhibition
|
8.2
|
pKi |
55 |
|
⤷ |
pKi
8.2
(Ki 6.3x10-9 M)
[55]
|
example 10 [WO2022129953]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
8.2
|
pKi |
12 |
|
⤷ |
pKi
8.2
(Ki 6.3x10-9 M)
[12]
|
compound 17 [PMID: 33655614]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
8.0
|
pKi |
6 |
|
⤷ |
pKi
8.0
(Ki 1x10-8 M)
[6]
|
compound 8 [PMID: 33655614]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.6
|
pKi |
6 |
|
⤷ |
pKi
7.6
(Ki 2.4x10-8 M)
[6]
|
YH-53
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.5 – 7.8
|
pKi |
23,27,33 |
|
⤷ |
pKi
7.8
(Ki 1.76x10-8 M)
[23,27]
pKi
7.5
(Ki 3.47x10-8 M)
[33]
|
CDD-1976
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.4
|
pKi |
8 |
|
⤷ |
pKi
7.4
(Ki 3.7x10-8 M)
[8]
|
TG-0205221
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV |
Inhibition
|
7.3
|
pKi |
68 |
|
⤷ |
pKi
7.3
(Ki 5.3x10-8 M)
[68]
|
TG-0203770
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV |
Inhibition
|
7.2
|
pKi |
36 |
|
⤷ |
pKi
7.2
(Ki 5.8x10-8 M)
[36]
|
compound 7d [PMID: 34528437]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.1
|
pKi |
23 |
|
⤷ |
pKi
7.1
(Ki 7.3x10-8 M)
[23]
|
compound 3 [PMID: 16884309]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV |
Inhibition
|
6.2
|
pKi |
68 |
|
⤷ |
pKi
6.2
(Ki 6.6x10-7 M)
[68]
|
boceprevir
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
5.9
|
pKi |
42 |
|
⤷ |
pKi
5.9
(Ki 1.18x10-6 M)
[42]
Description: Inhibition of recombinat enzyme in vitro.
|
Z-AVLD-FMK
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
9.1
|
pIC50 |
43 |
|
⤷ |
pIC50
9.1
(IC50 8x10-10 M)
[43]
Description: Inhibition in a FRET-based enzyme activity assay
|
compound 6 [WO2022133588]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
9.0
|
pIC50 |
45 |
|
⤷ |
pIC50
9.0
(IC50 1x10-9 M)
[45]
|
example 18 [WO2022013684]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
8.8
|
pIC50 |
47 |
|
⤷ |
pIC50
8.8
(IC50 1.55x10-9 M)
[47]
|
YH-6
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
8.4
|
pIC50 |
28 |
|
⤷ |
pIC50
8.4
(IC50 3.8x10-9 M)
[28]
|
compound 15g {PMID: 34242027]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
8.2
|
pIC50 |
3 |
|
⤷ |
pIC50
8.2
(IC50 6.4x10-9 M)
[3]
|
compound 17 [PMID: 33655614]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV |
Inhibition
|
8.1
|
pIC50 |
5 |
|
⤷ |
pIC50
8.1
(IC50 7x10-9 M)
[5]
|
example 37 [WO2022021841A1]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
8.1
|
pIC50 |
|
|
⤷ |
pIC50
8.1
(IC50 7x10-9 M)
Description: In vitro enzymatic activity inhibition
|
TKB245
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
8.1
|
pIC50 |
44 |
|
⤷ |
pIC50
8.1
(IC50 7x10-9 M)
[44]
Description: inhibition of enzyme activity
|
MI-23
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
8.1
|
pIC50 |
50 |
|
⤷ |
pIC50
8.1
(IC50 7.6x10-9 M)
[50]
Description: Inhibition of recombinant enzyme in vitro
|
MI-21
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
8.1
|
pIC50 |
50 |
|
⤷ |
pIC50
8.1
(IC50 7.6x10-9 M)
[50]
|
PF-00835231
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
8.1
|
pIC50 |
61 |
|
⤷ |
pIC50
8.1
(IC50 8x10-9 M)
[61]
|
TG-0205221
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
8.1
|
pIC50 |
61 |
|
⤷ |
pIC50
8.1
(IC50 9x10-9 M)
[61]
|
MI-28
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
8.0
|
pIC50 |
50 |
|
⤷ |
pIC50
8.0
(IC50 9.2x10-9 M)
[50]
|
UAWJ248
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.9
|
pIC50 |
53 |
|
⤷ |
pIC50
7.9
(IC50 1.2x10-8 M)
[53]
|
MI-13
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.9
|
pIC50 |
50 |
|
⤷ |
pIC50
7.9
(IC50 1.24x10-8 M)
[50]
|
ensitrelvir
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.9
|
pIC50 |
59 |
|
⤷ |
pIC50
7.9
(IC50 1.3x10-8 M)
[59]
|
MI-14
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.9
|
pIC50 |
50 |
|
⤷ |
pIC50
7.9
(IC50 1.3x10-8 M)
[50]
|
3CL protease (Mpro) inhibitor M3
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.9
|
pIC50 |
25 |
|
⤷ |
pIC50
7.9
(IC50 1.3x10-8 M)
[25]
|
MI-05
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.9
|
pIC50 |
50 |
|
⤷ |
pIC50
7.9
(IC50 1.32x10-8 M)
[50]
|
MI-11
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.9
|
pIC50 |
50 |
|
⤷ |
pIC50
7.9
(IC50 1.33x10-8 M)
[50]
|
compound 15m [PMID: 34242027]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.8
|
pIC50 |
3 |
|
⤷ |
pIC50
7.8
(IC50 1.4x10-8 M)
[3]
|
SY110
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.8
|
pIC50 |
31 |
|
⤷ |
pIC50
7.8
(IC50 1.44x10-8 M)
[31]
|
MI-06
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.8
|
pIC50 |
50 |
|
⤷ |
pIC50
7.8
(IC50 1.45x10-8 M)
[50]
|
MI-09
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.8
|
pIC50 |
50 |
|
⤷ |
pIC50
7.8
(IC50 1.52x10-8 M)
[50]
Description: Inhibition of recombinant enzyme in vitro
|
NK01-63
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.8
|
pIC50 |
39 |
|
⤷ |
pIC50
7.8
(IC50 1.6x10-8 M)
[39]
|
MI-30
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.8
|
pIC50 |
50 |
|
⤷ |
pIC50
7.8
(IC50 1.72x10-8 M)
[50]
Description: Inhibition of recombinant enzyme in vitro
|
compound 15l [PMID: 34242027]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.7
|
pIC50 |
3 |
|
⤷ |
pIC50
7.7
(IC50 1.9x10-8 M)
[3]
Description: Inhibition of enzymatic activity in a FRET-based kinetic assay.
|
CCF981
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV |
Inhibition
|
7.7
|
pIC50 |
26 |
|
⤷ |
pIC50
7.7
(IC50 1.9x10-8 M)
[26]
|
compound 21 [PMID: 33786375]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.7
|
pIC50 |
73 |
|
⤷ |
pIC50
7.7
(IC50 1.9x10-8 M)
[73]
|
compound 58 [WO2021252491A1]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
>7.7
|
pIC50 |
60 |
|
⤷ |
pIC50
>7.7
(IC50 <2x10-8 M)
[60]
|
GDI-036
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.7
|
pIC50 |
40 |
|
⤷ |
pIC50
7.7
(IC50 2x10-8 M)
[40]
|
example 100 [WO2022043374]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.6
|
pIC50 |
9 |
|
⤷ |
pIC50
7.6
(IC50 2.4x10-8 M)
[9]
|
compound 23 [PMID: 33786375]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.6
|
pIC50 |
73 |
|
⤷ |
pIC50
7.6
(IC50 2.4x10-8 M)
[73]
|
nirmatrelvir
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.5 – 7.7
|
pIC50 |
41 |
|
⤷ |
pIC50
7.7
(IC50 1.9x10-8 M)
Value provided at a session by Dafydd Owen (Pfizer) at the ACS Spring 2021 meeting; not yet published
pIC50
7.5
(IC50 3.3x10-8 M)
[41]
|
bofutrelvir
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.3 – 7.8
|
pIC50 |
15,61 |
|
⤷ |
pIC50
7.8
(IC50 1.4x10-8 M)
[61]
pIC50
7.3
(IC50 5.3x10-8 M)
[15]
Description: In vitro inhibition of recombinant SARS-CoV-2 Mpro enzymatic activity.
|
compound 11b [PMID: 32321856]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.4 – 7.6
|
pIC50 |
15,61 |
|
⤷ |
pIC50
7.6
(IC50 2.3x10-8 M)
[61]
pIC50
7.4
(IC50 4x10-8 M)
[15]
Description: In vitro inhibition of recombinant SARS-CoV-2 Mpro enzymatic activity.
|
GRL-0496
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV |
Inhibition
|
7.5
|
pIC50 |
22 |
|
⤷ |
pIC50
7.5
(IC50 3x10-8 M)
[22]
|
example 100 [WO2022043374]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV |
Inhibition
|
7.5
|
pIC50 |
9 |
|
⤷ |
pIC50
7.5
(IC50 3.1x10-8 M)
[9]
|
MP13
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.5
|
pIC50 |
67 |
|
⤷ |
pIC50
7.5
(IC50 3.3x10-8 M)
[67]
|
example 4 [WO2017114509]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.5
|
pIC50 |
14 |
|
⤷ |
pIC50
7.5
(IC50 3.4x10-8 M)
[14]
|
ML1000
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.5
|
pIC50 |
64 |
|
⤷ |
pIC50
7.5
(IC50 3.4x10-8 M)
[64]
|
compound 19 [PMID: 33786375]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.4
|
pIC50 |
70 |
|
⤷ |
pIC50
7.4
(IC50 4.4x10-8 M)
[70]
Description: Inhibition of Mpro proteolytic activity, determined using a substrate peptide cleavage FRET assay.
|
GC-376
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV |
Inhibition
|
7.3 – 7.4
|
pIC50 |
62,65 |
|
⤷ |
pIC50
7.4
(IC50 4.1x10-8 M)
[65]
pIC50
7.3
(IC50 5x10-8 M)
[62]
|
GRL-0496
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.3
|
pIC50 |
49 |
|
⤷ |
pIC50
7.3
(IC50 5x10-8 M)
[49]
|
compound 15c [PMID: 34865476]
|
|
|
|
|
|
|
|
|
|
|
MERS-CoV |
Inhibition
|
7.3
|
pIC50 |
18 |
|
⤷ |
pIC50
7.3
(IC50 5x10-8 M)
[18]
|
UAWJ9-36-3
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.3
|
pIC50 |
65 |
|
⤷ |
pIC50
7.3
(IC50 5.4x10-8 M)
[65]
|
WU-04
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV |
Inhibition
|
7.3
|
pIC50 |
30 |
|
⤷ |
pIC50
7.3
(IC50 5.5x10-8 M)
[30]
Description: inhibition of SARS-CoV Mpro
|
example 45 [WO2022229458]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.2
|
pIC50 |
7 |
|
⤷ |
pIC50
7.2
(IC50 5.7x10-8 M)
[7]
|
compound 17 [PMID: 34408808]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.2
|
pIC50 |
72 |
|
⤷ |
pIC50
7.2
(IC50 5.9x10-8 M)
[72]
|
INSCoV-614 (1B)
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.2
|
pIC50 |
69 |
|
⤷ |
pIC50
7.2
(IC50 6x10-8 M)
[69]
|
compound 21 [PMID: 34408808]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.2
|
pIC50 |
70 |
|
⤷ |
pIC50
7.2
(IC50 6.1x10-8 M)
[70]
Description: Inhibition of Mpro proteolytic activity, determined using a substrate peptide cleavage FRET assay.
|
compound 16 [PMID: 34408808]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.2
|
pIC50 |
72 |
|
⤷ |
pIC50
7.2
(IC50 6.1x10-8 M)
[72]
|
compound 21 [PMID: 34347470]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.2
|
pIC50 |
26 |
|
⤷ |
pIC50
7.2
(IC50 6.3x10-8 M)
[26]
|
compound 17 [PMID: 33655614]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.2
|
pIC50 |
61 |
|
⤷ |
pIC50
7.2
(IC50 6.5x10-8 M)
[61]
|
CCF981
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.2
|
pIC50 |
26 |
|
⤷ |
pIC50
7.2
(IC50 6.8x10-8 M)
[26]
|
GC-373
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV |
Inhibition
|
7.2
|
pIC50 |
62 |
|
⤷ |
pIC50
7.2
(IC50 7x10-8 M)
[62]
|
WU-04
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.1
|
pIC50 |
30 |
|
⤷ |
pIC50
7.1
(IC50 7.2x10-8 M)
[30]
Description: enzyme inhibition
|
compound 15 [PMID: 34438124]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.1
|
pIC50 |
13 |
|
⤷ |
pIC50
7.1
(IC50 7.2x10-8 M)
[13]
|
compound 19 [PMID: 35142215]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.1
|
pIC50 |
41 |
|
⤷ |
pIC50
7.1
(IC50 7.7x10-8 M)
[41]
Description: Inhibtion of protease activity
|
PET-UNK-29afea89-2
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.1
|
pIC50 |
24 |
|
⤷ |
pIC50
7.1
(IC50 8x10-8 M)
[24]
|
compound 2i [PMID: 23245752]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.0
|
pIC50 |
61 |
|
⤷ |
pIC50
7.0
(IC50 9.4x10-8 M)
[61]
|
UAWJ9-36-3
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV |
Inhibition
|
7.0
|
pIC50 |
65 |
|
⤷ |
pIC50
7.0
(IC50 9.9x10-8 M)
[65]
|
compound 19 [PMID: 34347470]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.0
|
pIC50 |
26 |
|
⤷ |
pIC50
7.0
(IC50 1.06x10-7 M)
[26]
|
compound 13 [PMID: 33984473]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
7.0
|
pIC50 |
21 |
|
⤷ |
pIC50
7.0
(IC50 1.1x10-7 M)
[21]
|
GC-376
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
6.4 – 7.5
|
pIC50 |
19,41-42,62,65 |
|
⤷ |
pIC50
7.5
(IC50 3x10-8 M)
[42]
pIC50
7.4
(IC50 4.1x10-8 M)
[65]
pIC50
7.1
(IC50 7.3x10-8 M)
[41]
pIC50
6.7
(IC50 1.9x10-7 M)
[62]
pIC50
6.4
(IC50 4.1x10-7 M)
[19]
|
GC-373
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
6.4 – 7.4
|
pIC50 |
61-62 |
|
⤷ |
pIC50
7.4
(IC50 4.2x10-8 M)
[61]
pIC50
6.4
(IC50 4x10-7 M)
[62]
|
compound 14 [PMID: 33786375]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
6.9
|
pIC50 |
73 |
|
⤷ |
pIC50
6.9
(IC50 1.29x10-7 M)
[73]
|
compound 5 [Zhang et al., 2021]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
6.8
|
pIC50 |
71 |
|
⤷ |
pIC50
6.8
(IC50 1.4x10-7 M)
[71]
|
compound 6e [PMID: 32747425]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
6.8
|
pIC50 |
51 |
|
⤷ |
pIC50
6.8
(IC50 1.7x10-7 M)
[51]
|
compound 15c [PMID: 34865476]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
6.8
|
pIC50 |
18 |
|
⤷ |
pIC50
6.8
(IC50 1.7x10-7 M)
[18]
|
compound 1 [PMID: 34210738]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
6.8
|
pIC50 |
19 |
|
⤷ |
pIC50
6.8
(IC50 1.7x10-7 M)
[19]
|
compound 40 [PMID: 34347470]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
6.8
|
pIC50 |
26 |
|
⤷ |
pIC50
6.8
(IC50 1.71x10-7 M)
[26]
|
compound 11r [PMID: 32045235]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
6.7
|
pIC50 |
75 |
|
⤷ |
pIC50
6.7
(IC50 1.8x10-7 M)
[75]
|
compound 2a [PMID: 34213885]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
6.7
|
pIC50 |
16 |
|
⤷ |
pIC50
6.7
(IC50 1.8x10-7 M)
[16]
Description: Determined in a FRET enzyme assay.
|
MAT-POS-932d1078-3
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
6.7
|
pIC50 |
57 |
|
⤷ |
pIC50
6.7
(IC50 1.91x10-7 M)
[57]
|
MAT-POS-b3e365b9-1
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
6.7
|
pIC50 |
24 |
|
⤷ |
pIC50
6.7
(IC50 2x10-7 M)
[24]
|
example I-1 [WO2023283831]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
>6.7
|
pIC50 |
54 |
|
⤷ |
pIC50
>6.7
(IC50 <2x10-7 M)
[54]
|
compound 10c [PMID: 35638577]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
6.6
|
pIC50 |
17 |
|
⤷ |
pIC50
6.6
(IC50 2.4x10-7 M)
[17]
|
walrycin B
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
6.6
|
pIC50 |
78 |
|
⤷ |
pIC50
6.6
(IC50 2.6x10-7 M)
[78]
Description: Inhibition determined in an HTS fluorogenic enzyme activity assay.
|
compound 3 [PMID: 16884309]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
6.5
|
pIC50 |
61 |
|
⤷ |
pIC50
6.5
(IC50 2.86x10-7 M)
[61]
|
compound 10c [PMID: 35638577]
|
|
|
|
|
|
|
|
|
|
|
MERS-CoV |
Inhibition
|
6.5
|
pIC50 |
17 |
|
⤷ |
pIC50
6.5
(IC50 3.3x10-7 M)
[17]
|
DAV-CRI-14a23e73-1
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
6.3
|
pIC50 |
49 |
|
⤷ |
pIC50
6.3
(IC50 4.7x10-7 M)
[49]
|
compound 6j [PMID: 32747425]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
6.3
|
pIC50 |
51 |
|
⤷ |
pIC50
6.3
(IC50 4.8x10-7 M)
[51]
|
compound 13b [PMID: 32198291]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
6.2
|
pIC50 |
75 |
|
⤷ |
pIC50
6.2
(IC50 6.7x10-7 M)
[75]
|
compound 6e [PMID: 32747425]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV |
Inhibition
|
6.1
|
pIC50 |
51 |
|
⤷ |
pIC50
6.1
(IC50 9x10-7 M)
[51]
|
WU-04
|
|
|
|
|
|
|
|
|
|
|
MERS-CoV |
Inhibition
|
6.0
|
pIC50 |
|
|
⤷ |
pIC50
6.0
(IC50 1.02x10-6 M)
Description: inhibition of MERS-CoV Mpro
|
compound 6j [PMID: 32747425]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV |
Inhibition
|
5.9
|
pIC50 |
51 |
|
⤷ |
pIC50
5.9
(IC50 1.2x10-6 M)
[51]
|
boceprevir
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV |
Inhibition
|
5.6 – 6.0
|
pIC50 |
1,4 |
|
⤷ |
pIC50
5.6 – 6.0
(IC50 2.5x10-6 – 9.49x10-7 M)
[1,4]
|
compound 2i [PMID: 23245752]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV |
Inhibition
|
5.8
|
pIC50 |
34 |
|
⤷ |
pIC50
5.8
(IC50 1.7x10-6 M)
[34]
|
MG-132
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
5.4
|
pIC50 |
42 |
|
⤷ |
pIC50
5.4
(IC50 3.9x10-6 M)
[42]
|
boceprevir
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
5.4
|
pIC50 |
42 |
|
⤷ |
pIC50
5.4
(IC50 4.13x10-6 M)
[42]
|
ML300
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV |
Inhibition
|
5.3 – 5.4
|
pIC50 |
26,58 |
|
⤷ |
pIC50
5.4
(IC50 4.1x10-6 M)
[58]
pIC50
5.3
(IC50 4.45x10-6 M)
[26]
|
compound 451 [WO2021252644A1]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
5.0 – 5.7
|
pIC50 |
2 |
|
⤷ |
pIC50
5.0 – 5.7
(IC50 1x10-5 – 2x10-6 M)
[2]
Description: In vitro inhibition of Mpro; binned IC50 value
|
ML300
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
5.3
|
pIC50 |
26 |
|
⤷ |
pIC50
5.3
(IC50 4.99x10-6 M)
[26]
|
MG-115
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
5.2
|
pIC50 |
42 |
|
⤷ |
pIC50
5.2
(IC50 6.14x10-6 M)
[42]
|
PRD_002214
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV |
Inhibition
|
5.1
|
pIC50 |
66 |
|
⤷ |
pIC50
5.1
(IC50 9x10-6 M)
[66]
|
calpeptin
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
5.0
|
pIC50 |
42 |
|
⤷ |
pIC50
5.0
(IC50 1.069x10-5 M)
[42]
|
telaprevir
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
4.9
|
pIC50 |
48 |
|
⤷ |
pIC50
4.9
(IC50 1.147x10-5 M)
[48]
|
Z-FA-FMK
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Inhibition
|
4.9
|
pIC50 |
78 |
|
⤷ |
pIC50
4.9
(IC50 1.139x10-5 M)
[78]
Description: Inhibition determined in an HTS fluorogenic enzyme activity assay.
|
compound 25c [PMID: 23747811]
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV |
Inhibition
|
4.7
|
pIC50 |
56 |
|
⤷ |
pIC50
4.7
(IC50 2.1x10-5 M)
[56]
|
PRD_002214
|
|
|
|
|
|
|
|
|
|
|
SARS-CoV-2 |
Irreversible inhibition
|
-
|
- |
32 |
|
⤷ |
[32]
|