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Assay Detail

CHEMBL5139999

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of SARS-CoV-2 3CL protease expressed in Escherichia coli BL21 (DE3) cells assessed as change in relative fluorescence unit using MCA-TSAVLQSGFRK(DNP)M as substrate preincubated for 30 mins followed by substrate addition and measured after 2 hrs by microplate reader based FRET assay
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Severe acute respiratory syndrome coronavirus 2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Replicase polyprotein 1ab (CHEMBL4523582)
Type SINGLE PROTEIN
Organism Severe acute respiratory syndrome coronavirus 2

Publication

The structure-based design of peptidomimetic inhibitors against SARS-CoV-2 3C like protease as Potent anti-viral drug candidate.
Wang H, Pei R, Li X, Deng W, Xing S, Zhang Y, Zhang C, He S, Sun H, Xiao S, Xiong J, Zhang Y, Chen X, Wang Y, Guo Y, Zhang B, Shang L.
Eur J Med Chem (2022) 238 : 114458 -114458
PubMed 35635946 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 6.31 6.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5192273 1 6.83
CHEMBL5206326 1 6.82
CHEMBL5197113 1 6.76
CHEMBL5185152 1 6.76
CHEMBL5199219 1 6.76
CHEMBL5189683 1 6.71
CHEMBL5176330 1 6.71
CHEMBL5182229 1 6.70
CHEMBL5205787 1 6.68
CHEMBL5192541 1 6.66
CHEMBL5189974 1 6.64
CHEMBL5175884 1 6.63
CHEMBL5207843 1 6.60
CHEMBL5191197 1 6.59
CHEMBL5198279 1 6.59
CHEMBL5203574 1 6.57
CHEMBL5207566 1 6.56
CHEMBL5183017 1 6.55
CHEMBL5173399 1 6.54
CHEMBL5179730 1 6.53
CHEMBL5169416 1 6.53
CHEMBL5199094 1 6.53
CHEMBL5201697 1 6.51
CHEMBL3885329 1 6.49
CHEMBL5190907 1 6.45
CHEMBL5195478 1 6.43
CHEMBL5200040 1 6.43
CHEMBL5191663 1 6.39
CHEMBL5172144 1 6.26
CHEMBL5197105 1 6.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5192273 IC50 = 148.0 nM 6.83
CHEMBL5206326 IC50 = 153.0 nM 6.82
CHEMBL5185152 IC50 = 172.0 nM 6.76
CHEMBL5199219 IC50 = 173.0 nM 6.76
CHEMBL5197113 IC50 = 173.0 nM 6.76
CHEMBL5189683 IC50 = 197.0 nM 6.71
CHEMBL5176330 IC50 = 196.0 nM 6.71
CHEMBL5182229 IC50 = 199.0 nM 6.70
CHEMBL5205787 IC50 = 209.0 nM 6.68
CHEMBL5192541 IC50 = 221.0 nM 6.66
CHEMBL5189974 IC50 = 230.0 nM 6.64
CHEMBL5175884 IC50 = 234.0 nM 6.63
CHEMBL5207843 IC50 = 249.0 nM 6.60
CHEMBL5191197 IC50 = 257.0 nM 6.59
CHEMBL5198279 IC50 = 255.0 nM 6.59
CHEMBL5203574 IC50 = 271.0 nM 6.57
CHEMBL5207566 IC50 = 277.0 nM 6.56
CHEMBL5183017 IC50 = 281.0 nM 6.55
CHEMBL5173399 IC50 = 285.0 nM 6.54
CHEMBL5199094 IC50 = 298.0 nM 6.53
CHEMBL5179730 IC50 = 295.0 nM 6.53
CHEMBL5169416 IC50 = 295.0 nM 6.53
CHEMBL5201697 IC50 = 307.0 nM 6.51
CHEMBL3885329 IC50 = 321.0 nM 6.49
CHEMBL5190907 IC50 = 357.0 nM 6.45
CHEMBL5195478 IC50 = 374.0 nM 6.43
CHEMBL5200040 IC50 = 373.0 nM 6.43
CHEMBL5191663 IC50 = 404.0 nM 6.39
CHEMBL5172144 IC50 = 543.0 nM 6.26
CHEMBL5197105 IC50 = 565.0 nM 6.25
CHEMBL5189874 IC50 = 592.0 nM 6.23
CHEMBL5179883 IC50 = 640.0 nM 6.19
CHEMBL4764751 IC50 = 858.0 nM 6.07
CHEMBL5207769 IC50 = 1338.0 nM 5.87
CHEMBL5179310 IC50 = 1409.0 nM 5.85
CHEMBL5182755 IC50 = 1426.0 nM 5.85
CHEMBL5174138 IC50 = 1497.0 nM 5.83
CHEMBL5186446 IC50 = 2044.0 nM 5.69
CHEMBL5173857 IC50 = 3275.0 nM 5.49
CHEMBL5182830 IC50 = 3436.0 nM 5.46
CHEMBL5180964 IC50 = 3889.0 nM 5.41
CHEMBL3884779 IC50 = 6928.0 nM 5.16
CHEMBL5203407 IC50 = 12320.0 nM 4.91