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Assay Detail

CHEMBL5117300

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

Binding
Inhibition of His/SUMO tagged SARS-CoV2 main protease expressed in Escherichia coli BL21 (DE3) cells using Dabcyl-KTSAVLQSGFRKME-Edans as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by fluorescence plate reader analysis
20
Total Activities
20
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

A multi-pronged evaluation of aldehyde-based tripeptidyl main protease inhibitors as SARS-CoV-2 antivirals.
Ma Y, Yang KS, Geng ZZ, Alugubelli YR, Shaabani N, Vatansever EC, Ma XR, Cho CC, Khatua K, Xiao J, Blankenship LR, Yu G, Sankaran B, Li P, Allen R, Ji H, Xu S, Liu WR.
Eur J Med Chem (2022) 240 : 114570 -114570
PubMed 35779291 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.35 8.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5205477 1 8.32
CHEMBL5189578 1 8.28
CHEMBL5208464 1 8.08
CHEMBL5178875 1 7.96
CHEMBL5178556 1 7.89
CHEMBL5185670 1 7.80
CHEMBL5202866 1 7.72
CHEMBL5205992 1 7.52
CHEMBL5203715 1 7.44
CHEMBL5204033 1 7.31
CHEMBL5203726 1 7.28
CHEMBL5176166 1 7.22
CHEMBL5201264 1 7.18
CHEMBL5169820 1 7.11
CHEMBL5190267 1 6.82
CHEMBL5177381 1 6.80
CHEMBL5199403 1 6.46
CHEMBL5173899 1 6.28
CHEMBL5193629 1 6.19
CHEMBL5172231 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5205477 IC50 = 4.8 nM 8.32
CHEMBL5189578 IC50 = 5.2 nM 8.28
CHEMBL5208464 IC50 = 8.4 nM 8.08
CHEMBL5178875 IC50 = 11.0 nM 7.96
CHEMBL5178556 IC50 = 13.0 nM 7.89
CHEMBL5185670 IC50 = 16.0 nM 7.80
CHEMBL5202866 IC50 = 19.0 nM 7.72
CHEMBL5205992 IC50 = 30.0 nM 7.52
CHEMBL5203715 IC50 = 36.0 nM 7.44
CHEMBL5204033 IC50 = 49.0 nM 7.31
CHEMBL5203726 IC50 = 52.0 nM 7.28
CHEMBL5176166 IC50 = 60.0 nM 7.22
CHEMBL5201264 IC50 = 66.0 nM 7.18
CHEMBL5169820 IC50 = 77.0 nM 7.11
CHEMBL5190267 IC50 = 150.0 nM 6.82
CHEMBL5177381 IC50 = 160.0 nM 6.80
CHEMBL5199403 IC50 = 350.0 nM 6.46
CHEMBL5173899 IC50 = 530.0 nM 6.28
CHEMBL5193629 IC50 = 650.0 nM 6.19
CHEMBL5172231 IC50 - -