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Assay Detail

CHEMBL5364588

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

Binding
Inhibition of His/SUMO tagged SARS-CoV-2 main protease transfected in Escherichia coli BL21 (DE3) using Dabcyl-KTSAVLQSGFRKME-Edans as substrate preincubated for 30 mins followed by substrate addition by fluorescence based analysis
30
Total Activities
30
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 Systematic Survey of Reversibly Covalent Dipeptidyl Inhibitors of the SARS-CoV-2 Main Protease.
Geng ZZ, Atla S, Shaabani N, Vulupala V, Yang KS, Alugubelli YR, Khatua K, Chen PH, Xiao J, Blankenship LR, Ma XR, Vatansever EC, Cho CD, Ma Y, Allen R, Ji H, Xu S, Liu WR.
J Med Chem (2023) 66 : 11040 -11055
PubMed 37561993 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 6.90 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5399799 1 7.66
CHEMBL5398911 1 7.60
CHEMBL5398423 1 7.60
CHEMBL5276875 1 7.60
CHEMBL5288416 1 7.55
CHEMBL5427537 1 7.54
CHEMBL5438286 1 7.52
CHEMBL5437518 1 7.41
CHEMBL5270743 1 7.40
CHEMBL5425010 1 7.39
CHEMBL5267952 1 7.38
CHEMBL5435470 1 7.31
CHEMBL4796938 1 7.28
CHEMBL5415290 1 7.28
CHEMBL5195325 1 7.26
CHEMBL3427168 1 7.25
CHEMBL5431050 1 7.13
CHEMBL5396546 1 7.01
CHEMBL3427141 1 6.96
CHEMBL5397315 1 6.40
CHEMBL5427578 1 6.29
CHEMBL5425267 1 6.25
CHEMBL5440769 1 6.00
CHEMBL5396421 1 5.85
CHEMBL5399253 1 5.82
CHEMBL5412310 1 5.66
CHEMBL5436573 1 5.44
CHEMBL5398479 1 5.22
CHEMBL5407572 1 -
CHEMBL5397334 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5399799 IC50 = 22.0 nM 7.66
CHEMBL5398911 IC50 = 25.0 nM 7.60
CHEMBL5398423 IC50 = 25.0 nM 7.60
CHEMBL5276875 IC50 = 25.0 nM 7.60
CHEMBL5288416 IC50 = 28.0 nM 7.55
CHEMBL5427537 IC50 = 29.0 nM 7.54
CHEMBL5438286 IC50 = 30.0 nM 7.52
CHEMBL5437518 IC50 = 39.0 nM 7.41
CHEMBL5270743 IC50 = 40.0 nM 7.40
CHEMBL5425010 IC50 = 41.0 nM 7.39
CHEMBL5267952 IC50 = 42.0 nM 7.38
CHEMBL5435470 IC50 = 49.0 nM 7.31
CHEMBL4796938 IC50 = 53.0 nM 7.28
CHEMBL5415290 IC50 = 53.0 nM 7.28
CHEMBL5195325 IC50 = 55.0 nM 7.26
CHEMBL3427168 IC50 = 56.0 nM 7.25
CHEMBL5431050 IC50 = 74.0 nM 7.13
CHEMBL5396546 IC50 = 98.0 nM 7.01
CHEMBL3427141 IC50 = 110.0 nM 6.96
CHEMBL5397315 IC50 = 400.0 nM 6.40
CHEMBL5427578 IC50 = 510.0 nM 6.29
CHEMBL5425267 IC50 = 560.0 nM 6.25
CHEMBL5440769 IC50 = 990.0 nM 6.00
CHEMBL5396421 IC50 = 1400.0 nM 5.85
CHEMBL5399253 IC50 = 1500.0 nM 5.82
CHEMBL5412310 IC50 = 2200.0 nM 5.66
CHEMBL5436573 IC50 = 3600.0 nM 5.44
CHEMBL5398479 IC50 = 6000.0 nM 5.22
CHEMBL5407572 IC50 > 2000.0 nM -
CHEMBL5397334 IC50 > 5000.0 nM -