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Assay Detail

CHEMBL3107397

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

Binding
Inhibition of SARS coronavirus 3C-like protease using 5-FAM-TSATLQSGFRK(QXL520)-NH2 as substrate preincubated for 5 mins followed by substrate addition measured after 6 mins by FRET assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Replicase polyprotein 1ab (CHEMBL5118)
Type SINGLE PROTEIN
Organism Severe acute respiratory syndrome-related coronavirus

Publication

Identification of novel drug scaffolds for inhibition of SARS-CoV 3-Chymotrypsin-like protease using virtual and high-throughput screenings.
Lee H, Mittal A, Patel K, Gatuz JL, Truong L, Torres J, Mulhearn DC, Johnson ME.
Bioorg Med Chem (2014) 22 : 167 -177
PubMed 24332657 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.01 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3105073 1 6.80
CHEMBL1876821 1 6.03
CHEMBL3105076 1 5.66
CHEMBL3105074 1 4.97
CHEMBL1478361 1 4.79
CHEMBL554041 ALEXIDINE DIHYDROCHLORIDE 1 4.61
CHEMBL1488602 1 4.59
CHEMBL1487869 1 4.56
CHEMBL1906723 1 4.54
CHEMBL3105075 1 4.53
CHEMBL3105072 1 4.53
CHEMBL3105071 1 4.52
CHEMBL1392147 1 -
CHEMBL1732790 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3105073 IC50 = 160.0 nM 6.80
CHEMBL1876821 IC50 = 940.0 nM 6.03
CHEMBL3105076 IC50 = 2200.0 nM 5.66
CHEMBL3105074 IC50 = 10800.0 nM 4.97
CHEMBL1478361 IC50 = 16100.0 nM 4.79
CHEMBL554041 ALEXIDINE DIHYDROCHLORIDE IC50 = 24500.0 nM 4.61
CHEMBL1488602 IC50 = 25600.0 nM 4.59
CHEMBL1487869 IC50 = 27600.0 nM 4.56
CHEMBL1906723 IC50 = 28800.0 nM 4.54
CHEMBL3105075 IC50 = 29800.0 nM 4.53
CHEMBL3105072 IC50 = 29800.0 nM 4.53
CHEMBL3105071 IC50 = 29900.0 nM 4.52
CHEMBL1392147 IC50 > 200000.0 nM -
CHEMBL1732790 IC50 > 200000.0 nM -