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Assay Detail

CHEMBL5112751

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

Binding
Irreversible inhibition of recombinant full length SARS-CoV-2 3CLpro expressed in Escherichia coli using Ac-Abu-Tle-Leu-Gln-MCA as fluorogenic substrate assessed as inhibition constant incubated for 60 mins by multimode plate reader analysis
2
Total Activities
2
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

Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease.
Hirose Y, Shindo N, Mori M, Onitsuka S, Isogai H, Hamada R, Hiramoto T, Ochi J, Takahashi D, Ueda T, Caaveiro JMM, Yoshida Y, Ohdo S, Matsunaga N, Toba S, Sasaki M, Orba Y, Sawa H, Sato A, Kawanishi E, Ojida A.
J Med Chem (2022) 65 : 13852 -13865
PubMed 36229406 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 6.95 7.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5179778 1 7.25
CHEMBL5190754 1 6.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5179778 Ki = 56.2 nM 7.25
CHEMBL5190754 Ki = 224.0 nM 6.65