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Assay Detail

CHEMBL5516207

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

Binding
Inhibition of MERS-CoV main protease using Boc-Abu-Tle-Leu-Gln-AMC as substrate preincubated for 5 mins followed by enzyme addition and measured for 10 mins
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Middle East respiratory syndrome-related coronavirus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Macrocyclic Azapeptide Nitriles: Structure-Based Discovery of Potent SARS-CoV-2 Main Protease Inhibitors as Antiviral Drugs.
Breidenbach J, Voget R, Si Y, Hingst A, Claff T, Sylvester K, Wolf V, Krasniqi V, Useini A, Sträter N, Ogura Y, Kawaguchi A, Müller CE, Gütschow M.
J Med Chem (2024) 67 : 8757 -8790
PubMed 38753594 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.29 8.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4802135 NIRMATRELVIR 4.0 1 8.99
CHEMBL5559068 1 8.49
CHEMBL5558707 1 7.25
CHEMBL5568269 1 6.97
CHEMBL5561728 1 6.89
CHEMBL5564222 1 6.66
CHEMBL5568382 1 6.61
CHEMBL5565472 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4802135 NIRMATRELVIR Ki = 1.02 nM 8.99
CHEMBL5559068 Ki = 3.22 nM 8.49
CHEMBL5558707 Ki = 56.8 nM 7.25
CHEMBL5568269 Ki = 106.0 nM 6.97
CHEMBL5561728 Ki = 129.0 nM 6.89
CHEMBL5564222 Ki = 219.0 nM 6.66
CHEMBL5568382 Ki = 246.0 nM 6.61
CHEMBL5565472 Ki = 339.0 nM 6.47