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Assay Detail

CHEMBL5136655

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

Binding
Inhibition of recombinant SARS CoV-1 main protease expressed using MCA-AVLQSGFR-K(DNP)-K-NH2 as substrate incubated for 2 hrs by FRET based assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Small-Molecule Thioesters as SARS-CoV-2 Main Protease Inhibitors: Enzyme Inhibition, Structure-Activity Relationships, Antiviral Activity, and X-ray Structure Determination.
Pillaiyar T, Flury P, Krüger N, Su H, Schäkel L, Barbosa Da Silva E, Eppler O, Kronenberger T, Nie T, Luedtke S, Rocha C, Sylvester K, Petry MRI, McKerrow JH, Poso A, Pöhlmann S, Gütschow M, O'Donoghue AJ, Xu Y, Müller CE, Laufer SA.
J Med Chem (2022) 65 : 9376 -9395
PubMed 35709506 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.07 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1821850 1 7.35
CHEMBL5169323 1 7.22
CHEMBL5184362 1 6.60
CHEMBL5207081 1 5.82
CHEMBL5191017 1 5.78
CHEMBL5199191 1 5.67
CHEMBL5207392 1 5.56
CHEMBL5204130 1 5.49
CHEMBL5173920 1 5.13
CHEMBL5204064 1 -
CHEMBL5204452 1 -
CHEMBL5199531 1 -
CHEMBL5188939 1 -
CHEMBL5177782 1 -
CHEMBL5208709 1 -
CHEMBL5192654 1 -
CHEMBL5189565 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1821850 IC50 = 44.6 nM 7.35
CHEMBL5169323 IC50 = 60.0 nM 7.22
CHEMBL5184362 IC50 = 253.0 nM 6.60
CHEMBL5207081 IC50 = 1520.0 nM 5.82
CHEMBL5191017 IC50 = 1650.0 nM 5.78
CHEMBL5199191 IC50 = 2150.0 nM 5.67
CHEMBL5207392 IC50 = 2760.0 nM 5.56
CHEMBL5204130 IC50 = 3210.0 nM 5.49
CHEMBL5173920 IC50 = 7350.0 nM 5.13
CHEMBL5204064 IC50 - -
CHEMBL5204452 IC50 - -
CHEMBL5199531 IC50 - -
CHEMBL5188939 IC50 - -
CHEMBL5177782 IC50 - -
CHEMBL5208709 IC50 - -
CHEMBL5192654 IC50 - -
CHEMBL5189565 IC50 - -