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Assay Detail

CHEMBL5136653

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

Functional
Antiviral activity against SARS-COV 2 infected in human Calu-3 cells assessed as inhibition of viral replication preincubated for 1 hr followed by viral infection and further incubated with compound for 24 hrs
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Severe acute respiratory syndrome coronavirus 2
Cell Type Calu-3
Confidence 1 — Organism
Curated By Autocuration

Target

SARS-CoV-2 (CHEMBL4303835)
Type ORGANISM
Organism Severe acute respiratory syndrome coronavirus 2

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
EC50 12 6.80 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL490820 1 7.54
CHEMBL5204064 1 7.42
CHEMBL5191017 1 7.35
CHEMBL4065616 REMDESIVIR 4.0 1 7.10
CHEMBL4855437 1 7.00
CHEMBL5169323 1 6.96
CHEMBL5192654 1 6.86
CHEMBL5189565 1 6.43
CHEMBL5199191 1 6.36
CHEMBL5204130 1 6.25
CHEMBL5199531 1 6.18
CHEMBL5207081 1 6.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL490820 EC50 = 28.5 nM 7.54
CHEMBL5204064 EC50 = 38.3 nM 7.42
CHEMBL5191017 EC50 = 45.0 nM 7.35
CHEMBL4065616 REMDESIVIR EC50 = 79.6 nM 7.10
CHEMBL4855437 EC50 = 100.0 nM 7.00
CHEMBL5169323 EC50 = 111.0 nM 6.96
CHEMBL5192654 EC50 = 137.0 nM 6.86
CHEMBL5189565 EC50 = 367.0 nM 6.43
CHEMBL5199191 EC50 = 437.0 nM 6.36
CHEMBL5204130 EC50 = 562.0 nM 6.25
CHEMBL5199531 EC50 = 659.0 nM 6.18
CHEMBL5207081 EC50 = 734.0 nM 6.13