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Assay Detail

CHEMBL5330612

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

Binding
Inhibition of SARS-CoV-2 MPro using protease substrate preincubated with enzyme for 10 mins followed by substrate addition and measured after 5 mins by FRET based assay
12
Total Activities
12
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

Identification of Ebselen derivatives as novel SARS-CoV-2 main protease inhibitors: Design, synthesis, biological evaluation, and structure-activity relationships exploration.
Zhang H, Li J, Toth K, Tollefson AE, Jing L, Gao S, Liu X, Zhan P.
Bioorg Med Chem (2023) 96 : 117531 -117531
PubMed 37972434 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.43 6.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5409716 1 6.63
CHEMBL5398922 1 6.57
CHEMBL5411764 1 6.54
CHEMBL5395762 1 6.49
CHEMBL51085 EBSELEN 3.0 1 6.47
CHEMBL5394951 1 6.45
CHEMBL3920474 1 6.44
CHEMBL5434494 1 6.38
CHEMBL5403838 1 6.34
CHEMBL5438913 1 6.31
CHEMBL5418023 1 6.28
CHEMBL5426830 1 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5409716 IC50 = 233.0 nM 6.63
CHEMBL5398922 IC50 = 268.0 nM 6.57
CHEMBL5411764 IC50 = 287.0 nM 6.54
CHEMBL5395762 IC50 = 322.0 nM 6.49
CHEMBL51085 EBSELEN IC50 = 339.0 nM 6.47
CHEMBL5394951 IC50 = 356.0 nM 6.45
CHEMBL3920474 IC50 = 364.0 nM 6.44
CHEMBL5434494 IC50 = 417.0 nM 6.38
CHEMBL5403838 IC50 = 459.0 nM 6.34
CHEMBL5438913 IC50 = 490.0 nM 6.31
CHEMBL5418023 IC50 = 528.0 nM 6.28
CHEMBL5426830 IC50 = 550.0 nM 6.26