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Assay Detail

CHEMBL5508580

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

Binding
Inhibition of amino-terminal His-SUMO tagged SARS-CoV-2 3CLpro using HilyteFluor 488-Glu-Ser-Ala-Thr-Leu-Gln-Ser-Gly-Leu-Arg-Lys-Ala-Lys-QXL 520 as FRET peptide substrate preincubated for 90 mins followed by substrate addition and measured over 30 mins by continuous FRET assay
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

Synthesis and biological evaluation of novel peptidomimetic inhibitors of the coronavirus 3C-like protease.
Amblard F, LeCher JC, De R, Zhou S, Liu P, Goh SL, Tao S, Patel D, Downs-Bowen J, Zandi K, Zhang H, Chaudhry G, McBrayer T, Muczynski M, Al-Homoudi A, Engel J, Lan S, Sarafianos SG, Kovari LC, Schinazi RF.
Eur J Med Chem (2024) 268 : 116263 -116263
PubMed 38432056 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.63 6.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5532059 1 6.78
CHEMBL4802135 NIRMATRELVIR 4.0 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5532059 IC50 = 165.7 nM 6.78
CHEMBL4802135 NIRMATRELVIR IC50 = 332.7 nM 6.48