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Assay Detail

CHEMBL5155119

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

Binding
Inhibition of SARS-CoV-2 3CL protease incubated for 30 mins by FRET assay
19
Total Activities
19
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

Peptidomimetic α-Acyloxymethylketone Warheads with Six-Membered Lactam P1 Glutamine Mimic: SARS-CoV-2 3CL Protease Inhibition, Coronavirus Antiviral Activity, and <i>in Vitro</i> Biological Stability.
Bai B, Belovodskiy A, Hena M, Kandadai AS, Joyce MA, Saffran HA, Shields JA, Khan MB, Arutyunova E, Lu J, Bajwa SK, Hockman D, Fischer C, Lamer T, Vuong W, van Belkum MJ, Gu Z, Lin F, Du Y, Xu J, Rahim M, Young HS, Vederas JC, Tyrrell DL, Lemieux MJ, Nieman JA.
J Med Chem (2022) 65 : 2905 -2925
PubMed 34242027 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.53 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5191092 1 9.00
CHEMBL5190876 1 8.40
CHEMBL5191464 1 8.19
CHEMBL5206120 1 7.90
CHEMBL5173658 1 7.85
CHEMBL5189954 1 7.77
CHEMBL5191060 1 7.72
CHEMBL5195798 1 7.71
CHEMBL5198667 1 7.70
CHEMBL5194822 1 7.66
CHEMBL5171263 1 7.66
CHEMBL5192585 1 7.48
CHEMBL5193390 1 7.20
CHEMBL5179259 1 7.19
CHEMBL5195086 1 7.15
CHEMBL5190213 1 7.06
CHEMBL5187784 1 6.90
CHEMBL3427166 1 6.72
CHEMBL5182169 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5191092 IC50 = 1.0 nM 9.00
CHEMBL5190876 IC50 = 4.0 nM 8.40
CHEMBL5191464 IC50 = 6.4 nM 8.19
CHEMBL5206120 IC50 = 12.5 nM 7.90
CHEMBL5173658 IC50 = 14.0 nM 7.85
CHEMBL5189954 IC50 = 17.0 nM 7.77
CHEMBL5191060 IC50 = 19.0 nM 7.72
CHEMBL5195798 IC50 = 19.5 nM 7.71
CHEMBL5198667 IC50 = 20.0 nM 7.70
CHEMBL5194822 IC50 = 21.9 nM 7.66
CHEMBL5171263 IC50 = 22.1 nM 7.66
CHEMBL5192585 IC50 = 32.9 nM 7.48
CHEMBL5193390 IC50 = 63.5 nM 7.20
CHEMBL5179259 IC50 = 64.1 nM 7.19
CHEMBL5195086 IC50 = 71.5 nM 7.15
CHEMBL5190213 IC50 = 86.3 nM 7.06
CHEMBL5187784 IC50 = 125.5 nM 6.90
CHEMBL3427166 IC50 = 190.0 nM 6.72
CHEMBL5182169 IC50 = 1500.0 nM 5.82