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Assay Detail

CHEMBL5043119

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

Binding
Inhibition of GST-tagged SARS-CoV-2 main protease expressed in Escherichia coli BL21 competent cells using DABCYL-Val-Asn-Ser-Thr-Leu-Gln-Ser-Gly-Leu-Arg-Lys-EDANS as substrate measured every 10 mins for 1 hr by FRET assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Severe acute respiratory syndrome coronavirus 2
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery and Mechanism of SARS-CoV-2 Main Protease Inhibitors.
Huff S, Kummetha IR, Tiwari SK, Huante MB, Clark AE, Wang S, Bray W, Smith D, Carlin AF, Endsley M, Rana TM.
J Med Chem (2022) 65 : 2866 -2879
PubMed 34570513 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 5.75 6.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL51085 EBSELEN 3.0 1 6.48
CHEMBL5076691 1 6.42
CHEMBL5093994 1 6.21
CHEMBL5071765 1 6.19
CHEMBL5089153 1 6.17
CHEMBL5078831 1 6.05
CHEMBL5084065 1 6.00
CHEMBL3913676 1 5.90
CHEMBL5087429 1 5.75
CHEMBL5077179 1 5.68
CHEMBL3894673 1 5.64
CHEMBL5085736 1 5.57
CHEMBL3964347 1 5.56
CHEMBL5092396 1 5.56
CHEMBL5088374 1 5.56
CHEMBL5085970 1 5.48
CHEMBL5087111 1 5.25
CHEMBL5084537 1 5.21
CHEMBL5077193 1 5.19
CHEMBL5094204 1 5.13
CHEMBL3892953 1 -
CHEMBL5090443 1 -
CHEMBL4777947 1 -
CHEMBL5087316 1 -
CHEMBL5074612 1 -
CHEMBL5085860 1 -
CHEMBL5074774 1 -
CHEMBL5086326 1 -
CHEMBL5069946 1 -
CHEMBL5084837 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL51085 EBSELEN IC50 = 330.0 nM 6.48
CHEMBL5076691 IC50 = 380.0 nM 6.42
CHEMBL5093994 IC50 = 610.0 nM 6.21
CHEMBL5071765 IC50 = 640.0 nM 6.19
CHEMBL5089153 IC50 = 680.0 nM 6.17
CHEMBL5078831 IC50 = 900.0 nM 6.05
CHEMBL5084065 IC50 = 1000.0 nM 6.00
CHEMBL3913676 IC50 = 1250.0 nM 5.90
CHEMBL5087429 IC50 = 1800.0 nM 5.75
CHEMBL5077179 IC50 = 2090.0 nM 5.68
CHEMBL3894673 IC50 = 2290.0 nM 5.64
CHEMBL5085736 IC50 = 2690.0 nM 5.57
CHEMBL3964347 IC50 = 2780.0 nM 5.56
CHEMBL5092396 IC50 = 2770.0 nM 5.56
CHEMBL5088374 IC50 = 2770.0 nM 5.56
CHEMBL5085970 IC50 = 3300.0 nM 5.48
CHEMBL5087111 IC50 = 5560.0 nM 5.25
CHEMBL5084537 IC50 = 6180.0 nM 5.21
CHEMBL5077193 IC50 = 6400.0 nM 5.19
CHEMBL5094204 IC50 = 7430.0 nM 5.13
CHEMBL3892953 IC50 > 10000.0 nM -
CHEMBL5090443 IC50 > 10000.0 nM -
CHEMBL4777947 IC50 > 10000.0 nM -
CHEMBL5087316 IC50 > 10000.0 nM -
CHEMBL5074612 IC50 > 10000.0 nM -
CHEMBL5085860 IC50 > 10000.0 nM -
CHEMBL5074774 IC50 > 10000.0 nM -
CHEMBL5086326 IC50 > 10000.0 nM -
CHEMBL5069946 IC50 > 10000.0 nM -
CHEMBL5084837 IC50 > 10000.0 nM -