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Assay Detail

CHEMBL4495583

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

Functional
SARS-CoV-2 3CL-Pro protease inhibition IC50 determined by FRET kind of response from peptide substrate
117
Total Activities
109
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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 inhibitors of SARS-Cov2 M-Pro enzymatic activity using a small molecule repurposing screen
Maria Kuzikov, Elisa Costanzi, Jeanette Reinshagen, Francesca Esposito, Laura Vangeel, Markus Wolf, Bernhard Ellinger, Carsten Claussen, Gerd Geisslinger, Angela Corona, Daniela Iaconis, Carmine Talarico, Candida Manelfi, Rolando Cannalire, Giulia Rossetti, Jonas Gossen, Simone Albani, Francesco Musiani, Katja Herzog, Yang Ye, Barbara Giabbai, Nicola Demitri, Dirk Jochmans, Steven De Jonghe, Jasper Rymenants, Vincenzo Summa, Enzo Tramontano, Andrea R. Beccari, Pieter Leyssen, Paola Storici, Johan Neyts, Philip Gribbon, and Andrea Zaliani
(2020)
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 117 6.21 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL508338 THIMEROSAL 3.0 1 8.00
CHEMBL1333953 PHENYLMERCURIC ACETATE 1 8.00
CHEMBL3963349 1 8.00
CHEMBL1725120 1 7.70
CHEMBL8260 BAICALEIN 2.0 1 7.70
CHEMBL51085 EBSELEN 3.0 1 7.52
CHEMBL510038 1 7.52
CHEMBL4303595 2 7.40
CHEMBL1356238 PYRITHIONE 4.0 1 7.30
CHEMBL120563 THIRAM 2.0 1 7.30
CHEMBL3545157 TIDEGLUSIB 2.0 2 7.10
CHEMBL505670 1 7.00
CHEMBL1255778 BENSERAZIDE HYDROCHLORIDE 1 6.85
CHEMBL406050 PX-12 2.0 1 6.85
CHEMBL284861 1 6.85
CHEMBL1096979 BENSERAZIDE 3.0 1 6.85
CHEMBL1422849 1 6.82
CHEMBL1917204 2 6.82
CHEMBL460499 CARMOFUR 2.0 1 6.80
CHEMBL508112 BENZOTHIAZYL DISULFIDE 1 6.80
CHEMBL3348861 AMPELOPSIN 2.0 1 6.75
CHEMBL105712 PHENACYL CHLORIDE 1 6.72
CHEMBL1886408 1 6.70
CHEMBL178459 OLTIPRAZ 3.0 2 6.68
CHEMBL4303702 1 6.68
CHEMBL1449651 PYRROLIDINE DITHIOCARBAMIC ACID, AMMONIUM SALT 1 6.68
CHEMBL164 MYRICETIN 2 6.66
CHEMBL964 DISULFIRAM 4.0 1 6.66
CHEMBL477197 HEMATOXYLIN 1 6.66
CHEMBL3833381 MERBROMIN 2.0 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1333953 PHENYLMERCURIC ACETATE IC50 = 10.0 nM 8.00
CHEMBL508338 THIMEROSAL IC50 = 10.0 nM 8.00
CHEMBL3963349 IC50 = 10.0 nM 8.00
CHEMBL1725120 IC50 = 20.0 nM 7.70
CHEMBL8260 BAICALEIN IC50 = 20.0 nM 7.70
CHEMBL510038 IC50 = 30.0 nM 7.52
CHEMBL51085 EBSELEN IC50 = 30.0 nM 7.52
CHEMBL4303595 IC50 = 40.0 nM 7.40
CHEMBL120563 THIRAM IC50 = 50.0 nM 7.30
CHEMBL1356238 PYRITHIONE IC50 = 50.0 nM 7.30
CHEMBL3545157 TIDEGLUSIB IC50 = 80.0 nM 7.10
CHEMBL505670 IC50 = 100.0 nM 7.00
CHEMBL284861 IC50 = 140.0 nM 6.85
CHEMBL406050 PX-12 IC50 = 140.0 nM 6.85
CHEMBL1255778 BENSERAZIDE HYDROCHLORIDE IC50 = 140.0 nM 6.85
CHEMBL1096979 BENSERAZIDE IC50 = 140.0 nM 6.85
CHEMBL1422849 IC50 = 150.0 nM 6.82
CHEMBL3545157 TIDEGLUSIB IC50 = 150.0 nM 6.82
CHEMBL1917204 IC50 = 150.0 nM 6.82
CHEMBL460499 CARMOFUR IC50 = 160.0 nM 6.80
CHEMBL4303595 IC50 = 160.0 nM 6.80
CHEMBL508112 BENZOTHIAZYL DISULFIDE IC50 = 160.0 nM 6.80
CHEMBL3348861 AMPELOPSIN IC50 = 180.0 nM 6.75
CHEMBL105712 PHENACYL CHLORIDE IC50 = 190.0 nM 6.72
CHEMBL1886408 IC50 = 200.0 nM 6.70
CHEMBL178459 OLTIPRAZ IC50 = 210.0 nM 6.68
CHEMBL4303702 IC50 = 210.0 nM 6.68
CHEMBL1449651 PYRROLIDINE DITHIOCARBAMIC ACID, AMMONIUM SALT IC50 = 210.0 nM 6.68
CHEMBL964 DISULFIRAM IC50 = 220.0 nM 6.66
CHEMBL164 MYRICETIN IC50 = 220.0 nM 6.66
CHEMBL477197 HEMATOXYLIN IC50 = 220.0 nM 6.66
CHEMBL1917204 IC50 = 230.0 nM 6.64
CHEMBL1474701 IC50 = 240.0 nM 6.62
CHEMBL1161936 IC50 = 240.0 nM 6.62
CHEMBL3833381 MERBROMIN IC50 = 240.0 nM 6.62
CHEMBL1374426 IC50 = 290.0 nM 6.54
CHEMBL508280 IC50 = 300.0 nM 6.52
CHEMBL4303312 IC50 = 330.0 nM 6.48
CHEMBL55400 PROFLAVINE IC50 = 360.0 nM 6.44
CHEMBL480 LANSOPRAZOLE IC50 = 390.0 nM 6.41
CHEMBL289356 IC50 = 390.0 nM 6.41
CHEMBL164 MYRICETIN IC50 = 400.0 nM 6.40
CHEMBL4303622 IC50 = 410.0 nM 6.39
CHEMBL1408862 BRONOPOL IC50 = 420.0 nM 6.38
CHEMBL4303361 IC50 = 480.0 nM 6.32
CHEMBL472940 IC50 = 510.0 nM 6.29
CHEMBL3187985 APOMORPHINE HYDROCHLORIDE IC50 = 520.0 nM 6.28
CHEMBL3797437 IC50 = 540.0 nM 6.27
CHEMBL2107818 ALDOXORUBICIN IC50 = 580.0 nM 6.24
CHEMBL596674 IC50 = 580.0 nM 6.24