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Assay Detail

CHEMBL2406591

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

Binding
Inhibition of SARS coronavirus Chymotrypsin-like protease
10
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Severe acute respiratory syndrome-related coronavirus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Replicase polyprotein 1a (CHEMBL3927)
Type SINGLE PROTEIN
Organism Severe acute respiratory syndrome-related coronavirus

Publication

Design, synthesis, and biological evaluation of novel dipeptide-type SARS-CoV 3CL protease inhibitors: structure-activity relationship study.
Thanigaimalai P, Konno S, Yamamoto T, Koiwai Y, Taguchi A, Takayama K, Yakushiji F, Akaji K, Kiso Y, Kawasaki Y, Chen SE, Naser-Tavakolian A, Schön A, Freire E, Hayashi Y.
Eur J Med Chem (2013) 65 : 436 -447
PubMed 23747811 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.53 8.12
IC50 5 5.86 7.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL497141 1 8.12
CHEMBL225515 1 7.19
CHEMBL1929019 1 7.19
CHEMBL2402691 1 6.22
CHEMBL2402692 2 6.18
CHEMBL539209 1 5.66
CHEMBL2402694 1 5.50
CHEMBL406516 1 5.00
CHEMBL18786 CINANSERIN 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL497141 Ki = 7.5 nM 8.12
CHEMBL225515 Ki = 65.0 nM 7.19
CHEMBL1929019 IC50 = 65.0 nM 7.19
CHEMBL2402691 IC50 = 600.0 nM 6.22
CHEMBL2402692 Ki = 660.0 nM 6.18
CHEMBL539209 Ki = 2200.0 nM 5.66
CHEMBL2402694 Ki = 3200.0 nM 5.50
CHEMBL2402692 IC50 = 9100.0 nM 5.04
CHEMBL406516 IC50 = 10000.0 nM 5.00
CHEMBL18786 CINANSERIN IC50 = 323000.0 nM -