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Assay Detail

CHEMBL2439385

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

Binding
Inhibition of SARS coronavirus 3CL-protease by fluorescence assay
18
Total Activities
18
Compounds Tested
1
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

Development of potent dipeptide-type SARS-CoV 3CL protease inhibitors with novel P3 scaffolds: design, synthesis, biological evaluation, and docking studies.
Thanigaimalai P, Konno S, Yamamoto T, Koiwai Y, Taguchi A, Takayama K, Yakushiji F, Akaji K, Chen SE, Naser-Tavakolian A, Schön A, Freire E, Hayashi Y.
Eur J Med Chem (2013) 68 : 372 -384
PubMed 23994330 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.62 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2435614 1 8.20
CHEMBL2435605 1 7.66
CHEMBL2435617 1 7.58
CHEMBL2435612 1 7.55
CHEMBL2435616 1 7.52
CHEMBL2435615 1 7.32
CHEMBL2435622 1 7.19
CHEMBL2435610 1 7.17
CHEMBL2435607 1 6.92
CHEMBL2435611 1 6.80
CHEMBL2435613 1 6.48
CHEMBL2435609 1 6.17
CHEMBL2435606 1 6.10
CHEMBL2435621 1 5.77
CHEMBL2435620 1 5.57
CHEMBL2435618 1 5.17
CHEMBL2435619 1 5.12
CHEMBL2435608 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2435614 Ki = 6.3 nM 8.20
CHEMBL2435605 Ki = 22.0 nM 7.66
CHEMBL2435617 Ki = 26.0 nM 7.58
CHEMBL2435612 Ki = 28.0 nM 7.55
CHEMBL2435616 Ki = 30.0 nM 7.52
CHEMBL2435615 Ki = 48.0 nM 7.32
CHEMBL2435622 Ki = 65.0 nM 7.19
CHEMBL2435610 Ki = 67.0 nM 7.17
CHEMBL2435607 Ki = 120.0 nM 6.92
CHEMBL2435611 Ki = 160.0 nM 6.80
CHEMBL2435613 Ki = 330.0 nM 6.48
CHEMBL2435609 Ki = 680.0 nM 6.17
CHEMBL2435606 Ki = 800.0 nM 6.10
CHEMBL2435621 Ki = 1700.0 nM 5.77
CHEMBL2435620 Ki = 2700.0 nM 5.57
CHEMBL2435618 Ki = 6700.0 nM 5.17
CHEMBL2435619 Ki = 7500.0 nM 5.12
CHEMBL2435608 Ki = 14000.0 nM 4.85