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Assay Detail

CHEMBL2395055

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Binding
Competitive inhibition of C-terminal His6-tagged recombinant SARS coronavirus 3C-like protease trans-cleavage activity expressed in Escherichia coli BL21 (DE3) using Dabcyl-KTSAVLQSGFRKME as substrate after 60 mins by Dixon plot analysis
9
Total Activities
9
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 1ab (CHEMBL5118)
Type SINGLE PROTEIN
Organism Severe acute respiratory syndrome-related coronavirus

Publication

Dieckol, a SARS-CoV 3CL(pro) inhibitor, isolated from the edible brown algae Ecklonia cava.
Park JY, Kim JH, Kwon JM, Kwon HJ, Jeong HJ, Kim YM, Kim D, Lee WS, Ryu YB.
Bioorg Med Chem (2013) 21 : 3730 -3737
PubMed 23647823 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 4.87 5.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL508791 DIECKOL 1 5.62
CHEMBL471187 ECKOL 1 5.09
CHEMBL510508 PHLOROFUCOFUROECKOL A 1 4.97
CHEMBL456228 1 4.71
CHEMBL2391423 2-PHLOROECKOL 1 4.62
CHEMBL459393 FUCODIPHLOROETHOL G 1 4.20
CHEMBL559870 DIOXINODEHYDROECKOL 1 -
CHEMBL2391422 TRIPHLORETHOL A 1 -
CHEMBL473159 PHLOROGLUCINOL 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL508791 DIECKOL Ki = 2400.0 nM 5.62
CHEMBL471187 ECKOL Ki = 8200.0 nM 5.09
CHEMBL510508 PHLOROFUCOFUROECKOL A Ki = 10600.0 nM 4.97
CHEMBL456228 Ki = 19300.0 nM 4.71
CHEMBL2391423 2-PHLOROECKOL Ki = 24000.0 nM 4.62
CHEMBL459393 FUCODIPHLOROETHOL G Ki = 63500.0 nM 4.20
CHEMBL559870 DIOXINODEHYDROECKOL Ki - -
CHEMBL2391422 TRIPHLORETHOL A Ki - -
CHEMBL473159 PHLOROGLUCINOL Ki - -