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Assay Detail

CHEMBL2395056

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Binding
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 FRET assay
17
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 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
IC50 9 4.89 5.57
Inhibition 8 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL508791 DIECKOL 2 5.57
CHEMBL471187 ECKOL 2 5.06
CHEMBL2391423 2-PHLOROECKOL 2 4.88
CHEMBL510508 PHLOROFUCOFUROECKOL A 2 4.78
CHEMBL459393 FUCODIPHLOROETHOL G 2 4.65
CHEMBL456228 2 4.38
CHEMBL473159 PHLOROGLUCINOL 3.0 1 -
CHEMBL559870 DIOXINODEHYDROECKOL 2 -
CHEMBL2391422 TRIPHLORETHOL A 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL508791 DIECKOL IC50 = 2700.0 nM 5.57
CHEMBL471187 ECKOL IC50 = 8800.0 nM 5.06
CHEMBL2391423 2-PHLOROECKOL IC50 = 13300.0 nM 4.88
CHEMBL510508 PHLOROFUCOFUROECKOL A IC50 = 16700.0 nM 4.78
CHEMBL459393 FUCODIPHLOROETHOL G IC50 = 22500.0 nM 4.65
CHEMBL456228 IC50 = 42100.0 nM 4.38
CHEMBL510508 PHLOROFUCOFUROECKOL A Inhibition - % -
CHEMBL508791 DIECKOL Inhibition - % -
CHEMBL459393 FUCODIPHLOROETHOL G Inhibition - % -
CHEMBL456228 Inhibition - % -
CHEMBL2391423 2-PHLOROECKOL Inhibition - % -
CHEMBL559870 DIOXINODEHYDROECKOL Inhibition - % -
CHEMBL471187 ECKOL Inhibition - % -
CHEMBL473159 PHLOROGLUCINOL IC50 > 200000.0 nM -
CHEMBL2391422 TRIPHLORETHOL A IC50 = 164700.0 nM -
CHEMBL559870 DIOXINODEHYDROECKOL IC50 = 158300.0 nM -
CHEMBL2391422 TRIPHLORETHOL A Inhibition - % -