Assay Detail

CHEMBL2213715

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

Binding

Inhibition of HCV genotype 2a JFH NS3/4A protease expressed in Escherichia coli incubated for 30 mins by time-resolved fluorescence assay

ChEMBL ↗

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Target

Unchecked (CHEMBL612545) ↗

Open DB target context

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Unchecked (CHEMBL612545) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Unchecked

CHEMBL612545

Anchored from Assay target.

Protein identity Unchecked

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Hepatitis C virus JFH-1
Confidence	0 — Uncurated / Unknown
Curated By	Autocuration

Target

Unchecked (CHEMBL612545) ↗

Type

UNCHECKED

Publication

Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2-P4 linkers.

Rudd MT, McIntyre CJ, Romano JJ, Butcher JW, Holloway MK, Bush K, Nguyen KT, Gilbert KF, Lyle TA, Liverton NJ, Wan BL, Summa V, Harper S, Rowley M, Vacca JP, Carroll SS, Burlein C, DiMuzio JM, Gates A, Graham DJ, Huang Q, Ludmerer SW, McClain S, McHale C, Stahlhut M, Fandozzi C, Taylor A, Trainor N, Olsen DB, McCauley JA.
Bioorg Med Chem Lett (2012) 22 : 7207 -7213
PubMed 23084906 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	3	9.82	9.85

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2203882	—	—	1	9.85
CHEMBL2203873	—	—	1	9.85
CHEMBL2203892	—	—	1	9.77

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2203882	—	Ki	=	0.14	nM	9.85
CHEMBL2203873	—	Ki	=	0.14	nM	9.85
CHEMBL2203892	—	Ki	=	0.17	nM	9.77