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Assay Detail

CHEMBL2213724

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

Binding
Inhibition of HCV genotype 1b BK NS3/4A protease expressed in Escherichia coli incubated for 30 mins by time-resolved fluorescence assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hepatitis C virus (isolate BK)
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 24 10.80 10.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2203882 1 10.80
CHEMBL2203873 1 10.80
CHEMBL2203892 1 10.80
CHEMBL2203875 1 -
CHEMBL2203876 1 -
CHEMBL2203877 1 -
CHEMBL2203878 1 -
CHEMBL2203879 1 -
CHEMBL2203880 1 -
CHEMBL2203881 1 -
CHEMBL2203883 1 -
CHEMBL2203884 1 -
CHEMBL2203885 1 -
CHEMBL2203887 1 -
CHEMBL2203888 1 -
CHEMBL2203889 1 -
CHEMBL2203890 1 -
CHEMBL2203891 1 -
CHEMBL2203293 1 -
CHEMBL2203893 1 -
CHEMBL2203894 1 -
CHEMBL2203895 1 -
CHEMBL2203874 1 -
CHEMBL2203886 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2203882 Ki = 0.016 nM 10.80
CHEMBL2203873 Ki = 0.016 nM 10.80
CHEMBL2203892 Ki = 0.016 nM 10.80
CHEMBL2203875 Ki < 0.05 nM -
CHEMBL2203876 Ki < 0.05 nM -
CHEMBL2203877 Ki < 0.05 nM -
CHEMBL2203878 Ki < 0.05 nM -
CHEMBL2203879 Ki < 0.05 nM -
CHEMBL2203880 Ki < 0.05 nM -
CHEMBL2203881 Ki < 0.05 nM -
CHEMBL2203883 Ki < 0.05 nM -
CHEMBL2203884 Ki < 0.05 nM -
CHEMBL2203885 Ki < 0.05 nM -
CHEMBL2203887 Ki < 0.05 nM -
CHEMBL2203888 Ki < 0.05 nM -
CHEMBL2203889 Ki < 0.05 nM -
CHEMBL2203890 Ki < 0.05 nM -
CHEMBL2203891 Ki < 0.05 nM -
CHEMBL2203293 Ki < 0.05 nM -
CHEMBL2203893 Ki < 0.05 nM -
CHEMBL2203894 Ki < 0.05 nM -
CHEMBL2203895 Ki < 0.05 nM -
CHEMBL2203874 Ki < 0.05 nM -
CHEMBL2203886 Ki < 0.05 nM -