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Assay Detail

CHEMBL923041

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

Binding
Inhibition of HCV NS3 protease by FRET assay
23
Total Activities
23
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Hepatitis C virus NS3 protease inhibitors comprising a novel aromatic P1 moiety.
Rönn R, Lampa A, Peterson SD, Gossas T, Akerblom E, Danielson UH, Karlén A, Sandström A.
Bioorg Med Chem (2008) 16 : 2955 -2967
PubMed 18194867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 5.98 9.18
IC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL297884 CILUPREVIR 2.0 1 9.18
CHEMBL218394 BOCEPREVIR 4.0 1 7.85
CHEMBL231813 TELAPREVIR 4.0 1 7.41
CHEMBL258843 1 6.51
CHEMBL259152 1 6.46
CHEMBL408047 1 6.21
CHEMBL258984 1 6.11
CHEMBL259478 1 6.08
CHEMBL436688 1 6.04
CHEMBL264323 1 5.96
CHEMBL259363 1 5.92
CHEMBL540191 1 5.85
CHEMBL246632 1 5.75
CHEMBL259193 1 5.70
CHEMBL402469 1 5.50
CHEMBL261778 1 5.41
CHEMBL436893 1 5.30
CHEMBL260783 1 5.23
CHEMBL407203 1 5.17
CHEMBL407079 1 4.92
CHEMBL261787 1 4.77
CHEMBL405518 CORBOXYLIC ACID 1 4.18
CHEMBL258734 DANOPREVIR 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL297884 CILUPREVIR Ki = 0.66 nM 9.18
CHEMBL218394 BOCEPREVIR Ki = 14.0 nM 7.85
CHEMBL231813 TELAPREVIR Ki = 39.0 nM 7.41
CHEMBL258843 Ki = 310.0 nM 6.51
CHEMBL259152 Ki = 350.0 nM 6.46
CHEMBL408047 Ki = 610.0 nM 6.21
CHEMBL258984 Ki = 780.0 nM 6.11
CHEMBL259478 Ki = 830.0 nM 6.08
CHEMBL436688 Ki = 920.0 nM 6.04
CHEMBL264323 Ki = 1100.0 nM 5.96
CHEMBL259363 Ki = 1200.0 nM 5.92
CHEMBL540191 Ki = 1400.0 nM 5.85
CHEMBL246632 Ki = 1800.0 nM 5.75
CHEMBL259193 Ki = 2000.0 nM 5.70
CHEMBL402469 Ki = 3200.0 nM 5.50
CHEMBL261778 Ki = 3900.0 nM 5.41
CHEMBL436893 Ki = 5000.0 nM 5.30
CHEMBL260783 Ki = 5900.0 nM 5.23
CHEMBL407203 Ki = 6800.0 nM 5.17
CHEMBL407079 Ki = 12000.0 nM 4.92
CHEMBL261787 Ki = 17000.0 nM 4.77
CHEMBL405518 CORBOXYLIC ACID Ki = 66000.0 nM 4.18
CHEMBL258734 DANOPREVIR IC50 < 0.25 nM -