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Assay Detail

CHEMBL1109899

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

Binding
Inhibition of HCV NS4A tagged recombinant single chain NS3 protease after 15 mins
43
Total Activities
43
Compounds Tested
1
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

The introduction of P4 substituted 1-methylcyclohexyl groups into Boceprevir: a change in direction in the search for a second generation HCV NS3 protease inhibitor.
Bennett F, Huang Y, Hendrata S, Lovey R, Bogen SL, Pan W, Guo Z, Prongay A, Chen KX, Arasappan A, Venkatraman S, Velazquez F, Nair L, Sannigrahi M, Tong X, Pichardo J, Cheng KC, Girijavallabhan VM, Saksena AK, Njoroge FG.
Bioorg Med Chem Lett (2010) 20 : 2617 -2621
PubMed 20303756 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 43 7.80 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1093977 1 8.70
CHEMBL1093632 1 8.52
CHEMBL1093982 1 8.52
CHEMBL1093978 1 8.40
CHEMBL1093975 1 8.40
CHEMBL1093980 1 8.30
CHEMBL1093976 1 8.30
CHEMBL1093973 1 8.22
CHEMBL1093647 1 8.15
CHEMBL1093015 1 8.10
CHEMBL1093643 1 8.05
CHEMBL1093641 1 8.05
CHEMBL1093971 1 8.05
CHEMBL1088786 1 8.00
CHEMBL1093972 1 8.00
CHEMBL1093644 1 8.00
CHEMBL1093974 1 8.00
CHEMBL1093646 1 7.96
CHEMBL1093645 1 7.96
CHEMBL1093979 1 7.96
CHEMBL1093637 1 7.96
CHEMBL1093635 1 7.96
CHEMBL1093631 1 7.92
CHEMBL1093981 1 7.92
CHEMBL218394 BOCEPREVIR 4.0 1 7.85
CHEMBL1092858 1 7.82
CHEMBL1093311 1 7.82
CHEMBL526753 1 7.80
CHEMBL1093640 1 7.72
CHEMBL1093636 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1093977 Ki = 2.0 nM 8.70
CHEMBL1093632 Ki = 3.0 nM 8.52
CHEMBL1093982 Ki = 3.0 nM 8.52
CHEMBL1093978 Ki = 4.0 nM 8.40
CHEMBL1093975 Ki = 4.0 nM 8.40
CHEMBL1093980 Ki = 5.0 nM 8.30
CHEMBL1093976 Ki = 5.0 nM 8.30
CHEMBL1093973 Ki = 6.0 nM 8.22
CHEMBL1093647 Ki = 7.0 nM 8.15
CHEMBL1093015 Ki = 8.0 nM 8.10
CHEMBL1093643 Ki = 9.0 nM 8.05
CHEMBL1093641 Ki = 9.0 nM 8.05
CHEMBL1093971 Ki = 9.0 nM 8.05
CHEMBL1093974 Ki = 10.0 nM 8.00
CHEMBL1093644 Ki = 10.0 nM 8.00
CHEMBL1088786 Ki = 10.0 nM 8.00
CHEMBL1093972 Ki = 10.0 nM 8.00
CHEMBL1093635 Ki = 11.0 nM 7.96
CHEMBL1093637 Ki = 11.0 nM 7.96
CHEMBL1093645 Ki = 11.0 nM 7.96
CHEMBL1093646 Ki = 11.0 nM 7.96
CHEMBL1093979 Ki = 11.0 nM 7.96
CHEMBL1093631 Ki = 12.0 nM 7.92
CHEMBL1093981 Ki = 12.0 nM 7.92
CHEMBL218394 BOCEPREVIR Ki = 14.0 nM 7.85
CHEMBL1092858 Ki = 15.0 nM 7.82
CHEMBL1093311 Ki = 15.0 nM 7.82
CHEMBL526753 Ki = 16.0 nM 7.80
CHEMBL1093640 Ki = 19.0 nM 7.72
CHEMBL1093636 Ki = 20.0 nM 7.70
CHEMBL1093633 Ki = 24.0 nM 7.62
CHEMBL1093420 Ki = 24.0 nM 7.62
CHEMBL1093648 Ki = 25.0 nM 7.60
CHEMBL1093642 Ki = 30.0 nM 7.52
CHEMBL1093970 Ki = 39.0 nM 7.41
CHEMBL1093638 Ki = 44.0 nM 7.36
CHEMBL1093630 Ki = 47.0 nM 7.33
CHEMBL1093634 Ki = 78.0 nM 7.11
CHEMBL502871 Ki = 100.0 nM 7.00
CHEMBL1091546 Ki = 100.0 nM 7.00
CHEMBL1088824 Ki = 140.0 nM 6.85
CHEMBL1093983 Ki = 280.0 nM 6.55
CHEMBL1093639 Ki = 300.0 nM 6.52