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Assay Detail

CHEMBL838839

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Binding
Inhibition constant for human immunodeficiency virus type 1 protease
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 9 — Direct single protein target
Curated By Expert

Target

Human immunodeficiency virus type 1 protease (CHEMBL243)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
Shuman CF, Vrang L, Danielson UH.
J Med Chem (2004) 47 : 5953 -5961
PubMed 15537350 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 8.78 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1161736 1 10.30
CHEMBL729 LOPINAVIR 4.0 1 10.10
CHEMBL1161737 1 10.05
CHEMBL114 SAQUINAVIR 4.0 1 9.64
CHEMBL116 AMPRENAVIR 4.0 1 9.64
CHEMBL1163 ATAZANAVIR 4.0 1 9.62
CHEMBL1161741 1 9.52
CHEMBL1161732 1 9.52
CHEMBL5483011 INDINAVIR 3.0 1 9.51
CHEMBL1161734 1 9.40
CHEMBL584 NELFINAVIR 4.0 1 9.27
CHEMBL1161738 1 9.26
CHEMBL163 RITONAVIR 4.0 1 9.23
CHEMBL1161742 1 9.22
CHEMBL1161743 1 9.21
CHEMBL1161733 1 9.10
CHEMBL365756 1 8.92
CHEMBL425182 1 8.85
CHEMBL610244 1 8.85
CHEMBL340616 1 8.51
CHEMBL190112 1 8.25
CHEMBL443 SULFAMETHOXAZOLE 4.0 1 8.00
CHEMBL345603 1 7.43
CHEMBL1161735 1 7.40
CHEMBL150908 1 7.26
CHEMBL1161739 1 5.62
CHEMBL1161740 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1161736 Ki = 0.05 nM 10.30
CHEMBL729 LOPINAVIR Ki = 0.08 nM 10.10
CHEMBL1161737 Ki = 0.09 nM 10.05
CHEMBL114 SAQUINAVIR Ki = 0.23 nM 9.64
CHEMBL116 AMPRENAVIR Ki = 0.23 nM 9.64
CHEMBL1163 ATAZANAVIR Ki = 0.24 nM 9.62
CHEMBL1161741 Ki = 0.3 nM 9.52
CHEMBL1161732 Ki = 0.3 nM 9.52
CHEMBL5483011 INDINAVIR Ki = 0.31 nM 9.51
CHEMBL1161734 Ki = 0.4 nM 9.40
CHEMBL584 NELFINAVIR Ki = 0.54 nM 9.27
CHEMBL1161738 Ki = 0.55 nM 9.26
CHEMBL163 RITONAVIR Ki = 0.59 nM 9.23
CHEMBL1161742 Ki = 0.6 nM 9.22
CHEMBL1161743 Ki = 0.61 nM 9.21
CHEMBL1161733 Ki = 0.8 nM 9.10
CHEMBL365756 Ki = 1.2 nM 8.92
CHEMBL425182 Ki = 1.4 nM 8.85
CHEMBL610244 Ki = 1.4 nM 8.85
CHEMBL340616 Ki = 3.1 nM 8.51
CHEMBL190112 Ki = 5.6 nM 8.25
CHEMBL443 SULFAMETHOXAZOLE Ki = 10.1 nM 8.00
CHEMBL345603 Ki = 37.0 nM 7.43
CHEMBL1161735 Ki = 40.0 nM 7.40
CHEMBL150908 Ki = 55.0 nM 7.26
CHEMBL1161739 Ki = 2400.0 nM 5.62
CHEMBL1161740 Ki = 5000.0 nM 5.30