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Assay Detail

CHEMBL841761

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Binding
Binding affinity 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
Kd 27 7.91 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL729 LOPINAVIR 4.0 1 10.00
CHEMBL114 SAQUINAVIR 4.0 1 9.51
CHEMBL1163 ATAZANAVIR 4.0 1 9.40
CHEMBL163 RITONAVIR 4.0 1 9.22
CHEMBL1161738 1 9.19
CHEMBL5483011 INDINAVIR 3.0 1 8.97
CHEMBL116 AMPRENAVIR 4.0 1 8.96
CHEMBL1161743 1 8.93
CHEMBL584 NELFINAVIR 4.0 1 8.79
CHEMBL1161737 1 8.71
CHEMBL365756 1 8.52
CHEMBL1161736 1 8.36
CHEMBL1161734 1 7.97
CHEMBL1161742 1 7.86
CHEMBL1161741 1 7.76
CHEMBL610244 1 7.74
CHEMBL1161732 1 7.68
CHEMBL1161733 1 7.47
CHEMBL425182 1 7.45
CHEMBL340616 1 7.40
CHEMBL190112 1 6.77
CHEMBL150908 1 6.44
CHEMBL345603 1 6.38
CHEMBL443 SULFAMETHOXAZOLE 4.0 1 6.24
CHEMBL1161735 1 5.52
CHEMBL1161739 1 4.42
CHEMBL1161740 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL729 LOPINAVIR Kd = 0.1 nM 10.00
CHEMBL114 SAQUINAVIR Kd = 0.31 nM 9.51
CHEMBL1163 ATAZANAVIR Kd = 0.4 nM 9.40
CHEMBL163 RITONAVIR Kd = 0.6 nM 9.22
CHEMBL1161738 Kd = 0.64 nM 9.19
CHEMBL5483011 INDINAVIR Kd = 1.07 nM 8.97
CHEMBL116 AMPRENAVIR Kd = 1.1 nM 8.96
CHEMBL1161743 Kd = 1.18 nM 8.93
CHEMBL584 NELFINAVIR Kd = 1.64 nM 8.79
CHEMBL1161737 Kd = 1.95 nM 8.71
CHEMBL365756 Kd = 3.04 nM 8.52
CHEMBL1161736 Kd = 4.42 nM 8.36
CHEMBL1161734 Kd = 10.8 nM 7.97
CHEMBL1161742 Kd = 13.9 nM 7.86
CHEMBL1161741 Kd = 17.5 nM 7.76
CHEMBL610244 Kd = 18.2 nM 7.74
CHEMBL1161732 Kd = 21.1 nM 7.68
CHEMBL1161733 Kd = 34.2 nM 7.47
CHEMBL425182 Kd = 35.8 nM 7.45
CHEMBL340616 Kd = 39.8 nM 7.40
CHEMBL190112 Kd = 169.0 nM 6.77
CHEMBL150908 Kd = 366.0 nM 6.44
CHEMBL345603 Kd = 420.0 nM 6.38
CHEMBL443 SULFAMETHOXAZOLE Kd = 577.0 nM 6.24
CHEMBL1161735 Kd = 2990.0 nM 5.52
CHEMBL1161739 Kd = 38400.0 nM 4.42
CHEMBL1161740 Kd = 309000.0 nM -