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Assay Detail

CHEMBL765640

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Binding
Inhibitory activity against HIV-I protease.
32
Total Activities
31
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

Structure-based design of nonpeptidic HIV protease inhibitors from a cyclooctylpyranone lead structure.
Romines KR, Watenpaugh KD, Howe WJ, Tomich PK, Lovasz KD, Morris JK, Janakiraman MN, Lynn JC, Horng MM, Chong KT.
J Med Chem (1995) 38 : 4463 -4473
PubMed 7473573 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 7.40 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL342947 1 8.52
CHEMBL16359 1 8.40
CHEMBL138388 1 8.26
CHEMBL138637 1 8.16
CHEMBL343163 2 8.05
CHEMBL343608 1 7.96
CHEMBL137832 1 7.93
CHEMBL434266 1 7.85
CHEMBL335789 1 7.62
CHEMBL138135 1 7.62
CHEMBL343044 1 7.55
CHEMBL138147 1 7.52
CHEMBL137977 1 7.51
CHEMBL343963 1 7.50
CHEMBL337760 1 7.48
CHEMBL139519 1 7.48
CHEMBL140074 1 7.38
CHEMBL336038 1 7.37
CHEMBL434808 1 7.30
CHEMBL138205 1 7.26
CHEMBL344442 1 7.24
CHEMBL132747 1 7.23
CHEMBL139397 1 7.14
CHEMBL16584 1 7.02
CHEMBL341707 1 6.92
CHEMBL137841 1 6.62
CHEMBL139434 1 6.58
CHEMBL343811 1 6.58
CHEMBL139850 1 6.48
CHEMBL436210 1 6.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL342947 Ki = 3.0 nM 8.52
CHEMBL16359 Ki = 4.0 nM 8.40
CHEMBL138388 Ki = 5.5 nM 8.26
CHEMBL138637 Ki = 6.9 nM 8.16
CHEMBL343163 Ki = 9.0 nM 8.05
CHEMBL343608 Ki = 11.0 nM 7.96
CHEMBL137832 Ki = 11.7 nM 7.93
CHEMBL434266 Ki = 14.0 nM 7.85
CHEMBL335789 Ki = 24.0 nM 7.62
CHEMBL138135 Ki = 24.0 nM 7.62
CHEMBL343163 Ki = 26.0 nM 7.58
CHEMBL343044 Ki = 28.0 nM 7.55
CHEMBL138147 Ki = 30.0 nM 7.52
CHEMBL137977 Ki = 31.0 nM 7.51
CHEMBL343963 Ki = 32.0 nM 7.50
CHEMBL337760 Ki = 33.0 nM 7.48
CHEMBL139519 Ki = 33.0 nM 7.48
CHEMBL140074 Ki = 42.0 nM 7.38
CHEMBL336038 Ki = 43.0 nM 7.37
CHEMBL434808 Ki = 50.0 nM 7.30
CHEMBL138205 Ki = 55.0 nM 7.26
CHEMBL344442 Ki = 57.0 nM 7.24
CHEMBL132747 Ki = 58.3 nM 7.23
CHEMBL139397 Ki = 72.0 nM 7.14
CHEMBL16584 Ki = 96.0 nM 7.02
CHEMBL341707 Ki = 120.0 nM 6.92
CHEMBL137841 Ki = 240.0 nM 6.62
CHEMBL139434 Ki = 260.0 nM 6.58
CHEMBL343811 Ki = 266.0 nM 6.58
CHEMBL139850 Ki = 330.0 nM 6.48
CHEMBL436210 Ki = 450.0 nM 6.35
CHEMBL139070 Ki = 470.0 nM 6.33