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Assay Detail

CHEMBL769364

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Binding
Inhibition of purified recombinant HIV-1 protease in a fluorogenic assay
78
Total Activities
78
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

Symmetry-based inhibitors of HIV protease. Structure-activity studies of acylated 2,4-diamino-1,5-diphenyl-3-hydroxypentane and 2,5-diamino-1,6-diphenylhexane-3,4-diol.
Kempf DJ, Codacovi L, Wang XC, Kohlbrenner WE, Wideburg NE, Saldivar A, Vasavanonda S, Marsh KC, Bryant P, Sham HL.
J Med Chem (1993) 36 : 320 -330
PubMed 8426362 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 78 8.01 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL432806 1 9.00
CHEMBL320126 1 8.92
CHEMBL320322 1 8.85
CHEMBL324916 1 8.82
CHEMBL324747 1 8.80
CHEMBL331363 1 8.80
CHEMBL112930 1 8.80
CHEMBL113575 1 8.78
CHEMBL322804 1 8.77
CHEMBL113626 1 8.66
CHEMBL109221 1 8.64
CHEMBL109371 1 8.52
CHEMBL430891 1 8.52
CHEMBL113627 1 8.40
CHEMBL106486 1 8.32
CHEMBL111957 1 8.28
CHEMBL323955 1 8.28
CHEMBL112578 1 8.24
CHEMBL112186 1 8.17
CHEMBL419580 1 8.15
CHEMBL112546 1 8.15
CHEMBL112846 1 8.12
CHEMBL320321 1 8.11
CHEMBL112412 1 8.05
CHEMBL330915 1 8.05
CHEMBL114192 1 8.00
CHEMBL331829 1 7.92
CHEMBL110865 1 7.89
CHEMBL113264 1 7.89
CHEMBL112569 1 7.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL432806 IC50 = 1.0 nM 9.00
CHEMBL320126 IC50 = 1.2 nM 8.92
CHEMBL320322 IC50 = 1.4 nM 8.85
CHEMBL324916 IC50 = 1.5 nM 8.82
CHEMBL324747 IC50 = 1.6 nM 8.80
CHEMBL331363 IC50 = 1.6 nM 8.80
CHEMBL112930 IC50 = 1.6 nM 8.80
CHEMBL113575 IC50 = 1.66 nM 8.78
CHEMBL322804 IC50 = 1.7 nM 8.77
CHEMBL113626 IC50 = 2.2 nM 8.66
CHEMBL109221 IC50 = 2.3 nM 8.64
CHEMBL109371 IC50 = 3.0 nM 8.52
CHEMBL430891 IC50 = 3.0 nM 8.52
CHEMBL113627 IC50 = 4.0 nM 8.40
CHEMBL106486 IC50 = 4.8 nM 8.32
CHEMBL111957 IC50 = 5.3 nM 8.28
CHEMBL323955 IC50 = 5.2 nM 8.28
CHEMBL112578 IC50 = 5.7 nM 8.24
CHEMBL112186 IC50 = 6.8 nM 8.17
CHEMBL419580 IC50 = 7.1 nM 8.15
CHEMBL112546 IC50 = 7.0 nM 8.15
CHEMBL112846 IC50 = 7.5 nM 8.12
CHEMBL320321 IC50 = 7.8 nM 8.11
CHEMBL112412 IC50 = 9.0 nM 8.05
CHEMBL330915 IC50 = 9.0 nM 8.05
CHEMBL114192 IC50 = 10.0 nM 8.00
CHEMBL331829 IC50 = 12.0 nM 7.92
CHEMBL110865 IC50 = 13.0 nM 7.89
CHEMBL113264 IC50 = 13.0 nM 7.89
CHEMBL112569 IC50 = 14.0 nM 7.85
CHEMBL333611 IC50 = 20.0 nM 7.70
CHEMBL442010 IC50 = 22.0 nM 7.66
CHEMBL109220 IC50 = 22.0 nM 7.66
CHEMBL109699 IC50 = 23.0 nM 7.64
CHEMBL322939 IC50 = 24.0 nM 7.62
CHEMBL113268 IC50 = 26.0 nM 7.58
CHEMBL411507 IC50 = 28.0 nM 7.55
CHEMBL263534 IC50 = 31.0 nM 7.51
CHEMBL325731 IC50 = 38.0 nM 7.42
CHEMBL113554 IC50 = 43.0 nM 7.37
CHEMBL322964 IC50 = 43.0 nM 7.37
CHEMBL110603 IC50 = 63.0 nM 7.20
CHEMBL326053 IC50 = 71.0 nM 7.15
CHEMBL325847 IC50 = 180.0 nM 6.75
CHEMBL320243 IC50 = 240.0 nM 6.62
CHEMBL325673 IC50 = 1300.0 nM 5.89
CHEMBL331814 IC50 < 1.0 nM -
CHEMBL324746 IC50 < 1.0 nM -
CHEMBL109976 IC50 < 1.0 nM -
CHEMBL324163 IC50 < 1.0 nM -