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Assay Detail

CHEMBL800043

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Binding
Inhibitory concentration for 50% inhibition of HIV-1 reverse transcriptase
34
Total Activities
32
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 reverse transcriptase (CHEMBL247)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Synthesis and evaluation of quinoxalinones as HIV-1 reverse transcriptase inhibitors.
Patel M, McHugh RJ, Cordova BC, Klabe RM, Erickson-Viitanen S, Trainor GL, Rodgers JD.
Bioorg Med Chem Lett (2000) 10 : 1729 -1731
PubMed 10937734 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 6.63 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL300087 2 7.35
CHEMBL223228 EFAVIRENZ 4.0 1 7.32
CHEMBL49316 1 6.97
CHEMBL48628 1 6.96
CHEMBL297897 1 6.92
CHEMBL295606 1 6.91
CHEMBL48376 1 6.91
CHEMBL299394 1 6.90
CHEMBL50550 2 6.90
CHEMBL431936 1 6.89
CHEMBL299978 1 6.83
CHEMBL295893 1 6.80
CHEMBL297851 1 6.80
CHEMBL50664 1 6.77
CHEMBL301370 OPAVIRALINE 2.0 1 6.75
CHEMBL49733 1 6.74
CHEMBL299073 1 6.58
CHEMBL46008 1 6.50
CHEMBL49531 1 6.48
CHEMBL48286 1 6.47
CHEMBL300721 1 6.39
CHEMBL297103 1 6.30
CHEMBL46209 1 6.22
CHEMBL48629 1 6.19
CHEMBL301986 1 6.17
CHEMBL439929 1 5.94
CHEMBL301996 1 5.74
CHEMBL49030 1 5.74
CHEMBL295567 1 -
CHEMBL48735 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL300087 IC50 = 45.0 nM 7.35
CHEMBL223228 EFAVIRENZ IC50 = 48.0 nM 7.32
CHEMBL49316 IC50 = 108.0 nM 6.97
CHEMBL48628 IC50 = 109.0 nM 6.96
CHEMBL300087 IC50 = 118.0 nM 6.93
CHEMBL297897 IC50 = 121.0 nM 6.92
CHEMBL295606 IC50 = 124.0 nM 6.91
CHEMBL48376 IC50 = 123.0 nM 6.91
CHEMBL50550 IC50 = 127.0 nM 6.90
CHEMBL299394 IC50 = 127.0 nM 6.90
CHEMBL431936 IC50 = 130.0 nM 6.89
CHEMBL299978 IC50 = 147.0 nM 6.83
CHEMBL295893 IC50 = 160.0 nM 6.80
CHEMBL297851 IC50 = 160.0 nM 6.80
CHEMBL50664 IC50 = 169.0 nM 6.77
CHEMBL301370 OPAVIRALINE IC50 = 179.0 nM 6.75
CHEMBL49733 IC50 = 183.0 nM 6.74
CHEMBL50550 IC50 = 253.0 nM 6.60
CHEMBL299073 IC50 = 263.0 nM 6.58
CHEMBL46008 IC50 = 315.0 nM 6.50
CHEMBL49531 IC50 = 329.0 nM 6.48
CHEMBL48286 IC50 = 340.0 nM 6.47
CHEMBL300721 IC50 = 404.0 nM 6.39
CHEMBL297103 IC50 = 504.0 nM 6.30
CHEMBL46209 IC50 = 601.0 nM 6.22
CHEMBL48629 IC50 = 650.0 nM 6.19
CHEMBL301986 IC50 = 672.0 nM 6.17
CHEMBL439929 IC50 = 1142.0 nM 5.94
CHEMBL301996 IC50 = 1818.0 nM 5.74
CHEMBL49030 IC50 = 1807.0 nM 5.74
CHEMBL295567 IC50 > 5000.0 nM -
CHEMBL48735 IC50 > 5000.0 nM -
CHEMBL299788 IC50 > 5000.0 nM -
CHEMBL48255 IC50 > 5000.0 nM -