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Assay Detail

CHEMBL802759

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
In vitro inhibitory activity against human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT)
122
Total Activities
122
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

Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones.
Hargrave KD, Proudfoot JR, Grozinger KG, Cullen E, Kapadia SR, Patel UR, Fuchs VU, Mauldin SC, Vitous J, Behnke ML.
J Med Chem (1991) 34 : 2231 -2241
PubMed 1712395 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 122 6.24 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129 ZIDOVUDINE 4.0 1 8.22
CHEMBL37628 1 7.46
CHEMBL70629 1 7.44
CHEMBL307220 1 7.42
CHEMBL439943 1 7.40
CHEMBL70719 1 7.21
CHEMBL57 NEVIRAPINE 4.0 1 7.08
CHEMBL37842 1 7.02
CHEMBL73672 1 6.96
CHEMBL37343 1 6.90
CHEMBL74690 1 6.85
CHEMBL288305 1 6.77
CHEMBL305965 1 6.77
CHEMBL69894 1 6.77
CHEMBL71311 1 6.72
CHEMBL70483 1 6.70
CHEMBL308248 1 6.64
CHEMBL308686 1 6.64
CHEMBL305521 1 6.62
CHEMBL70850 1 6.62
CHEMBL70255 1 6.54
CHEMBL306032 1 6.46
CHEMBL309574 1 6.44
CHEMBL70312 1 6.42
CHEMBL73845 1 6.42
CHEMBL71927 1 6.40
CHEMBL311349 1 6.39
CHEMBL70930 1 6.38
CHEMBL424046 1 6.37
CHEMBL291024 1 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129 ZIDOVUDINE IC50 = 6.0 nM 8.22
CHEMBL37628 IC50 = 35.0 nM 7.46
CHEMBL70629 IC50 = 36.0 nM 7.44
CHEMBL307220 IC50 = 38.0 nM 7.42
CHEMBL439943 IC50 = 40.0 nM 7.40
CHEMBL70719 IC50 = 62.0 nM 7.21
CHEMBL57 NEVIRAPINE IC50 = 84.0 nM 7.08
CHEMBL37842 IC50 = 95.0 nM 7.02
CHEMBL73672 IC50 = 110.0 nM 6.96
CHEMBL37343 IC50 = 125.0 nM 6.90
CHEMBL74690 IC50 = 140.0 nM 6.85
CHEMBL305965 IC50 = 170.0 nM 6.77
CHEMBL69894 IC50 = 170.0 nM 6.77
CHEMBL288305 IC50 = 170.0 nM 6.77
CHEMBL71311 IC50 = 190.0 nM 6.72
CHEMBL70483 IC50 = 200.0 nM 6.70
CHEMBL308686 IC50 = 230.0 nM 6.64
CHEMBL308248 IC50 = 230.0 nM 6.64
CHEMBL305521 IC50 = 240.0 nM 6.62
CHEMBL70850 IC50 = 240.0 nM 6.62
CHEMBL70255 IC50 = 290.0 nM 6.54
CHEMBL306032 IC50 = 350.0 nM 6.46
CHEMBL309574 IC50 = 360.0 nM 6.44
CHEMBL73845 IC50 = 380.0 nM 6.42
CHEMBL70312 IC50 = 380.0 nM 6.42
CHEMBL71927 IC50 = 400.0 nM 6.40
CHEMBL311349 IC50 = 410.0 nM 6.39
CHEMBL70930 IC50 = 420.0 nM 6.38
CHEMBL424046 IC50 = 430.0 nM 6.37
CHEMBL291024 IC50 = 440.0 nM 6.36
CHEMBL289816 IC50 = 450.0 nM 6.35
CHEMBL290957 IC50 = 450.0 nM 6.35
CHEMBL305010 IC50 = 500.0 nM 6.30
CHEMBL312340 IC50 = 580.0 nM 6.24
CHEMBL71023 IC50 = 590.0 nM 6.23
CHEMBL302931 IC50 = 650.0 nM 6.19
CHEMBL303466 IC50 = 650.0 nM 6.19
CHEMBL70562 IC50 = 690.0 nM 6.16
CHEMBL39950 IC50 = 760.0 nM 6.12
CHEMBL310490 IC50 = 850.0 nM 6.07
CHEMBL70743 IC50 = 850.0 nM 6.07
CHEMBL290410 IC50 = 850.0 nM 6.07
CHEMBL305416 IC50 = 890.0 nM 6.05
CHEMBL73015 IC50 = 1000.0 nM 6.00
CHEMBL419629 IC50 = 1000.0 nM 6.00
CHEMBL418885 IC50 = 1100.0 nM 5.96
CHEMBL291113 IC50 = 1250.0 nM 5.90
CHEMBL72535 IC50 = 1400.0 nM 5.85
CHEMBL289429 IC50 = 1900.0 nM 5.72
CHEMBL71310 IC50 = 2100.0 nM 5.68