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Assay Detail

CHEMBL798355

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Binding
Compound was evaluated for its ability to inhibit HIV-1 Reverse Transcriptase in an in vitro enzyme assay
24
Total Activities
24
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

4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.
Cocuzza AJ, Chidester DR, Cordova BC, Klabe RM, Jeffrey S, Diamond S, Weigelt CA, Ko SS, Bacheler LT, Erickson-Viitanen SK, Rodgers JD.
Bioorg Med Chem Lett (2001) 11 : 1389 -1392
PubMed 11378361 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.61 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL29274 1 7.64
CHEMBL283619 1 7.50
CHEMBL223228 EFAVIRENZ 4.0 1 7.42
CHEMBL31977 1 7.34
CHEMBL2114369 1 7.09
CHEMBL2114370 1 7.02
CHEMBL29171 1 6.97
CHEMBL287650 1 6.89
CHEMBL30752 1 6.82
CHEMBL2114371 1 6.77
CHEMBL281230 1 6.76
CHEMBL284065 1 6.73
CHEMBL31771 1 6.71
CHEMBL31285 1 6.63
CHEMBL2115317 1 6.60
CHEMBL32290 1 6.37
CHEMBL283614 1 6.37
CHEMBL32038 1 6.22
CHEMBL283630 1 6.10
CHEMBL281239 1 6.02
CHEMBL2115319 1 5.94
CHEMBL2115318 1 5.71
CHEMBL31455 1 5.60
CHEMBL32460 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL29274 IC50 = 23.0 nM 7.64
CHEMBL283619 IC50 = 32.0 nM 7.50
CHEMBL223228 EFAVIRENZ IC50 = 38.0 nM 7.42
CHEMBL31977 IC50 = 46.0 nM 7.34
CHEMBL2114369 IC50 = 82.0 nM 7.09
CHEMBL2114370 IC50 = 95.0 nM 7.02
CHEMBL29171 IC50 = 108.0 nM 6.97
CHEMBL287650 IC50 = 129.0 nM 6.89
CHEMBL30752 IC50 = 151.0 nM 6.82
CHEMBL2114371 IC50 = 171.0 nM 6.77
CHEMBL281230 IC50 = 173.0 nM 6.76
CHEMBL284065 IC50 = 185.0 nM 6.73
CHEMBL31771 IC50 = 193.0 nM 6.71
CHEMBL31285 IC50 = 235.0 nM 6.63
CHEMBL2115317 IC50 = 249.0 nM 6.60
CHEMBL32290 IC50 = 432.0 nM 6.37
CHEMBL283614 IC50 = 423.0 nM 6.37
CHEMBL32038 IC50 = 597.0 nM 6.22
CHEMBL283630 IC50 = 799.0 nM 6.10
CHEMBL281239 IC50 = 964.0 nM 6.02
CHEMBL2115319 IC50 = 1140.0 nM 5.94
CHEMBL2115318 IC50 = 1940.0 nM 5.71
CHEMBL31455 IC50 = 2510.0 nM 5.60
CHEMBL32460 IC50 = 3300.0 nM 5.48