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Assay Detail

CHEMBL4387463

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Binding
Inhibition of HIV reverse transcriptase RNase H activity
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design, synthesis and biological evaluation of 3-hydroxyquinazoline-2,4(1H,3H)-diones as dual inhibitors of HIV-1 reverse transcriptase-associated RNase H and integrase.
Gao P, Cheng X, Sun L, Song S, Álvarez M, Luczkowiak J, Pannecouque C, De Clercq E, Menéndez-Arias L, Zhan P, Liu X.
Bioorg Med Chem (2019) 27 : 3836 -3845
PubMed 31324562 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.16 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3290940 1 7.50
CHEMBL1270611 1 7.35
CHEMBL3818057 1 6.19
CHEMBL3414865 1 6.10
CHEMBL572124 1 5.85
CHEMBL4537833 1 5.72
CHEMBL550937 BETA-THUJAPLICINOL 1 5.42
CHEMBL4076949 1 5.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3290940 IC50 = 32.0 nM 7.50
CHEMBL1270611 IC50 = 45.0 nM 7.35
CHEMBL3818057 IC50 = 650.0 nM 6.19
CHEMBL3414865 IC50 = 800.0 nM 6.10
CHEMBL572124 IC50 = 1400.0 nM 5.85
CHEMBL4537833 IC50 = 1900.0 nM 5.72
CHEMBL550937 BETA-THUJAPLICINOL IC50 = 3800.0 nM 5.42
CHEMBL4076949 IC50 = 7300.0 nM 5.14