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Assay Detail

CHEMBL1016224

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

Binding
Inhibition of HIV1 RNase H
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design, synthesis, and biological evaluation of a series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as dual inhibitors of human immunodeficiency virus type 1 integrase and the reverse transcriptase RNase H domain.
Billamboz M, Bailly F, Barreca ML, De Luca L, Mouscadet JF, Calmels C, Andréola ML, Witvrouw M, Christ F, Debyser Z, Cotelle P.
J Med Chem (2008) 51 : 7717 -7730
PubMed 19053754 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 4.78 5.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL502584 1 5.24
CHEMBL16755 1 5.23
CHEMBL456338 1 5.18
CHEMBL444813 1 5.15
CHEMBL456337 1 5.14
CHEMBL456325 1 4.97
CHEMBL526563 1 4.97
CHEMBL509261 1 4.65
CHEMBL446740 1 4.54
CHEMBL456326 1 4.45
CHEMBL455061 1 4.43
CHEMBL461247 1 4.39
CHEMBL443423 1 4.32
CHEMBL461036 1 4.24
CHEMBL446644 1 -
CHEMBL444646 1 -
CHEMBL512021 1 -
CHEMBL456120 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL502584 IC50 = 5700.0 nM 5.24
CHEMBL16755 IC50 = 5900.0 nM 5.23
CHEMBL456338 IC50 = 6600.0 nM 5.18
CHEMBL444813 IC50 = 7100.0 nM 5.15
CHEMBL456337 IC50 = 7200.0 nM 5.14
CHEMBL456325 IC50 = 10800.0 nM 4.97
CHEMBL526563 IC50 = 10700.0 nM 4.97
CHEMBL509261 IC50 = 22200.0 nM 4.65
CHEMBL446740 IC50 = 28900.0 nM 4.54
CHEMBL456326 IC50 = 35300.0 nM 4.45
CHEMBL455061 IC50 = 37400.0 nM 4.43
CHEMBL461247 IC50 = 40700.0 nM 4.39
CHEMBL443423 IC50 = 48000.0 nM 4.32
CHEMBL461036 IC50 = 58000.0 nM 4.24
CHEMBL446644 IC50 > 80000.0 nM -
CHEMBL444646 IC50 > 96000.0 nM -
CHEMBL512021 IC50 > 80000.0 nM -
CHEMBL456120 IC50 > 80000.0 nM -