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Assay Detail

CHEMBL1225823

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Binding
Inhibition of HIV1 integrase strand transfer activity after 1 hr
12
Total Activities
12
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 Autocuration

Target

Human immunodeficiency virus type 1 integrase (CHEMBL3471)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Synthesis of polyhydroxylated aromatics having amidation of piperazine nitrogen as HIV-1 integrase inhibitor.
Yang L, Xu X, Huang Y, Zhang B, Zeng C, He H, Wang C, Hu L.
Bioorg Med Chem Lett (2010) 20 : 5469 -5471
PubMed 20709544 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 4.91 6.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19977 1 6.11
CHEMBL1224051 1 4.89
CHEMBL1224124 1 4.81
CHEMBL1224052 1 4.76
CHEMBL1224122 1 4.71
CHEMBL1224053 1 4.60
CHEMBL1224123 1 4.50
CHEMBL1223934 1 -
CHEMBL1223935 1 -
CHEMBL1223936 1 -
CHEMBL1223937 1 -
CHEMBL1224050 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19977 IC50 = 770.0 nM 6.11
CHEMBL1224051 IC50 = 12830.0 nM 4.89
CHEMBL1224124 IC50 = 15410.0 nM 4.81
CHEMBL1224052 IC50 = 17470.0 nM 4.76
CHEMBL1224122 IC50 = 19270.0 nM 4.71
CHEMBL1224053 IC50 = 24940.0 nM 4.60
CHEMBL1224123 IC50 = 31310.0 nM 4.50
CHEMBL1223934 IC50 > 100000.0 nM -
CHEMBL1223935 IC50 > 100000.0 nM -
CHEMBL1223936 IC50 > 100000.0 nM -
CHEMBL1223937 IC50 > 100000.0 nM -
CHEMBL1224050 IC50 > 100000.0 nM -