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Assay Detail

CHEMBL957610

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Binding
Inhibition of HIV1 recombinant integrase strand transfer activity
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 Autocuration

Target

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

Publication

3-Hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidine-2-carboxylates--a new class of HIV-1 integrase inhibitors.
Donghi M, Kinzel OD, Summa V.
Bioorg Med Chem Lett (2009) 19 : 1930 -1934
PubMed 19269170 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.47 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL523678 1 8.05
CHEMBL492930 1 7.75
CHEMBL494944 1 7.75
CHEMBL523833 1 7.75
CHEMBL492538 1 7.72
CHEMBL492329 1 7.68
CHEMBL492543 1 7.68
CHEMBL492350 1 7.68
CHEMBL494945 1 7.68
CHEMBL495145 1 7.68
CHEMBL499184 1 7.66
CHEMBL492932 1 7.64
CHEMBL492526 1 7.62
CHEMBL522653 1 7.60
CHEMBL492537 1 7.58
CHEMBL522534 1 7.44
CHEMBL493335 1 7.44
CHEMBL492328 1 7.30
CHEMBL495144 1 7.30
CHEMBL493531 1 7.16
CHEMBL492727 1 6.89
CHEMBL492524 1 6.77
CHEMBL494946 1 6.73
CHEMBL492525 1 6.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL523678 IC50 = 9.0 nM 8.05
CHEMBL492930 IC50 = 18.0 nM 7.75
CHEMBL494944 IC50 = 18.0 nM 7.75
CHEMBL523833 IC50 = 18.0 nM 7.75
CHEMBL492538 IC50 = 19.0 nM 7.72
CHEMBL492329 IC50 = 21.0 nM 7.68
CHEMBL492543 IC50 = 21.0 nM 7.68
CHEMBL492350 IC50 = 21.0 nM 7.68
CHEMBL494945 IC50 = 21.0 nM 7.68
CHEMBL495145 IC50 = 21.0 nM 7.68
CHEMBL499184 IC50 = 22.0 nM 7.66
CHEMBL492932 IC50 = 23.0 nM 7.64
CHEMBL492526 IC50 = 24.0 nM 7.62
CHEMBL522653 IC50 = 25.0 nM 7.60
CHEMBL492537 IC50 = 26.0 nM 7.58
CHEMBL522534 IC50 = 36.0 nM 7.44
CHEMBL493335 IC50 = 36.0 nM 7.44
CHEMBL492328 IC50 = 50.0 nM 7.30
CHEMBL495144 IC50 = 50.0 nM 7.30
CHEMBL493531 IC50 = 70.0 nM 7.16
CHEMBL492727 IC50 = 130.0 nM 6.89
CHEMBL492524 IC50 = 170.0 nM 6.77
CHEMBL494946 IC50 = 185.0 nM 6.73
CHEMBL492525 IC50 = 185.0 nM 6.73