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Assay Detail

CHEMBL933189

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Binding
Inhibition of recombinant HIV1 integrase strand transfer activity
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors.
Muraglia E, Kinzel O, Gardelli C, Crescenzi B, Donghi M, Ferrara M, Nizi E, Orvieto F, Pescatore G, Laufer R, Gonzalez-Paz O, Di Marco A, Fiore F, Monteagudo E, Fonsi M, Felock PJ, Rowley M, Summa V.
J Med Chem (2008) 51 : 861 -874
PubMed 18217703 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 51 7.89 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL410516 1 8.52
CHEMBL272009 1 8.40
CHEMBL260102 1 8.40
CHEMBL270536 1 8.30
CHEMBL279547 1 8.30
CHEMBL271627 1 8.30
CHEMBL270744 1 8.30
CHEMBL406657 1 8.22
CHEMBL269845 1 8.22
CHEMBL412090 1 8.22
CHEMBL412089 1 8.15
CHEMBL272883 1 8.15
CHEMBL412109 1 8.15
CHEMBL270514 1 8.15
CHEMBL272446 1 8.15
CHEMBL408479 1 8.15
CHEMBL272871 1 8.15
CHEMBL406656 1 8.15
CHEMBL272172 1 8.15
CHEMBL271821 1 8.15
CHEMBL259896 1 8.10
CHEMBL405261 1 8.10
CHEMBL271757 1 8.05
CHEMBL269844 1 8.05
CHEMBL408480 1 8.05
CHEMBL411489 1 8.00
CHEMBL216683 1 8.00
CHEMBL271744 1 8.00
CHEMBL270513 1 8.00
CHEMBL271541 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL410516 IC50 = 3.0 nM 8.52
CHEMBL272009 IC50 = 4.0 nM 8.40
CHEMBL260102 IC50 = 4.0 nM 8.40
CHEMBL270536 IC50 = 5.0 nM 8.30
CHEMBL279547 IC50 = 5.0 nM 8.30
CHEMBL271627 IC50 = 5.0 nM 8.30
CHEMBL270744 IC50 = 5.0 nM 8.30
CHEMBL406657 IC50 = 6.0 nM 8.22
CHEMBL269845 IC50 = 6.0 nM 8.22
CHEMBL412090 IC50 = 6.0 nM 8.22
CHEMBL272871 IC50 = 7.0 nM 8.15
CHEMBL272883 IC50 = 7.0 nM 8.15
CHEMBL412109 IC50 = 7.0 nM 8.15
CHEMBL270514 IC50 = 7.0 nM 8.15
CHEMBL272446 IC50 = 7.0 nM 8.15
CHEMBL412089 IC50 = 7.0 nM 8.15
CHEMBL408479 IC50 = 7.0 nM 8.15
CHEMBL406656 IC50 = 7.0 nM 8.15
CHEMBL272172 IC50 = 7.0 nM 8.15
CHEMBL271821 IC50 = 7.0 nM 8.15
CHEMBL259896 IC50 = 8.0 nM 8.10
CHEMBL405261 IC50 = 8.0 nM 8.10
CHEMBL271757 IC50 = 9.0 nM 8.05
CHEMBL269844 IC50 = 9.0 nM 8.05
CHEMBL408480 IC50 = 9.0 nM 8.05
CHEMBL411489 IC50 = 10.0 nM 8.00
CHEMBL270513 IC50 = 10.0 nM 8.00
CHEMBL216683 IC50 = 10.0 nM 8.00
CHEMBL271744 IC50 = 10.0 nM 8.00
CHEMBL271541 IC50 = 11.0 nM 7.96
CHEMBL409932 IC50 = 12.0 nM 7.92
CHEMBL408962 IC50 = 12.0 nM 7.92
CHEMBL410850 IC50 = 12.0 nM 7.92
CHEMBL270535 IC50 = 13.0 nM 7.89
CHEMBL271743 IC50 = 14.0 nM 7.85
CHEMBL259673 IC50 = 16.0 nM 7.80
CHEMBL269873 IC50 = 17.0 nM 7.77
CHEMBL259894 IC50 = 18.0 nM 7.75
CHEMBL270552 IC50 = 19.0 nM 7.72
CHEMBL429408 IC50 = 19.0 nM 7.72
CHEMBL270308 IC50 = 20.0 nM 7.70
CHEMBL259885 IC50 = 35.0 nM 7.46
CHEMBL271629 IC50 = 45.0 nM 7.35
CHEMBL386710 IC50 = 60.0 nM 7.22
CHEMBL217566 IC50 = 60.0 nM 7.22
CHEMBL260094 IC50 = 62.0 nM 7.21
CHEMBL429583 IC50 = 62.0 nM 7.21
CHEMBL409490 IC50 = 63.0 nM 7.20
CHEMBL429737 IC50 = 69.0 nM 7.16
CHEMBL216317 IC50 = 100.0 nM 7.00