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Assay Detail

CHEMBL3240945

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Binding
Inhibition of HIV1 RNase H function of recombinant reverse transcriptase using an 18-nt 3'-fluorescein-labeled RNA annealed to complementary 18-nt 5'-dabsyl-labeled DNA as substrate after 10 mins by fluorescence spectrometer analysis
19
Total Activities
19
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 reverse transcriptase (CHEMBL247)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Basic quinolinonyl diketo acid derivatives as inhibitors of HIV integrase and their activity against RNase H function of reverse transcriptase.
Costi R, Métifiot M, Chung S, Cuzzucoli Crucitti G, Maddali K, Pescatori L, Messore A, Madia VN, Pupo G, Scipione L, Tortorella S, Di Leva FS, Cosconati S, Marinelli L, Novellino E, Le Grice SF, Corona A, Pommier Y, Marchand C, Di Santo R.
J Med Chem (2014) 57 : 3223 -3234
PubMed 24684270 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 4.92 5.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3238130 1 5.48
CHEMBL496454 1 5.29
CHEMBL3238134 1 5.24
CHEMBL3238133 1 5.18
CHEMBL3238132 1 5.17
CHEMBL3238121 1 4.73
CHEMBL3238122 1 4.58
CHEMBL3238127 1 4.54
CHEMBL204656 ELVITEGRAVIR 4.0 1 4.04
CHEMBL3238123 1 -
CHEMBL3238124 1 -
CHEMBL3238125 1 -
CHEMBL3238126 1 -
CHEMBL3238128 1 -
CHEMBL3238129 1 -
CHEMBL3238131 1 -
CHEMBL456365 1 -
CHEMBL3238120 1 -
CHEMBL254316 RALTEGRAVIR 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3238130 IC50 = 3300.0 nM 5.48
CHEMBL496454 IC50 = 5100.0 nM 5.29
CHEMBL3238134 IC50 = 5700.0 nM 5.24
CHEMBL3238133 IC50 = 6600.0 nM 5.18
CHEMBL3238132 IC50 = 6800.0 nM 5.17
CHEMBL3238121 IC50 = 18500.0 nM 4.73
CHEMBL3238122 IC50 = 26200.0 nM 4.58
CHEMBL3238127 IC50 = 28700.0 nM 4.54
CHEMBL204656 ELVITEGRAVIR IC50 = 91000.0 nM 4.04
CHEMBL3238123 IC50 - -
CHEMBL3238124 IC50 - -
CHEMBL3238125 IC50 - -
CHEMBL3238126 IC50 - -
CHEMBL3238128 IC50 - -
CHEMBL3238129 IC50 - -
CHEMBL3238131 IC50 - -
CHEMBL456365 IC50 - -
CHEMBL3238120 IC50 - -
CHEMBL254316 RALTEGRAVIR IC50 > 100000.0 nM -