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Assay Detail

CHEMBL954256

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Binding
Inhibition of HIV1 reverse transcriptase p66/p51 L100I mutant
27
Total Activities
27
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

Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
Piscitelli F, Coluccia A, Brancale A, La Regina G, Sansone A, Giordano C, Balzarini J, Maga G, Zanoli S, Samuele A, Cirilli R, La Torre F, Lavecchia A, Novellino E, Silvestri R.
J Med Chem (2009) 52 : 1922 -1934
PubMed 19281225 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.95 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL398174 1 8.70
CHEMBL502565 1 8.40
CHEMBL470630 1 7.89
CHEMBL470007 1 7.60
CHEMBL469562 1 7.39
CHEMBL85059 1 7.22
CHEMBL127012 1 6.95
CHEMBL502566 1 6.90
CHEMBL513080 1 6.89
CHEMBL469985 1 6.84
CHEMBL126603 1 6.79
CHEMBL469986 1 6.77
CHEMBL512486 1 6.72
CHEMBL512673 1 6.70
CHEMBL472217 1 6.69
CHEMBL470403 1 6.69
CHEMBL511290 1 6.68
CHEMBL469358 1 6.60
CHEMBL511963 1 6.57
CHEMBL521183 1 6.57
CHEMBL469569 1 6.53
CHEMBL470404 1 6.50
CHEMBL485180 1 6.44
CHEMBL469804 1 6.41
CHEMBL524360 1 6.41
CHEMBL502297 1 -
CHEMBL383700 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL398174 IC50 = 2.0 nM 8.70
CHEMBL502565 IC50 = 4.0 nM 8.40
CHEMBL470630 IC50 = 13.0 nM 7.89
CHEMBL470007 IC50 = 25.0 nM 7.60
CHEMBL469562 IC50 = 41.0 nM 7.39
CHEMBL85059 IC50 = 60.0 nM 7.22
CHEMBL127012 IC50 = 112.0 nM 6.95
CHEMBL502566 IC50 = 125.0 nM 6.90
CHEMBL513080 IC50 = 130.0 nM 6.89
CHEMBL469985 IC50 = 143.0 nM 6.84
CHEMBL126603 IC50 = 161.0 nM 6.79
CHEMBL469986 IC50 = 169.0 nM 6.77
CHEMBL512486 IC50 = 191.0 nM 6.72
CHEMBL512673 IC50 = 199.0 nM 6.70
CHEMBL472217 IC50 = 204.0 nM 6.69
CHEMBL470403 IC50 = 206.0 nM 6.69
CHEMBL511290 IC50 = 209.0 nM 6.68
CHEMBL469358 IC50 = 252.0 nM 6.60
CHEMBL511963 IC50 = 270.0 nM 6.57
CHEMBL521183 IC50 = 267.0 nM 6.57
CHEMBL469569 IC50 = 296.0 nM 6.53
CHEMBL470404 IC50 = 319.0 nM 6.50
CHEMBL485180 IC50 = 364.0 nM 6.44
CHEMBL469804 IC50 = 390.0 nM 6.41
CHEMBL524360 IC50 = 388.0 nM 6.41
CHEMBL502297 IC50 - -
CHEMBL383700 IC50 - -