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Assay Detail

CHEMBL3411709

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Binding
Inhibition of HIV1 reverse transcriptase Tyr181Cys mutant-associated RNA-dependent DNA polymerase activity after 30 mins
3
Total Activities
3
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

(3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase.
Meleddu R, Distinto S, Corona A, Bianco G, Cannas V, Esposito F, Artese A, Alcaro S, Matyus P, Bogdan D, Cottiglia F, Tramontano E, Maccioni E.
Eur J Med Chem (2015) 93 : 452 -460
PubMed 25728026 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.49 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL223228 EFAVIRENZ 4.0 1 6.17
CHEMBL3409201 1 4.81
CHEMBL45578 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL223228 EFAVIRENZ IC50 = 680.0 nM 6.17
CHEMBL3409201 IC50 = 15400.0 nM 4.81
CHEMBL45578 IC50 - -