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Assay Detail

CHEMBL3411705

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Binding
Inhibition of HIV1 reverse transcriptase-associated DNA polymerase-independent RNase H activity after 1 hr
14
Total Activities
14
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 14 5.20 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3409201 1 5.60
CHEMBL3409202 1 5.58
CHEMBL2005185 1 5.55
CHEMBL1968193 1 5.54
CHEMBL1958265 1 5.50
CHEMBL3409205 1 5.41
CHEMBL3409204 1 5.33
CHEMBL3409200 1 5.19
CHEMBL3409203 1 5.05
CHEMBL45578 1 5.00
CHEMBL3409199 1 4.97
CHEMBL1976117 1 4.83
CHEMBL1976450 1 4.00
CHEMBL223228 EFAVIRENZ 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3409201 IC50 = 2500.0 nM 5.60
CHEMBL3409202 IC50 = 2600.0 nM 5.58
CHEMBL2005185 IC50 = 2800.0 nM 5.55
CHEMBL1968193 IC50 = 2900.0 nM 5.54
CHEMBL1958265 IC50 = 3200.0 nM 5.50
CHEMBL3409205 IC50 = 3900.0 nM 5.41
CHEMBL3409204 IC50 = 4700.0 nM 5.33
CHEMBL3409200 IC50 = 6400.0 nM 5.19
CHEMBL3409203 IC50 = 9000.0 nM 5.05
CHEMBL45578 IC50 = 10100.0 nM 5.00
CHEMBL3409199 IC50 = 10600.0 nM 4.97
CHEMBL1976117 IC50 = 14900.0 nM 4.83
CHEMBL1976450 IC50 = 100000.0 nM 4.00
CHEMBL223228 EFAVIRENZ IC50 - -