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Assay Detail

CHEMBL799138

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of HIV-1 reverse transcriptase (RT)
12
Total Activities
12
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 Expert

Target

Human immunodeficiency virus type 1 reverse transcriptase (CHEMBL247)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

A new series of pyridinone derivatives as potent non-nucleoside human immunodeficiency virus type 1 specific reverse transcriptase inhibitors.
Dollé V, Fan E, Nguyen CH, Aubertin AM, Kirn A, Andreola ML, Jamieson G, Tarrago-Litvak L, Bisagni E.
J Med Chem (1995) 38 : 4679 -4686
PubMed 7473595 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.89 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL336237 1 7.82
CHEMBL416107 1 7.52
CHEMBL140532 1 7.00
CHEMBL341931 1 6.40
CHEMBL37067 1 6.40
CHEMBL357409 1 6.22
CHEMBL140048 1 -
CHEMBL126931 1 -
CHEMBL341880 1 -
CHEMBL31871 HEPT 1 -
CHEMBL142098 1 -
CHEMBL356674 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL336237 IC50 = 15.0 nM 7.82
CHEMBL416107 IC50 = 30.0 nM 7.52
CHEMBL140532 IC50 = 100.0 nM 7.00
CHEMBL341931 IC50 = 400.0 nM 6.40
CHEMBL37067 IC50 = 400.0 nM 6.40
CHEMBL357409 IC50 = 600.0 nM 6.22
CHEMBL140048 IC50 > 4000.0 nM -
CHEMBL126931 IC50 > 4000.0 nM -
CHEMBL341880 IC50 > 4000.0 nM -
CHEMBL31871 HEPT IC50 > 6000.0 nM -
CHEMBL142098 IC50 > 10000.0 nM -
CHEMBL356674 IC50 > 10000.0 nM -