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Assay Detail

CHEMBL798324

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

Binding
Inhibitory activity against Y188H mutant HIV-1 reverse transcriptase
2
Total Activities
2
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

(-)-6-Chloro-2-[(1-furo[2, 3-c]pyridin-5-ylethyl)thio]-4-pyrimidinamine, PNU-142721, a new broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitor.
Wishka DG, Graber DR, Kopta LA, Olmsted RA, Friis JM, Hosley JD, Adams WJ, Seest EP, Castle TM, Dolak LA, Keiser BJ, Yagi Y, Jeganathan A, Schlachter ST, Murphy MJ, Cleek GJ, Nugent RA, Poppe SM, Swaney SM, Han F, Watt W, White WL, Poel TJ, Thomas RC, Morris J.
J Med Chem (1998) 41 : 1357 -1360
PubMed 9554867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.19 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL280752 1 7.26
CHEMBL280541 1 7.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL280752 IC50 = 55.0 nM 7.26
CHEMBL280541 IC50 = 77.0 nM 7.11