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Assay Detail

CHEMBL3602695

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

Binding
Inhibition of HIV-1 HXB2 gp41 N-terminal heptad repeat-mediated fusion between infected HL2/3 cells to target TZM-bl cells after 6 hrs by luciferase reporter gene assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Cell Type HL2/3
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Envelope glycoprotein gp160 (CHEMBL3520)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus type 1 group M subtype B (isolate HXB2)(HIV-1)

Publication

The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
Chong H, Qiu Z, Su Y, He Y.
J Med Chem (2015) 58 : 6378 -6388
PubMed 26256053 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.65 9.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3600949 1 9.47
CHEMBL529902 1 9.46
CHEMBL3600950 1 9.36
CHEMBL428607 1 9.08
CHEMBL411406 1 9.07
CHEMBL3600952 1 8.66
CHEMBL3600951 1 8.64
CHEMBL3600954 1 7.75
CHEMBL3600953 1 7.75
CHEMBL3600956 1 7.23
CHEMBL3600955 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3600949 IC50 = 0.34 nM 9.47
CHEMBL529902 IC50 = 0.35 nM 9.46
CHEMBL3600950 IC50 = 0.44 nM 9.36
CHEMBL428607 IC50 = 0.84 nM 9.08
CHEMBL411406 IC50 = 0.86 nM 9.07
CHEMBL3600952 IC50 = 2.18 nM 8.66
CHEMBL3600951 IC50 = 2.27 nM 8.64
CHEMBL3600954 IC50 = 17.7 nM 7.75
CHEMBL3600953 IC50 = 17.74 nM 7.75
CHEMBL3600956 IC50 = 58.79 nM 7.23
CHEMBL3600955 IC50 > 2250.0 nM -