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Assay Detail

CHEMBL4337640

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

Binding
Inhibition of HIV1 gp41-induced cell-cell fusion between viral envelope expressing human HL2/3 cells to CD4/CCR5 receptor expressing TZM-bl cells after 6 hrs by luciferase assay
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

Envelope glycoprotein gp160 (CHEMBL1293311)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Design and Biological Evaluation of <i>m</i>-Xylene Thioether-Stapled Short Helical Peptides Targeting the HIV-1 gp41 Hexameric Coiled-Coil Fusion Complex.
Meng G, Pu J, Li Y, Han A, Tian Y, Xu W, Zhang T, Li X, Lu L, Wang C, Jiang S, Liu K.
J Med Chem (2019) 62 : 8773 -8783
PubMed 31513410 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 7.20 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4474461 1 8.14
CHEMBL4575700 1 7.97
CHEMBL4579547 1 7.90
CHEMBL4551966 1 7.65
CHEMBL4476199 1 7.47
CHEMBL4474236 1 7.02
CHEMBL4552479 1 6.91
CHEMBL4468452 1 6.89
CHEMBL4588738 1 6.88
CHEMBL4439355 1 6.87
CHEMBL4578610 1 6.83
CHEMBL4451659 1 6.78
CHEMBL4545032 1 6.77
CHEMBL4455835 1 6.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4474461 EC50 = 7.2 nM 8.14
CHEMBL4575700 EC50 = 10.6 nM 7.97
CHEMBL4579547 EC50 = 12.5 nM 7.90
CHEMBL4551966 EC50 = 22.4 nM 7.65
CHEMBL4476199 EC50 = 33.9 nM 7.47
CHEMBL4474236 EC50 = 95.7 nM 7.02
CHEMBL4552479 EC50 = 123.2 nM 6.91
CHEMBL4468452 EC50 = 127.3 nM 6.89
CHEMBL4588738 EC50 = 132.1 nM 6.88
CHEMBL4439355 EC50 = 136.4 nM 6.87
CHEMBL4578610 EC50 = 147.1 nM 6.83
CHEMBL4451659 EC50 = 166.2 nM 6.78
CHEMBL4545032 EC50 = 171.4 nM 6.77
CHEMBL4455835 EC50 = 213.6 nM 6.67