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Assay Detail

CHEMBL3096027

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

Binding
Inhibition of HIV-1 gp41-mediated 6-helix bundle formation after 30 mins by sandwich ELISA
19
Total Activities
19
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Small molecule fusion inhibitors: design, synthesis and biological evaluation of (Z)-3-(5-(3-benzyl-4-oxo-2-thioxothiazolidinylidene)methyl)-N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrroles and related derivatives targeting HIV-1 gp41.
He XY, Lu L, Qiu J, Zou P, Yu F, Jiang XK, Li L, Jiang S, Liu S, Xie L.
Bioorg Med Chem (2013) 21 : 7539 -7548
PubMed 23673219 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.01 6.05
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3092871 1 6.05
CHEMBL3092878 1 5.75
CHEMBL3092872 1 5.75
CHEMBL3092877 1 5.68
CHEMBL3092874 1 5.58
CHEMBL3092876 1 5.11
CHEMBL3092875 1 5.04
CHEMBL3092870 1 4.99
CHEMBL3092867 1 4.92
CHEMBL3092868 1 4.90
CHEMBL3092869 1 4.73
CHEMBL3092879 1 4.68
CHEMBL3092880 1 4.65
CHEMBL3092882 1 4.46
CHEMBL214344 1 4.43
CHEMBL3092865 1 4.34
CHEMBL3092873 1 4.17
CHEMBL3092881 1 -
CHEMBL3092866 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3092871 IC50 = 900.0 nM 6.05
CHEMBL3092878 IC50 = 1800.0 nM 5.75
CHEMBL3092872 IC50 = 1800.0 nM 5.75
CHEMBL3092877 IC50 = 2100.0 nM 5.68
CHEMBL3092874 IC50 = 2600.0 nM 5.58
CHEMBL3092876 IC50 = 7800.0 nM 5.11
CHEMBL3092875 IC50 = 9200.0 nM 5.04
CHEMBL3092870 IC50 = 10300.0 nM 4.99
CHEMBL3092867 IC50 = 11900.0 nM 4.92
CHEMBL3092868 IC50 = 12500.0 nM 4.90
CHEMBL3092869 IC50 = 18800.0 nM 4.73
CHEMBL3092879 IC50 = 20800.0 nM 4.68
CHEMBL3092880 IC50 = 22600.0 nM 4.65
CHEMBL3092882 IC50 = 34300.0 nM 4.46
CHEMBL214344 IC50 = 37400.0 nM 4.43
CHEMBL3092865 IC50 = 45700.0 nM 4.34
CHEMBL3092873 IC50 = 68000.0 nM 4.17
CHEMBL3092881 IC50 - -
CHEMBL3092866 Inhibition - % -