Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2214225

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

Binding
Inhibition of HIV1 capsid protein assembly using 5'-fluorescein-labeled (TG)25 oligonucleotide after 2 hrs by fluorometry-based capsid disassembly 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

Structural capsid protein (CHEMBL2366504)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Inhibition of HIV-1 capsid assembly: optimization of the antiviral potency by site selective modifications at N1, C2 and C16 of a 5-(5-furan-2-yl-pyrazol-1-yl)-1H-benzimidazole scaffold.
Tremblay M, Bonneau P, Bousquet Y, DeRoy P, Duan J, Duplessis M, Gagnon A, Garneau M, Goudreau N, Guse I, Hucke O, Kawai SH, Lemke CT, Mason SW, Simoneau B, Surprenant S, Titolo S, Yoakim C.
Bioorg Med Chem Lett (2012) 22 : 7512 -7517
PubMed 23122820 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.62 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2204005 1 7.39
CHEMBL2204007 1 7.31
CHEMBL2204004 1 7.26
CHEMBL2204006 1 7.25
CHEMBL2204002 1 7.06
CHEMBL2204003 1 6.92
CHEMBL2204016 1 6.77
CHEMBL2204001 1 6.55
CHEMBL2204013 1 6.44
CHEMBL2204000 1 6.39
CHEMBL2204014 1 6.10
CHEMBL2204015 1 6.08
CHEMBL2204012 1 6.00
CHEMBL2204011 1 5.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2204005 IC50 = 41.0 nM 7.39
CHEMBL2204007 IC50 = 49.0 nM 7.31
CHEMBL2204004 IC50 = 55.0 nM 7.26
CHEMBL2204006 IC50 = 56.0 nM 7.25
CHEMBL2204002 IC50 = 88.0 nM 7.06
CHEMBL2204003 IC50 = 120.0 nM 6.92
CHEMBL2204016 IC50 = 170.0 nM 6.77
CHEMBL2204001 IC50 = 280.0 nM 6.55
CHEMBL2204013 IC50 = 360.0 nM 6.44
CHEMBL2204000 IC50 = 410.0 nM 6.39
CHEMBL2204014 IC50 = 790.0 nM 6.10
CHEMBL2204015 IC50 = 830.0 nM 6.08
CHEMBL2204012 IC50 = 1000.0 nM 6.00
CHEMBL2204011 IC50 = 6000.0 nM 5.22