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Assay Detail

CHEMBL1100196

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

Binding
Inhibition of HIV1 TAT transfected to human HeLa cells assessed as decrease in luminescence after 48 hrs by duel luciferase reporter gene assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Protein Tat (CHEMBL4011)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus type 1 group M subtype B (isolate HXB2)(HIV-1)

Publication

Multivalent binding oligomers inhibit HIV Tat-TAR interaction critical for viral replication.
Wang D, Iera J, Baker H, Hogan P, Ptak R, Yang L, Hartman T, Buckheit RW, Desjardins A, Yang A, Legault P, Yedavalli V, Jeang KT, Appella DH.
Bioorg Med Chem Lett (2009) 19 : 6893 -6897
PubMed 19896372 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.98 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1075826 1 6.05
CHEMBL1075815 1 5.22
CHEMBL1075830 1 5.16
CHEMBL1075824 1 5.00
CHEMBL1075821 1 4.92
CHEMBL1075825 1 4.80
CHEMBL1081563 1 4.72
CHEMBL1075829 1 4.52
CHEMBL1075823 1 4.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1075826 IC50 = 900.0 nM 6.05
CHEMBL1075815 IC50 = 6000.0 nM 5.22
CHEMBL1075830 IC50 = 7000.0 nM 5.16
CHEMBL1075824 IC50 = 10000.0 nM 5.00
CHEMBL1075821 IC50 = 12000.0 nM 4.92
CHEMBL1075825 IC50 = 16000.0 nM 4.80
CHEMBL1081563 IC50 = 19000.0 nM 4.72
CHEMBL1075829 IC50 = 30000.0 nM 4.52
CHEMBL1075823 IC50 = 35000.0 nM 4.46