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Assay Detail

CHEMBL1100192

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

Binding
Inhibition of fluorescein labeled Tat-peptide binding to HIV1 TAR RNA after 60 mins by FRET assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 3 — Cell-line / Tissue
Curated By Autocuration

Target

Nucleic Acid (CHEMBL345)
Type NUCLEIC-ACID

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
EC50 18 5.85 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1075826 1 6.75
CHEMBL1075831 1 6.75
CHEMBL1075824 1 6.62
CHEMBL1075822 1 6.52
CHEMBL1075823 1 6.44
CHEMBL1075821 1 6.35
CHEMBL1075621 1 6.33
CHEMBL1075825 1 6.30
CHEMBL1075815 1 5.79
CHEMBL1075830 1 5.77
CHEMBL1075832 1 5.71
CHEMBL1075829 1 5.53
CHEMBL1075817 1 5.49
CHEMBL1075833 1 5.48
CHEMBL1075816 1 5.41
CHEMBL1075828 1 5.05
CHEMBL1081399 1 4.86
CHEMBL1081563 1 4.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1075826 EC50 = 180.0 nM 6.75
CHEMBL1075831 EC50 = 180.0 nM 6.75
CHEMBL1075824 EC50 = 240.0 nM 6.62
CHEMBL1075822 EC50 = 300.0 nM 6.52
CHEMBL1075823 EC50 = 360.0 nM 6.44
CHEMBL1075821 EC50 = 450.0 nM 6.35
CHEMBL1075621 EC50 = 470.0 nM 6.33
CHEMBL1075825 EC50 = 500.0 nM 6.30
CHEMBL1075815 EC50 = 1630.0 nM 5.79
CHEMBL1075830 EC50 = 1700.0 nM 5.77
CHEMBL1075832 EC50 = 1930.0 nM 5.71
CHEMBL1075829 EC50 = 2960.0 nM 5.53
CHEMBL1075817 EC50 = 3260.0 nM 5.49
CHEMBL1075833 EC50 = 3320.0 nM 5.48
CHEMBL1075816 EC50 = 3940.0 nM 5.41
CHEMBL1075828 EC50 = 8900.0 nM 5.05
CHEMBL1081399 EC50 = 13890.0 nM 4.86
CHEMBL1081563 EC50 = 83800.0 nM 4.08