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Assay Detail

CHEMBL2162208

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

Binding
Inhibition of HIV-1 reverse transcriptase using 0.05 ug/mL of Poly(rA).p(dT) (12 to 18) as substrate after 30 mins by single point PCR assay
8
Total Activities
8
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

Human immunodeficiency virus type 1 reverse transcriptase (CHEMBL247)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Inhibition of therapeutically important polymerases with high affinity bis-intercalators.
Jain N, Francis S, Friedman SH.
Bioorg Med Chem Lett (2012) 22 : 4844 -4848
PubMed 22695131 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.48 8.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2159008 1 8.31
CHEMBL2159009 1 8.04
CHEMBL2159010 1 7.98
CHEMBL2159003 1 7.97
CHEMBL2159011 1 7.65
CHEMBL2159012 1 7.51
CHEMBL2159014 ACRIDINE DIMER 1 6.66
CHEMBL48166 HOMIDIUM 2.0 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2159008 IC50 = 4.9 nM 8.31
CHEMBL2159009 IC50 = 9.2 nM 8.04
CHEMBL2159010 IC50 = 10.5 nM 7.98
CHEMBL2159003 IC50 = 10.8 nM 7.97
CHEMBL2159011 IC50 = 22.3 nM 7.65
CHEMBL2159012 IC50 = 30.7 nM 7.51
CHEMBL2159014 ACRIDINE DIMER IC50 = 220.0 nM 6.66
CHEMBL48166 HOMIDIUM IC50 = 2100.0 nM 5.68