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Assay Detail

CHEMBL3418256

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

Binding
Inhibition of Moloney murine leukemia virus reverse transcriptase polymerase activity using Td100/Pd18 DNA-DNA substrate incubated for 30 mins by fluorescence assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Moloney murine leukemia virus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Gag-Pol polyprotein (CHEMBL3562)
Type SINGLE PROTEIN
Organism Moloney murine leukemia virus isolate Shinnick

Publication

Design, synthesis, biochemical, and antiviral evaluations of C6 benzyl and C6 biarylmethyl substituted 2-hydroxylisoquinoline-1,3-diones: dual inhibition against HIV reverse transcriptase-associated RNase H and polymerase with antiviral activities.
Vernekar SK, Liu Z, Nagy E, Miller L, Kirby KA, Wilson DJ, Kankanala J, Sarafianos SG, Parniak MA, Wang Z.
J Med Chem (2015) 58 : 651 -664
PubMed 25522204 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.25 5.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3414871 1 5.62
CHEMBL3414876 1 5.55
CHEMBL3414864 1 5.51
CHEMBL3414857 1 5.50
CHEMBL3414870 1 5.41
CHEMBL3414862 1 5.16
CHEMBL3414860 1 5.15
CHEMBL3414868 1 5.07
CHEMBL3414867 1 4.96
CHEMBL3414869 1 4.96
CHEMBL3414865 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3414871 IC50 = 2400.0 nM 5.62
CHEMBL3414876 IC50 = 2800.0 nM 5.55
CHEMBL3414864 IC50 = 3100.0 nM 5.51
CHEMBL3414857 IC50 = 3200.0 nM 5.50
CHEMBL3414870 IC50 = 3900.0 nM 5.41
CHEMBL3414862 IC50 = 6900.0 nM 5.16
CHEMBL3414860 IC50 = 7100.0 nM 5.15
CHEMBL3414868 IC50 = 8500.0 nM 5.07
CHEMBL3414867 IC50 = 11000.0 nM 4.96
CHEMBL3414869 IC50 = 11000.0 nM 4.96
CHEMBL3414865 IC50 = 13000.0 nM 4.89