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Assay Detail

CHEMBL4034152

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

Binding
Inhibition of full length HIV RT-RNase H activity using 18-nucleotide 3'-fluorescein-labeled RNA/5'-dabsyl-labeled DNA hybrid as substrate
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis, biological evaluation and molecular modeling of 2-Hydroxyisoquinoline-1,3-dione analogues as inhibitors of HIV reverse transcriptase associated ribonuclease H and polymerase.
Tang J, Vernekar SKV, Chen YL, Miller L, Huber AD, Myshakina N, Sarafianos SG, Parniak MA, Wang Z.
Eur J Med Chem (2017) 133 : 85 -96
PubMed 28384548 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 6.03 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4085574 1 6.70
CHEMBL4063160 1 6.70
CHEMBL4089954 1 6.70
CHEMBL4071684 1 6.70
CHEMBL4068016 1 6.52
CHEMBL4077477 1 6.22
CHEMBL4100254 1 6.09
CHEMBL4090239 1 6.08
CHEMBL1928102 1 6.05
CHEMBL4104588 1 6.00
CHEMBL1928103 1 5.96
CHEMBL1928107 1 5.96
CHEMBL1928110 1 5.96
CHEMBL1928097 1 5.92
CHEMBL1928112 1 5.92
CHEMBL4105411 1 5.89
CHEMBL1928115 1 5.89
CHEMBL4068900 1 5.85
CHEMBL4077002 1 5.85
CHEMBL1928105 1 5.85
CHEMBL461036 1 5.85
CHEMBL4089987 1 5.82
CHEMBL4101076 1 5.80
CHEMBL4070690 1 5.80
CHEMBL1928108 1 5.77
CHEMBL1928098 1 5.77
CHEMBL1928111 1 5.75
CHEMBL4075643 1 5.70
CHEMBL1928099 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4085574 IC50 = 200.0 nM 6.70
CHEMBL4063160 IC50 = 200.0 nM 6.70
CHEMBL4089954 IC50 = 200.0 nM 6.70
CHEMBL4071684 IC50 = 200.0 nM 6.70
CHEMBL4068016 IC50 = 300.0 nM 6.52
CHEMBL4077477 IC50 = 600.0 nM 6.22
CHEMBL4100254 IC50 = 820.0 nM 6.09
CHEMBL4090239 IC50 = 830.0 nM 6.08
CHEMBL1928102 IC50 = 900.0 nM 6.05
CHEMBL4104588 IC50 = 1000.0 nM 6.00
CHEMBL1928103 IC50 = 1100.0 nM 5.96
CHEMBL1928107 IC50 = 1100.0 nM 5.96
CHEMBL1928110 IC50 = 1100.0 nM 5.96
CHEMBL1928097 IC50 = 1200.0 nM 5.92
CHEMBL1928112 IC50 = 1200.0 nM 5.92
CHEMBL4105411 IC50 = 1300.0 nM 5.89
CHEMBL1928115 IC50 = 1300.0 nM 5.89
CHEMBL4068900 IC50 = 1400.0 nM 5.85
CHEMBL4077002 IC50 = 1400.0 nM 5.85
CHEMBL1928105 IC50 = 1400.0 nM 5.85
CHEMBL461036 IC50 = 1400.0 nM 5.85
CHEMBL4089987 IC50 = 1500.0 nM 5.82
CHEMBL4101076 IC50 = 1600.0 nM 5.80
CHEMBL4070690 IC50 = 1600.0 nM 5.80
CHEMBL1928108 IC50 = 1700.0 nM 5.77
CHEMBL1928098 IC50 = 1700.0 nM 5.77
CHEMBL1928111 IC50 = 1800.0 nM 5.75
CHEMBL4075643 IC50 = 2000.0 nM 5.70
CHEMBL1928099 IC50 = 2000.0 nM 5.70