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Assay Detail

CHEMBL2162206

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Binding
Inhibition of HIV-1 reverse transcriptase using Poly(rA).p(dT) (12 to 18) as substrate after 30 mins by single point PCR assay
14
Total Activities
14
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 14 4.79 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284328 HOMIDIUM BROMIDE 2.0 1 5.70
CHEMBL345124 PROPIDIUM 1 5.52
CHEMBL582355 1 4.70
CHEMBL1985453 ACRIDINE YELLOW 1 4.50
CHEMBL53463 DOXORUBICIN 4.0 1 4.28
CHEMBL2159004 1 4.03
CHEMBL178 DAUNORUBICIN 4.0 1 -
CHEMBL123 ELLIPTECINE 1 -
CHEMBL81880 ACRIDINE ORANGE 1 -
CHEMBL1554 DACTINOMYCIN 4.0 1 -
CHEMBL76954 1 -
CHEMBL2159005 1 -
CHEMBL2159006 1 -
CHEMBL2159007 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284328 HOMIDIUM BROMIDE IC50 = 2000.0 nM 5.70
CHEMBL345124 PROPIDIUM IC50 = 3000.0 nM 5.52
CHEMBL582355 IC50 = 20000.0 nM 4.70
CHEMBL1985453 ACRIDINE YELLOW IC50 = 32000.0 nM 4.50
CHEMBL53463 DOXORUBICIN IC50 = 52000.0 nM 4.28
CHEMBL2159004 IC50 = 93000.0 nM 4.03
CHEMBL178 DAUNORUBICIN IC50 = 139000.0 nM -
CHEMBL123 ELLIPTECINE IC50 = 182000.0 nM -
CHEMBL81880 ACRIDINE ORANGE IC50 = 200000.0 nM -
CHEMBL1554 DACTINOMYCIN IC50 = 270000.0 nM -
CHEMBL76954 IC50 - -
CHEMBL2159005 IC50 - -
CHEMBL2159006 IC50 - -
CHEMBL2159007 IC50 - -