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Assay Detail

CHEMBL1058997

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

Binding
Inhibition of HIV1 recombinant reverse transcriptase p66/p51 heterodimer in presence of Mg2+
12
Total Activities
12
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

RNase H active site inhibitors of human immunodeficiency virus type 1 reverse transcriptase: design, biochemical activity, and structural information.
Kirschberg TA, Balakrishnan M, Squires NH, Barnes T, Brendza KM, Chen X, Eisenberg EJ, Jin W, Kutty N, Leavitt S, Liclican A, Liu Q, Liu X, Mak J, Perry JK, Wang M, Watkins WJ, Lansdon EB.
J Med Chem (2009) 52 : 5781 -5784
PubMed 19791799 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 4.24 4.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL562080 1 4.32
CHEMBL572124 1 4.16
CHEMBL557770 1 -
CHEMBL16755 1 -
CHEMBL550937 BETA-THUJAPLICINOL 1 -
CHEMBL183852 1 -
CHEMBL559337 7-DESHYDROXYPYROGALLIN-4-CARBOXYLIC ACID 1 -
CHEMBL440562 1 -
CHEMBL204900 1 -
CHEMBL561881 1 -
CHEMBL551212 1 -
CHEMBL539211 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL562080 IC50 = 48000.0 nM 4.32
CHEMBL572124 IC50 = 70000.0 nM 4.16
CHEMBL557770 IC50 - -
CHEMBL16755 IC50 - -
CHEMBL550937 BETA-THUJAPLICINOL IC50 - -
CHEMBL183852 IC50 - -
CHEMBL559337 7-DESHYDROXYPYROGALLIN-4-CARBOXYLIC ACID IC50 - -
CHEMBL440562 IC50 > 100000.0 nM -
CHEMBL204900 IC50 > 100000.0 nM -
CHEMBL561881 IC50 > 100000.0 nM -
CHEMBL551212 IC50 > 100000.0 nM -
CHEMBL539211 IC50 - -