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Assay Detail

CHEMBL3057585

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

Binding
Inhibition of RNA-dependent DNA polymerase activity of Human immunodeficiency virus 1 recombinant reverse transcriptase expressed in Escherichia coli using poly(rA)oligo(dT) template primer after 30 min
7
Total Activities
7
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

Design, synthesis, and biological evaluation of new 3-hydroxy-2-oxo-3-trifluoromethylindole as potential HIV-1 reverse transcriptase inhibitors
Boechat N, Kover WB, Bastos MM, Romeiro NC, Silva ASC, Santos FC, Valverde AL, Azevedo MLG, Wollinger W, Souza TML, de Souza SLO, de Frugulhetti ICPP
Med Chem Res (2006) 15 : 492 -510
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.72 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL223228 EFAVIRENZ 4.0 1 7.40
CHEMBL57 NEVIRAPINE 4.0 1 6.30
CHEMBL2262683 1 5.47
CHEMBL2262682 1 5.44
CHEMBL84383 1 5.22
CHEMBL2262681 1 5.15
CHEMBL2262684 1 5.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL223228 EFAVIRENZ IC50 = 40.0 nM 7.40
CHEMBL57 NEVIRAPINE IC50 = 500.0 nM 6.30
CHEMBL2262683 IC50 = 3410.0 nM 5.47
CHEMBL2262682 IC50 = 3610.0 nM 5.44
CHEMBL84383 IC50 = 6070.0 nM 5.22
CHEMBL2262681 IC50 = 7100.0 nM 5.15
CHEMBL2262684 IC50 = 8370.0 nM 5.08