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Assay Detail

CHEMBL950150

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Binding
Inhibition of HIV1 reverse transcriptase
8
Total Activities
8
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

Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
Cullen MD, Cheung YF, Houslay MD, Hartman TL, Watson KM, Buckheit RW, Pannecouque C, De Clercq E, Cushman M.
Bioorg Med Chem Lett (2008) 18 : 1530 -1533
PubMed 18222088 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.90 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL226735 1 7.70
CHEMBL57 NEVIRAPINE 4.0 1 7.08
CHEMBL107200 1 6.52
CHEMBL256906 1 6.30
CHEMBL110359 1 -
CHEMBL130984 1 -
CHEMBL110175 1 -
CHEMBL63 ROLIPRAM 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL226735 IC50 = 20.0 nM 7.70
CHEMBL57 NEVIRAPINE IC50 = 84.0 nM 7.08
CHEMBL107200 IC50 = 300.0 nM 6.52
CHEMBL256906 IC50 = 500.0 nM 6.30
CHEMBL110359 IC50 - -
CHEMBL130984 IC50 > 100000.0 nM -
CHEMBL110175 IC50 > 100000.0 nM -
CHEMBL63 ROLIPRAM IC50 - -