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Assay Detail

CHEMBL4479167

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

Functional
Antiviral activity against HIV1 infected in human PBMC assessed as inhibition of viral replication by measuring reverse transcriptase activity in cell supernatant preincubated with cells followed by viral infection measured after 7 days by radioactive incorporation polymerization assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Confidence 1 — Organism
Curated By Autocuration

Target

Human immunodeficiency virus 1 (CHEMBL378)
Type ORGANISM
Organism Human immunodeficiency virus 1

Publication

Reduction Sensitive Lipid Conjugates of Tenofovir: Synthesis, Stability, and Antiviral Activity.
Giesler KE, Marengo J, Liotta DC.
J Med Chem (2016) 59 : 7097 -7110
PubMed 27405794 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 24 7.12 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4591641 1 9.30
CHEMBL4559882 1 9.22
CHEMBL4574633 1 9.19
CHEMBL4522332 1 8.52
CHEMBL1486 TENOFOVIR DISOPROXIL FUMARATE 4.0 1 8.34
CHEMBL4526488 1 8.30
CHEMBL4530614 1 7.75
CHEMBL515564 TENOFOVIR EXALIDEX 2.0 1 7.70
CHEMBL4581747 1 7.58
CHEMBL4540957 1 7.31
CHEMBL4535399 1 7.07
CHEMBL4547349 1 6.85
CHEMBL4583653 1 6.72
CHEMBL4582521 1 6.72
CHEMBL4532461 1 6.67
CHEMBL483 TENOFOVIR ANHYDROUS 3.0 1 6.50
CHEMBL4529939 1 6.48
CHEMBL4558053 1 6.46
CHEMBL4536590 1 6.46
CHEMBL4581778 1 6.04
CHEMBL4572472 1 5.93
CHEMBL4590974 1 5.79
CHEMBL4578738 1 5.20
CHEMBL4557355 1 4.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4591641 EC50 = 0.5 nM 9.30
CHEMBL4559882 EC50 = 0.6 nM 9.22
CHEMBL4574633 EC50 = 0.65 nM 9.19
CHEMBL4522332 EC50 = 3.0 nM 8.52
CHEMBL1486 TENOFOVIR DISOPROXIL FUMARATE EC50 = 4.6 nM 8.34
CHEMBL4526488 EC50 = 5.0 nM 8.30
CHEMBL4530614 EC50 = 18.0 nM 7.75
CHEMBL515564 TENOFOVIR EXALIDEX EC50 = 20.0 nM 7.70
CHEMBL4581747 EC50 = 26.0 nM 7.58
CHEMBL4540957 EC50 = 49.0 nM 7.31
CHEMBL4535399 EC50 = 85.0 nM 7.07
CHEMBL4547349 EC50 = 140.0 nM 6.85
CHEMBL4583653 EC50 = 189.0 nM 6.72
CHEMBL4582521 EC50 = 190.0 nM 6.72
CHEMBL4532461 EC50 = 216.0 nM 6.67
CHEMBL483 TENOFOVIR ANHYDROUS EC50 = 319.0 nM 6.50
CHEMBL4529939 EC50 = 331.0 nM 6.48
CHEMBL4558053 EC50 = 349.0 nM 6.46
CHEMBL4536590 EC50 = 349.0 nM 6.46
CHEMBL4581778 EC50 = 911.0 nM 6.04
CHEMBL4572472 EC50 = 1180.0 nM 5.93
CHEMBL4590974 EC50 = 1610.0 nM 5.79
CHEMBL4578738 EC50 = 6320.0 nM 5.20
CHEMBL4557355 EC50 = 18600.0 nM 4.73