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Assay Detail

CHEMBL906564

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

Functional
Inhibition of virus-induced cytopathic effect in wild type HIV 3a infected MT2 cells after 5 days
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type MT2
Confidence 1 — Organism
Curated By Intermediate

Target

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

Publication

Synthesis, anti-HIV activity, and resistance profile of thymidine phosphonomethoxy nucleosides and their bis-isopropyloxymethylcarbonyl (bisPOC) prodrugs.
Mackman RL, Zhang L, Prasad V, Boojamra CG, Douglas J, Grant D, Hui H, Kim CU, Laflamme G, Parrish J, Stoycheva AD, Swaminathan S, Wang K, Cihlar T.
Bioorg Med Chem (2007) 15 : 5519 -5528
PubMed 17562366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 5.81 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1486 TENOFOVIR DISOPROXIL FUMARATE 4.0 1 7.82
CHEMBL129 ZIDOVUDINE 4.0 1 6.80
CHEMBL373954 1 6.04
CHEMBL229283 1 5.89
CHEMBL483 TENOFOVIR ANHYDROUS 3.0 1 5.44
CHEMBL991 STAVUDINE 4.0 1 5.32
CHEMBL485652 STAVUDINE TRIPHOSPHATE -1.0 1 4.58
CHEMBL122885 1 4.58
CHEMBL229284 1 -
CHEMBL229111 1 -
CHEMBL229987 1 -
CHEMBL444314 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1486 TENOFOVIR DISOPROXIL FUMARATE EC50 = 15.0 nM 7.82
CHEMBL129 ZIDOVUDINE EC50 = 160.0 nM 6.80
CHEMBL373954 EC50 = 910.0 nM 6.04
CHEMBL229283 EC50 = 1300.0 nM 5.89
CHEMBL483 TENOFOVIR ANHYDROUS EC50 = 3600.0 nM 5.44
CHEMBL991 STAVUDINE EC50 = 4800.0 nM 5.32
CHEMBL485652 STAVUDINE TRIPHOSPHATE EC50 = 26000.0 nM 4.58
CHEMBL122885 EC50 = 26000.0 nM 4.58
CHEMBL229284 EC50 > 200000.0 nM -
CHEMBL229111 EC50 > 200000.0 nM -
CHEMBL229987 EC50 > 200000.0 nM -
CHEMBL444314 EC50 > 200000.0 nM -