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Assay Detail

CHEMBL1034082

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

Functional
Antiviral activity against HIV1 3a infected human MT2 cells assessed as inhibition of viral-induced cytopathic effect after 3 days by XTT assay
9
Total Activities
9
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 Autocuration

Target

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

Publication

Design, synthesis, and anti-HIV activity of 4'-modified carbocyclic nucleoside phosphonate reverse transcriptase inhibitors.
Boojamra CG, Parrish JP, Sperandio D, Gao Y, Petrakovsky OV, Lee SK, Markevitch DY, Vela JE, Laflamme G, Chen JM, Ray AS, Barron AC, Sparacino ML, Desai MC, Kim CU, Cihlar T, Mackman RL.
Bioorg Med Chem (2009) 17 : 1739 -1746
PubMed 19179082 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 5.56 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129 ZIDOVUDINE 4.0 1 6.80
CHEMBL1380 ABACAVIR 4.0 1 6.50
CHEMBL472269 1 6.09
CHEMBL420843 1 5.68
CHEMBL483 TENOFOVIR ANHYDROUS 3.0 1 5.44
CHEMBL252036 GS-9148 -1.0 1 4.92
CHEMBL525256 1 4.80
CHEMBL428083 1 4.28
CHEMBL471431 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129 ZIDOVUDINE EC50 = 160.0 nM 6.80
CHEMBL1380 ABACAVIR EC50 = 320.0 nM 6.50
CHEMBL472269 EC50 = 810.0 nM 6.09
CHEMBL420843 EC50 = 2100.0 nM 5.68
CHEMBL483 TENOFOVIR ANHYDROUS EC50 = 3600.0 nM 5.44
CHEMBL252036 GS-9148 EC50 = 12000.0 nM 4.92
CHEMBL525256 EC50 = 16000.0 nM 4.80
CHEMBL428083 EC50 = 52000.0 nM 4.28
CHEMBL471431 EC50 = 244000.0 nM -