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Assay Detail

CHEMBL757789

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

Functional
Tested in vitro for anti HIV-1 activity against PBM cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type PBM
Confidence 1 — Organism
Curated By Expert

Target

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

Publication

Synthesis and biological evaluation of 2',3'-didehydro-2',3'- dideoxy-5-fluorocytidine (D4FC) analogues: discovery of carbocyclic nucleoside triphosphates with potent inhibitory activity against HIV-1 reverse transcriptase.
Shi J, McAtee JJ, Schlueter Wirtz S, Tharnish P, Juodawlkis A, Liotta DC, Schinazi RF.
J Med Chem (1999) 42 : 859 -867
PubMed 10072683 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 6.32 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129 ZIDOVUDINE 4.0 1 8.70
CHEMBL38700 ELVUCITABINE 2.0 1 7.47
CHEMBL109831 DEXELVUCITABINE 2.0 1 7.34
CHEMBL354904 1 7.25
CHEMBL171878 1 6.89
CHEMBL171286 1 6.82
CHEMBL169267 1 6.58
CHEMBL355081 1 6.00
CHEMBL2368322 1 5.12
CHEMBL355426 1 5.10
CHEMBL171444 1 5.09
CHEMBL168395 1 5.05
CHEMBL2368321 1 4.70
CHEMBL366529 1 -
CHEMBL169434 1 -
CHEMBL169277 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129 ZIDOVUDINE EC50 = 2.0 nM 8.70
CHEMBL38700 ELVUCITABINE EC50 = 34.0 nM 7.47
CHEMBL109831 DEXELVUCITABINE EC50 = 46.0 nM 7.34
CHEMBL354904 EC50 = 56.0 nM 7.25
CHEMBL171878 EC50 = 130.0 nM 6.89
CHEMBL171286 EC50 = 150.0 nM 6.82
CHEMBL169267 EC50 = 260.0 nM 6.58
CHEMBL355081 EC50 = 1000.0 nM 6.00
CHEMBL2368322 EC50 = 7500.0 nM 5.12
CHEMBL355426 EC50 = 7900.0 nM 5.10
CHEMBL171444 EC50 = 8200.0 nM 5.09
CHEMBL168395 EC50 = 9000.0 nM 5.05
CHEMBL2368321 EC50 = 20000.0 nM 4.70
CHEMBL366529 EC50 > 10000.0 nM -
CHEMBL169434 EC50 > 10000.0 nM -
CHEMBL169277 EC50 > 100000.0 nM -