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Assay Detail

CHEMBL655577

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

Functional
Concentration required to protect CEM/0 cells against the cytopathicity of HIV-1 by 50%
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type CEM/0
Confidence 1 — Organism
Curated By Expert

Target

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

Publication

Design and synthesis of lipophilic phosphoramidate d4T-MP prodrugs expressing high potency against HIV in cell culture: structural determinants for in vitro activity and QSAR.
Siddiqui AQ, McGuigan C, Ballatore C, Zuccotto F, Gilbert IH, De Clercq E, Balzarini J.
J Med Chem (1999) 42 : 4122 -4128
PubMed 10514282 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 7.52 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3349838 1 8.30
CHEMBL3349834 1 8.10
CHEMBL320833 STAMPIDINE 1 8.05
CHEMBL3349831 1 8.00
CHEMBL3349837 1 7.89
CHEMBL3350117 1 7.89
CHEMBL3349843 1 7.85
CHEMBL3349832 1 7.82
CHEMBL3349839 1 7.80
CHEMBL3349830 1 7.75
CHEMBL3349846 1 7.75
CHEMBL3349842 1 7.60
CHEMBL3349835 1 7.60
CHEMBL3349845 1 7.40
CHEMBL3349836 1 7.28
CHEMBL323261 1 7.24
CHEMBL107184 1 7.12
CHEMBL3349844 1 7.10
CHEMBL3349841 1 6.96
CHEMBL3349833 1 6.89
CHEMBL3349840 1 6.82
CHEMBL991 STAVUDINE 4.0 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3349838 EC50 = 5.0 nM 8.30
CHEMBL3349834 EC50 = 8.0 nM 8.10
CHEMBL320833 STAMPIDINE EC50 = 9.0 nM 8.05
CHEMBL3349831 EC50 = 10.0 nM 8.00
CHEMBL3349837 EC50 = 13.0 nM 7.89
CHEMBL3350117 EC50 = 13.0 nM 7.89
CHEMBL3349843 EC50 = 14.0 nM 7.85
CHEMBL3349832 EC50 = 15.0 nM 7.82
CHEMBL3349839 EC50 = 16.0 nM 7.80
CHEMBL3349830 EC50 = 18.0 nM 7.75
CHEMBL3349846 EC50 = 18.0 nM 7.75
CHEMBL3349842 EC50 = 25.0 nM 7.60
CHEMBL3349835 EC50 = 25.0 nM 7.60
CHEMBL3349845 EC50 = 40.0 nM 7.40
CHEMBL3349836 EC50 = 53.0 nM 7.28
CHEMBL323261 EC50 = 57.0 nM 7.24
CHEMBL107184 EC50 = 75.0 nM 7.12
CHEMBL3349844 EC50 = 80.0 nM 7.10
CHEMBL3349841 EC50 = 110.0 nM 6.96
CHEMBL3349833 EC50 = 130.0 nM 6.89
CHEMBL3349840 EC50 = 150.0 nM 6.82
CHEMBL991 STAVUDINE EC50 = 651.0 nM 6.19