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Assay Detail

CHEMBL953189

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

Functional
Antiviral activity against HIV1 3B in presence of 10% fetal calf serum
17
Total Activities
17
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

Combination of non-natural D-amino acid derivatives and allophenylnorstatine-dimethylthioproline scaffold in HIV protease inhibitors have high efficacy in mutant HIV.
Nakatani S, Hidaka K, Ami E, Nakahara K, Sato A, Nguyen JT, Hamada Y, Hori Y, Ohnishi N, Nagai A, Kimura T, Hayashi Y, Kiso Y.
J Med Chem (2008) 51 : 2992 -3004
PubMed 18426195 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 7.82 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL509787 1 8.40
CHEMBL449552 1 8.10
CHEMBL455816 1 8.03
CHEMBL449945 1 7.92
CHEMBL230484 1 7.89
CHEMBL502912 1 7.85
CHEMBL448032 1 7.85
CHEMBL504713 1 7.85
CHEMBL449213 1 7.80
CHEMBL448021 1 7.75
CHEMBL503829 1 7.70
CHEMBL449836 1 7.70
CHEMBL584 NELFINAVIR 4.0 1 7.68
CHEMBL414640 1 7.66
CHEMBL163 RITONAVIR 4.0 1 7.62
CHEMBL505525 1 7.60
CHEMBL462726 1 7.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL509787 EC50 = 4.0 nM 8.40
CHEMBL449552 EC50 = 8.0 nM 8.10
CHEMBL455816 EC50 = 9.4 nM 8.03
CHEMBL449945 EC50 = 12.0 nM 7.92
CHEMBL230484 EC50 = 13.0 nM 7.89
CHEMBL502912 EC50 = 14.0 nM 7.85
CHEMBL448032 EC50 = 14.0 nM 7.85
CHEMBL504713 EC50 = 14.0 nM 7.85
CHEMBL449213 EC50 = 16.0 nM 7.80
CHEMBL448021 EC50 = 18.0 nM 7.75
CHEMBL503829 EC50 = 20.0 nM 7.70
CHEMBL449836 EC50 = 20.0 nM 7.70
CHEMBL584 NELFINAVIR EC50 = 21.0 nM 7.68
CHEMBL414640 EC50 = 22.0 nM 7.66
CHEMBL163 RITONAVIR EC50 = 24.0 nM 7.62
CHEMBL505525 EC50 = 25.0 nM 7.60
CHEMBL462726 EC50 = 27.0 nM 7.57