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Assay Detail

CHEMBL1260087

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Functional
Antiviral activity against HIV1 NL4-3 infected in human Hut78 cells assessed as inhibition of viral replication in 50 % normal human serum
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Tissue Serum
Cell Type HuT78
Confidence 1 — Organism
Curated By Autocuration

Target

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

Publication

Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: selection of the scaffold.
Jones ED, Vandegraaff N, Le G, Choi N, Issa W, Macfarlane K, Thienthong N, Winfield LJ, Coates JA, Lu L, Li X, Feng X, Yu C, Rhodes DI, Deadman JJ.
Bioorg Med Chem Lett (2010) 20 : 5913 -5917
PubMed 20727748 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 7.14 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1258278 1 8.40
CHEMBL518520 RALTEGRAVIR POTASSIUM 4.0 1 8.15
CHEMBL1258045 1 7.75
CHEMBL1258162 1 7.40
CHEMBL1258046 1 7.37
CHEMBL1258163 1 7.37
CHEMBL1257819 1 7.30
CHEMBL1258277 1 7.21
CHEMBL1257935 1 7.16
CHEMBL1257936 1 6.80
CHEMBL1257696 1 6.23
CHEMBL1257575 1 5.85
CHEMBL1257818 1 5.81
CHEMBL1257580 1 -
CHEMBL1257576 1 -
CHEMBL1257697 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1258278 EC50 = 4.0 nM 8.40
CHEMBL518520 RALTEGRAVIR POTASSIUM EC50 = 7.1 nM 8.15
CHEMBL1258045 EC50 = 18.0 nM 7.75
CHEMBL1258162 EC50 = 40.0 nM 7.40
CHEMBL1258046 EC50 = 43.0 nM 7.37
CHEMBL1258163 EC50 = 43.0 nM 7.37
CHEMBL1257819 EC50 = 50.0 nM 7.30
CHEMBL1258277 EC50 = 61.5 nM 7.21
CHEMBL1257935 EC50 = 70.0 nM 7.16
CHEMBL1257936 EC50 = 158.0 nM 6.80
CHEMBL1257696 EC50 = 590.0 nM 6.23
CHEMBL1257575 EC50 = 1400.0 nM 5.85
CHEMBL1257818 EC50 = 1550.0 nM 5.81
CHEMBL1257580 EC50 - -
CHEMBL1257576 EC50 - -
CHEMBL1257697 EC50 - -