Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1930242

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

Functional
Antiviral activity against R5 tropic Human immunodeficiency virus 1 BAL infected in human PBMC cells assessed as reduction in viral replication by p24 detection based ELISA
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type PBMC
Confidence 1 — Organism
Curated By Autocuration

Target

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

Publication

Design and synthesis of pyridin-2-ylmethylaminopiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication.
Skerlj R, Bridger G, Zhou Y, Bourque E, McEachern E, Langille J, Harwig C, Veale D, Yang W, Li T, Zhu Y, Bey M, Baird I, Sartori M, Metz M, Mosi R, Nelson K, Bodart V, Wong R, Fricker S, Mac Farland R, Huskens D, Schols D.
Bioorg Med Chem Lett (2011) 21 : 6950 -6954
PubMed 22033460 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 7.31 9.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1926899 1 9.02
CHEMBL1926884 1 9.00
CHEMBL1926886 1 8.70
CHEMBL1926900 1 8.70
CHEMBL1926893 1 8.66
CHEMBL1926896 1 8.66
CHEMBL1926904 1 8.48
CHEMBL1927009 1 8.46
CHEMBL1927010 1 8.44
CHEMBL1927008 1 8.41
CHEMBL1926885 1 7.85
CHEMBL1926894 1 7.72
CHEMBL1926891 1 7.65
CHEMBL1926902 1 7.64
CHEMBL1926898 1 7.59
CHEMBL1926897 1 7.53
CHEMBL1926901 1 7.49
CHEMBL1926874 1 7.23
CHEMBL1926883 1 7.05
CHEMBL1926878 1 7.02
CHEMBL1926872 1 6.96
CHEMBL1926876 1 6.75
CHEMBL1762313 1 6.66
CHEMBL1926887 1 6.42
CHEMBL1926875 1 6.42
CHEMBL1926880 1 6.40
CHEMBL1926890 1 5.98
CHEMBL1926888 1 5.74
CHEMBL1926873 1 5.66
CHEMBL1926882 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1926899 IC50 = 0.96 nM 9.02
CHEMBL1926884 IC50 = 1.0 nM 9.00
CHEMBL1926886 IC50 = 2.0 nM 8.70
CHEMBL1926900 IC50 = 2.0 nM 8.70
CHEMBL1926893 IC50 = 2.2 nM 8.66
CHEMBL1926896 IC50 = 2.2 nM 8.66
CHEMBL1926904 IC50 = 3.3 nM 8.48
CHEMBL1927009 IC50 = 3.5 nM 8.46
CHEMBL1927010 IC50 = 3.6 nM 8.44
CHEMBL1927008 IC50 = 3.9 nM 8.41
CHEMBL1926885 IC50 = 14.0 nM 7.85
CHEMBL1926894 IC50 = 18.9 nM 7.72
CHEMBL1926891 IC50 = 22.3 nM 7.65
CHEMBL1926902 IC50 = 23.1 nM 7.64
CHEMBL1926898 IC50 = 25.4 nM 7.59
CHEMBL1926897 IC50 = 29.6 nM 7.53
CHEMBL1926901 IC50 = 32.3 nM 7.49
CHEMBL1926874 IC50 = 59.0 nM 7.23
CHEMBL1926883 IC50 = 89.0 nM 7.05
CHEMBL1926878 IC50 = 96.0 nM 7.02
CHEMBL1926872 IC50 = 110.0 nM 6.96
CHEMBL1926876 IC50 = 177.0 nM 6.75
CHEMBL1762313 IC50 = 220.0 nM 6.66
CHEMBL1926887 IC50 = 376.0 nM 6.42
CHEMBL1926875 IC50 = 380.0 nM 6.42
CHEMBL1926880 IC50 = 400.0 nM 6.40
CHEMBL1926890 IC50 = 1044.0 nM 5.98
CHEMBL1926888 IC50 = 1830.0 nM 5.74
CHEMBL1926873 IC50 = 2170.0 nM 5.66
CHEMBL1926882 IC50 = 2880.0 nM 5.54
CHEMBL1926877 IC50 = 9633.0 nM 5.02
CHEMBL1926889 IC50 = 11479.0 nM 4.94
CHEMBL1926881 IC50 > 1300.0 nM -
CHEMBL1926879 IC50 > 1250.0 nM -
CHEMBL1926903 IC50 > 32149.0 nM -