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Assay Detail

CHEMBL815090

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

Functional
Inhibition of HIV-1 (ADA) entry into U-87 (human glioblastoma) 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 U-87
Confidence 1 — Organism
Curated By Expert

Target

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

Publication

Oximino-piperidino-piperidine-based CCR5 antagonists. Part 2: synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides.
Palani A, Shapiro S, Clader JW, Greenlee WJ, Vice S, McCombie S, Cox K, Strizki J, Baroudy BM.
Bioorg Med Chem Lett (2003) 13 : 709 -712
PubMed 12639564 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 9.22 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL343520 1 9.89
CHEMBL164484 1 9.82
CHEMBL140552 1 9.59
CHEMBL140912 1 9.55
CHEMBL141683 1 9.46
CHEMBL351625 1 9.44
CHEMBL161664 1 9.40
CHEMBL82301 VICRIVIROC 3.0 1 9.22
CHEMBL350563 1 9.16
CHEMBL140390 1 9.05
CHEMBL335120 1 9.03
CHEMBL349008 1 8.98
CHEMBL341758 1 8.93
CHEMBL162880 1 8.91
CHEMBL161587 1 8.74
CHEMBL141201 1 8.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL343520 IC50 = 0.13 nM 9.89
CHEMBL164484 IC50 = 0.15 nM 9.82
CHEMBL140552 IC50 = 0.26 nM 9.59
CHEMBL140912 IC50 = 0.28 nM 9.55
CHEMBL141683 IC50 = 0.35 nM 9.46
CHEMBL351625 IC50 = 0.36 nM 9.44
CHEMBL161664 IC50 = 0.4 nM 9.40
CHEMBL82301 VICRIVIROC IC50 = 0.6 nM 9.22
CHEMBL350563 IC50 = 0.69 nM 9.16
CHEMBL140390 IC50 = 0.89 nM 9.05
CHEMBL335120 IC50 = 0.93 nM 9.03
CHEMBL349008 IC50 = 1.04 nM 8.98
CHEMBL341758 IC50 = 1.17 nM 8.93
CHEMBL162880 IC50 = 1.24 nM 8.91
CHEMBL161587 IC50 = 1.83 nM 8.74
CHEMBL141201 IC50 = 3.8 nM 8.42