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Assay Detail

CHEMBL873878

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

Functional
Concentration required to inhibit the entry of HIV-1 reporter virus [ADA] into U-87 cells
15
Total Activities
15
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

Discovery of 4-[(Z)-(4-bromophenyl)- (ethoxyimino)methyl]-1'-[(2,4-dimethyl-3- pyridinyl)carbonyl]-4'-methyl-1,4'- bipiperidine N-oxide (SCH 351125): an orally bioavailable human CCR5 antagonist for the treatment of HIV infection.
Palani A, Shapiro S, Clader JW, Greenlee WJ, Cox K, Strizki J, Endres M, Baroudy BM.
J Med Chem (2001) 44 : 3339 -3342
PubMed 11585437 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.72 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL105821 1 9.70
CHEMBL109158 1 9.30
CHEMBL323172 1 9.30
CHEMBL78535 ANCRIVIROC 2.0 1 9.22
CHEMBL105784 1 9.22
CHEMBL112686 1 8.92
CHEMBL324643 1 8.89
CHEMBL2111747 1 8.82
CHEMBL112760 1 8.55
CHEMBL106767 1 8.40
CHEMBL292625 1 8.26
CHEMBL106098 1 8.25
CHEMBL331140 1 8.04
CHEMBL106247 1 8.00
CHEMBL106209 1 7.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL105821 IC50 = 0.2 nM 9.70
CHEMBL109158 IC50 = 0.5 nM 9.30
CHEMBL323172 IC50 = 0.5 nM 9.30
CHEMBL78535 ANCRIVIROC IC50 = 0.6 nM 9.22
CHEMBL105784 IC50 = 0.6 nM 9.22
CHEMBL112686 IC50 = 1.2 nM 8.92
CHEMBL324643 IC50 = 1.3 nM 8.89
CHEMBL2111747 IC50 = 1.5 nM 8.82
CHEMBL112760 IC50 = 2.8 nM 8.55
CHEMBL106767 IC50 = 4.0 nM 8.40
CHEMBL292625 IC50 = 5.5 nM 8.26
CHEMBL106098 IC50 = 5.6 nM 8.25
CHEMBL331140 IC50 = 9.2 nM 8.04
CHEMBL106247 IC50 = 10.0 nM 8.00
CHEMBL106209 IC50 = 13.0 nM 7.89