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Assay Detail

CHEMBL643637

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

Binding
Inhibitory activity against [3H]WB-4101 binding to Alpha-1 adrenergic receptor in rat whole brain membrane
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
Klein JT, Davis L, Olsen GE, Wong GS, Huger FP, Smith CP, Petko WW, Cornfeldt M, Wilker JC, Blitzer RD, Landau E, Haroutunian V, Martin LL, Effland RC.
J Med Chem (1996) 39 : 570 -581
PubMed 8558529 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.64 6.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL154488 1 6.29
CHEMBL152842 1 5.92
CHEMBL435034 1 5.50
CHEMBL154541 1 5.48
CHEMBL29835 BESIPIRDINE 2.0 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL154488 IC50 = 510.0 nM 6.29
CHEMBL152842 IC50 = 1200.0 nM 5.92
CHEMBL435034 IC50 = 3200.0 nM 5.50
CHEMBL154541 IC50 = 3300.0 nM 5.48
CHEMBL29835 BESIPIRDINE IC50 = 10000.0 nM 5.00