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Assay Detail

CHEMBL645247

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

Binding
Displacement of [3H]prazosin at alpha-1 adrenergic receptor in rat brain cortices (n=1)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Subtype-selective N-methyl-D-aspartate receptor antagonists: synthesis and biological evaluation of 1-(heteroarylalkynyl)-4-benzylpiperidines.
Wright JL, Gregory TF, Kesten SR, Boxer PA, Serpa KA, Meltzer LT, Wise LD, Espitia SA, Konkoy CS, Whittemore ER, Woodward RM.
J Med Chem (2000) 43 : 3408 -3419
PubMed 10978188 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.45 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL117260 1 6.30
CHEMBL19636 1 6.16
CHEMBL19506 1 5.92
CHEMBL419399 1 5.51
CHEMBL325825 1 5.24
CHEMBL326568 1 4.77
CHEMBL326742 1 4.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL117260 IC50 = 500.0 nM 6.30
CHEMBL19636 IC50 = 700.0 nM 6.16
CHEMBL19506 IC50 = 1200.0 nM 5.92
CHEMBL419399 IC50 = 3100.0 nM 5.51
CHEMBL325825 IC50 = 5800.0 nM 5.24
CHEMBL326568 IC50 = 17000.0 nM 4.77
CHEMBL326742 IC50 = 55000.0 nM 4.26