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Assay Detail

CHEMBL647024

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

Binding
Binding affinity towards Alpha-1 adrenergic receptor in rat cerebral cortex membranes using [3H]prazosin as radioligand
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and synthesis of S-(-)-2-[[4-(napht-1-yl)piperazin-1-yl]methyl]-1,4-dioxoperhydropyrrolo[1,2-a]pyrazine (CSP-2503) using computational simulation. A 5-HT1A receptor agonist.
López-Rodríguez ML, Morcillo MJ, Fernández E, Benhamú B, Tejada I, Ayala D, Viso A, Olivella M, Pardo L, Delgado M, Manzanares J, Fuentes JA.
Bioorg Med Chem Lett (2003) 13 : 1429 -1432
PubMed 12668005 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.10 7.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL33150 1 7.19
CHEMBL33258 1 5.00
CHEMBL445055 1 -
CHEMBL430914 1 -
CHEMBL285066 1 -
CHEMBL34287 1 -
CHEMBL2113340 1 -
CHEMBL2113339 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL33150 Ki = 64.9 nM 7.19
CHEMBL33258 Ki = 10000.0 nM 5.00
CHEMBL445055 Ki > 1000.0 nM -
CHEMBL430914 Ki > 1000.0 nM -
CHEMBL285066 Ki > 1000.0 nM -
CHEMBL34287 Ki > 1000.0 nM -
CHEMBL2113340 Ki > 1000.0 nM -
CHEMBL2113339 Ki > 1000.0 nM -