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Assay Detail

CHEMBL616054

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

Binding
Binding affinity towards 5-HT 1A receptor in rat cerebral cortex membranes using [3H]8-OH-DPAT 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 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
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 8.22 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL33150 1 8.62
CHEMBL33258 1 8.39
CHEMBL285066 1 8.39
CHEMBL445055 1 8.25
CHEMBL2113339 1 8.21
CHEMBL34287 1 8.03
CHEMBL430914 1 7.98
CHEMBL2113340 1 7.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL33150 Ki = 2.4 nM 8.62
CHEMBL33258 Ki = 4.1 nM 8.39
CHEMBL285066 Ki = 4.1 nM 8.39
CHEMBL445055 Ki = 5.6 nM 8.25
CHEMBL2113339 Ki = 6.1 nM 8.21
CHEMBL34287 Ki = 9.3 nM 8.03
CHEMBL430914 Ki = 10.4 nM 7.98
CHEMBL2113340 Ki = 12.3 nM 7.91