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Assay Detail

CHEMBL617029

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Binding
Binding affinity against rat 5-hydroxytryptamine 2 receptor in rat cerebral cortex tissue using [3H]spiperone as radioligand
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone.
Cipollina JA, Ruediger EH, New JS, Wire ME, Shepherd TA, Smith DW, Yevich JP.
J Med Chem (1991) 34 : 3316 -3328
PubMed 1683407 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.32 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL35057 TIOSPIRONE 2.0 1 9.40
CHEMBL115486 1 8.96
CHEMBL114451 1 8.69
CHEMBL115367 1 8.54
CHEMBL321591 1 8.35
CHEMBL326775 1 7.99
CHEMBL114131 1 7.70
CHEMBL1154 BENZISOTHIAZOLE-3-YL-PIPERAZINE 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL35057 TIOSPIRONE IC50 = 0.4 nM 9.40
CHEMBL115486 IC50 = 1.1 nM 8.96
CHEMBL114451 IC50 = 2.05 nM 8.69
CHEMBL115367 IC50 = 2.92 nM 8.54
CHEMBL321591 IC50 = 4.5 nM 8.35
CHEMBL326775 IC50 = 10.2 nM 7.99
CHEMBL114131 IC50 = 19.8 nM 7.70
CHEMBL1154 BENZISOTHIAZOLE-3-YL-PIPERAZINE IC50 = 110.0 nM 6.96