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Assay Detail

CHEMBL820504

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

Binding
Binding affinity against alpha-1 adrenergic receptor in rat cerebral cortex tissue using [3H]WB-4101 as radioligand
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
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 6 8.60 9.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL114451 1 9.06
CHEMBL115367 1 8.89
CHEMBL115486 1 8.79
CHEMBL321591 1 8.60
CHEMBL114131 1 8.15
CHEMBL326775 1 8.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL114451 IC50 = 0.876 nM 9.06
CHEMBL115367 IC50 = 1.3 nM 8.89
CHEMBL115486 IC50 = 1.63 nM 8.79
CHEMBL321591 IC50 = 2.5 nM 8.60
CHEMBL114131 IC50 = 7.15 nM 8.15
CHEMBL326775 IC50 = 8.3 nM 8.08