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Assay Detail

CHEMBL617604

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

Binding
Compound was tested for the inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Effect of modifications of the alkylpiperazine moiety of trazodone on 5HT2A and alpha1 receptor binding affinity.
Giannangeli M, Cazzolla N, Luparini MR, Magnani M, Mabilia M, Picconi G, Tomaselli M, Baiocchi L.
J Med Chem (1999) 42 : 336 -345
PubMed 9986703 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.37 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL621 TRAZODONE 4.0 1 7.77
CHEMBL117507 1 7.77
CHEMBL323688 1 7.51
CHEMBL325489 1 7.03
CHEMBL118691 1 6.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL621 TRAZODONE IC50 = 17.0 nM 7.77
CHEMBL117507 IC50 = 17.0 nM 7.77
CHEMBL323688 IC50 = 31.0 nM 7.51
CHEMBL325489 IC50 = 94.0 nM 7.03
CHEMBL118691 IC50 = 169.0 nM 6.77