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Assay Detail

CHEMBL617114

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

Binding
Tested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptor
7
Total Activities
7
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

Synthesis and pharmacological characterization of a series of geometrically constrained 5-HT(2A/2C) receptor ligands.
Chambers JJ, Parrish JC, Jensen NH, Kurrasch-Orbaugh DM, Marona-Lewicka D, Nichols DE.
J Med Chem (2003) 46 : 3526 -3535
PubMed 12877591 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.56 8.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL263881 LYSERGIDE 2.0 1 8.01
CHEMBL6607 BROLAMFETAMINE 2.0 1 7.14
CHEMBL116940 1 6.92
CHEMBL119323 1 5.96
CHEMBL445106 1 5.68
CHEMBL65547 PSILOCIN 2.0 1 5.64
CHEMBL119584 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL263881 LYSERGIDE EC50 = 9.8 nM 8.01
CHEMBL6607 BROLAMFETAMINE EC50 = 72.0 nM 7.14
CHEMBL116940 EC50 = 120.0 nM 6.92
CHEMBL119323 EC50 = 1100.0 nM 5.96
CHEMBL445106 EC50 = 2090.0 nM 5.68
CHEMBL65547 PSILOCIN EC50 = 2300.0 nM 5.64
CHEMBL119584 EC50 > 10000.0 nM -