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Assay Detail

CHEMBL883722

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

Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.
Sard H, Kumaran G, Morency C, Roth BL, Toth BA, He P, Shuster L.
Bioorg Med Chem Lett (2005) 15 : 4555 -4559
PubMed 16061378 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.56 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL65547 PSILOCIN 2.0 1 7.62
CHEMBL198124 1 7.50
CHEMBL197664 1 6.20
CHEMBL197646 1 6.02
CHEMBL194378 PSILOCYBIN 3.0 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL65547 PSILOCIN EC50 = 24.0 nM 7.62
CHEMBL198124 EC50 = 32.0 nM 7.50
CHEMBL197664 EC50 = 633.0 nM 6.20
CHEMBL197646 EC50 = 949.0 nM 6.02
CHEMBL194378 PSILOCYBIN EC50 = 3475.0 nM 5.46