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Assay Detail

CHEMBL5346485

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

Functional
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
10
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Pioneering Methods in Brain Optimization and Mental Health Treatment.
Kargbo RB.
ACS Med Chem Lett (2024) 15 : 337 -339
PubMed 38505858 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 7.96 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4648350 2 8.62
CHEMBL442 ERGOTAMINE 4.0 2 8.14
CHEMBL263881 LYSERGIDE 2.0 2 7.80
CHEMBL65547 PSILOCIN 2.0 2 7.70
CHEMBL39 SEROTONIN 3.0 2 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4648350 EC50 = 2.4 nM 8.62
CHEMBL4648350 EC50 = 2.512 nM 8.60
CHEMBL442 ERGOTAMINE EC50 = 7.3 nM 8.14
CHEMBL442 ERGOTAMINE EC50 = 7.943 nM 8.10
CHEMBL263881 LYSERGIDE EC50 = 15.85 nM 7.80
CHEMBL263881 LYSERGIDE EC50 = 16.0 nM 7.80
CHEMBL65547 PSILOCIN EC50 = 19.95 nM 7.70
CHEMBL65547 PSILOCIN EC50 = 22.0 nM 7.66
CHEMBL39 SEROTONIN EC50 = 25.12 nM 7.60
CHEMBL39 SEROTONIN EC50 = 28.0 nM 7.55