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Assay Detail

CHEMBL833276

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

Functional
Serotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type A7R5
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Beta-oxygenated analogues of the 5-HT2A serotonin receptor agonist 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane.
Glennon RA, Bondarev ML, Khorana N, Young R, May JA, Hellberg MR, McLaughlin MA, Sharif NA.
J Med Chem (2004) 47 : 6034 -6041
PubMed 15537358 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 6.50 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69700 1 7.70
CHEMBL6607 BROLAMFETAMINE 2.0 1 7.22
CHEMBL188709 1 7.00
CHEMBL191051 1 6.92
CHEMBL365958 1 6.89
CHEMBL6737 1 6.13
CHEMBL191286 1 6.08
CHEMBL364718 1 5.88
CHEMBL191420 1 5.85
CHEMBL363772 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69700 EC50 = 20.0 nM 7.70
CHEMBL6607 BROLAMFETAMINE EC50 = 60.0 nM 7.22
CHEMBL188709 EC50 = 100.0 nM 7.00
CHEMBL191051 EC50 = 120.0 nM 6.92
CHEMBL365958 EC50 = 130.0 nM 6.89
CHEMBL6737 EC50 = 740.0 nM 6.13
CHEMBL191286 EC50 = 840.0 nM 6.08
CHEMBL364718 EC50 = 1330.0 nM 5.88
CHEMBL191420 EC50 = 1410.0 nM 5.85
CHEMBL363772 EC50 = 5040.0 nM 5.30