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Assay Detail

CHEMBL4009965

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

Binding
Displacement of [3H]ketanserin from 5HT2A in Sprague-Dawley rat frontal cortex membranes measured after 15 mins by scintillation counting method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Frontal cortex
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The "Phenylalkylaminome" with a Focus on Selected Drugs of Abuse.
Glennon RA.
J Med Chem (2017) 60 : 2605 -2628
PubMed 28244748 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.85 6.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1927025 1 6.71
CHEMBL6731 TENAMFETAMINE 2.0 1 6.41
CHEMBL382757 1 5.48
CHEMBL195390 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1927025 Ki = 197.0 nM 6.71
CHEMBL6731 TENAMFETAMINE Ki = 387.0 nM 6.41
CHEMBL382757 Ki = 3310.0 nM 5.48
CHEMBL195390 Ki = 15800.0 nM 4.80