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Assay Detail

CHEMBL5334700

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

Binding
Displacement of [3H]ketanserin from postmortem human brain membrane homogenate 5-HT2A receptor incubated for 120 mins by microbeta liquid scintillation counter analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, Synthesis, Molecular Docking, and Biological Evaluation of Novel Pimavanserin-Based Analogues as Potential Serotonin 5-HT<sub>2A</sub> Receptor Inverse Agonists.
Albujuq NR, Meana JJ, Diez-Alarcia R, Muneta-Arrate I, Naqvi A, Althumayri K, Alsehli M.
J Med Chem (2023) 66 : 9057 -9075
PubMed 37378639 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 9.30 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5414859 1 10.30
CHEMBL2111101 PIMAVANSERIN 4.0 1 9.30
CHEMBL5414080 1 9.30
CHEMBL5403965 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5414859 Ki = 0.05012 nM 10.30
CHEMBL2111101 PIMAVANSERIN Ki = 0.5012 nM 9.30
CHEMBL5414080 Ki = 0.5012 nM 9.30
CHEMBL5403965 Ki = 5.012 nM 8.30