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Assay Detail

CHEMBL616891

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

Binding
Inhibitory constant for human 5-hydroxytryptamine 2A receptor transfected in to CHO cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

New serotonin 5-HT(2A), 5-HT(2B), and 5-HT(2C) receptor antagonists: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo and heterocycloalkanones.
Brea J, Rodrigo J, Carrieri A, Sanz F, Cadavid MI, Enguix MJ, Villazón M, Mengod G, Caro Y, Masaguer CF, Raviña E, Centeno NB, Carotti A, Loza MI.
J Med Chem (2002) 45 : 54 -71
PubMed 11754579 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.05 9.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL164471 1 9.14
CHEMBL333174 1 8.93
CHEMBL95098 1 7.17
CHEMBL310734 1 6.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL164471 Ki = 0.7244 nM 9.14
CHEMBL333174 Ki = 1.175 nM 8.93
CHEMBL95098 Ki = 67.61 nM 7.17
CHEMBL310734 Ki = 114.82 nM 6.94