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Assay Detail

CHEMBL617952

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

Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2A receptor of Rat thoracic aorta
17
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Thoracic aorta
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

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
pA2 16 - -
Kd 1 7.50 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL155006 1 7.50
CHEMBL111352 1 -
CHEMBL163012 1 -
CHEMBL263790 1 -
CHEMBL142316 1 -
CHEMBL358895 1 -
CHEMBL160907 1 -
CHEMBL141600 1 -
CHEMBL142668 1 -
CHEMBL357517 1 -
CHEMBL320572 2 -
CHEMBL159771 1 -
CHEMBL321682 1 -
CHEMBL143937 1 -
CHEMBL163605 1 -
CHEMBL162901 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL155006 Kd = 31.62 nM 7.50
CHEMBL320572 pA2 - -
CHEMBL163012 pA2 - -
CHEMBL263790 pA2 - -
CHEMBL142316 pA2 - -
CHEMBL358895 pA2 - -
CHEMBL160907 pA2 - -
CHEMBL141600 pA2 - -
CHEMBL142668 pA2 - -
CHEMBL111352 pA2 - -
CHEMBL159771 pA2 - -
CHEMBL321682 pA2 - -
CHEMBL143937 pA2 - -
CHEMBL163605 pA2 - -
CHEMBL320572 pA2 - -
CHEMBL162901 pA2 - -
CHEMBL357517 pA2 - -