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Assay Detail

CHEMBL617262

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

Binding
Compound was tested in vitro for its binding affinity towards 5-hydroxytryptamine 2A receptor from rat frontal cortex using [3H]-ketanserin as radioligand
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Frontal cortex
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical antipsychotics.
Raviña E, Negreira J, Cid J, Masaguer CF, Rosa E, Rivas ME, Fontenla JA, Loza MI, Tristán H, Cadavid MI, Sanz F, Lozoya E, Carotti A, Carrieri A.
J Med Chem (1999) 42 : 2774 -2797
PubMed 10425088 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.55 8.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL543613 1 8.56
CHEMBL545488 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL543613 Ki = 2.754 nM 8.56
CHEMBL545488 Ki = 288.4 nM 6.54