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Assay Detail

CHEMBL617646

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

Binding
In vitro ability to displace [3H]mesulergine binding from 5-hydroxytryptamine 2C receptor from bovine choroid plexus.
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2C (CHEMBL225)
Type SINGLE PROTEIN
Organism Homo sapiens

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 7 6.37 7.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL554199 1 7.06
CHEMBL544091 1 6.48
CHEMBL542181 1 6.44
CHEMBL92673 1 6.38
CHEMBL545727 1 5.96
CHEMBL95112 1 5.90
CHEMBL544089 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL554199 Ki = 87.1 nM 7.06
CHEMBL544091 Ki = 331.13 nM 6.48
CHEMBL542181 Ki = 363.08 nM 6.44
CHEMBL92673 Ki = 416.87 nM 6.38
CHEMBL545727 Ki = 1096.48 nM 5.96
CHEMBL95112 Ki = 1258.93 nM 5.90
CHEMBL544089 Ki < 10000.0 nM -