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Assay Detail

CHEMBL617513

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

Binding
In vitro binding affinity towards 5-hydroxytryptamine 2A receptor in human using [3H]ketanserin as radioligand
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.
Campiani G, Butini S, Fattorusso C, Catalanotti B, Gemma S, Nacci V, Morelli E, Cagnotto A, Mereghetti I, Mennini T, Carli M, Minetti P, Di Cesare MA, Mastroianni D, Scafetta N, Galletti B, Stasi MA, Castorina M, Pacifici L, Vertechy M, Di Serio S, Ghirardi O, Tinti O, Carminati P.
J Med Chem (2004) 47 : 143 -157
PubMed 14695828 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.99 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL367045 1 8.96
CHEMBL42 CLOZAPINE 4.0 1 8.11
CHEMBL54 HALOPERIDOL 4.0 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL367045 Ki = 1.1 nM 8.96
CHEMBL42 CLOZAPINE Ki = 7.8 nM 8.11
CHEMBL54 HALOPERIDOL Ki = 130.0 nM 6.89