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Assay Detail

CHEMBL617425

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

Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2 receptor rat tissue homogenate
6
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Tissue
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 2 (5-HT2) receptor (CHEMBL2093870)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

New antipsychotic agents with serotonin and dopamine antagonist properties based on a pyrrolo[2,1-b][1,3]benzothiazepine structure.
Campiani G, Nacci V, Bechelli S, Ciani SM, Garofalo A, Fiorini I, Wikström H, de Boer P, Liao Y, Tepper PG, Cagnotto A, Mennini T.
J Med Chem (1998) 41 : 3763 -3772
PubMed 9748351 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.42 8.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL120512 3 8.94
CHEMBL333246 1 8.11
CHEMBL42 CLOZAPINE 4.0 1 7.96
CHEMBL715 OLANZAPINE 4.0 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL120512 Ki = 1.14 nM 8.94
CHEMBL120512 Ki = 1.48 nM 8.83
CHEMBL120512 Ki = 1.72 nM 8.76
CHEMBL333246 Ki = 7.85 nM 8.11
CHEMBL42 CLOZAPINE Ki = 11.0 nM 7.96
CHEMBL715 OLANZAPINE Ki = 12.0 nM 7.92