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Assay Detail

CHEMBL617017

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

Binding
pKi value for 5-hydroxytryptamine 2 receptor binding site
7
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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 7 8.53 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL122536 METHIOTHEPINE 1 9.40
CHEMBL120512 3 8.90
CHEMBL333246 1 8.10
CHEMBL715 OLANZAPINE 4.0 1 7.90
CHEMBL42 CLOZAPINE 4.0 1 7.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL122536 METHIOTHEPINE Ki = 0.3981 nM 9.40
CHEMBL120512 Ki = 1.259 nM 8.90
CHEMBL120512 Ki = 1.585 nM 8.80
CHEMBL120512 Ki = 1.995 nM 8.70
CHEMBL333246 Ki = 7.943 nM 8.10
CHEMBL715 OLANZAPINE Ki = 12.59 nM 7.90
CHEMBL42 CLOZAPINE Ki = 12.59 nM 7.90