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Assay Detail

CHEMBL666363

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]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
7
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(1A) dopamine receptor (CHEMBL265)
Type SINGLE PROTEIN
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 7.25 7.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL120512 3 7.79
CHEMBL42055 E-FLUPENTIXOL 2.0 1 7.42
CHEMBL715 OLANZAPINE 4.0 1 7.07
CHEMBL333246 1 6.80
CHEMBL42 CLOZAPINE 4.0 1 6.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL120512 Ki = 16.4 nM 7.79
CHEMBL120512 Ki = 22.0 nM 7.66
CHEMBL120512 Ki = 27.0 nM 7.57
CHEMBL42055 E-FLUPENTIXOL Ki = 37.8 nM 7.42
CHEMBL715 OLANZAPINE Ki = 85.0 nM 7.07
CHEMBL333246 Ki = 160.0 nM 6.80
CHEMBL42 CLOZAPINE Ki = 353.0 nM 6.45