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Assay Detail

CHEMBL671589

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

Binding
pKi value for Dopamine receptor D2 binding site
7
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL339)
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 7.86 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL122536 METHIOTHEPINE 1 9.70
CHEMBL120512 3 8.70
CHEMBL715 OLANZAPINE 4.0 1 7.20
CHEMBL333246 1 7.15
CHEMBL42 CLOZAPINE 4.0 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL122536 METHIOTHEPINE Ki = 0.1995 nM 9.70
CHEMBL120512 Ki = 1.995 nM 8.70
CHEMBL120512 Ki = 3.981 nM 8.40
CHEMBL120512 Ki = 50.12 nM 7.30
CHEMBL715 OLANZAPINE Ki = 63.1 nM 7.20
CHEMBL333246 Ki = 70.79 nM 7.15
CHEMBL42 CLOZAPINE Ki = 251.19 nM 6.60