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Assay Detail

CHEMBL672100

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

Binding
In vitro binding affinity towards Dopamine receptor D2 in human using [3H]-spiperone 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

D(2) dopamine receptor (CHEMBL217)
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 7.63 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.43
CHEMBL367045 1 7.89
CHEMBL42 CLOZAPINE 4.0 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 3.7 nM 8.43
CHEMBL367045 Ki = 13.0 nM 7.89
CHEMBL42 CLOZAPINE Ki = 260.0 nM 6.58