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Assay Detail

CHEMBL671740

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

Binding
Tested in vitro for its ability to inhibit [3H]spiperone binding to Dopamine receptor D2 in rat striatal membrane
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

New cyclic butyrophenone derivatives in the indole series as potential atypical antipsychotics. A simple and practical synthesis of 6-aminomethyl-tetrahydroindol-4-ones and their affinites for D2 and 5-HT2A receptors
Masaguer CF, Ravina E, Loza I, Fontenla J
Bioorg Med Chem Lett (1997) 7 : 913 -918
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.94 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.30
CHEMBL460 MOLINDONE 4.0 1 7.48
CHEMBL163012 1 7.04
CHEMBL42 CLOZAPINE 4.0 1 7.00
CHEMBL163605 1 6.55
CHEMBL162901 1 6.20
CHEMBL349832 1 6.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 5.012 nM 8.30
CHEMBL460 MOLINDONE Ki = 33.11 nM 7.48
CHEMBL163012 Ki = 91.2 nM 7.04
CHEMBL42 CLOZAPINE Ki = 100.0 nM 7.00
CHEMBL163605 Ki = 281.84 nM 6.55
CHEMBL162901 Ki = 630.96 nM 6.20
CHEMBL349832 Ki = 954.99 nM 6.02