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Assay Detail

CHEMBL671031

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

Binding
In vitro inhibition of [3H]spiperone binding to Dopamine receptor D2 in Macaca nemestrina striatal membranes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Macaca nemestrina
Tissue Striatum
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Dopamine receptor (CHEMBL2096905)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

N-fluoroalkylated and N-alkylated analogues of the dopaminergic D-2 receptor antagonist raclopride.
Lannoye GS, Moerlein SM, Parkinson D, Welch MJ.
J Med Chem (1990) 33 : 2430 -2437
PubMed 2391685 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.89 8.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8809 RACLOPRIDE 2.0 1 8.06
CHEMBL80127 1 7.76
CHEMBL418922 1 7.39
CHEMBL80126 1 7.05
CHEMBL81778 1 6.89
CHEMBL312602 1 6.80
CHEMBL77448 1 5.58
CHEMBL2021339 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8809 RACLOPRIDE Ki = 8.7 nM 8.06
CHEMBL80127 Ki = 17.3 nM 7.76
CHEMBL418922 Ki = 41.1 nM 7.39
CHEMBL80126 Ki = 88.5 nM 7.05
CHEMBL81778 Ki = 130.0 nM 6.89
CHEMBL312602 Ki = 159.0 nM 6.80
CHEMBL77448 Ki = 2610.0 nM 5.58
CHEMBL2021339 Ki = 2620.0 nM 5.58