Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL671490

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

Binding
Binding affinity at Dopamine receptor D2 in rat striatal membrane by [3H]spiperone displacement.
19
Total Activities
19
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 Expert

Target

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

Publication

Aryl 1-but-3-ynyl-4-phenyl-1,2,3,6-tetrahydropyridines as potential antipsychotic agents: synthesis and structure-activity relationships.
Glase SA, Akunne HC, Heffner TG, Jaen JC, MacKenzie RG, Meltzer LT, Pugsley TA, Smith SJ, Wise LD.
J Med Chem (1996) 39 : 3179 -3187
PubMed 8759640 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.94 8.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL431367 ROXINDOLE 2.0 1 8.04
CHEMBL108790 1 7.52
CHEMBL110489 1 7.50
CHEMBL109063 1 7.48
CHEMBL108463 1 7.43
CHEMBL108186 1 7.40
CHEMBL321828 1 7.25
CHEMBL109101 1 7.20
CHEMBL324445 1 7.14
CHEMBL108375 1 6.90
CHEMBL110488 1 6.87
CHEMBL109199 1 6.71
CHEMBL108462 1 6.59
CHEMBL108530 1 6.49
CHEMBL419021 1 6.36
CHEMBL110843 1 5.78
CHEMBL432972 1 5.27
CHEMBL110136 1 -
CHEMBL108386 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL431367 ROXINDOLE Ki = 9.1 nM 8.04
CHEMBL108790 Ki = 30.0 nM 7.52
CHEMBL110489 Ki = 32.0 nM 7.50
CHEMBL109063 Ki = 33.0 nM 7.48
CHEMBL108463 Ki = 37.0 nM 7.43
CHEMBL108186 Ki = 40.0 nM 7.40
CHEMBL321828 Ki = 56.0 nM 7.25
CHEMBL109101 Ki = 63.0 nM 7.20
CHEMBL324445 Ki = 73.0 nM 7.14
CHEMBL108375 Ki = 127.0 nM 6.90
CHEMBL110488 Ki = 136.0 nM 6.87
CHEMBL109199 Ki = 193.0 nM 6.71
CHEMBL108462 Ki = 255.0 nM 6.59
CHEMBL108530 Ki = 327.0 nM 6.49
CHEMBL419021 Ki = 440.0 nM 6.36
CHEMBL110843 Ki = 1673.0 nM 5.78
CHEMBL432972 Ki = 5388.0 nM 5.27
CHEMBL110136 Ki > 10000.0 nM -
CHEMBL108386 Ki > 10000.0 nM -