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Assay Detail

CHEMBL1033196

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

Binding
Displacement of [3H]N-methylspiperone from human dopamine D3 receptor by liquid scintillation counting
16
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups.
Sikazwe DM, Nkansah NT, Altundas R, Zhu XY, Roth BL, Setola V, Ablordeppey SY.
Bioorg Med Chem (2009) 17 : 1716 -1723
PubMed 19155177 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.90 8.29
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL210578 1 8.29
CHEMBL54 HALOPERIDOL 4.0 1 8.26
CHEMBL514747 1 7.96
CHEMBL460854 1 7.75
CHEMBL3084502 1 7.60
CHEMBL514590 1 6.89
CHEMBL456430 1 6.76
CHEMBL150161 1 6.70
CHEMBL514591 1 6.66
CHEMBL458342 1 6.47
CHEMBL460223 1 6.43
CHEMBL460644 1 5.82
CHEMBL460855 1 5.54
CHEMBL517564 1 5.51
CHEMBL513776 1 -
CHEMBL456429 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL210578 Ki = 5.1 nM 8.29
CHEMBL54 HALOPERIDOL Ki = 5.5 nM 8.26
CHEMBL514747 Ki = 11.0 nM 7.96
CHEMBL460854 Ki = 18.0 nM 7.75
CHEMBL3084502 Ki = 25.0 nM 7.60
CHEMBL514590 Ki = 128.0 nM 6.89
CHEMBL456430 Ki = 172.0 nM 6.76
CHEMBL150161 Ki = 200.0 nM 6.70
CHEMBL514591 Ki = 220.0 nM 6.66
CHEMBL458342 Ki = 335.5 nM 6.47
CHEMBL460223 Ki = 370.0 nM 6.43
CHEMBL460644 Ki = 1500.0 nM 5.82
CHEMBL460855 Ki = 2874.0 nM 5.54
CHEMBL517564 Ki = 3074.0 nM 5.51
CHEMBL513776 Activity - -
CHEMBL456429 Ki > 10000.0 nM -