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Assay Detail

CHEMBL885383

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

Binding
High binding affinity towards human dopamine receptor 3 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type ovary
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists.
Elsner J, Boeckler F, Heinemann FW, Hübner H, Gmeiner P.
J Med Chem (2005) 48 : 5771 -5779
PubMed 16134944 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.29 9.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301265 PRAMIPEXOLE 4.0 1 9.06
CHEMBL193337 1 8.40
CHEMBL194099 1 8.21
CHEMBL196928 1 8.17
CHEMBL240773 QUINPIROLE 2.0 1 7.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301265 PRAMIPEXOLE Ki = 0.88 nM 9.06
CHEMBL193337 Ki = 4.0 nM 8.40
CHEMBL194099 Ki = 6.1 nM 8.21
CHEMBL196928 Ki = 6.7 nM 8.17
CHEMBL240773 QUINPIROLE Ki = 24.0 nM 7.62