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Assay Detail

CHEMBL981820

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

Binding
Displacement of [3H]spiperone from human wild type D3 receptor expressed in human HEK293 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Novel D3 selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies.
Dörfler M, Tschammer N, Hamperl K, Hübner H, Gmeiner P.
J Med Chem (2008) 51 : 6829 -6838
PubMed 18834111 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.00 9.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL484358 1 9.11
CHEMBL484202 1 8.60
CHEMBL285755 1 8.44
CHEMBL59 DOPAMINE 4.0 1 7.14
CHEMBL162762 1 6.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL484358 Ki = 0.78 nM 9.11
CHEMBL484202 Ki = 2.5 nM 8.60
CHEMBL285755 Ki = 3.6 nM 8.44
CHEMBL59 DOPAMINE Ki = 72.0 nM 7.14
CHEMBL162762 Ki = 190.0 nM 6.72