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Assay Detail

CHEMBL672424

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

Binding
Affinity for Dopamine receptor D2 using [3H]YM-09151-2 was carried out on bovine retinal membrane preparations (low-affinity)
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Tissue Retina
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL3998)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

New N-n-propyl-substituted 3-aryl- and 3-cyclohexylpiperidines as partial agonists at the D4 dopamine receptor.
Macchia M, Cervetto L, Demontis GC, Longoni B, Minutolo F, Orlandini E, Ortore G, Papi C, Sbrana A, Macchia B.
J Med Chem (2003) 46 : 161 -168
PubMed 12502370 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 4.62 5.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45244 PD-168,077 1 5.20
CHEMBL554818 1 5.12
CHEMBL544000 1 4.80
CHEMBL542106 1 4.60
CHEMBL545188 1 4.57
CHEMBL553258 1 4.57
CHEMBL543078 1 4.45
CHEMBL538486 1 4.37
CHEMBL544711 1 4.36
CHEMBL544961 1 4.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45244 PD-168,077 Ki = 6300.0 nM 5.20
CHEMBL554818 Ki = 7600.0 nM 5.12
CHEMBL544000 Ki = 15900.0 nM 4.80
CHEMBL542106 Ki = 24900.0 nM 4.60
CHEMBL545188 Ki = 27000.0 nM 4.57
CHEMBL553258 Ki = 26700.0 nM 4.57
CHEMBL543078 Ki = 35400.0 nM 4.45
CHEMBL538486 Ki = 43200.0 nM 4.37
CHEMBL544711 Ki = 43700.0 nM 4.36
CHEMBL544961 Ki = 64000.0 nM 4.19