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Assay Detail

CHEMBL3136959

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

Binding
Displacement of [3H]spiperone from human recombinant dopamine D2L receptor expressed in CHOFlpIn cells after 3 hrs by liquid scintillation counting
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, functional and binding profile of (R)-apomorphine based homobivalent ligands targeting the dopamine D2 receptor
Shonberg J, Lane JR, Scammells PJ, Capuano B
Medchemcomm (2013) 4 : 1290 -1296
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.80 6.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53 APOMORPHINE 4.0 1 6.93
CHEMBL3134068 1 6.74
CHEMBL3134067 1 5.87
CHEMBL3134071 1 5.81
CHEMBL3134070 1 5.57
CHEMBL3134066 1 5.44
CHEMBL3134064 1 5.36
CHEMBL3134065 1 5.27
CHEMBL3134063 1 5.18
CHEMBL3134069 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53 APOMORPHINE IC50 = 117.0 nM 6.93
CHEMBL3134068 IC50 = 183.0 nM 6.74
CHEMBL3134067 IC50 = 1350.0 nM 5.87
CHEMBL3134071 IC50 = 1550.0 nM 5.81
CHEMBL3134070 IC50 = 2680.0 nM 5.57
CHEMBL3134066 IC50 = 3600.0 nM 5.44
CHEMBL3134064 IC50 = 4360.0 nM 5.36
CHEMBL3134065 IC50 = 5320.0 nM 5.27
CHEMBL3134063 IC50 = 6540.0 nM 5.18
CHEMBL3134069 IC50 - -