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Assay Detail

CHEMBL3136960

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

Binding
Agonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assay
12
Total Activities
12
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
EC50 12 6.97 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53 APOMORPHINE 4.0 1 8.77
CHEMBL3134061 1 8.00
CHEMBL3134067 1 7.10
CHEMBL3134068 1 6.96
CHEMBL3134062 1 6.88
CHEMBL3134065 1 6.83
CHEMBL3134069 1 6.65
CHEMBL3134071 1 6.61
CHEMBL3134063 1 6.58
CHEMBL3134070 1 6.42
CHEMBL3134064 1 6.40
CHEMBL3134066 1 6.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53 APOMORPHINE EC50 = 1.7 nM 8.77
CHEMBL3134061 EC50 = 10.0 nM 8.00
CHEMBL3134067 EC50 = 79.0 nM 7.10
CHEMBL3134068 EC50 = 110.0 nM 6.96
CHEMBL3134062 EC50 = 132.0 nM 6.88
CHEMBL3134065 EC50 = 149.0 nM 6.83
CHEMBL3134069 EC50 = 224.0 nM 6.65
CHEMBL3134071 EC50 = 248.0 nM 6.61
CHEMBL3134063 EC50 = 266.0 nM 6.58
CHEMBL3134070 EC50 = 385.0 nM 6.42
CHEMBL3134064 EC50 = 396.0 nM 6.40
CHEMBL3134066 EC50 = 419.0 nM 6.38