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Assay Detail

CHEMBL971390

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Functional
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Bioisosteric heterocyclic versions of 7-{[2-(4-phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol: identification of highly potent and selective agonists for dopamine D3 receptor with potent in vivo activity.
Biswas S, Hazeldine S, Ghosh B, Parrington I, Kuzhikandathil E, Reith ME, Dutta AK.
J Med Chem (2008) 51 : 3005 -3019
PubMed 18410082 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 7.41 7.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL468017 1 7.87
CHEMBL467540 1 7.70
CHEMBL285755 1 7.40
CHEMBL59 DOPAMINE 4.0 1 6.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL468017 EC50 = 13.4 nM 7.87
CHEMBL467540 EC50 = 19.9 nM 7.70
CHEMBL285755 EC50 = 39.8 nM 7.40
CHEMBL59 DOPAMINE EC50 = 209.0 nM 6.68