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Assay Detail

CHEMBL926384

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Functional
Agonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S binding
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type AtT20
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Further structure-activity relationships study of hybrid 7-{[2-(4-phenylpiperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol analogues: identification of a high-affinity D3-preferring agonist with potent in vivo activity with long duration of action.
Biswas S, Zhang S, Fernandez F, Ghosh B, Zhen J, Kuzhikandathil E, Reith ME, Dutta AK.
J Med Chem (2008) 51 : 101 -117
PubMed 18072730 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 9.31 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL399164 1 10.10
CHEMBL250552 1 9.92
CHEMBL156639 1 9.16
CHEMBL59 DOPAMINE 4.0 1 8.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL399164 EC50 = 0.08 nM 10.10
CHEMBL250552 EC50 = 0.12 nM 9.92
CHEMBL156639 EC50 = 0.69 nM 9.16
CHEMBL59 DOPAMINE EC50 = 8.53 nM 8.07