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Assay Detail

CHEMBL2212937

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Functional
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
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(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel bivalent ligands for D2/D3 dopamine receptors: Significant co-operative gain in D2 affinity and potency.
Gogoi S, Biswas S, Modi G, Antonio T, Reith ME, Dutta AK.
ACS Med Chem Lett (2012) 3 : 991 -996
PubMed 23275802 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 8.94 9.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2206264 1 9.28
CHEMBL269004 1 9.20
CHEMBL2206265 1 9.03
CHEMBL59 DOPAMINE 4.0 1 8.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2206264 EC50 = 0.53 nM 9.28
CHEMBL269004 EC50 = 0.63 nM 9.20
CHEMBL2206265 EC50 = 0.94 nM 9.03
CHEMBL59 DOPAMINE EC50 = 5.8 nM 8.24