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Assay Detail

CHEMBL834253

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

Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(4) dopamine receptor (CHEMBL219)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand.
Matulenko MA, Surber B, Fan L, Kolasa T, Nakane M, Terranova MA, Uchic ME, Miller LN, Chang R, Donnelly-Roberts DL, Namovic MT, Moreland RB, Brioni JD, Stewart AO.
Bioorg Med Chem Lett (2004) 14 : 5095 -5098
PubMed 15380206 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 7.57 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL362542 1 8.12
CHEMBL184486 1 7.57
CHEMBL185149 1 7.02
CHEMBL184853 1 -
CHEMBL183466 1 -
CHEMBL182432 1 -
CHEMBL184772 1 -
CHEMBL184263 1 -
CHEMBL183601 1 -
CHEMBL363308 1 -
CHEMBL185263 1 -
CHEMBL364865 1 -
CHEMBL54 HALOPERIDOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL362542 EC50 = 7.5 nM 8.12
CHEMBL184486 EC50 = 26.8 nM 7.57
CHEMBL185149 EC50 = 96.0 nM 7.02
CHEMBL184853 EC50 > 10000.0 nM -
CHEMBL183466 EC50 > 10000.0 nM -
CHEMBL182432 EC50 > 10000.0 nM -
CHEMBL184772 EC50 > 10000.0 nM -
CHEMBL184263 EC50 > 10000.0 nM -
CHEMBL183601 EC50 > 10000.0 nM -
CHEMBL363308 EC50 > 10000.0 nM -
CHEMBL185263 EC50 > 10000.0 nM -
CHEMBL364865 EC50 > 10000.0 nM -
CHEMBL54 HALOPERIDOL EC50 > 10000.0 nM -