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Assay Detail

CHEMBL4392164

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

Binding
Displacement of [3H]N-methylspiperone from human D3 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Dopamine D4 Receptor-Selective Compounds Reveal Structure-Activity Relationships that Engender Agonist Efficacy.
Keck TM, Free RB, Day MM, Brown SL, Maddaluna MS, Fountain G, Cooper C, Fallon B, Holmes M, Stang CT, Burkhardt R, Bonifazi A, Ellenberger MP, Newman AH, Sibley DR, Wu C, Boateng CA.
J Med Chem (2019) 62 : 3722 -3740
PubMed 30883109 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 5.52 6.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL216393 1 6.36
CHEMBL4437912 1 6.30
CHEMBL375596 1 5.78
CHEMBL4464861 1 5.52
CHEMBL4473792 1 5.43
CHEMBL4454068 1 5.42
CHEMBL4588808 1 5.34
CHEMBL4473652 1 4.94
CHEMBL4436479 1 4.58
CHEMBL4587925 1 -
CHEMBL4448320 1 -
CHEMBL4443054 1 -
CHEMBL4453069 1 -
CHEMBL4591118 1 -
CHEMBL4592753 1 -
CHEMBL4443848 1 -
CHEMBL4442548 1 -
CHEMBL4572245 1 -
CHEMBL4456754 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL216393 Ki = 433.0 nM 6.36
CHEMBL4437912 Ki = 496.0 nM 6.30
CHEMBL375596 Ki = 1680.0 nM 5.78
CHEMBL4464861 Ki = 3040.0 nM 5.52
CHEMBL4473792 Ki = 3681.0 nM 5.43
CHEMBL4454068 Ki = 3790.0 nM 5.42
CHEMBL4588808 Ki = 4530.0 nM 5.34
CHEMBL4473652 Ki = 11459.0 nM 4.94
CHEMBL4436479 Ki = 26320.0 nM 4.58
CHEMBL4587925 Ki > 50000.0 nM -
CHEMBL4448320 Ki > 10000.0 nM -
CHEMBL4443054 Ki > 10000.0 nM -
CHEMBL4453069 Ki > 50000.0 nM -
CHEMBL4591118 Ki > 50000.0 nM -
CHEMBL4592753 Ki > 50000.0 nM -
CHEMBL4443848 Ki > 50000.0 nM -
CHEMBL4442548 Ki > 50000.0 nM -
CHEMBL4572245 Ki > 50000.0 nM -
CHEMBL4456754 Ki > 50000.0 nM -