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Assay Detail

CHEMBL4179172

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

Binding
Displacement of [3H]methyl-spiperone from human recombinant dopamine D2 receptor expressed in HEK293 cells
2
Total Activities
2
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(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New 5-HT1A, 5HT2A and 5HT2C receptor ligands containing a picolinic nucleus: Synthesis, in vitro and in vivo pharmacological evaluation.
Fiorino F, Magli E, Kędzierska E, Ciano A, Corvino A, Severino B, Perissutti E, Frecentese F, Di Vaio P, Saccone I, Izzo AA, Capasso R, Massarelli P, Rossi I, Orzelska-Gòrka J, Kotlińska JH, Santagada V, Caliendo G.
Bioorg Med Chem (2017) 25 : 5820 -5837
PubMed 28943244 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 6.12 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4208744 1 6.60
CHEMBL3763633 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4208744 Ki = 250.0 nM 6.60
CHEMBL3763633 Ki = 2300.0 nM 5.64