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Assay Detail

CHEMBL4195152

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

Functional
Agonist activity at human D2 receptor expressed in CHO-K1 cells co-expressing Galphaqi5 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and activity of di- or trisubstituted N-(phenoxyalkyl)- or N-{2-[2-(phenoxy)ethoxy]ethyl}piperazine derivatives on the central nervous system.
Pańczyk K, Pytka K, Jakubczyk M, Rapacz A, Sałat K, Furgała A, Siwek A, Głuch-Lutwin M, Gryboś A, Słoczyńska K, Pękala E, Żmudzki P, Bucki A, Kołaczkowski M, Żelaszczyk D, Marona H, Waszkielewicz AM.
Bioorg Med Chem Lett (2018) 28 : 2039 -2049
PubMed 29730027 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.01 7.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53 APOMORPHINE 4.0 1 7.90
CHEMBL4212812 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53 APOMORPHINE EC50 = 12.7 nM 7.90
CHEMBL4212812 EC50 = 757.0 nM 6.12