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Assay Detail

CHEMBL4195136

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

Binding
Displacement of [3H]methylspiperonee from recombinant human D2 receptor expressed in HEK293 cells cell membranes after 60 mins by liquid scintillation counting method
7
Total Activities
7
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

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
Ki 7 6.64 8.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.23
CHEMBL4209888 1 7.01
CHEMBL4213352 1 6.79
CHEMBL4207653 1 6.72
CHEMBL4212812 1 6.52
CHEMBL4217761 1 5.92
CHEMBL4205526 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 5.9 nM 8.23
CHEMBL4209888 Ki = 97.0 nM 7.01
CHEMBL4213352 Ki = 162.0 nM 6.79
CHEMBL4207653 Ki = 189.0 nM 6.72
CHEMBL4212812 Ki = 299.0 nM 6.52
CHEMBL4217761 Ki = 1206.0 nM 5.92
CHEMBL4205526 Ki = 4963.0 nM 5.30