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Assay Detail

CHEMBL5235434

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

Binding
Agonist activity at human D4R expressed in HEK293 cells by calcium flux assay
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(4) dopamine receptor (CHEMBL219)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Recent findings leading to the discovery of selective dopamine D<sub>4</sub> receptor ligands for the treatment of widespread diseases.
Giorgioni G, Del Bello F, Pavletić P, Quaglia W, Botticelli L, Cifani C, Micioni Di Bonaventura E, Micioni Di Bonaventura MV, Piergentili A.
Eur J Med Chem (2021) 212 : 113141 -113141
PubMed 33422983 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 8.14 8.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45244 PD-168,077 1 8.16
CHEMBL362542 1 8.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45244 PD-168,077 EC50 = 6.9 nM 8.16
CHEMBL362542 EC50 = 7.5 nM 8.12