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Assay Detail

CHEMBL5235442

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

Binding
Displacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constant
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
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
Ki 9 7.02 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3480577 UCSF924 1 8.52
CHEMBL5290993 1 8.37
CHEMBL5278957 1 7.10
CHEMBL5290570 1 6.89
CHEMBL5272829 1 6.85
CHEMBL5277325 1 6.82
CHEMBL5283608 1 6.50
CHEMBL5267339 1 6.30
CHEMBL5289845 1 5.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3480577 UCSF924 Ki = 3.0 nM 8.52
CHEMBL5290993 Ki = 4.3 nM 8.37
CHEMBL5278957 Ki = 80.0 nM 7.10
CHEMBL5290570 Ki = 130.0 nM 6.89
CHEMBL5272829 Ki = 140.0 nM 6.85
CHEMBL5277325 Ki = 150.0 nM 6.82
CHEMBL5283608 Ki = 320.0 nM 6.50
CHEMBL5267339 Ki = 500.0 nM 6.30
CHEMBL5289845 Ki = 1380.0 nM 5.86