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Assay Detail

CHEMBL5151486

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

Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
8
Total Activities
4
Compounds Tested
2
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

Abolishing Dopamine D<sub>2long</sub>/D<sub>3</sub> Receptor Affinity of Subtype-Selective Carbamoylguanidine-Type Histamine H<sub>2</sub> Receptor Agonists.
Tropmann K, Bresinsky M, Forster L, Mönnich D, Buschauer A, Wittmann HJ, Hübner H, Gmeiner P, Pockes S, Strasser A.
J Med Chem (2021) 64 : 8684 -8709
PubMed 34110814 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 10.11 10.11
EC50 4 5.99 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4860528 2 10.11
CHEMBL5207281 2 10.11
CHEMBL5206565 2 10.11
CHEMBL5201074 2 10.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4860528 Kd = 0.078 nM 10.11
CHEMBL5207281 Kd = 0.078 nM 10.11
CHEMBL5206565 Kd = 0.078 nM 10.11
CHEMBL5201074 Kd = 0.078 nM 10.11
CHEMBL4860528 EC50 = 109.65 nM 6.96
CHEMBL5206565 EC50 = 676.08 nM 6.17
CHEMBL5207281 EC50 = 2238.72 nM 5.65
CHEMBL5201074 EC50 = 6606.93 nM 5.18