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Assay Detail

CHEMBL5151495

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

Binding
Displacement of [3H]CGP12177 from human beta-1 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs 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
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Beta-1 adrenergic receptor (CHEMBL213)
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
EC50 4 4.49 4.66
Kd 4 10.12 10.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4860528 2 10.12
CHEMBL5207281 2 10.12
CHEMBL5206565 2 10.12
CHEMBL5201074 2 10.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4860528 Kd = 0.075 nM 10.12
CHEMBL5207281 Kd = 0.075 nM 10.12
CHEMBL5206565 Kd = 0.075 nM 10.12
CHEMBL5201074 Kd = 0.075 nM 10.12
CHEMBL4860528 EC50 = 21877.62 nM 4.66
CHEMBL5201074 EC50 = 48977.88 nM 4.31
CHEMBL5207281 EC50 > 100000.0 nM -
CHEMBL5206565 EC50 > 100000.0 nM -