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Assay Detail

CHEMBL4815488

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Functional
Agonist activity at human histamine D2L receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the H<sub>2</sub>R and D<sub>3</sub>R.
Biselli S, Bresinsky M, Tropmann K, Forster L, Honisch C, Buschauer A, Bernhardt G, Pockes S.
Eur J Med Chem (2021) 214 : 113190 -113190
PubMed 33548637 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 5.94 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL240773 QUINPIROLE 2.0 1 7.55
CHEMBL4856059 1 6.47
CHEMBL4875600 1 6.23
CHEMBL4860528 1 5.98
CHEMBL4846380 1 5.97
CHEMBL4853107 1 5.96
CHEMBL4848815 1 5.95
CHEMBL4853772 1 5.82
CHEMBL4856005 1 5.78
CHEMBL4857560 1 5.77
CHEMBL4853668 1 5.76
CHEMBL4867962 1 5.57
CHEMBL4846201 1 5.53
CHEMBL4846638 1 5.49
CHEMBL4865765 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL240773 QUINPIROLE EC50 = 28.18 nM 7.55
CHEMBL4856059 EC50 = 338.84 nM 6.47
CHEMBL4875600 EC50 = 588.84 nM 6.23
CHEMBL4860528 EC50 = 1047.13 nM 5.98
CHEMBL4846380 EC50 = 1071.52 nM 5.97
CHEMBL4853107 EC50 = 1096.48 nM 5.96
CHEMBL4848815 EC50 = 1122.02 nM 5.95
CHEMBL4853772 EC50 = 1513.56 nM 5.82
CHEMBL4856005 EC50 = 1659.59 nM 5.78
CHEMBL4857560 EC50 = 1698.24 nM 5.77
CHEMBL4853668 EC50 = 1737.8 nM 5.76
CHEMBL4867962 EC50 = 2691.53 nM 5.57
CHEMBL4846201 EC50 = 2951.21 nM 5.53
CHEMBL4846638 EC50 = 3235.94 nM 5.49
CHEMBL4865765 EC50 = 5370.32 nM 5.27