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Assay Detail

CHEMBL4815477

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

Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
29
Total Activities
29
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Right cardiac atrium
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H2 receptor (CHEMBL2882)
Type SINGLE PROTEIN
Organism Cavia porcellus

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 28 7.41 8.24
pEC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4860528 1 8.24
CHEMBL4856059 1 8.12
CHEMBL4846380 1 8.01
CHEMBL4861704 1 8.00
CHEMBL4870510 1 7.97
CHEMBL4865965 1 7.93
CHEMBL4864852 1 7.91
CHEMBL4869389 1 7.89
CHEMBL4853668 1 7.80
CHEMBL4869194 1 7.65
CHEMBL4867962 1 7.63
CHEMBL4848697 1 7.63
CHEMBL4863347 1 7.61
CHEMBL4852212 1 7.59
CHEMBL4875600 1 7.58
CHEMBL4858849 1 7.46
CHEMBL4848026 1 7.42
CHEMBL4876025 1 7.40
CHEMBL4850448 1 7.32
CHEMBL4876267 1 7.26
CHEMBL4856602 1 7.18
CHEMBL4853772 1 7.05
CHEMBL4845733 1 6.83
CHEMBL4866734 1 6.76
CHEMBL4854278 1 6.65
CHEMBL4850490 1 6.31
CHEMBL90 HISTAMINE 4.0 1 6.16
CHEMBL4863523 1 6.14
CHEMBL4856200 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4860528 EC50 = 5.754 nM 8.24
CHEMBL4856059 EC50 = 7.586 nM 8.12
CHEMBL4846380 EC50 = 9.772 nM 8.01
CHEMBL4861704 EC50 = 10.0 nM 8.00
CHEMBL4870510 EC50 = 10.72 nM 7.97
CHEMBL4865965 EC50 = 11.75 nM 7.93
CHEMBL4864852 EC50 = 12.3 nM 7.91
CHEMBL4869389 EC50 = 12.88 nM 7.89
CHEMBL4853668 EC50 = 15.85 nM 7.80
CHEMBL4869194 EC50 = 22.39 nM 7.65
CHEMBL4867962 EC50 = 23.44 nM 7.63
CHEMBL4848697 EC50 = 23.44 nM 7.63
CHEMBL4863347 EC50 = 24.55 nM 7.61
CHEMBL4852212 EC50 = 25.7 nM 7.59
CHEMBL4875600 EC50 = 26.3 nM 7.58
CHEMBL4858849 EC50 = 34.67 nM 7.46
CHEMBL4848026 EC50 = 38.02 nM 7.42
CHEMBL4876025 EC50 = 39.81 nM 7.40
CHEMBL4850448 EC50 = 47.86 nM 7.32
CHEMBL4876267 EC50 = 54.95 nM 7.26
CHEMBL4856602 EC50 = 66.07 nM 7.18
CHEMBL4853772 EC50 = 89.13 nM 7.05
CHEMBL4845733 EC50 = 147.91 nM 6.83
CHEMBL4866734 EC50 = 173.78 nM 6.76
CHEMBL4854278 EC50 = 223.87 nM 6.65
CHEMBL4850490 EC50 = 489.78 nM 6.31
CHEMBL90 HISTAMINE EC50 = 691.83 nM 6.16
CHEMBL4863523 EC50 = 724.44 nM 6.14
CHEMBL4856200 pEC50 - -