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Assay Detail

CHEMBL693276

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

Binding
Activity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atrium
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Cardiac atrium
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Development of a new class of nonimidazole histamine H(3) receptor ligands with combined inhibitory histamine N-methyltransferase activity.
Apelt J, Ligneau X, Pertz HH, Arrang JM, Ganellin CR, Schwartz JC, Schunack W, Stark H.
J Med Chem (2002) 45 : 1128 -1141
PubMed 11855993 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 4.77 5.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14587 1 5.30
CHEMBL274041 1 5.00
CHEMBL276938 1 4.90
CHEMBL14868 1 4.70
CHEMBL14484 1 4.70
CHEMBL14754 1 4.70
CHEMBL14364 1 4.70
CHEMBL15056 1 4.50
CHEMBL15153 1 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14587 Kd = 5011.87 nM 5.30
CHEMBL274041 Kd = 10000.0 nM 5.00
CHEMBL276938 Kd = 12589.25 nM 4.90
CHEMBL14868 Kd = 19952.62 nM 4.70
CHEMBL14484 Kd = 19952.62 nM 4.70
CHEMBL14754 Kd = 19952.62 nM 4.70
CHEMBL14364 Kd = 19952.62 nM 4.70
CHEMBL15056 Kd = 31622.78 nM 4.50
CHEMBL15153 Kd = 39810.72 nM 4.40