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Assay Detail

CHEMBL692283

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Binding
Activity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileum
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histamine H1 receptor (CHEMBL3943)
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 8 5.38 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14587 1 6.10
CHEMBL14364 1 5.60
CHEMBL14484 1 5.50
CHEMBL274041 1 5.40
CHEMBL15153 1 5.30
CHEMBL14868 1 5.10
CHEMBL15056 1 5.00
CHEMBL14754 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14587 Kd = 794.33 nM 6.10
CHEMBL14364 Kd = 2511.89 nM 5.60
CHEMBL14484 Kd = 3162.28 nM 5.50
CHEMBL274041 Kd = 3981.07 nM 5.40
CHEMBL15153 Kd = 5011.87 nM 5.30
CHEMBL14868 Kd = 7943.28 nM 5.10
CHEMBL15056 Kd = 10000.0 nM 5.00
CHEMBL14754 Kd = 10000.0 nM 5.00