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Assay Detail

CHEMBL857121

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Functional
H1-antihistamine activity in guinea pig ileum
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histamine H1 receptor (CHEMBL3943)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Studies on 1,2,3-triazoles. 13. (Piperazinylalkoxy) [1]benzopyrano[2,3-d]-1,2,3-triazol-9(1H)-ones with combined H1-antihistamine and mast cell stabilizing properties.
Buckle DR, Rockell CJ, Smith H, Spicer BA.
J Med Chem (1986) 29 : 2262 -2267
PubMed 2431143 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 8.73 9.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL534 KETOTIFEN 4.0 1 9.50
CHEMBL74870 1 9.10
CHEMBL511 PYRILAMINE 4.0 1 9.10
CHEMBL308791 1 8.80
CHEMBL420934 1 8.40
CHEMBL74989 1 8.40
CHEMBL420567 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL534 KETOTIFEN Kd = 0.3162 nM 9.50
CHEMBL74870 Kd = 0.7943 nM 9.10
CHEMBL511 PYRILAMINE Kd = 0.7943 nM 9.10
CHEMBL308791 Kd = 1.585 nM 8.80
CHEMBL420934 Kd = 3.981 nM 8.40
CHEMBL74989 Kd = 3.981 nM 8.40
CHEMBL420567 Kd = 15.85 nM 7.80