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Assay Detail

CHEMBL855751

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

Functional
Antagonist potency on BK-induced contraction of guinea pig ileum longitudinal smooth muscle
8
Total Activities
8
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 Expert

Target

B2 bradykinin receptor (CHEMBL4111)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Design and synthesis of novel sulfonamide-containing bradykinin hB2 receptor antagonists. 2. Synthesis and structure-activity relationships of alpha,alpha-cycloalkylglycine sulfonamides.
Fattori D, Rossi C, Fincham CI, Caciagli V, Catrambone F, D'Andrea P, Felicetti P, Gensini M, Marastoni E, Nannicini R, Paris M, Terracciano R, Bressan A, Giuliani S, Maggi CA, Meini S, Valenti C, Quartara L.
J Med Chem (2007) 50 : 550 -565
PubMed 17266207 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 8 9.93 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL220596 1 10.40
CHEMBL375689 1 10.00
CHEMBL375820 1 10.00
CHEMBL205093 1 10.00
CHEMBL380273 1 10.00
CHEMBL220595 1 9.80
CHEMBL383167 1 9.70
CHEMBL207939 1 9.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL220596 Kd = 0.03981 nM 10.40
CHEMBL375689 Kd = 0.1 nM 10.00
CHEMBL375820 Kd = 0.1 nM 10.00
CHEMBL205093 Kd = 0.1 nM 10.00
CHEMBL380273 Kd = 0.1 nM 10.00
CHEMBL220595 Kd = 0.1585 nM 9.80
CHEMBL383167 Kd = 0.1995 nM 9.70
CHEMBL207939 Kd = 0.3162 nM 9.50