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Assay Detail

CHEMBL879280

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

Functional
Antagonistic potency for NK-1 receptor was determined in vitro, using isolated rabbit vena cava.
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Vena cava
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Substance-P receptor (CHEMBL249)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The dipeptide neurokinin-1 receptor antagonist S19752 is a potent and long-acting inhibitor of bronchoconstriction when administered by aerosol to the guinea pig in vivo
Fauchere J, Kucharczyk N, Jacoby E, Lonchampt M, Robineau P, Dacquet C, Regoli D, Canet E
Bioorg Med Chem Lett (1997) 7 : 203 -208
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 8.65 8.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL441225 CP-99994 1 8.90
CHEMBL22870 L-732138 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL441225 CP-99994 Kd = 1.259 nM 8.90
CHEMBL22870 L-732138 Kd = 3.981 nM 8.40