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Assay Detail

CHEMBL2215516

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Functional
Agonist activity at human NK3 H316W mutant expressed in HEK293 cells assessed as [3H]IP accumulation after 45 mins
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuromedin-K receptor (CHEMBL4429)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.
Bissantz C, Bohnert C, Hoffmann T, Marcuz A, Schnider P, Malherbe P.
J Med Chem (2012) 55 : 5061 -5076
PubMed 22574973 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 8.46 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL583102 1 8.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL583102 EC50 = 3.48 nM 8.46