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Assay Detail

CHEMBL2210307

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

Binding
Partial noncompetitive inhibition of human F264Y6.51 mutant expressed in HEK293 cells assessed as decrease in SP1-induced [3H]IP accumulation after 20 mins
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Substance-P receptor (CHEMBL249)
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
Kd 3 7.57 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2203707 1 7.77
CHEMBL2203703 1 7.54
CHEMBL2203705 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2203707 Kd = 16.98 nM 7.77
CHEMBL2203703 Kd = 28.84 nM 7.54
CHEMBL2203705 Kd = 39.81 nM 7.40