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Assay Detail

CHEMBL750293

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

Binding
Tested for inhibition of tachykinin 1 (NK1) receptor in rat brain synaptosomal membranes using [125I]BH-SP as radioligand
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Substance-P receptor (CHEMBL4027)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Application of the multipin peptide synthesis technique for peptide receptor binding studies: Substance P as A model system
Wang J, Bray AM, DiPasquale AJ, Maeji N, Geysen H
Bioorg Med Chem Lett (1993) 3 : 447 -450
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.71 9.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL235363 SUBSTANCE P 1.0 1 9.43
CHEMBL2370874 1 8.64
CHEMBL2370873 1 7.51
CHEMBL217406 NEUROKININ A 1 7.50
CHEMBL436706 KASSININ 1 7.12
CHEMBL437797 NEUROKININ B 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL235363 SUBSTANCE P IC50 = 0.37 nM 9.43
CHEMBL2370874 IC50 = 2.3 nM 8.64
CHEMBL2370873 IC50 = 31.0 nM 7.51
CHEMBL217406 NEUROKININ A IC50 = 32.0 nM 7.50
CHEMBL436706 KASSININ IC50 = 75.0 nM 7.12
CHEMBL437797 NEUROKININ B IC50 = 870.0 nM 6.06