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Assay Detail

CHEMBL842694

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

Binding
Tested for binding affinity against H265A mutant NK1 receptor using [125]SP radioligand in COS cells.
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type COS
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis of a substance P antagonist with a somatostatin scaffold: factors affecting agonism/antagonism at GPCRs and the role of pseudosymmetry.
Liu J, Underwood DJ, Cascieri MA, Rohrer SP, Cantin LD, Chicchi G, Smith AB, Hirschmann R.
J Med Chem (2000) 43 : 3827 -3831
PubMed 11052787 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.07 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL235363 SUBSTANCE P 1.0 1 8.96
CHEMBL2112246 1 5.21
CHEMBL2369630 1 5.09
CHEMBL2112245 1 5.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL235363 SUBSTANCE P IC50 = 1.1 nM 8.96
CHEMBL2112246 IC50 = 6100.0 nM 5.21
CHEMBL2369630 IC50 = 8200.0 nM 5.09
CHEMBL2112245 IC50 = 9600.0 nM 5.02