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Assay Detail

CHEMBL745320

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

Binding
Compound was tested for its binding affinity to NK1 receptor in [3H]SP binding assay on rat brain membranes.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

4,4-Diphenyl-7-perhydrothiapyrano[3,4-c]pyrrolone, a new series of substance P receptors antagonists
Grisonl S, Huon C, Peyronel J
Bioorg Med Chem Lett (1995) 5 : 1591 -1594
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.21 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288371 1 8.70
CHEMBL289666 1 8.30
CHEMBL131171 1 8.10
CHEMBL288942 1 7.58
CHEMBL291146 1 7.39
CHEMBL41375 1 7.11
CHEMBL297244 1 6.33
CHEMBL38824 DAPITANT 2.0 1 5.85
CHEMBL295845 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL288371 IC50 = 2.0 nM 8.70
CHEMBL289666 IC50 = 5.0 nM 8.30
CHEMBL131171 IC50 = 8.0 nM 8.10
CHEMBL288942 IC50 = 26.0 nM 7.58
CHEMBL291146 IC50 = 41.0 nM 7.39
CHEMBL41375 IC50 = 77.0 nM 7.11
CHEMBL297244 IC50 = 470.0 nM 6.33
CHEMBL38824 DAPITANT IC50 = 1400.0 nM 5.85
CHEMBL295845 IC50 = 3000.0 nM 5.52