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Assay Detail

CHEMBL809502

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

Binding
Inhibitory concentration for displacement of [3H]-Substance P (SP) in human IM-9 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type IM-9
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

2-Aryl-1-azabicyclo[2.2.2]octanes as novel nonpeptide substance P antagonists
Lowe JA, Ewing FE, Snider R, Longo KP, Constantine JW, Lebel WS, Woody HA, Bordner J
Bioorg Med Chem Lett (1994) 4 : 839 -842
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.02 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16192 CP-96345 1 8.70
CHEMBL122580 1 8.04
CHEMBL166610 1 7.70
CHEMBL2115528 1 7.41
CHEMBL166816 1 6.85
CHEMBL354564 1 6.80
CHEMBL332140 1 6.64
CHEMBL167066 1 6.62
CHEMBL352697 1 6.46
CHEMBL353416 1 6.16
CHEMBL119947 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16192 CP-96345 IC50 = 2.0 nM 8.70
CHEMBL122580 IC50 = 9.2 nM 8.04
CHEMBL166610 IC50 = 20.0 nM 7.70
CHEMBL2115528 IC50 = 39.0 nM 7.41
CHEMBL166816 IC50 = 140.0 nM 6.85
CHEMBL354564 IC50 = 160.0 nM 6.80
CHEMBL332140 IC50 = 230.0 nM 6.64
CHEMBL167066 IC50 = 240.0 nM 6.62
CHEMBL352697 IC50 = 350.0 nM 6.46
CHEMBL353416 IC50 = 700.0 nM 6.16
CHEMBL119947 IC50 = 1400.0 nM 5.85