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Assay Detail

CHEMBL812542

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

Binding
Binding affinity against human Tachykinin receptor 1 expressed in astrocytoma UC11MG cells using [125I]- SP radioligand
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type UC11MG
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

A non-peptide NK1 receptor agonist showing subpicomolar affinity.
Cappelli A, Giuliani G, Pericot Mohr Gl Gl, Gallelli A, Anzini M, Vomero S, Cupello A, Scarrone S, Matarrese M, Moresco RM, Fazio F, Finetti F, Morbidelli L, Ziche M.
J Med Chem (2004) 47 : 1315 -1318
PubMed 14998319 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.85 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL281797 1 11.00
CHEMBL26761 1 10.96
CHEMBL413027 1 10.52
CHEMBL282853 1 10.12
CHEMBL235363 SUBSTANCE P 1.0 1 9.92
CHEMBL24829 1 9.66
CHEMBL24999 1 8.80
CHEMBL281491 1 8.51
CHEMBL25521 1 8.05
CHEMBL25398 1 7.96
CHEMBL25639 1 7.80
CHEMBL23982 1 7.77
CHEMBL24136 1 7.58
CHEMBL24194 1 7.28
CHEMBL25065 1 6.75
CHEMBL277004 1 -
CHEMBL25058 1 -
CHEMBL24872 1 -
CHEMBL24135 1 -
CHEMBL24894 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL281797 IC50 = 0.01 nM 11.00
CHEMBL26761 IC50 = 0.011 nM 10.96
CHEMBL413027 IC50 = 0.03 nM 10.52
CHEMBL282853 IC50 = 0.075 nM 10.12
CHEMBL235363 SUBSTANCE P IC50 = 0.12 nM 9.92
CHEMBL24829 IC50 = 0.22 nM 9.66
CHEMBL24999 IC50 = 1.6 nM 8.80
CHEMBL281491 IC50 = 3.1 nM 8.51
CHEMBL25521 IC50 = 9.0 nM 8.05
CHEMBL25398 IC50 = 11.0 nM 7.96
CHEMBL25639 IC50 = 16.0 nM 7.80
CHEMBL23982 IC50 = 17.0 nM 7.77
CHEMBL24136 IC50 = 26.0 nM 7.58
CHEMBL24194 IC50 = 52.0 nM 7.28
CHEMBL25065 IC50 = 180.0 nM 6.75
CHEMBL277004 IC50 = 0.0001 nM -
CHEMBL25058 IC50 > 1000.0 nM -
CHEMBL24872 IC50 > 1000.0 nM -
CHEMBL24135 IC50 = 0.0017 nM -
CHEMBL24894 IC50 > 1000.0 nM -