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Assay Detail

CHEMBL3365188

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

Functional
Antagonist activity at NTSR1 (unknown origin) expressed in CHO cells assessed as inhibition of NT(8-13) peptide-induced change in intracellular Ca2+ level preincubated for 45 mins by FLIPR assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neurotensin receptor type 1 (CHEMBL4123)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of indole full agonists of the neurotensin receptor 1 (NTSR1).
Di Fruscia P, He Y, Koenig M, Tabrizifard S, Nieto A, McDonald PH, Kamenecka TM.
Bioorg Med Chem Lett (2014) 24 : 3974 -3978
PubMed 24997685 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.75 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3040381 1 8.40
CHEMBL506981 REMINERTANT 3.0 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3040381 IC50 = 4.0 nM 8.40
CHEMBL506981 REMINERTANT IC50 = 82.0 nM 7.09