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Assay Detail

CHEMBL4338732

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Functional
Agonist activity at human neurotensin receptor 1 in HT-29 cells assessed as intracellular calcium mobilization by Fura-2 dye based spectrofluorimetry analysis
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HT-29
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Fluorescence Labeling of Neurotensin(8-13) via Arginine Residues Gives Molecular Tools with High Receptor Affinity.
Keller M, Mahuroof SA, Hong Yee V, Carpenter J, Schindler L, Littmann T, Pegoli A, Hübner H, Bernhardt G, Gmeiner P, Holliday ND.
ACS Med Chem Lett (2020) 11 : 16 -22
PubMed 31938457 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
pEC50 6 - -
EC50 3 8.71 8.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4564746 1 8.99
CHEMBL415788 1 8.92
CHEMBL4457798 1 8.23
CHEMBL4534768 1 -
CHEMBL4584647 1 -
CHEMBL4537266 1 -
CHEMBL4463399 1 -
CHEMBL4592541 1 -
CHEMBL4566971 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4564746 EC50 = 1.023 nM 8.99
CHEMBL415788 EC50 = 1.202 nM 8.92
CHEMBL4457798 EC50 = 5.888 nM 8.23
CHEMBL4534768 pEC50 - -
CHEMBL4584647 pEC50 - -
CHEMBL4537266 pEC50 - -
CHEMBL4463399 pEC50 - -
CHEMBL4592541 pEC50 - -
CHEMBL4566971 pEC50 - -