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Assay Detail

CHEMBL4338739

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

Binding
Binding affinity to human neurotensin receptor 1 stably expressed in CHO cells incubated for 60 mins in presence of NT (8 to 13) without compound washout by Hoechst H33342 staining confocal microscopy analysis
8
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

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
Kd 4 7.90 8.20
pKd 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4457798 1 8.20
CHEMBL4534768 1 7.99
CHEMBL4564746 1 7.82
CHEMBL4537266 1 7.59
CHEMBL4584647 1 -
CHEMBL4463399 1 -
CHEMBL4592541 1 -
CHEMBL4566971 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4457798 Kd = 6.31 nM 8.20
CHEMBL4534768 Kd = 10.23 nM 7.99
CHEMBL4564746 Kd = 15.14 nM 7.82
CHEMBL4537266 Kd = 25.7 nM 7.59
CHEMBL4584647 pKd - -
CHEMBL4463399 pKd - -
CHEMBL4592541 pKd - -
CHEMBL4566971 pKd - -