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Assay Detail

CHEMBL4338737

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

Binding
Displacement of [3H] UR-MK300 from human neurotensin receptor 1 stably expressed in CHO cells incubated in dark after 30 mins by liquid scintillation counter analysis
9
Total Activities
9
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
Ki 6 8.66 8.89
pKi 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4463399 1 8.89
CHEMBL4457798 1 8.88
CHEMBL4537266 1 8.81
CHEMBL4534768 1 8.61
CHEMBL4584647 1 8.60
CHEMBL4564746 1 8.15
CHEMBL415788 1 -
CHEMBL4592541 1 -
CHEMBL4566971 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4463399 Ki = 1.288 nM 8.89
CHEMBL4457798 Ki = 1.318 nM 8.88
CHEMBL4537266 Ki = 1.549 nM 8.81
CHEMBL4534768 Ki = 2.455 nM 8.61
CHEMBL4584647 Ki = 2.512 nM 8.60
CHEMBL4564746 Ki = 7.079 nM 8.15
CHEMBL415788 pKi - -
CHEMBL4592541 pKi - -
CHEMBL4566971 pKi - -