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Assay Detail

CHEMBL4338741

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

Binding
Displacement of [3H] UR-MK300 from human neurotensin receptor 2 in HEK293 cells homogenate 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 HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neurotensin receptor type 2 (CHEMBL2514)
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 8.68 9.13
pKi 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415788 1 9.13
CHEMBL4534768 1 9.02
CHEMBL4564746 1 8.92
CHEMBL4537266 1 8.46
CHEMBL4457798 1 8.40
CHEMBL4592541 1 8.14
CHEMBL4463399 1 -
CHEMBL4584647 1 -
CHEMBL4566971 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415788 Ki = 0.7413 nM 9.13
CHEMBL4534768 Ki = 0.955 nM 9.02
CHEMBL4564746 Ki = 1.202 nM 8.92
CHEMBL4537266 Ki = 3.467 nM 8.46
CHEMBL4457798 Ki = 3.981 nM 8.40
CHEMBL4592541 Ki = 7.244 nM 8.14
CHEMBL4463399 pKi - -
CHEMBL4584647 pKi - -
CHEMBL4566971 pKi - -