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Assay Detail

CHEMBL4338736

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 expressed in HT-29 cells incubated in dark after 30 mins by liquid scintillation counter analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 9 8.78 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415788 1 9.89
CHEMBL4463399 1 9.12
CHEMBL4457798 1 8.86
CHEMBL4537266 1 8.70
CHEMBL4534768 1 8.66
CHEMBL4592541 1 8.57
CHEMBL4566971 1 8.45
CHEMBL4564746 1 8.38
CHEMBL4584647 1 8.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415788 Ki = 0.1288 nM 9.89
CHEMBL4463399 Ki = 0.7586 nM 9.12
CHEMBL4457798 Ki = 1.38 nM 8.86
CHEMBL4537266 Ki = 1.995 nM 8.70
CHEMBL4534768 Ki = 2.188 nM 8.66
CHEMBL4592541 Ki = 2.692 nM 8.57
CHEMBL4566971 Ki = 3.548 nM 8.45
CHEMBL4564746 Ki = 4.169 nM 8.38
CHEMBL4584647 Ki = 4.266 nM 8.37