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Assay Detail

CHEMBL3625239

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

Binding
Displacement of [125I]-Tyr3-NT from human NTS2 receptor expressed in 1321N1 cell membranes incubated for 30 mins by gamma-counting based competitive radioligand binding assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type 1321-N1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neurotensin receptor type 2 (CHEMBL2514)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and Characterization in Vitro and in Vivo of (l)-(Trimethylsilyl)alanine Containing Neurotensin Analogues.
Fanelli R, Besserer-Offroy É, René A, Côté J, Tétreault P, Collerette-Tremblay J, Longpré JM, Leduc R, Martinez J, Sarret P, Cavelier F.
J Med Chem (2015) 58 : 7785 -7795
PubMed 26348111 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.53 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3622802 1 9.59
CHEMBL415788 1 8.12
CHEMBL3622806 1 7.67
CHEMBL3622803 1 7.54
CHEMBL3622805 1 7.53
CHEMBL3622801 1 6.39
CHEMBL3622804 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3622802 IC50 = 0.26 nM 9.59
CHEMBL415788 IC50 = 7.52 nM 8.12
CHEMBL3622806 IC50 = 21.2 nM 7.67
CHEMBL3622803 IC50 = 28.9 nM 7.54
CHEMBL3622805 IC50 = 29.7 nM 7.53
CHEMBL3622801 IC50 = 405.0 nM 6.39
CHEMBL3622804 IC50 = 1425.0 nM 5.85