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Assay Detail

CHEMBL3625720

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

Binding
Agonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing hNTS1-GFP10/RlucII-beta-arrestin 2 assessed as beta-arrestin2 recruitment incubated for 15 mins by BRET assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neurotensin receptor type 1 (CHEMBL4123)
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
EC50 6 8.60 9.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3622803 1 9.47
CHEMBL3622802 1 8.83
CHEMBL415788 1 8.73
CHEMBL3622805 1 8.38
CHEMBL3622801 1 7.58
CHEMBL3622804 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3622803 EC50 = 0.34 nM 9.47
CHEMBL3622802 EC50 = 1.49 nM 8.83
CHEMBL415788 EC50 = 1.85 nM 8.73
CHEMBL3622805 EC50 = 4.19 nM 8.38
CHEMBL3622801 EC50 = 26.6 nM 7.58
CHEMBL3622804 EC50 > 1000.0 nM -