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Assay Detail

CHEMBL4255799

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

Binding
Displacement of 125I-[Tyr3]-NT from human NTS1 receptor expressed in CHO-K1 cell membranes after 60 mins by gamma-counting method
13
Total Activities
13
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

In Search of the Optimal Macrocyclization Site for Neurotensin.
Sousbie M, Besserer-Offroy É, Brouillette RL, Longpré JM, Leduc R, Sarret P, Marsault É.
ACS Med Chem Lett (2018) 9 : 227 -232
PubMed 29541365 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.55 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415788 1 9.10
CHEMBL4289739 1 6.40
CHEMBL4279055 1 5.85
CHEMBL4283301 1 5.77
CHEMBL4286324 1 5.12
CHEMBL4286652 1 5.00
CHEMBL4294207 1 4.99
CHEMBL4279408 1 4.84
CHEMBL4291157 1 4.77
CHEMBL4290088 1 4.70
CHEMBL4284772 1 4.53
CHEMBL4292651 1 -
CHEMBL4294560 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415788 IC50 = 0.8 nM 9.10
CHEMBL4289739 IC50 = 400.0 nM 6.40
CHEMBL4279055 IC50 = 1400.0 nM 5.85
CHEMBL4283301 IC50 = 1700.0 nM 5.77
CHEMBL4286324 IC50 = 7600.0 nM 5.12
CHEMBL4286652 IC50 = 10000.0 nM 5.00
CHEMBL4294207 IC50 = 10300.0 nM 4.99
CHEMBL4279408 IC50 = 14300.0 nM 4.84
CHEMBL4291157 IC50 = 17000.0 nM 4.77
CHEMBL4290088 IC50 = 19800.0 nM 4.70
CHEMBL4284772 IC50 = 29800.0 nM 4.53
CHEMBL4292651 IC50 > 100000.0 nM -
CHEMBL4294560 IC50 > 100000.0 nM -