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Assay Detail

CHEMBL3101955

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

Binding
Agonist activity at NTR1 in human U2OS cells after 1 hr by beta-arrestin GFP reporter gene assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U2OS
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neurotensin receptor type 1 (CHEMBL4123)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Imidazole-derived agonists for the neurotensin 1 receptor.
Hershberger PM, Hedrick MP, Peddibhotla S, Mangravita-Novo A, Gosalia P, Li Y, Gray W, Vicchiarelli M, Smith LH, Chung TD, Thomas JB, Caron MG, Pinkerton AB, Barak LS, Roth GP.
Bioorg Med Chem Lett (2014) 24 : 262 -267
PubMed 24332089 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 5.05 6.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL508044 1 6.12
CHEMBL3099772 1 6.01
CHEMBL3099773 1 5.70
CHEMBL3099769 1 5.64
CHEMBL3099777 1 5.42
CHEMBL3099767 1 5.28
CHEMBL3099768 1 5.04
CHEMBL3099774 1 5.03
CHEMBL506981 REMINERTANT 3.0 1 4.51
CHEMBL3099771 1 4.34
CHEMBL3099775 1 4.25
CHEMBL3099780 1 4.18
CHEMBL3099776 1 4.14
CHEMBL3099783 1 -
CHEMBL3099782 1 -
CHEMBL3099781 1 -
CHEMBL3099779 1 -
CHEMBL3099778 1 -
CHEMBL3099770 1 -
CHEMBL2431105 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL508044 EC50 = 750.0 nM 6.12
CHEMBL3099772 EC50 = 970.0 nM 6.01
CHEMBL3099773 EC50 = 2000.0 nM 5.70
CHEMBL3099769 EC50 = 2300.0 nM 5.64
CHEMBL3099777 EC50 = 3800.0 nM 5.42
CHEMBL3099767 EC50 = 5200.0 nM 5.28
CHEMBL3099768 EC50 = 9200.0 nM 5.04
CHEMBL3099774 EC50 = 9400.0 nM 5.03
CHEMBL506981 REMINERTANT EC50 = 31000.0 nM 4.51
CHEMBL3099771 EC50 = 46000.0 nM 4.34
CHEMBL3099775 EC50 = 56000.0 nM 4.25
CHEMBL3099780 EC50 = 66000.0 nM 4.18
CHEMBL3099776 EC50 = 72000.0 nM 4.14
CHEMBL3099783 EC50 > 80000.0 nM -
CHEMBL3099782 EC50 > 80000.0 nM -
CHEMBL3099781 EC50 > 80000.0 nM -
CHEMBL3099779 EC50 > 80000.0 nM -
CHEMBL3099778 EC50 > 80000.0 nM -
CHEMBL3099770 EC50 > 80000.0 nM -
CHEMBL2431105 EC50 > 80000.0 nM -