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Assay Detail

CHEMBL2433839

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Binding
Agonist activity at NTR1 (unknown origin) expressed in CHOK1 cells by beta-arrestin assay
2
Total Activities
2
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

Discovery of ML314, a Brain Penetrant Non-Peptidic β-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor.
Peddibhotla S, Hedrick MP, Hershberger P, Maloney PR, Li Y, Milewski M, Gosalia P, Gray W, Mehta A, Sugarman E, Hood B, Suyama E, Nguyen K, Heynen-Genel S, Vasile S, Salaniwal S, Stonich D, Su Y, Mangravita-Novo A, Vicchiarelli M, Roth GP, Smith LH, Chung TD, Hanson GR, Thomas JB, Caron MG, Barak LS, Pinkerton AB.
ACS Med Chem Lett (2013) 4 : 846 -851
PubMed 24611085 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 5.47 5.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2431120 1 5.47
CHEMBL508044 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2431120 EC50 = 3410.0 nM 5.47
CHEMBL508044 EC50 > 33000.0 nM -