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Assay Detail

CHEMBL4375476

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

Binding
Positive allosteric modulation of recombinant human NTR1 expressed in HEK293 cells assessed as increase in [125I]-neurotensin binding measured after 45 mins
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators.
Pinkerton AB, Peddibhotla S, Yamamoto F, Slosky LM, Bai Y, Maloney P, Hershberger P, Hedrick MP, Falter B, Ardecky RJ, Smith LH, Chung TDY, Jackson MR, Caron MG, Barak LS.
J Med Chem (2019) 62 : 8357 -8363
PubMed 31390201 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 6.85 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4576388 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4576388 EC50 = 140.0 nM 6.85