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Assay Detail

CHEMBL5327158

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Functional
Agonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

Neurotensin(8-13) analogs as dual NTS1 and NTS2 receptor ligands with enhanced effects on a mouse model of Parkinson's disease.
Kühl T, Georgieva MG, Hübner H, Lazarova M, Vogel M, Haas B, Peeva MI, Balacheva AA, Bogdanov IP, Milella L, Ponticelli M, Garev T, Faraone I, Detcheva R, Minchev B, Petkova-Kirova P, Tancheva L, Kalfin R, Atanasov AG, Antonov L, Pajpanova TI, Kirilov K, Gastreich M, Gmeiner P, Imhof D, Tzvetkov NT.
Eur J Med Chem (2023) 254 : 115386 -115386
PubMed 37094450 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 8.54 9.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5420374 1 9.13
CHEMBL5441066 1 9.09
CHEMBL5402152 1 9.07
CHEMBL415788 1 9.06
CHEMBL5434985 1 9.05
CHEMBL5409459 1 8.89
CHEMBL423487 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5420374 EC50 = 0.74 nM 9.13
CHEMBL5441066 EC50 = 0.82 nM 9.09
CHEMBL5402152 EC50 = 0.85 nM 9.07
CHEMBL415788 EC50 = 0.88 nM 9.06
CHEMBL5434985 EC50 = 0.89 nM 9.05
CHEMBL5409459 EC50 = 1.3 nM 8.89
CHEMBL423487 EC50 = 3200.0 nM 5.50