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Assay Detail

CHEMBL1768194

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Functional
Agonist activity at human NTS2 receptor expressed in HEK293 cells assessed as inhibition of constitutive activity on MAPK-mediated luciferase activity
5
Total Activities
5
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 2 (CHEMBL2514)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of highly potent and neurotensin receptor 2 selective neurotensin mimetics.
Einsiedel J, Held C, Hervet M, Plomer M, Tschammer N, Hübner H, Gmeiner P.
J Med Chem (2011) 54 : 2915 -2923
PubMed 21446649 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.35 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL407196 NEUROTENSIN 1 6.96
CHEMBL1766825 1 6.32
CHEMBL1766946 1 6.23
CHEMBL1766945 1 6.16
CHEMBL1766944 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL407196 NEUROTENSIN EC50 = 110.0 nM 6.96
CHEMBL1766825 EC50 = 480.0 nM 6.32
CHEMBL1766946 EC50 = 590.0 nM 6.23
CHEMBL1766945 EC50 = 690.0 nM 6.16
CHEMBL1766944 EC50 = 840.0 nM 6.08