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Assay Detail

CHEMBL870326

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

Binding
Displacement of [125I]Tyr3-NT from human NTS1R expressed in HT29 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HT-29
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Toward stable N4-modified neurotensins for NTS1-receptor-targeted tumor imaging with 99mTc.
Nock BA, Nikolopoulou A, Reubi JC, Maes V, Conrath P, Tourwé D, Maina T.
J Med Chem (2006) 49 : 4767 -4776
PubMed 16854083 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 9.20 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2369722 Demotensin 1 1 9.49
CHEMBL1791383 DEMOTENSIN 2 1 9.39
CHEMBL407196 NEUROTENSIN 1 9.21
CHEMBL375002 DEMOTENSIN 4 1 9.07
CHEMBL219862 DEMOTENSIN 3 1 8.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2369722 Demotensin 1 IC50 = 0.32 nM 9.49
CHEMBL1791383 DEMOTENSIN 2 IC50 = 0.41 nM 9.39
CHEMBL407196 NEUROTENSIN IC50 = 0.62 nM 9.21
CHEMBL375002 DEMOTENSIN 4 IC50 = 0.85 nM 9.07
CHEMBL219862 DEMOTENSIN 3 IC50 = 1.5 nM 8.82