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Assay Detail

CHEMBL754790

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

Binding
Binding affinity towards neurotensin receptor in membranes prepared from HT-29 cell line, relative to [111In]-labeled neurotensin peptide
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HT-29
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Novel bioactive and stable neurotensin peptide analogues capable of delivering radiopharmaceuticals and molecular beacons to tumors.
Achilefu S, Srinivasan A, Schmidt MA, Jimenez HN, Bugaj JE, Erion JL.
J Med Chem (2003) 46 : 3403 -3411
PubMed 12852770 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 8.55 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL407196 NEUROTENSIN 1 9.70
CHEMBL408127 1 9.52
CHEMBL408381 1 9.52
CHEMBL2370478 1 9.40
CHEMBL409477 1 9.40
CHEMBL408638 1 9.40
CHEMBL404942 1 9.40
CHEMBL3142915 1 9.30
CHEMBL2369628 1 9.30
CHEMBL386387 1 9.22
CHEMBL2369133 1 9.22
CHEMBL3706654 1 9.22
CHEMBL3706655 1 8.92
CHEMBL437707 1 8.82
CHEMBL424896 1 8.60
CHEMBL3706653 1 8.47
CHEMBL413192 1 8.20
CHEMBL2369627 1 7.99
CHEMBL405160 1 7.94
CHEMBL407187 1 7.93
CHEMBL405804 1 7.66
CHEMBL2369629 1 7.66
CHEMBL2370477 1 7.61
CHEMBL413010 1 7.37
CHEMBL2370480 1 7.22
CHEMBL2370479 1 6.97
CHEMBL410289 1 6.95
CHEMBL436717 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL407196 NEUROTENSIN IC50 = 0.2 nM 9.70
CHEMBL408127 IC50 = 0.3 nM 9.52
CHEMBL408381 IC50 = 0.3 nM 9.52
CHEMBL2370478 IC50 = 0.4 nM 9.40
CHEMBL409477 IC50 = 0.4 nM 9.40
CHEMBL408638 IC50 = 0.4 nM 9.40
CHEMBL404942 IC50 = 0.4 nM 9.40
CHEMBL3142915 IC50 = 0.5 nM 9.30
CHEMBL2369628 IC50 = 0.5 nM 9.30
CHEMBL386387 IC50 = 0.6 nM 9.22
CHEMBL2369133 IC50 = 0.6 nM 9.22
CHEMBL3706654 IC50 = 0.6 nM 9.22
CHEMBL3706655 IC50 = 1.2 nM 8.92
CHEMBL437707 IC50 = 1.5 nM 8.82
CHEMBL424896 IC50 = 2.5 nM 8.60
CHEMBL3706653 IC50 = 3.4 nM 8.47
CHEMBL413192 IC50 = 6.3 nM 8.20
CHEMBL2369627 IC50 = 10.2 nM 7.99
CHEMBL405160 IC50 = 11.5 nM 7.94
CHEMBL407187 IC50 = 11.87 nM 7.93
CHEMBL405804 IC50 = 21.7 nM 7.66
CHEMBL2369629 IC50 = 22.1 nM 7.66
CHEMBL2370477 IC50 = 24.6 nM 7.61
CHEMBL413010 IC50 = 42.4 nM 7.37
CHEMBL2370480 IC50 = 59.6 nM 7.22
CHEMBL2370479 IC50 = 106.0 nM 6.97
CHEMBL410289 IC50 = 113.0 nM 6.95
CHEMBL436717 IC50 > 1000.0 nM -