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Displacement of [3H]NT(8-13) from human NTSR1 F2.65C mutant expressed in HEK293 cell membranes by radioligand displacement assay
Assay data:5 Active, 5 Activity ≤ 1 µM, 5 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Displacement of [3H]NT(8-13) from human NTSR2 expressed in HEK293 cell membranes by radioligand displacement assay
Displacement of [3H]neurotensin from human NTSR1 expressed in CHO cell membranes by radioligand depletion assay
Assay data:5 Active, 1 Activity ≤ 1 nM, 5 Activity ≤ 1 µM, 5 Tested
Myorelaxant activity in Sprague-Dawley rat ileum assessed as reduction in carbachol-induced contractions by force transducer relaxation assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Agonist activity at human NTS1 expressed in HEK293 cells co-expressing Galphaq/RlucII/GFP10-Ggamma1/Gbeta1 assessed as increase in Galphaq activation incubated for 10 mins in presence of coelenterazine 400A by BRET assay
Assay data:12 Active, 4 Activity ≤ 1 nM, 11 Activity ≤ 1 µM, 13 Tested
Displacement of [125I]-neurotensin from human recombinant NTS2 stably expressed in human 1321N1 cell membranes incubated for 60 mins by gamma counter method
Assay data:18 Active, 11 Activity ≤ 1 nM, 18 Activity ≤ 1 µM, 18 Tested
Displacement of [125I]-neurotensin from human recombinant NTS1 stably expressed in CHO-K1 cell membranes incubated for 60 mins by gamma counter method
Assay data:18 Active, 3 Activity ≤ 1 nM, 14 Activity ≤ 1 µM, 18 Tested
Binding affinity to human NTS1R
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Displacement of [3H] UR-MK300 from human neurotensin receptor 2 in HEK293 cells homogenate incubated in dark after 30 mins by liquid scintillation counter analysis
Assay data:6 Active, 2 Activity ≤ 1 nM, 6 Activity ≤ 1 µM, 9 Tested
Displacement of [3H] UR-MK300 from human neurotensin receptor 1 expressed in HT-29 cells incubated in dark after 30 mins by liquid scintillation counter analysis
Assay data:9 Active, 2 Activity ≤ 1 nM, 9 Activity ≤ 1 µM, 9 Tested
Binding affinity to human neurotensin receptor 1
Assay data:3 Active, 2 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
Agonist activity at human neurotensin receptor 1 in HT-29 cells assessed as intracellular calcium mobilization by Fura-2 dye based spectrofluorimetry analysis
Assay data:3 Active, 3 Activity ≤ 1 µM, 9 Tested
Agonist activity at human neurotensin receptor 1 expressed in CHO cells assessed as increase in intracellular calcium by Fluo-4 dye based fluorescence assay
Assay data:3 Active, 3 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 9 Tested
Displacement of [3H]UR-MK300 from human NSTR1 in HT-29 cells incubated for 2 hrs by liquid scintillation counter
Assay data:10 Active, 5 Activity ≤ 1 nM, 11 Activity ≤ 1 µM, 11 Tested
Displacement of 125I-[Tyr3]-NT from HA-tagged human NTS1 R212E mutant receptor expressed in HEK293 cell membranes after 30 mins by gamma counting analysis
Assay data:3 Active, 3 Activity ≤ 1 µM, 5 Tested
Displacement of 125I-[Tyr3]-NT from human NTS2 receptor expressed in human 1321N1 cell membranes after 30 mins by gamma counting analysis
Assay data:7 Active, 5 Activity ≤ 1 µM, 7 Tested
Displacement of 125I-[Tyr3]-NT from human NTS1 receptor expressed in CHOK1 cell membranes after 30 mins by gamma counting analysis
Assay data:4 Active, 3 Activity ≤ 1 µM, 7 Tested
Displacement of 125I-[Tyr3]-NT from human NTS1 receptor expressed in CHO-K1 cell membranes after 60 mins by gamma-counting method
Assay data:6 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 13 Tested
Agonist activity at GFP10/beta-arrestin2-Rluc2 fused human NTS1 expressed in CHO-K1 cell membranes assessed as beta-arrestin2 recruitment after 20 mins by BRET assay
Assay data:12 Active, 1 Activity ≤ 1 nM, 11 Activity ≤ 1 µM, 13 Tested
Agonist activity at GFP10/beta-arrestin1-Rluc2 fused human NTS1 expressed in CHO-K1 cell membranes assessed as beta-arrestin1 recruitment after 20 mins by BRET assay
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