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Radioligand Competitive Binding Assay from US Patent US20240287046: "COMPOUNDS AND RADIOLIGANDS FOR TARGETING NEUROTENSIN RECEPTOR AND USES THEREOF"
Assay data:21 Active, 13 Activity ≤ 1 nM, 21 Activity ≤ 1 µM, 21 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Activity against NT1/H in the Eurofins SafetyScreen44 (BI) by Radioactive Assay (Old_Cerep_27)
Assay data:1 Tested
SummaryRelated BioAssays by Target
Agonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production by measuring maximal efficacy incubated for 90 mins by IP-one HTRF assay relative to full effect of (2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-amino-5-guanidino-pentanoyl]amino]-5-guanidino-pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methyl-pentanoyl]amino]-4-methyl-pentanoic acid
Assay data:6 Tested
SummaryPubMed CitationRelated BioAssays by Target
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
Assay data:7 Active, 5 Activity ≤ 1 nM, 6 Activity ≤ 1 µM, 7 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity to human NTSR1 transfected in HEK293 cells assessed as inhibition constant incubated for 60 mins in the presence of [Leu3H]NT(8-13) by radioligand competition binding assay
Assay data:6 Active, 1 Activity ≤ 1 nM, 6 Activity ≤ 1 µM, 7 Tested
Binding affinity to human NTS1R assessed as dissociation constant
Assay data:2 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
Binding affinity towards human NTSR1 in an in vitro assay with cellular components measured by scintillation proximity assay
Assay data:2 Active, 294 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of human NTR1
Assay data:3 Active, 2 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
Displacement of [3H]NT(8-13) from human NTSR1 F2.65C mutant expressed in HEK293 cell membranes assessed as amount of blocking at 10 nM incubated for 120 mins by radioligand depletion assay
Displacement of [3H]NT(8-13) from human NTSR1 F2.65C mutant expressed in HEK293 cell membranes assessed as amount of blocking at 1 uM incubated for 120 mins by radioligand depletion assay
Assay data:4 Tested
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
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
NT1 (h) (NTS1) CEREP panel
Radioligand Binding Assay NTR1 from US Patent US10799605: "Conjugate comprising a neurotensin receptor ligand and use thereof"
Assay data:6 Active, 1 Activity ≤ 1 nM, 6 Activity ≤ 1 µM, 6 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Functional Ca2+ Mobilisation Assay from US Patent US10799605: "Conjugate comprising a neurotensin receptor ligand and use thereof"
Assay data:7 Active, 7 Activity ≤ 1 µM, 7 Tested
NTR1 Ca2+ Flux Dose Response from US Patent US10584103: "Small molecule agonists of neurotensin receptor 1"
Assay data:131 Active, 20 Activity ≤ 1 µM, 211 Tested
SPR Screening Assay from Article 10.1021/acschembio.6b00646: "Ligand Discovery for a Peptide-Binding GPCR by Structure-Based Screening of Fragment- and Lead-Like Chemical Libraries."
Assay data:3 Active, 1 Activity ≤ 1 µM, 5 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Assay data:5 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 7 Tested
NTR1 Ca2+ Flux Dose Response from US Patent US10118902: "Small molecule agonists of neurotensin receptor 1"
Assay data:131 Active, 20 Activity ≤ 1 µM, 210 Tested
Neurotensin NT1 Eurofins-Panlabs radioligand binding assay
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