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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
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
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
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
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
SummaryPubMed CitationRelated BioAssays by Target
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
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
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
Assay data:1 Active, 3 Tested
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