neurotensin [Ligand Id: 1579] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL407196 (Neurotensin)
  • NTS1 receptor/Neurotensin receptor 1 in Human [ChEMBL: CHEMBL4123] [GtoPdb: 309] [UniProtKB: P30989]
  • NTS1 receptor/Neurotensin receptor 1 in Mouse [ChEMBL: CHEMBL3570] [GtoPdb: 309] [UniProtKB: O88319]
  • NTS1 receptor/Neurotensin receptor 1 in Rat [ChEMBL: CHEMBL3027] [GtoPdb: 309] [UniProtKB: P20789]
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  • NTS2 receptor/Neurotensin receptor 2 in Human [ChEMBL: CHEMBL2514] [GtoPdb: 310] [UniProtKB: O95665]
  • NTS2 receptor in Mouse [GtoPdb: 310] [UniProtKB: P70310]
  • NTS2 receptor/Neurotensin receptor 2 in Rat [ChEMBL: CHEMBL5106] [GtoPdb: 310] [UniProtKB: Q63384]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
NTS1 receptor/Neurotensin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4123] [GtoPdb: 309] [UniProtKB: P30989]
ChEMBL Displacement of [3H]neurotensin from human NTS1 receptor expressed in CHO cells B 9.23 pKd 0.59 nM Kd J. Med. Chem. (2011) 54: 2915-2923 [PMID:21446649]
ChEMBL Displacement of [3H]neurotensin from human NTS1 receptor expressed in CHO cells B 9.29 pKd 0.51 nM Kd J. Med. Chem. (2013) 56: 9361-9365 [PMID:24160350]
ChEMBL Displacement of [125I]Tyr3-neurotensin from human recombinant NTS1 stably expressed in CHO-K1 cell membranes incubated for 60 mins by gamma counter analysis B 8.48 pKi 3.3 nM Ki J Med Chem (2021) 64: 2110-2124 [PMID:33538583]
ChEMBL Displacement of [3H]NT(8-13) from wild type human NTR1 expressed in HEK293 cells B 8.68 pKi 2.1 nM Ki Bioorg. Med. Chem. (2008) 16: 9359-9368 [PMID:18809332]
ChEMBL Displacement of [125I]I-Tyr(3)NT from human NTR1 B 8.79 pKi 1.64 nM Ki J. Med. Chem. (2009) 52: 1803-1813 [PMID:19290594]
ChEMBL Displacement of radiolabeled neurotensin from human neurotensin receptor 1 B 8.82 pKi 1.5 nM Ki J. Med. Chem. (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Binding affinity to human neurotensin receptor 1 B 8.92 pKi 1.2 nM Ki ACS Med Chem Lett (2020) 11: 16-22 [PMID:31938457]
ChEMBL Binding affinity to human NTS1 receptor by radioligand displacement assay B 9.57 pKi 0.27 nM Ki Eur. J. Med. Chem. (2013) 63: 85-94 [PMID:23466604]
GtoPdb - - 9.7 pKi - - - Mol Pharmacol (2001) 60: 1392-8 [PMID:11723247];
Biochem Pharmacol (2000) 60: 793-801 [PMID:10930533]
ChEMBL Antagonist activity at human NTS1 receptor expressed in CHOK1 cells assessed as inhibition of intracellular calcium elevation pretreated 30 mins before with SR-48692 by FLIPR assay F 8.22 pIC50 6.03 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 5789-5789 [PMID:18849166]
ChEMBL Displacement of [125I]I-Tyr(3)NT from human NTR1 B 8.66 pIC50 2.19 nM IC50 J. Med. Chem. (2009) 52: 1803-1813 [PMID:19290594]
ChEMBL Displacement of radiolabeled neurotensin from human neurotensin receptor 1 B 8.74 pIC50 1.8 nM IC50 J. Med. Chem. (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Inhibition of human NTS1 receptor B 8.85 pIC50 1.4 nM IC50 J. Med. Chem. (2008) 51: 4150-4169 [PMID:18588282]
ChEMBL Displacement of [125I]Tyr3-NT from human NTS1R expressed in HT29 cells B 9.21 pIC50 0.62 nM IC50 J. Med. Chem. (2006) 49: 4767-4776 [PMID:16854083]
ChEMBL Displacement of [125I]Tyr3-neurotensin from human recombinant NTS1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method B 9.31 pIC50 0.49 nM IC50 Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
ChEMBL Displacement of [125I]Tyr3-neurotensin from human recombinant NT1 receptor expressed in CHO cells B 9.31 pIC50 0.49 nM IC50 Bioorg. Med. Chem. (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL Displacement of [125I]Tyr3-NT from human NTS1R expressed in WiDr cells B 9.34 pIC50 0.46 nM IC50 J. Med. Chem. (2006) 49: 4767-4776 [PMID:16854083]
ChEMBL Binding affinity to human NTS1 receptor by radioligand displacement assay B 9.48 pIC50 0.33 nM IC50 Eur. J. Med. Chem. (2013) 63: 85-94 [PMID:23466604]
ChEMBL Binding affinity to NTS1 receptor (unknown origin) by radioligand displacement assay B 9.62 pIC50 0.24 nM IC50 Bioorg. Med. Chem. (2013) 21: 2764-2771 [PMID:23582449]
ChEMBL Binding affinity towards neurotensin receptor in membranes prepared from HT-29 cell line, relative to [111In]-labeled neurotensin peptide B 9.7 pIC50 0.2 nM IC50 J. Med. Chem. (2003) 46: 3403-3411 [PMID:12852770]
ChEMBL Agonist activity at human NTS1 receptor expressed in CHOK1 cells assessed as increase in intracellular calcium level by FLIPR assay F 6.51 pEC50 310 nM EC50 Bioorg. Med. Chem. Lett. (2008) 18: 5789-5789 [PMID:18849166]
ChEMBL Agonist activity at human NTR1 assessed as increase in intracellular calcium concentration F 8.7 pEC50 2 nM EC50 J. Med. Chem. (2009) 52: 1803-1813 [PMID:19290594]
ChEMBL Agonist activity at NTR1 in human HT-29 cells assessed as increase in intracellular calcium concentration by FLIPR assay F 8.7 pEC50 1.98 nM EC50 J. Med. Chem. (2009) 52: 1803-1813 [PMID:19290594]
ChEMBL Agonist activity at human NTS1 receptor expressed in HEK293 cells assessed as inhibition of constitutive activity on MAPK-mediated luciferase activity F 8.8 pEC50 1.6 nM EC50 J. Med. Chem. (2011) 54: 2915-2923 [PMID:21446649]
ChEMBL Agonist activity at NTR1 expressed in CHOK1 cells by calcium mobilization assay F 9.64 pEC50 0.23 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 1438-1441 [PMID:19195889]
NTS1 receptor/Neurotensin receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3570] [GtoPdb: 309] [UniProtKB: O88319]
ChEMBL Concentration producing half maximal inhibition of specific binding of [125I]-Tyr3-NT(1-13) to NT receptor in neonatal mouse whole brain (minus cerebellum) B 9.77 pKi 0.17 nM Ki Bioorg. Med. Chem. Lett. (1993) 3: 949-952
ChEMBL Agonist activity at NTR1 in mouse N1E-115 cells assessed as increase in intracellular calcium concentration F 8.7 pEC50 2 nM EC50 J. Med. Chem. (2009) 52: 1803-1813 [PMID:19290594]
NTS1 receptor/Neurotensin receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3027] [GtoPdb: 309] [UniProtKB: P20789]
ChEMBL Displacement of [125L]NT from rat neurotensin receptor type 1 expressed in CHOK1 cells by radioligand binding assay B 8.77 pKi 1.7 nM Ki Bioorg. Med. Chem. Lett. (2015) 25: 292-296 [PMID:25499438]
ChEMBL Displacement of [125I]neurotensin from rat NTS1 receptor expressed in CHO-K1 cells by competitive binding assay B 8.96 pKi 1.1 nM Ki J. Med. Chem. (2014) 57: 7472-7477 [PMID:25157640]
GtoPdb - - 10 pKi - - - Mol Pharmacol (2003) 64: 421-9 [PMID:12869647];
Biochem Pharmacol (2000) 60: 793-801 [PMID:10930533];
J Biol Chem (1998) 273: 16351-7 [PMID:9632698]
ChEMBL Agonist activity at rat NTS1 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay F 10.4 pEC50 0.04 nM EC50 J. Med. Chem. (2014) 57: 5318-5332 [PMID:24856674]
NTS2 receptor/Neurotensin receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2514] [GtoPdb: 310] [UniProtKB: O95665]
ChEMBL Displacement of [3H]NT from human NTS2 receptor expressed in HEK293 cells B 8.31 pKi 4.9 nM Ki J. Med. Chem. (2011) 54: 2915-2923 [PMID:21446649]
ChEMBL Displacement of [3H]NT(8 to 13) from human NTS2 receptor expressed in HEK293 cells B 8.31 pKi 4.9 nM Ki J. Med. Chem. (2013) 56: 9361-9365 [PMID:24160350]
ChEMBL Displacement of [125I]Tyr3-neurotensin from human recombinant NTS2 stably expressed in human 1321N1 cell membranes incubated for 60 mins by gamma counter analysis B 8.39 pKi 4.1 nM Ki J Med Chem (2021) 64: 2110-2124 [PMID:33538583]
GtoPdb - - 8.8 pKi - - - Mol Pharmacol (2001) 60: 1392-8 [PMID:11723247]
ChEMBL Agonist activity at human NTS2 receptor expressed in HEK293 cells assessed as inhibition of constitutive activity on MAPK-mediated luciferase activity F 6.96 pEC50 110 nM EC50 J. Med. Chem. (2011) 54: 2915-2923 [PMID:21446649]
NTS2 receptor in Mouse [GtoPdb: 310] [UniProtKB: P70310]
GtoPdb - - 8.7 pIC50 - - - Biochem Biophys Res Commun (1998) 243: 585-90 [PMID:9480852]
NTS2 receptor/Neurotensin receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5106] [GtoPdb: 310] [UniProtKB: Q63384]
ChEMBL Displacement of [125I]neurotensin from rat NTS2 receptor expressed in CHO-K1 cells by competitive binding assay B 7.55 pKi 28 nM Ki J. Med. Chem. (2014) 57: 7472-7477 [PMID:25157640]
ChEMBL Displacement of [125L]NT from rat neurotensin receptor type 2 expressed in CHOK1 cells by radioligand binding assay B 7.68 pKi 21 nM Ki Bioorg. Med. Chem. Lett. (2015) 25: 292-296 [PMID:25499438]
ChEMBL Displacement of [125I]NT at rat NTS2 overexpressed in CHOK1 cells after 30 mins by gamma counting B 7.72 pKi 18.9 nM Ki J. Med. Chem. (2014) 57: 5318-5332 [PMID:24856674]
ChEMBL Antagonist activity at rat NTS2 receptor expressed in CHO-K1 cells assessed as inhibition of SR142948a-induced calcium mobilization by FLIPR assay F 6.94 pIC50 114 nM IC50 J. Med. Chem. (2014) 57: 7472-7477 [PMID:25157640]
ChEMBL Antagonist activity at rat neurotensin receptor type 2 expressed in CHOK1 cells assessed as inhibition of SR142948a-induced calcium release by FLIPR assay F 7.38 pIC50 42 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 292-296 [PMID:25499438]
ChEMBL Antagonist activity at rat NTS2 stably expressed in CHOK1 cells assessed as inhibition of SR142948a-induced calcium release by FLIPR assay F 7.73 pIC50 18.5 nM IC50 J. Med. Chem. (2014) 57: 5318-5332 [PMID:24856674]
GtoPdb - - 8.2 pIC50 - - - J Biol Chem (1999) 274: 13752-9 [PMID:10318778]
ChEMBL Agonist activity at rat neurotensin receptor type 2 expressed in CHOK1 cells assessed as increase in calcium release by FLIPR assay F 7 pEC50 >100 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 292-296 [PMID:25499438]
Neurotensin receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3091] [UniProtKB: Q99523]
ChEMBL Displacement of [3H]-neurotensin from human sortilin incubated 30 mins prior to [3H]-neurotensin addition measured after 6 hrs by scintillation proximity assay B 6.44 pIC50 360 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 177-180 [PMID:24355129]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]