neurotensin [Ligand Id: 1579] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL407196 (Neurotensin) |
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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 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-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-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 | Inhibition of human NTR1 | B | 9.8 | pIC50 | 0.16 | nM | IC50 | Bioorg Med Chem Lett (2022) 75: 128983-128983 [PMID:36096342] |
| 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 | Inhibition of human NTR2 | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem Lett (2022) 75: 128983-128983 [PMID:36096342] |
| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
