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 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
