SR142948A [Ligand Id: 1580] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3040381 |
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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]-{Nomega-[N-(4-propanoylaminobutyl)aminocarbonyl]}Arg-Arg-ProTyr-Ile-Leu-OH Tris(hydrotrifluoroacetate) from NTSR1 in human HT-29 cells after 2 hrs by liquid scintillation counting | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (2016) 59: 1925-1945 [PMID:26824643] |
| ChEMBL | Displacement of [3H]neurotensin from human NTS1 receptor expressed in CHO cells | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2013) 56: 9361-9365 [PMID:24160350] |
| ChEMBL | Antagonist activity at NTSR1 (unknown origin) expressed in CHO cells assessed as inhibition of NT(8-13) peptide-induced change in intracellular Ca2+ level preincubated for 45 mins by FLIPR assay | F | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 3974-3978 [PMID:24997685] |
| ChEMBL | Antagonist activity at NTR1 (unknown origin) | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2019) 62: 8357-8363 [PMID:31390201] |
| ChEMBL | Displacement of [3H]-{Nomega-[N-(4-propanoylaminobutyl)aminocarbonyl]}Arg-Arg-ProTyr-Ile-Leu-OH Tris(hydrotrifluoroacetate) from NTSR1 in human HT-29 cells after 2 hrs by liquid scintillation counting | B | 8.5 | pIC50 | 3.16 | nM | IC50 | J Med Chem (2016) 59: 1925-1945 [PMID:26824643] |
| GtoPdb | - | - | 8.9 | pIC50 | - | - | - | J Pharmacol Exp Ther (1997) 280: 802-12 [PMID:9023294] |
| 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 | 8.7 | pKi | 2 | 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 | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2014) 57: 7472-7477 [PMID:25157640] |
| NTS2 receptor/Neurotensin receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2514] [GtoPdb: 310] [UniProtKB: O95665] | ||||||||
| ChEMBL | Displacement of [3H]NT(8 to 13) from human NTS2 receptor expressed in HEK293 cells | B | 7.13 | pKi | 74 | nM | Ki | J Med Chem (2013) 56: 9361-9365 [PMID:24160350] |
| NTS2 receptor/Neurotensin receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5106] [GtoPdb: 310] [UniProtKB: Q63384] | ||||||||
| ChEMBL | Displacement of [125L]NT from rat neurotensin receptor type 2 expressed in CHOK1 cells by radioligand binding assay | B | 8.15 | pKi | 7 | 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 | 8.22 | pKi | 6 | nM | Ki | J Med Chem (2014) 57: 5318-5332 [PMID:24856674] |
| ChEMBL | Displacement of [125I]neurotensin from rat NTS2 receptor expressed in CHO-K1 cells by competitive binding assay | B | 8.24 | pKi | 5.8 | nM | Ki | J Med Chem (2014) 57: 7472-7477 [PMID:25157640] |
| ChEMBL | Agonist activity at rat NTS2 receptor expressed in CHO-K1 cells assessed as calcium mobilization by FLIPR assay | F | 7.66 | pEC50 | 22 | nM | EC50 | J Med Chem (2014) 57: 7472-7477 [PMID:25157640] |
| ChEMBL | Agonist activity at rat NTS2 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay | F | 7.7 | pEC50 | 20 | nM | EC50 | J Med Chem (2014) 57: 5318-5332 [PMID:24856674] |
| ChEMBL | Agonist activity at rat neurotensin receptor type 2 expressed in CHOK1 cells assessed as increase in calcium release by FLIPR assay | F | 7.74 | pEC50 | 18 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 292-296 [PMID:25499438] |
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]
