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 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]
