meclinertant [Ligand Id: 1582] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL506981 (Meclinertant, Reminertant, Sr48692, SR-48692) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GPR183/G-protein coupled receptor 183 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3259470] [GtoPdb: 81] [UniProtKB: P32249] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183 | F | 5.2 | pIC50 | 6269.08 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| NTS1 receptor/Neurotensin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4123] [GtoPdb: 309] [UniProtKB: P30989] | ||||||||
| ChEMBL | Displacement of [3H]SR48692 from human NTR1 extracellular loop 1 F136A mutant expressed in HEK293 cells | B | 7.48 | pKd | 33 | nM | Kd | Bioorg Med Chem (2008) 16: 9359-9368 [PMID:18809332] |
| ChEMBL | Displacement of [3H]SR48692 from human NTR1 extracellular loop 1 W129A mutant expressed in HEK293 cells | B | 7.57 | pKd | 27 | nM | Kd | Bioorg Med Chem (2008) 16: 9359-9368 [PMID:18809332] |
| ChEMBL | Displacement of [3H]SR48692 from human NTR1 extracellular loop 1 W134A mutant expressed in HEK293 cells | B | 7.64 | pKd | 23 | nM | Kd | Bioorg Med Chem (2008) 16: 9359-9368 [PMID:18809332] |
| ChEMBL | Displacement of [3H]SR48692 from human NTR1 extracellular loop 1 F127A mutant expressed in HEK293 cells | B | 7.72 | pKd | 19 | nM | Kd | Bioorg Med Chem (2008) 16: 9359-9368 [PMID:18809332] |
| ChEMBL | Displacement of [3H]SR48692 from human NTR1 extracellular loop 1 P133A mutant expressed in HEK293 cells | B | 8.04 | pKd | 9.2 | nM | Kd | Bioorg Med Chem (2008) 16: 9359-9368 [PMID:18809332] |
| ChEMBL | Displacement of [3H]SR48692 from wild type human NTR1 expressed in HEK293 cells | B | 8.05 | pKd | 8.9 | nM | Kd | Bioorg Med Chem (2008) 16: 9359-9368 [PMID:18809332] |
| ChEMBL | Displacement of [3H]SR48692 from human NTR1 extracellular loop 1 H131A mutant expressed in HEK293 cells | B | 8.08 | pKd | 8.4 | nM | Kd | Bioorg Med Chem (2008) 16: 9359-9368 [PMID:18809332] |
| GtoPdb | - | - | 8.4 | pKi | - | - | - | Mol Pharmacol (2001) 60: 1392-8 [PMID:11723247] |
| 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 | 7.09 | pIC50 | 82 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 3974-3978 [PMID:24997685] |
| GtoPdb | - | - | 8.2 | pIC50 | 6.31 | nM | IC50 | J Pharmacol Exp Ther (1997) 280: 802-12 [PMID:9023294] |
| ChEMBL | Displacement of [125I]I-Tyr(3)NT from human NTR1 | B | 9 | pIC50 | 0.99 | nM | IC50 | J Med Chem (2009) 52: 1803-1813 [PMID:19290594] |
| ChEMBL | Agonist activity at NTR1 in human U2OS cells after 1 hr by beta-arrestin GFP reporter gene assay | B | 4.51 | pEC50 | 31000 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 262-267 [PMID:24332089] |
| NTS1 receptor/Neurotensin receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3027] [GtoPdb: 309] [UniProtKB: P20789] | ||||||||
| ChEMBL | Displacement of [125I]NT from rat NTR1 transfected in mouse LTK cells | B | 8.59 | pKi | 2.6 | nM | Ki | Bioorg Med Chem (2013) 21: 4378-4387 [PMID:23721919] |
| GtoPdb | - | - | 8.6 | pKi | - | - | - |
Mol Pharmacol (1995) 47: 1050-6 [PMID:7746272]; J Biol Chem (1998) 273: 16351-7 [PMID:9632698] |
| ChEMBL | Displacement of [125I]neurotensin from rat brain NTR1 | B | 7.09 | pIC50 | 82 | nM | IC50 | J Med Chem (2019) 62: 8357-8363 [PMID:31390201] |
| NTS2 receptor/Neurotensin receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2514] [GtoPdb: 310] [UniProtKB: O95665] | ||||||||
| ChEMBL | Binding affinity to NTR2 (unknown origin) | B | 6.38 | pKi | 418 | nM | Ki | Bioorg Med Chem (2013) 21: 4378-4387 [PMID:23721919] |
| GtoPdb | - | - | 6.4 | pKi | - | - | - | Mol Pharmacol (2001) 60: 1392-8 [PMID:11723247] |
| NTS2 receptor in Mouse [GtoPdb: 310] [UniProtKB: P70310] | ||||||||
| GtoPdb | - | - | 7.1 | 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]NT at rat NTS2 overexpressed in CHOK1 cells after 30 mins by gamma counting | B | 7.21 | pKi | 62 | nM | Ki | J Med Chem (2014) 57: 5318-5332 [PMID:24856674] |
| ChEMBL | Agonist activity at rat NTS2 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay | F | 6.92 | pEC50 | 120 | nM | EC50 | J Med Chem (2014) 57: 5318-5332 [PMID:24856674] |
| sortilin 1/Neurotensin receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3091] [GtoPdb: 3300] [UniProtKB: Q99523] | ||||||||
| ChEMBL | Binding affinity to NTR3 (unknown origin) | B | 6.62 | pIC50 | 238 | nM | IC50 | Bioorg Med Chem (2013) 21: 4378-4387 [PMID:23721919] |
| FPR3/N-formyl peptide receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5646] [GtoPdb: 224] [UniProtKB: P25089] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: FPR3 | F | 5.3 | pIC50 | 4991.46 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
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]
