seglitide [Ligand Id: 2051] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL311695 (L-363586, Seglitida, Seglitide) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| NK1 receptor/Neurokinin 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103] | ||||||||
| ChEMBL | Inhibition of Tachykinin receptor 1 | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1996) 39: 2441-2448 [PMID:8691440] |
| SST1 receptor/Somatostatin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1917] [GtoPdb: 355] [UniProtKB: P30872] | ||||||||
| ChEMBL | Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (2003) 46: 2334-2344 [PMID:12773038] |
| ChEMBL | Binding affinity to human sst1 by in vitro receptor autoradiography assay | B | 6 | pIC50 | >1000 | nM | IC50 | ACS Med Chem Lett (2011) 2: 509-514 [PMID:24900340] |
| SST2 receptor/Somatostatin receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1804] [GtoPdb: 356] [UniProtKB: P30874] | ||||||||
| ChEMBL | In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligand | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (1998) 41: 4693-4705 [PMID:9822540] |
| ChEMBL | Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells | B | 10.1 | pKi | 0.08 | nM | Ki | J Med Chem (2003) 46: 2334-2344 [PMID:12773038] |
| GtoPdb | - | - | 10.3 | pKi | - | - | - |
Metab Clin Exp (1996) 45: 17-20 [PMID:8769372]; Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 483-9 [PMID:9650799]; Naunyn Schmiedebergs Arch Pharmacol (1999) 360: 488-99 [PMID:10598788]; Endocrinology (1994) 135: 2814-7 [PMID:7988476]; Proc Natl Acad Sci USA (1998) 95: 10836-41 [PMID:9724791]; Eur J Pharmacol (1998) 348: 311-20 [PMID:9652348] |
| ChEMBL | Binding affinity to human sst2 by in vitro receptor autoradiography assay | B | 8.8 | pIC50 | 1.6 | nM | IC50 | ACS Med Chem Lett (2011) 2: 509-514 [PMID:24900340] |
| SST2 receptor in Mouse [GtoPdb: 356] [UniProtKB: P30875] | ||||||||
| GtoPdb | - | - | 9.9 | pKi | - | - | - | Rev Physiol Biochem Pharmacol (1998) 133: 55-108 [PMID:9600011] |
| SST2 receptor in Rat [GtoPdb: 356] [UniProtKB: P30680] | ||||||||
| GtoPdb | - | - | 9.3 | pKi | - | - | - | Rev Physiol Biochem Pharmacol (1998) 133: 55-108 [PMID:9600011] |
| SST3 receptor/Somatostatin receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2028] [GtoPdb: 357] [UniProtKB: P32745] | ||||||||
| ChEMBL | Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells | B | 7.5 | pKi | 31.62 | nM | Ki | J Med Chem (2003) 46: 2334-2344 [PMID:12773038] |
| GtoPdb | - | - | 7.9 | pKi | - | - | - |
Metab Clin Exp (1996) 45: 17-20 [PMID:8769372]; Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 483-9 [PMID:9650799]; Naunyn Schmiedebergs Arch Pharmacol (1999) 360: 488-99 [PMID:10598788]; Endocrinology (1994) 135: 2814-7 [PMID:7988476]; Proc Natl Acad Sci USA (1998) 95: 10836-41 [PMID:9724791] |
| ChEMBL | Binding affinity to human sst3 by in vitro receptor autoradiography assay | B | 6.98 | pIC50 | 105 | nM | IC50 | ACS Med Chem Lett (2011) 2: 509-514 [PMID:24900340] |
| SST3 receptor in Mouse [GtoPdb: 357] [UniProtKB: P30935] | ||||||||
| GtoPdb | - | - | 7.9 | pIC50 | - | - | - | Mol Pharmacol (1993) 43: 838-44 [PMID:8100350] |
| SST3 receptor in Rat [GtoPdb: 357] [UniProtKB: P30936] | ||||||||
| GtoPdb | - | - | 7.4 | pKi | - | - | - | Rev Physiol Biochem Pharmacol (1998) 133: 55-108 [PMID:9600011] |
| SST4 receptor/Somatostatin receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1853] [GtoPdb: 358] [UniProtKB: P31391] | ||||||||
| ChEMBL | In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand | B | 5.49 | pKi | 3200 | nM | Ki | J Med Chem (1998) 41: 4693-4705 [PMID:9822540] |
| ChEMBL | Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (2003) 46: 2334-2344 [PMID:12773038] |
| ChEMBL | Binding affinity to human sst4 by in vitro receptor autoradiography assay | B | 6 | pIC50 | >1000 | nM | IC50 | ACS Med Chem Lett (2011) 2: 509-514 [PMID:24900340] |
| SST5 receptor/Somatostatin receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1792] [GtoPdb: 359] [UniProtKB: P35346] | ||||||||
| ChEMBL | Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell | B | 7.9 | pKi | 12.59 | nM | Ki | J Med Chem (2003) 46: 2334-2344 [PMID:12773038] |
| GtoPdb | - | - | 10.2 | pKi | - | - | - |
Metab Clin Exp (1996) 45: 17-20 [PMID:8769372]; Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 483-9 [PMID:9650799]; Naunyn Schmiedebergs Arch Pharmacol (1999) 360: 488-99 [PMID:10598788]; Rev Physiol Biochem Pharmacol (1998) 133: 55-108 [PMID:9600011]; Endocrinology (1994) 135: 2814-7 [PMID:7988476]; Proc Natl Acad Sci USA (1998) 95: 10836-41 [PMID:9724791]; Eur J Pharmacol (1998) 348: 311-20 [PMID:9652348] |
| ChEMBL | Binding affinity to human sst5 by in vitro receptor autoradiography assay | B | 7.09 | pIC50 | 81 | nM | IC50 | ACS Med Chem Lett (2011) 2: 509-514 [PMID:24900340] |
| SST5 receptor in Mouse [GtoPdb: 359] [UniProtKB: O08858] | ||||||||
| GtoPdb | - | - | 8.5 | pKi | - | - | - | Neuropharmacology (2000) 39: 1451-62 [PMID:10818261] |
| SST5 receptor in Rat [GtoPdb: 359] [UniProtKB: P30938] | ||||||||
| GtoPdb | - | - | 7.1 | pKi | - | - | - | Rev Physiol Biochem Pharmacol (1998) 133: 55-108 [PMID:9600011] |
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]
