seglitide [Ligand Id: 2051] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL311695 (L-363586, 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]; Rev Physiol Biochem Pharmacol (1998) 133: 55-108 [PMID:9600011]; Endocrinology (1994) 135: 2814-7 [PMID:7988476]; Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 483-9 [PMID:9650799]; Eur J Pharmacol (1998) 348: 311-20 [PMID:9652348]; Naunyn Schmiedebergs Arch Pharmacol (1999) 360: 488-99 [PMID:10598788]; Proc Natl Acad Sci USA (1998) 95: 10836-41 [PMID:9724791] |
| 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 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]
