L-803,087 [Ligand Id: 2082] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1450103 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 5579-5586 [PMID:14667212] |
| ChEMBL | Binding affinity at human Somatostatin receptor type 1 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement. | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 5587-5596 [PMID:14667213] |
| ChEMBL | Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand. | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 5597-5605 [PMID:14667214] |
| SST2 receptor/Somatostatin receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1804] [GtoPdb: 356] [UniProtKB: P30874] | ||||||||
| ChEMBL | Displacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST2 receptor expressed in CHOK1 cell membranes after 45 mins by scintillation counting method | B | 5.33 | pKi | 4720 | nM | Ki | Medchemcomm (2018) 9: 2083-2090 [PMID:30746066] |
| ChEMBL | Binding affinity at human Somatostatin receptor type 2 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement. | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2003) 46: 5587-5596 [PMID:14667213] |
| ChEMBL | Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand. | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2003) 46: 5597-5605 [PMID:14667214] |
| ChEMBL | Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 5579-5586 [PMID:14667212] |
| SST3 receptor/Somatostatin receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2028] [GtoPdb: 357] [UniProtKB: P32745] | ||||||||
| ChEMBL | Binding affinity at human Somatostatin receptor type 3 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement. | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2003) 46: 5587-5596 [PMID:14667213] |
| ChEMBL | Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand. | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2003) 46: 5597-5605 [PMID:14667214] |
| ChEMBL | Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 5579-5586 [PMID:14667212] |
| SST4 receptor/Somatostatin receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1853] [GtoPdb: 358] [UniProtKB: P31391] | ||||||||
| ChEMBL | Displacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 45 mins by scintillation counting method | B | 9.15 | pKi | 0.7 | nM | Ki | Medchemcomm (2018) 9: 2083-2090 [PMID:30746066] |
| GtoPdb | - | - | 9.2 | pKi | - | - | - | Science (1998) 282: 737-40 [PMID:9784130] |
| ChEMBL | Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand | B | 8.38 | pIC50 | 4.2 | nM | IC50 | J Med Chem (2003) 46: 5579-5586 [PMID:14667212] |
| ChEMBL | Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement. | B | 8.38 | pIC50 | 4.2 | nM | IC50 | J Med Chem (2003) 46: 5587-5596 [PMID:14667213] |
| ChEMBL | Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand. | B | 8.38 | pIC50 | 4.2 | nM | IC50 | J Med Chem (2003) 46: 5597-5605 [PMID:14667214] |
| 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 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2003) 46: 5579-5586 [PMID:14667212] |
| ChEMBL | Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement. | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2003) 46: 5587-5596 [PMID:14667213] |
| ChEMBL | Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand. | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2003) 46: 5597-5605 [PMID:14667214] |
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]
