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 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]
