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ChEMBL ligand: CHEMBL2069499 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Displacement of [35S]MK499 from human Erg expressed in HEK293 cells after 60 mins by scintillation counting | B | 6.82 | pIC50 | 150 | nM | IC50 | ACS Med Chem Lett (2012) 3: 289-293 [PMID:24900466] |
SST1 receptor/Somatostatin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1917] [GtoPdb: 355] [UniProtKB: P30872] | ||||||||
ChEMBL | Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-1) subtype | B | 5.43 | pKi | 3700 | nM | Ki | J Med Chem (2001) 44: 2990-3000 [PMID:11520208] |
SST2 receptor/Somatostatin receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1804] [GtoPdb: 356] [UniProtKB: P30874] | ||||||||
ChEMBL | Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-2) subtype | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2001) 44: 2990-3000 [PMID:11520208] |
SST3 receptor/Somatostatin receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2028] [GtoPdb: 357] [UniProtKB: P32745] | ||||||||
ChEMBL | Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype | B | 9.19 | pKi | 0.64 | nM | Ki | J Med Chem (2001) 44: 2990-3000 [PMID:11520208] |
ChEMBL | Binding affinity to human SST3 receptor | B | 9.19 | pKi | 0.64 | nM | Ki | ACS Med Chem Lett (2012) 3: 289-293 [PMID:24900466] |
GtoPdb | - | - | 9.2 | pKi | - | - | - | J Med Chem (2001) 44: 2990-3000 [PMID:11520208] |
ChEMBL | Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor. | F | 8.57 | pIC50 | 2.7 | nM | IC50 | J Med Chem (2001) 44: 2990-3000 [PMID:11520208] |
SST4 receptor/Somatostatin receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1853] [GtoPdb: 358] [UniProtKB: P31391] | ||||||||
ChEMBL | Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtype | B | 5.15 | pKi | 7100 | nM | Ki | J Med Chem (2001) 44: 2990-3000 [PMID:11520208] |
SST5 receptor/Somatostatin receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1792] [GtoPdb: 359] [UniProtKB: P35346] | ||||||||
ChEMBL | Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-5) subtype | B | 5.66 | pKi | 2200 | nM | Ki | J Med Chem (2001) 44: 2990-3000 [PMID:11520208] |
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]