BN-81,644 [Ligand Id: 2070] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2069499
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  • SST1 receptor/Somatostatin receptor 1 in Human [ChEMBL: CHEMBL1917] [GtoPdb: 355] [UniProtKB: P30872]
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  • SST2 receptor/Somatostatin receptor 2 in Human [ChEMBL: CHEMBL1804] [GtoPdb: 356] [UniProtKB: P30874]
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  • SST3 receptor/Somatostatin receptor 3 in Human [ChEMBL: CHEMBL2028] [GtoPdb: 357] [UniProtKB: P32745]
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  • SST4 receptor/Somatostatin receptor 4 in Human [ChEMBL: CHEMBL1853] [GtoPdb: 358] [UniProtKB: P31391]
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  • SST5 receptor/Somatostatin receptor 5 in Human [ChEMBL: CHEMBL1792] [GtoPdb: 359] [UniProtKB: P35346]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]