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 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]