L-054,522 [Ligand Id: 2046] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL99895
  • 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
SST1 receptor/Somatostatin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1917] [GtoPdb: 355] [UniProtKB: P30872]
ChEMBL Binding affinity towards Somatostatin receptor type 1 (hsst1) B 5.62 pKi 2392 nM Ki J Med Chem (2002) 45: 5609-5616 [PMID:12477342]
ChEMBL Binding affinity to human somatostatin receptor type 1 B 5.62 pKi 2392 nM Ki J Med Chem (2016) 59: 10865-10890 [PMID:27690430]
SST2 receptor/Somatostatin receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1804] [GtoPdb: 356] [UniProtKB: P30874]
GtoPdb - - 11 pKi - - - Proc Natl Acad Sci USA (1998) 95: 10836-41 [PMID:9724791]
ChEMBL Binding affinity towards Somatostatin receptor type 2 (hsst2) B 11 pKi 0.01 nM Ki J Med Chem (2002) 45: 5609-5616 [PMID:12477342]
ChEMBL Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing each of the cloned human SRIF receptor (sst-2) subtypes B 11 pKi 0.01 nM Ki J Med Chem (2001) 44: 2990-3000 [PMID:11520208]
ChEMBL Binding affinity to human somatostatin receptor type 2 B 11 pKi 0.01 nM Ki J Med Chem (2016) 59: 10865-10890 [PMID:27690430]
SST3 receptor/Somatostatin receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2028] [GtoPdb: 357] [UniProtKB: P32745]
ChEMBL Binding affinity towards Somatostatin receptor type 3 (hsst3) B 7.51 pKi 31 nM Ki J Med Chem (2002) 45: 5609-5616 [PMID:12477342]
ChEMBL Binding affinity to human somatostatin receptor type 3 B 7.51 pKi 31 nM Ki J Med Chem (2016) 59: 10865-10890 [PMID:27690430]
SST4 receptor/Somatostatin receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1853] [GtoPdb: 358] [UniProtKB: P31391]
ChEMBL Binding affinity towards Somatostatin receptor type 4 (hsst4) B 7.09 pKi 81 nM Ki J Med Chem (2002) 45: 5609-5616 [PMID:12477342]
ChEMBL Binding affinity to human somatostatin receptor type 4 B 7.09 pKi 81 nM Ki J Med Chem (2016) 59: 10865-10890 [PMID:27690430]
SST5 receptor/Somatostatin receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1792] [GtoPdb: 359] [UniProtKB: P35346]
ChEMBL Binding affinity towards Somatostatin receptor type 5 (hsst5) B 6.79 pKi 163 nM Ki J Med Chem (2002) 45: 5609-5616 [PMID:12477342]
ChEMBL Binding affinity to human somatostatin receptor type 5 B 6.79 pKi 163 nM Ki J Med Chem (2016) 59: 10865-10890 [PMID:27690430]

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]