paltusotine [Ligand Id: 14237] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL5267842 (Crn00808, CRN-00808, CRN00808, Paltusotine) |
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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 | Agonist activity at human SST1 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay | B | 6 | pEC50 | >1000 | nM | EC50 | ACS Med Chem Lett (2023) 14: 66-74 [PMID:36655128] |
| SST2 receptor/Somatostatin receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1804] [GtoPdb: 356] [UniProtKB: P30874] | ||||||||
| ChEMBL | Agonist activity at human SST2 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay | B | 9.6 | pEC50 | 0.25 | nM | EC50 | ACS Med Chem Lett (2023) 14: 66-74 [PMID:36655128] |
| GtoPdb | - | - | 9.6 | pEC50 | 0.25 | nM | EC50 | ACS Med Chem Lett (2023) 14: 66-74 [PMID:36655128] |
| ChEMBL | Agonist activity at human SST2 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay | B | 9.6 | pEC50 | 0.25 | nM | EC50 | ACS Med Chem Lett (2023) 14: 66-74 [PMID:36655128] |
| SST2 receptor/Somatostatin receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2978] [GtoPdb: 356] [UniProtKB: P30680] | ||||||||
| GtoPdb | - | - | 8.92 | pEC50 | 1.2 | nM | EC50 | ACS Med Chem Lett (2023) 14: 66-74 [PMID:36655128] |
| ChEMBL | Agonist activity at rat SST2 receptor | B | 8.92 | pEC50 | 1.2 | nM | EC50 | ACS Med Chem Lett (2023) 14: 66-74 [PMID:36655128] |
| SST3 receptor/Somatostatin receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2028] [GtoPdb: 357] [UniProtKB: P32745] | ||||||||
| ChEMBL | Agonist activity at human SST3 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay | B | 6 | pEC50 | >1000 | nM | EC50 | ACS Med Chem Lett (2023) 14: 66-74 [PMID:36655128] |
| SST4 receptor/Somatostatin receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1853] [GtoPdb: 358] [UniProtKB: P31391] | ||||||||
| ChEMBL | Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay | B | 6 | pEC50 | 1000 | nM | EC50 | ACS Med Chem Lett (2023) 14: 66-74 [PMID:36655128] |
| SST5 receptor/Somatostatin receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1792] [GtoPdb: 359] [UniProtKB: P35346] | ||||||||
| ChEMBL | Agonist activity at human SST5 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay | B | 6 | pEC50 | >1000 | nM | EC50 | ACS Med Chem Lett (2023) 14: 66-74 [PMID:36655128] |
| Somatostatin receptor type 2 in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5291563] [UniProtKB: Q49LX6] | ||||||||
| ChEMBL | Agonist activity at dog SST2 receptor | B | 8.18 | pEC50 | 6.6 | nM | EC50 | ACS Med Chem Lett (2023) 14: 66-74 [PMID:36655128] |
ChEMBL data shown on this page come from version 35:
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]
