SKF-83959 [Ligand Id: 8443] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL574558 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| ChEMBL | Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting | B | 8.71 | pKi | 1.93 | nM | Ki | Bioorg Med Chem (2009) 17: 4873-4880 [PMID:19559623] |
| ChEMBL | Agonist activity at dopamine D1 receptor | F | 8.93 | pKi | 1.18 | nM | Ki | Bioorg Med Chem (2009) 17: 4873-4880 [PMID:19559623] |
| ChEMBL | Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| ChEMBL | Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay | F | 9.7 | pEC50 | 0.2 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| GtoPdb | Biased towards G-protein signalling in a cellular assay expressing only D1 receptor. | - | 9.7 | pEC50 | 0.2 | nM | EC50 | ACS Chem Neurosci (2015) 6: 681-92 [PMID:25660762] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5HT1A receptor expressed in CHO cells by liquid scintillation counting | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem (2009) 17: 4873-4880 [PMID:19559623] |
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]
