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 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]
