SKF-81297 [Ligand Id: 938] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL353335 |
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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 wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assay | B | 7.82 | pKi | 15 | nM | Ki | ACS Med Chem Lett (2019) 10: 792-799 [PMID:31098001] |
| ChEMBL | Agonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay | B | 5.02 | pEC50 | 9500 | nM | EC50 | J Med Chem (2019) 62: 5132-5147 [PMID:31021617] |
| ChEMBL | Agonist activity at N-terminal Flag epitope tagged human dopamine D1 receptor expressed in HTLA cells assessed as beta-arrestin translocation activity by luminescence based GPCR-TANGO assay | F | 5.75 | pEC50 | 1778 | nM | EC50 | J Med Chem (2023) 66: 10060-10079 [PMID:37421373] |
| ChEMBL | Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay | B | 6.44 | pEC50 | 360 | nM | EC50 | ACS Med Chem Lett (2019) 10: 792-799 [PMID:31098001] |
| ChEMBL | Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay | F | 8.33 | pEC50 | 4.7 | nM | EC50 | ACS Med Chem Lett (2019) 10: 792-799 [PMID:31098001] |
| D1 receptor in Rat [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| GtoPdb | - | - | 8.7 | pKi | 1.99 | nM | Ki | Eur J Pharmacol (1990) 188: 335-47 [PMID:1973652] |
| D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
| ChEMBL | Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay | F | 8.85 | pEC50 | 1.4 | nM | EC50 | ACS Med Chem Lett (2019) 10: 792-799 [PMID:31098001] |
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]
