SKF-81297 [Ligand Id: 938] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL353335
  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
  • D1 receptor in Rat [GtoPdb: 214] [UniProtKB: P18901]
  • 8.7
1 CHEMBL353335_lig_chart_1 Dopamine D1 receptor HumanRat
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  • D5 receptor/Dopamine D5 receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
  • This target only has 0 pki data point
  • 0
2 CHEMBL353335_lig_chart_2 Dopamine D5 receptor Human
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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 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 B 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 B 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]