4P-PDOT [Ligand Id: 1358] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL285718
  • MT1 receptor/Melatonin receptor 1A in Human [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039]
There should be some charts here, you may need to enable JavaScript!
  • MT2 receptor/Melatonin receptor 1B in Human [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
MT1 receptor/Melatonin receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039]
ChEMBL Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells B 6.3 pKi 501 nM Ki J. Med. Chem. (2014) 57: 3161-3185 [PMID:24228714]
ChEMBL Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells B 6.98 pKi 104.71 nM Ki J. Med. Chem. (2005) 48: 4049-4060 [PMID:15943478]
GtoPdb - - 7.2 pKi - - - Naunyn Schmiedebergs Arch. Pharmacol. (2003) 367: 553-61 [PMID:12764576];
Naunyn Schmiedebergs Arch. Pharmacol. (1997) 355: 365-75 [PMID:9089668];
FASEB J. (1998) 12: 1211-20 [PMID:9737724]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells B 7.23 pKi 59 nM Ki J. Med. Chem. (2009) 52: 826-833 [PMID:19193160]
MT2 receptor/Melatonin receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286]
ChEMBL Displacement of [125I]2-iodomelatonin from human recombinant MT2 receptor expressed in African green monkey COS7 cells B 8.82 pKi 1.5 nM Ki J. Med. Chem. (2014) 57: 3161-3185 [PMID:24228714]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells B 9.34 pKi 0.46 nM Ki J. Med. Chem. (2009) 52: 826-833 [PMID:19193160]
GtoPdb - - 9.41 pKi 0.39 nM Ki Naunyn Schmiedebergs Arch. Pharmacol. (2003) 367: 553-61 [PMID:12764576];
Naunyn Schmiedebergs Arch. Pharmacol. (1997) 355: 365-75 [PMID:9089668];
FASEB J. (1998) 12: 1211-20 [PMID:9737724]
ChEMBL Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor MT2 expressed in NIH3T3 rat fibroblast cells B 10.8 pKi 0.02 nM Ki J. Med. Chem. (2005) 48: 4049-4060 [PMID:15943478]

ChEMBL data shown on this page come from version 27:

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]