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ChEMBL ligand: CHEMBL286615 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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MT1 receptor/Melatonin receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039] | ||||||||
ChEMBL | Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells | B | 6.1 | pKi | 794.33 | nM | Ki | Eur J Med Chem (2007) 42: 1004-1013 [PMID:17346859] |
ChEMBL | Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay | B | 6.22 | pKi | 603 | nM | Ki | J Med Chem (2000) 43: 1050-1061 [PMID:10737738] |
GtoPdb | - | - | 6.8 | pKi | - | - | - |
Br J Pharmacol (2000) 129: 877-86 [PMID:10696085]; Naunyn Schmiedebergs Arch Pharmacol (2003) 367: 553-61 [PMID:12764576]; Naunyn Schmiedebergs Arch Pharmacol (1997) 355: 365-75 [PMID:9089668]; J Pharmacol Exp Ther (1988) 246: 902-10 [PMID:2843633] |
ChEMBL | Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells | B | 6.8 | pKi | 158 | nM | Ki | J Med Chem (2014) 57: 3161-3185 [PMID:24228714] |
MT2 receptor/Melatonin receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286] | ||||||||
ChEMBL | Displacement of 2[125I]iodomelatonin from recombinant human MT2 receptor expressed in NIH 3T3 cells | B | 7.33 | pKi | 46.77 | nM | Ki | Eur J Med Chem (2007) 42: 1004-1013 [PMID:17346859] |
ChEMBL | Binding affinity towards recombinant human melatonin receptor type 1B expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay | B | 7.35 | pKi | 44.7 | nM | Ki | J Med Chem (2000) 43: 1050-1061 [PMID:10737738] |
ChEMBL | Displacement of [125I]2-iodomelatonin from human recombinant MT2 receptor expressed in African green monkey COS7 cells | B | 7.99 | pKi | 10.2 | nM | Ki | J Med Chem (2014) 57: 3161-3185 [PMID:24228714] |
GtoPdb | - | - | 8.1 | pKi | - | - | - |
Br J Pharmacol (2000) 129: 877-86 [PMID:10696085]; 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]; J Pharmacol Exp Ther (1988) 246: 902-10 [PMID:2843633] |
Melatonin receptor 1C in Xenopus laevis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5495] [UniProtKB: P49219] | ||||||||
ChEMBL | Antagonist activity in Xenopus laevis melanophores assessed as melatoninergic activity after 60 mins | F | 5.61 | pIC50 | 2454.71 | nM | IC50 | Eur J Med Chem (2007) 42: 1004-1013 [PMID:17346859] |
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]