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ChEMBL ligand: CHEMBL289233 (2-Iodomelatonin, Iodomelatonin) |
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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 human Melatonin receptor type 1A expressed in CHO cells | B | 10.1 | pKi | 0.08 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2409-2414 |
ChEMBL | Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells | B | 10.17 | pKi | 0.07 | nM | Ki | J Med Chem (2014) 57: 3161-3185 [PMID:24228714] |
ChEMBL | Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells | B | 10.89 | pKi | 0.01 | nM | Ki | J Med Chem (2002) 45: 1853-1859 [PMID:11960497] |
GtoPdb | - | - | 11 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2003) 367: 553-61 [PMID:12764576]; J Pharmacol Exp Ther (1985) 234: 395-401 [PMID:2991499] |
ChEMBL | Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates. | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (1998) 41: 4453-4465 [PMID:9804685] |
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 | 9.66 | pKi | 0.22 | nM | Ki | J Med Chem (2014) 57: 3161-3185 [PMID:24228714] |
ChEMBL | Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1B expressed in HEK293 cells | B | 9.8 | pKi | 0.16 | nM | Ki | J Med Chem (2002) 45: 1853-1859 [PMID:11960497] |
ChEMBL | Compound was tested for binding affinity against human Melatonin receptor type 1B in CHO cells | B | 9.82 | pKi | 0.15 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2409-2414 |
GtoPdb | - | - | 10.3 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2003) 367: 553-61 [PMID:12764576]; Naunyn Schmiedebergs Arch Pharmacol (1997) 355: 365-75 [PMID:9089668]; J Pharmacol Exp Ther (1998) 285: 1239-45 [PMID:9618428]; J Pharmacol Exp Ther (1985) 234: 395-401 [PMID:2991499] |
Quinone reductase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3959] [UniProtKB: P16083] | ||||||||
ChEMBL | Inhibition of 2-[125I]iodomelatonin binding to Melatonin receptor 3 (MT3) of Syrian hamster brain membrane | B | 8.19 | pKi | 6.5 | nM | Ki | J Med Chem (2002) 45: 1853-1859 [PMID:11960497] |
ChEMBL | Inhibition of human quinone reductase 2 expressed in Escherichia coli BL21(DE3) incubated at 23 degC by MTT assay | B | 5.96 | pIC50 | 1100 | nM | IC50 | J Med Chem (2009) 52: 1873-1884 [PMID:19265439] |
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]