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ChEMBL ligand: CHEMBL33549 |
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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 | Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells | B | 7.39 | pKi | 40.74 | nM | Ki | J Med Chem (2005) 48: 4049-4060 [PMID:15943478] |
ChEMBL | Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand. | B | 7.39 | pKi | 40.6 | nM | Ki | J Med Chem (2002) 45: 2788-2800 [PMID:12061881] |
ChEMBL | Displacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cells | B | 7.39 | pKi | 40.6 | nM | Ki | J Med Chem (2014) 57: 3161-3185 [PMID:24228714] |
GtoPdb | - | - | 7.5 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2003) 367: 553-61 [PMID:12764576] |
ChEMBL | Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells | B | 7.57 | pKi | 27 | nM | Ki | J Med Chem (2009) 52: 826-833 [PMID:19193160] |
ChEMBL | Intrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A | F | 7.43 | pEC50 | 37 | nM | EC50 | J Med Chem (2002) 45: 2788-2800 [PMID:12061881] |
MT2 receptor/Melatonin receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286] | ||||||||
ChEMBL | Displacement of [125I]2-iodomelatonin from MT2 receptor (unknown origin) expressed in HEK293 cells | B | 9.48 | pKi | 0.33 | nM | Ki | J Med Chem (2014) 57: 3161-3185 [PMID:24228714] |
ChEMBL | Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor MT2 expressed in NIH3T3 rat fibroblast cells | B | 9.49 | pKi | 0.32 | nM | Ki | J Med Chem (2005) 48: 4049-4060 [PMID:15943478] |
ChEMBL | Binding affinity on human melatonin receptor type 1B stably transfected in human embryonic kidney (HEK 293) cells using 2-[125I]iodomelatonin as radioligand. | B | 9.49 | pKi | 0.32 | nM | Ki | J Med Chem (2002) 45: 2788-2800 [PMID:12061881] |
GtoPdb | - | - | 9.6 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2003) 367: 553-61 [PMID:12764576] |
ChEMBL | Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells | B | 9.6 | pKi | 0.25 | nM | Ki | J Med Chem (2009) 52: 826-833 [PMID:19193160] |
ChEMBL | Intrinsic activity at human Melatonin receptor type 1B evaluated on [35S]GTP-gamma-S, binding in Chinese hamster ovarian (CHO) cells | F | 9.14 | pEC50 | 0.72 | nM | EC50 | J Med Chem (2002) 45: 2788-2800 [PMID:12061881] |
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]