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ChEMBL ligand: CHEMBL33185 |
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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 MT1 receptor expressed in CHO cells | B | 5.89 | pKi | 1290 | nM | Ki | J Med Chem (2009) 52: 826-833 [PMID:19193160] |
ChEMBL | Antagonist activity at human MT1 receptor | B | 5.89 | pKi | 1290 | nM | Ki | J Med Chem (2014) 57: 3161-3185 [PMID:24228714] |
ChEMBL | Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand | B | 5.89 | pKi | 1288.25 | nM | Ki | J Med Chem (2001) 44: 2900-2912 [PMID:11520198] |
ChEMBL | Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells | B | 5.89 | pKi | 1288.25 | nM | Ki | J Med Chem (2005) 48: 4049-4060 [PMID:15943478] |
MT2 receptor/Melatonin receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286] | ||||||||
ChEMBL | Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells | B | 8.05 | pKi | 9 | nM | Ki | J Med Chem (2009) 52: 826-833 [PMID:19193160] |
ChEMBL | Binding affinity towards melatonin receptor type 1B stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin | B | 8.06 | pKi | 8.71 | nM | Ki | J Med Chem (2001) 44: 2900-2912 [PMID:11520198] |
ChEMBL | Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor MT2 expressed in NIH3T3 rat fibroblast cells | B | 8.06 | pKi | 8.71 | nM | Ki | J Med Chem (2005) 48: 4049-4060 [PMID:15943478] |
ChEMBL | Antagonist activity at human MT2 receptor | B | 8.06 | pKi | 8.7 | nM | Ki | J Med Chem (2014) 57: 3161-3185 [PMID:24228714] |
GtoPdb | - | - | 8.1 | pKi | - | - | - | J Med Chem (2005) 48: 4049-60 [PMID:15943478] |
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]