K185 [Ligand Id: 1359] 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: CHEMBL274438
  • 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 Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay B 7.18 pKi 66.1 nM Ki J Med Chem (2000) 43: 1050-1061 [PMID:10737738]
ChEMBL Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in mouse NIH3T3 cells B 7.18 pKi 66.1 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 7.18 pKi 66.07 nM Ki J Med Chem (2005) 48: 4049-4060 [PMID:15943478]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells B 7.18 pKi 66 nM Ki J Med Chem (2009) 52: 826-833 [PMID:19193160]
GtoPdb - - 7.2 pKi - - - J Med Chem (2000) 43: 1050-61 [PMID:10737738]
MT2 receptor/Melatonin receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286]
GtoPdb - - 9.29 pKi 0.51 nM Ki J Med Chem (2000) 43: 1050-61 [PMID:10737738];
Reprod Nutr Dev (1999) 39: 335-44 [PMID:10420436]
ChEMBL Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor MT2 expressed in NIH3T3 rat fibroblast cells B 9.3 pKi 0.5 nM Ki J Med Chem (2005) 48: 4049-4060 [PMID:15943478]
ChEMBL Binding affinity towards recombinant human melatonin receptor type 1B expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay B 9.3 pKi 0.5 nM Ki J Med Chem (2000) 43: 1050-1061 [PMID:10737738]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells B 9.3 pKi 0.5 nM Ki J Med Chem (2009) 52: 826-833 [PMID:19193160]
ChEMBL Displacement of [125I]2-iodomelatonin from human recombinant MT2 receptor expressed in mouse NIH3T3 cells B 9.3 pKi 0.5 nM Ki J Med Chem (2014) 57: 3161-3185 [PMID:24228714]

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]