IIK7 [Ligand Id: 1350] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL10009
  • MT1 receptor/Melatonin receptor 1A in Human [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039]
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  • MT2 receptor/Melatonin receptor 1B in Human [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286]
  • MT2 receptor in Mouse [GtoPdb: 288] [UniProtKB: Q8CIQ6]
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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]
GtoPdb - - 8.3 pKi - - - J Med Chem (2000) 43: 1050-61 [PMID:10737738]
ChEMBL Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay B 8.35 pKi 4.47 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 8.35 pKi 4.47 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]
GtoPdb - - 10.3 pKi 0.05 nM Ki J Med Chem (2000) 43: 1050-61 [PMID:10737738];
Reprod Nutr Dev (1999) 39: 335-44 [PMID:10420436]
ChEMBL Binding affinity towards recombinant human melatonin receptor type 1B expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay B 10.3 pKi 0.05 nM Ki J Med Chem (2000) 43: 1050-1061 [PMID:10737738]
ChEMBL Displacement of [125I]2-iodomelatonin from human recombinant MT2 receptor expressed in mouse NIH3T3 cells B 10.3 pKi 0.05 nM Ki J Med Chem (2014) 57: 3161-3185 [PMID:24228714]
MT2 receptor in Mouse [GtoPdb: 288] [UniProtKB: Q8CIQ6]
GtoPdb - - 10.3 pKi 0.05 nM Ki Sci Signal (2013) 6: ra89 [PMID:24106342]

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]