[3H]melatonin [Ligand Id: 1357] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL45 (5-methoxy n-acetyl-tryptamine, BCI-049, Circadin, General nutrit, Health aid, Heidadouppi, Icenia, J5.258B, Life ext, Melapure, Melatol, Melatonin, Melatonine, Melovine, N-(2-(5-Methoxy-1H-Indol-3-Yl)Ethyl)Acetamide, N-Acetyl-5-Methoxytryptamine, Natrol, Nature's blend, Natures bounty, NSC-113928, NSC-302012, NSC-56423, Quality health, Regulin, S.gard, Tartrol, Travelag, Vespro, Vytalonin)
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  • Butyrylcholinesterase in Equus caballus [ChEMBL: CHEMBL5077] [UniProtKB: Q9N1N9]
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  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
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  • MT1 receptor/Melatonin receptor 1A in Human [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039]
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  • Melatonin receptor 1C in Xenopus laevis [ChEMBL: CHEMBL5495] [UniProtKB: P49219]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acetylcholinesterase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4768] [UniProtKB: P23795]
ChEMBL Inhibition of AchE from bovine erythrocytes B 7 pIC50 >100 nM IC50 J. Med. Chem. (2006) 49: 459-462 [PMID:16420031]
Butyrylcholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5077] [UniProtKB: Q9N1N9]
ChEMBL Inhibition of BuChE from horse serum B 7 pIC50 >100 nM IC50 J. Med. Chem. (2006) 49: 459-462 [PMID:16420031]
CYP1B1/Cytochrome P450 1B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4878] [GtoPdb: 1320] [UniProtKB: Q16678]
ChEMBL Mixed type inhibition of human hepatic microsomes CYP1B1 expressed in supersomes coexpressing NADPH-cytochrome P450 reductase using 7-Ethoxyresorufin as substrate measured every 30 secs for 3 mins in presence of NADPH by spectrofluorometric analysis B 4.85 pKi 14000 nM Ki Eur J Med Chem (2017) 135: 296-306 [PMID:28458135]
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL Displacement of [3H]-N-alpha-methylhistamine from human H3 receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method B 9.3 pKi 0.5 nM Ki J Med Chem (2019) 62: 11416-11422 [PMID:31724859]
MT1 receptor/Melatonin receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039]
ChEMBL Binding affinity to melatonin receptor MT1 (unknown origin) B 9.82 pKd 0.15 nM Kd MedChemComm (2015) 6: 1340-1344
GtoPdb - - 9.9 pKd 0.13 nM Kd Br J Pharmacol (2000) 129: 877-86 [PMID:10696085]
ChEMBL Binding affinity to MT1 receptor (unknown origin) assessed as inhibition constant B 9.06 pKi 0.88 nM Ki Eur J Med Chem (2020) 185: 111847-111847 [PMID:31727472]
ChEMBL Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method B 9.06 pKi 0.88 nM Ki Eur J Med Chem (2020) 185: 111847-111847 [PMID:31727472]
ChEMBL Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay B 9.18 pKi 0.66 nM Ki J. Med. Chem. (2000) 43: 1050-1061 [PMID:10737738]
ChEMBL Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assay B 9.18 pKi 0.66 nM Ki Eur J Med Chem (2020) 185: 111847-111847 [PMID:31727472]
ChEMBL Binding affinity towards human melatonin receptor type 1A B 9.28 pKi 0.53 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1023-1026 [PMID:15013015]
ChEMBL Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells B 9.28 pKi 0.53 nM Ki Bioorg. Med. Chem. (2008) 16: 7654-7661 [PMID:18657980]
ChEMBL Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting method B 9.34 pKi 0.46 nM Ki Eur J Med Chem (2020) 185: 111847-111847 [PMID:31727472]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells B 9.34 pKi 0.46 nM Ki J. Med. Chem. (2009) 52: 826-833 [PMID:19193160]
ChEMBL Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells B 9.34 pKi 0.46 nM Ki MedChemComm (2011) 2: 991-994
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting B 9.34 pKi 0.46 nM Ki Bioorg. Med. Chem. (2009) 17: 4583-4594 [PMID:19473848]
ChEMBL Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis B 9.34 pKi 0.46 nM Ki MedChemComm (2015) 6: 1340-1344
ChEMBL Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells. B 9.4 pKi 0.4 nM Ki Bioorg. Med. Chem. Lett. (2003) 13: 4381-4384 [PMID:14643330]
ChEMBL Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A B 9.4 pKi 0.4 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1197-1200 [PMID:14980664]
ChEMBL Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand B 9.4 pKi 0.4 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 3799-3802 [PMID:15203165]
ChEMBL Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells B 9.41 pKi 0.39 nM Ki J. Med. Chem. (2006) 49: 3509-3519 [PMID:16759094]
ChEMBL Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells B 9.41 pKi 0.39 nM Ki Eur. J. Med. Chem. (2007) 42: 1004-1013 [PMID:17346859]
ChEMBL Displacement of [125I]2-iodomelatonin from human MT1 receptor B 9.43 pKi 0.37 nM Ki J. Med. Chem. (2011) 54: 5320-5334 [PMID:21726069]
ChEMBL Binding affinity to human MT1A receptor by radioligand displacement assay B 9.46 pKi 0.35 nM Ki Eur. J. Med. Chem. (2013) 63: 85-94 [PMID:23466604]
ChEMBL Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins B 9.48 pKi 0.33 nM Ki Bioorg. Med. Chem. (2010) 18: 6496-6511 [PMID:20674373]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells B 9.49 pKi 0.32 nM Ki J. Med. Chem. (2006) 49: 7393-7403 [PMID:17149869]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis B 9.52 pKi 0.3 nM Ki J Nat Prod (2017) 80: 3324-3329 [PMID:29144746]
ChEMBL Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A B 9.52 pKi 0.3 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 5157-5160 [PMID:15380218]
ChEMBL Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin B 9.52 pKi 0.3 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 1345-1349 [PMID:15713384]
ChEMBL Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method B 9.53 pKi 0.3 nM Ki Bioorg. Med. Chem. (2013) 21: 547-552 [PMID:23228808]
ChEMBL Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting B 9.53 pKi 0.3 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 2582-2585 [PMID:20227878]
ChEMBL Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells B 9.53 pKi 0.3 nM Ki J. Med. Chem. (1998) 41: 3624-3634 [PMID:9733487]
ChEMBL Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells B 9.54 pKi 0.29 nM Ki J. Med. Chem. (2005) 48: 4049-4060 [PMID:15943478]
ChEMBL Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells B 9.54 pKi 0.29 nM Ki J. Med. Chem. (2004) 47: 4202-4212 [PMID:15293992]
ChEMBL Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand B 9.54 pKi 0.29 nM Ki J. Med. Chem. (2001) 44: 2900-2912 [PMID:11520198]
ChEMBL Displacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysis B 9.57 pKi 0.27 nM Ki Eur J Med Chem (2020) 190: 112090-112090 [PMID:32018096]
ChEMBL Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells B 9.58 pKi 0.26 nM Ki Bioorg. Med. Chem. (2007) 15: 4543-4551 [PMID:17459711]
ChEMBL Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane B 9.58 pKi 0.26 nM Ki Bioorg. Med. Chem. (2011) 19: 4910-4916 [PMID:21775151]
ChEMBL Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay B 9.6 pKi 0.25 nM Ki Eur. J. Med. Chem. (2016) 109: 268-275 [PMID:26785296]
ChEMBL Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells B 9.6 pKi 0.25 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 2316-2319 [PMID:21420861]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay B 9.6 pKi 0.25 nM Ki Eur. J. Med. Chem. (2011) 46: 4252-4257 [PMID:21764185]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells B 9.62 pKi 0.24 nM Ki J. Med. Chem. (2011) 54: 4207-4218 [PMID:21568291]
ChEMBL Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting B 9.62 pKi 0.24 nM Ki J. Med. Chem. (2011) 54: 3436-3444 [PMID:21473625]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins B 9.64 pKi 0.23 nM Ki Eur. J. Med. Chem. (2016) 109: 360-370 [PMID:26820449]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells B 9.66 pKi 0.22 nM Ki Eur. J. Med. Chem. (2011) 46: 1835-1840 [PMID:21392858]
ChEMBL Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis B 9.69 pKi 0.2 nM Ki J Med Chem (2018) 61: 7902-7916 [PMID:30126274]
ChEMBL Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis B 9.69 pKi 0.2 nM Ki Eur J Med Chem (2020) 185: 111847-111847 [PMID:31727472]
ChEMBL Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting B 9.7 pKi 0.2 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 430-434 [PMID:23265885]
ChEMBL Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells B 9.7 pKi 0.2 nM Ki Bioorg. Med. Chem. (2007) 15: 4643-4650 [PMID:17481904]
ChEMBL Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells B 9.7 pKi 0.2 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 2409-2414
ChEMBL Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand) B 9.7 pKi 0.2 nM Ki J. Med. Chem. (2000) 43: 4051-4062 [PMID:11063602]
ChEMBL Binding Affinity (pKi) towards human Melatonin receptor type 1A B 9.78 pKi 0.17 nM Ki J. Med. Chem. (2003) 46: 1429-1439 [PMID:12672242]
ChEMBL Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells B 9.85 pKi 0.14 nM Ki J. Med. Chem. (2007) 50: 6618-6626 [PMID:18052314]
ChEMBL Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand B 9.85 pKi 0.14 nM Ki J. Med. Chem. (2003) 46: 1127-1129 [PMID:12646022]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting B 9.85 pKi 0.14 nM Ki Eur. J. Med. Chem. (2014) 86: 700-709 [PMID:25232966]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells B 9.85 pKi 0.14 nM Ki Bioorg. Med. Chem. (2008) 16: 8339-8348 [PMID:18778943]
ChEMBL Binding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cells B 9.89 pKi 0.13 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 2177-2180
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins B 9.92 pKi 0.12 nM Ki Eur J Med Chem (2017) 127: 621-631 [PMID:28131094]
ChEMBL Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand. B 9.92 pKi 0.12 nM Ki J. Med. Chem. (2002) 45: 2788-2800 [PMID:12061881]
ChEMBL Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells B 9.92 pKi 0.12 nM Ki J. Med. Chem. (2002) 45: 1853-1859 [PMID:11960497]
ChEMBL Displacement of radiolabeled melatonin from human MT1 receptor B 9.96 pKi 0.11 nM Ki J. Med. Chem. (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins B 10.04 pKi 0.09 nM Ki J. Med. Chem. (2015) 58: 4998-5014 [PMID:26023814]
ChEMBL Displacement of 2-[125I]iodomelatonin from human recombinant MT1 expressed in CHO cell membranes incubated for 60 mins by liquid scintillation spectrometry B 10.04 pKi 0.09 nM Ki Eur. J. Med. Chem. (2015) 103: 370-373 [PMID:26367450]
ChEMBL Binding affinity against human Melatonin receptor type 1A (MT1) B 10.08 pKi 0.08 nM Ki J. Med. Chem. (2002) 45: 4222-4239 [PMID:12213063]
ChEMBL Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cells B 10.1 pKi 0.08 nM Ki J. Med. Chem. (1997) 40: 4195-4198 [PMID:9435890]
ChEMBL Binding affinity for melatonin 1A receptor was 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]
ChEMBL In vitro receptor binding at MT1 (Melatonin) receptor. B 9.22 pIC50 0.6 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1199-1202 [PMID:12643943]
ChEMBL Binding affinity to human ML1A receptor by radioligand displacement assay B 9.28 pIC50 0.53 nM IC50 Bioorg. Med. Chem. (2013) 21: 2764-2771 [PMID:23582449]
ChEMBL Binding affinity to human MT1A receptor by radioligand displacement assay B 9.36 pIC50 0.44 nM IC50 Eur. J. Med. Chem. (2013) 63: 85-94 [PMID:23466604]
ChEMBL Binding affinity to human MT1 receptor B 9.7 pIC50 0.2 nM IC50 Eur. J. Med. Chem. (2011) 46: 1622-1629 [PMID:21377769]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells B 9.7 pIC50 0.2 nM IC50 Bioorg. Med. Chem. (2008) 16: 4954-4962 [PMID:18372181]
ChEMBL Displacement of radiolabeled melatonin from human MT1 receptor B 9.74 pIC50 0.18 nM IC50 J. Med. Chem. (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Displacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cells B 9.96 pIC50 0.11 nM IC50 Bioorg. Med. Chem. (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method B 9.96 pIC50 0.11 nM IC50 Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
ChEMBL Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A F 8.65 pEC50 2.24 nM EC50 J. Med. Chem. (2003) 46: 1127-1129 [PMID:12646022]
ChEMBL Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay F 8.66 pEC50 2.2 nM EC50 Bioorg. Med. Chem. (2010) 18: 3426-3436 [PMID:20444610]
ChEMBL Intrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A F 8.72 pEC50 1.92 nM EC50 J. Med. Chem. (2002) 45: 2788-2800 [PMID:12061881]
ChEMBL Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay F 8.82 pEC50 1.5 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 2316-2319 [PMID:21420861]
ChEMBL Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay F 9 pEC50 1 nM EC50 Bioorg Med Chem (2019) 27: 3299-3306 [PMID:31204226]
ChEMBL Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay F 10.01 pEC50 0.1 nM EC50 J. Med. Chem. (2015) 58: 4998-5014 [PMID:26023814]
ChEMBL Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader F 10.59 pEC50 0.03 nM EC50 J. Med. Chem. (2011) 54: 4207-4218 [PMID:21568291]
ChEMBL Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers F 10.59 pEC50 0.03 nM EC50 J. Med. Chem. (2011) 54: 3436-3444 [PMID:21473625]
Melatonin receptor 1B in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4466] [UniProtKB: P51050]
ChEMBL Binding affinity measured against Chicken brain melatonin receptor by using 2-[125I]iodomelatonin as radioligand B 9.15 pKi 0.7 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 3325-3330 [PMID:9873728]
MT2 receptor/Melatonin receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286]
GtoPdb - - 9.6 pKd 0.28 nM Kd Br J Pharmacol (2000) 129: 877-86 [PMID:10696085]
ChEMBL Binding affinity to melatonin receptor MT2 (unknown origin) B 9.82 pKd 0.15 nM Kd MedChemComm (2015) 6: 1340-1344
ChEMBL Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT2 expressed in CHO cells after 1 hr by gamma counting analysis B 9.02 pKi 0.95 nM Ki MedChemComm (2015) 6: 1340-1344
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells by gamma counting B 9.02 pKi 0.95 nM Ki Bioorg. Med. Chem. (2009) 17: 4583-4594 [PMID:19473848]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells B 9.02 pKi 0.95 nM Ki J. Med. Chem. (2009) 52: 826-833 [PMID:19193160]
ChEMBL Displacement of 2-[125I]-iodomelatonin from human MT2 receptor expressed in CHO cells B 9.02 pKi 0.95 nM Ki MedChemComm (2011) 2: 991-994
ChEMBL Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in CHO cells incubated for 1 hr by gamma counting method B 9.02 pKi 0.95 nM Ki Eur J Med Chem (2020) 185: 111847-111847 [PMID:31727472]
ChEMBL Displacement of 2-[125I]iodomelatonin from human melatonin MT2 receptor expressed in CHO cells B 9.13 pKi 0.74 nM Ki Bioorg. Med. Chem. (2008) 16: 7654-7661 [PMID:18657980]
ChEMBL Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1B B 9.15 pKi 0.7 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 5157-5160 [PMID:15380218]
ChEMBL Binding affinity against Melatonin receptor type 1B stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin B 9.15 pKi 0.7 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 1345-1349 [PMID:15713384]
ChEMBL Displacement of [125I]iodomelatonin from human cloned MT2 receptor expressed in rat NIH3T3 cells after 90 mins B 9.21 pKi 0.62 nM Ki Bioorg. Med. Chem. (2010) 18: 6496-6511 [PMID:20674373]
ChEMBL Binding affinity for melatonin receptor type 1B, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand) B 9.28 pKi 0.53 nM Ki J. Med. Chem. (2000) 43: 4051-4062 [PMID:11063602]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cell membranes after 120 mins B 9.28 pKi 0.52 nM Ki Eur. J. Med. Chem. (2016) 109: 360-370 [PMID:26820449]
ChEMBL Displacement of [125I]2-iodomelatonin from human recombinant MT2 receptor expressed in HEK293 cells after 2 hrs by gamma counting B 9.3 pKi 0.5 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 430-434 [PMID:23265885]
ChEMBL Displacement of [3H]melatonin from human MT2 receptor expressed in CHO cells after 60 mins by microbeta scintillation method B 9.37 pKi 0.43 nM Ki Bioorg. Med. Chem. (2013) 21: 547-552 [PMID:23228808]
ChEMBL Displacement of [3H]melatonin from human melatonin MT2 receptor expressed in CHO cells after 60 mins by scintillation counting B 9.37 pKi 0.43 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 2582-2585 [PMID:20227878]
ChEMBL Binding affinity for human Melatonin receptor type 1B stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand B 9.39 pKi 0.41 nM Ki J. Med. Chem. (2003) 46: 1127-1129 [PMID:12646022]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT2 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting B 9.39 pKi 0.41 nM Ki Eur. J. Med. Chem. (2014) 86: 700-709 [PMID:25232966]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells B 9.39 pKi 0.41 nM Ki Bioorg. Med. Chem. (2008) 16: 8339-8348 [PMID:18778943]
ChEMBL Displacement of 2[125I]iodomelatonin from recombinant human MT2 receptor expressed in NIH 3T3 cells B 9.45 pKi 0.35 nM Ki Eur. J. Med. Chem. (2007) 42: 1004-1013 [PMID:17346859]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells B 9.46 pKi 0.35 nM Ki Eur. J. Med. Chem. (2011) 46: 1835-1840 [PMID:21392858]
ChEMBL Displacement of 2-[125I]iodomelatonin from human recombinant MT2 receptor expressed in NIH3T3 cells B 9.46 pKi 0.35 nM Ki J. Med. Chem. (2006) 49: 3509-3519 [PMID:16759094]
ChEMBL Displacement of 2-[125I]-iodomelatonin from human MT2 receptor expressed in HEK293 cells B 9.47 pKi 0.34 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 2316-2319 [PMID:21420861]
ChEMBL Displacement of [125I]2-Iodomelatonin from human MT2 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay B 9.47 pKi 0.34 nM Ki Eur. J. Med. Chem. (2016) 109: 268-275 [PMID:26785296]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in human HEK293 cells by radioligand binding assay B 9.47 pKi 0.34 nM Ki Eur. J. Med. Chem. (2011) 46: 4252-4257 [PMID:21764185]
ChEMBL Displacement of 2[125I]iodomelatonin from human recombinant MT2 receptor expressed in NIH3T3 cells B 9.47 pKi 0.34 nM Ki Bioorg. Med. Chem. (2007) 15: 4543-4551 [PMID:17459711]
ChEMBL Displacement of 2-[125I]iodomelatonin from human cloned MT2 receptor expressed in mouse NIH-3T3 cell membrane B 9.47 pKi 0.34 nM Ki Bioorg. Med. Chem. (2011) 19: 4910-4916 [PMID:21775151]
ChEMBL Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in NIH3T3 cells membranes by radioligand binding assay B 9.48 pKi 0.33 nM Ki Eur J Med Chem (2020) 185: 111847-111847 [PMID:31727472]
ChEMBL Binding affinity towards recombinant human melatonin receptor type 1B expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay B 9.48 pKi 0.33 nM Ki J. Med. Chem. (2000) 43: 1050-1061 [PMID:10737738]
ChEMBL Binding affinity towards human melatonin receptor type 1B B 9.49 pKi 0.32 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1023-1026 [PMID:15013015]
ChEMBL Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1B expressed in HEK293 cells B 9.51 pKi 0.31 nM Ki J. Med. Chem. (2002) 45: 1853-1859 [PMID:11960497]
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 9.51 pKi 0.31 nM Ki J. Med. Chem. (2002) 45: 2788-2800 [PMID:12061881]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in HEK or CHO cell membranes after 120 mins B 9.51 pKi 0.31 nM Ki Eur J Med Chem (2017) 127: 621-631 [PMID:28131094]
ChEMBL Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis B 9.52 pKi 0.3 nM Ki Eur J Med Chem (2020) 185: 111847-111847 [PMID:31727472]
ChEMBL Binding affinity against human Melatonin receptor type 1B by using 2-[125I]iodomelatonin as radioligand B 9.52 pKi 0.3 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 3799-3802 [PMID:15203165]
ChEMBL Binding affinity against human MT2 melatonin receptor expressed in NIH3T3 cells B 9.52 pKi 0.3 nM Ki Bioorg. Med. Chem. Lett. (2003) 13: 4381-4384 [PMID:14643330]
ChEMBL Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1B B 9.52 pKi 0.3 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1197-1200 [PMID:14980664]
ChEMBL Displacement of 2-[125I]iodomelatonin from human cloned MT2 receptor expressed in rat NIH3T3 cells B 9.52 pKi 0.3 nM Ki Bioorg. Med. Chem. (2007) 15: 4643-4650 [PMID:17481904]
ChEMBL Binding Affinity (pKi) towards human Melatonin receptor type 1B B 9.53 pKi 0.3 nM Ki J. Med. Chem. (2003) 46: 1429-1439 [PMID:12672242]
ChEMBL Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1B expressed in CHO cells B 9.54 pKi 0.29 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 2409-2414
ChEMBL Displacement of [125I]iodomelatonin from human MT2 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis B 9.54 pKi 0.29 nM Ki J Med Chem (2018) 61: 7902-7916 [PMID:30126274]
ChEMBL Binding affinity for human recombinant Melatonin receptor type 2 expressed in NIH3T3 cells B 9.55 pKi 0.28 nM Ki J. Med. Chem. (2004) 47: 4202-4212 [PMID:15293992]
ChEMBL Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1B (MT2) expressed in NIH3T3 rat fibroblast cells B 9.55 pKi 0.28 nM Ki J. Med. Chem. (2005) 48: 4049-4060 [PMID:15943478]
ChEMBL Binding affinity towards melatonin receptor type 1B stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin B 9.55 pKi 0.28 nM Ki J. Med. Chem. (2001) 44: 2900-2912 [PMID:11520198]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in NIH3T3 cells B 9.59 pKi 0.26 nM Ki J. Med. Chem. (2006) 49: 7393-7403 [PMID:17149869]
ChEMBL Displacement of 2-[125I]iodomelatonin from human cloned MT2 receptor expressed in rat NIH3T3 cells B 9.62 pKi 0.24 nM Ki J. Med. Chem. (2007) 50: 6618-6626 [PMID:18052314]
ChEMBL Binding affinity against human Melatonin receptor type 1B by displacement of [125I]iodomelatonin stably expressed in CHO cells B 9.64 pKi 0.23 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 2177-2180
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells B 9.68 pKi 0.21 nM Ki J. Med. Chem. (2011) 54: 4207-4218 [PMID:21568291]
ChEMBL Displacement of [125I]-2-iodomelatonin from human MT2 receptor expressed on CHO cells microscintillation counting B 9.68 pKi 0.21 nM Ki J. Med. Chem. (2011) 54: 3436-3444 [PMID:21473625]
ChEMBL Binding affinity against human Melatonin receptor type 1B (MT2) B 9.71 pKi 0.2 nM Ki J. Med. Chem. (2002) 45: 4222-4239 [PMID:12213063]
ChEMBL Binding affinity to MT2 receptor (unknown origin) assessed as inhibition constant B 9.74 pKi 0.18 nM Ki Eur J Med Chem (2020) 185: 111847-111847 [PMID:31727472]
ChEMBL Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method B 9.74 pKi 0.18 nM Ki Eur J Med Chem (2020) 185: 111847-111847 [PMID:31727472]
ChEMBL Displacement of 2-[125I]iodomelatonin from human recombinant MT2 expressed in CHO cell membranes incubated for 60 mins by liquid scintillation spectrometry B 9.82