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: CHEMBL45 (5-methoxy n-acetyl-tryptamine, BCI-049, Circadin, General nutrit, Health aid, Heidadouppi, Icenia, J5.258B, Life ext, Melapure, Melatol, Melatonin, Melatonine, Melatonin neurim, 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) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 |
---|---|---|---|---|---|---|---|---|
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 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assay | B | 9.56 | pKi | 0.28 | nM | Ki | J Med Chem (2022) 65: 11229-11240 [PMID:35930058] |
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 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 [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 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-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay | B | 9.62 | pKi | 0.24 | nM | Ki | J Med Chem (2021) 64: 3059-3074 [PMID:33682410] |
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 cells | B | 9.62 | pKi | 0.24 | nM | Ki | J Med Chem (2011) 54: 4207-4218 [PMID:21568291] |
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 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 [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 | 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 | 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 | Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis | B | 9.74 | pKi | 0.18 | nM | Ki | J Med Chem (2021) 64: 1904-1929 [PMID:33626870] |
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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis | F | 9.96 | pEC50 | 0.11 | nM | EC50 | J Med Chem (2021) 64: 1904-1929 [PMID:33626870] |
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 melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay | F | 10.16 | pEC50 | 0.07 | nM | EC50 | J Med Chem (2022) 65: 11229-11240 [PMID:35930058] |
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] |
ChEMBL | Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay | F | 10.66 | pEC50 | 0.02 | nM | EC50 | J Med Chem (2021) 64: 3059-3074 [PMID:33682410] |
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 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 | 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 for human recombinant Melatonin receptor type 2 expressed in NIH3T3 cells | B | 9.55 |