5-MeOT [Ligand Id: 107] 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: CHEMBL8165 |
|---|
|
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!
|
|
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 |
|---|---|---|---|---|---|---|---|---|
| DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] | ||||||||
| ChEMBL | Induction of DAT-mediated dopamine release in rat brain synaptosomes by [3H]DA release assay | B | 4.96 | pEC50 | 11031 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4754-4758 [PMID:25193229] |
| Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4] | ||||||||
| ChEMBL | Induction of NET-mediated norepinephrine release in rat brain synaptosomes by [3H]NE release assay | B | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4754-4758 [PMID:25193229] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | In vitro affinity at human cloned 5-hydroxytryptamine 1A receptor by [3H]8-OH-DPAT displacement. | B | 8.49 | pKi | 3.2 | nM | Ki | J Med Chem (1996) 39: 314-322 [PMID:8568822] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement | B | 7.97 | pKi | 10.72 | nM | Ki | J Med Chem (1996) 39: 126-134 [PMID:8568799] |
| ChEMBL | Evaluated for the binding affinity to hippocampus striatal membranes at 5-hydroxytryptamine 1A receptor binding site by using [3H]-8-OH- DPAT as a radioligand. | B | 8.05 | pKi | 9 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1A receptor using [3H]-8-OH-DPAT as radioligand | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (1990) 33: 2777-2784 [PMID:2213830] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor | B | 8.49 | pKi | 3.2 | nM | Ki | J Med Chem (1988) 31: 867-870 [PMID:2965244] |
| ChEMBL | Binding affinity of compound towards 5-hydroxytryptamine 1A receptor in rat striatal membranes by [3H]OH-DPAT displacement. | B | 8.49 | pKi | 3.2 | nM | Ki | J Med Chem (1989) 32: 1921-1926 [PMID:2754715] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| GtoPdb | - | - | 7.5 | pKi | - | - | - |
Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658]; J Neurochem (1996) 67: 2096-103 [PMID:8863519] |
| ChEMBL | Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta | B | 8.46 | pKi | 3.5 | nM | Ki | J Med Chem (1996) 39: 314-322 [PMID:8568822] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] | ||||||||
| ChEMBL | Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand. | B | 6.4 | pKi | 400 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| ChEMBL | Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand. | B | 6.4 | pKi | 400 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| ChEMBL | Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate | B | 8.19 | pKi | 6.46 | nM | Ki | J Med Chem (1988) 31: 1406-1412 [PMID:3385733] |
| ChEMBL | Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptor | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (1988) 31: 867-870 [PMID:2965244] |
| 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| ChEMBL | Selectivity towards 5-hydroxytryptamine 1D receptor beta to that of 5-hydroxytryptamine 1D receptor alpha | B | 8.27 | pKi | 5.4 | nM | Ki | J Med Chem (1996) 39: 314-322 [PMID:8568822] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1D receptor was determined in calf striatum homogenate | B | 8.39 | pKi | 4.1 | nM | Ki | J Med Chem (1996) 39: 314-322 [PMID:8568822] |
| GtoPdb | - | - | 8.7 | pKi | - | - | - |
Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658]; Mol Pharmacol (1996) 50: 1567-80 [PMID:8967979]; Mol Pharmacol (1991) 40: 143-8 [PMID:1652050] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Affinity against 5-hydroxytryptamine 2A receptor (K) labeled with [3H]ketanserin. | B | 6.52 | pKi | 300 | nM | Ki | J Med Chem (1994) 37: 1929-1935 [PMID:8027974] |
| ChEMBL | Affinity against 5-hydroxytryptamine 2A receptor (D) labeled with [125I]DOI. | B | 8.32 | pKi | 4.8 | nM | Ki | J Med Chem (1994) 37: 1929-1935 [PMID:8027974] |
| GtoPdb | - | - | 8.9 | pKi | - | - | - | Mol Pharmacol (1994) 45: 277-86 [PMID:8114677] |
| ChEMBL | Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay | F | 9.3 | pEC50 | 0.5 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4754-4758 [PMID:25193229] |
| 5-HT2A receptor in Rat [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| GtoPdb | - | - | 8.1 | pKi | - | - | - | Mol Pharmacol (1994) 45: 277-86 [PMID:8114677] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Evaluated for the binding affinity to porcine choroid plexus at 5-hydroxytryptamine 2C receptor binding site by using [3H]-MES as a radioligand. | B | 7.35 | pKi | 45 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| GtoPdb | - | - | 7.8 | pKi | - | - | - | Synapse (2000) 35: 144-150 [PMID:10611640] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
| GtoPdb | - | - | 6.3 | pKi | - | - | - | J Neurochem (1997) 69: 1138-44 [PMID:9282936] |
| ChEMBL | Affinity against 5-hydroxytryptamine 2C receptor in J1 cells transfected with the rat 5-HT2C gene labeled with [3H]mesulergine. | B | 6.3 | pKi | 500 | nM | Ki | J Med Chem (1994) 37: 1929-1935 [PMID:8027974] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639] | ||||||||
| ChEMBL | Displacement of [3H]GR-113808 from human recombinant 5HT4b receptor expressed in HEK293 cells by scintillation counting | B | 6.61 | pKi | 245.47 | nM | Ki | Eur J Med Chem (2009) 44: 2952-2959 [PMID:19223092] |
| GtoPdb | - | - | 6.8 | pKi | - | - | - |
J Neurochem (1997) 69: 1810-9 [PMID:9349523]; J Neurochem (1998) 70: 2252-61 [PMID:9603189]; J Neurochem (2000) 74: 478-89 [PMID:10646498]; Naunyn Schmiedebergs Arch Pharmacol (2001) 363: 146-60 [PMID:11218067]; Br J Pharmacol (2000) 129: 771-81 [PMID:10683202]; Br J Pharmacol (2000) 131: 827-35 [PMID:11030734] |
| ChEMBL | Displacement of [3H]GR-113808 from human 5HT4b receptor expressed in COS7 cell membrane by scintillation counting | B | 7.57 | pKi | 26.92 | nM | Ki | Eur J Med Chem (2009) 44: 2952-2959 [PMID:19223092] |
| 5-HT4 receptor in Mouse [GtoPdb: 9] [UniProtKB: P97288] | ||||||||
| GtoPdb | - | - | 6.6 | pKi | - | - | - | FEBS Lett (1996) 398: 19-25 [PMID:8946946] |
| 5-HT4 receptor in Rat [GtoPdb: 9] [UniProtKB: Q62758] | ||||||||
| GtoPdb | - | - | 7.4 | pKi | - | - | - |
EMBO J (1995) 14: 2806-15 [PMID:7796807]; Eur J Pharmacol (1996) 304: 231-5 [PMID:8813606]; Neuropharmacology (1997) 36: 671-9 [PMID:9225293] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand | B | 7.06 | pKi | 88 | nM | Ki | J Med Chem (2000) 43: 1011-1018 [PMID:10715164] |
| ChEMBL | Binding affinity for human 5-hydroxytryptamine 6 receptor | B | 7.3 | pKi | <50 | nM | Ki | J Med Chem (2005) 48: 1781-1795 [PMID:15771424] |
| GtoPdb | - | - | 7.4 | pKi | - | - | - | J Neurochem (1996) 66: 47-56 [PMID:8522988] |
| 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388] | ||||||||
| GtoPdb | - | - | 8.4 | pKi | - | - | - |
Mol Pharmacol (1993) 43: 320-7 [PMID:7680751]; Neuropharmacology (1997) 36: 713-20 [PMID:9225298]; J Neurochem (1998) 71: 2169-77 [PMID:9798944] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells | B | 8.3 | pKi | 5.01 | nM | Ki | Eur J Med Chem (2019) 183: 111705-111705 [PMID:31581003] |
| ChEMBL | Binding affinity of compound towards rodent 5-hydroxytryptamine 7 receptor | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| GtoPdb | - | - | 9.5 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2001) 363: 620-32 [PMID:11414657]; Br J Pharmacol (1997) 122: 126-32 [PMID:9298538]; J Biol Chem (1993) 268: 23422-6 [PMID:8226867] |
| 5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304] | ||||||||
| GtoPdb | - | - | 8.2 | pKi | - | - | - | Mol Pharmacol (1993) 44: 229-36 [PMID:8394987] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305] | ||||||||
| ChEMBL | Binding affinity at rat 5-hydroxytryptamine 7 receptor. | B | 9.03 | pKi | 0.93 | nM | Ki | J Med Chem (2003) 46: 5365-5374 [PMID:14640545] |
| GtoPdb | - | - | 9.2 | pKi | - | - | - |
J Biol Chem (1993) 268: 18200-4 [PMID:8394362]; Proc Natl Acad Sci USA (1993) 90: 8547-51 [PMID:8397408] |
| SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| ChEMBL | Induction of 5-HTT-mediated 5-HT release in rat brain synaptosomes by [3H]5-HT release assay | B | 5.66 | pEC50 | 2169 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4754-4758 [PMID:25193229] |
| TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7] | ||||||||
| ChEMBL | Antagonist activity at human TRPM8 receptor expressed in human T-REx-293 cells assessed as inhibition of menthol-induced 45calcium influx treated 5 mins before menthol challenge measured after 5 mins | F | 4.91 | pIC50 | 12400 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7076-7079 [PMID:20965726] |
| ChEMBL | Antagonist activity at human TRPM8 receptor expressed in human T-REx-293 cells assessed as inhibition of icilin-induced 45calcium influx treated 5 mins before icilin challenge measured after 5 mins | F | 4.94 | pIC50 | 11600 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7076-7079 [PMID:20965726] |
| 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
| GtoPdb | - | - | 6.2 | pKi | - | - | - |
J Neurochem (1996) 67: 2096-103 [PMID:8863519]; Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]; Eur J Pharmacol (2004) 484: 127-39 [PMID:14744596]; Bioorg Med Chem (2004) 12: 2545-52 [PMID:15110837] |
| 5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939] | ||||||||
| GtoPdb | - | - | 5.9 | pKi | - | - | - | Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639] |
| 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994] | ||||||||
| GtoPdb | - | - | 8 | pKi | - | - | - | Mol Pharmacol (1993) 43: 419-26 [PMID:8450835] |
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]
