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: CHEMBL7257 ([2-(5-Methoxy-1H-Indol-3-Yl)-Ethyl]-Dimethyl-Amine, 5-meo-dmt, 5-methoxydimethyltryptamine, 5-methoxy-n-dimethyltryptamine, 5-OME-DMT, Mebufotenin, NSC-88624) |
---|
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 |
---|---|---|---|---|---|---|---|---|
Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275] | ||||||||
ChEMBL | Inhibition of Electric eel AChE assessed as amount of thiocholine released using acetylthiocholine iodide as substrate after 6 mins by Ellman's method | B | 4.85 | pIC50 | 14000 | nM | IC50 | J Nat Prod (2014) 77: 650-656 [PMID:24521095] |
MT1 receptor/Melatonin receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039] | ||||||||
ChEMBL | Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins | B | 6.68 | pKi | 210 | nM | Ki | J Med Chem (2015) 58: 4998-5014 [PMID:26023814] |
ChEMBL | Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay | F | 6.59 | pEC50 | 257 | nM | EC50 | J Med Chem (2015) 58: 4998-5014 [PMID:26023814] |
MT2 receptor/Melatonin receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286] | ||||||||
ChEMBL | Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-2 transfected in CHO cell membranes after 120 mins | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2015) 58: 4998-5014 [PMID:26023814] |
ChEMBL | Agonist activity at human melatonin receptor-2 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay | F | 6.95 | pEC50 | 112 | nM | EC50 | J Med Chem (2015) 58: 4998-5014 [PMID:26023814] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
ChEMBL | Displacement of [3H]8-OH-DPAT from 5HT1A receptor by vacuum filtration | B | 7.55 | pKi | 28 | nM | Ki | J Nat Prod (1997) 60: 1196-1198 |
ChEMBL | Binding affinity against 5-hydroxytryptamine 1A receptor | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (1992) 35: 4503-4505 [PMID:1447752] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
ChEMBL | Affinity on 5-hydroxytryptamine 1A receptor labeled by [3H]8-OH-DPAT | B | 7.16 | pKi | 69 | nM | Ki | J Med Chem (1992) 35: 2061-2064 [PMID:1534585] |
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 | 7.7 | pKi | 20 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
ChEMBL | Displacement of [3H]8-OH DPAT from rat 5HT1A receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2015) 58: 4998-5014 [PMID:26023814] |
ChEMBL | Binding affinity of compound towards 5-hydroxytryptamine 1A receptor in rat striatal membranes by [3H]OH-DPAT displacement. | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1989) 32: 1921-1926 [PMID:2754715] |
ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor | B | 8.11 | pKi | 7.8 | nM | Ki | J Med Chem (1988) 31: 867-870 [PMID:2965244] |
ChEMBL | Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement | B | 8.26 | pKi | 5.5 | nM | Ki | J Med Chem (1996) 39: 126-134 [PMID:8568799] |
ChEMBL | Compound was evaluated for binding affinity towards 5-hydroxytryptamine 1A receptor in rat cortex using [3H]-8-OH-DPAT as radioligand | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (1992) 35: 3625-3632 [PMID:1433172] |
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
ChEMBL | Binding affinity against 5-hydroxytryptamine 1B receptor | B | 6.26 | pIC50 | 550 | nM | IC50 | J Med Chem (1992) 35: 4503-4505 [PMID:1447752] |
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] | ||||||||
ChEMBL | Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptor | B | 6.46 | pKi | 350 | nM | Ki | J Med Chem (1988) 31: 867-870 [PMID:2965244] |
ChEMBL | Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand. | B | 7.05 | pKi | 90 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
ChEMBL | Binding affinity towards 5-hydroxytryptamine 1D receptor was determined in calf striatum homogenate | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (1996) 39: 314-322 [PMID:8568822] |
ChEMBL | Compound was evaluated for binding affinity towards 5-hydroxytryptamine 1D receptor in bovine caudate using [3H]- serotonin as radioligand | B | 7.31 | pIC50 | 49 | nM | IC50 | J Med Chem (1992) 35: 3625-3632 [PMID:1433172] |
Serotonin 1d (5-HT1d) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304407] [UniProtKB: Q60484] | ||||||||
ChEMBL | Binding affinity against 5-hydroxytryptamine 1D receptor | B | 7.31 | pIC50 | 49 | nM | IC50 | J Med Chem (1992) 35: 4503-4505 [PMID:1447752] |
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 | 6.21 | pKi | 620 | nM | Ki | J Med Chem (1994) 37: 1929-1935 [PMID:8027974] |
ChEMBL | Affinity against 5-hydroxytryptamine 2A receptor (D) labeled with [125I]DOI. | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (1994) 37: 1929-1935 [PMID:8027974] |
ChEMBL | Displacement of [125I]DOI from cloned human 5HT2A receptor expressed in CHO cells | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2006) 49: 318-328 [PMID:16392816] |
ChEMBL | Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay | F | 8.75 | pEC50 | 1.76 | nM | EC50 | ACS Med Chem Lett (2021) 12: 1874-1875 [PMID:34917241] |
ChEMBL | Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay | F | 8.75 | pEC50 | 1.76 | nM | EC50 | ACS Med Chem Lett (2022) 13: 537-539 [PMID:35450349] |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
ChEMBL | Compound was tested for binding affinity using [3H]MDL-100,907 at 5-hydroxytryptamine 2A receptor sites in rat cortical homogenate. | B | 5.8 | pKi | 1600 | nM | Ki | J Med Chem (1999) 42: 4257-4263 [PMID:10514296] |
ChEMBL | Displacement of [3H]DOB from rat 5HT2A receptor expressed in mouse NIH/3T3 cells after 30 mins by liquid scintillation counting analysis | B | 7.04 | pKi | 92 | nM | Ki | J Med Chem (2015) 58: 4998-5014 [PMID:26023814] |
ChEMBL | Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex | B | 8.02 | pIC50 | 9.53 | nM | IC50 | J Med Chem (2006) 49: 318-328 [PMID:16392816] |
ChEMBL | Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells | F | 6.34 | pEC50 | 462 | nM | EC50 | J Med Chem (2006) 49: 318-328 [PMID:16392816] |
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
ChEMBL | Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells | B | 7.28 | pKi | 52 | nM | Ki | J Med Chem (2006) 49: 318-328 [PMID:16392816] |
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994] | ||||||||
ChEMBL | The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus | B | 7.08 | pKd | 83.18 | nM | Kd | J Med Chem (1982) 25: 68-70 [PMID:7086824] |
ChEMBL | Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats | F | 6.62 | pEC50 | 240 | nM | EC50 | J Med Chem (2006) 49: 318-328 [PMID:16392816] |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
GtoPdb | - | - | 7 | pKi | - | - | - | J Neurochem (1999) 72: 2127-34 [PMID:10217294] |
ChEMBL | Displacement of [125I]DOI from cloned human 5HT2C receptor expressed in CHO cells | B | 7.38 | pKi | 42 | nM | Ki | J Med Chem (2006) 49: 318-328 [PMID:16392816] |
ChEMBL | Binding affinity towards 5-hydroxytryptamine 1C receptor using [3H]mesulergine as radioligand | B | 6.6 | pIC50 | 250 | nM | IC50 | J Med Chem (1992) 35: 3625-3632 [PMID:1433172] |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
ChEMBL | Affinity against 5-hydroxytryptamine 2C receptor in J1 cells transfected with the rat 5-HT2C gene labeled with [3H]mesulergine. | B | 6.02 | pKi | 960 | nM | Ki | J Med Chem (1994) 37: 1929-1935 [PMID:8027974] |
ChEMBL | Binding affinity against 5-hydroxytryptamine 1C receptor | B | 6.6 | pIC50 | 250 | nM | IC50 | J Med Chem (1992) 35: 4503-4505 [PMID:1447752] |
ChEMBL | Activity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cells | F | 7.11 | pEC50 | 77.8 | nM | EC50 | J Med Chem (2006) 49: 318-328 [PMID:16392816] |
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 | 7.11 | pKi | 78 | nM | Ki | J Med Chem (2000) 43: 1011-1018 [PMID:10715164] |
ChEMBL | Binding affinity to Homo sapiens (human) 5-HT6 receptor | B | 7.15 | pKi | 70 | nM | Ki | Med Chem Res (2005) 14: 1-18 |
ChEMBL | Binding affinity towards human 5-hydroxytryptamine 6 receptor | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
ChEMBL | Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 2295-2299 [PMID:11055342] |
ChEMBL | Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells | B | 7.89 | pKi | 13 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 5832-5835 [PMID:16945532] |
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388] | ||||||||
GtoPdb | - | - | 6.9 | pKi | - | - | - | 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 | Binding affinity of compound towards rodent 5-hydroxytryptamine 7 receptor | B | 7.52 | pKi | 30 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
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 | 7.4 | pKi | 39.81 | nM | Ki | J Med Chem (2003) 46: 5365-5374 [PMID:14640545] |
GtoPdb | - | - | 7.7 | pKi | - | - | - | J Biol Chem (1993) 268: 18200-4 [PMID:8394362] |
5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
GtoPdb | - | - | 6.3 | pKi | - | - | - |
Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]; Bioorg Med Chem (2004) 12: 2545-52 [PMID:15110837] |
5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939] | ||||||||
GtoPdb | - | - | 7.4 | pKi | - | - | - | Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639] |
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]