5-MeO-DMT [Ligand Id: 145] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL7257 ([2-(5-Methoxy-1H-Indol-3-Yl)-Ethyl]-Dimethyl-Amine, 5-OME-DMT)
  • Acetylcholinesterase in Electrophorus electricus [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
  • This target only has 0 pki data point
  • 0
1 CHEMBL7257_lig_chart_1 Acetylcholinesterase Electrophorus electricus
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  • MT1 receptor/Melatonin receptor 1A in Human [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039]
  • This target only has 1 pki data point
  • 6.68
2 CHEMBL7257_lig_chart_2 Melatonin receptor 1A Human
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  • MT2 receptor/Melatonin receptor 1B in Human [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286]
  • This target only has 1 pki data point
  • 7.8
3 CHEMBL7257_lig_chart_3 Melatonin receptor 1B Human
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
  • 7.98
4 CHEMBL7257_lig_chart_4 Serotonin 1a (5-HT1a) receptor HumanRat
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
  • 6.75
5 CHEMBL7257_lig_chart_5 Serotonin 1b (5-HT1b) receptor HumanRat
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
  • Serotonin 1d (5-HT1d) receptor in Guinea pig [ChEMBL: CHEMBL2304407] [UniProtKB: Q60484]
  • This target only has 1 pki data point
  • 0
6 CHEMBL7257_lig_chart_6 Serotonin 1d (5-HT1d) receptor HumanGuinea pig
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
  • 6.42
7 CHEMBL7257_lig_chart_7 Serotonin 2a (5-HT2a) receptor HumanRat
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994]
  • This target only has 1 pki data point
  • 0
8 CHEMBL7257_lig_chart_8 Serotonin 2b (5-HT2b) receptor HumanRat
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
  • 6.02
9 CHEMBL7257_lig_chart_9 Serotonin 2c (5-HT2c) receptor HumanRat
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
  • 6.9
10 CHEMBL7257_lig_chart_10 Serotonin 6 (5-HT6) receptor HumanRat
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
  • 7.55
11 CHEMBL7257_lig_chart_11 Serotonin 7 (5-HT7) receptor HumanRat
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  • 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
  • This target only has 1 pki data point
  • 6.3
12 CHEMBL7257_lig_chart_12 5-ht1e receptor Human
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  • 5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
  • This target only has 1 pki data point
  • 7.4
13 CHEMBL7257_lig_chart_13 5-HT1F receptor Human
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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 B 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 B 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]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]