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)
Acetylcholinesterase in Electrophorus electricus [ChEMBL: CHEMBL4078] [UniProtKB: O42275] There should be some charts here, you may need to enable JavaScript!
MT1 receptor/Melatonin receptor 1A in Human [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039] There should be some charts here, you may need to enable JavaScript!
MT2 receptor/Melatonin receptor 1B in Human [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566] There should be some charts here, you may need to enable JavaScript!
5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939] 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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]