Target Information

Target General Information

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Target ID

T16691 (Former ID: TTDC00185)

Target Name

5-HT 6 receptor (HTR6)

Synonyms

Serotonin receptor 6; 5-hydroxytryptamine receptor 6; 5-HT6 receptor; 5-HT6; 5-HT-6

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Gene Name

HTR6

Target Type

Clinical trial target

[1]

Disease

[+] 2 Target-related Diseases

Alzheimer disease [ICD-11: 8A20]

Schizophrenia [ICD-11: 6A20]

Function

The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase. It has a high affinity for tricyclic psychotropic drugs. Controls pyramidal neurons migration during corticogenesis, through the regulation of CDK5 activity. Is an activator of TOR signaling. This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen.

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BioChemical Class

GPCR rhodopsin

UniProt ID

5HT6R_HUMAN

Sequence

MVPEPGPTANSTPAWGAGPPSAPGGSGWVAAALCVVIALTAAANSLLIALICTQPALRNT
SNFFLVSLFTSDLMVGLVVMPPAMLNALYGRWVLARGLCLLWTAFDVMCCSASILNLCLI
SLDRYLLILSPLRYKLRMTPLRALALVLGAWSLAALASFLPLLLGWHELGHARPPVPGQC
RLLASLPFVLVASGLTFFLPSGAICFTYCRILLAARKQAVQVASLTTGMASQASETLQVP
RTPRPGVESADSRRLATKHSRKALKASLTLGILLGMFFVTWLPFFVANIVQAVCDCISPG
LFDVLTWLGYCNSTMNPIIYPLFMRDFKRALGRFLPCPRCPRERQASLASPSLRTSHSGP
RPGLSLQQVLPLPLPPDSDSDSDAGSGGSSGLRLTAQLLLPGEATQDPPLPTRAAAAVNF
FNIDPAEPELRPHPLGIPTN

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3D Structure

Click to Show 3D Structure of This Target

AlphaFold

Drugs and Modes of Action

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Clinical Trial Drug(s)

[+] 15 Clinical Trial Drugs

LU AE58054

Drug Info

Phase 3

Schizophrenia

[2], [3]

SB-742457

Drug Info

Phase 3

Alzheimer disease

[4]

AVN 211

Drug Info

Phase 2/3

Schizophrenia

[5]

AVN 101

Drug Info

Phase 2

Anxiety disorder

[6]

AVN 322

Drug Info

Phase 2

Cognitive impairment

[7]

PF-05212377

Drug Info

Phase 2

Alzheimer disease

[8]

SAM-531

Drug Info

Phase 2

Alzheimer disease

[9], [10]

SUVN-502

Drug Info

Phase 2

Neurological disorder

[11]

SYN-120

Drug Info

Phase 2

Alzheimer disease

[12]

SYN120

Drug Info

Phase 2

Parkinson disease

[13]

11C-GSK-215083

Drug Info

Phase 1

Neurodegenerative disorder

[14], [15]

ABT-354

Drug Info

Phase 1

Alzheimer disease

[16]

AVN-322

Drug Info

Phase 1

Alzheimer disease

[17]

BVT-74316

Drug Info

Phase 1

Obesity

[18]

PRX-07034

Drug Info

Phase 1

Obesity

[19]

Patented Agent(s)

[+] 2 Patented Agents

PMID30124346-Compound-13TABLE4

Drug Info

Patented

Attention deficit hyperactivity disorder

[20]

PMID30124346-Compound-34TABLE4

Drug Info

Patented

Attention deficit hyperactivity disorder

[20]

Discontinued Drug(s)

[+] 3 Discontinued Drugs

AVN 397

Drug Info

Discontinued in Phase 2

Anxiety disorder

[21]

SYN-114

Drug Info

Discontinued in Phase 1

Cognitive impairment

[22]

WAY-181187

Drug Info

Discontinued in Phase 1

Anxiety disorder

[23], [24]

Mode of Action

[+] 6 Modes of Action

Enhancer

[+] 1 Enhancer drugs

LU AE58054

Drug Info

[25]

Antagonist

[+] 24 Antagonist drugs

SB-742457

Drug Info

[26], [27]

PF-05212377

Drug Info

[29]

SAM-531

Drug Info

[30]

SUVN-502

Drug Info

[31]

SYN-120

Drug Info

[32]

SYN120

Drug Info

[33]

11C-GSK-215083

Drug Info

[34]

AVN-322

Drug Info

[36]

BVT-74316

Drug Info

[37]

PRX-07034

Drug Info

[38]

AVN 397

Drug Info

[28]

SYN-114

Drug Info

[39]

2-bromo-LSD

Drug Info

[48]

alpha-ergocryptine

Drug Info

[68]

bufotenine

Drug Info

[57]

fluperlapine

Drug Info

[75]

MPDT

Drug Info

[74]

SB 258585

Drug Info

[77]

SB399885

Drug Info

[80]

SUVN-501

Drug Info

[69]

SUVN-504

Drug Info

[69]

SUVN-507

Drug Info

[69]

[125I]SB-258585

Drug Info

[77]

[3H]Ro 63-0563

Drug Info

[1], [79]

Modulator

[+] 8 Modulator drugs

AVN 211

Drug Info

[28]

AVN 101

Drug Info

[28]

AVN 322

Drug Info

[26]

ABT-354

Drug Info

[35]

WAY-181187

Drug Info

[40]

AMR-SIX-1

Drug Info

[69]

SB-214111

Drug Info

[78]

SEL-73

Drug Info

[69]

Ligand

[+] 2 Ligand drugs

PMID30124346-Compound-13TABLE4

Drug Info

[20]

PMID30124346-Compound-34TABLE4

Drug Info

[20]

Inhibitor

[+] 75 Inhibitor drugs

(+/-)-nantenine

Drug Info

[41]

1-(2-Methoxy-phenyl)-piperazine

Drug Info

[42]

1-(3-(benzyloxy)-2-methylphenyl)piperazine

Drug Info

[43]

1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine

Drug Info

[44]

1-(phenylsulfonyl)-4-(piperazin-1-yl)-1H-indole

Drug Info

[45]

1-Benzenesulfonyl-3-piperidin-3-yl-1H-indole

Drug Info

[46]

1-Benzenesulfonyl-3-piperidin-4-yl-1H-indole

Drug Info

[47]

1-phenylthio-N,N-dimethyltryptamine

Drug Info

[49]

2-(1-(phenylsulfonyl)-1H-indol-3-yl)ethanamine

Drug Info

[50]

2-(1-benzyl-1H-inden-3-yl)-N,N-dimethylethanamine

Drug Info

[51]

2-(1-benzyl-1H-indol-3-yl)-N,N-dimethylethanamine

Drug Info

[51]

2-(1-tosyl-1H-indol-3-yl)ethanamine

Drug Info

[50]

2-(1H-indol-3-yl)-N,N-dimethylethanamine

Drug Info

[52]

2-(3-(phenylsulfonyl)-1H-indol-1-yl)ethanamine

Drug Info

[53]

2-(3-benzenesulfonyl)phenyl-1-aminoethane

Drug Info

[54]

2-(3-phenylthio)phenyl)-1-aminoethane

Drug Info

[54]

2-(4-(benzenesulfonyl)phenyl)-1-aminoethane

Drug Info

[54]

2-Benzyl-4-piperazin-1-yl-1H-benzimidazole

Drug Info

[55]

2-Ethyl-5-methoxy-3-piperidin-4-yl-1H-indole

Drug Info

[56]

3-(phenylsulfonyl)-1-(piperidin-3-yl)-1H-indole

Drug Info

[58]

3-(phenylsulfonyl)-1-(piperidin-4-yl)-1H-indole

Drug Info

[58]

3-(phenylsulfonyl)-1-(pyrrolidin-3-yl)-1H-indole

Drug Info

[58]

4-((1H-indol-1-yl)methyl)benzenamine

Drug Info

[59]

4-(1H-Inden-1-ylmethyl)-phenylamine

Drug Info

[60]

4-(1H-indol-1-ylsulfonyl)benzenamine

Drug Info

[45]

4-(1H-Indol-3-ylmethyl)-phenylamine

Drug Info

[60]

4-(2-benzenesulfonylphenyl)piperazine

Drug Info

[54]

4-(3-benzenesulfonamidophenyl)piperazine

Drug Info

[54]

4-(3-benzenesulfonylphenyl)piperazine

Drug Info

[54]

4-(3-Methyl-indole-1-sulfonyl)-phenylamine

Drug Info

[42]

4-(3H-Inden-1-ylmethyl)-phenylamine

Drug Info

[60]

4-(4,6-dinitro-1H-indol-1-ylsulfonyl)benzenamine

Drug Info

[45]

4-(4-benzenesulfonamidophenyl)piperazine

Drug Info

[54]

4-(4-benzenesulfonylphenyl)piperazine

Drug Info

[54]

4-(4-methoxy-1H-indol-1-ylsulfonyl)benzenamine

Drug Info

[61]

4-(6-methoxy-1H-indol-1-ylsulfonyl)benzenamine

Drug Info

[61]

4-(Indan-1-ylsulfanyl)-phenylamine

Drug Info

[60]

4-(Indane-1-sulfonyl)-phenylamine

Drug Info

[60]

4-(Naphthalene-1-sulfonyl)-phenylamine

Drug Info

[42]

4-(piperazin-1-yl)-1H-indole

Drug Info

[45]

4-(piperazin-1-yl)-3-tosyl-1H-indazole

Drug Info

[62]

4-Indan-1-ylmethyl-phenylamine

Drug Info

[60]

4-Inden-(1E)-ylidenemethyl-phenylamine

Drug Info

[60]

5,6-dichloro-3,4-dihydroquinazolin-2-amine

Drug Info

[63]

5-(4-Methylpiperazin-1-yl)-3-tosyl-1H-indazole

Drug Info

[62]

5-MEO-DMT

Drug Info

[65]

5-METHOXYTRYPTAMINE

Drug Info

[66]

6-(piperazin-1-yl)-3-tosyl-1H-indazole

Drug Info

[62]

6-tosyl-1,2,3,4,5,6-hexahydroazepino[4,5-b]indole

Drug Info

[67]

CHLOROPHENYLPIPERAZINE

Drug Info

[71]

DIMEBOLIN

Drug Info

[72]

E-6837

Drug Info

[51]

EDMT

Drug Info

[51], [74]

METHIOTHEPIN

Drug Info

[76]

N,N-diethyl-2-(1H-indol-3-yl)ethanamine

Drug Info

[65]

N,N-dimethyl-2-(1-tosyl-1H-indol-3-yl)ethanamine

Drug Info

[59]

N-(3-(2-aminoethyl)phenyl)benzenesulfonamide

Drug Info

[54]

N-(3-(3-aminopropyl)phenyl)benzenesulfonamide

Drug Info

[54]

N-(3-(aminomethyl)phenyl)benzenesulfonamide

Drug Info

[54]

N-(3-aminophenyl)benzenesulfonamide

Drug Info

[54]

N-(4-(2-aminoethyl)phenyl)benzenesulfonamide

Drug Info

[54]

N-phenyl-3-(2-aminoethyl)benzenesulfonamide

Drug Info

[54]

OCTOCLOTHEPIN

Drug Info

[66]

QUIPAZINE

Drug Info

[71]

Ro-04-6790

Drug Info

[51]

SB-271046

Drug Info

[43]

SB-357134

Drug Info

[79]

SEROTONIN

Drug Info

[76]

WAY-208466

Drug Info

[53]

WAY-466

Drug Info

[81]

[2-(3-Benzyl-3H-inden-1-yl)-ethyl]-methyl-amine

Drug Info

[60]

[2-(3-Benzyl-3H-indol-1-yl)-ethyl]-dimethyl-amine

Drug Info

[82]

[2-(3-Benzyl-indol-1-yl)-ethyl]-dimethyl-amine

Drug Info

[60]

[2-(3H-Indol-1-yl)-ethyl]-dimethyl-amine

Drug Info

[82]

[3H]spiperone

Drug Info

[71]

Agonist

[+] 15 Agonist drugs

1-naphthylpiperazine

Drug Info

[42], [48]

2-methyl-5-HT

Drug Info

[57]

5-CT

Drug Info

[64]

alpha-methyl-5-HT

Drug Info

[68]

BRL-15572

Drug Info

[70]

DM-1451

Drug Info

[73]

E6801

Drug Info

[66]

EMD-386088

Drug Info

[56]

lergotrile

Drug Info

[48]

LY 165,163

Drug Info

[48]

m-chlorophenylpiperazine

Drug Info

[48]

OPC 4392

Drug Info

[73]

TFMPP

Drug Info

[48]

[3H]5-CT

Drug Info

[69]

[3H]LSD

Drug Info

[73]

Cell-based Target Expression Variations

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Cell-based Target Expression Variations

Cell-based Target Expression Variations Info

Different Human System Profiles of Target	Top
Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target. A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020). Human Pathway Affiliation of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function. Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes (Pharmacol Rev, 58: 259-279, 2006). Human Similarity Proteins Human Pathway Affiliation

Different Human System Profiles of Target

Top

Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.

A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020).

Human Pathway Affiliation of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.

Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes (Pharmacol Rev, 58: 259-279, 2006).

Human Similarity Proteins

Human Pathway Affiliation

Protein Name	Pfam ID	Percentage of Identity (%)	E value
Olfactory receptor 7A5 (OR7A5)	PF13853	25.466 (41/161)	3.05E-08
Olfactory receptor 2AG2 (OR2AG2)	PF13853	24.225 (86/355)	6.00E-08
Olfactory receptor 6X1 (OR6X1)	PF13853	30.597 (41/134)	6.73E-08
Olfactory receptor 1L6 (OR1L6)	PF13853	25.943 (55/212)	8.10E-08
Olfactory receptor 6M1 (OR6M1)	PF13853	30.534 (40/131)	9.96E-08
Olfactory receptor 1L4 (OR1L4)	PF13853	27.778 (45/162)	1.01E-07
Olfactory receptor 1C1 (OR1C1)	PF13853	30.822 (45/146)	2.03E-07
Olfactory receptor 1A2 (OR1A2)	PF13853	30.088 (34/113)	3.66E-07
Olfactory receptor 2T6 (OR2T6)	PF13853	24.171 (51/211)	3.92E-07
Olfactory receptor 51I1 (OR51I1)	PF13853	29.323 (39/133)	5.26E-07
Olfactory receptor 2L13 (OR2L13)	PF13853	28.485 (47/165)	5.71E-07
Olfactory receptor 2D2 (OR2D2)	PF13853	31.944 (46/144)	9.10E-07
Olfactory receptor 4C6 (OR4C6)	PF13853	26.702 (51/191)	1.17E-06
Olfactory receptor 9A2 (OR9A2)	PF13853	22.759 (33/145)	1.57E-06
Olfactory receptor 7C1 (OR7C1)	PF13853	30.233 (39/129)	1.84E-06
Olfactory receptor 10A6 (OR10A6)	PF13853	22.535 (48/213)	1.98E-06
Olfactory receptor 2AT4 (OR2AT4)	PF13853	30.702 (35/114)	1.99E-06
Olfactory receptor 6S1 (OR6S1)	PF13853	24.503 (37/151)	2.39E-06
Olfactory receptor 51B2 (OR51B2)	PF13853	26.106 (59/226)	2.69E-06
Olfactory receptor 10C1 (OR10C1)	PF13853	28.788 (38/132)	2.96E-06
Olfactory receptor 10G4 (OR10G4)	PF13853	28.289 (43/152)	5.05E-06
Olfactory receptor 51S1 (OR51S1)	PF13853	32.203 (38/118)	6.65E-06
Olfactory receptor 2M5 (OR2M5)	PF13853	25.258 (49/194)	7.24E-06
Olfactory receptor 4K2 (OR4K2)	PF13853	26.891 (32/119)	7.36E-06
Olfactory receptor 1G1 (OR1G1)	PF13853	27.933 (50/179)	1.00E-05
Olfactory receptor 2AG1 (OR2AG1)	PF13853	22.849 (77/337)	1.16E-05
Olfactory receptor 4D6 (OR4D6)	PF13853	25.581 (33/129)	1.29E-05
Olfactory receptor 10G7 (OR10G7)	PF13853	28.105 (43/153)	1.89E-05
Olfactory receptor 14J1 (OR14J1)	PF13853	28.689 (35/122)	1.99E-05
Olfactory receptor 2T35 (OR2T35)	PF13853	24.779 (56/226)	2.08E-05
Olfactory receptor 2T34 (OR2T34)	PF13853	24.169 (80/331)	2.21E-05
Olfactory receptor 2T4 (OR2T4)	PF13853	27.228 (55/202)	2.23E-05
Olfactory receptor 10G6 (OR10G6)	PF13853	28.099 (34/121)	2.35E-05
Olfactory receptor 4D1 (OR4D1)	PF13853	24.390 (80/328)	2.37E-05
Olfactory receptor 51I2 (OR51I2)	PF13853	26.490 (40/151)	2.41E-05
Olfactory receptor 10Q1 (OR10Q1)	PF13853	29.282 (53/181)	2.47E-05
Olfactory receptor 2A14 (OR2A14)	PF13853	25.146 (43/171)	2.76E-05
Olfactory receptor 13J1 (OR13J1)	PF13853	26.042 (50/192)	2.93E-05
Olfactory receptor 2AE1 (OR2AE1)	PF13853	27.972 (40/143)	3.07E-05
Olfactory receptor 1A1 (OR1A1)	PF13853	28.319 (32/113)	3.41E-05
Olfactory receptor 2T2 (OR2T2)	PF13853	23.451 (53/226)	4.16E-05
Olfactory receptor 2V1 (OR2V1)	PF13853	27.820 (37/133)	4.88E-05
Olfactory receptor 4A15 (OR4A15)	PF13853	24.645 (52/211)	5.43E-05
Olfactory receptor 2T10 (OR2T10)	PF13853	24.742 (48/194)	5.67E-05
Olfactory receptor 13H1 (OR13H1)	PF13853	28.421 (54/190)	5.70E-05
Olfactory receptor 8B4 (OR8B4)	PF13853	28.448 (33/116)	6.14E-05
Olfactory receptor 2D3 (OR2D3)	PF13853	28.682 (37/129)	6.71E-05
Olfactory receptor 10G9 (OR10G9)	PF13853	27.451 (42/153)	7.78E-05
Olfactory receptor 8A1 (OR8A1)	PF13853	25.833 (31/120)	7.79E-05
Olfactory receptor 52H1 (OR52H1)	PF13853	25.503 (38/149)	8.00E-05
Olfactory receptor 2T3 (OR2T3)	PF13853	24.398 (81/332)	1.08E-04
Olfactory receptor 2A1/2A42 (OR2A1; OR2A42)	PF13853	28.191 (53/188)	1.11E-04
Olfactory receptor 7D2 (OR7D2)	PF13853	23.469 (46/196)	1.19E-04
Olfactory receptor 52E4 (OR52E4)	PF13853	23.864 (42/176)	1.21E-04
Olfactory receptor 2M7 (OR2M7)	PF13853	24.742 (48/194)	1.34E-04
Olfactory receptor 4D5 (OR4D5)	PF13853	26.724 (31/116)	1.39E-04
Olfactory receptor 13A1 (OR13A1)	PF13853	28.319 (32/113)	1.43E-04
Olfactory receptor 7A17 (OR7A17)	PF13853	28.333 (34/120)	1.51E-04
Olfactory receptor 52B6 (OR52B6)	PF13853	26.974 (41/152)	1.60E-04
Olfactory receptor 51A7 (OR51A7)	PF13853	27.465 (39/142)	1.74E-04
Olfactory receptor 4F3/4F16/4F29 (OR4F3; OR4F16; OR4F29)	PF13853	26.829 (33/123)	1.78E-04
Olfactory receptor 2M4 (OR2M4)	PF13853	25.197 (32/127)	1.89E-04
Olfactory receptor 2L5 (OR2L5)	PF13853	27.273 (39/143)	2.21E-04
Olfactory receptor 8H1 (OR8H1)	PF13853	29.839 (37/124)	2.28E-04
Olfactory receptor 1M1 (OR1M1)	PF13853	22.467 (51/227)	2.34E-04
Olfactory receptor 1J1 (OR1J1)	PF13853	26.957 (31/115)	2.39E-04
Olfactory receptor 10G8 (OR10G8)	PF13853	26.974 (41/152)	2.77E-04
Olfactory receptor 2M2 (OR2M2)	PF13853	24.731 (46/186)	3.17E-04
Olfactory receptor 5M3 (OR5M3)	PF13853	25.207 (61/242)	3.21E-04
Olfactory receptor 10G3 (OR10G3)	PF13853	29.661 (35/118)	3.61E-04
Putative olfactory receptor 10J6 (OR10J6P)	PF13853	26.050 (31/119)	3.61E-04
Olfactory receptor 4F21 (OR4F21)	PF13853	26.016 (32/123)	3.63E-04
Olfactory receptor 7C2 (OR7C2)	PF13853	27.200 (34/125)	3.80E-04
Putative olfactory receptor 1F12P (OR1F12P)	PF13853	28.500 (57/200)	3.80E-04
Olfactory receptor 52E8 (OR52E8)	PF13853	23.810 (35/147)	3.88E-04
Putative olfactory receptor 7A2 (OR7A2P)	PF13853	25.263 (48/190)	4.39E-04
Olfactory receptor 8S1 (OR8S1)	PF13853	27.692 (36/130)	4.58E-04
Olfactory receptor 2T1 (OR2T1)	PF13853	24.257 (49/202)	5.32E-04
Olfactory receptor 2V2 (OR2V2)	PF13853	27.907 (36/129)	5.55E-04
Olfactory receptor 12D3 (OR12D3)	PF13853	21.805 (29/133)	7.19E-04
Olfactory receptor 11A1 (OR11A1)	PF13853	30.172 (35/116)	7.30E-04
Olfactory receptor 1E1 (OR1E1)	PF13853	25.152 (83/330)	8.03E-04
Olfactory receptor 10J1 (OR10J1)	PF13853	31.405 (38/121)	1.00E-03
Olfactory receptor 1D2 (OR1D2)	PF13853	25.532 (48/188)	1.00E-03
Olfactory receptor 10AG1 (OR10AG1)	PF13853	23.770 (29/122)	1.00E-03
Putative olfactory receptor 8G2 (OR8G2P)	PF13853	23.529 (36/153)	1.00E-03
Olfactory receptor 2T27 (OR2T27)	PF13853	23.415 (48/205)	1.00E-03
Olfactory receptor 2A2 (OR2A2)	PF13853	25.694 (37/144)	1.00E-03
Olfactory receptor 14I1 (OR14I1)	PF13853	30.556 (33/108)	2.00E-03
Olfactory receptor 4E2 (OR4E2)	PF13853	27.500 (33/120)	2.00E-03
Olfactory receptor 1P1 (OR1P1)	PF13853	27.731 (33/119)	2.00E-03
Olfactory receptor 6T1 (OR6T1)	PF13853	30.409 (52/171)	2.00E-03
Olfactory receptor 51F1 (OR51F1)	PF13853	26.119 (35/134)	2.00E-03
Olfactory receptor 10W1 (OR10W1)	PF13853	29.310 (34/116)	2.00E-03
Olfactory receptor 4D10 (OR4D10)	PF13853	22.400 (28/125)	2.00E-03
Olfactory receptor 52B2 (OR52B2)	PF13853	24.427 (32/131)	2.00E-03
Olfactory receptor 5M1 (OR5M1)	PF13853	27.815 (42/151)	2.00E-03
Olfactory receptor 4C16 (OR4C16)	PF13853	23.762 (48/202)	2.00E-03
Olfactory receptor 1K1 (OR1K1)	PF13853	30.579 (37/121)	2.00E-03
Olfactory receptor 12D1 (OR12D1)	PF13853	22.449 (33/147)	2.00E-03
Olfactory receptor 4K17 (OR4K17)	PF13853	24.823 (35/141)	3.00E-03
Olfactory receptor 4N5 (OR4N5)	PF13853	27.419 (34/124)	3.00E-03
Olfactory receptor 2AJ1 (OR2AJ1)	PF13853	25.197 (32/127)	3.00E-03
Olfactory receptor 51E1 (OR51E1)	PF13853	25.444 (43/169)	3.00E-03
Olfactory receptor 3A1 (OR3A1)	PF13853	29.299 (46/157)	3.00E-03
Olfactory receptor 4D9 (OR4D9)	PF13853	23.529 (32/136)	3.00E-03
Olfactory receptor 11L1 (OR11L1)	PF13853	22.674 (78/344)	3.00E-03
Olfactory receptor 10H1 (OR10H1)	PF13853	23.977 (41/171)	3.00E-03
Olfactory receptor 6V1 (OR6V1)	PF13853	24.113 (34/141)	4.00E-03
Olfactory receptor 52N2 (OR52N2)	PF13853	26.230 (32/122)	4.00E-03
Olfactory receptor 4C11 (OR4C11)	PF13853	26.389 (38/144)	4.00E-03
Olfactory receptor 1N2 (OR1N2)	PF13853	29.310 (34/116)	4.00E-03
Olfactory receptor 10P1 (OR10P1)	PF13853	30.000 (33/110)	4.00E-03
Olfactory receptor 1L1 (OR1L1)	PF13853	22.170 (47/212)	4.00E-03
Putative olfactory receptor 52L2 (OR52L2P)	PF13853	25.806 (32/124)	4.00E-03
Olfactory receptor 52Z1P (OR52Z1P)	PF13853	25.410 (31/122)	4.00E-03
Olfactory receptor 52N4 (OR52N4)	PF13853	26.230 (32/122)	5.00E-03
Olfactory receptor 7A10 (OR7A10)	PF13853	25.397 (32/126)	5.00E-03
Olfactory receptor 1L8 (OR1L8)	PF13853	24.615 (32/130)	5.00E-03
Olfactory receptor 10H2 (OR10H2)	PF13853	24.648 (35/142)	5.00E-03
Click to Show/Hide the Information of Human Similarity Proteins

KEGG Pathway	Pathway ID	Affiliated Target
Calcium signaling pathway	hsa04020	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
cAMP signaling pathway	hsa04024	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
Neuroactive ligand-receptor interaction	hsa04080	Affiliated Target
Class: Environmental Information Processing => Signaling molecules and interaction	Pathway Hierarchy
Serotonergic synapse	hsa04726	Affiliated Target
Class: Organismal Systems => Nervous system	Pathway Hierarchy

Chemical Structure based Activity Landscape of Target

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Drug Property Profile of Target

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(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

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Co-Targets

Co-Targets Info

Target Poor or Non Binders

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Target Poor or Non Binders

Target Poor or Non Binders Info

Target Regulators

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Target-interacting Proteins

Target-interacting Proteins Info

Target Profiles in Patients

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Target Expression
Profile (TEP)

Target Expression Profile Info

Target Affiliated Biological Pathways

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KEGG Pathway

[+] 4 KEGG Pathways

Calcium signaling pathway

cAMP signaling pathway

Neuroactive ligand-receptor interaction

Serotonergic synapse

Panther Pathway

[+] 1 Panther Pathways

Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway

Pathwhiz Pathway

[+] 1 Pathwhiz Pathways

Excitatory Neural Signalling Through 5-HTR 6 and Serotonin

Reactome

[+] 2 Reactome Pathways

Serotonin receptors

G alpha (s) signalling events

WikiPathways

[+] 5 WikiPathways

Serotonin Receptor 4/6/7 and NR3C Signaling

Monoamine GPCRs

GPCRs, Class A Rhodopsin-like

GPCR ligand binding

GPCR downstream signaling

Target-Related Models and Studies

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Target Validation

Target Validation Info

Target QSAR Model

References

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Conformationally constrained N1-arylsulfonyltryptamine derivatives as 5-HT6 receptor antagonists. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4780-5.

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N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists. Bioorg Med Chem Lett. 2005 Jan 17;15(2):379-83.

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Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol Pharmacol. 1993 Mar;43(3):320-7.

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