Target Information

Target General Information

Top

Target ID

T32060 (Former ID: TTDS00103)

Target Name

5-HT 2A receptor (HTR2A)

Synonyms

Serotonin receptor 2A; HTR2; 5-hydroxytryptamine receptor 2A; 5-HT-2A; 5-HT-2

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Gene Name

HTR2A

Target Type

Successful target

[1]

Disease

[+] 7 Target-related Diseases

Acute diabete complication [ICD-11: 5A2Y]

Anxiety disorder [ICD-11: 6B00-6B0Z]

Cerebral ischaemia [ICD-11: 8B1Z]

Mood disorder [ICD-11: 6A60-6E23]

Parkinsonism [ICD-11: 8A00]

Pituitary gland disorder [ICD-11: 5A60-5A61]

Schizophrenia [ICD-11: 6A20]

Function

G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling activates phospholipase C and a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and promotes the release of Ca(2+) ions from intracellular stores. Affects neural activity, perception, cognition and mood. Plays a role in the regulation of behavior, including responses to anxiogenic situations and psychoactive substances. Plays a role in intestinal smooth muscle contraction, and may play a role in arterial vasoconstriction.

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BioChemical Class

GPCR rhodopsin

UniProt ID

5HT2A_HUMAN

Sequence

MDILCEENTSLSSTTNSLMQLNDDTRLYSNDFNSGEANTSDAFNWTVDSENRTNLSCEGC
LSPSCLSLLHLQEKNWSALLTAVVIILTIAGNILVIMAVSLEKKLQNATNYFLMSLAIAD
MLLGFLVMPVSMLTILYGYRWPLPSKLCAVWIYLDVLFSTASIMHLCAISLDRYVAIQNP
IHHSRFNSRTKAFLKIIAVWTISVGISMPIPVFGLQDDSKVFKEGSCLLADDNFVLIGSF
VSFFIPLTIMVITYFLTIKSLQKEATLCVSDLGTRAKLASFSFLPQSSLSSEKLFQRSIH
REPGSYTGRRTMQSISNEQKACKVLGIVFFLFVVMWCPFFITNIMAVICKESCNEDVIGA
LLNVFVWIGYLSSAVNPLVYTLFNKTYRSAFSRYIQCQYKENKKPLQLILVNTIPALAYK
SSQLQMGQKKNSKQDAKTTDNDCSMVALGKQHSEEASKDNSDGVNEKVSCV

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3D Structure

Click to Show 3D Structure of This Target

AlphaFold

ADReCS ID

BADD_A00273 ; BADD_A02979 ; BADD_A04075

HIT2.0 ID

T64BED

Drugs and Modes of Action

Top

Approved Drug(s)

[+] 9 Approved Drugs

Aniracetam

Drug Info

Approved

Cerebrovascular ischaemia

[2], [3]

Flibanserin

Drug Info

Approved

Mood disorder

[4], [5]

Iloperidone

Drug Info

Approved

Schizophrenia

[6], [7]

lumateperone tosylate

Drug Info

Approved

Schizophrenia

[8]

Lurasidone hydrochloride

Drug Info

Approved

Schizophrenia

[9], [10], [11], [12]

Metergolin

Drug Info

Approved

Hyperprolactinaemia

[12]

Pimavanserin

Drug Info

Approved

Parkinson disease

[13]

Sarpogrelate

Drug Info

Approved

Diabetic complication

[14], [15]

ZOTEPINE

Drug Info

Approved

Anxiety disorder

[16], [12]

Clinical Trial Drug(s)

[+] 22 Clinical Trial Drugs

Blonanserin

Drug Info

Phase 3

Schizophrenia

[17], [18]

ITI-007

Drug Info

Phase 3

Insomnia

[19], [20]

M100907

Drug Info

Phase 3

Sleep-wake disorder

[21]

MIN-101

Drug Info

Phase 3

Schizophrenia

[22]

SR46349B

Drug Info

Phase 3

Schizophrenia

[18]

TNX-102

Drug Info

Phase 3

Fibromyalgia

[23]

Zicronapine

Drug Info

Phase 3

Schizophrenia

[24]

BVT.28949

Drug Info

Phase 2

Glaucoma/ocular hypertension

[25]

FKW00GA

Drug Info

Phase 2

Social phobia

[26]

NELOTANSERIN

Drug Info

Phase 2

Lewy body dementia

[27]

Nuplazid

Drug Info

Phase 2

Alzheimer disease

[28]

Ocaperidone

Drug Info

Phase 2

Schizoaffective disorder

[29], [18], [30]

PRUVANSERIN

Drug Info

Phase 2

Sleep-wake disorder

[31]

RP5063

Drug Info

Phase 2

Schizophrenia

[32]

SYN120

Drug Info

Phase 2

Parkinson disease

[33]

1192U90

Drug Info

Phase 1

Psychotic disorder

[34]

Abaperidone

Drug Info

Phase 1

Schizophrenia

[35]

ATI-9242

Drug Info

Phase 1

Schizophrenia

[26]

DSP-1200

Drug Info

Phase 1

Depression

[26]

SKL-10406

Drug Info

Phase 1

Major depressive disorder

[36]

Temanogrel

Drug Info

Phase 1

Cardiovascular disease

[37]

YKP-1358

Drug Info

Phase 1

Schizoaffective disorder

[18]

Patented Agent(s)

[+] 3 Patented Agents

PMID30124346-Compound-13TABLE4

Drug Info

Patented

Attention deficit hyperactivity disorder

[38]

PMID30124346-Compound-34TABLE4

Drug Info

Patented

Attention deficit hyperactivity disorder

[38]

PMID30124346-Compound-LDT8

Drug Info

Patented

Benign prostatic hyperplasia

[38]

Discontinued Drug(s)

[+] 21 Discontinued Drugs

LYSERGIC ACID DIETHYLAMIDE

Drug Info

Withdrawn from market

Addictive disorder

[39], [40]

Deramciclane

Drug Info

Discontinued in Phase 3

Anxiety disorder

[41], [42]

Iferanserin-Ventrus

Drug Info

Discontinued in Phase 3

Hemorrhoids

[43]

MDL-11939

Drug Info

Discontinued in Phase 3

Anxiety disorder

[44], [45]

Ritanserin

Drug Info

Discontinued in Phase 3

Anxiety disorder

[46], [47]

Adatanserin

Drug Info

Discontinued in Phase 2

Mood disorder

[48]

AMESERGIDE

Drug Info

Discontinued in Phase 2

Mood disorder

[49], [50]

FCE-22716

Drug Info

Discontinued in Phase 2

Hypertension

[51]

SERAZAPINE HYDROCHLORIDE

Drug Info

Discontinued in Phase 2

Anxiety disorder

[52]

SERGOLEXOLE MALEATE

Drug Info

Discontinued in Phase 2

Migraine

[53]

SL65.0472

Drug Info

Discontinued in Phase 2

Cardiovascular disease

[54]

YM-992

Drug Info

Discontinued in Phase 2

Depression

[55]

AM-831

Drug Info

Discontinued in Phase 1

Schizophrenia

[56]

DUP-734

Drug Info

Discontinued in Phase 1

Psychotic disorder

[57]

AMPEROZIDE

Drug Info

Terminated

Alcohol dependence

[58]

DV-7028

Drug Info

Terminated

Cardiovascular disease

[59]

Fananserin

Drug Info

Terminated

Schizophrenia

[60], [18]

GMC-283

Drug Info

Terminated

Schizophrenia

[18]

ICI-169369

Drug Info

Terminated

Anxiety disorder

[61], [62]

R-102444

Drug Info

Terminated

Pancreatitis

[63]

ZD-3638

Drug Info

Terminated

Schizophrenia

[18]

Preclinical Drug(s)

[+] 1 Preclinical Drugs

Org-23366

Drug Info

Preclinical

Schizophrenia

[18]

Mode of Action

[+] 7 Modes of Action

Inhibitor

[+] 191 Inhibitor drugs

Aniracetam

Drug Info

[64]

ZOTEPINE

Drug Info

[69]

TRYPTAMINE

Drug Info

[75]

LYSERGIC ACID DIETHYLAMIDE

Drug Info

[88]

MDL-11939

Drug Info

[93]

TIOSPIRONE

Drug Info

[97]

MAZAPERTINE

Drug Info

[100]

YM-992

Drug Info

[104]

A-80426

Drug Info

[107]

MDL-28161

Drug Info

[93]

Ro-60-0175

Drug Info

[120]

RP-68303

Drug Info

[121]

(+/-)-nantenine

Drug Info

[122]

(1-Phenethyl-piperidin-4-yl)-phenyl-methanone

Drug Info

[69]

(2-Indol-1-yl-ethyl)-dimethyl-amine

Drug Info

[123]

(2S)-1-(1H-furo[2,3-g]indazol-1-yl)propan-2-amine

Drug Info

[120]

(2S)-1-(5-fluoro-1H-indazol-1-yl)propan-2-amine

Drug Info

[120]

(2S)-1-(6-fluoro-1H-indazol-1-yl)propan-2-amine

Drug Info

[120]

(2S)-1-(6-methoxy-1H-indazol-1-yl)propan-2-amine

Drug Info

[124]

(E)-2-(4-fluorostyryl)-5-(phenylsulfinyl)pyridine

Drug Info

[125]

(E)-2-(4-fluorostyryl)-5-(phenylsulfonyl)pyridine

Drug Info

[125]

(R)-(+)-(4,5,6-trimethoxyindan-1-yl)methanamine

Drug Info

[88]

(R)-(-)-11-hydroxy-N-n-propylnoraporphine

Drug Info

[126]

(R)-1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine

Drug Info

[127]

(R)-3-(4-propylmorpholin-2-yl)phenol

Drug Info

[128]

(R,S)-1-(5-bromo-1H-indol-1-yl)propan-2-amine

Drug Info

[129]

(R,S)-1-(5-chloro-1H-indol-1-yl)propan-2-amine

Drug Info

[129]

(R,S)-1-(5-fluoro-1H-indol-1-yl)propan-2-amine

Drug Info

[129]

(R,S)-1-(5-methyl-1H-indol-1-yl)propan-2-amine

Drug Info

[129]

(R,S)-1-(6-fluoro-1H-indol-1-yl)propan-2-amine

Drug Info

[129]

(S)-(-)-(4,5,6-trimethoxyindan-1-yl)methanamine

Drug Info

[88]

(S)-1-(5,6-difluoro-1H-indol-1-yl)propan-2-amine

Drug Info

[129]

1,2,3,4-Tetrahydro-naphthalen-2-ylamine

Drug Info

[130]

1,2,3,4-Tetrahydro-pyrazino[1,2-a]indole

Drug Info

[123]

1,6-bis(4-(3-chlorophenyl)piperazin-1-yl)hexane

Drug Info

[131]

1,6-bis(4-(3-methoxyphenyl)piperazin-1-yl)hexane

Drug Info

[131]

1,6-bis(4-(pyridin-2-yl)piperazin-1-yl)hexane

Drug Info

[131]

1,6-bis(4-m-tolylpiperazin-1-yl)hexane

Drug Info

[131]

1,6-bis(4-phenylpiperazin-1-yl)hexane

Drug Info

[131]

1-((R)-2-aminopropyl)-1H-indazol-6-ol

Drug Info

[124]

1-((S)-2-aminopropyl)-1H-indazol-6-ol

Drug Info

[124]

1-((S)-2-aminopropyl)-7-chloro-1H-indazol-6-ol

Drug Info

[124]

1-((S)-2-aminopropyl)-7-fluoro-1H-indazol-6-ol

Drug Info

[124]

1-((S)-2-aminopropyl)-7-iodo-1H-indazol-6-ol

Drug Info

[124]

1-((S)-2-aminopropyl)-7-methyl-1H-indazol-6-ol

Drug Info

[124]

1-(10-Bromoanthracen-9-yl)-2-aminopropane

Drug Info

[132]

1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazine

Drug Info

[133]

1-(2,5-Dimethoxy-phenyl)-piperazine

Drug Info

[133]

1-(2,5-dimethoxyphenyl)propan-2-amine

Drug Info

[132]

1-(2,6-dimethoxy-4-methylphenyl)propan-2-amine

Drug Info

[132]

1-(2-aminoethyl)-1H-indazol-6-ol

Drug Info

[124]

1-(2-Methoxy-phenyl)-4-propyl-piperazine

Drug Info

[134]

1-(2-Methoxy-phenyl)-piperazine

Drug Info

[133]

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

Drug Info

[135]

1-(3-(phenylthio)propyl)-4-m-tolylpiperazine

Drug Info

[136]

1-(4-Bromo-2,5-difluorophenyl)-2-aminopropane

Drug Info

[132]

1-(4-Bromo-2,5-dimethoxy-phenyl)-piperazine

Drug Info

[133]

1-(4-ethyl-2,5-dimethoxyphenyl)propan-2-amine

Drug Info

[132]

1-Butyl-3-(2-dimethylamino-ethyl)-1H-indol-4-ol

Drug Info

[137]

1-Butyl-4-(2-methoxy-phenyl)-piperazine

Drug Info

[134]

1-Ethyl-4-(2-methoxy-phenyl)-piperazine

Drug Info

[134]

1-methoxy-9-aminomethyl-9,10-dihydroanthracene

Drug Info

[138]

1-Methyl-1,3-dihydro-indol-2-one

Drug Info

[139]

1-Naphthalen-2-yl-piperazine

Drug Info

[130]

1-naphthylpiperazine

Drug Info

[130]

1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine

Drug Info

[140]

11-Butyryloxy-N-n-propylnoraporphine

Drug Info

[126]

11-Heptanoyloxy-N-n-propylnoraporphine

Drug Info

[126]

11-Hexanoyloxy-N-n-propylnoraporphine

Drug Info

[126]

11-Propionyloxy-N-n-propylnoraporphine

Drug Info

[126]

11-valeryloxynoraporphine

Drug Info

[126]

2,2-Diphenyl-ethylamine

Drug Info

[141]

2,5-dimethoxy-4-bromophenethylamine

Drug Info

[142]

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

Drug Info

[143], [132]

2-(2-Amino-propyl)-5-bromo-4-methoxy-phenol

Drug Info

[144]

2-(2-Methoxy-phenyl)-1-methyl-ethylamine

Drug Info

[144]

2-(3,5-dimethoxy-4-phenethoxyphenyl)ethanamine

Drug Info

[132]

2-(3-Methoxy-phenyl)-1-methyl-ethylamine

Drug Info

[144]

2-(4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamine

Drug Info

[144]

2-(4-Bromo-phenyl)-1-methyl-ethylamine

Drug Info

[144]

2-(4-Methyl-piperazin-1-yl)-4-phenyl-pyrimidine

Drug Info

[145]

2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine

Drug Info

[124]

2-(9,10-dihydroanthracen-9-yl)-N-methylethanamine

Drug Info

[146]

2-(piperazin-1-yl)-5,6,7,8-tetrahydroquinoline

Drug Info

[147]

2-methoxy-9-aminomethyl-9,10-dihydroanthracene

Drug Info

[138]

2-Phenyl-3-(2-piperidin-1-yl-ethyl)-1H-indole

Drug Info

[148]

2-Phenyl-3-piperidin-4-yl-1H-indole

Drug Info

[148]

2-Piperazin-1-yl-phenol

Drug Info

[133]

3-(1-Benzyl-piperidin-4-yl)-2-phenyl-1H-indole

Drug Info

[148]

3-(1-Methyl-piperidin-4-yl)-2-phenyl-1H-indole

Drug Info

[148]

3-(1-Phenethyl-piperidin-4-yl)-2-phenyl-1H-indole

Drug Info

[148]

3-(2-Amino-propyl)-1H-indol-5-ol

Drug Info

[124]

3-(2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-ol

Drug Info

[137]

3-(2-Dimethylamino-ethyl)-1H-indol-6-ol

Drug Info

[137]

3-(2-Dimethylamino-ethyl)-2-methyl-1H-indol-4-ol

Drug Info

[137]

3-(2-Dimethylamino-propyl)-1H-indol-4-ol

Drug Info

[137]

3-(2-Pyrrolidin-1-yl-ethyl)-1H-indol-4-ol

Drug Info

[137]

3-(3-Dimethylamino-propyl)-1H-indol-4-ol

Drug Info

[137]

3-Amino-1-(2-amino-5-methoxy-phenyl)-propan-1-one

Drug Info

[133]

100

3-Dimethylaminomethyl-1-methyl-1H-indol-4-ol

Drug Info

[137]

101

3-Dimethylaminomethyl-1H-indol-4-ol

Drug Info

[137]

102

3-methoxy-9-aminomethyl-9,10-dihydroanthracene

Drug Info

[138]

103

3-Naphthalen-1-yl-1-propyl-pyrrolidine

Drug Info

[140]

104

3-Naphthalen-1-yl-pyrrolidine

Drug Info

[140]

105

4,4-Diphenylbutan-1-amine

Drug Info

[146]

106

4-(10H-Anthracen-9-ylidene)-1-methyl-piperidine

Drug Info

[141]

107

4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one

Drug Info

[149]

108

4-(4-Fluoro-benzyl)-piperidine hydrochloride

Drug Info

[93]

109

4-Benzyl-1-methyl-piperidine hydrochloride

Drug Info

[93]

110

4-methoxy-9-aminomethyl-9,10-dihydroanthracene

Drug Info

[138]

111

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

Drug Info

[150]

112

5-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline

Drug Info

[151]

113

5-chloro-3,4-dihydroquinazolin-2-amine

Drug Info

[150]

114

5-chloro-N-(pyridin-3-yl)indoline-1-carboxamide

Drug Info

[129]

115

5-MEO-DMT

Drug Info

[124]

116

5-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline

Drug Info

[151]

117

5-Methoxy-4,9-dihydro-3H-beta-carboline

Drug Info

[151]

118

5-METHOXYTRYPTAMINE

Drug Info

[75]

119

6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine

Drug Info

[152]

120

6-bromoaplysinopsin

Drug Info

[153]

121

6-Chloro-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole

Drug Info

[123]

122

6-chloro-N-(pyridin-3-yl)indoline-1-carboxamide

Drug Info

[129]

123

6-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline

Drug Info

[151]

124

7,8,9,10-tetrahydro-6H-furo-[2,3-g][3]benzazepine

Drug Info

[152]

125

7,8,9,10-tetrahydro-6H-furo-[3,2-g][3]benzazepine

Drug Info

[152]

126

7-Chloro-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole

Drug Info

[123]

127

7-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline

Drug Info

[151]

128

8-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline

Drug Info

[151]

129

8-Bromo-4,9-dihydro-3H-beta-carboline

Drug Info

[151]

130

8-Chloro-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole

Drug Info

[123]

131

8-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline

Drug Info

[151]

132

8-Methoxy-2-(4-methyl-piperazin-1-yl)-quinoline

Drug Info

[130]

133

8-Methoxy-2-piperazin-1-yl-quinoline

Drug Info

[130]

134

8-Methoxy-4,9-dihydro-3H-beta-carboline

Drug Info

[151]

135

9-(2-aminoethyl)-9,10-dihydroanthracene

Drug Info

[146]

136

9-(2-aminopropyl)-9,10-dihydroanthracene

Drug Info

[146]

137

9-(Aminomethyl)-9,10-dihydroanthracene

Drug Info

[141]

138

9-(N-benzylaminomethyl)-9,10-dihydroanthracene

Drug Info

[154]

139

A-987306

Drug Info

[156]

140

ALTANSERIN

Drug Info

[72]

141

Aplysinopsin

Drug Info

[129]

142

BARETTIN

Drug Info

[159]

143

Brolamfetamine

Drug Info

[161]

144

C-(5-bromo-4,7-dimethoxyindan-1-yl)methylamine

Drug Info

[142]

145

C-(5H-Dibenzo[a,d]cyclohepten-5-yl)-methylamine

Drug Info

[141]

146

C-(9H-Thioxanthen-9-yl)-methylamine

Drug Info

[141]

147

C-(9H-Xanthen-9-yl)-methylamine

Drug Info

[141]

148

CHLOROPHENYLPIPERAZINE

Drug Info

[163]

149

CINANSERIN

Drug Info

[75]

150

DOM

Drug Info

[132]

151

Etisulergine

Drug Info

[167]

152

FLUANISONE

Drug Info

[168]

153

ISOCLOZAPINE

Drug Info

[169]

154

LY433222

Drug Info

[104]

155

MESCALINE

Drug Info

[132]

156

N,N-dimethyl-2,2-diphenylethanamine

Drug Info

[146]

157

N,N-Dimethyl-3,3-diphenylpropan-1-amine

Drug Info

[146]

158

N,N-dimethyl-4,4-diphenylbutan-1-amine

Drug Info

[146]

159

N-(1-(1-phenylethyl)piperidin-4-yl)-1-naphthamide

Drug Info

[177]

160

N-(1-(1-phenylethyl)piperidin-4-yl)-2-naphthamide

Drug Info

[177]

161

N-(1-(3-bromobenzyl)piperidin-4-yl)-1-naphthamide

Drug Info

[178]

162

N-(1-(3-bromobenzyl)piperidin-4-yl)-2-naphthamide

Drug Info

[178]

163

N-(1-(4-bromobenzyl)piperidin-4-yl)-2-naphthamide

Drug Info

[178]

164

N-(1-(4-nitrobenzyl)piperidin-4-yl)-2-naphthamide

Drug Info

[178]

165

N-(1-(4-phenylbutyl)piperidin-4-yl)-1-naphthamide

Drug Info

[177]

166

N-(1-(4-phenylbutyl)piperidin-4-yl)-2-naphthamide

Drug Info

[177]

167

N-(1-benzylpiperidine-4-yl)-2-naphthamide

Drug Info

[178]

168

N-(1-phenethylpiperidin-4-yl)-1-naphthamide

Drug Info

[177]

169

N-(1-phenethylpiperidin-4-yl)-2-naphthamide

Drug Info

[177]

170

N-3'-ethylaplysinopsin

Drug Info

[153]

171

N-methyl-3,3-diphenylpropan-1-amine

Drug Info

[146]

172

N-methyl-4,4-diphenylbutan-1-amine

Drug Info

[146]

173

PG-01037

Drug Info

[180]

174

PHENETHYLAMINE

Drug Info

[141]

175

PHENYLPIPERAZINE

Drug Info

[130]

176

PSILOCIN

Drug Info

[132]

177

QUIPAZINE

Drug Info

[181]

178

Racemic DOI

Drug Info

[132]

179

Racemic DOTFM

Drug Info

[132]

180

SB-271046

Drug Info

[185]

181

SEROTONIN

Drug Info

[181]

182

TRYPTOLINE

Drug Info

[151]

183

VER-2692

Drug Info

[186]

184

VER-3323

Drug Info

[187]

185

VER-5384

Drug Info

[187]

186

VER-5593

Drug Info

[187]

187

WAY-208466

Drug Info

[188]

188

YM-348

Drug Info

[152]

189

[2-(4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amine

Drug Info

[137]

190

[2-(6-Methoxy-indol-1-yl)-ethyl]-dimethyl-amine

Drug Info

[123]

191

[3H]spiperone

Drug Info

[192]

Modulator

[+] 21 Modulator drugs

Flibanserin

Drug Info

[5]

Lurasidone hydrochloride

Drug Info

[10], [11]

Pimavanserin

Drug Info

[13], [66]

SR46349B

Drug Info

[73]

Zicronapine

Drug Info

[76]

NELOTANSERIN

Drug Info

[78]

Ocaperidone

Drug Info

[30]

PRUVANSERIN

Drug Info

[80]

Abaperidone

Drug Info

[82]

ATI-9242

Drug Info

[83], [30]

YKP-1358

Drug Info

[86]

Deramciclane

Drug Info

[89], [90], [91]

Iferanserin-Ventrus

Drug Info

[92]

SL65.0472

Drug Info

[103]

DUP-734

Drug Info

[106]

AMPEROZIDE

Drug Info

[108]

ICI-169369

Drug Info

[113]

R-102444

Drug Info

[117], [118], [119]

EPLIVANSERIN MESILATE

Drug Info

[166]

SEL-73

Drug Info

[30]

Very low dose (VLD) cyclobenzaprine

Drug Info

[30]

Antagonist

[+] 70 Antagonist drugs

Iloperidone

Drug Info

[7], [18]

lumateperone tosylate

Drug Info

[8]

Metergolin

Drug Info

[65]

Sarpogrelate

Drug Info

[1], [67], [68]

Blonanserin

Drug Info

[18]

ITI-007

Drug Info

[70]

M100907

Drug Info

[71], [72]

MIN-101

Drug Info

[30]

TNX-102

Drug Info

[74]

BVT.28949

Drug Info

[77], [30]

FKW00GA

Drug Info

[26]

SYN120

Drug Info

[81]

1192U90

Drug Info

[18]

DSP-1200

Drug Info

[26]

3-phenyl pyrazole derivative 1

Drug Info

[87]

Benzoyl-piperidine derivative 1

Drug Info

[87]

Benzoyl-piperidine derivative 2

Drug Info

[87]

L-piperazino-3-phenyl-indane derivative 1

Drug Info

[87]

Piperazine derivative 3

Drug Info

[87]

Piperazine derivative 4

Drug Info

[87]

PMID26609882-Compound-34

Drug Info

[87]

PMID26609882-Compound-35

Drug Info

[87]

PMID26609882-Compound-36

Drug Info

[87]

PMID30124346-Compound-LDT8

Drug Info

[38]

Pyrazole derivative 67

Drug Info

[87]

Pyrazole derivative 68

Drug Info

[87]

Pyrazole derivative 69

Drug Info

[87]

Pyrazole derivative 70

Drug Info

[87]

Pyrazole derivative 71

Drug Info

[87]

Pyrazole derivative 72

Drug Info

[87]

Pyrazole derivative 73

Drug Info

[87]

Pyrazole derivative 74

Drug Info

[87]

Pyrazole derivative 75

Drug Info

[87]

Pyrimidine derivative 23

Drug Info

[87]

Pyrimidine derivative 24

Drug Info

[87]

Pyrimidine derivative 25

Drug Info

[87]

Pyrimidine derivative 26

Drug Info

[87]

Pyrimidine derivative 27

Drug Info

[87]

Pyrimidine derivative 28

Drug Info

[87]

Pyrimidine derivative 29

Drug Info

[87]

Ritanserin

Drug Info

[94], [95], [96]

Adatanserin

Drug Info

[48], [98]

AMESERGIDE

Drug Info

[99], [30]

FCE-22716

Drug Info

[51], [30]

SERAZAPINE HYDROCHLORIDE

Drug Info

[101], [30]

SERGOLEXOLE MALEATE

Drug Info

[102], [30]

Org-23366

Drug Info

[18]

Fananserin

Drug Info

[112], [18]

GMC-283

Drug Info

[18]

LY53857

Drug Info

[96], [114], [115], [116]

9-OH-risperidone

Drug Info

[155]

bufotenine

Drug Info

[162]

cyamemazine

Drug Info

[164]

EGIS-7625

Drug Info

[165]

LY063518

Drug Info

[171]

LY108742

Drug Info

[172]

LY215840

Drug Info

[172]

LY314228

Drug Info

[171]

LY320954

Drug Info

[171]

LY86057

Drug Info

[172]

MPDT

Drug Info

[176]

norfluoxetine

Drug Info

[179]

SB 215505

Drug Info

[182]

SB 221284

Drug Info

[65]

SB 228357

Drug Info

[183]

SB 242084

Drug Info

[184]

spiramide

Drug Info

[65]

[11C]volinanserin

Drug Info

[189]

[18F]altanserin

Drug Info

[191]

[3H]N-methylspiperone

Drug Info

[158]

Agonist

[+] 25 Agonist drugs

Nuplazid

Drug Info

[79]

Temanogrel

Drug Info

[85], [30]

Aryl piperazine derivative 9

Drug Info

[87]

Diarylamine and arylheteroarylamine pyrazole derivative 1

Drug Info

[87]

Diarylamine and arylheteroarylamine pyrazole derivative 2

Drug Info

[87]

Diarylamine and arylheteroarylamine pyrazole derivative 3

Drug Info

[87]

AM-831

Drug Info

[105]

DV-7028

Drug Info

[109], [110], [111]

5-CT

Drug Info

[65]

ACP-106

Drug Info

[30]

AL-37350A

Drug Info

[157]

alpha-methyl-5-HT

Drug Info

[158]

BRL-15572

Drug Info

[160]

BW723C86

Drug Info

[65]

LP-12

Drug Info

[170]

LP-44

Drug Info

[170]

m-chlorophenylpiperazine

Drug Info

[173]

METHYLENEDIOXYMETHAMPHETAMINE

Drug Info

[174]

MMDA

Drug Info

[175]

N-1-isopropyl-5-MeOT

Drug Info

[172]

N-1-isopropyltryptamine

Drug Info

[172]

Org 12962

Drug Info

[65]

SB 216641

Drug Info

[160]

TFMPP

Drug Info

[65], [133]

[125I]DOI

Drug Info

[190]

Partial agonist

[+] 1 Partial agonist drugs

RP5063

Drug Info

[26]

Binder

[+] 2 Binder drugs

SKL-10406

Drug Info

[84]

ZD-3638

Drug Info

[18]

Ligand

[+] 4 Ligand drugs

Aryl piperazine derivative 1

Drug Info

[38]

Aryl piperazine derivative 6

Drug Info

[38]

PMID30124346-Compound-13TABLE4

Drug Info

[38]

PMID30124346-Compound-34TABLE4

Drug Info

[38]

Cell-based Target Expression Variations

Top

Cell-based Target Expression Variations

Cell-based Target Expression Variations Info

Drug Binding Sites of Target

Top

Ligand Name: Lisuride

Ligand Info

Structure Description

Crystal structure of serotonin 2A receptor in complex with lisuride

PDB:7WC7

Method

X-ray diffraction

Resolution

2.60 Å

Mutation

Yes

[193]

PDB Sequence

LQEKNWSALL

⁸⁰

TAVVIILTIA

⁹⁰

GNILVIMAVS

¹⁰⁰

LEKKLQNATN

¹¹⁰

YFLMSLAIAD

¹²⁰

MLLGFLVMPV

¹³⁰

SMLTILYGYR

¹⁴⁰

WPLPSKLCAV

¹⁵⁰

WIYLDVLFST

¹⁶⁰

AKIWHLCAIS

¹⁷⁰

LDRYVAIQNP

¹⁸⁰

SRTKAFLKII

¹⁹⁷

AVWTISVGIS

²⁰⁷

MPIPVFGLQD

²¹⁷

DSKVFKEGSC

²²⁷

LLADDNFVLI

²³⁷

GSFVSFFIPL

²⁴⁷

TIMVITYFLT

²⁵⁷

IKSLQKEAAD

¹⁰⁰²

LEDNWETLND

¹⁰¹²

NLKVIEKADN

¹⁰²²

AAQVKDALTK

¹⁰³²

MRAAALDADI

¹⁰⁶⁷

LVGQIDDALK

¹⁰⁷⁷

LANEGKVKEA

¹⁰⁸⁷

QAAAEQLKTT

¹⁰⁹⁷

INAYIQKYGQ

³¹³

SISNEQKACK

³²³

VLGIVFFLFV

³³³

VMWCPFFITN

³⁴³

IMAVICKESC

³⁵³

NEDVIGALLN

³⁶³

VFVWIGYLNS

³⁷³

AVNPLVYTLF

³⁸³

NKTYRSAFSR

³⁹³

YIQCQYKE

Residue

Distance (Å)

VAL127

4.932

TRP151

3.653

ILE152

3.847

ASP155

2.651

VAL156

3.672

SER159

3.181

THR160

4.377

CYS227

3.864

LEU228

4.061

LEU229

3.662

PHE234

4.085

Residue

Distance (Å)

VAL235

3.987

GLY238

3.016

SER239

4.099

SER242

3.516

TRP336

3.407

PHE339

3.456

PHE340

3.807

ASN343

3.493

VAL366

3.752

TYR370

3.530

Ligand Name: Aripiprazole

Ligand Info

Structure Description

Crystal structure of 5-HT2AR in complex with aripiprazole

PDB:7VOE

Method

X-ray diffraction

Resolution

2.90 Å

Mutation

Yes

[194]

PDB Sequence

KNWSALLTAV

⁸³

VIILTIAGNI

⁹³

LVIMAVSLEK

¹⁰³

KLQNATNYFL

¹¹³

MSLAIADMLL

¹²³

GFLVMPVSML

¹³³

TILYGYRWPL

¹⁴³

PSKLCAVWIY

¹⁵³

LDVLFSTAKI

¹⁶³

WHLCAISLDR

¹⁷³

YVAIQNPSRT

¹⁹⁰

KAFLKIIAVW

²⁰⁰

TISVGISMPI

²¹⁰

PVFGLQDDSK

²²⁰

VFKEGSCLLA

²³⁰

DDNFVLIGSF

²⁴⁰

VSFFIPLTIM

²⁵⁰

VITYFLTIKS

²⁶⁰

LQKEAADLED

¹⁰⁰⁵

NWETLNDNLK

¹⁰¹⁵

VIEKADNAAQ

¹⁰²⁵

VKDALTKMRA

¹⁰³⁵

AALDAGDILV

¹⁰⁶⁹

GQIDDALKLA

¹⁰⁷⁹

NEGKVKEAQA

¹⁰⁸⁹

AAEQLKTTIN

¹⁰⁹⁹

AYIQKYGQSI

³¹⁵

SNEQKACKVL

³²⁵

GIVFFLFVVM

³³⁵

WCPFFITNIM

³⁴⁵

AVICKESCNE

³⁵⁵

DVIGALLNVF

³⁶⁵

VWIGYLNSAV

³⁷⁵

NPLVYTLFNK

³⁸⁵

TYRSAFSRYI

³⁹⁵

QCQYKE

Residue

Distance (Å)

TRP151

3.568

ILE152

4.226

ASP155

3.388

VAL156

3.688

SER159

3.854

ILE163

4.350

CYS227

3.564

LEU228

3.663

LEU229

4.086

PHE243

3.466

LEU247

3.793

Residue

Distance (Å)

PHE332

3.488

VAL333

3.741

TRP336

3.361

CYS337

3.701

PHE339

2.607

PHE340

3.506

LEU362

4.368

ASN363

3.457

VAL366

3.428

TYR370

4.095

Click to View More Binding Site Information of This Target with Different Ligands

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). Biological Network Descriptors of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database. The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information (Front Pharmacol, 9, 1245, 2018; Curr Opin Struct Biol. 44:134-142, 2017). Human Similarity Proteins Human Pathway Affiliation Biological Network Descriptors

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).

Biological Network Descriptors of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.

The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information (Front Pharmacol, 9, 1245, 2018; Curr Opin Struct Biol. 44:134-142, 2017).

Human Similarity Proteins

Human Pathway Affiliation

Biological Network Descriptors

Protein Name	Pfam ID	Percentage of Identity (%)	E value
Olfactory receptor 10J1 (OR10J1)	PF13853	27.273 (54/198)	2.56E-10
Olfactory receptor 10J3 (OR10J3)	PF13853	26.500 (53/200)	1.47E-09
Olfactory receptor 10A6 (OR10A6)	PF13853	23.715 (60/253)	2.18E-09
Olfactory receptor 4D10 (OR4D10)	PF13853	26.718 (35/131)	4.14E-09
Olfactory receptor 9A4 (OR9A4)	PF13853	26.271 (31/118)	1.54E-08
Olfactory receptor 4K2 (OR4K2)	PF13853	29.688 (38/128)	1.87E-08
Olfactory receptor 10A7 (OR10A7)	PF13853	27.869 (34/122)	2.78E-08
Olfactory receptor 51H1 (OR51H1)	PF13853	30.496 (43/141)	3.65E-08
Olfactory receptor 1M1 (OR1M1)	PF13853	25.203 (31/123)	4.13E-08
Olfactory receptor 14J1 (OR14J1)	PF13853	26.923 (35/130)	4.34E-08
Olfactory receptor 1D2 (OR1D2)	PF13853	25.822 (55/213)	6.05E-08
Olfactory receptor 1A2 (OR1A2)	PF13853	26.016 (32/123)	6.70E-08
Olfactory receptor 1B1 (OR1B1)	PF13853	23.881 (32/134)	8.09E-08
Olfactory receptor 4A15 (OR4A15)	PF13853	27.119 (32/118)	1.06E-07
Olfactory receptor 6M1 (OR6M1)	PF13853	27.193 (31/114)	1.16E-07
Olfactory receptor 2T34 (OR2T34)	PF13853	21.408 (73/341)	1.29E-07
Olfactory receptor 1P1 (OR1P1)	PF13853	25.547 (35/137)	1.83E-07
Olfactory receptor 10J5 (OR10J5)	PF13853	25.726 (62/241)	2.34E-07
Olfactory receptor 2B6 (OR2B6)	PF13853	23.077 (78/338)	2.45E-07
Olfactory receptor 51A7 (OR51A7)	PF13853	24.701 (62/251)	2.79E-07
Olfactory receptor 4D11 (OR4D11)	PF13853	26.866 (36/134)	2.95E-07
Olfactory receptor 2H2 (OR2H2)	PF13853	30.303 (30/99)	3.05E-07
Putative olfactory receptor 52L2 (OR52L2P)	PF13853	27.119 (32/118)	3.47E-07
Olfactory receptor 2B2 (OR2B2)	PF13853	22.154 (72/325)	3.69E-07
Olfactory receptor 5AS1 (OR5AS1)	PF13853	32.432 (36/111)	4.13E-07
Olfactory receptor 2T3 (OR2T3)	PF13853	20.772 (70/337)	4.99E-07
Olfactory receptor 4D9 (OR4D9)	PF13853	23.451 (53/226)	5.17E-07
Olfactory receptor 4E2 (OR4E2)	PF13853	28.571 (34/119)	5.48E-07
Olfactory receptor 1L3 (OR1L3)	PF13853	28.182 (31/110)	6.62E-07
Olfactory receptor 1L1 (OR1L1)	PF13853	29.000 (29/100)	6.68E-07
Olfactory receptor 1J1 (OR1J1)	PF13853	24.138 (28/116)	7.71E-07
Olfactory receptor 6C74 (OR6C74)	PF13853	25.714 (36/140)	7.94E-07
Olfactory receptor 6B1 (OR6B1)	PF13853	26.923 (35/130)	8.27E-07
Olfactory receptor 9A1 (OR9A1P)	PF13853	24.786 (29/117)	8.38E-07
Olfactory receptor 2D2 (OR2D2)	PF13853	23.118 (43/186)	9.00E-07
Putative olfactory receptor 2B3 (OR2B3)	PF13853	24.779 (56/226)	9.21E-07
Olfactory receptor 4K3 (OR4K3)	PF13853	25.373 (34/134)	9.29E-07
Olfactory receptor 10G9 (OR10G9)	PF13853	23.729 (28/118)	9.71E-07
Olfactory receptor 2W1 (OR2W1)	PF13853	25.397 (32/126)	9.83E-07
Olfactory receptor 2AT4 (OR2AT4)	PF13853	31.967 (39/122)	1.16E-06
Olfactory receptor 3A1 (OR3A1)	PF13853	28.696 (33/115)	1.30E-06
Olfactory receptor 6S1 (OR6S1)	PF13853	25.000 (33/132)	1.40E-06
Olfactory receptor 10G4 (OR10G4)	PF13853	23.729 (28/118)	1.59E-06
Olfactory receptor 10C1 (OR10C1)	PF13853	29.204 (33/113)	1.67E-06
Olfactory receptor 7E24 (OR7E24)	PF13853	29.915 (35/117)	2.03E-06
Olfactory receptor 51I1 (OR51I1)	PF13853	27.007 (37/137)	2.49E-06
Olfactory receptor 2B11 (OR2B11)	PF13853	24.201 (53/219)	2.88E-06
Olfactory receptor 10A2 (OR10A2)	PF13853	28.182 (31/110)	3.00E-06
Olfactory receptor 52L1 (OR52L1)	PF13853	27.434 (31/113)	3.18E-06
Olfactory receptor 6C2 (OR6C2)	PF13853	25.517 (37/145)	3.44E-06
Olfactory receptor 1C1 (OR1C1)	PF13853	26.496 (31/117)	3.66E-06
Olfactory receptor 7C1 (OR7C1)	PF13853	26.050 (31/119)	4.02E-06
Olfactory receptor 1A1 (OR1A1)	PF13853	21.739 (30/138)	4.32E-06
Olfactory receptor 8U3 (OR8U3)	PF13853	27.132 (35/129)	4.34E-06
Olfactory receptor 2J3 (OR2J3)	PF13853	19.814 (64/323)	4.44E-06
Olfactory receptor 7D4 (OR7D4)	PF13853	26.496 (31/117)	4.74E-06
Olfactory receptor 10A5 (OR10A5)	PF13853	28.182 (31/110)	5.19E-06
Olfactory receptor 1J2 (OR1J2)	PF13853	23.140 (28/121)	5.90E-06
Olfactory receptor 1I1 (OR1I1)	PF13853	31.579 (30/95)	6.40E-06
Olfactory receptor 4K17 (OR4K17)	PF13853	25.735 (35/136)	6.73E-06
Olfactory receptor 1E2 (OR1E2)	PF13853	27.434 (31/113)	6.93E-06
Olfactory receptor 2T7 (OR2T7)	PF13853	26.446 (32/121)	7.10E-06
Olfactory receptor 8J3 (OR8J3)	PF13853	30.631 (34/111)	7.17E-06
Olfactory receptor 10G7 (OR10G7)	PF13853	22.881 (27/118)	7.38E-06
Olfactory receptor 4K1 (OR4K1)	PF13853	27.419 (34/124)	7.58E-06
Olfactory receptor 4P4 (OR4P4)	PF13853	26.829 (33/123)	8.24E-06
Olfactory receptor 1E1 (OR1E1)	PF13853	24.242 (32/132)	8.68E-06
Olfactory receptor 5V1 (OR5V1)	PF13853	30.392 (31/102)	9.23E-06
Olfactory receptor 2A2 (OR2A2)	PF13853	24.402 (51/209)	9.29E-06
Olfactory receptor 10A4 (OR10A4)	PF13853	28.000 (28/100)	9.53E-06
Olfactory receptor 4S1 (OR4S1)	PF13853	28.696 (33/115)	1.07E-05
Olfactory receptor 2H1 (OR2H1)	PF13853	28.283 (28/99)	1.12E-05
Olfactory receptor 7D2 (OR7D2)	PF13853	24.390 (30/123)	1.26E-05
Olfactory receptor 1L8 (OR1L8)	PF13853	25.893 (29/112)	1.34E-05
Olfactory receptor 2T27 (OR2T27)	PF13853	26.446 (32/121)	1.41E-05
Olfactory receptor 6C1 (OR6C1)	PF13853	27.419 (34/124)	1.42E-05
Olfactory receptor 5B12 (OR5B12)	PF13853	28.713 (29/101)	1.49E-05
Olfactory receptor 7A5 (OR7A5)	PF13853	25.926 (35/135)	1.58E-05
Olfactory receptor 4D6 (OR4D6)	PF13853	23.188 (32/138)	1.75E-05
Olfactory receptor 2V1 (OR2V1)	PF13853	28.972 (31/107)	1.81E-05
Olfactory receptor 6X1 (OR6X1)	PF13853	31.633 (31/98)	1.84E-05
Olfactory receptor 4E1 (OR4E1)	PF13853	25.000 (29/116)	2.08E-05
Olfactory receptor 6C6 (OR6C6)	PF13853	25.000 (33/132)	2.17E-05
Olfactory receptor 10H3 (OR10H3)	PF13853	25.510 (25/98)	2.27E-05
Olfactory receptor 10G8 (OR10G8)	PF13853	22.881 (27/118)	2.35E-05
Olfactory receptor 4B1 (OR4B1)	PF13853	25.641 (30/117)	2.55E-05
Olfactory receptor 2J2 (OR2J2)	PF13853	24.898 (61/245)	2.55E-05
Olfactory receptor 5B3 (OR5B3)	PF13853	28.000 (28/100)	2.99E-05
Olfactory receptor 4A5 (OR4A5)	PF13853	23.894 (27/113)	3.11E-05
Olfactory receptor 1N2 (OR1N2)	PF13853	26.271 (31/118)	3.12E-05
Olfactory receptor 7C2 (OR7C2)	PF13853	26.891 (32/119)	3.29E-05
Olfactory receptor 6C68 (OR6C68)	PF13853	22.280 (43/193)	3.68E-05
Olfactory receptor 4D1 (OR4D1)	PF13853	21.014 (29/138)	3.68E-05
Olfactory receptor 5AK2 (OR5AK2)	PF13853	26.446 (32/121)	3.77E-05
Olfactory receptor 13A1 (OR13A1)	PF13853	24.370 (29/119)	3.94E-05
Putative olfactory receptor 1F12P (OR1F12P)	PF13853	24.390 (40/164)	3.97E-05
Olfactory receptor 6C76 (OR6C76)	PF13853	24.138 (35/145)	4.16E-05
Olfactory receptor 4Q2 (OR4Q2)	PF13853	25.893 (29/112)	4.19E-05
Olfactory receptor 4K15 (OR4K15)	PF13853	25.000 (28/112)	4.25E-05
Olfactory receptor 7A17 (OR7A17)	PF13853	26.271 (31/118)	4.35E-05
Olfactory receptor 1L4 (OR1L4)	PF13853	25.664 (29/113)	4.42E-05
Olfactory receptor 2J1 (OR2J1)	PF13853	29.457 (38/129)	4.76E-05
Olfactory receptor 10K1 (OR10K1)	PF13853	26.271 (31/118)	4.95E-05
Olfactory receptor 8A1 (OR8A1)	PF13853	25.185 (34/135)	4.97E-05
Olfactory receptor 9A2 (OR9A2)	PF13853	24.786 (29/117)	5.50E-05
Olfactory receptor 5P3 (OR5P3)	PF13853	31.683 (32/101)	5.71E-05
Olfactory receptor 4N5 (OR4N5)	PF13853	23.358 (32/137)	6.41E-05
Olfactory receptor 2A25 (OR2A25)	PF13853	26.667 (28/105)	6.57E-05
Olfactory receptor 51L1 (OR51L1)	PF13853	22.302 (31/139)	6.67E-05
Olfactory receptor 51T1 (OR51T1)	PF13853	24.771 (27/109)	7.23E-05
Olfactory receptor 2F1 (OR2F1)	PF13853	23.790 (59/248)	7.40E-05
Olfactory receptor 14I1 (OR14I1)	PF13853	23.967 (29/121)	7.46E-05
Olfactory receptor 13J1 (OR13J1)	PF13853	25.000 (51/204)	7.96E-05
Olfactory receptor 10Z1 (OR10Z1)	PF13853	27.481 (36/131)	7.99E-05
Olfactory receptor 10R2 (OR10R2)	PF13853	25.410 (31/122)	8.01E-05
Olfactory receptor 13C2 (OR13C2)	PF13853	20.354 (69/339)	8.04E-05
Olfactory receptor 10A3 (OR10A3)	PF13853	21.757 (52/239)	8.61E-05
Olfactory receptor 10J4 (OR10J4)	PF13853	23.721 (51/215)	8.68E-05
Olfactory receptor 5K1 (OR5K1)	PF13853	26.667 (32/120)	8.98E-05
Olfactory receptor 6C65 (OR6C65)	PF13853	22.798 (44/193)	9.02E-05
Olfactory receptor 8G1 (OR8G1)	PF13853	26.446 (32/121)	9.65E-05
Olfactory receptor 4F6 (OR4F6)	PF13853	23.932 (28/117)	9.94E-05
Olfactory receptor 10Q1 (OR10Q1)	PF13853	25.243 (26/103)	1.06E-04
Olfactory receptor 52Z1P (OR52Z1P)	PF13853	28.571 (36/126)	1.07E-04
Olfactory receptor 1D4 (OR1D4)	PF13853	27.731 (33/119)	1.09E-04
Olfactory receptor 4F3/4F16/4F29 (OR4F3; OR4F16; OR4F29)	PF13853	25.203 (31/123)	1.14E-04
Olfactory receptor 8U9 (OR8U9)	PF13853	28.000 (28/100)	1.15E-04
Putative olfactory receptor 2W6 (OR2W6P)	PF13853	25.490 (26/102)	1.16E-04
Olfactory receptor 52M1 (OR52M1)	PF13853	27.523 (30/109)	1.18E-04
Olfactory receptor 1G1 (OR1G1)	PF13853	26.087 (30/115)	1.19E-04
Olfactory receptor 8J2 (OR8J2)	PF13853	31.959 (31/97)	1.21E-04
Olfactory receptor 5M3 (OR5M3)	PF13853	28.099 (34/121)	1.29E-04
Putative olfactory receptor 8G2 (OR8G2P)	PF13853	23.967 (29/121)	1.31E-04
Olfactory receptor 14A16 (OR14A16)	PF13853	24.390 (30/123)	1.36E-04
Olfactory receptor 51I2 (OR51I2)	PF13853	26.549 (30/113)	1.38E-04
Olfactory receptor 6C3 (OR6C3)	PF13853	22.000 (44/200)	1.39E-04
Olfactory receptor 2T2 (OR2T2)	PF13853	22.727 (35/154)	1.52E-04
Olfactory receptor 4C15 (OR4C15)	PF13853	25.210 (30/119)	1.60E-04
Olfactory receptor 4K13 (OR4K13)	PF13853	27.451 (28/102)	1.67E-04
Olfactory receptor 2A1/2A42 (OR2A1; OR2A42)	PF13853	27.619 (29/105)	1.70E-04
Olfactory receptor 52R1 (OR52R1)	PF13853	28.440 (31/109)	1.88E-04
Olfactory receptor 2C1 (OR2C1)	PF13853	23.834 (46/193)	2.15E-04
Olfactory receptor 4F5 (OR4F5)	PF13853	29.167 (28/96)	2.20E-04
Olfactory receptor 4F21 (OR4F21)	PF13853	24.390 (30/123)	2.23E-04
Olfactory receptor 5C1 (OR5C1)	PF13853	25.743 (26/101)	2.30E-04
Olfactory receptor 2V2 (OR2V2)	PF13853	28.972 (31/107)	2.33E-04
Olfactory receptor 10G3 (OR10G3)	PF13853	24.370 (29/119)	2.34E-04
Olfactory receptor 4F4 (OR4F4)	PF13853	29.167 (28/96)	2.36E-04
Olfactory receptor 4F17 (OR4F17)	PF13853	29.167 (28/96)	2.36E-04
Olfactory receptor 4C16 (OR4C16)	PF13853	25.217 (29/115)	2.38E-04
Olfactory receptor 51S1 (OR51S1)	PF13853	24.638 (34/138)	2.43E-04
Olfactory receptor 4D2 (OR4D2)	PF13853	23.077 (33/143)	2.69E-04
Olfactory receptor 2D3 (OR2D3)	PF13853	27.835 (27/97)	2.70E-04
Olfactory receptor 2F2 (OR2F2)	PF13853	22.549 (23/102)	2.85E-04
Olfactory receptor 5K2 (OR5K2)	PF13853	26.667 (32/120)	2.94E-04
Olfactory receptor 5M11 (OR5M11)	PF13853	27.928 (31/111)	3.08E-04
Putative olfactory receptor 8G3 pseudogene (OR8G3P)	PF13853	25.620 (31/121)	3.30E-04
Olfactory receptor 1N1 (OR1N1)	PF13853	26.050 (31/119)	3.62E-04
Olfactory receptor 2K2 (OR2K2)	PF13853	28.037 (30/107)	3.84E-04
Olfactory receptor 6C75 (OR6C75)	PF13853	21.477 (32/149)	3.89E-04
Olfactory receptor 4C6 (OR4C6)	PF13853	23.729 (28/118)	4.18E-04
Olfactory receptor 9Q2 (OR9Q2)	PF13853	24.107 (27/112)	4.20E-04
Olfactory receptor 5B2 (OR5B2)	PF13853	25.472 (27/106)	4.45E-04
Olfactory receptor 2AK2 (OR2AK2)	PF13853	26.429 (37/140)	4.52E-04
Olfactory receptor 2AE1 (OR2AE1)	PF13853	23.944 (34/142)	4.54E-04
Olfactory receptor 2L5 (OR2L5)	PF13853	22.581 (35/155)	4.57E-04
Olfactory receptor 2G6 (OR2G6)	PF13853	21.809 (41/188)	4.70E-04
Olfactory receptor 11A1 (OR11A1)	PF13853	26.050 (31/119)	4.73E-04
Olfactory receptor 5I1 (OR5I1)	PF13853	28.125 (36/128)	4.76E-04
Olfactory receptor 1D5 (OR1D5)	PF13853	26.891 (32/119)	4.77E-04
Olfactory receptor 5B17 (OR5B17)	PF13853	25.472 (27/106)	4.93E-04
Olfactory receptor 5AR1 (OR5AR1)	PF13853	27.103 (29/107)	5.28E-04
Olfactory receptor 51D1 (OR51D1)	PF13853	25.688 (28/109)	5.34E-04
Olfactory receptor 4L1 (OR4L1)	PF13853	26.415 (28/106)	5.36E-04
Olfactory receptor 51V1 (OR51V1)	PF13853	28.689 (35/122)	5.54E-04
Olfactory receptor 5G3 (OR5G3)	PF13853	25.833 (31/120)	5.73E-04
Olfactory receptor 1F1 (OR1F1)	PF13853	23.276 (27/116)	6.34E-04
Olfactory receptor 5M8 (OR5M8)	PF13853	28.571 (32/112)	6.38E-04
Putative olfactory receptor 4A4 (OR4A4P)	PF13853	23.276 (27/116)	6.72E-04
Olfactory receptor 3A3 (OR3A3)	PF13853	26.087 (30/115)	6.84E-04
Putative olfactory receptor 7A2 (OR7A2P)	PF13853	26.016 (32/123)	7.26E-04
Olfactory receptor 5M10 (OR5M10)	PF13853	28.571 (32/112)	7.43E-04
Olfactory receptor 2T33 (OR2T33)	PF13853	19.171 (37/193)	7.66E-04
Olfactory receptor 4K5 (OR4K5)	PF13853	24.031 (31/129)	7.78E-04
Olfactory receptor 6F1 (OR6F1)	PF13853	25.758 (34/132)	7.96E-04
Olfactory receptor 2G3 (OR2G3)	PF13853	24.762 (26/105)	7.98E-04
Olfactory receptor 2C3 (OR2C3)	PF13853	22.826 (42/184)	8.00E-04
Olfactory receptor 13H1 (OR13H1)	PF13853	25.714 (27/105)	8.03E-04
Olfactory receptor 4N2 (OR4N2)	PF13853	23.418 (37/158)	8.30E-04
Olfactory receptor 51E1 (OR51E1)	PF13853	24.540 (40/163)	8.75E-04
Olfactory receptor 2AJ1 (OR2AJ1)	PF13853	24.603 (31/126)	8.84E-04
Olfactory receptor 10S1 (OR10S1)	PF13853	27.119 (32/118)	1.00E-03
Olfactory receptor 7G2 (OR7G2)	PF13853	27.826 (32/115)	1.00E-03
Olfactory receptor 1S2 (OR1S2)	PF13853	23.843 (67/281)	1.00E-03
Olfactory receptor 8G5 (OR8G5)	PF13853	26.446 (32/121)	1.00E-03
Olfactory receptor 4D5 (OR4D5)	PF13853	22.689 (27/119)	1.00E-03
Olfactory receptor 5M9 (OR5M9)	PF13853	29.907 (32/107)	1.00E-03
Olfactory receptor 8K3 (OR8K3)	PF13853	28.182 (31/110)	1.00E-03
Olfactory receptor 52E4 (OR52E4)	PF13853	24.771 (27/109)	1.00E-03
Olfactory receptor 8H3 (OR8H3)	PF13853	23.585 (25/106)	1.00E-03
Olfactory receptor 5F1 (OR5F1)	PF13853	26.316 (30/114)	1.00E-03
Olfactory receptor 2T10 (OR2T10)	PF13853	21.000 (42/200)	1.00E-03
Olfactory receptor 8J1 (OR8J1)	PF13853	28.155 (29/103)	1.00E-03
Olfactory receptor 5W2 (OR5W2)	PF13853	22.951 (28/122)	1.00E-03
Olfactory receptor 1L6 (OR1L6)	PF13853	24.561 (28/114)	1.00E-03
Olfactory receptor 2T35 (OR2T35)	PF13853	23.377 (36/154)	1.00E-03
Olfactory receptor 4F15 (OR4F15)	PF13853	22.917 (22/96)	1.00E-03
Olfactory receptor 2M4 (OR2M4)	PF13853	24.138 (28/116)	1.00E-03
Olfactory receptor 11L1 (OR11L1)	PF13853	24.060 (32/133)	1.00E-03
Olfactory receptor 8H2 (OR8H2)	PF13853	25.203 (31/123)	1.00E-03
Olfactory receptor 10H4 (OR10H4)	PF13853	26.804 (26/97)	1.00E-03
Olfactory receptor 4C3 (OR4C3)	PF13853	22.034 (26/118)	2.00E-03
Olfactory receptor 9I1 (OR9I1)	PF13853	24.880 (52/209)	2.00E-03
Putative olfactory receptor 14L1 (OR14L1P)	PF13853	27.358 (29/106)	2.00E-03
Olfactory receptor 13C5 (OR13C5)	PF13853	25.225 (28/111)	2.00E-03
Olfactory receptor 10G6 (OR10G6)	PF13853	24.576 (29/118)	2.00E-03
Olfactory receptor 8B3 (OR8B3)	PF13853	28.155 (29/103)	2.00E-03
Olfactory receptor 2L2 (OR2L2)	PF13853	23.387 (29/124)	2.00E-03
Olfactory receptor 2T4 (OR2T4)	PF13853	21.429 (42/196)	2.00E-03
Olfactory receptor 4K14 (OR4K14)	PF13853	26.582 (42/158)	2.00E-03
Olfactory receptor 8B2 (OR8B2)	PF13853	25.893 (29/112)	2.00E-03
Olfactory receptor 7A10 (OR7A10)	PF13853	24.667 (37/150)	2.00E-03
Olfactory receptor 5T1 (OR5T1)	PF13853	29.245 (31/106)	2.00E-03
Olfactory receptor 5M1 (OR5M1)	PF13853	28.571 (32/112)	2.00E-03
Olfactory receptor 6V1 (OR6V1)	PF13853	24.167 (29/120)	2.00E-03
Olfactory receptor 51G1 (OR51G1)	PF13853	25.225 (28/111)	2.00E-03
Olfactory receptor 13C9 (OR13C9)	PF13853	23.770 (29/122)	2.00E-03
Olfactory receptor 52A5 (OR52A5)	PF13853	25.941 (62/239)	2.00E-03
Olfactory receptor 6C70 (OR6C70)	PF13853	21.081 (39/185)	2.00E-03
Olfactory receptor 5D13 (OR5D13)	PF13853	23.485 (31/132)	2.00E-03
Olfactory receptor 13C7 (OR13C7)	PF13853	24.265 (33/136)	2.00E-03
Olfactory receptor 14A2 (OR14A2)	PF13853	32.609 (30/92)	2.00E-03
Olfactory receptor 5T2 (OR5T2)	PF13853	28.713 (29/101)	3.00E-03
Olfactory receptor 56A3 (OR56A3)	PF13853	24.476 (35/143)	3.00E-03
Olfactory receptor 6N1 (OR6N1)	PF13853	24.561 (28/114)	3.00E-03
Olfactory receptor 4A8 (OR4A8)	PF13853	21.094 (27/128)	3.00E-03
Olfactory receptor 51E2 (OR51E2)	PF13853	24.167 (58/240)	3.00E-03
Olfactory receptor 5AL1 (OR5AL1)	PF13853	27.559 (35/127)	3.00E-03
Olfactory receptor 2AG1 (OR2AG1)	PF13853	23.438 (30/128)	3.00E-03
Olfactory receptor 2A12 (OR2A12)	PF13853	28.571 (28/98)	3.00E-03
Olfactory receptor 4A47 (OR4A47)	PF13853	24.490 (24/98)	3.00E-03
Olfactory receptor 4C11 (OR4C11)	PF13853	24.779 (28/113)	4.00E-03
Olfactory receptor 8D4 (OR8D4)	PF13853	25.000 (29/116)	4.00E-03
Olfactory receptor 5T3 (OR5T3)	PF13853	31.959 (31/97)	4.00E-03
Olfactory receptor 1Q1 (OR1Q1)	PF13853	24.800 (31/125)	4.00E-03
Olfactory receptor 7G1 (OR7G1)	PF13853	22.642 (48/212)	4.00E-03
Olfactory receptor 10P1 (OR10P1)	PF13853	23.404 (22/94)	4.00E-03
Olfactory receptor 8D1 (OR8D1)	PF13853	29.592 (29/98)	5.00E-03
Putative olfactory receptor 10J6 (OR10J6P)	PF13853	22.951 (28/122)	5.00E-03
Olfactory receptor 52E5 (OR52E5)	PF13853	25.600 (32/125)	5.00E-03
Olfactory receptor 52J3 (OR52J3)	PF13853	26.733 (27/101)	5.00E-03
Olfactory receptor 5P2 (OR5P2)	PF13853	28.302 (30/106)	5.00E-03
Olfactory receptor 2T29 (OR2T29)	PF13853	22.835 (29/127)	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
Neuroactive ligand-receptor interaction	hsa04080	Affiliated Target
Class: Environmental Information Processing => Signaling molecules and interaction	Pathway Hierarchy
Gap junction	hsa04540	Affiliated Target
Class: Cellular Processes => Cellular community - eukaryotes	Pathway Hierarchy
Serotonergic synapse	hsa04726	Affiliated Target
Class: Organismal Systems => Nervous system	Pathway Hierarchy
Inflammatory mediator regulation of TRP channels	hsa04750	Affiliated Target
Class: Organismal Systems => Sensory system	Pathway Hierarchy

Degree	2	Degree centrality	2.15E-04	Betweenness centrality	2.02E-04
Closeness centrality	1.86E-01	Radiality	1.31E+01	Clustering coefficient	0.00E+00
Neighborhood connectivity	2.65E+01	Topological coefficient	5.00E-01	Eccentricity	12
Download	Click to Download the Full PPI Network of This Target

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 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

[+] 5 KEGG Pathways

Calcium signaling pathway

Neuroactive ligand-receptor interaction

Gap junction

Serotonergic synapse

Inflammatory mediator regulation of TRP channels

Panther Pathway

[+] 1 Panther Pathways

5HT2 type receptor mediated signaling pathway

Reactome

[+] 2 Reactome Pathways

Serotonin receptors

G alpha (q) signalling events

WikiPathways

[+] 9 WikiPathways

Serotonin Receptor 2 and STAT3 Signaling

Serotonin Receptor 2 and ELK-SRF/GATA4 signaling

SIDS Susceptibility Pathways

Monoamine GPCRs

GPCRs, Class A Rhodopsin-like

Gastrin-CREB signalling pathway via PKC and MAPK

GPCR ligand binding

GPCR downstream signaling

GPCRs, Other

Target-Related Models and Studies

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Target Validation

Target Validation Info

References

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REF 1

Beneficial effects of sarpogrelate hydrochloride, a 5-HT2A receptor antagonist, supplemented with pioglitazone on diabetic model mice. Endocr Res. 2009;34(1-2):18-30.

REF 2

URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4133).

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Anxiolytic effects of aniracetam in three different mouse models of anxiety and the underlying mechanism. Eur J Pharmacol. 2001 May 18;420(1):33-43.

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Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019

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Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.

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Pharmacological profile of lurasidone, a novel antipsychotic agent with potent 5-hydroxytryptamine 7 (5-HT7) and 5-HT1A receptor activity. J Pharmacol Exp Ther. 2010 Jul;334(1):171-81.

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Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

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The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.

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ClinicalTrials.gov (NCT00495885) Efficacy and Safety of M100907 on Sleep Maintenance Insomnia With a Sub-study in Stable Type II Diabetes Mellitus. U.S. National Institutes of Health.

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ClinicalTrials.gov (NCT03397134) Study to Evaluate Efficacy and Safety of Roluperidone (MIN-101) in Adult Patients With Negative Symptoms of Schizophrenia. U.S. National Institutes of Health.

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ClinicalTrials.gov (NCT01295372) Safety and Efficacy of Zicronapine in Patients With Schizophrenia. U.S. National Institutes of Health.

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Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023041)

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Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

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Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

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ClinicalTrials.gov (NCT02035553) A Study of the Safety and Efficacy of Pimavanserin in Patients With Alzheimer's Disease Psychosis. U.S. National Institutes of Health.

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Pharmacological profile of the new potent neuroleptic ocaperidone (R 79,598). J Pharmacol Exp Ther. 1992 Jan;260(1):146-59.

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ClinicalTrials.gov (NCT00259311) Efficacy Study of LY2422347 to Treat Insomnia. U.S. National Institutes of Health.

REF 32

ClinicalTrials.gov (NCT01490086) RP5063 in Subjects With Schizophrenia or Schizoaffective Disorder. U.S. National Institutes of Health.

REF 33

ClinicalTrials.gov (NCT02258152) SYN120 Study to Evaluate Its Safety, Tolerability and Efficacy in Parkinson's Disease Dementia (SYNAPSE) (SYNAPSE). U.S. National Institutes of Health.

REF 34

1192U90 in animal tests that predict antipsychotic efficacy, anxiolysis, and extrapyramidal side effects. Neuropsychopharmacology. 1996 Sep;15(3):231-42.

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Small Molecule Therapeutics for Schizophrenia, Sylvain Celanire. Page(30).

REF 36

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032727)

REF 37

ClinicalTrials.gov (NCT02034292) Safety Study of APD-791 With Aspirin and/or Clopidogrel. U.S. National Institutes of Health.

REF 38

5-HT1A receptor ligands and their therapeutic applications: review of new patents.Expert Opin Ther Pat. 2018 Sep;28(9):679-689.

REF 39

REF 40

Psychopathology and psychophysiology of minimal LSD-25 dosage; a preliminary dosage-response spectrum. AMA Arch Neurol Psychiatry. 1958 Feb;79(2):208-10.

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Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001479)

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Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014343)

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Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000314)

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