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

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]

Chemical Structure based Activity Landscape of Target

Top

Drug Property Profile of Target

Top

(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

Top

Co-Targets

Co-Targets Info

Target Poor or Non Binders

Top

Target Poor or Non Binders

Target Poor or Non Binders Info

Target Profiles in Patients

Top

Target Expression
Profile (TEP)

Target Expression Profile Info

Target Affiliated Biological Pathways

Top

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

Top

Target Validation

Target Validation Info

References

Top

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Effects of R-102444 and its active metabolite R-96544, selective 5-HT2A receptor antagonists, on experimental acute and chronic pancreatitis: Additional evidence for possible involvement of 5-HT2A receptors in the development of experimental pancreatitis.Eur J Pharmacol.2005 Oct 3;521(1-3):156-63.

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Effects of R-102444, an orally active 5-HT2A receptor antagonist, in rat models of peripheral vascular disease. Vascul Pharmacol. 2004 Feb;41(1):7-13.

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