Target Information

Target General Information

Top

Target ID

T78709 (Former ID: TTDS00098)

Target Name

5-HT 1A receptor (HTR1A)

Synonyms

Serotonin receptor 1A; G-21; ADRBRL1; ADRB2RL1; 5-hydroxytryptamine receptor 1A; 5-HT1A receptor; 5-HT1A; 5-HT-1A

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Gene Name

HTR1A

Target Type

Successful target

[1]

Disease

[+] 5 Target-related Diseases

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

Depression [ICD-11: 6A70-6A7Z]

Hypertension [ICD-11: BA00-BA04]

Migraine [ICD-11: 8A80]

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

Function

Functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling inhibits adenylate cyclase activity and activates a phosphatidylinositol-calcium second messenger system that regulates the release of Ca(2+) ions from intracellular stores. Plays a role in the regulation of 5-hydroxytryptamine release and in the regulation of dopamine and 5-hydroxytryptamine metabolism. Plays a role in the regulation of dopamine and 5-hydroxytryptamine levels in the brain, and thereby affects neural activity, mood and behavior. Plays a role in the response to anxiogenic stimuli. G-protein coupled receptor for 5-hydroxytryptamine (serotonin).

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BioChemical Class

GPCR rhodopsin

UniProt ID

5HT1A_HUMAN

Sequence

MDVLSPGQGNNTTSPPAPFETGGNTTGISDVTVSYQVITSLLLGTLIFCAVLGNACVVAA
IALERSLQNVANYLIGSLAVTDLMVSVLVLPMAALYQVLNKWTLGQVTCDLFIALDVLCC
TSSILHLCAIALDRYWAITDPIDYVNKRTPRRAAALISLTWLIGFLISIPPMLGWRTPED
RSDPDACTISKDHGYTIYSTFGAFYIPLLLMLVLYGRIFRAARFRIRKTVKKVEKTGADT
RHGASPAPQPKKSVNGESGSRNWRLGVESKAGGALCANGAVRQGDDGAALEVIEVHRVGN
SKEHLPLPSEAGPTPCAPASFERKNERNAEAKRKMALARERKTVKTLGIIMGTFILCWLP
FFIVALVLPFCESSCHMPTLLGAIINWLGYSNSLLNPVIYAYFNKDFQNAFKKIIKCKFC
RQ

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3D Structure

Click to Show 3D Structure of This Target

AlphaFold

HIT2.0 ID

T31QEZ

Drugs and Modes of Action

Top

Approved Drug(s)

[+] 9 Approved Drugs

Buspirone

Drug Info

Approved

Anxiety disorder

[2], [3]

Flibanserin

Drug Info

Approved

Mood disorder

[4], [5]

Gepirone

Drug Info

Approved

Major depressive disorder

[6]

OPC-34712

Drug Info

Approved

Major depressive disorder

[7], [8]

TERTATOLOL

Drug Info

Approved

Hypertension

[9], [10]

Trazodone

Drug Info

Approved

Depression

[11], [12]

Treximet

Drug Info

Approved

Migraine

[13]

Urapidil

Drug Info

Approved

Hypertension

[10]

Vilazodone

Drug Info

Approved

Major depressive disorder

[14], [15]

Clinical Trial Drug(s)

[+] 32 Clinical Trial Drugs

CM-2395

Drug Info

Phase 3

Schizophrenia

[16]

Eltoprazine

Drug Info

Phase 3

Attention deficit hyperactivity disorder

[17]

SEP-363856

Drug Info

Phase 3

Schizophrenia

[18]

Xaliproden

Drug Info

Phase 3

Juvenile idiopathic arthritis

[19]

LECOZOTAN HYDROCHLORIDE

Drug Info

Phase 2/3

Cognitive impairment

[20]

Sarizotan

Drug Info

Phase 2/3

Rett syndrome

[21]

Ensaculin hydrochloride

Drug Info

Phase 2

Parkinson disease

[22]

FKW00GA

Drug Info

Phase 2

Social phobia

[17]

Mazapertine succinate

Drug Info

Phase 2

Psychotic disorder

[23]

MIN-117

Drug Info

Phase 2

Major depressive disorder

[24]

MN-305

Drug Info

Phase 2

Mood disorder

[25]

Neu-P11

Drug Info

Phase 2

Insomnia

[26]

OPC-14523

Drug Info

Phase 2

Mood disorder

[27]

ORG-13011

Drug Info

Phase 2

Psychotic disorder

[28]

RP5063

Drug Info

Phase 2

Schizophrenia

[29]

S-15535

Drug Info

Phase 2

Anxiety disorder

[30], [31]

S-16924

Drug Info

Phase 2

Anxiety disorder

[32], [33], [34]

SDZ-MAR-327

Drug Info

Phase 2

Psychotic disorder

[35], [36]

SUN N4057

Drug Info

Phase 2

Coronary artery disease

[37]

TGBA01AD

Drug Info

Phase 2

Mood disorder

[25]

TGFK08AA

Drug Info

Phase 2

Generalized anxiety disorder

[38]

TGFK09SD

Drug Info

Phase 2

Hypoactive sexual desire dysfunction

[39]

TGWOOAA

Drug Info

Phase 2

Social phobia

[40]

Zalospirone

Drug Info

Phase 2

Anxiety disorder

[41], [42]

1192U90

Drug Info

Phase 1

Psychotic disorder

[43]

AV-965

Drug Info

Phase 1

Alzheimer disease

[44]

DSP-1053

Drug Info

Phase 1

Major depressive disorder

[45]

GSK-958108

Drug Info

Phase 1

Premature ejaculation

[46]

NLX-101

Drug Info

Phase 1

Rett syndrome

[47]

SKL-PSY

Drug Info

Phase 1

Bipolar disorder

[48]

SSR-181507

Drug Info

Phase 1

Schizophrenia

[35]

Umespirone

Drug Info

Phase 1

Anxiety disorder

[49]

Patented Agent(s)

[+] 5 Patented Agents

PMID30124346-Compound-13TABLE4

Drug Info

Patented

Attention deficit hyperactivity disorder

[50]

PMID30124346-Compound-34TABLE4

Drug Info

Patented

Attention deficit hyperactivity disorder

[50]

PMID30124346-Compound-60TABLE5

Drug Info

Patented

Parkinson disease

[50], [51], [52]

PMID30124346-Compound-LDT66

Drug Info

Patented

Benign prostatic hyperplasia

[50]

PMID30124346-Compound-LDT8

Drug Info

Patented

Benign prostatic hyperplasia

[50]

Discontinued Drug(s)

[+] 35 Discontinued Drugs

LYSERGIC ACID DIETHYLAMIDE

Drug Info

Withdrawn from market

Addictive disorder

[53], [54]

Bifeprunox

Drug Info

Discontinued in Phase 3

Schizophrenia

[35]

BMS-181100

Drug Info

Discontinued in Phase 3

Psychotic disorder

[55], [56]

Flesinoxan

Drug Info

Discontinued in Phase 3

Anxiety disorder

[57], [58]

Adatanserin

Drug Info

Discontinued in Phase 2

Mood disorder

[25]

ALNESPIRONE

Drug Info

Discontinued in Phase 2

Anxiety disorder

[59]

AP-521

Drug Info

Discontinued in Phase 2

Anxiety disorder

[60]

DU 125530

Drug Info

Discontinued in Phase 2

Mood disorder

[61]

GSK163090

Drug Info

Discontinued in Phase 2

Anxiety disorder

[62]

LESOPITRON DIHYDROCHLORIDE

Drug Info

Discontinued in Phase 2

Mood disorder

[63]

PRX-00023

Drug Info

Discontinued in Phase 2

Mood disorder

[25]

REC-15/3079

Drug Info

Discontinued in Phase 2

Urinary incontinence

[64], [65]

Robalzotan

Drug Info

Discontinued in Phase 2

Anxiety disorder

[66], [67]

BINOSPIRONE MESYLATE

Drug Info

Discontinued in Phase 1

Anxiety disorder

[68]

DU-29894

Drug Info

Discontinued in Phase 1

Psychotic disorder

[69]

E2101

Drug Info

Discontinued in Phase 1

Spasm

[70]

Ebalzotan

Drug Info

Discontinued in Phase 1

Anxiety disorder

[71]

Eptapirone

Drug Info

Discontinued in Phase 1

Anxiety disorder

[72]

GR-127607

Drug Info

Discontinued in Phase 1

Migraine

[73]

Nerisopam

Drug Info

Discontinued in Phase 1

Anxiety disorder

[74]

SLV-313

Drug Info

Discontinued in Phase 1

Schizophrenia

[35]

SUN-8399

Drug Info

Discontinued in Phase 1

Anxiety disorder

[75]

U-93385

Drug Info

Discontinued in Phase 1

Anxiety disorder

[76]

A-74283

Drug Info

Terminated

Hypertension

[78]

Anpirtoline

Drug Info

Terminated

Pain

[79]

BTS-79018

Drug Info

Terminated

Schizophrenia

[35]

CGS-18102A

Drug Info

Terminated

Anxiety disorder

[80]

Du-123015

Drug Info

Terminated

Anxiety disorder

[81]

HT-90B

Drug Info

Terminated

Anxiety disorder

[82]

Ipsapirone

Drug Info

Terminated

Anxiety disorder

[83], [84]

LY-293284

Drug Info

Terminated

Anxiety disorder

[85], [86]

RWJ-25730

Drug Info

Terminated

Psychotic disorder

[87]

S-14506

Drug Info

Terminated

Anxiety disorder

[88], [89]

SLV-307

Drug Info

Terminated

Parkinson disease

[90]

WAY-100635

Drug Info

Terminated

Eating disorder

[91], [92]

Preclinical Drug(s)

[+] 2 Preclinical Drugs

CM-2236

Drug Info

Preclinical

Post-traumatic stress disorder

[77]

PD-158771

Drug Info

Preclinical

Schizophrenia

[35]

Mode of Action

[+] 7 Modes of Action

Agonist

[+] 50 Agonist drugs

Buspirone

Drug Info

[1]

Gepirone

Drug Info

[6]

Urapidil

Drug Info

[98]

CM-2395

Drug Info

[99]

Eltoprazine

Drug Info

[100]

SEP-363856

Drug Info

[21]

MN-305

Drug Info

[25]

Neu-P11

Drug Info

[106]

SUN N4057

Drug Info

[114]

Zalospirone

Drug Info

[42]

1192U90

Drug Info

[35]

Aryl piperazine derivative 14

Drug Info

[50]

Aryl piperazine derivative 15

Drug Info

[50]

Aryl piperazine derivative 16

Drug Info

[50]

PMID30124346-Compound-13TABLE4

Drug Info

[50]

Flesinoxan

Drug Info

[130]

Adatanserin

Drug Info

[25], [133]

ALNESPIRONE

Drug Info

[134], [10]

AP-521

Drug Info

[135], [10]

LESOPITRON DIHYDROCHLORIDE

Drug Info

[137]

Ebalzotan

Drug Info

[145]

Eptapirone

Drug Info

[146]

GR-127607

Drug Info

[147]

Nerisopam

Drug Info

[148]

SUN-8399

Drug Info

[150]

U-93385

Drug Info

[151], [10]

CM-2236

Drug Info

[152]

A-74283

Drug Info

[153]

Ipsapirone

Drug Info

[160]

LY-293284

Drug Info

[161]

1-naphthylpiperazine

Drug Info

[185], [174]

5-CT

Drug Info

[200]

7-methoxy-1-naphthylpiperazine

Drug Info

[185]

BRL-15572

Drug Info

[204]

CP 93129

Drug Info

[200]

EDMT

Drug Info

[207]

FG-5893

Drug Info

[211]

L-772,405

Drug Info

[213]

LP-12

Drug Info

[214]

LP-211

Drug Info

[215]

LP-44

Drug Info

[214]

LY 165,163

Drug Info

[211]

nafadotride

Drug Info

[211]

piribedil

Drug Info

[222]

S-14671

Drug Info

[112]

SB 216641

Drug Info

[204]

spiroxatrine

Drug Info

[211]

U92016A

Drug Info

[232]

[3H]8-OH-DPAT

Drug Info

[237]

[3H]NLX-112

Drug Info

[238]

Modulator

[+] 34 Modulator drugs

Flibanserin

Drug Info

[5]

OPC-34712

Drug Info

[93], [94]

Trazodone

Drug Info

[96]

Vilazodone

Drug Info

[15]

Sarizotan

Drug Info

[103]

Ensaculin hydrochloride

Drug Info

[22], [104]

FKB01MD

Drug Info

[17]

Mazapertine succinate

Drug Info

[103]

OPC-14523

Drug Info

[107]

S-16924

Drug Info

[33], [34]

SDZ-MAR-327

Drug Info

[113]

TGBA01AD

Drug Info

[115]

TGFK08AA

Drug Info

[116]

TGFK09SD

Drug Info

[117]

NLX-101

Drug Info

[122]

SKL-PSY

Drug Info

[123]

SSR-181507

Drug Info

[124]

Bifeprunox

Drug Info

[127]

BMS-181100

Drug Info

[128], [129]

PRX-00023

Drug Info

[139]

DU-29894

Drug Info

[143]

E2101

Drug Info

[144]

SLV-313

Drug Info

[149]

Anpirtoline

Drug Info

[79]

CGS-18102A

Drug Info

[156]

Du-123015

Drug Info

[158]

HT-90B

Drug Info

[159]

RWJ-25730

Drug Info

[163]

S-14506

Drug Info

[164]

CGS-19480A

Drug Info

[205], [10]

EMD 56551

Drug Info

[208]

NPT-500

Drug Info

[123]

SEL-73

Drug Info

[123]

SR-59026

Drug Info

[231]

Inhibitor

[+] 142 Inhibitor drugs

TERTATOLOL

Drug Info

[95]

LYSERGIC ACID DIETHYLAMIDE

Drug Info

[126]

Sunepitron

Drug Info

[131]

TIOSPIRONE

Drug Info

[132]

MAZAPERTINE

Drug Info

[138]

A-80426

Drug Info

[154]

BMY-7378

Drug Info

[155]

CP-293019

Drug Info

[157]

WB-4101

Drug Info

[169]

(3-Chloro-phenyl)-piperazin-1-yl-methanone

Drug Info

[170]

(R)-(-)-10-methyl-11-hydroxyaporphine

Drug Info

[171]

(R)-11-Amino-2-methoxyaporphine

Drug Info

[172]

(R)-2,11-Diaminoaporphine

Drug Info

[172]

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

Drug Info

[174]

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

Drug Info

[175]

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

Drug Info

[175]

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

Drug Info

[175]

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

Drug Info

[175]

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

Drug Info

[175]

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

Drug Info

[176]

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

Drug Info

[170]

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

Drug Info

[170]

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

Drug Info

[177]

1-(2-((3-fluorophenoxy)methyl)phenyl)piperazine

Drug Info

[178]

1-(2-(2-chlorophenoxy)pyridin-3-yl)piperazine

Drug Info

[179]

1-(2-(2-fluorobenzyloxy)phenyl)piperazine

Drug Info

[178]

1-(2-(3-fluorophenoxy)phenyl)piperazine

Drug Info

[178]

1-(2-(4-fluorophenoxy)phenyl)piperazine

Drug Info

[178]

1-(2-(benzyloxy)phenyl)piperazine

Drug Info

[178]

1-(2-(phenoxymethyl)phenyl)piperazine

Drug Info

[178]

1-(2-Butoxy-phenyl)-piperazine

Drug Info

[180]

1-(2-Chloro-phenyl)-piperazine

Drug Info

[181]

1-(2-Ethoxy-phenyl)-piperazine

Drug Info

[180]

1-(2-Fluoro-phenyl)-piperazine

Drug Info

[180]

1-(2-Isopropoxy-phenyl)-piperazine

Drug Info

[180]

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

Drug Info

[182]

1-(2-Methoxy-phenyl)-piperazine

Drug Info

[181]

1-(2-methoxyphenyl)-4-pentylpiperazine

Drug Info

[183]

1-(2-phenoxyphenyl)piperazine

Drug Info

[178]

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

Drug Info

[184]

1-(3-Fluoro-phenyl)-piperazine

Drug Info

[180]

1-(3-Nitro-phenyl)-piperazine

Drug Info

[180]

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

Drug Info

[170]

1-(7-Methoxy-naphthalen-2-yl)-piperazine

Drug Info

[185]

1-(benzyloxy)-2-(2-phenylethyl)benzene

Drug Info

[186]

1-(benzyloxy)-2-[2-(3-methoxyphenyl)ethyl]benzene

Drug Info

[186]

1-Benzyl-4-chroman-2-ylmethyl-piperazine

Drug Info

[187]

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

Drug Info

[182]

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

Drug Info

[182]

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

Drug Info

[188]

1-Naphthalen-2-yl-piperazine

Drug Info

[174]

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

Drug Info

[189]

1-[(3-methoxybenzyl)oxy]-2-(2-phenylethyl)benzene

Drug Info

[186]

2-(2'-methyl-biphenyl-3-yl)-ethylamine

Drug Info

[190]

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

Drug Info

[177]

2-(2-chlorophenoxy)-3-(piperidin-4-yl)pyridine

Drug Info

[179]

2-(2-fluorophenoxy)-3-(piperidin-4-yl)pyridine

Drug Info

[179]

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

Drug Info

[177]

2-(2-methoxyphenoxy)-3-(piperidin-4-yl)pyridine

Drug Info

[179]

2-(3-Bromophenylthio)-N,N-dimethylethanamine

Drug Info

[191]

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

Drug Info

[177]

2-(4-Benzyl-piperidin-1-ylmethyl)-chroman-4-one

Drug Info

[187]

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

Drug Info

[177]

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

Drug Info

[177]

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

Drug Info

[192]

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

Drug Info

[193]

2-(Biphenyl-3-ylthio)-N,N-dimethylethanamine

Drug Info

[191]

2-Dipropylamino-1,2,3,4-tetrahydro-anthracen-9-ol

Drug Info

[95]

2-phenoxy-3-(piperidin-4-yl)pyridine

Drug Info

[179]

2-Piperazin-1-yl-benzonitrile

Drug Info

[180]

2-Piperazin-1-yl-phenol

Drug Info

[170]

2-{[2-(2-phenylethyl)phenoxy]methyl}pyridine

Drug Info

[186]

3-(1,2,3,6-Tetrahydro-pyridin-4-yl)-1H-indole

Drug Info

[194]

3-(1-Propyl-pyrrolidin-3-yl)-phenol

Drug Info

[189]

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

Drug Info

[193]

3-(2-Benzylamino-ethoxy)-phenol

Drug Info

[195]

3-(3-Methanesulfonyl-phenyl)-1-propyl-pyrrolidine

Drug Info

[189]

3-(4-Benzyl-piperidin-1-ylmethyl)-chroman-4-one

Drug Info

[187]

3-(4-Benzyl-piperidin-1-ylmethyl)-chromen-4-one

Drug Info

[187]

3-(piperidin-4-yl)-2-(o-tolyloxy)pyridine

Drug Info

[179]

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

Drug Info

[170]

3-Butyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol

Drug Info

[196]

3-Ethyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol

Drug Info

[196]

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

Drug Info

[189]

3-Naphthalen-1-yl-pyrrolidine

Drug Info

[189]

3-Phenyl-1-propyl-pyrrolidine

Drug Info

[189]

3-{[2-(2-phenylethyl)phenoxy]methyl}pyridine

Drug Info

[186]

4-(1H-indol-4-yloxy)-1-(isopropylamino)butan-2-ol

Drug Info

[197]

4-(2-(2-fluoro-5-methylphenoxy)phenyl)piperidine

Drug Info

[178]

4-(2-(2-fluorobenzyloxy)phenyl)piperidine

Drug Info

[178]

4-(2-(3-chlorophenoxy)phenyl)piperidine

Drug Info

[178]

4-(2-(3-fluorophenoxy)phenyl)piperidine

Drug Info

[178]

4-(2-(4-fluorobenzyloxy)phenyl)piperidine

Drug Info

[178]

4-(2-(4-fluorophenoxy)phenyl)piperidine

Drug Info

[178]

4-(2-(benzyloxy)-3-fluorophenyl)piperidine

Drug Info

[178]

4-(2-(benzyloxy)-6-fluorophenyl)piperidine

Drug Info

[178]

4-(2-(benzyloxy)phenyl)piperidine

Drug Info

[178]

4-(2-fluoro-6-(2-fluorophenoxy)phenyl)piperidine

Drug Info

[179]

4-(2-fluoro-6-(3-fluorophenoxy)phenyl)piperidine

Drug Info

[178]

100

4-(2-fluoro-6-(4-fluorophenoxy)phenyl)piperidine

Drug Info

[178]

101

4-(2-fluoro-6-phenoxyphenyl)piperidine

Drug Info

[178]

102

4-(2-phenoxyphenyl)piperidine

Drug Info

[178]

103

4-(3-fluoro-2-phenoxyphenyl)piperidine

Drug Info

[178]

104

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

Drug Info

[198]

105

4-Benzyl-1-chroman-2-ylmethyl-piperidine

Drug Info

[187]

106

4-Benzyl-1-chroman-3-ylmethyl-piperidine

Drug Info

[187]

107

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

Drug Info

[199]

108

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

Drug Info

[199]

109

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

Drug Info

[199]

110

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

Drug Info

[199]

111

8-Methoxy-1,2,3,4-tetrahydro-naphthalen-2-ylamine

Drug Info

[95]

112

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

Drug Info

[174]

113

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

Drug Info

[174]

114

8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine

Drug Info

[199]

115

8-Methoxy-quinolin-2-ylamine

Drug Info

[174]

116

9-Methoxy-1,2,3,4-tetrahydro-anthracen-2-ylamine

Drug Info

[95]

117

A-987306

Drug Info

[202]

118

AGROCLAVINE

Drug Info

[203]

119

Brolamfetamine

Drug Info

[177]

120

CHLOROPHENYLPIPERAZINE

Drug Info

[180]

121

ESCHOLTZINE

Drug Info

[209]

122

Etisulergine

Drug Info

[210]

123

JNJ-10392980

Drug Info

[212]

124

MCL-516

Drug Info

[172]

125

N-(3-(1H-indol-4-yloxy)propyl)cyclohexanamine

Drug Info

[197]

126

N-(3-(1H-indol-4-yloxy)propyl)cyclopentanamine

Drug Info

[197]

127

N-Benzyl-4-(2-diphenyl)-1-piperazinehexanamide

Drug Info

[215]

128

N-methyllaurotetanine

Drug Info

[209]

129

N-[4-(4-Phenyl-piperazin-1-yl)-butyl]-benzamide

Drug Info

[217]

130

PB-28

Drug Info

[220]

131

PG-01037

Drug Info

[221]

132

PHENYLPIPERAZINE

Drug Info

[174]

133

QUIPAZINE

Drug Info

[223]

134

SB-271046

Drug Info

[228]

135

SB-656104

Drug Info

[229]

136

SEROTONIN

Drug Info

[223]

137

SNAP-8719

Drug Info

[230]

138

TFMPP

Drug Info

[170]

139

UH-232

Drug Info

[233]

140

UH-301

Drug Info

[234]

141

WAY-466

Drug Info

[235]

142

[3H]spiperone

Drug Info

[169]

Antagonist

[+] 41 Antagonist drugs

Treximet

Drug Info

[97]

Xaliproden

Drug Info

[101]

LECOZOTAN HYDROCHLORIDE

Drug Info

[10], [102]

FKW00GA

Drug Info

[17]

MIN-117

Drug Info

[105]

ORG-13011

Drug Info

[10], [108]

RP5063

Drug Info

[109], [110]

S-15535

Drug Info

[10], [111], [112]

TGWOOAA

Drug Info

[118]

AV-965

Drug Info

[119]

DSP-1053

Drug Info

[120]

GSK-958108

Drug Info

[121]

Umespirone

Drug Info

[125]

PMID30124346-Compound-LDT8

Drug Info

[50]

DU 125530

Drug Info

[136]

GSK163090

Drug Info

[97]

REC-15/3079

Drug Info

[140]

Robalzotan

Drug Info

[141]

BINOSPIRONE MESYLATE

Drug Info

[142], [10]

PD-158771

Drug Info

[35]

NAN-190

Drug Info

[162]

SDZ 216-525

Drug Info

[162]

SLV-307

Drug Info

[165]

WAY-100635

Drug Info

[136], [166], [167], [168]

(R)-flurocarazolol

Drug Info

[173]

(S)-flurocarazolol

Drug Info

[173]

9-OH-risperidone

Drug Info

[201]

cyamemazine

Drug Info

[206]

GR 125,743

Drug Info

[200]

LY433221

Drug Info

[216]

MPDT

Drug Info

[207]

P-MPPI

Drug Info

[218], [162]

p-[18F]MPPF

Drug Info

[219]

repinotan

Drug Info

[224]

SB 272183

Drug Info

[226]

SB 649915

Drug Info

[227]

SB 714786

Drug Info

[227]

WAY 100135

Drug Info

[162]

[11C]WAY100635

Drug Info

[236]

[3H]p-MPPF

Drug Info

[239]

[3H]robalzotan

Drug Info

[240]

Ligand

[+] 4 Ligand drugs

Aryl piperazine derivative 1

Drug Info

[50]

Aryl piperazine derivative 6

Drug Info

[50]

PMID30124346-Compound-34TABLE4

Drug Info

[50]

PMID30124346-Compound-60TABLE5

Drug Info

[50]

Binder

[+] 1 Binder drugs

BTS-79018

Drug Info

[35]

Modulator (allosteric modulator)

[+] 1 Modulator (allosteric modulator) drugs

RS-30199

Drug Info

[225]

Cell-based Target Expression Variations

Top

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). 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 1B1 (OR1B1)	PF13853	29.861 (43/144)	2.61E-09
Olfactory receptor 4D11 (OR4D11)	PF13853	30.833 (37/120)	4.02E-08
Olfactory receptor 2M2 (OR2M2)	PF13853	25.362 (35/138)	2.63E-07
Olfactory receptor 2H2 (OR2H2)	PF13853	25.000 (63/252)	3.26E-07
Olfactory receptor 1A1 (OR1A1)	PF13853	24.044 (44/183)	4.24E-07
Olfactory receptor 2AG2 (OR2AG2)	PF13853	28.571 (36/126)	4.87E-07
Olfactory receptor 6C74 (OR6C74)	PF13853	23.188 (32/138)	5.84E-07
Olfactory receptor 2G6 (OR2G6)	PF13853	25.000 (53/212)	6.04E-07
Olfactory receptor 5M10 (OR5M10)	PF13853	24.242 (64/264)	7.13E-07
Olfactory receptor 9A2 (OR9A2)	PF13853	22.667 (34/150)	7.37E-07
Olfactory receptor 2M7 (OR2M7)	PF13853	25.217 (29/115)	8.43E-07
Olfactory receptor 7D2 (OR7D2)	PF13853	25.676 (57/222)	1.26E-06
Olfactory receptor 2M3 (OR2M3)	PF13853	26.087 (30/115)	1.47E-06
Olfactory receptor 4D6 (OR4D6)	PF13853	29.167 (35/120)	1.80E-06
Olfactory receptor 2M5 (OR2M5)	PF13853	26.087 (30/115)	1.82E-06
Olfactory receptor 2D2 (OR2D2)	PF13853	25.000 (52/208)	2.34E-06
Olfactory receptor 11A1 (OR11A1)	PF13853	28.477 (43/151)	2.61E-06
Olfactory receptor 5M1 (OR5M1)	PF13853	25.926 (42/162)	2.93E-06
Olfactory receptor 9A4 (OR9A4)	PF13853	25.984 (33/127)	3.37E-06
Olfactory receptor 1D4 (OR1D4)	PF13853	29.412 (40/136)	3.58E-06
Putative olfactory receptor 10D4 (OR10D4P)	PF13853	28.571 (36/126)	4.17E-06
Olfactory receptor 2T34 (OR2T34)	PF13853	27.632 (42/152)	4.40E-06
Olfactory receptor 52M1 (OR52M1)	PF13853	27.568 (51/185)	4.79E-06
Olfactory receptor 1A2 (OR1A2)	PF13853	22.513 (43/191)	5.46E-06
Olfactory receptor 8J3 (OR8J3)	PF13853	27.434 (31/113)	5.94E-06
Olfactory receptor 2T3 (OR2T3)	PF13853	27.632 (42/152)	7.51E-06
Olfactory receptor 14J1 (OR14J1)	PF13853	22.917 (33/144)	7.52E-06
Olfactory receptor 8D4 (OR8D4)	PF13853	26.957 (31/115)	8.24E-06
Olfactory receptor 4K3 (OR4K3)	PF13853	28.030 (37/132)	9.63E-06
Olfactory receptor 10A6 (OR10A6)	PF13853	24.378 (49/201)	1.33E-05
Olfactory receptor 2AT4 (OR2AT4)	PF13853	28.099 (34/121)	1.40E-05
Putative olfactory receptor 10D3 (OR10D3)	PF13853	26.718 (35/131)	2.03E-05
Olfactory receptor 2B11 (OR2B11)	PF13853	26.887 (57/212)	2.38E-05
Olfactory receptor 13J1 (OR13J1)	PF13853	24.031 (31/129)	2.50E-05
Olfactory receptor 2M4 (OR2M4)	PF13853	25.362 (35/138)	2.56E-05
Olfactory receptor 11H4 (OR11H4)	PF13853	29.915 (35/117)	2.84E-05
Olfactory receptor 51I2 (OR51I2)	PF13853	29.016 (56/193)	2.88E-05
Olfactory receptor 2L5 (OR2L5)	PF13853	28.571 (36/126)	2.90E-05
Olfactory receptor 11H7 (OR11H7)	PF13853	26.119 (35/134)	3.92E-05
Olfactory receptor 5V1 (OR5V1)	PF13853	27.049 (33/122)	3.94E-05
Olfactory receptor 4K2 (OR4K2)	PF13853	22.388 (30/134)	4.37E-05
Olfactory receptor 4K15 (OR4K15)	PF13853	24.409 (31/127)	4.50E-05
Olfactory receptor 1D5 (OR1D5)	PF13853	27.941 (38/136)	4.62E-05
Olfactory receptor 1J1 (OR1J1)	PF13853	28.148 (38/135)	4.72E-05
Olfactory receptor 2L8 (OR2L8)	PF13853	29.412 (35/119)	4.74E-05
Olfactory receptor 52B2 (OR52B2)	PF13853	30.120 (50/166)	4.78E-05
Olfactory receptor 4F6 (OR4F6)	PF13853	25.203 (31/123)	5.09E-05
Olfactory receptor 1K1 (OR1K1)	PF13853	26.064 (49/188)	5.44E-05
Olfactory receptor 2T12 (OR2T12)	PF13853	27.338 (38/139)	5.55E-05
Olfactory receptor 51B2 (OR51B2)	PF13853	32.558 (42/129)	5.62E-05
Olfactory receptor 2T29 (OR2T29)	PF13853	24.638 (51/207)	5.62E-05
Olfactory receptor 2AG1 (OR2AG1)	PF13853	26.829 (33/123)	5.69E-05
Olfactory receptor 2T5 (OR2T5)	PF13853	24.638 (51/207)	5.72E-05
Olfactory receptor 4D2 (OR4D2)	PF13853	25.974 (40/154)	6.97E-05
Olfactory receptor 2A2 (OR2A2)	PF13853	26.220 (43/164)	7.14E-05
Olfactory receptor 4D9 (OR4D9)	PF13853	24.167 (29/120)	8.07E-05
Olfactory receptor 4D10 (OR4D10)	PF13853	25.641 (30/117)	9.89E-05
Olfactory receptor 5M3 (OR5M3)	PF13853	27.083 (39/144)	1.02E-04
Olfactory receptor 4K13 (OR4K13)	PF13853	24.590 (30/122)	1.11E-04
Putative olfactory receptor 2W6 (OR2W6P)	PF13853	26.531 (39/147)	1.24E-04
Olfactory receptor 8J1 (OR8J1)	PF13853	26.549 (30/113)	1.24E-04
Olfactory receptor 51H1 (OR51H1)	PF13853	31.532 (35/111)	1.36E-04
Olfactory receptor 4K17 (OR4K17)	PF13853	23.776 (34/143)	1.45E-04
Olfactory receptor 2D3 (OR2D3)	PF13853	27.273 (33/121)	1.49E-04
Olfactory receptor 2T4 (OR2T4)	PF13853	22.941 (39/170)	1.50E-04
Olfactory receptor 12D3 (OR12D3)	PF13853	22.689 (27/119)	1.53E-04
Olfactory receptor 4K1 (OR4K1)	PF13853	24.390 (30/123)	1.63E-04
Olfactory receptor 4L1 (OR4L1)	PF13853	24.138 (35/145)	1.97E-04
Olfactory receptor 1C1 (OR1C1)	PF13853	24.812 (33/133)	1.98E-04
Olfactory receptor 52D1 (OR52D1)	PF13853	30.928 (30/97)	2.15E-04
Olfactory receptor 4M1 (OR4M1)	PF13853	28.082 (41/146)	2.20E-04
Olfactory receptor 10H4 (OR10H4)	PF13853	27.928 (31/111)	2.34E-04
Olfactory receptor 2L3 (OR2L3)	PF13853	28.125 (36/128)	2.61E-04
Olfactory receptor 8J2 (OR8J2)	PF13853	27.679 (31/112)	2.66E-04
Olfactory receptor 2G3 (OR2G3)	PF13853	29.310 (34/116)	2.69E-04
Olfactory receptor 8H3 (OR8H3)	PF13853	26.027 (38/146)	3.21E-04
Olfactory receptor 4A15 (OR4A15)	PF13853	24.390 (30/123)	3.41E-04
Olfactory receptor 4N5 (OR4N5)	PF13853	27.559 (35/127)	3.43E-04
Olfactory receptor 4F21 (OR4F21)	PF13853	24.576 (29/118)	3.80E-04
Olfactory receptor 10H1 (OR10H1)	PF13853	25.210 (30/119)	4.11E-04
Olfactory receptor 4F3/4F16/4F29 (OR4F3; OR4F16; OR4F29)	PF13853	24.576 (29/118)	4.49E-04
Olfactory receptor 51T1 (OR51T1)	PF13853	27.419 (34/124)	4.51E-04
Olfactory receptor 9A1 (OR9A1P)	PF13853	22.764 (28/123)	4.68E-04
Olfactory receptor 1D2 (OR1D2)	PF13853	27.731 (33/119)	4.87E-04
Olfactory receptor 11H6 (OR11H6)	PF13853	26.316 (30/114)	5.09E-04
Olfactory receptor 10G7 (OR10G7)	PF13853	26.154 (34/130)	5.85E-04
Olfactory receptor 2A14 (OR2A14)	PF13853	21.519 (34/158)	5.94E-04
Olfactory receptor 14A16 (OR14A16)	PF13853	22.059 (30/136)	6.59E-04
Olfactory receptor 4F15 (OR4F15)	PF13853	21.642 (29/134)	6.64E-04
Olfactory receptor 1L1 (OR1L1)	PF13853	25.000 (40/160)	6.76E-04
Olfactory receptor 52N4 (OR52N4)	PF13853	28.221 (46/163)	6.92E-04
Olfactory receptor 6C70 (OR6C70)	PF13853	21.014 (29/138)	7.00E-04
Olfactory receptor 52E5 (OR52E5)	PF13853	25.444 (43/169)	7.14E-04
Olfactory receptor 6C4 (OR6C4)	PF13853	20.290 (28/138)	7.46E-04
Olfactory receptor 1J2 (OR1J2)	PF13853	26.667 (36/135)	7.67E-04
Olfactory receptor 6K3 (OR6K3)	PF13853	25.197 (32/127)	7.74E-04
Olfactory receptor 8I2 (OR8I2)	PF13853	25.899 (36/139)	7.96E-04
Olfactory receptor 2H1 (OR2H1)	PF13853	25.455 (42/165)	8.08E-04
Olfactory receptor 10H3 (OR10H3)	PF13853	21.101 (23/109)	8.60E-04
Olfactory receptor 6C3 (OR6C3)	PF13853	20.290 (28/138)	8.72E-04
Olfactory receptor 4D1 (OR4D1)	PF13853	25.000 (30/120)	1.00E-03
Olfactory receptor 4C6 (OR4C6)	PF13853	25.203 (31/123)	1.00E-03
Olfactory receptor 6M1 (OR6M1)	PF13853	21.642 (29/134)	1.00E-03
Olfactory receptor 7E24 (OR7E24)	PF13853	22.368 (34/152)	1.00E-03
Putative olfactory receptor 1F12P (OR1F12P)	PF13853	23.684 (36/152)	1.00E-03
Olfactory receptor 11H2 (OR11H2)	PF13853	23.913 (33/138)	1.00E-03
Olfactory receptor 51L1 (OR51L1)	PF13853	31.776 (34/107)	1.00E-03
Olfactory receptor 6C1 (OR6C1)	PF13853	20.000 (28/140)	1.00E-03
Olfactory receptor 8B4 (OR8B4)	PF13853	25.410 (31/122)	1.00E-03
Olfactory receptor 10H2 (OR10H2)	PF13853	26.126 (29/111)	1.00E-03
Olfactory receptor 2T33 (OR2T33)	PF13853	25.180 (35/139)	1.00E-03
Olfactory receptor 6C2 (OR6C2)	PF13853	22.464 (31/138)	1.00E-03
Olfactory receptor 2T10 (OR2T10)	PF13853	26.357 (34/129)	1.00E-03
Olfactory receptor 2V1 (OR2V1)	PF13853	24.000 (30/125)	2.00E-03
Olfactory receptor 1E1 (OR1E1)	PF13853	25.641 (40/156)	2.00E-03
Olfactory receptor 5M11 (OR5M11)	PF13853	25.373 (34/134)	2.00E-03
Olfactory receptor 8H2 (OR8H2)	PF13853	26.000 (39/150)	2.00E-03
Olfactory receptor 2Y1 (OR2Y1)	PF13853	28.387 (44/155)	2.00E-03
Olfactory receptor 4D5 (OR4D5)	PF13853	25.410 (31/122)	2.00E-03
Olfactory receptor 2C3 (OR2C3)	PF13853	23.443 (64/273)	2.00E-03
Olfactory receptor 52H1 (OR52H1)	PF13853	28.846 (30/104)	2.00E-03
Olfactory receptor 6C75 (OR6C75)	PF13853	21.019 (33/157)	2.00E-03
Olfactory receptor 2A12 (OR2A12)	PF13853	24.370 (29/119)	2.00E-03
Olfactory receptor 5T3 (OR5T3)	PF13853	25.641 (30/117)	2.00E-03
Olfactory receptor 4M2 (OR4M2B)	PF13853	23.611 (34/144)	3.00E-03
Olfactory receptor 5P2 (OR5P2)	PF13853	24.031 (31/129)	3.00E-03
Olfactory receptor 6C6 (OR6C6)	PF13853	21.014 (29/138)	3.00E-03
Olfactory receptor 4Q3 (OR4Q3)	PF13853	28.571 (36/126)	3.00E-03
Olfactory receptor 11H1 (OR11H1)	PF13853	24.390 (30/123)	3.00E-03
Olfactory receptor 5T1 (OR5T1)	PF13853	25.984 (33/127)	3.00E-03
Olfactory receptor 51A7 (OR51A7)	PF13853	27.419 (34/124)	3.00E-03
Olfactory receptor 4S1 (OR4S1)	PF13853	25.564 (34/133)	3.00E-03
Olfactory receptor 5AU1 (OR5AU1)	PF13853	26.891 (32/119)	3.00E-03
Olfactory receptor 51D1 (OR51D1)	PF13853	27.692 (36/130)	3.00E-03
Olfactory receptor 2V2 (OR2V2)	PF13853	25.641 (30/117)	4.00E-03
Olfactory receptor 2AP1 (OR2AP1)	PF13853	22.581 (35/155)	4.00E-03
Olfactory receptor 1L8 (OR1L8)	PF13853	23.423 (26/111)	4.00E-03
Olfactory receptor 4M2 (OR4M2)	PF13853	23.611 (34/144)	4.00E-03
Putative olfactory receptor 14L1 (OR14L1P)	PF13853	22.388 (30/134)	4.00E-03
Olfactory receptor 2T1 (OR2T1)	PF13853	23.000 (46/200)	4.00E-03
Olfactory receptor 11H12 (OR11H12)	PF13853	39.623 (21/53)	4.00E-03
Olfactory receptor 2L2 (OR2L2)	PF13853	28.788 (38/132)	4.00E-03
Olfactory receptor 2J3 (OR2J3)	PF13853	23.786 (49/206)	4.00E-03
Olfactory receptor 2AE1 (OR2AE1)	PF13853	24.699 (41/166)	4.00E-03
Olfactory receptor 8B8 (OR8B8)	PF13853	25.600 (32/125)	5.00E-03
Olfactory receptor 51I1 (OR51I1)	PF13853	29.661 (35/118)	5.00E-03
Putative olfactory receptor 52L2 (OR52L2P)	PF13853	28.182 (31/110)	5.00E-03
Olfactory receptor 12D1 (OR12D1)	PF13853	25.000 (36/144)	5.00E-03
Olfactory receptor 8H1 (OR8H1)	PF13853	25.000 (40/160)	5.00E-03
Click to Show/Hide the Information of Human Similarity Proteins

KEGG Pathway	Pathway ID	Affiliated Target
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
Taste transduction	hsa04742	Affiliated Target
Class: Organismal Systems => Sensory system	Pathway Hierarchy

Degree	2	Degree centrality	2.15E-04	Betweenness centrality	6.17E-05
Closeness centrality	1.92E-01	Radiality	1.33E+01	Clustering coefficient	0.00E+00
Neighborhood connectivity	1.70E+01	Topological coefficient	5.00E-01	Eccentricity	13
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

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

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Co-Targets

Co-Targets Info

Target Poor or Non Binders

Top

Target Poor or Non Binders

Target Poor or Non Binders Info

Target Regulators

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Target-regulating Transcription Factors

Target-regulating Transcription Factors 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

[+] 3 KEGG Pathways

cAMP signaling pathway

Neuroactive ligand-receptor interaction

Serotonergic synapse

Panther Pathway

[+] 2 Panther Pathways

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

5HT1 type receptor mediated signaling pathway

Reactome

[+] 2 Reactome Pathways

Serotonin receptors

G alpha (i) signalling events

WikiPathways

[+] 6 WikiPathways

Serotonin HTR1 Group and FOS Pathway

SIDS Susceptibility Pathways

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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The serotonin 5-HT receptor agonist tandospirone improves executive function in common marmosets. Behav Brain Res. 2015 Jul 1;287:120-6.

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Neither in vivo MRI nor behavioural assessment indicate therapeutic efficacy for a novel 5HT1A agonist in rat models of ischaemic stroke. BMC Neuroscience 2009, 10:82.

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Effects of brexpiprazole, a novel serotonin-dopamine activity modulator, on phencyclidine-induced cognitive deficits in mice: a role for serotonin 5-HT1A receptors.Pharmacol Biochem Behav.2014 Sep;124:245-9.

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A positron emission tomography study to assess binding of lecozotan, a novel 5-hydroxytryptamine-1A silent antagonist, to brain 5-HT1A receptors in... Clin Pharmacol Ther. 2008 Jan;83(1):86-96.

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Dual ligands targeting dopamine D2 and serotonin 5-HT1A receptors as new antipsychotical or anti-Parkinsonian agents.Curr Med Chem.2014;21(4):437-57.

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The discriminative stimulus effects of KA 672, a putative cognitive enhancer: evidence for a 5-HT1A component. Pharmacol Biochem Behav. 1998 Jul;60(3):703-7.

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S 15535, a benzodioxopiperazine acting as presynaptic agonist and postsynaptic 5-HT1A receptor antagonist, prevents the impairment of spatial learning caused by intrahippocampal scopolamine. Br J Pharmacol. 1999 Nov;128(6):1207-14.

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Labelling of recombinant human and native rat serotonin 5-HT1A receptors by a novel, selective radioligand, [3H]-S 15535: definition of its binding profile using agonists, antagonists and inverse agonists. Naunyn Schmiedebergs Arch Pharmacol. 1998 Mar;357(3):205-17.

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DOI: 10.1038/sj.mp.4002062

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50 years of hurdles and hope in anxiolytic drug discovery. Nat Rev Drug Discov. 2013 Sep;12(9):667-87.

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Chronic alnespirone-induced desensitization of somatodendritic 5-HT1A autoreceptors in the rat dorsal raphe nucleus. Eur J Pharmacol. 1999 Jan 22;365(2-3):165-73.

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