Target Information

Target General Information

Top

Target ID

T92072 (Former ID: TTDS00186)

Target Name

Adenosine A1 receptor (ADORA1)

Synonyms

Adenosine receptor A1; A(1) adenosine receptor

Gene Name

ADORA1

Target Type

Successful target

[1]

Disease

[+] 1 Target-related Diseases

Orthostatic hypotension [ICD-11: BA21]

Function

The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase. Receptor for adenosine.

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BioChemical Class

GPCR rhodopsin

UniProt ID

AA1R_HUMAN

Sequence

MPPSISAFQAAYIGIEVLIALVSVPGNVLVIWAVKVNQALRDATFCFIVSLAVADVAVGA
LVIPLAILINIGPQTYFHTCLMVACPVLILTQSSILALLAIAVDRYLRVKIPLRYKMVVT
PRRAAVAIAGCWILSFVVGLTPMFGWNNLSAVERAWAANGSMGEPVIKCEFEKVISMEYM
VYFNFFVWVLPPLLLMVLIYLEVFYLIRKQLNKKVSASSGDPQKYYGKELKIAKSLALIL
FLFALSWLPLHILNCITLFCPSCHKPSILTYIAIFLTHGNSAMNPIVYAFRIQKFRVTFL
KIWNDHFRCQPAPPIDEDLPEERPDD

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3D Structure

Click to Show 3D Structure of This Target

PDB

ADReCS ID

BADD_A01328 ; BADD_A01334

HIT2.0 ID

T35LKG

Drugs and Modes of Action

Top

Approved Drug(s)

[+] 1 Approved Drugs

Caffeine

Drug Info

Approved

Orthostatic hypotension

[2], [3]

Clinical Trial Drug(s)

[+] 12 Clinical Trial Drugs

Rolofylline

Drug Info

Phase 3

Heart failure

[4], [5]

AMP-579

Drug Info

Phase 2

Hyperlipidaemia

[6]

Apaxifylline

Drug Info

Phase 2

Cognitive impairment

[7]

BAY 1067197

Drug Info

Phase 2

Heart failure

[8]

Capadenoson

Drug Info

Phase 2

Atrial fibrillation

[9]

DTI-0009

Drug Info

Phase 2

Atrial fibrillation

[10]

SELODENOSON

Drug Info

Phase 2

Cardiac arrhythmias

[10]

SLV320

Drug Info

Phase 2

Heart failure

[11], [12]

Tonapofylline

Drug Info

Phase 2

Acute and chronic heart failure

[13]

INO-8875

Drug Info

Phase 1/2

Glaucoma/ocular hypertension

[14]

GS 9667

Drug Info

Phase 1

Hypertriglyceridemia

[15], [16]

KF-17837

Drug Info

Phase 1

Parkinson disease

[17]

Discontinued Drug(s)

[+] 11 Discontinued Drugs

CVT-124

Drug Info

Discontinued in Phase 3

Autoimmune diabetes

[18]

N-0861

Drug Info

Discontinued in Phase 3

Cardiac disease

[19]

Tecadenoson

Drug Info

Discontinued in Phase 3

Cardiac arrhythmias

[20], [21]

BRL-61063

Drug Info

Discontinued in Phase 2

Allergy

[22]

FK-352

Drug Info

Discontinued in Phase 2

Hypertension

[23]

FK-453

Drug Info

Discontinued in Phase 2

Renal failure

[24], [25]

FK-838

Drug Info

Discontinued in Phase 2

Hypertension

[26]

GW-493838

Drug Info

Discontinued in Phase 2

Neuropathic pain

[27]

GR-79236

Drug Info

Discontinued in Phase 1

Diabetic complication

[28], [29]

SDZ-WAG-994

Drug Info

Discontinued in Phase 1

Hypertension

[30]

METHYLTHIOADENOSINE

Drug Info

Terminated

Multiple sclerosis

[32]

Preclinical Drug(s)

[+] 1 Preclinical Drugs

BAY 60-6583

Drug Info

Preclinical

Myocardial ischemia

[31]

Mode of Action

[+] 4 Modes of Action

Antagonist

[+] 42 Antagonist drugs

Caffeine

Drug Info

[1], [33]

Rolofylline

Drug Info

[5]

Apaxifylline

Drug Info

[35]

SLV320

Drug Info

[12]

CVT-124

Drug Info

[48], [49]

N-0861

Drug Info

[50]

FK-352

Drug Info

[52]

(E)-8-(3-chlorostyryl)-caffeine

Drug Info

[64]

4-Ethoxy-7-((E)-styryl)-furo[3,2-g]chromen-5-one

Drug Info

[95]

8-cyclopentyltheophylline

Drug Info

[100]

AS100

Drug Info

[106]

AS70

Drug Info

[106]

AS99

Drug Info

[106]

ATL802

Drug Info

[107]

CPFPX

Drug Info

[110]

flavone

Drug Info

[95]

FR194921

Drug Info

[114]

isobutylmethylxanthine

Drug Info

[120], [121]

KF26777

Drug Info

[123]

MRE 2029F20

Drug Info

[128]

MRE 3008F20

Drug Info

[109]

MRS1041

Drug Info

[95]

MRS1042

Drug Info

[95]

MRS1062

Drug Info

[95]

MRS1065

Drug Info

[95]

MRS1084

Drug Info

[95]

MRS1086

Drug Info

[95]

MRS1093

Drug Info

[95]

MRS1132

Drug Info

[95]

MRS1191

Drug Info

[125]

MRS1523

Drug Info

[125]

MRS923

Drug Info

[95]

MRS928

Drug Info

[95]

PSB-10

Drug Info

[138]

PSB-11

Drug Info

[138]

PSB36

Drug Info

[139]

PSB603

Drug Info

[137]

sakuranetin

Drug Info

[95]

VUF5574

Drug Info

[145]

WRC-0571

Drug Info

[146]

xanthine amine congener

Drug Info

[120]

[3H]DPCPX

Drug Info

[147]

Modulator

[+] 7 Modulator drugs

AMP-579

Drug Info

[34]

BAY 1067197

Drug Info

[36]

FK-453

Drug Info

[53]

FK-838

Drug Info

[54]

GW-493838

Drug Info

[37]

L-97-1 intravenous

Drug Info

[125]

Paeoniflorin

Drug Info

[125]

Agonist

[+] 22 Agonist drugs

Capadenoson

Drug Info

[37]

DTI-0009

Drug Info

[38], [39]

SELODENOSON

Drug Info

[38], [39], [40]

INO-8875

Drug Info

[43]

GS 9667

Drug Info

[44]

PMID27387065-Compound-6

Drug Info

[47]

Tecadenoson

Drug Info

[48], [49]

GR-79236

Drug Info

[55]

SDZ-WAG-994

Drug Info

[56]

BAY 60-6583

Drug Info

[57]

(R,S)-PHPNECA

Drug Info

[65]

(S)-PIA

Drug Info

[66]

2-chloroadenosine

Drug Info

[88]

5-Cl-5-deoxy-(+/-)-ENBA

Drug Info

[73]

CP608,039

Drug Info

[109]

LUF5831

Drug Info

[127]

MRS5151

Drug Info

[129]

N(6)-cyclohexyladenosine

Drug Info

[130]

PENECA

Drug Info

[65]

TCPA

Drug Info

[142]

[3H]CCPA

Drug Info

[140], [71]

[3H]HEMADO

Drug Info

[148]

Inhibitor

[+] 239 Inhibitor drugs

Tonapofylline

Drug Info

[41], [42]

KF-17837

Drug Info

[45]

SCH-442416

Drug Info

[46]

BRL-61063

Drug Info

[51]

ARISTEROMYCIN

Drug Info

[58]

METHYLTHIOADENOSINE

Drug Info

[59]

METRIFUDIL

Drug Info

[60]

ZM-241385

Drug Info

[61]

(1-Phenyl-propyl)-(9-phenyl-9H-purin-6-yl)-amine

Drug Info

[62]

(1H-Imidazo[4,5-c]quinolin-4-yl)-phenyl-amine HCl

Drug Info

[63]

(2-Chloro-9-methyl-9H-purin-6-yl)-phenyl-amine

Drug Info

[62]

(9-Methyl-9H-purin-6-yl)-phenyl-amine

Drug Info

[62]

1,3-Diallyl-3,7-dihydro-purine-2,6-dione

Drug Info

[67]

1,3-Diethyl-3,7-dihydro-purine-2,6-dione

Drug Info

[67]

1,3-Diisobutyl-3,7-dihydro-purine-2,6-dione

Drug Info

[67]

1,3-Dipropyl-3,7-dihydro-purine-2,6-dione

Drug Info

[67]

1-Butyl-8-phenyl-3,7-dihydro-purine-2,6-dione

Drug Info

[68]

1-Methyl-8-phenyl-3,7-dihydro-purine-2,6-dione

Drug Info

[69]

1-METHYLXANTHINE

Drug Info

[67]

1-Propyl-3,7-dihydro-purine-2,6-dione

Drug Info

[70]

1H-Imidazo[4,5-c]quinolin-4-ylamine HCl

Drug Info

[63]

2'-Me-tecadenoson

Drug Info

[71]

2,4-Dichloro-N-(4-phenyl-thiazol-2-yl)-benzamide

Drug Info

[72]

2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine

Drug Info

[73]

2,6,8-triphenyl-9H-purine

Drug Info

[74]

2,6-bis(4-tolyl)-9H-purine

Drug Info

[74]

2,6-dimethyl-8-ethyl-1-deazapurine

Drug Info

[75]

2,6-diphenyl-1-deazapurine

Drug Info

[75]

2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine

Drug Info

[75]

2,6-diphenyl-8-ethyl-1-deazapurine

Drug Info

[75]

2,6-diphenyl-8-methyl-1-deazapurine

Drug Info

[75]

2,6-diphenyl-8-tButyl-1-deazapurine

Drug Info

[75]

2,6-diphenyl-9H-purine

Drug Info

[74]

2,6-Diphenyl-pyrimidin-4-ylamine

Drug Info

[76]

2,6-dphenyl-8-propyl-1-deazapurine

Drug Info

[75]

2-(1H-benzo[d]imidazol-2-yl)quinoxaline

Drug Info

[77]

2-(2''-indolylethyloxy)adenosine

Drug Info

[78]

2-(2-furyl)-6-(1H-pyrazol-1-yl)pyrimidin-4-amine

Drug Info

[79]

2-(3''(5''-chloro-indolyl)ethyloxy)adenosine

Drug Info

[78]

2-(3''(7''-bromo-indolyl)ethyloxy)adenosine

Drug Info

[78]

2-(3''-(4''-bromo-indolyl)ethyloxy)adenosine

Drug Info

[78]

2-(3''-(5''-bromo-indolyl)ethyloxy)adenosine

Drug Info

[78]

2-(3''-(5''-fluoro-indolyl)ethyloxy)adenosine

Drug Info

[78]

2-(3''-(5''-hydroxyindolyl)ethyloxy)adenosine

Drug Info

[78]

2-(3''-(5''-iodo-indolyl)ethyloxy)adenosine

Drug Info

[78]

2-(3''-(5''-methoxy-indolyl)ethyloxy)adenosine

Drug Info

[78]

2-(3''-(6''-bromo-indolyl)ethyloxy)adenosine

Drug Info

[78]

2-(3''-(6''-chloro-indolyl)ethyloxy)adenosine

Drug Info

[78]

2-(3''-indolylethyloxy)adenosine

Drug Info

[78]

2-(3''-pyrrolylethyloxy)adenosine

Drug Info

[78]

2-(4-chloro-1H-benzo[d]imidazol-2-yl)quinoxaline

Drug Info

[80]

2-(4-chlorophenyl)-6-phenyl-9H-purine

Drug Info

[74]

2-(4-ethylthiobenzimidazol-2-yl)quinoxaline

Drug Info

[80]

2-(4-hydroxypent-1-yl)-N6-methoxyadenosine

Drug Info

[81]

2-(4-methoxyphenyl)-6-phenyl-9H-purine

Drug Info

[74]

2-(4-methyl-1H-benzo[d]imidazol-2-yl)quinoxaline

Drug Info

[77]

2-(5-cyano-1-pent-1-ynyl)-N6-methoxyadenosine

Drug Info

[81]

2-(6-amino-8-bromo-9H-purin-9-yl)ethanol

Drug Info

[82]

2-(6-Cyclopentylamino-purin-9-yl)-ethanol

Drug Info

[62]

2-(hex-1-ynyl)-N6-methoxyadenosine

Drug Info

[81]

2-Amino-4,6-di-furan-2-yl-nicotinonitrile

Drug Info

[83]

2-Amino-4,6-di-thiophen-2-yl-nicotinonitrile

Drug Info

[83]

2-Amino-4,6-diphenyl-nicotinonitrile

Drug Info

[83]

2-Amino-4,6-diphenyl-pyrimidin-5-carbonitrile

Drug Info

[76]

2-Amino-4,6-diphenyl-pyrimidine

Drug Info

[76]

2-Amino-4-furan-2-yl-6-phenyl-nicotinonitrile

Drug Info

[83]

2-Amino-4-phenyl-6-thiophen-2-yl-nicotinonitrile

Drug Info

[83]

2-Amino-6-furan-2-yl-4-phenyl-nicotinonitrile

Drug Info

[83]

2-amino-6-phenyl-4-p-tolylnicotinonitrile

Drug Info

[84]

2-Amino-6-phenyl-4-thiophen-2-yl-nicotinonitrile

Drug Info

[83]

2-amino-N-benzyl-6-phenyl-9H-purine-9-carboxamide

Drug Info

[85]

2-azido-N6-methyl-9-(beta-D-ribofuranosyl)adenine

Drug Info

[86]

2-chloro-2'-C-methyl-tecadenoson

Drug Info

[71]

2-chloro-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine

Drug Info

[87]

2-chloro-4-(thiophen-2-yl)thieno[3,2-d]pyrimidine

Drug Info

[87]

2-Cyclopentyl-1H-imidazo[4,5-c]quinolin-4-ylamine

Drug Info

[63]

2-ethyl-4-(furan-2-yl)thieno[3,2-d]pyrimidine

Drug Info

[87]

2-ethyl-4-(furan-3-yl)thieno[3,2-d]pyrimidine

Drug Info

[87]

2-ethyl-4-(pyridin-2-yl)thieno[3,2-d]pyrimidine

Drug Info

[87]

2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine

Drug Info

[87]

2-ethyl-4-(thiophen-2-yl)thieno[3,2-d]pyrimidine

Drug Info

[87]

2-ethynyl-N6-methoxyadenosine

Drug Info

[81]

2-m-tolyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one

Drug Info

[89]

2-m-tolyl-2H-pyrazolo[3,4-c]quinolin-4-amine

Drug Info

[89]

2-p-tolyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one

Drug Info

[89]

2-p-tolyl-2H-pyrazolo[3,4-c]quinolin-4-amine

Drug Info

[89]

2-Phenyl-1H-imidazo[4,5-c]quinolin-4-ylamine

Drug Info

[63]

2-phenyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one

Drug Info

[89]

2-phenyl-2H-pyrazolo[3,4-c]quinolin-4-amine

Drug Info

[89]

2-phenylpropoxyadenosine

Drug Info

[78]

2-tolyl-6-phenyl-9H-purine

Drug Info

[74]

2-[(4-acetylphenyl)ethynyl]-N6-methoxyadenosine

Drug Info

[81]

2-[(4-fluorophenyl)ethynyl]-N6-methoxyadenosine

Drug Info

[81]

3,4-Dichloro-N-(4-phenyl-thiazol-2-yl)-benzamide

Drug Info

[72]

3-(3-chloro-1H-pyrazol-5-yl)quinoxalin-2(1H)-one

Drug Info

[77]

3-Benzyl-7-methyl-[1,8]naphthyridin-4-ol

Drug Info

[90]

3-Benzyl-7-methyl-[1,8]naphthyridine-4-thiol

Drug Info

[90]

3-Chloro-N-(4-phenyl-thiazol-2-yl)-benzamide

Drug Info

[72]

3-noradamantyl-1,3-dipropylxanthine

Drug Info

[91]

100

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

Drug Info

[92]

101

4-(ethylthio)-6-phenyl-1,3,5-triazin-2-amine

Drug Info

[84]

102

4-(furan-2-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-amine

Drug Info

[93]

103

4-(furan-2-yl)thieno[3,2-d]pyrimidin-2-amine

Drug Info

[85]

104

4-(thiazol-2-yl)thieno[3,2-d]pyrimidin-2-amine

Drug Info

[87]

105

4-Amino-2,6-diphenyl-pyrimidine-5-carbonitrile

Drug Info

[76]

106

4-Bromo-N-(4-phenyl-thiazol-2-yl)-benzamide

Drug Info

[72]

107

4-Chloro-7-methyl-2-phenyl-[1,8]naphthyridine

Drug Info

[94]

108

4-Chloro-N-(4-phenyl-thiazol-2-yl)-benzamide

Drug Info

[72]

109

4-Methoxy-N-(3-phenyl-isoquinolin-1-yl)-benzamide

Drug Info

[72]

110

4-Methyl-N-(4-phenyl-thiazol-2-yl)-benzamide

Drug Info

[72]

111

4-Nitro-N-(4-phenyl-thiazol-2-yl)-benzamide

Drug Info

[72]

112

4-tert-Butyl-N-(4-phenyl-thiazol-2-yl)-benzamide

Drug Info

[72]

113

5,7-dibromo-9H-pyrido[3,4-b]indol-6-ol

Drug Info

[96]

114

5,7-diphenyl-3H-imidazo[4,5-b]pyridin-2-ol

Drug Info

[75]

115

6-(furan-2-yl)-9H-purin-2-amine

Drug Info

[93]

116

6-ethylamino-2-(3''-indolyl)ethyloxy)adenosine

Drug Info

[78]

117

6-guanidino-2-(3''-indolylethyloxy)adenosine

Drug Info

[78]

118

7-(3,6,9,12-tetraoxatricos-22-enyl)theophylline

Drug Info

[97]

119

7-Bromo-2-phenyl-[1,8]naphthyridin-4-ol

Drug Info

[98]

120

7-Chloro-2-phenyl-[1,8]naphthyridin-4-ol

Drug Info

[98]

121

7-Dimethylamino-2-phenyl-[1,8]naphthyridin-4-ol

Drug Info

[98]

122

7-Methyl-2-propyl-[1,8]naphthyridin-4-ol

Drug Info

[98]

123

8-Bromo-9-(2,3-dihydroxypropyl)-9H-adenine

Drug Info

[99]

124

8-Bromo-9-(2-butyl)-9H-adenine

Drug Info

[99]

125

8-Bromo-9-(2-hydroxypropyl)-9H-adenine

Drug Info

[99]

126

8-Bromo-9-(3-hydroxypropyl)-9H-adenine

Drug Info

[99]

127

8-Bromo-9-(but-3-enyl)-9H-adenine

Drug Info

[99]

128

8-Bromo-9-(sec-butyl)-9H-adenine

Drug Info

[99]

129

8-Bromo-9-cyclobutyl-9H-adenine

Drug Info

[99]

130

8-Bromo-9-cyclohexyl-9H-adenine

Drug Info

[99]

131

8-Bromo-9-cyclopentyl-9H-adenine

Drug Info

[99]

132

8-Bromo-9-ethyl-9H-adenine

Drug Info

[99]

133

8-bromo-9-isobutyl-9H-purin-6-amine

Drug Info

[82]

134

8-Bromo-9-isopropyl-9H-adenine

Drug Info

[99]

135

8-Bromo-9-methyl-9H-adenine

Drug Info

[99]

136

8-Bromo-9-phenylethyl-9H-adenine

Drug Info

[99]

137

8-Bromo-9-propyl-9H-adenine

Drug Info

[99]

138

8-cyclohexyl-6-(4-tolyl)-2-phenyl-9H-purine

Drug Info

[74]

139

8-PHENYL THEOPHYLLINE

Drug Info

[63]

140

8-Phenyl-1-propyl-3,7-dihydro-purine-2,6-dione

Drug Info

[101]

141

8-Phenyl-3,7-dihydro-purine-2,6-dione

Drug Info

[101]

142

8-propyl-2,6-diphenyl-9H-purine

Drug Info

[74]

143

9-(3-aminobenzyl)-6-(furan-2-yl)-9H-purin-2-amine

Drug Info

[85]

144

9-(3-nitrobenzyl)-6-(furan-2-yl)-9H-purin-2-amine

Drug Info

[85]

145

9-(4-nitrobenzyl)-6-(furan-2-yl)-9H-purin-2-amine

Drug Info

[85]

146

9-Allyl-8-bromo-9H-adenine

Drug Info

[99]

147

9-benzyl-6-(furan-2-yl)-9H-purin-2-amine

Drug Info

[85]

148

9-Benzyl-8-bromo-9H-adenine

Drug Info

[99]

149

9-Cyclobutyl-9H-adenine

Drug Info

[99]

150

9-Cyclopentyl-9H-adenine

Drug Info

[62]

151

9-Ethyl-8-phenylethynyl-9H-purin-6-ylamine

Drug Info

[102]

152

9-Ethyl-9H-adenine

Drug Info

[99]

153

9-Isopropyl-9H-adenine

Drug Info

[99]

154

9-Methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine

Drug Info

[103]

155

9-Methyl-9H-adenine

Drug Info

[59]

156

9-Phenyl-9H-purin-6-ylamine

Drug Info

[62]

157

9-Propyl-9H-adenine

Drug Info

[99]

158

A-987306

Drug Info

[104]

159

Anthoptilide C

Drug Info

[105]

160

Cirsimarin

Drug Info

[108]

161

Cyclohexyl-(2-phenylsulfanyl-9H-purin-6-yl)-amine

Drug Info

[111]

162

Cyclohexyl-(9-ethyl-9H-purin-6-yl)-amine

Drug Info

[62]

163

Cyclohexyl-(9-methyl-9H-purin-6-yl)-amine

Drug Info

[62]

164

Cyclopentyl-(9-cyclopentyl-9H-purin-6-yl)-amine

Drug Info

[62]

165

Cyclopentyl-(9-ethyl-9H-purin-6-yl)-amine

Drug Info

[62]

166

Cyclopentyl-(9-methyl-9H-purin-6-yl)-amine

Drug Info

[62]

167

Cyclopentyl-(9-phenyl-9H-purin-6-yl)-amine

Drug Info

[62]

168

DEPX

Drug Info

[112]

169

Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate

Drug Info

[41]

170

FR-166124

Drug Info

[113]

171

GNF-PF-2224

Drug Info

[115], [116], [117], [118]

172

GNF-PF-2700

Drug Info

[82]

173

Hexanoic Acid (2,6-diphenylpyrimidin-4-yl)amide

Drug Info

[119]

174

Isoguanosine

Drug Info

[122]

175

Kuanoniamine D

Drug Info

[124]

176

L-249313

Drug Info

[45]

177

LUF-5417

Drug Info

[41]

178

LUF-5433

Drug Info

[41]

179

LUF-5735

Drug Info

[119]

180

LUF-5737

Drug Info

[119]

181

LUF-5764

Drug Info

[119]

182

LUF-5767

Drug Info

[119]

183

LUF-5816

Drug Info

[75]

184

LUF-5853

Drug Info

[76]

185

LUF-5956

Drug Info

[74]

186

LUF-5957

Drug Info

[74]

187

LUF-5962

Drug Info

[74]

188

LUF-5978

Drug Info

[75]

189

LUF-5980

Drug Info

[75]

190

LUF-5981

Drug Info

[75]

191

LUF-6258

Drug Info

[126]

192

N*6*-Cyclohexyl-N*2*-ethyl-9H-purine-2,6-diamine

Drug Info

[111]

193

N*6*-Cyclohexyl-N*2*-phenyl-9H-purine-2,6-diamine

Drug Info

[111]

194

N*6*-Cyclooctyl-N*2*-phenyl-9H-purine-2,6-diamine

Drug Info

[111]

195

N-(2,6-diphenylpyrimidin-4-yl)-2-ethylbutyramide

Drug Info

[119]

196

N-(2,6-diphenylpyrimidin-4-yl)-3-methylbutyramide

Drug Info

[119]

197

N-(2,6-diphenylpyrimidin-4-yl)acetamide

Drug Info

[119]

198

N-(2,6-diphenylpyrimidin-4-yl)benzamide

Drug Info

[119]

199

N-(2,6-diphenylpyrimidin-4-yl)butyramide

Drug Info

[119]

200

N-(2,6-diphenylpyrimidin-4-yl)isobutyramide

Drug Info

[119]

201

N-(2,6-diphenylpyrimidin-4-yl)propionamide

Drug Info

[119]

202

N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide

Drug Info

[131]

203

N-(4,5-diphenylpyrimidin-2-yl)acetamide

Drug Info

[119]

204

N-(4,6-diphenylpyrimidin-2-yl)-2-ethylbutyramide

Drug Info

[119]

205

N-(4,6-diphenylpyrimidin-2-yl)-3-chlorobenzamide

Drug Info

[119]

206

N-(4,6-diphenylpyrimidin-2-yl)-3-methylbutyramide

Drug Info

[119]

207

N-(4,6-diphenylpyrimidin-2-yl)benzamide

Drug Info

[119]

208

N-(4,6-diphenylpyrimidin-2-yl)propionamide

Drug Info

[119]

209

N-(4-Phenyl-thiazol-2-yl)-benzamide

Drug Info

[72]

210

N-(5-Benzoyl-4-phenylthiazol-2-yl)benzamide

Drug Info

[41]

211

N6-((+/-)-endo-norborn-2-yl)adenosine

Drug Info

[73]

212

N6-CYCLOPENTYLADENOSINE

Drug Info

[71]

213

N6-methoxy-2-phenylethynyladenosine

Drug Info

[81]

214

N6-methoxy-2-[(2-pyridinyl)ethynyl]adenosine

Drug Info

[81]

215

N6-methoxy-2-[(3-pyridinyl)ethynyl]-adenosine

Drug Info

[81]

216

N6-methoxy-2-[(4-methoxyphenyl)ethynyl]adenosine

Drug Info

[81]

217

N6-methoxy-2-[(4-methylphenyl)ethynyl]adenosine

Drug Info

[81]

218

N6-methoxy-2-[(4-pentylphenyl)ethynyl]adenosine

Drug Info

[81]

219

N6-methoxy-2-[(4-pyridinyl)ethynyl]adenosine

Drug Info

[81]

220

N6-methoxy-2-[2-(trimethylsilyl)ethynyl]adenosine

Drug Info

[81]

221

N6-[(4-Amino)-phenyl]-9-benzyl-2-phenyladenine

Drug Info

[132]

222

N6-[(4-Nitro)-phenyl]-9-benzyl-2-phenyladenine

Drug Info

[132]

223

P-IODOAMPHETAMINE

Drug Info

[133]

224

PD-115199

Drug Info

[134]

225

PD-81723

Drug Info

[135]

226

Pentanoic acid (4,6-diphenylpyrimidin-2-yl)amide

Drug Info

[119]

227

Phenyl(2-(trifluoromethyl)quinolin-4-yl)methanol

Drug Info

[136]

228

Phenyl-(9-phenyl-9H-purin-6-yl)-amine

Drug Info

[62]

229

PSB-0788

Drug Info

[137]

230

PSB-1115

Drug Info

[137]

231

PSB-601

Drug Info

[137]

232

R-N6-(phenylisopropyl)adenosine

Drug Info

[140], [78]

233

SB-298

Drug Info

[137]

234

SCH-63390

Drug Info

[141]

235

ST-1535

Drug Info

[103]

236

VCP-28

Drug Info

[143]

237

VUF-8507

Drug Info

[144]

238

[3H]NECA

Drug Info

[149]

239

[3H]OSIP339391

Drug Info

[82]

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

cGMP-PKG signaling pathway

cAMP signaling pathway

Sphingolipid signaling pathway

Neuroactive ligand-receptor interaction

Morphine addiction

NetPath Pathway

[+] 2 NetPath Pathways

TCR Signaling Pathway

RANKL Signaling Pathway

Panther Pathway

[+] 2 Panther Pathways

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

Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway

Reactome

[+] 2 Reactome Pathways

Adenosine P1 receptors

G alpha (i) signalling events

WikiPathways

[+] 4 WikiPathways

Nucleotide GPCRs

GPCRs, Class A Rhodopsin-like

GPCR ligand binding

GPCR downstream signaling

Target-Related Models and Studies

Top

Target Validation

Target Validation Info

Target QSAR Model

References

Top

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2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists. J Med Chem. 2004 Dec 16;47(26):6529-40.

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