Target Information

Target General Information

Top

Target ID

T36059 (Former ID: TTDS00189)

Target Name

Adenosine A3 receptor (ADORA3)

Synonyms

Adenosine receptor A3A; Adenosine receptor A3; Adenosine 3 receptor; A3AR; A3 Adenosine receptor

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Gene Name

ADORA3

Target Type

Clinical trial target

[1]

Disease

[+] 2 Target-related Diseases

Psoriasis [ICD-11: EA90]

Solid tumour/cancer [ICD-11: 2A00-2F9Z]

Function

The activity of this receptor is mediated by G proteins which inhibits adenylyl cyclase. Isoform 2: Receptor for adenosine.

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BioChemical Class

GPCR rhodopsin

UniProt ID

AA3R_HUMAN

Sequence

MPNNSTALSLANVTYITMEIFIGLCAIVGNVLVICVVKLNPSLQTTTFYFIVSLALADIA
VGVLVMPLAIVVSLGITIHFYSCLFMTCLLLIFTHASIMSLLAIAVDRYLRVKLTVRYKR
VTTHRRIWLALGLCWLVSFLVGLTPMFGWNMKLTSEYHRNVTFLSCQFVSVMRMDYMVYF
SFLTWIFIPLVVMCAIYLDIFYIIRNKLSLNLSNSKETGAFYGREFKTAKSLFLVLFLFA
LSWLPLSIINCIIYFNGEVPQLVLYMGILLSHANSMMNPIVYAYKIKKFKETYLLILKAC
VVCHPSDSLDTSIEKNSE

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3D Structure

Click to Show 3D Structure of This Target

AlphaFold

HIT2.0 ID

T62FNY

Drugs and Modes of Action

Top

Clinical Trial Drug(s)

[+] 4 Clinical Trial Drugs

IB-MECA

Drug Info

Phase 3

Solid tumour/cancer

[2], [3], [4]

CF102

Drug Info

Phase 2

Hepatocellular carcinoma

[5]

NITD609

Drug Info

Phase 2

Malaria

[6]

Tonapofylline

Drug Info

Phase 2

Acute and chronic heart failure

[7]

Preclinical Drug(s)

[+] 3 Preclinical Drugs

BAY 60-6583

Drug Info

Preclinical

Myocardial ischemia

[8]

CF502

Drug Info

Preclinical

Inflammation

[9], [10]

CF602

Drug Info

Preclinical

Inflammation

[10]

Discontinued Drug(s)

[+] 2 Discontinued Drugs

DIZOCILPINE

Drug Info

Terminated

Cerebrovascular ischaemia

[11], [12]

METHYLTHIOADENOSINE

Drug Info

Terminated

Multiple sclerosis

[13]

Mode of Action

[+] 4 Modes of Action

Agonist

[+] 24 Agonist drugs

IB-MECA

Drug Info

[1], [14]

CF102

Drug Info

[10]

BAY 60-6583

Drug Info

[19]

CF502

Drug Info

[10]

CF602

Drug Info

[10]

(R,S)-PHPNECA

Drug Info

[24]

(S)-PIA

Drug Info

[25]

2'-Me-CCPA

Drug Info

[30]

2-chloroadenosine

Drug Info

[23]

2-phenylethylyl-adenosine derivative

Drug Info

[44]

AB-MECA

Drug Info

[25]

CP608,039

Drug Info

[58]

I-ABA

Drug Info

[62]

MPC-MECA

Drug Info

[25]

MRE 3008F20

Drug Info

[25], [66]

MRS5151

Drug Info

[72]

MRS5698

Drug Info

[73]

N(6)-cyclohexyladenosine

Drug Info

[74]

PENECA

Drug Info

[24]

TCPA

Drug Info

[83]

[125I]AB-MECA

Drug Info

[25]

[125I]APNEA

Drug Info

[86]

[3H]HEMADO

Drug Info

[87]

[3H]NECA

Drug Info

[88], [89]

Inhibitor

[+] 164 Inhibitor drugs

NITD609

Drug Info

[15]

Tonapofylline

Drug Info

[16]

SCH-442416

Drug Info

[17]

BEMESETRON

Drug Info

[18]

DIZOCILPINE

Drug Info

[18]

METHYLTHIOADENOSINE

Drug Info

[20]

METRIFUDIL

Drug Info

[21]

(+)-BUTACLAMOL

Drug Info

[18]

(2R,3S)-3-(6-Amino-purin-9-yl)-nonan-2-ol

Drug Info

[22]

1,2-dihydro-2-oxoquinazoline-4-carboxyanilide

Drug Info

[26]

1-(2-(diethylamino)quinazolin-4-yl)-3-phenylurea

Drug Info

[27]

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

Drug Info

[28]

1-Benzyl-1H-1,3,4b,9-tetraaza-fluorene-2,4-dione

Drug Info

[29]

1-Benzyl-3-methyl-3,7-dihydro-purine-2,6-dione

Drug Info

[28]

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

Drug Info

[28]

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

Drug Info

[28]

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

Drug Info

[28]

1-phenyl-3-(2-(pyridin-2-yl)quinazolin-4-yl)urea

Drug Info

[27]

1-phenyl-3-(2-(pyridin-3-yl)quinazolin-4-yl)urea

Drug Info

[27]

1-phenyl-3-(3-(pyridin-2-yl)isoquinolin-1-yl)urea

Drug Info

[27]

1-phenyl-3-(quinazolin-4-yl)urea

Drug Info

[27]

1-Prop-2-ynyl-3,7-dihydro-purine-2,6-dione

Drug Info

[28]

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

Drug Info

[28]

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

Drug Info

[31]

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

Drug Info

[32]

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

Drug Info

[32]

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

Drug Info

[32]

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

Drug Info

[32]

2,6-diphenyl-1-deazapurine

Drug Info

[33]

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

Drug Info

[33]

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

Drug Info

[33]

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

Drug Info

[33]

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

Drug Info

[33]

2,6-diphenyl-9H-purine

Drug Info

[32]

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

Drug Info

[33]

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

Drug Info

[34]

2-(1H-imidazo[4,5-c]pyridin-2-yl)quinoxaline

Drug Info

[35]

2-(2''-indolylethyloxy)adenosine

Drug Info

[36]

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

Drug Info

[36]

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

Drug Info

[36]

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

Drug Info

[36]

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

Drug Info

[36]

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

Drug Info

[36]

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

Drug Info

[36]

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

Drug Info

[36]

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

Drug Info

[36]

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

Drug Info

[36]

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

Drug Info

[36]

2-(3''-(benzoimidazole-1''-yl)ethyloxy)adenosine

Drug Info

[36]

2-(3''-(benzotriazole-1''-yl)ethyloxy)adenosine

Drug Info

[36]

2-(3''-indolylethyloxy)adenosine

Drug Info

[36]

2-(3''-pyrrolylethyloxy)adenosine

Drug Info

[36]

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

Drug Info

[35]

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

Drug Info

[32]

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

Drug Info

[35]

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

Drug Info

[37]

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

Drug Info

[32]

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

Drug Info

[34]

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

Drug Info

[35]

2-(5-chloro-1H-benzo[d]imidazol-2-yl)quinoxaline

Drug Info

[35]

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

Drug Info

[37]

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

Drug Info

[37]

2-acetylaminoquinazoline-4-carboxyanilide

Drug Info

[26]

2-aminoquinazoline-4-carboxy-(4-bromophenyl)amide

Drug Info

[26]

2-aminoquinazoline-4-carboxyanilide

Drug Info

[26]

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

Drug Info

[38]

2-benzoylaminoquinazoline-4-carboxyanilide

Drug Info

[26]

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

Drug Info

[39]

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

Drug Info

[40]

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

Drug Info

[41]

2-ethynyl-N6-methoxyadenosine

Drug Info

[37]

2-Phenyl-2H-pyrazolo[4,3-c]quinoline

Drug Info

[42]

2-phenyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one

Drug Info

[43]

2-phenylpropoxyadenosine

Drug Info

[36]

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

Drug Info

[32]

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

Drug Info

[37]

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

Drug Info

[37]

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

Drug Info

[34]

3-Methyl-1-phenethyl-3,7-dihydro-purine-2,6-dione

Drug Info

[28]

3-noradamantyl-1,3-dipropylxanthine

Drug Info

[45]

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

Drug Info

[46]

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

Drug Info

[47]

4-Methoxy-2-phenyl-2H-pyrazolo[4,3-c]quinoline

Drug Info

[42]

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

Drug Info

[48]

5,6,7-Trimethyl-2-p-tolyl-chromen-4-one

Drug Info

[49]

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

Drug Info

[50]

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

Drug Info

[33]

5-Butyl-8-phenyl-3H-[1,2,4]triazolo[5,1-i]purine

Drug Info

[51]

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

Drug Info

[36]

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

Drug Info

[36]

6-Hydroxy-5,7-dimethyl-beta-carboline

Drug Info

[50]

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

Drug Info

[52]

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

Drug Info

[52]

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

Drug Info

[52]

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

Drug Info

[52]

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

Drug Info

[52]

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

Drug Info

[53]

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

Drug Info

[52]

8-Hydroxy-5,7,9-trimethyl-delta-carboline

Drug Info

[50]

100

8-Hydroxy-7,9-dimethyl-delta-carboline

Drug Info

[50]

101

8-PHENYL THEOPHYLLINE

Drug Info

[54]

102

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

Drug Info

[32]

103

9-Cyclopentyl-9H-adenine

Drug Info

[52]

104

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

Drug Info

[55]

105

9H-purine derivative

Drug Info

[18]

106

CIRSIMARITIN

Drug Info

[49]

107

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

Drug Info

[59]

108

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

Drug Info

[59]

109

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

Drug Info

[16]

110

Galangin

Drug Info

[49]

111

GNF-PF-2224

Drug Info

[60]

112

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

Drug Info

[61]

113

isobutylmethylxanthine

Drug Info

[54]

114

L-249313

Drug Info

[64]

115

LUF-5417

Drug Info

[16]

116

LUF-5433

Drug Info

[16]

117

LUF-5767

Drug Info

[61]

118

LUF-5816

Drug Info

[33]

119

LUF-5956

Drug Info

[32]

120

LUF-5957

Drug Info

[32]

121

LUF-5962

Drug Info

[32]

122

LUF-5978

Drug Info

[33]

123

LUF-5980

Drug Info

[33]

124

LUF-5981

Drug Info

[33]

125

MESULERGINE

Drug Info

[18]

126

METHOCTRAMINE

Drug Info

[18]

127

N*2*-Benzyl-N*6*-cyclohexyl-9H-purine-2,6-diamine

Drug Info

[59]

128

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

Drug Info

[59]

129

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

Drug Info

[59]

130

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

Drug Info

[59]

131

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

Drug Info

[61]

132

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

Drug Info

[61]

133

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

Drug Info

[61]

134

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

Drug Info

[61]

135

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

Drug Info

[61]

136

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

Drug Info

[61]

137

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

Drug Info

[75]

138

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

Drug Info

[61]

139

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

Drug Info

[61]

140

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

Drug Info

[61]

141

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

Drug Info

[16]

142

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

Drug Info

[31]

143

N6-(3-Iodobenzyl)-2'-O-methyladenosine

Drug Info

[76]

144

N6-CYCLOPENTYLADENOSINE

Drug Info

[77]

145

N6-methoxy-2-phenylethynyladenosine

Drug Info

[37]

146

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

Drug Info

[37]

147

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

Drug Info

[37]

148

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

Drug Info

[37]

149

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

Drug Info

[37]

150

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

Drug Info

[37]

151

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

Drug Info

[37]

152

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

Drug Info

[37]

153

NIPECOTIC ACID

Drug Info

[18]

154

NSC-407228

Drug Info

[49]

155

R-N6-(phenylisopropyl)adenosine

Drug Info

[36], [82]

156

REVERSINE

Drug Info

[59]

157

SB-298

Drug Info

[81]

158

SEROTONIN

Drug Info

[18]

159

VUF-8504

Drug Info

[27]

160

VUF-8507

Drug Info

[27]

161

[1,2,4]triazolo[1,5-a]quinoxalin-4(5H)-one

Drug Info

[85]

162

[3H]CCPA

Drug Info

[40]

163

[3H]kainate

Drug Info

[18]

164

[3H]OSIP339391

Drug Info

[53]

Antagonist

[+] 32 Antagonist drugs

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

Drug Info

[23]

ACN-1052

Drug Info

[56]

ATL802

Drug Info

[57]

flavone

Drug Info

[47], [49]

I-ABOPX

Drug Info

[62]

KF26777

Drug Info

[63]

MRE 2029F20

Drug Info

[65]

MRE 3010F20

Drug Info

[25]

MRS-1220

Drug Info

[67]

MRS1041

Drug Info

[47]

MRS1042

Drug Info

[47]

MRS1067

Drug Info

[68]

MRS1088

Drug Info

[47]

MRS1093

Drug Info

[47]

MRS1097

Drug Info

[69]

MRS1177

Drug Info

[70]

MRS1186

Drug Info

[70]

MRS1191

Drug Info

[56]

MRS1476

Drug Info

[71]

MRS1486

Drug Info

[71]

MRS1505

Drug Info

[71]

MRS1523

Drug Info

[71]

MRS928

Drug Info

[47], [49]

PSB-10

Drug Info

[78]

PSB-11

Drug Info

[79]

PSB36

Drug Info

[80]

PSB603

Drug Info

[81]

sakuranetin

Drug Info

[47]

visnagin

Drug Info

[47]

VUF5574

Drug Info

[84]

xanthine amine congener

Drug Info

[25]

[3H]PSB-11

Drug Info

[79]

Enhancer

[+] 1 Enhancer drugs

LUF-5833

Drug Info

[56]

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). Human Similarity Proteins Human Pathway Affiliation

Different Human System Profiles of Target

Top

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

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

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

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

Human Similarity Proteins

Human Pathway Affiliation

Protein Name	Pfam ID	Percentage of Identity (%)	E value
Olfactory receptor 13J1 (OR13J1)	PF13853	25.623 (72/281)	1.79E-11
Olfactory receptor 2A14 (OR2A14)	PF13853	23.273 (64/275)	4.95E-10
Olfactory receptor 5V1 (OR5V1)	PF13853	24.460 (68/278)	3.69E-09
Olfactory receptor 2T3 (OR2T3)	PF13853	25.000 (72/288)	4.22E-09
Olfactory receptor 2T10 (OR2T10)	PF13853	25.540 (71/278)	5.16E-09
Olfactory receptor 2T34 (OR2T34)	PF13853	26.360 (63/239)	7.57E-09
Olfactory receptor 51I2 (OR51I2)	PF13853	23.264 (67/288)	1.40E-08
Olfactory receptor 6C1 (OR6C1)	PF13853	22.300 (64/287)	5.59E-08
Olfactory receptor 51E1 (OR51E1)	PF13853	25.249 (76/301)	1.04E-07
Olfactory receptor 1N2 (OR1N2)	PF13853	29.268 (36/123)	1.05E-07
Olfactory receptor 8J2 (OR8J2)	PF13853	30.000 (36/120)	1.42E-07
Olfactory receptor 51I1 (OR51I1)	PF13853	32.787 (40/122)	1.72E-07
Olfactory receptor 10A6 (OR10A6)	PF13853	23.944 (34/142)	1.82E-07
Olfactory receptor 51H1 (OR51H1)	PF13853	27.632 (42/152)	3.46E-07
Olfactory receptor 51E2 (OR51E2)	PF13853	26.148 (74/283)	5.62E-07
Olfactory receptor 52M1 (OR52M1)	PF13853	26.441 (78/295)	5.93E-07
Olfactory receptor 51F2 (OR51F2)	PF13853	23.611 (68/288)	7.94E-07
Olfactory receptor 8A1 (OR8A1)	PF13853	23.381 (65/278)	9.50E-07
Olfactory receptor 52E4 (OR52E4)	PF13853	22.997 (66/287)	9.76E-07
Olfactory receptor 2A12 (OR2A12)	PF13853	22.628 (62/274)	1.11E-06
Olfactory receptor 13H1 (OR13H1)	PF13853	24.540 (40/163)	1.38E-06
Olfactory receptor 2T5 (OR2T5)	PF13853	23.827 (66/277)	1.65E-06
Olfactory receptor 2T29 (OR2T29)	PF13853	23.827 (66/277)	1.67E-06
Olfactory receptor 1B1 (OR1B1)	PF13853	28.333 (51/180)	1.91E-06
Olfactory receptor 51B5 (OR51B5)	PF13853	23.906 (71/297)	2.18E-06
Olfactory receptor 51S1 (OR51S1)	PF13853	23.958 (69/288)	2.20E-06
Olfactory receptor 52R1 (OR52R1)	PF13853	23.469 (69/294)	2.31E-06
Olfactory receptor 52E8 (OR52E8)	PF13853	26.923 (42/156)	2.52E-06
Olfactory receptor 1L1 (OR1L1)	PF13853	29.245 (31/106)	2.74E-06
Olfactory receptor 7G1 (OR7G1)	PF13853	23.567 (74/314)	3.15E-06
Putative olfactory receptor 14L1 (OR14L1P)	PF13853	21.300 (59/277)	4.05E-06
Olfactory receptor 52D1 (OR52D1)	PF13853	29.221 (45/154)	4.07E-06
Olfactory receptor 10G7 (OR10G7)	PF13853	25.664 (29/113)	4.86E-06
Olfactory receptor 2T4 (OR2T4)	PF13853	21.864 (61/279)	4.87E-06
Olfactory receptor 4M1 (OR4M1)	PF13853	30.172 (35/116)	4.93E-06
Olfactory receptor 52Z1P (OR52Z1P)	PF13853	26.263 (78/297)	4.95E-06
Olfactory receptor 2H1 (OR2H1)	PF13853	21.786 (61/280)	5.55E-06
Olfactory receptor 5AS1 (OR5AS1)	PF13853	30.693 (31/101)	5.73E-06
Olfactory receptor 1D2 (OR1D2)	PF13853	25.490 (39/153)	5.73E-06
Olfactory receptor 4S1 (OR4S1)	PF13853	27.586 (32/116)	6.00E-06
Olfactory receptor 2A1/2A42 (OR2A1; OR2A42)	PF13853	29.703 (30/101)	6.24E-06
Olfactory receptor 51B2 (OR51B2)	PF13853	22.064 (62/281)	6.62E-06
Olfactory receptor 52A5 (OR52A5)	PF13853	29.630 (32/108)	7.02E-06
Olfactory receptor 10G8 (OR10G8)	PF13853	25.664 (29/113)	7.10E-06
Olfactory receptor 6C3 (OR6C3)	PF13853	20.423 (58/284)	7.49E-06
Olfactory receptor 51A7 (OR51A7)	PF13853	22.968 (65/283)	7.65E-06
Olfactory receptor 52J3 (OR52J3)	PF13853	22.759 (66/290)	7.98E-06
Olfactory receptor 52E5 (OR52E5)	PF13853	28.800 (36/125)	9.57E-06
Olfactory receptor 14A16 (OR14A16)	PF13853	30.894 (38/123)	9.76E-06
Olfactory receptor 1L8 (OR1L8)	PF13853	30.556 (33/108)	1.03E-05
Olfactory receptor 51V1 (OR51V1)	PF13853	32.432 (36/111)	1.11E-05
Olfactory receptor 52A1 (OR52A1)	PF13853	30.435 (42/138)	1.11E-05
Olfactory receptor 8K5 (OR8K5)	PF13853	29.412 (35/119)	1.14E-05
Olfactory receptor 1N1 (OR1N1)	PF13853	22.261 (63/283)	1.19E-05
Olfactory receptor 4C16 (OR4C16)	PF13853	26.119 (35/134)	1.59E-05
Olfactory receptor 2A25 (OR2A25)	PF13853	27.273 (27/99)	1.65E-05
Olfactory receptor 4C15 (OR4C15)	PF13853	25.210 (30/119)	1.74E-05
Olfactory receptor 6S1 (OR6S1)	PF13853	26.797 (41/153)	1.76E-05
Olfactory receptor 6N2 (OR6N2)	PF13853	26.667 (32/120)	1.86E-05
Olfactory receptor 2D3 (OR2D3)	PF13853	21.019 (66/314)	1.89E-05
Olfactory receptor 1J1 (OR1J1)	PF13853	21.951 (27/123)	2.01E-05
Olfactory receptor 4A15 (OR4A15)	PF13853	28.346 (36/127)	2.06E-05
Olfactory receptor 4K2 (OR4K2)	PF13853	27.451 (28/102)	2.07E-05
Olfactory receptor 2H2 (OR2H2)	PF13853	20.415 (59/289)	2.12E-05
Olfactory receptor 1P1 (OR1P1)	PF13853	25.203 (31/123)	2.18E-05
Olfactory receptor 10G4 (OR10G4)	PF13853	18.900 (55/291)	2.21E-05
Olfactory receptor 2F1 (OR2F1)	PF13853	24.000 (36/150)	3.08E-05
Olfactory receptor 6M1 (OR6M1)	PF13853	26.050 (31/119)	3.36E-05
Olfactory receptor 4K15 (OR4K15)	PF13853	26.891 (32/119)	3.62E-05
Olfactory receptor 52B2 (OR52B2)	PF13853	25.442 (72/283)	3.91E-05
Olfactory receptor 2A2 (OR2A2)	PF13853	21.168 (58/274)	4.00E-05
Olfactory receptor 4C11 (OR4C11)	PF13853	26.724 (31/116)	4.17E-05
Olfactory receptor 10C1 (OR10C1)	PF13853	26.812 (37/138)	4.43E-05
Olfactory receptor 5D13 (OR5D13)	PF13853	28.704 (31/108)	4.62E-05
Olfactory receptor 14A2 (OR14A2)	PF13853	26.154 (34/130)	5.05E-05
Olfactory receptor 13A1 (OR13A1)	PF13853	28.571 (28/98)	5.99E-05
Olfactory receptor 1L6 (OR1L6)	PF13853	28.947 (33/114)	7.01E-05
Olfactory receptor 4E2 (OR4E2)	PF13853	28.800 (36/125)	7.21E-05
Olfactory receptor 4C13 (OR4C13)	PF13853	26.496 (31/117)	7.26E-05
Olfactory receptor 2D2 (OR2D2)	PF13853	22.794 (62/272)	7.31E-05
Olfactory receptor 4K1 (OR4K1)	PF13853	24.576 (29/118)	7.78E-05
Olfactory receptor 10A2 (OR10A2)	PF13853	22.183 (63/284)	7.88E-05
Olfactory receptor 51F1 (OR51F1)	PF13853	24.476 (70/286)	8.23E-05
Olfactory receptor 10G9 (OR10G9)	PF13853	23.894 (27/113)	8.51E-05
Olfactory receptor 52A4 (OR52A4P)	PF13853	30.392 (31/102)	8.57E-05
Olfactory receptor 10AG1 (OR10AG1)	PF13853	24.490 (24/98)	8.89E-05
Olfactory receptor 9A4 (OR9A4)	PF13853	24.615 (32/130)	8.97E-05
Olfactory receptor 4N5 (OR4N5)	PF13853	26.316 (30/114)	8.98E-05
Olfactory receptor 1E2 (OR1E2)	PF13853	24.000 (30/125)	9.68E-05
Olfactory receptor 9A2 (OR9A2)	PF13853	21.141 (63/298)	9.88E-05
Olfactory receptor 14I1 (OR14I1)	PF13853	25.385 (33/130)	1.06E-04
Olfactory receptor 7G2 (OR7G2)	PF13853	27.885 (29/104)	1.19E-04
Olfactory receptor 6C4 (OR6C4)	PF13853	23.701 (73/308)	1.33E-04
Olfactory receptor 2T6 (OR2T6)	PF13853	24.348 (56/230)	1.35E-04
Olfactory receptor 4Q3 (OR4Q3)	PF13853	31.092 (37/119)	1.36E-04
Olfactory receptor 10A4 (OR10A4)	PF13853	25.203 (31/123)	1.41E-04
Olfactory receptor 2F2 (OR2F2)	PF13853	23.529 (36/153)	1.44E-04
Olfactory receptor 4K5 (OR4K5)	PF13853	24.590 (30/122)	1.50E-04
Olfactory receptor 10P1 (OR10P1)	PF13853	20.567 (58/282)	1.52E-04
Olfactory receptor 5I1 (OR5I1)	PF13853	26.804 (26/97)	1.76E-04
Olfactory receptor 10A5 (OR10A5)	PF13853	24.390 (30/123)	1.80E-04
Olfactory receptor 4D5 (OR4D5)	PF13853	25.000 (29/116)	1.81E-04
Olfactory receptor 52I1 (OR52I1)	PF13853	24.342 (37/152)	1.92E-04
Putative olfactory receptor 2B3 (OR2B3)	PF13853	20.783 (69/332)	1.92E-04
Olfactory receptor 1L3 (OR1L3)	PF13853	28.302 (30/106)	1.95E-04
Olfactory receptor 11H4 (OR11H4)	PF13853	26.016 (32/123)	1.95E-04
Putative olfactory receptor 56B2 (OR56B2P)	PF13853	23.420 (63/269)	2.01E-04
Olfactory receptor 2B2 (OR2B2)	PF13853	18.531 (53/286)	2.09E-04
Olfactory receptor 1E1 (OR1E1)	PF13853	23.077 (27/117)	2.14E-04
Olfactory receptor 6C2 (OR6C2)	PF13853	17.958 (51/284)	2.19E-04
Olfactory receptor 2T27 (OR2T27)	PF13853	19.149 (54/282)	2.26E-04
Olfactory receptor 5M9 (OR5M9)	PF13853	27.907 (24/86)	2.45E-04
Olfactory receptor 51G2 (OR51G2)	PF13853	22.887 (65/284)	2.83E-04
Olfactory receptor 7E24 (OR7E24)	PF13853	26.050 (31/119)	2.86E-04
Olfactory receptor 4L1 (OR4L1)	PF13853	21.094 (27/128)	2.97E-04
Olfactory receptor 11H7 (OR11H7)	PF13853	22.901 (30/131)	3.01E-04
Olfactory receptor 5M3 (OR5M3)	PF13853	28.409 (25/88)	3.01E-04
Putative olfactory receptor 52L2 (OR52L2P)	PF13853	34.043 (32/94)	3.02E-04
Putative olfactory receptor 8G2 (OR8G2P)	PF13853	27.273 (30/110)	3.51E-04
Olfactory receptor 7G3 (OR7G3)	PF13853	27.869 (34/122)	3.65E-04
Olfactory receptor 52B6 (OR52B6)	PF13853	33.333 (35/105)	3.67E-04
Olfactory receptor 52E2 (OR52E2)	PF13853	25.843 (46/178)	3.83E-04
Olfactory receptor 2T2 (OR2T2)	PF13853	23.129 (68/294)	3.89E-04
Olfactory receptor 1I1 (OR1I1)	PF13853	26.230 (32/122)	3.91E-04
Olfactory receptor 1J2 (OR1J2)	PF13853	22.222 (28/126)	3.93E-04
Olfactory receptor 2V2 (OR2V2)	PF13853	26.016 (32/123)	4.28E-04
Olfactory receptor 1C1 (OR1C1)	PF13853	26.027 (38/146)	4.30E-04
Olfactory receptor 4M2 (OR4M2B)	PF13853	28.448 (33/116)	4.33E-04
Olfactory receptor 2A5 (OR2A5)	PF13853	26.804 (26/97)	4.63E-04
Olfactory receptor 14J1 (OR14J1)	PF13853	23.770 (29/122)	4.78E-04
Olfactory receptor 11L1 (OR11L1)	PF13853	21.603 (62/287)	4.97E-04
Olfactory receptor 6C70 (OR6C70)	PF13853	21.538 (28/130)	5.26E-04
Olfactory receptor 7A17 (OR7A17)	PF13853	21.429 (60/280)	5.27E-04
Olfactory receptor 10J1 (OR10J1)	PF13853	22.293 (35/157)	5.31E-04
Olfactory receptor 8B4 (OR8B4)	PF13853	26.154 (34/130)	5.77E-04
Olfactory receptor 4C6 (OR4C6)	PF13853	25.862 (30/116)	6.36E-04
Olfactory receptor 1M1 (OR1M1)	PF13853	24.793 (30/121)	6.54E-04
Olfactory receptor 8U3 (OR8U3)	PF13853	26.613 (33/124)	6.95E-04
Olfactory receptor 2C1 (OR2C1)	PF13853	21.834 (50/229)	7.07E-04
Olfactory receptor 52P1 (OR52P1)	PF13853	30.769 (32/104)	7.35E-04
Olfactory receptor 6Q1 (OR6Q1)	PF13853	25.899 (36/139)	7.48E-04
Olfactory receptor 10A7 (OR10A7)	PF13853	23.026 (70/304)	8.23E-04
Olfactory receptor 1L4 (OR1L4)	PF13853	30.120 (25/83)	8.67E-04
Olfactory receptor 4A5 (OR4A5)	PF13853	26.549 (30/113)	1.00E-03
Olfactory receptor 8J1 (OR8J1)	PF13853	26.087 (30/115)	1.00E-03
Olfactory receptor 2B6 (OR2B6)	PF13853	20.714 (58/280)	1.00E-03
Olfactory receptor 5B17 (OR5B17)	PF13853	23.292 (75/322)	1.00E-03
Olfactory receptor 51M1 (OR51M1)	PF13853	21.453 (62/289)	1.00E-03
Putative olfactory receptor 8G3 pseudogene (OR8G3P)	PF13853	27.586 (32/116)	1.00E-03
Olfactory receptor 1F1 (OR1F1)	PF13853	26.496 (31/117)	1.00E-03
Olfactory receptor 6K2 (OR6K2)	PF13853	26.144 (40/153)	1.00E-03
Olfactory receptor 5AL1 (OR5AL1)	PF13853	28.571 (26/91)	1.00E-03
Olfactory receptor 8B3 (OR8B3)	PF13853	22.022 (61/277)	1.00E-03
Olfactory receptor 51G1 (OR51G1)	PF13853	23.158 (66/285)	1.00E-03
Olfactory receptor 52N4 (OR52N4)	PF13853	22.635 (67/296)	1.00E-03
Olfactory receptor 52N2 (OR52N2)	PF13853	21.071 (59/280)	1.00E-03
Olfactory receptor 4B1 (OR4B1)	PF13853	25.424 (30/118)	1.00E-03
Olfactory receptor 2T7 (OR2T7)	PF13853	18.571 (52/280)	1.00E-03
Olfactory receptor 5M11 (OR5M11)	PF13853	26.364 (29/110)	1.00E-03
Olfactory receptor 8D2 (OR8D2)	PF13853	26.724 (31/116)	2.00E-03
Olfactory receptor 5D14 (OR5D14)	PF13853	20.861 (63/302)	2.00E-03
Olfactory receptor 2T1 (OR2T1)	PF13853	22.022 (61/277)	2.00E-03
Olfactory receptor 6N1 (OR6N1)	PF13853	29.204 (33/113)	2.00E-03
Olfactory receptor 2AG2 (OR2AG2)	PF13853	21.466 (41/191)	2.00E-03
Olfactory receptor 52N5 (OR52N5)	PF13853	23.759 (67/282)	2.00E-03
Olfactory receptor 8D1 (OR8D1)	PF13853	27.500 (33/120)	2.00E-03
Olfactory receptor 4N2 (OR4N2)	PF13853	25.439 (29/114)	2.00E-03
Olfactory receptor 51A4 (OR51A4)	PF13853	24.014 (67/279)	2.00E-03
Olfactory receptor 8J3 (OR8J3)	PF13853	25.217 (29/115)	2.00E-03
Olfactory receptor 2V1 (OR2V1)	PF13853	23.841 (36/151)	2.00E-03
Olfactory receptor 1J4 (OR1J4)	PF13853	26.829 (33/123)	2.00E-03
Olfactory receptor 52L1 (OR52L1)	PF13853	31.915 (30/94)	3.00E-03
Olfactory receptor 4C3 (OR4C3)	PF13853	23.478 (27/115)	3.00E-03
Olfactory receptor 10H1 (OR10H1)	PF13853	25.833 (31/120)	3.00E-03
Olfactory receptor 52K2 (OR52K2)	PF13853	28.000 (28/100)	3.00E-03
Olfactory receptor 4D10 (OR4D10)	PF13853	24.561 (28/114)	3.00E-03
Olfactory receptor 2G3 (OR2G3)	PF13853	26.050 (31/119)	3.00E-03
Olfactory receptor 6C68 (OR6C68)	PF13853	19.081 (54/283)	3.00E-03
Olfactory receptor 51L1 (OR51L1)	PF13853	29.032 (45/155)	3.00E-03
Olfactory receptor 13F1 (OR13F1)	PF13853	22.059 (60/272)	3.00E-03
Olfactory receptor 5D16 (OR5D16)	PF13853	32.787 (20/61)	3.00E-03
Olfactory receptor 9Q1 (OR9Q1)	PF13853	21.875 (63/288)	3.00E-03
Olfactory receptor 4K3 (OR4K3)	PF13853	20.492 (25/122)	4.00E-03
Olfactory receptor 5M8 (OR5M8)	PF13853	26.531 (26/98)	4.00E-03
Olfactory receptor 4K17 (OR4K17)	PF13853	21.533 (59/274)	4.00E-03
Olfactory receptor 8K3 (OR8K3)	PF13853	26.016 (32/123)	4.00E-03
Olfactory receptor 52K1 (OR52K1)	PF13853	21.300 (59/277)	4.00E-03
Olfactory receptor 52I2 (OR52I2)	PF13853	25.490 (26/102)	4.00E-03
Olfactory receptor 9Q2 (OR9Q2)	PF13853	20.727 (57/275)	4.00E-03
Olfactory receptor 4D2 (OR4D2)	PF13853	24.138 (28/116)	4.00E-03
Olfactory receptor 5M1 (OR5M1)	PF13853	27.344 (35/128)	5.00E-03
Translation factor GUF1, mitochondrial (GUF1)	PF00679 ; PF00009 ; PF03144 ; PF06421 More >>	44.898 (22/49)	5.00E-03
Olfactory receptor 2B11 (OR2B11)	PF13853	23.810 (35/147)	5.00E-03
Olfactory receptor 5M10 (OR5M10)	PF13853	28.571 (36/126)	5.00E-03
Olfactory receptor 4K13 (OR4K13)	PF13853	24.074 (26/108)	5.00E-03
Click to Show/Hide the Information of Human Similarity Proteins

KEGG Pathway	Pathway ID	Affiliated Target
cGMP-PKG signaling pathway	hsa04022	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
Sphingolipid signaling pathway	hsa04071	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

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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Reactome

[+] 2 Reactome Pathways

Adenosine P1 receptors

G alpha (i) signalling events

WikiPathways

[+] 3 WikiPathways

Nucleotide GPCRs

GPCRs, Class A Rhodopsin-like

GPCRs, Other

Target-Related Models and Studies

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Target Validation

Target Validation Info

Target QSAR Model

References

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REF 1

A role for central A3-adenosine receptors. Mediation of behavioral depressant effects. FEBS Lett. 1993 Dec 20;336(1):57-60.

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: 422).

REF 3

Methotrexate enhances the anti-inflammatory effect of CF101 via up-regulation of the A3 adenosine receptor expression. Arthritis Res Ther. 2006;8(6):R169.

REF 4

CF101, an agonist to the A3 adenosine receptor, enhances the chemotherapeutic effect of 5-fluorouracil in a colon carcinoma murine model. Neoplasia. 2005 Jan;7(1):85-90.

REF 5

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

REF 6

ClinicalTrials.gov (NCT01836458) A Study to Find the Minimum Inhibitory Concentration of KAE609 in Adult Male Patients With P. Falciparum Monoinfection. U.S. National Institutes of Health.

REF 7

Emerging drugs for acute and chronic heart failure: current and future developments. Expert Opin Emerg Drugs. 2007 Mar;12(1):75-95.

REF 8

Circadian rhythm as a therapeutic target. Nat Rev Drug Discov. 2021 Apr;20(4):287-307.

REF 9

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2011 Pipeline of Can-Fite BioPharm.

REF 11

REF 12

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000713)

REF 13

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000987)

REF 14

A3 adenosine receptor as a target for cancer therapy. Anticancer Drugs. 2002 Jun;13(5):437-43.

REF 15

Spiroindolones, a potent compound class for the treatment of malaria. Science. 2010 Sep 3;329(5996):1175-80.

REF 16

2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists. Bioorg Med Chem. 2010 Mar 15;18(6):2195-2203.

REF 17

Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5690-4.

REF 18

2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacolog... J Med Chem. 2005 Nov 3;48(22):6887-96.

REF 19

Protein kinase C protects preconditioned rabbit hearts by increasing sensitivity of adenosine A2b-dependent signaling during early reperfusion. J Mol Cell Cardiol. 2007 Sep;43(3):262-71.

REF 20

Novel amino acid derived natural products from the ascidian Atriolum robustum: identification and pharmacological characterization of a unique aden... J Med Chem. 2004 Apr 22;47(9):2243-55.

REF 21

(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists. J Med Chem. 2005 Mar 24;48(6):1745-58.

REF 22

Structure-activity relationships of 9-alkyladenine and ribose-modified adenosine derivatives at rat A3 adenosine receptors. J Med Chem. 1995 May 12;38(10):1720-35.

REF 23

A binding site model and structure-activity relationships for the rat A3 adenosine receptor. Mol Pharmacol. 1994 Jun;45(6):1101-11.

REF 24

N(6)-alkyl-2-alkynyl derivatives of adenosine as potent and selective agonists at the human adenosine A(3) receptor and a starting point for searching A(2B) ligands. J Med Chem. 2002 Jul 18;45(15):3271-9.

REF 25

[(3)H]MRE 3008F20: a novel antagonist radioligand for the pharmacological and biochemical characterization of human A(3) adenosine receptors. Mol Pharmacol. 2000 May;57(5):968-75.

REF 26

Scouting human A3 adenosine receptor antagonist binding mode using a molecular simplification approach: from triazoloquinoxaline to a pyrimidine sk... J Med Chem. 2007 Dec 27;50(26):6596-606.

REF 27

Pharmacophore based receptor modeling: the case of adenosine A3 receptor antagonists. An approach to the optimization of protein models. J Med Chem. 2006 Jul 13;49(14):4085-97.

REF 28

Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions. J Med Chem. 2002 May 23;45(11):2131-8.

REF 29

Pyrido[2,1-f]purine-2,4-dione derivatives as a novel class of highly potent human A(3) adenosine receptor antagonists. J Med Chem. 2002 Aug 1;45(16):3337-44.

REF 30

2'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies. J Med Chem. 1998 May 7;41(10):1708-15.

REF 31

N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine recept... J Med Chem. 2009 Apr 23;52(8):2393-406.

REF 32

2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists. J Med Chem. 2006 May 18;49(10):2861-7.

REF 33

2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. J Med Chem. 2007 Feb 22;50(4):828-34.

REF 34

Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists. J Med Chem. 2008 Mar 27;51(6):1764-70.

REF 35

2-(Benzimidazol-2-yl)quinoxalines: a novel class of selective antagonists at human A(1) and A(3) adenosine receptors designed by 3D database search... J Med Chem. 2005 Dec 29;48(26):8253-60.

REF 36

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