Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T82083 | Target Info | |||
| Target Name | P2Y purinoceptor 4 (P2RY4) | ||||
| Synonyms |
Uridine nucleotide receptor; UNR; P2Y4; P2P; NRU
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| Target Type | Discontinued Target | ||||
| Gene Name | P2RY4 | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 41 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Suramin
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|
Phase 1 | Compound Info | ||
| Synonyms |
Antrypol; Belganyl; Farma; Fourneau; Germanin; Moranyl; Naganil; Naganin; Naganine; Naganol; Naphuride; SVR; Suramine; SURAMIN SODIUM; Sodium suramin; Suramine sodium; Farma 939; Naganol 6 Na; Germanin (TN); SGCTO-001
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| Activity |
EC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
PSB-716
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Investigative | Compound Info | ||
| Synonyms |
78510-27-7; PSB-716; Sodium 1-amino-4-o-methoxyanilino-9,10-dihydro-9,10-dioxoanthracene-2-sulphonate; CHEMBL257495; EINECS 278-930-3; SCHEMBL790524; DTXSID00229133; 1-Amino-2-(sodiooxysulfonyl)-4-(2-methoxyphenylamino)-9,10-anthraquinone; Sodium 1-amino-4-o-methoxyanilino-9,10-dihydro-9,10-dioxoanthracene-2-sulfonate
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| Activity |
IC50 = 50000 nM
|
[2] | |||
| Compound Name |
PSB-0952
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL590956
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
6-Hydroxyuridine-5'-Phosphate
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Investigative | Compound Info | ||
| Synonyms |
6-hydroxy-UMP; 6-HYDROXYURIDINE-5'-PHOSPHATE; 6-hydroxyuridine 5'-(dihydrogen phosphate); CHEMBL383923; 29741-00-2; Prfb acid; 1lor; 1dqx; 1eix; 6-hydroxyuridine 5'-phosphate; AC1Q69HY; AC1L4PT5; 5'-Uridylic acid,6-hydroxy-; SCHEMBL2130675; 5'-Uridylic acid, 6-hydroxy-; CTK4G3746; DTXSID50183892; Phosphoribofuranosylbarbituric acid; BDBM50199178; 6-Hydroxyuridine 5'-phosphoric acid; DB02890; 6-HYDROXYURIDINE-5''-PHOSPHATE; Barbituric acid ribonucleoside 5'-phosphate; 1-beta-D-ribofuranosyl(3H)pyrimidine-2,4,6-trione 5''-monophosp
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
3-phenacyl-UDP
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Investigative | Compound Info | ||
| Synonyms |
phenacyl-UDP
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
Tetrasodium;4-[[3-formyl-4-hydroxy-5-methyl-2-(phosphonatooxymethyl)phenyl]diazenyl]benzene-1,3-disulfonate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL477339
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| Activity |
IC50 = 73000 nM
|
[5] | |||
| Compound Name |
((2R,3S,4R,5R)-3,4-Dihydroxy-5-(2-(methylamino)-4-oxopyrimidin-1(4H)-yl)tetrahydrofuran-2-yl)methyl dihydrogen phosphate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1767423; BDBM50341894
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| Activity |
EC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
2-[(4-Amino-9,10-dioxo-3-sulfoanthracen-1-yl)amino]-5-fluorobenzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1208510; SCHEMBL19948045; BDBM50237584
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
1-(beta-D-Ribofuranosyl)-2-thio-uracil-5'-phosphate
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Investigative | Compound Info | ||
| Synonyms |
2-Thiouridine 5'-phosphate; CHEMBL384771; Polys2U; Poly-2-thiouridylic acid; 2-Thiouridine5'-phosphate; 2-thiouridine-5'-phosphate; SCHEMBL1881780; DTXSID60961901; 2-Thiouridine 5'-phosphoric acid; BDBM50199180; ZINC13517211; 5'-Uridylic acid, 2-thio-, homopolymer; Q27465498; 1-(BETA-D-RIBOFURANOSYL)-2-THIO-URACIL-5''-PHOSPHATE; 4-Hydroxy-1-(5-O-phosphonopentofuranosyl)pyrimidine-2(1H)-thione; 2-thio-1-beta-D-ribofuranosyl(3H)pyrimidine-2,4-dione 5''-monophosphate; 1-(5-O-phosphono-beta-D-ribofuranosyl)-2-thioxo-2,3-dihydropyrimidin-4(1H)-one
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
5'-Uridylic acid, 3-(2-oxo-2-phenylethyl)-
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL215381; CTK3I0370; DTXSID20475413; BDBM50199174; 3-phenacyl-1-beta-D-ribofuranosylpyrimidine-2,4-dione 5''-monophosphate
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
6-Propyl-3-beta-D-ribofuranosyl(1H)pyrimidine-2,4-dione 5''-diphosphate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL385506; BDBM50199181
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
2-Phenylethylthio-1-beta-D-ribofuranosylpyrimidine-4-one-5''-diphosphate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1767413; BDBM50341884
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| Activity |
EC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
2-[(4-Amino-3-methyl-9,10-dioxoanthracen-1-yl)amino]-5-fluorobenzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4080560; BDBM50237585
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| Activity |
IC50 = 100000 nM
|
[3] | |||
| Compound Name |
6-Methyl-3-beta-D-ribofuranosyl(1H)pyrimidine-2,4-dione 5''-diphosphate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL386096; BDBM50199175
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
Dichloro(((((2R,3S,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methoxy)(hydroxy)phosphoryloxy)(hydroxy)phosphoryl)methylphosphonic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1765114; BDBM50341896; Uridine 5'-[dichloro[beta,gamma-methylene]triphosphoric acid]
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| Activity |
EC50 ~ 100000 nM
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[6] | |||
| Compound Name |
2-Methoxy-UMP
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1767422; BDBM50341892; 2-Methoxy-1-beta-D-ribofuranosylpyrimidine-4-one-5''-monophosphate
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| Activity |
EC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
2-Methylamino-1-beta-D-ribofuranosylpyrimidine-4-one-5''-diphosphate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1767416; BDBM50341887
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| Activity |
EC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
[[(2R,3R,4R,5R)-5-(2,4-Dioxo-3-phenacylpyrimidin-1-yl)-3-hydroxy-4-phosphonooxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL265170; BDBM50199193; 3-phenacyl-1-beta-D-ribofuranosylpyrimidine-2,4-dione 2''-Monophosphate-5''-triphosphate
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
2-Amino-1-beta-D-ribofuranosylpyrimidine-4-one-5''-diphosphate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1767415; BDBM50341886
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| Activity |
EC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
6-Propyl-3-beta-D-ribofuranosyl(1H)pyrimidine-2,4-dione 5''-triphosphate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL425805; BDBM50199172
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|
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
6-Propyl-3-beta-D-ribofuranosyl(1H)pyrimidine-2,4-dione 5''-monophosphate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL217391; BDBM50199182
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|
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
5-Bromouridine 5'-monophosphate
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|
Investigative | Compound Info | ||
| Synonyms |
5-Brump; 5-bromo-5'-uridylic acid; 5-Bromo-Uridine-5'-Monophosphate; 5-Br-UMP; 5-bromouridine 5'-phosphate; 5-bromouridine 5'-(dihydrogen phosphate); CHEMBL214830; 5-Bromouridine-5'-monophosphate; Poly(5-bru); Poly(BU); Poly-5-bromouridylic acid; 5'-Uridylic acid, 5-bromo-; 5-Bromo-UMP; SCHEMBL3469958; CTK7F2755; DTXSID30944089; BDBM50199184; ZINC13518134; 5'-Uridylic acid, 5-bromo-, homopolymer; 5-BROMO-URIDINE-5''-MONOPHOSPHATE; Q27104588; 5-bromo-1-beta-D-ribofuranosyl(3H)pyrimidine-2,4-dione 5''-monophosphate; 5-Bromo-4-hydroxy-1-(5-O-phosphonopentofuranosyl)pyrimidin-2(1H)-one
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|
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
[(2R,3S,5R)-5-[6-(Methylamino)purin-9-yl]-2-(phosphonooxymethyl)oxolan-3-yl] dihydrogen phosphate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL129841; MRS 2179; MRS-2179; CHEMBL1096400; MRS 2179 ammonium salt; Lopac0_000756; SCHEMBL134008; DTXSID701016926; ZINC3985980; BDBM50118229; BDBM50318029; n6-methyl-2'-deoxyadenosine-3',5'-bisphosphate; J-000339
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| Activity |
EC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-Benzylthio-1-beta-D-ribofuranosylpyrimidine-4-one-5''-monophosphate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1767420; BDBM50341903
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|
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| Activity |
EC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
[(1R,2R,4S,5S)-4-[2-Chloro-6-(methylamino)purin-9-yl]-2-phosphonooxy-1-bicyclo[3.1.0]hexanyl]methyl dihydrogen phosphate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3085531; BDBM50026893
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| Activity |
EC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
[(2R,3S,4R,5R)-3,4-Dihydroxy-5-(3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl]methyl trihydrogen diphosphate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL215447; 3-methyluridine 5'-pyrophosphate; BDBM50194162; 3-methyl-1-beta-D-ribofuranosylpyrimidine-2,4-dione 5''-diphosphate
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
Sodium;1-amino-4-(2-carboxy-5-fluoroanilino)-9,10-dioxoanthracene-2-sulfonate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL603678; BDBM50237578
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| Activity |
IC50 ~ 100000 nM
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[3] | |||
| Compound Name |
Sodium;1-amino-4-(4-bromo-2-carboxyanilino)-9,10-dioxoanthracene-2-sulfonate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL603260; BDBM50237565
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| Activity |
IC50 ~ 100000 nM
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[3] | |||
| Compound Name |
2-Phenylethylthio-1-beta-D-ribofuranosylpyrimidine-4-one-5''-monophosphate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1767421; BDBM50341891
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| Activity |
EC50 ~ 100000 nM
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[6] | |||
| Compound Name |
[[(2S,3R,4S,5S)-5-(2,4-Dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] [[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] hydrogen phosphate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1162193; BDBM50371609
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| Activity |
EC50 ~ 100000 nM
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[7] | |||
| Compound Name |
[[(3Ar,4R,6R,6aR)-4-(2,4-dioxo-6-propyl-1H-pyrimidin-3-yl)-2-hydroxy-2-oxo-3a,4,6,6a-tetrahydrofuro[3,4-d][1,3,2]dioxaphosphol-6-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL217370; BDBM50199187; 6-propyl-3-beta-D-ribofuranosyl(1H)pyrimidine-2,4-dione 2'',3''-(cyclic phosphate) 5''-triphosphate
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
N(3)-Methyluridine 5'-monophosphate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL215940; N(3)-methyl-UMP; 3-N-methyluridine-5 '-phosphate; N(3)-methyluridine 5'-phosphate; BDBM50199190; 3-METHYLURIDINE-5'-MONOPHOSHATE; 3-METHYLURIDINE-5''-MONOPHOSHATE; 3-methyluridine 5'-(dihydrogen phosphate); Q27105026; 3-methyl-1-beta-D-ribofuranosyl-pyrimidine-2,4-dione 5''-monophosphate
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
6-Methyl-3-beta-D-ribofuranosyl(1H)pyrimidine-2,4-dione 5''-triphosphate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL413841; BDBM50199189
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
Sodium;1-amino-4-(2-carboxy-3-fluoroanilino)-9,10-dioxoanthracene-2-sulfonate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4079524; BDBM50237566
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
1-beta-D-Ribofuranosyl(3H)pyrimidine-2,4,6-trione 5''-triphosphate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL436959; BDBM50199188
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
2-Methylthio-1-beta-D-ribofuranosylpyrimidine-4-one-5''-monophosphate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1767417; BDBM50341888
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| Activity |
EC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
4-Thiouridine-5'-monophosphate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1230331; 1-(5-O-Phosphono-beta-D-ribofuranosyl)-4-thioxo-3,4-dihydropyrimidin-2(1H)-one; 4-Thiouridylic acid; 4-thio-UMP; S4UMP; 4-thiouridine monophosphate; 5'-Uridylic acid, 4-thio-; 4-Thiouracil 5'-monophosphate; SCHEMBL1402556; 4-Thiouridine 5'-phosphoric acid; 4-THIOURIDINE-5''-PHOSPHATE; BDBM50341895; ZINC13518042; 4-THIOURIDINE-5''-MONOPHOSPHATE; Q27454935
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| Activity |
EC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
6-Methyl-3-beta-D-ribofuranosyl(1H)pyrimidine-2,4-dione 5''-monophosphate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL215263; BDBM50199179
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
[[[(2R,3S,4R,5R)-5-(5-Bromo-2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl]oxy-N-phenylphosphonamidic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1765120; BDBM50341902; 5-Bromo-1-beta-D-ribofuranosyl(3H)pyrimidine-2,4-dione 5''-(gamma-phenylamino)triphosphate
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| Activity |
EC50 ~ 100000 nM
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[6] | |||
| Compound Name |
2-Propylthio-1-beta-D-ribofuranosylpyrimidine-4-one-5''-monophosphate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1767419; BDBM50341890
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| Activity |
EC50 ~ 100000 nM
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[6] | |||
| Compound Name |
(((((2R,3S,4R,5R)-5-(2,4-Dioxo-3,4-dihydropyrimidin-1(2H)-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methoxy)(hydroxy)phosphoryloxy)(hydroxy)phosphoryl)difluoromethylphosphonic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1765117; BDBM50341899; Uridine 5'-[difluoro[beta,gamma-methylene]triphosphoric acid]
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| Activity |
EC50 ~ 100000 nM
|
[6] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Purine and pyrimidine (P2) receptors as drug targets. J Med Chem. 2002 Sep 12;45(19):4057-93. | ||||
| REF 2 | Combinatorial synthesis of anilinoanthraquinone derivatives and evaluation as non-nucleotide-derived P2Y2 receptor antagonists. Bioorg Med Chem Lett. 2008 Jan 1;18(1):223-7. | ||||
| REF 3 | Development of Potent and Selective Antagonists for the UTP-Activated P2Y 4 Receptor. J Med Chem. 2017 Apr 13;60(7):3020-3038. | ||||
| REF 4 | Synthesis and structure-activity relationships of uracil nucleotide derivatives and analogues as agonists at human P2Y2, P2Y4, and P2Y6 receptors. J Med Chem. 2006 Nov 30;49(24):7076-87. | ||||
| REF 5 | Selective nucleoside triphosphate diphosphohydrolase-2 (NTPDase2) inhibitors: nucleotide mimetics derived from uridine-5'-carboxamide. J Med Chem. 2008 Aug 14;51(15):4518-28. | ||||
| REF 6 | Structural modifications of UMP, UDP, and UTP leading to subtype-selective agonists for P2Y2, P2Y4, and P2Y6 receptors. J Med Chem. 2011 Apr 28;54(8):2878-90. | ||||
| REF 7 | Synthesis and P2Y receptor activity of a series of uridine dinucleoside 5'-polyphosphates. Bioorg Med Chem Lett. 2001 Jan 22;11(2):157-60. | ||||
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