Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T93515 | Target Info | |||
| Target Name | P2Y purinoceptor 2 (P2RY2) | ||||
| Synonyms |
P2Y2; P2U1; P2U receptor; P2U purinoceptor 1; P2U nucleotide receptor; P2RY2; Adenosine P2Y2 receptor
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| Target Type | Clinical trial Target | ||||
| Gene Name | P2RY2 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 26 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 |
IC50 = 50000 nM
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[1] | |||
| Compound Name |
2-amino-uridine-5'-monophosphate
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Investigative | Compound Info | ||
| Synonyms |
iso-CMP; compound 13g [PMID: 21417463]
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| Activity |
EC50 ~ 100000 nM
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[2] | |||
| Compound Name |
Uridine-5'-Diphosphate
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Investigative | Compound Info | ||
| Synonyms |
Uridine 5'-diphosphate; URIDINE DIPHOSPHATE; 58-98-0; Uridine 5'-(trihydrogen diphosphate); uridine-5'-diphosphate; UDP; UNII-5G0F599A1Y; 5'-UDP; Uridine 5'-pyrophosphate; EINECS 200-409-6; Uridine 5'-pyrophosphoric acid; CHEMBL130266; CHEBI:17659; 5G0F599A1Y; uridine-diphosphate; ((2R,3S,4R,5R)-5-(2,4-Dioxo-3,4-dihydropyrimidin-1(2H)-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl trihydrogen diphosphate; [(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methyl phosphono hydrogen phosphate; Uridine Pyrophosp
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| Activity |
EC50 ~ 100000 nM
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[3] | |||
| Compound Name |
adenosine diphosphate
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Investigative | Compound Info | ||
| Synonyms |
Adenosine diphosphate; 58-64-0; ADP; Adenosine 5'-(trihydrogen diphosphate); adenosine pyrophosphate; adenosine 5'-pyrophosphate; ADP (nucleotide); adenosine-diphosphate; 5'-Adenylphosphoric acid; 5'-Adp; Adenosindiphosphorsaeure; Adenosine 5'-pyrophosphoric acid; Adenosine-5'-diphosphat; Adenosine 5'-diphosphoric acid; Adenosine diphosphoric acid; Ado-5'-P-P; UNII-61D2G4IYVH; H3adp; BRN 0067722; CHEBI:16761; EINECS 200-392-5; 61D2G4IYVH; CHEMBL14830
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| Activity |
EC50 ~ 100000 nM
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[3] | |||
| Compound Name |
2MeSADP
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Investigative | Compound Info | ||
| Synonyms |
2-Methylthio-adenosine-5'-diphosphate; 2-MeSADP; 2-methylthio-ADP; 2-Mes-ADP; 2-methylthio-adenosine-5'-diphosphate; CHEMBL435402; 2-(methylsulfanyl)adenosine 5'-(trihydrogen diphosphate); methylthio-ADP; [(2R,3S,4R,5R)-5-(6-amino-2-methylsulfanylpurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl phosphono hydrogen phosphate; 2-(Methylthio)adenosine 5'-diphosphate; [3H]2-methylthio-ADP; [3H]2MeSADP; (3H)2-Mes-ADP; AC1L3TRY; SCHEMBL195864; GTPL1763; GTPL1710; AC1Q6S18; adenosine, 2-(methylthio)-, 5'-(trihydrogen diphosphate); 2-(Methylthio)-Adenosinediphosphate; 2-methylthio-ADP
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| Activity |
EC50 ~ 100000 nM
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[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
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[4] | |||
| Compound Name |
Chembl4215280
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Investigative | Compound Info | ||
| Synonyms |
BDBM50458838
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| Activity |
EC50 ~ 50000 nM
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[5] | |||
| Compound Name |
N,4-Dimethyl-N-(2-(thiophene-3-carbonyl)phenyl)benzenesulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL604583; BDBM50305731
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| Activity |
IC50 ~ 60000 nM
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[6] | |||
| Compound Name |
[(4-Methylphenyl)sulfonyl](2-{[(4-methylphenyl)sulfonyl]prop-2-enylamino}pheny l)prop-2-enylamine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL604277; ZINC2573080; BDBM50305737; SBB057090; AKOS024364667; MCULE-3639320640; ST50997002; N,N'-Diallyl-N,N'-ditosyl-1,2-benzenediamine; N,N''-(1,2-phenylene)bis(N-allyl-4-methylbenzenesulfonamide)
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| Activity |
IC50 ~ 60000 nM
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[6] | |||
| Compound Name |
n,n'-1,2-Phenylenebis(n,4-dimethylbenzenesulfonamide)
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL595990; NSC101062; Oprea1_370376; CBDivE_001423; DTXSID20295299; ZINC636919; BDBM50305735; AKOS002161609; MCULE-1311888097; NSC-101062; N,N-o-phenylene-bis(p-toluenesulfonamide); ST50036099; p-Toluenesulfonamide,N'-o-phenylenebis[N-methyl-; N,N'-Ditosyl-N,N'-dimethyl-1,2-phenylenediamine; N,N''-(1,2-phenylene)bis(N-methyl-1-phenylmethanesulfonamide)
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| Activity |
IC50 ~ 60000 nM
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[6] | |||
| Compound Name |
CID 70692052
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2029009
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| Activity |
EC50 = 64200 nM
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[7] | |||
| Compound Name |
CID 70694094
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2029005
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| Activity |
EC50 = 64200 nM
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[7] | |||
| Compound Name |
Diadenosine tetraphosphate
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Investigative | Compound Info | ||
| Synonyms |
AppppA; 5',5'''-Diadenosine tetraphosphate; P(1),P(4)-bis(5'-adenosyl) tetraphosphate; (ppA)2; BIS(ADENOSINE)-5'-TETRAPHOSPHATE; CHEMBL339385; adenosine(5')tetraphospho(5')adenosine; P1,P4-Bis(5'-adenosyl) tetraphosphate; A(5')p4(5')A; Diadenosine 5',5'''-P(sup 1),P(sup 2)-tetraphosphate; ADENOSINE 5'-(PENTAHYDROGEN TETRAPHOSPHATE), 5'-5'-ESTER with ADENOSINE; SCHEMBL849869; Adenosine 5'-tetraphosphate, 5'-ester with adenosine; bis(5''-adenylyl) diphosphate; DTXSID60203994; BDBM50118220; ZINC96014967; P1,P4-Diadenosine-5'-tetraphosphate; P1,P4-bis(5'-adenosyl)tetraphosphate; A(5'')p4(5'')A; P1,P4-Di(adenosin-5'-yl)tetraphosphate; adenosine(5'')tetraphospho(5'')adenosine; adenosine-(5')-tetraphospho-(5')-adenosine; Diadenosine 5',5'''-P1,P4-tetraphosphate; C01260; P(1),P(4)-bis(5''-adenosyl) tetraphosphate; Q27102391; Adenosine 5'-tetraphosphate, 5'-ester with adenosine (7CI)
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| Activity |
EC50 = 81000 nM
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[8] | |||
| 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
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[2] | |||
| 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
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[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
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[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
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[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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| Activity |
EC50 ~ 100000 nM
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[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
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[3] | |||
| 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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| Activity |
EC50 ~ 100000 nM
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[2] | |||
| 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
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[3] | |||
| 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
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[4] | |||
| 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
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[2] | |||
| 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
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[4] | |||
| Compound Name |
Hexasodium;8-[[4-fluoro-3-[[3-[[3-[[2-fluoro-5-[(4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl]phenyl]carbamoyl]phenyl]carbamoylamino]benzoyl]amino]benzoyl]amino]naphthalene-1,3,5-trisulfonate
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Investigative | Compound Info | ||
| Synonyms |
NF157; CHEMBL413145
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| Activity |
IC50 = 169824.37 nM
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[9] | |||
| Compound Name |
Trypan blue
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Investigative | Compound Info | ||
| Synonyms |
Direct Blue 14; VisionBlue; C.I. Direct Blue 14; Niagara Blue; Niagara Blue 3B; trypan-blue; Diamineblue; Dianilblau; Pyrotropblau; Parkibleu; Parkipan; Benzamine Blue; Bleu diamine; Chloramine Blue; Dianil blue; Diphenyl Blue; Trypane Blue; Tripan Blue; Benzaminblau 3B; Benzo Blue; Chloramiblau 3B; Congo Blue; Bleu trypane N; Benzanil Blue R; Diaminblau 3B; Directblau 3B; Triazolblau 3BX; Benzoblau 3B; Congoblau 3B; Dianilblau H3G; Renolblau 3B; Bleu directe 3B; Naphthylamine Blue; Azidine Blue 3B; C.I. 23850; Diamine Blue 3B; Diazine Blue 3B; Pyrazol Blue 3B; Trypan Blue BPC; Bleue diretto 3B; Bencidal Blue 3B; Dianil Blue H3G; Diazol Blue 3B; Diphenyl Blue 3B; Direct Blue 3B; Direct Blue 3BX; Direct Blue D3B; Direct Blue H3G; Direct Blue M3B; Paramine Blue 3B; Azurro diretto 3B; Benzo Blue 3B; Benzo Blue 3BS; Blue EMB; Naphthaminblau 3BX; Orion Blue 3B; Benzamine Blue 3B; Chlorazol Blue 3B; Cresotine Blue 3B; UNII-I2ZWO3LS3M; Amanil Sky Blue R; Benzanil Blue 3BN; Centraline Blue 3B; Chloramine Blue 3B; Hispamin Blue 3BX; I2ZWO3LS3M; Diaphtamine Blue TH; Bleu diazole N 3B; Blue 3B; Pontamine Blue 3BX; Brasilamina Blue 3B; Brasilazina Blue 3B; Directakol Blue 3BL; Naphthamine Blue 3BX; C.I. Direct Blue 14, tetrasodium salt; Chrome Leather Blue 3B; Trianol Direct Blue 3B; Trypanblau; MFCD00003969; C34H24N6O14S4.4Na; Diaminine Blue; Vision Blue; Azidinblau 3B; Trypanblau [German]; Trypan (Congo) Blue; Modr Trypanova [Czech]; NCGC00167554-01; Modr Prima 14 [Czech]; RCRA waste no. U236; RCRA waste number U236; Membraneblue; CCRIS 616; Modr Trypanova; Trypan blue (commercial grade); HSDB 2945; NCI C61289; EINECS 200-786-7; Modr Prima 14; NSC 11247; Trypan Blue solution; AI3-26698; DSSTox_CID_6268; CHEMBL1640; DSSTox_RID_78083; DSSTox_GSID_26268; CHEMBL177987; Trypan Blue, dye content 60%; DTXSID4026268; KS-00000YE3; Tox21_112549; 2084AH; 6952AF; AKOS015902434; AKOS030228627; FT-0690008; C19307; C.I. Direct Blue 14, tetrasodium salt (8CI)
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| Activity |
IC50 = 171000 nM
|
[3] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 2 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Chembl4209172
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Investigative | Compound Info | ||
| Synonyms |
BDBM50454135; uridine 5'-(tetrahydrogen triphosphate), 4-O-hexyl-
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| Activity |
EC50 = 489300 nM
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[10] | |||
| Compound Name |
Click to Show/Hide
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Compound Info | |||
| Activity |
EC50 > 300000 nM
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[8] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | 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 2 | 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 3 | Purine and pyrimidine (P2) receptors as drug targets. J Med Chem. 2002 Sep 12;45(19):4057-93. | ||||
| 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 | 3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17. J Med Chem. 2018 Sep 27;61(18):8136-8154. | ||||
| REF 6 | Identification of a new class of small molecule C5a receptor antagonists. Bioorg Med Chem Lett. 2010 Jan 15;20(2):662-4. | ||||
| REF 7 | Boranophosphate isoster controls P2Y-receptor subtype selectivity and metabolic stability of dinucleoside polyphosphate analogues. J Med Chem. 2012 Jan 12;55(1):437-48. | ||||
| REF 8 | Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling. J Med Chem. 2009 May 14;52(9):2762-75. | ||||
| REF 9 | Synthesis and structure-activity relationships of suramin-derived P2Y11 receptor antagonists with nanomolar potency. J Med Chem. 2005 Nov 3;48(22):7040-8. | ||||
| REF 10 | Current knowledge on the nucleotide agonists for the P2Y2 receptor. Bioorg Med Chem. 2018 Jan 15;26(2):366-375. | ||||
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