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Ligand source activities (1 row/activity)
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
AR-C118925XX | 460 | None | 26 | Human | Binding | Ki | = | 41.69 | 7.38 | - | 1 | Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay | ChEMBL | 537.2 | 5 | 3 | 8 | 4.59 | Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2ccc(C(=O)Nc3nnn[nH]3)o2)c(=O)[nH]c1=S | https://dx.doi.org/10.1021/acs.jmedchem.8b00139 | |
AR-C118925XX | 460 | None | 26 | Human | Binding | Ki | = | 21.88 | 7.66 | - | 1 | Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(2-(4-(2-(5,5-difluoro-7-(thiophen-2-yl)-5H-4-lambda4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-vinyl)phenoxy)acetamido)hexanamido)ethyl)amino)-3-oxopropyl)-amino)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)-thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay | ChEMBL | 537.2 | 5 | 3 | 8 | 4.59 | Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2ccc(C(=O)Nc3nnn[nH]3)o2)c(=O)[nH]c1=S | https://dx.doi.org/10.1021/acs.jmedchem.8b00139 | |
AR-C118925XX | 460 | None | 26 | Human | Binding | Ki | = | 47.86 | 7.32 | - | 1 | Displacement of N-(2-(2-(2-(3-((7-Chloro-4-(1-methyl-2-oxo-4-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-2-yl)amino)propanamido)ethoxy)ethoxy)ethyl)-6-(3-(5,5-difluoro-7,9-dimethyl-5H-4-lambda4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)propanamido)hexanamide from recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay | ChEMBL | 537.2 | 5 | 3 | 8 | 4.59 | Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2ccc(C(=O)Nc3nnn[nH]3)o2)c(=O)[nH]c1=S | https://dx.doi.org/10.1021/acs.jmedchem.8b00139 | |
AR-C118925XX | 460 | None | 26 | Human | Binding | Ki | = | 35.48 | 7.45 | - | 1 | Displacement of N-(2-(3-((7-Chloro-4-(1-methyl-2-oxo-4-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-2-yl)-amino)propanamido)ethyl)-6-(3-(5,5-difluoro-7,9-dimethyl-5H-4-lamba4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamide from recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay | ChEMBL | 537.2 | 5 | 3 | 8 | 4.59 | Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2ccc(C(=O)Nc3nnn[nH]3)o2)c(=O)[nH]c1=S | https://dx.doi.org/10.1021/acs.jmedchem.8b00139 | |
ATP | 520 | None | 42 | Human | Binding | EC50 | = | 230.00 | 6.64 | - | 10 | Agonist activity at human P2Y2 transfected in human 1321N1 cells | ChEMBL | 507.0 | 8 | 7 | 14 | -1.63 | Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O | https://dx.doi.org/10.1021/acs.jmedchem.5b01972 | |
CHEMBL2333767 | 87497 | None | 0 | Human | Binding | Ki | = | 2700.00 | 5.57 | -134 | 3 | Inhibition of human P2Y2 receptor | ChEMBL | 391.2 | 4 | 2 | 3 | 6.48 | Cc1ccc(NC(=O)Nc2cccnc2Sc2ccccc2C(C)(C)C)cc1 | https://dx.doi.org/10.1021/jm301708u | |
CHEMBL2333773 | 87501 | None | 0 | Human | Binding | Ki | = | 6400.00 | 5.19 | -407 | 3 | Inhibition of human P2Y2 receptor | ChEMBL | 431.1 | 6 | 2 | 4 | 6.54 | CC(C)c1ccccc1Oc1ncccc1NC(=O)Nc1ccc(OC(F)(F)F)cc1 | https://dx.doi.org/10.1021/jm301708u | |
CHEMBL3261379 | 110981 | None | 0 | Human | Binding | EC50 | = | 389.00 | 6.41 | - | 3 | Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells by functional assay | ChEMBL | 923.1 | 19 | 10 | 22 | -2.08 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4cc/c(=N/OCCCc5ccccc5)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 | https://dx.doi.org/10.1021/jm500367e | |
CHEMBL4117043 | 161199 | None | 0 | Human | Binding | Ki | = | 83.18 | 7.08 | - | 1 | Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay | ChEMBL | 758.0 | 9 | 7 | 11 | 3.39 | O=c1[nH]c(=S)c(C2c3ccccc3CCc3ccccc32)cn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O | https://dx.doi.org/10.1021/acs.jmedchem.8b00139 | |
CHEMBL4125833 | 161436 | None | 0 | Human | Binding | Kd | = | 891.25 | 6.05 | - | 1 | Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay | ChEMBL | 1128.2 | 18 | 6 | 17 | 7.91 | O=C(CCNc1nc2c(s1)C=Cc1cc(Cl)ccc1C2c1cn(Cc2nc(C(=O)Nc3nnn[nH]3)cs2)c(=O)[nH]c1=S)NCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1 | https://dx.doi.org/10.1021/acs.jmedchem.8b00139 | |
CHEMBL4125853 | 161440 | None | 0 | Human | Binding | Kd | = | 758.58 | 6.12 | - | 1 | Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay | ChEMBL | 1153.4 | 21 | 5 | 14 | 8.80 | Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2cc(C(=O)NCCOCCOCCNC(=O)COc3ccc(/C=C/C4=[N+]5C(=Cc6ccc(-c7cccs7)n6[B-]5(F)F)C=C4)cc3)cc(C(=O)Nc3nnn[nH]3)c2)c(=O)[nH]c1=S | https://dx.doi.org/10.1021/acs.jmedchem.8b00139 | |
CHEMBL4125987 | 161447 | None | 0 | Human | Binding | Kd | = | 851.14 | 6.07 | - | 1 | Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay | ChEMBL | 1268.5 | 27 | 6 | 15 | 9.05 | Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2cc(C(=O)NCCOCCOCCNC(=O)CCCCCNC(=O)COc3ccc(/C=C/C4=[N+]5C(C=C4)Cc4ccc(-c6cccs6)n4[B-]5(F)F)cc3)cc(C(=O)Nc3nnn[nH]3)c2)c(=O)[nH]c1=S | https://dx.doi.org/10.1021/acs.jmedchem.8b00139 | |
CHEMBL4126655 | 161502 | None | 0 | Human | Binding | Kd | = | 478.63 | 6.32 | - | 1 | Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay | ChEMBL | 1185.3 | 23 | 7 | 16 | 8.03 | Cc1cc(C)n2c1C=C1C=CC(/C=C/c3ccc(CCC(=O)NCCCCCC(=O)NCCNC(=O)CCNc4nc5c(s4)C=Cc4cc(Cl)ccc4C5c4cn(Cc5nc(C(=O)Nc6nnn[nH]6)cs5)c(=O)[nH]c4=S)cc3)=[N+]1[B-]2(F)F | https://dx.doi.org/10.1021/acs.jmedchem.8b00139 | |
CHEMBL4126826 | 161514 | None | 0 | Human | Binding | Kd | = | 2754.23 | 5.56 | - | 1 | Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay | ChEMBL | 1065.3 | 15 | 5 | 12 | 8.77 | Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2cc(C(=O)NCCNC(=O)COc3ccc(/C=C/C4=[N+]5C(=Cc6ccc(-c7cccs7)n6[B-]5(F)F)C=C4)cc3)cc(C(=O)Nc3nnn[nH]3)c2)c(=O)[nH]c1=S | https://dx.doi.org/10.1021/acs.jmedchem.8b00139 | |
CHEMBL4127230 | 161532 | None | 0 | Human | Binding | Kd | = | 1659.59 | 5.78 | - | 1 | Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay | ChEMBL | 1180.4 | 21 | 6 | 13 | 9.02 | Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2cc(C(=O)NCCNC(=O)CCCCCNC(=O)COc3ccc(/C=C/C4=[N+]5C(C=C4)Cc4ccc(-c6cccs6)n4[B-]5(F)F)cc3)cc(C(=O)Nc3nnn[nH]3)c2)c(=O)[nH]c1=S | https://dx.doi.org/10.1021/acs.jmedchem.8b00139 | |
CHEMBL4127889 | 161584 | None | 0 | Human | Binding | Kd | = | 89.13 | 7.05 | - | 1 | Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay | ChEMBL | 970.2 | 15 | 6 | 15 | 5.48 | Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCNC(=O)CCNc3nc4c(s3)C=Cc3cc(Cl)ccc3C4c3cn(Cc4nc(C(=O)Nc5nnn[nH]5)cs4)c(=O)[nH]c3=S)=[N+]1[B-]2(F)F | https://dx.doi.org/10.1021/acs.jmedchem.8b00139 | |
CHEMBL4127983 | 161587 | None | 0 | Human | Binding | Ki | = | 1548.82 | 5.81 | - | 1 | Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay | ChEMBL | 387.0 | 1 | 1 | 5 | 4.53 | Cc1nc2c(s1)C=Cc1cc(Cl)ccc1C2c1cn(C)c(=O)[nH]c1=S | https://dx.doi.org/10.1021/acs.jmedchem.8b00139 | |
CHEMBL4128024 | 161592 | None | 0 | Human | Binding | Kd | = | 295.12 | 6.53 | - | 1 | Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay | ChEMBL | 526.2 | 5 | 3 | 5 | 5.25 | Cc1ccc2c(c1)CCc1cc(C)ccc1C2c1cn(Cc2cc(C(=O)O)cc(C(=O)O)c2)c(=O)[nH]c1=S | https://dx.doi.org/10.1021/acs.jmedchem.8b00139 | |
CHEMBL4128024 | 161592 | None | 0 | Human | Binding | Ki | = | 144.54 | 6.84 | - | 1 | Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay | ChEMBL | 526.2 | 5 | 3 | 5 | 5.25 | Cc1ccc2c(c1)CCc1cc(C)ccc1C2c1cn(Cc2cc(C(=O)O)cc(C(=O)O)c2)c(=O)[nH]c1=S | https://dx.doi.org/10.1021/acs.jmedchem.8b00139 | |
CHEMBL4128059 | 161595 | None | 0 | Human | Binding | Ki | = | 5248.07 | 5.28 | - | 1 | Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay | ChEMBL | 460.1 | 6 | 2 | 7 | 4.67 | CCOCCNc1nc2c(s1)C=Cc1cc(Cl)ccc1[C@@H]2c1cn(C)c(=O)[nH]c1=S | https://dx.doi.org/10.1021/acs.jmedchem.8b00139 |
Showing 1 to 20 of 32 entries
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
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Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
2-chloroadenosine-5-triphosphate | 59 | None | 11 | Human | Functional | EC50 | = | 2300.00 | 5.64 | -630 | 4 | Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2 | ChEMBL | 541.0 | 8 | 7 | 14 | -0.98 | Nc1nc(Cl)nc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O | https://dx.doi.org/10.1021/jm010538v | |
2-thioUTP | 90 | None | 3 | Human | Functional | pEC50 | = | - | 7.30 | 17 | 3 | Unclassified | Guide to Pharmacology | 499.9 | 8 | 7 | 12 | -1.13 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 | https://pubmed.ncbi.nlm.nih.gov/17125260 | |
2-thioUTP | 90 | None | 3 | Human | Functional | EC50 | = | 35.00 | 7.46 | 17 | 3 | Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay | ChEMBL | 499.9 | 8 | 7 | 12 | -1.13 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 | https://dx.doi.org/10.1021/jm101591j | |
2-thioUTP | 90 | None | 3 | Human | Functional | EC50 | = | 35.00 | 7.46 | 17 | 3 | Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay | ChEMBL | 499.9 | 8 | 7 | 12 | -1.13 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 | https://dx.doi.org/10.1016/j.bmc.2008.05.013 | |
2-thioUTP | 90 | None | 3 | Human | Functional | EC50 | = | 35.00 | 7.46 | 17 | 3 | Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C | ChEMBL | 499.9 | 8 | 7 | 12 | -1.13 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 | https://dx.doi.org/10.1021/jm060903o | |
2-thioUTP | 90 | None | 3 | Human | Functional | EC50 | = | 50.00 | 7.30 | 17 | 3 | Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA | ChEMBL | 499.9 | 8 | 7 | 12 | -1.13 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 | https://dx.doi.org/10.1021/jm060848j | |
4-thio-UTP | 125 | None | 8 | Human | Functional | pEC50 | None | - | 7.50 | -3 | 2 | Unclassified | Guide to Pharmacology | 499.9 | 8 | 7 | 12 | -1.13 | O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O | https://pubmed.ncbi.nlm.nih.gov/16475938 | |
4-thio-UTP | 125 | None | 8 | Human | Functional | EC50 | = | 26.00 | 7.58 | -3 | 2 | Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay | ChEMBL | 499.9 | 8 | 7 | 12 | -1.13 | O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O | https://dx.doi.org/10.1021/jm1016297 | |
4-thio-UTP | 125 | None | 8 | Human | Functional | EC50 | = | 710.00 | 6.15 | -3 | 2 | Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as [3H]-inositol phosphate accumulation measured after 90 mins by anion exchange chromatographic method | ChEMBL | 499.9 | 8 | 7 | 12 | -1.13 | O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O | https://dx.doi.org/10.1016/j.bmc.2017.11.043 | |
5BrUTP | 130 | None | 8 | Human | Functional | pEC50 | None | - | 5.70 | -1 | 3 | Unclassified | Guide to Pharmacology | 561.9 | 8 | 7 | 12 | -1.74 | O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)cc1Br | https://pubmed.ncbi.nlm.nih.gov/8564228 | |
5BrUTP | 130 | None | 8 | Human | Functional | EC50 | = | 347.00 | 6.46 | -1 | 3 | Agonist activity at human P2Y2 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA | ChEMBL | 561.9 | 8 | 7 | 12 | -1.74 | O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)cc1Br | https://dx.doi.org/10.1021/jm060848j | |
5BrUTP | 130 | None | 8 | Human | Functional | EC50 | = | 750.00 | 6.12 | -1 | 3 | Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C | ChEMBL | 561.9 | 8 | 7 | 12 | -1.74 | O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)cc1Br | https://dx.doi.org/10.1021/jm060903o | |
5BrUTP | 130 | None | 8 | Human | Functional | EC50 | = | 220.00 | 6.66 | -1 | 3 | Agonist activity at P2Y2 receptor (unknown origin) | ChEMBL | 561.9 | 8 | 7 | 12 | -1.74 | O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)cc1Br | https://dx.doi.org/10.1016/j.bmc.2017.11.043 | |
5BrUTP | 130 | None | 8 | Human | Functional | EC50 | = | 2060.00 | 5.69 | -1 | 3 | Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay | ChEMBL | 561.9 | 8 | 7 | 12 | -1.74 | O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)cc1Br | https://dx.doi.org/10.1021/jm901450d | |
ADENOSINE PHOSPHATE | 207273 | None | 55 | Human | Functional | EC50 | = | 3700.00 | 5.43 | -1 | 9 | Measure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cell | ChEMBL | 347.1 | 4 | 5 | 10 | -1.86 | Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O | https://dx.doi.org/10.1021/jm010369e | |
ADENOSINE PHOSPHATE | 207273 | None | 55 | Human | Functional | EC50 | = | 85.00 | 7.07 | -1 | 9 | Measure of Agonist Potency at human P2Y purinoceptor 2 (hP2Y2) stably expressed in 131N1 astrocytoma cell | ChEMBL | 347.1 | 4 | 5 | 10 | -1.86 | Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O | https://dx.doi.org/10.1021/jm010369e | |
Ap4A | 450 | None | 0 | Human | Functional | pEC50 | = | - | 6.10 | -3 | 4 | Unclassified | Guide to Pharmacology | 832.0 | 14 | 6 | 29 | -4.97 | Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)([O-])OP(=O)([O-])OP(=O)([O-])OP(=O)([O-])OC[C@H]2O[C@@H](n3cnc4c(N)ncnc43)[C@H](O)[C@@H]2O)[C@@H](O)[C@H]1O | https://pubmed.ncbi.nlm.nih.gov/11711032 | |
Ap4A | 450 | None | 0 | Human | Functional | pEC50 | = | - | 6.10 | -3 | 4 | Unclassified | Guide to Pharmacology | 832.0 | 14 | 6 | 29 | -4.97 | Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)([O-])OP(=O)([O-])OP(=O)([O-])OP(=O)([O-])OC[C@H]2O[C@@H](n3cnc4c(N)ncnc43)[C@H](O)[C@@H]2O)[C@@H](O)[C@H]1O | https://pubmed.ncbi.nlm.nih.gov/1393282 | |
AR-C118925XX | 460 | None | 26 | Human | Functional | pIC50 | ~ | - | 6.00 | - | 1 | Unclassified | Guide to Pharmacology | 537.2 | 5 | 3 | 8 | 4.59 | Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2ccc(C(=O)Nc3nnn[nH]3)o2)c(=O)[nH]c1=S | https://pubmed.ncbi.nlm.nih.gov/15231488 | |
AR-C118925XX | 460 | None | 26 | Human | Functional | IC50 | = | 57.40 | 7.24 | - | 1 | Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay | ChEMBL | 537.2 | 5 | 3 | 8 | 4.59 | Cc1ccc2c(c1)C=Cc1cc(C)ccc1C2c1cn(Cc2ccc(C(=O)Nc3nnn[nH]3)o2)c(=O)[nH]c1=S | https://dx.doi.org/10.1016/j.ejmech.2019.111789 |
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