Assay ID | Title | Year | Journal | Article |
AID165068 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(F226A) human P2Y1 receptor in presence of MRS2179. | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID751212 | Agonist activity at human GFP-tagged P2Y11R transfected in human 1321N1 cells assessed as induction of intracellular calcium mobilization by fluorescence assay | 2013 | Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12
| Highly efficient biocompatible neuroprotectants with dual activity as antioxidants and P2Y receptor agonists. |
AID240230 | Effective concentration to activate wild-type P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID165252 | Activation of Purinoceptor P2Y1-mediated phospholipase C in turkey erythrocyte membranes | 2002 | Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
| Adenine nucleotide analogues locked in a Northern methanocarba conformation: enhanced stability and potency as P2Y(1) receptor agonists. |
AID240281 | Effective concentration to activate human Y273F mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID150470 | Evaluated for agonist activity against phospholipase C coupled P2Y purinoceptor 1 (P2Y1) of turkey erythrocytes | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
| Purine and pyrimidine (P2) receptors as drug targets. |
AID162990 | Relative half maximal velocity of Pyruvate kinase and Phosphoenolpyruvate | 1982 | Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
| Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives. |
AID240328 | Effective concentration required for the activation of human D289A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID240339 | Effective concentration required for the activation of human K196A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID165080 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(S314T) human P2Y1 receptor in presence of MRS2179 | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID240353 | Effective concentration required for the activation of human R310K mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID227598 | Ratio of Km(ADP)/Ki or Km for rat muscle pyruvate kinase | 1982 | Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
| Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives. |
AID240297 | Effective concentration to activate human Y203A (EL2) mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID165091 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(Y136A) human P2Y1 receptor. | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID165089 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(WT) human P2Y1 receptor. | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID705934 | Stability of the compound assessed as human eNPP1-mediated degradation of compound measuring increase in NMP level at pH 8.5 at 0.2 mM after 20 mins by HPLC relative to control | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification of a promising drug candidate for the treatment of type 2 diabetes based on a P2Y(1) receptor agonist. |
AID261697 | Activity against rat P2Y2-GFP transfected in HEK293 cells by intracellular calcium increase | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
| Diadenosine and diuridine poly(borano)phosphate analogues: synthesis, chemical and enzymatic stability, and activity at P2Y1 and P2Y2 receptors. |
AID1415779 | Competitive-inhibition of recombinant human N-terminal His-tagged soluble NPP1 (Val191 to Leu591 residues) expressed in mouse NSO cells using p-Nph-5'-AMP as substrate after 30 mins by capillary electrophoresis method | 2017 | MedChemComm, May-01, Volume: 8, Issue:5
| Nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) and its inhibitors. |
AID240342 | Effective concentration required for the activation of human Q307A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID1465390 | Selectivity ratio of EC50 for P2Y2 receptor K46A mutant (unknown origin) to EC50 for wild type P2Y2 receptor (unknown origin) | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Molecular Recognition of Agonists and Antagonists by the Nucleotide-Activated G Protein-Coupled P2Y |
AID240357 | Effective concentration required for the activation of human T221A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID165081 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(S314T) human P2Y1 receptor. | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID240329 | Effective concentration required for the activation of human D300A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID240350 | Effective concentration required for the activation of human R287Q mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID462461 | Activation of human P2Y1 receptor expressed in human 1321N1 cells assessed as induction of calcium flux by FLIPR assay | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Structure-activity relationship of (N)-Methanocarba phosphonate analogues of 5'-AMP as cardioprotective agents acting through a cardiac P2X receptor. |
AID240324 | Effective concentration required for the activation of human D204A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID462821 | Stability in human serum assessed as half life of hydrolysis | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| A novel insulin secretagogue based on a dinucleoside polyphosphate scaffold. |
AID475246 | Agonist activity at turkey P2Y1 receptor expressed in human 132N1 receptor assessed as induction of intracellular calcium mobilization | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| 2-MeS-beta,gamma-CCl2-ATP is a potent agent for reducing intraocular pressure. |
AID165085 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(T221A) human P2Y1 receptor. | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID234672 | Relative inhibitory potency as ratio of kidney and liver pyruvate kinases | 1982 | Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
| Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives. |
AID150330 | Accumulation of inositol phosphate in 1321N1 astrocytoma cells expressing human P2Y1 purinoceptor | 2002 | Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
| Adenine nucleotide analogues locked in a Northern methanocarba conformation: enhanced stability and potency as P2Y(1) receptor agonists. |
AID647893 | Agonist activity at turkey P2Y purinoceptor 1 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
| Boranophosphate isoster controls P2Y-receptor subtype selectivity and metabolic stability of dinucleoside polyphosphate analogues. |
AID240279 | Effective concentration to activate human Y203F mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID163119 | Relative half maximal velocity of Pyruvate kinase and Phosphoenolpyruvate | 1982 | Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
| Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives. |
AID240283 | Effective concentration to activate human Y306F mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID240294 | Effective concentration required for the activation of wild-type P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID462811 | Agonist activity at G-protein coupled P2Y1 receptor expressed in human 1321N1 cells assessed as increase in calcium by Fura2 assay | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| A novel insulin secretagogue based on a dinucleoside polyphosphate scaffold. |
AID165072 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(H277A) human P2Y1 receptor in presence of MRS2179 | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID1465393 | Selectivity ratio of EC50 for P2Y2 receptor Y303F mutant (unknown origin) to EC50 for wild type P2Y2 receptor (unknown origin) | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Molecular Recognition of Agonists and Antagonists by the Nucleotide-Activated G Protein-Coupled P2Y |
AID240334 | Effective concentration required for the activation of human F131A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID705925 | Half life in human serum at 40 mM by HPLC | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification of a promising drug candidate for the treatment of type 2 diabetes based on a P2Y(1) receptor agonist. |
AID165090 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(Y136A) human P2Y1 receptor in presence of MRS2179 (P<0.005) | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID240341 | Effective concentration required for the activation of human K280A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID242698 | Inhibition concentration required against human Y203A (EL2) mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID240326 | Effective concentration required for the activation of human D204N mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID70544 | Agonism at turkey erythrocyte P2Y receptor. | 1993 | Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
| Identification of potent, selective P2Y-purinoceptor agonists: structure-activity relationships for 2-thioether derivatives of adenosine 5'-triphosphate. |
AID240352 | Effective concentration required for the activation of human R310A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID162978 | Michaelis-Menten constant for inhibition of rat kidney pyruvate kinase (PK-K) | 1982 | Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
| Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives. |
AID165073 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(H277A) human P2Y1 receptor. | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID240331 | Effective concentration required for the activation of human E209D mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID705933 | Half life in Tris buffer at pH 9.8 at 0.2 mg by HPLC in presence of alkaline phosphatase | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification of a promising drug candidate for the treatment of type 2 diabetes based on a P2Y(1) receptor agonist. |
AID240280 | Effective concentration to activate human Y273A mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID165075 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(K280A) human P2Y1 receptor. | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID165078 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(R310K) human P2Y1 receptor in presence of MRS2179 | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID240282 | Effective concentration to activate human Y306A mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID240336 | Effective concentration required for the activation of human H132A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID1256111 | Agonist activity at GFP-tagged human P2Y11R transfected in human 1321N1 cells assessed as increase in intracellular Ca2+ level by fura 2/AM probe-based fluorescence assay | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
| Identification of Highly Promising Antioxidants/Neuroprotectants Based on Nucleoside 5'-Phosphorothioate Scaffold. Synthesis, Activity, and Mechanisms of Action. |
AID302988 | Agonist activity at P2Y1 receptor expressed in 1321N1 cells assessed as cytosolic calcium level | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
| New iantherans from the marine sponge Ianthella quadrangulata: novel agonists of the P2Y(11) receptor. |
AID240327 | Effective concentration required for the activation of human D208A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID240358 | Effective concentration required for the activation of human T222A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID240335 | Effective concentration required for the activation of human F226A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID165088 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(WT) human P2Y1 receptor in presence of MRS2179 (P<0.005) | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID167874 | Tested for relaxation of carbachol-contracted rabbit aorta at 37 degree C; Significantly more potent than 2MeSATP | 1993 | Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
| Identification of potent, selective P2Y-purinoceptor agonists: structure-activity relationships for 2-thioether derivatives of adenosine 5'-triphosphate. |
AID165079 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(R310K) human P2Y1 receptor. | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID165086 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(T222A) human P2Y1 receptor in presence of MRS2179 (P<0.005) | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID261698 | Activity against human P2Y1-GFP expressed in 1321N1 cells by intracellular calcium increase | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
| Diadenosine and diuridine poly(borano)phosphate analogues: synthesis, chemical and enzymatic stability, and activity at P2Y1 and P2Y2 receptors. |
AID240344 | Effective concentration required for the activation of human R195A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID242673 | Inhibition concentration required against human Y306F mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID165071 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(H132A) human P2Y1 receptor. | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID240323 | Effective concentration required for the activation of human C296A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID150623 | Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2r; No effect as either agonist or antagonist at 10 uM | 2002 | Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
| Adenine nucleotide analogues locked in a Northern methanocarba conformation: enhanced stability and potency as P2Y(1) receptor agonists. |
AID240354 | Effective concentration required for the activation of human S314A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID240392 | Effective concentration required for the activation of wild-type P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate is determined in separate experiment | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID165066 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(F131A) human P2Y1 receptor in presence of MRS2179 (P<0.05) | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID227596 | Ratio of Km(ADP)/Ki or Km for rat liver pyruvate kinase | 1982 | Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
| Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives. |
AID240348 | Effective concentration required for the activation of human R287E mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID240340 | Effective concentration required for the activation of human K198A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID240346 | Effective concentration required for the activation of human R285A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID240345 | Effective concentration required for the activation of human R212A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID240333 | Effective concentration required for the activation of human E209R mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID242670 | Inhibition concentration required against human Y273A mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]-MRS2279 as radioligand | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID1465392 | Selectivity ratio of EC50 for P2Y2 receptor A286W mutant (unknown origin) to EC50 for wild type P2Y2 receptor (unknown origin) | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Molecular Recognition of Agonists and Antagonists by the Nucleotide-Activated G Protein-Coupled P2Y |
AID240321 | Effective concentration required for the activation of human C124A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID1465391 | Selectivity ratio of EC50 for P2Y2 receptor R195A mutant (unknown origin) to EC50 for wild type P2Y2 receptor (unknown origin) | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Molecular Recognition of Agonists and Antagonists by the Nucleotide-Activated G Protein-Coupled P2Y |
AID1256110 | Agonist activity at GFP-tagged human P2Y1R transfected in human 1321N1 cells assessed as increase in intracellular Ca2+ level by fura 2/AM probe-based fluorescence assay | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
| Identification of Highly Promising Antioxidants/Neuroprotectants Based on Nucleoside 5'-Phosphorothioate Scaffold. Synthesis, Activity, and Mechanisms of Action. |
AID234673 | Relative inhibitory potency as ratio of muscle and liver pyruvate kinases | 1982 | Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
| Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives. |
AID240325 | Effective concentration required for the activation of human D204E mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID165082 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(S317A) human P2Y1 receptor in presence of MRS2179 | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID162985 | Michaelis-Menten constant for inhibition of pyruvate kinase obtained from rat liver (PK-L) was determined using ADP as competitive inhibitor | 1982 | Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
| Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives. |
AID150630 | Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 4; No effect as either agonist or antagonist at 10 uM | 2002 | Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
| Adenine nucleotide analogues locked in a Northern methanocarba conformation: enhanced stability and potency as P2Y(1) receptor agonists. |
AID165084 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(T221A) human P2Y1 receptor in presence of MRS2179 (P<0.005) | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID240351 | Effective concentration required for the activation of human R301A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID1415776 | Competitive-inhibition of recombinant human N-terminal His-tagged soluble NPP1 (Val191 to Leu591 residues) expressed in mouse NSO cells using ATP as substrate by capillary electrophoresis method | 2017 | MedChemComm, May-01, Volume: 8, Issue:5
| Nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) and its inhibitors. |
AID240338 | Effective concentration required for the activation of human K125A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID165083 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(S317A) human P2Y1 receptor. | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID242669 | Inhibition concentration required against human Y203F mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID462462 | Induction of calcium flux in human 1321N1 cells at 10 uM by FLIPR assay | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
| Structure-activity relationship of (N)-Methanocarba phosphonate analogues of 5'-AMP as cardioprotective agents acting through a cardiac P2X receptor. |
AID240349 | Effective concentration required for the activation of human R287K mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID261696 | Activity against rat P2Y1-GFP transfected in HEK293 cells by intracellular calcium increase | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
| Diadenosine and diuridine poly(borano)phosphate analogues: synthesis, chemical and enzymatic stability, and activity at P2Y1 and P2Y2 receptors. |
AID240332 | Effective concentration required for the activation of human E209Q mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID150321 | Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2) | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
| Purine and pyrimidine (P2) receptors as drug targets. |
AID150492 | Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 11; No effect as either agonist or antagonist at 10 uM | 2002 | Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
| Adenine nucleotide analogues locked in a Northern methanocarba conformation: enhanced stability and potency as P2Y(1) receptor agonists. |
AID373705 | Agonist activity at turkey P2Y1 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysis | 2009 | European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
| Identification of hydrolytically stable and selective P2Y(1) receptor agonists. |
AID162984 | Relative half maximal velocity of Pyruvate kinase to Phosphoenolpyruvate was determined | 1982 | Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
| Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives. |
AID242671 | Inhibition concentration required against human Y273F mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID240330 | Effective concentration required for the activation of human E209A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID240355 | Effective concentration required for the activation of human S314T mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID242607 | Inhibition concentration required against wild type strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]-MRS2279 as radioligand | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID1415778 | Competitive-inhibition of recombinant human N-terminal His-tagged soluble NPP1 (Val191 to Leu591 residues) expressed in mouse NSO cells using p-Nph-5'-TMP as substrate after 15 mins by capillary electrophoresis method | 2017 | MedChemComm, May-01, Volume: 8, Issue:5
| Nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) and its inhibitors. |
AID240347 | Effective concentration required for the activation of human R287A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID165070 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(H132A) human P2Y1 receptor in presence of MRS2179 (P<0.005) | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID165074 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(K280A) human P2Y1 receptor in presence of MRS2179 | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID165404 | Tested for relaxation of carbachol-contracted rabbit mesenteric artery at 37 degree C; Significantly more potent than 2MeSATP | 1993 | Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
| Identification of potent, selective P2Y-purinoceptor agonists: structure-activity relationships for 2-thioether derivatives of adenosine 5'-triphosphate. |
AID1850681 | Displacement of [3H]-2MesADP from recombinant human P2Y12 transfected in HEK cell membrane assessed as inhibition constant | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Strategies for targeting the P2Y |
AID165067 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(F131A) human P2Y1 receptor. | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID240322 | Effective concentration required for the activation of human C202A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID227594 | Ratio of Km(ADP)/Ki or Km for rat kidney pyruvate kinase (PK-K) | 1982 | Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
| Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives. |
AID240343 | Effective concentration required for the activation of human R128A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID240337 | Effective concentration required for the activation of human H277A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID1465394 | Selectivity ratio of EC50 for P2Y2 receptor Y306F mutant (unknown origin) to EC50 for wild type P2Y2 receptor (unknown origin) | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Molecular Recognition of Agonists and Antagonists by the Nucleotide-Activated G Protein-Coupled P2Y |
AID705929 | Agonist activity at turkey P2Y1R expressed in 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification of a promising drug candidate for the treatment of type 2 diabetes based on a P2Y(1) receptor agonist. |
AID1415777 | Competitive-inhibition of recombinant human N-terminal His-tagged soluble NPP1 (Val191 to Leu591 residues) expressed in mouse NSO cells using ATP as substrate after 30 mins by capillary electrophoresis method | 2017 | MedChemComm, May-01, Volume: 8, Issue:5
| Nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) and its inhibitors. |
AID162991 | Michaelis-Menten constant for inhibition of pyruvate kinase obtained from rat muscle (PK-M) was determined using ADP as competitive inhibitor | 1982 | Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
| Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives. |
AID165076 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(Q307A) human P2Y1 receptor in presence of MRS2179 | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID751213 | Agonist activity at human GFP-tagged P2Y1R transfected in human 1321N1 cells assessed as induction of intracellular calcium mobilization by fluorescence assay | 2013 | Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12
| Highly efficient biocompatible neuroprotectants with dual activity as antioxidants and P2Y receptor agonists. |
AID165077 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(Q307A) human P2Y1 receptor. | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID240359 | Effective concentration required for the activation of human Y136A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID705926 | Metabolic stability in human serum assessed as hydrolysis of compound at 40 mM incubated for 24 hrs measured after every 1 hr over 24 hrs by HPLC | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification of a promising drug candidate for the treatment of type 2 diabetes based on a P2Y(1) receptor agonist. |
AID165069 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(F226A) human P2Y1 receptor. | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID373709 | Dissociation constant, pKa of the compound | 2009 | European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
| Identification of hydrolytically stable and selective P2Y(1) receptor agonists. |
AID240356 | Effective concentration required for the activation of human S317A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID242672 | Inhibition concentration required against human Y306A mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
| Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. |
AID165087 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(T222A) human P2Y1 receptor. | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. |
AID1346320 | Human P2Y12 receptor (P2Y receptors) | 2001 | Molecular pharmacology, Sep, Volume: 60, Issue:3
| Molecular cloning of the platelet P2T(AC) ADP receptor: pharmacological comparison with another ADP receptor, the P2Y(1) receptor. |
AID1346309 | Human P2Y1 receptor (P2Y receptors) | 2001 | Molecular pharmacology, Sep, Volume: 60, Issue:3
| Molecular cloning of the platelet P2T(AC) ADP receptor: pharmacological comparison with another ADP receptor, the P2Y(1) receptor. |
AID1346305 | Human P2Y13 receptor (P2Y receptors) | 2003 | Molecular pharmacology, Jul, Volume: 64, Issue:1
| Pharmacological characterization of the human P2Y13 receptor. |
AID1346309 | Human P2Y1 receptor (P2Y receptors) | 1997 | British journal of pharmacology, May, Volume: 121, Issue:2
| An examination of deoxyadenosine 5'(alpha-thio)triphosphate as a ligand to define P2Y receptors and its selectivity as a low potency partial agonist of the P2Y1 receptor. |
AID1346309 | Human P2Y1 receptor (P2Y receptors) | 2002 | Molecular pharmacology, Nov, Volume: 62, Issue:5
| Quantitation of the P2Y(1) receptor with a high affinity radiolabeled antagonist. |
AID1346320 | Human P2Y12 receptor (P2Y receptors) | 2003 | Seminars in vascular medicine, May, Volume: 3, Issue:2
| P2Y12, a new platelet ADP receptor, target of clopidogrel. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |