| AID766356 | Inhibition of human recombinant CYP3A4 | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. |
| AID1153652 | Binding affinity to thromboxane A2 receptor (unknown origin) at 10 uM | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
| Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. |
| AID766343 | Antithrombotic activity in Beagle dog modified Folts model assessed as inhibition of ADP-induced platelet aggregation administered as bolus infusion measured after 30 mins | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. |
| AID1153650 | Binding affinity to P2Y1 receptor (unknown origin) at 10 uM | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
| Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. |
| AID1153646 | Toxicity in conscious dog assessed as prolongation of bleeding time at 0.02 to 8700 nmol/kg/min administered via infusion relative to control | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
| Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. |
| AID766347 | In vivo antithrombotic activity in Beagle dog modified Folts model assessed as increase in blood flow administered as bolus infusion measured after 30 mins | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. |
| AID1866084 | Antagonist activity at P2Y12 receptor in human platelet rich plasma | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Structural modification aimed for improving solubility of lead compounds in early phase drug discovery. |
| AID766362 | Lipophilicity, log D of the compound at pH 6.8 by chromatographic method | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. |
| AID766361 | Kinetic solubility of the compound at pH 6.8 after 16 hrs by LC-UV/MS analysis | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. |
| AID766340 | Antagonist activity at P2Y12 receptor in human whole blood assessed as inhibition of ADP-induced platelet aggregation after 5 mins by residual platelet count assay | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. |
| AID1153654 | Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 30 seconds | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
| Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. |
| AID766341 | Antagonist activity at P2Y12 receptor (unknown origin) expressed in CHO cell membrane by [35S]GTPgammaS binding assay | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. |
| AID1153655 | Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 60 seconds | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
| Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. |
| AID1153644 | Antithrombotic activity in conscious dog assessed as inhibition of platelet aggregation administered via infusion | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
| Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. |
| AID766358 | Dissociation constant, pKa of the compound | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. |
| AID766352 | Clearance in Beagle dog at 3 mg/kg, iv | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. |
| AID766346 | Toxicity in Beagle dog modified Folts model assessed as dose required to increase in bleeding time by 3.5 fold compound administered as bolus infusion | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. |
| AID1153636 | Half life in human liver microsomes at 1 mg/ml | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
| Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. |
| AID1866020 | Thermodynamic aqueous solubility of the compound | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Structural modification aimed for improving solubility of lead compounds in early phase drug discovery. |
| AID1153647 | Antithrombotic activity in dog Folt's model of arterial thrombosis assessed as inhibition of platelet aggregation | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
| Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. |
| AID766349 | Half life in Beagle dog at 2 mg/kg, po | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. |
| AID766345 | Therapeutic index, ratio of ED50 for antithrombotic activity in Beagle dog modified Folts model to dose required to increase in bleeding time by 3.5 fold in Beagle dog modified Folts model | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. |
| AID766355 | Plasma protein binding in dog assessed as fraction unbound level by equilibrium dialysis method | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. |
| AID1153649 | Toxicity in dog Folt's model of arterial thrombosis assessed as prolongation of bleeding time at 0.001 to 0.1 umol/kg/min | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
| Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. |
| AID766359 | Intrinsic clearance in dog liver microsomes by LC/MS analysis | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. |
| AID1153653 | Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 10 seconds | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
| Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. |
| AID1153656 | Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 60 mins | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
| Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. |
| AID1153635 | Antagonist activity P2Y12 receptor in human blood assessed as inhibition of ADP-induced platelet aggregation measured as residual platelet count after 5 mins by flow cytometric analysis | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
| Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. |
| AID1153642 | Half life in Beagle dog at 1 umol/kg, iv | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
| Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. |
| AID1153634 | Antagonist activity at P2Y12 receptor (unknown origin) assessed as inhibition of ADP-induced [35S]GTPgammaS binding after 45 mins by scintillation counting analysis | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
| Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. |
| AID1153638 | Lipophilicity, log D of the compound at pH 7.4 by HPLC analysis | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
| Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. |
| AID1153657 | Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
| Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. |
| AID1153651 | Binding affinity to PAF receptor (unknown origin) at 10 uM | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
| Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. |
| AID766357 | Inhibition of human recombinant CYP2C9 | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. |
| AID1153643 | AUC in Beagle dog at 1 umol/kg, iv | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
| Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. |
| AID766342 | Displacement of [125I]-AZ11931285 from P2Y12 receptor (unknown origin) expressed in CHO cell membrane after 1 hr by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. |
| AID1153637 | Apparent permeability from apical to basolateral side in human Caco2 cells at 10 uM at pH 7.4 after 60 mins by LC-MS analysis | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
| Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. |
| AID766360 | Permeability across apical to basolateral side in human Caco2 cells by LC/MS analysis | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. |
| AID1153641 | Fraction unbound in Beagle dog plasma at 37 degC after 18 hrs by equilibrium dialysis technique | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
| Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. |
| AID766351 | Oral bioavailability in Beagle dog at 2 mg/kg | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. |
| AID1153640 | Antagonist activity P2Y12 receptor in human washed platelets assessed as inhibition of ADP-induced platelet aggregation after 5 to 90 mins by spectrophotometric analysis | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
| Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2014 | Nature, May-01, Volume: 509, Issue:7498
| Structure of the human P2Y12 receptor in complex with an antithrombotic drug. |
| AID1346320 | Human P2Y12 receptor (P2Y receptors) | 2013 | Future medicinal chemistry, Nov, Volume: 5, Issue:17
| 5-alkyl-1,3-oxazole derivatives of 6-amino-nicotinic acids as alkyl ester bioisosteres are antagonists of the P2Y12 receptor. |
| AID1346320 | Human P2Y12 receptor (P2Y receptors) | 2014 | Nature, May-01, Volume: 509, Issue:7498
| Structure of the human P2Y12 receptor in complex with an antithrombotic drug. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |