| Assay ID | Title | Year | Journal | Article |
|---|
| AID1138020 | Selectivity ratio of Ki for human recombinant adenosine A1 receptor to Ki for human recombinant adenosine receptor A2a | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
| Adenosine A2A receptor as a drug discovery target. |
| AID306068 | Antagonist activity at rat adenosine A2A receptor assessed as CGS 21680-induced inhibition of adenylate cyclase activity by cell-based assay | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines. |
| AID607232 | Inverse agonist activity at human adenosine receptor A2a S277A'7.42 mutant expressed in HEK293 cells followed by receptor capturing on Biocore chips assessed as log difference in receptor affinity by SPR method relative to wild type stabilized A2A recepto | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Biophysical mapping of the adenosine A2A receptor. |
| AID1138024 | Inhibition of human recombinant adenosine A1 receptor | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
| Adenosine A2A receptor as a drug discovery target. |
| AID1854970 | Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in HEK293 cell membrane incubated for 1 hr by microplate beta scintillation counting based radioligand inhibition assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | High ligand efficiency quinazoline compounds as novel A |
| AID1138042 | AUC in rat at 3 mg/kg, po | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
| Adenosine A2A receptor as a drug discovery target. |
| AID569674 | Inhibition of recombinant CYP2D6 after 45 mins | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3
| Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| AID1138051 | Anticataleptic activity in rat assessed as minimum efficacious dose after 1 hr | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
| Adenosine A2A receptor as a drug discovery target. |
| AID1810549 | Displacement of [3H]MSX-2 from human recombinant adenosine A2A receptor expressed in CHO cells by liquid scintillation counting analysis | | | |
| AID747680 | Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones. |
| AID1138046 | Anticataleptic activity in rat assessed as inhibition at 1 mg/kg, po after 4 hrs | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
| Adenosine A2A receptor as a drug discovery target. |
| AID1171839 | Reversal of 1.5 mg/kg haloperidol-induced catalepsy in Sprague-Dawley rat at 30 mg/kg, ip | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
| Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): a novel, CNS penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM). |
| AID312872 | Solubility in PBS at pH 7.4 | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
| Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy. |
| AID1138025 | Inhibition of human recombinant adenosine A3 receptor | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
| Adenosine A2A receptor as a drug discovery target. |
| AID306070 | Reversal of haloperidol-induced catalepsy in orally dosed rat after 1 hr | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines. |
| AID569676 | Displacement of [3H]-DPCPX from human adenosine A1 receptor expressed in CHO cells at 200 nM after 30 mins by scintillation counting | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3
| Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| AID607203 | Binding affinity at human adenosine receptor A2a I66A'2.64 mutant expressed in HEK293 cells followed by receptor capturing on Biocore chips assessed as log difference in receptor affinity by SPR method relative to wild type stabilized A2A receptor | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Biophysical mapping of the adenosine A2A receptor. |
| AID1061809 | Inhibition of adenosine A2A receptor (unknown origin) at 100 umol/L relative to control | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
| Replacement of amide with bioisosteres led to a new series of potent adenosine A2A receptor antagonists. |
| AID1810548 | Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells by liquid scintillation counting analysis | | | |
| AID569664 | Displacement of [3H]-ZM241385 from human adenosine A2A receptor expressed in high five cells after 30 mins by scintillation counting | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3
| Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| AID367121 | Inhibition of haloperidol-induced catalepsy in rat at 1 mg/kg, po after 1 hr | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
| Potent and selective adenosine A2A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines. |
| AID306071 | Binding affinity to human adenosine A1 receptor | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines. |
| AID1370514 | Cytotoxicity against human A549 cells assessed as cell viability at 0.1 uM by MTT assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
| Identification of novel small-molecule inhibitors of Zika virus infection. |
| AID1138045 | Anticataleptic activity in rat assessed as inhibition at 1 mg/kg, po after 1 hr | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
| Adenosine A2A receptor as a drug discovery target. |
| AID501545 | Reversal of haloperidol-induced hypolocomotion in po dosed NMRI mouse model of Parkinson's disease measured for 20 mins | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists. |
| AID1138047 | Oral bioavailability in rat | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
| Adenosine A2A receptor as a drug discovery target. |
| AID747682 | Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones. |
| AID1061810 | Displacement of [3H]-ZM241385 from human adenosine A2A receptor expressed in HEK293 cells | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
| Replacement of amide with bioisosteres led to a new series of potent adenosine A2A receptor antagonists. |
| AID1370515 | Cytotoxicity against human A549 cells assessed as cell viability at 1 uM by MTT assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
| Identification of novel small-molecule inhibitors of Zika virus infection. |
| AID501540 | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells by liquid scintillation counting | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists. |
| AID1696210 | Displacement of [3H]SCH58261 from human adenosine 2A receptor expressed in HEK293 cell membranes incubated for 1.5 hrs by radioligand competition binding assay | | | |
| AID1871328 | Antagonist activity at adenosine A2A receptor (unknown origin) | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Adenosine receptor antagonists: Recent advances and therapeutic perspective. |
| AID1138052 | Anticataleptic activity in rat assessed as minimum efficacious dose after 4 hrs | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
| Adenosine A2A receptor as a drug discovery target. |
| AID367125 | Inhibition of haloperidol-induced catalepsy in rat at 0.1 mg/kg, po after 1 hr | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
| Potent and selective adenosine A2A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines. |
| AID306064 | Inhibition of haloperidol-induced catalepsy in rat at 1 mg/kg, po after 4 hrs | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines. |
| AID1138021 | Inhibition of human recombinant adenosine receptor A2b | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
| Adenosine A2A receptor as a drug discovery target. |
| AID747683 | Displacement of [3H]MSX2 from adenosine A2A receptor in rat brain striatal membranes after 30 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones. |
| AID1138050 | Ratio of drug level from brain to plasma in rat | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
| Adenosine A2A receptor as a drug discovery target. |
| AID589726 | Aqueous solubility of the compound at pH 5.1 | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8
| Potent and selective adenosine A(2A) receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones. |
| AID607198 | Displacement of [3H]ZM241385 from stabilized human adenosine receptor A2a expressed in HEK293 cells followed by receptor capturing on Biocore chips by SPR method | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Biophysical mapping of the adenosine A2A receptor. |
| AID1696185 | Selectivity ratio of Ki for human adenosine A1 receptor to Ki for human Adenosine 2A receptor | | | |
| AID747679 | Displacement of [3H]PSB-11 from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones. |
| AID747684 | Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membranes after 90 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones. |
| AID306067 | Selectivity of human adenosine A2A receptor over human adenosine A3 receptor | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines. |
| AID501542 | Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in buculovirus system by liquid scintillation counting | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists. |
| AID1370513 | Antiviral activity against Zika virus infected in human A549 cells preincubated for 5 hrs followed by compound wash measured after 48 hrs by viral plague-forming assay | 2018 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
| Identification of novel small-molecule inhibitors of Zika virus infection. |
| AID306073 | Binding affinity to human adenosine A3 receptor | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines. |
| AID1696236 | Selectivity ratio of Ki for human adenosine 2B receptor expressed in HEK293 cells to Ki for human adenosine 2A receptor expressed in HEK293 cells | | | |
| AID589721 | Inhibition of haloperidol -induced catalepsy in rat at 10 mg/kg, po measured after 4 hrs | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8
| Potent and selective adenosine A(2A) receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones. |
| AID367122 | Inhibition of haloperidol-induced catalepsy in rat at 1 mg/kg, po after 4 hrs | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
| Potent and selective adenosine A2A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines. |
| AID747681 | Displacement of [3H]MSX2 from human recombinant adenosine A2A receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones. |
| AID501544 | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells at 2000 nM by liquid scintillation counting | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists. |
| AID1696186 | Selectivity ratio of Ki for human adenosine A3 receptor to Ki for human Adenosine 2A receptor | | | |
| AID607202 | Binding affinity at human adenosine receptor A2a receptor Y271A'7.36 mutant expressed in HEK293 cells followed by receptor capturing on Biocore chips assessed as log difference in receptor affinity by SPR method relative to wild type stabilized A2A recept | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Biophysical mapping of the adenosine A2A receptor. |
| AID306083 | Solubility in 0.01 N Hcl | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines. |
| AID306062 | Selectivity of human adenosine A2A receptor over human adenosine A1 receptor | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines. |
| AID306063 | Inhibition of haloperidol-induced catalepsy in rat at 1 mg/kg, po after 1 hr | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines. |
| AID589720 | Inhibition of haloperidol -induced catalepsy in rat at 10 mg/kg, po measured after 1 hr | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8
| Potent and selective adenosine A(2A) receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones. |
| AID1370517 | Cytotoxicity against human A549 cells assessed as cell viability at 100 uM by MTT assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
| Identification of novel small-molecule inhibitors of Zika virus infection. |
| AID569670 | Efflux ratio of permeability from apical to basolateral over basolateral to apical side in human Caco2 cells after 21 to 28 days by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3
| Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| AID607200 | Binding affinity at human adenosine receptor A2a L167A'extracellular loop 2 mutant expressed in HEK293 cells followed by receptor capturing on Biocore chips assessed as log difference in receptor affinity by SPR method relative to wild type stabilized A2A | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Biophysical mapping of the adenosine A2A receptor. |
| AID569703 | Reversal of haloperidol-induced hypolocomotion in po dosed NMRI mouse administered 30 mins before haloperidol challenge measured for 20 mins | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3
| Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| AID367124 | Inhibition of haloperidol-induced catalepsy in rat at 0.3 mg/kg, po after 4 hrs | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
| Potent and selective adenosine A2A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines. |
| AID367126 | Inhibition of haloperidol-induced catalepsy in rat at 0.1 mg/kg, po after 4 hrs | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
| Potent and selective adenosine A2A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines. |
| AID607199 | Binding affinity at stabilized human adenosine receptor A2a L85A'3.33 mutant expressed in HEK293 cells followed by receptor capturing on Biocore chips assessed as log difference in receptor affinity by SPR method relative to wild type stabilized A2A recep | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Biophysical mapping of the adenosine A2A receptor. |
| AID306072 | Binding affinity to human adenosine A2B receptor | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines. |
| AID589725 | Solubility of the compound at pH 7.4 | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8
| Potent and selective adenosine A(2A) receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones. |
| AID1138048 | Half life in rat at 1 mg/kg, iv | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
| Adenosine A2A receptor as a drug discovery target. |
| AID1402799 | Antagonist activity at adenosine A2A receptor (unknown origin) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Antagonists of the adenosine A |
| AID1575642 | Antagonist activity at human adenosine A2A receptor | | | |
| AID607231 | Binding affinity at human adenosine receptor A2a N181A'5.42 mutant expressed in HEK293 cells followed by receptor capturing on Biocore chips assessed as log difference in receptor affinity by SPR method relative to wild type stabilized A2A receptor | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Biophysical mapping of the adenosine A2A receptor. |
| AID569673 | Inhibition of recombinant CYP2C19 after 45 mins | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3
| Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| AID1370516 | Cytotoxicity against human A549 cells assessed as cell viability at 10 uM by MTT assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
| Identification of novel small-molecule inhibitors of Zika virus infection. |
| AID1138023 | Inhibition of human recombinant adenosine receptor A2a | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
| Adenosine A2A receptor as a drug discovery target. |
| AID607201 | Binding affinity at human adenosine receptor A2a M177A'5.38 mutant expressed in HEK293 cells followed by receptor capturing on Biocore chips assessed as log difference in receptor affinity by SPR method relative to wild type stabilized A2A receptor | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Biophysical mapping of the adenosine A2A receptor. |
| AID367123 | Inhibition of haloperidol-induced catalepsy in rat at 0.3 mg/kg, po after 1 hr | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
| Potent and selective adenosine A2A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines. |
| AID306066 | Selectivity of human adenosine A2A receptor over human adenosine A2B receptor | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines. |
| AID306065 | Binding affinity to rat adenosine A2A receptor | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines. |
| AID1138049 | Plasma clearance in rat | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
| Adenosine A2A receptor as a drug discovery target. |
| AID1370518 | Antiviral activity against Zika virus infected in human A549 cells assessed as virus titer preincubated for 5 hrs followed by compound wash measured after 48 hrs by viral plague-forming assay | 2018 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
| Identification of novel small-molecule inhibitors of Zika virus infection. |
| AID306082 | Solubility in water at pH 5.1 | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines. |
| AID306061 | Binding affinity to human adenosine A2A receptor | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines. |
| AID1810550 | Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells by liquid scintillation counting analysis | | | |
| AID569669 | Apparent permeability across human Caco2 cell membrane after 21 to 28 days by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3
| Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| AID1810551 | Displacement of [3H]PSB-11 from human recombinant adenosine A3 receptor expressed in CHO cells by liquid scintillation counting analysis | | | |
| AID569671 | Inhibition of recombinant CYP1A2 after 28 mins | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3
| Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| AID569668 | Intrinsic clearance in rat liver microsomes at 1 uM after 60 mins by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3
| Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| AID569667 | Intrinsic clearance in human liver microsomes at 1 uM after 60 mins by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3
| Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| AID306069 | Antagonist activity at human adenosine A2A receptor assessed as CGS 21680-induced inhibition of adenylate cyclase activity by cell-based assay | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines. |
| 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. |
| 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. |
| 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. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1345685 | Human A1 receptor (Adenosine receptors) | 2007 | Recent patents on CNS drug discovery, Jan, Volume: 2, Issue:1
| Blocking striatal adenosine A2A receptors: a new strategy for basal ganglia disorders. |
| AID1345822 | Human A3 receptor (Adenosine receptors) | 2007 | Recent patents on CNS drug discovery, Jan, Volume: 2, Issue:1
| Blocking striatal adenosine A2A receptors: a new strategy for basal ganglia disorders. |
| AID1345618 | Human A2A receptor (Adenosine receptors) | 2007 | Recent patents on CNS drug discovery, Jan, Volume: 2, Issue:1
| Blocking striatal adenosine A2A receptors: a new strategy for basal ganglia disorders. |
| AID1345721 | Human A2B receptor (Adenosine receptors) | 2007 | Recent patents on CNS drug discovery, Jan, Volume: 2, Issue:1
| Blocking striatal adenosine A2A receptors: a new strategy for basal ganglia disorders. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |