Assay ID | Title | Year | Journal | Article |
AID1345822 | Human A3 receptor (Adenosine receptors) | 2006 | Nature reviews. Drug discovery, Mar, Volume: 5, Issue:3
| Adenosine receptors as therapeutic targets. |
AID1345721 | Human A2B receptor (Adenosine receptors) | 2000 | Molecular pharmacology, Dec, Volume: 58, Issue:6
| Why are A(2B) receptors low-affinity adenosine receptors? Mutation of Asn273 to Tyr increases affinity of human A(2B) receptor for 2-(1-Hexynyl)adenosine. |
AID1345685 | Human A1 receptor (Adenosine receptors) | 1999 | Naunyn-Schmiedeberg's archives of pharmacology, Jan, Volume: 359, Issue:1
| Comparison of CGS 15943, ZM 241385 and SCH 58261 as antagonists at human adenosine receptors. |
AID1345618 | Human A2A receptor (Adenosine receptors) | 1999 | Biochemical pharmacology, Jan-01, Volume: 57, Issue:1
| Differences in the order of potency for agonists but not antagonists at human and rat adenosine A2A receptors. |
AID1345685 | Human A1 receptor (Adenosine receptors) | 2006 | Nature reviews. Drug discovery, Mar, Volume: 5, Issue:3
| Adenosine receptors as therapeutic targets. |
AID1345685 | Human A1 receptor (Adenosine receptors) | 1994 | The Journal of biological chemistry, Jan-28, Volume: 269, Issue:4
| A threonine residue in the seventh transmembrane domain of the human A1 adenosine receptor mediates specific agonist binding. |
AID1345618 | Human A2A receptor (Adenosine receptors) | 1997 | British journal of pharmacology, Jun, Volume: 121, Issue:3
| Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261. |
AID1345721 | Human A2B receptor (Adenosine receptors) | 2006 | Nature reviews. Drug discovery, Mar, Volume: 5, Issue:3
| Adenosine receptors as therapeutic targets. |
AID1345618 | Human A2A receptor (Adenosine receptors) | 1999 | Naunyn-Schmiedeberg's archives of pharmacology, Jan, Volume: 359, Issue:1
| Comparison of CGS 15943, ZM 241385 and SCH 58261 as antagonists at human adenosine receptors. |
AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection | 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. |
AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500
| Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
| Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID588378 | qHTS for Inhibitors of ATXN expression: Validation | | | |
AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500
| Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7
| A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7
| A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | | | |
AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7
| Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7
| Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7
| Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500
| Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1347151 | Optimization of GU AMC 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. |
AID1810051 | Inhibition of HDAC1 (unknown origin) assessed as release of 7-amino-4-methylcoumarin incubated in room temperature for 15 min measured by Spectra max microtitre plate reader | | | |
AID1810015 | Displacement of [3H]DPCPX from human adenosine A1 receptor membrane (unknown origin) measured after 60 mins by scintillation counting analysis | | | |
AID1871401 | Binding affinity to human adenosine A2A receptor assessed as apparent first-order rate constant(kobs) | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Adenosine receptor antagonists: Recent advances and therapeutic perspective. |
AID476441 | Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by rapid filtration assay | 2010 | Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
| Novel 8-(furan-2-yl)-3-substituted thiazolo [5,4-e][1,2,4] triazolo[1,5-c] pyrimidine-2(3H)-thione derivatives as potential adenosine A(2A) receptor antagonists. |
AID281575 | Displacement of [3h]DPCPX from adenosine A receptor in rat cerebral cortex membrane | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
| Novel bicyclic piperazine derivatives of triazolotriazine and triazolopyrimidines as highly potent and selective adenosine A2A receptor antagonists. |
AID33611 | Displacement of [3H]-CGS- 21680 from rat striatal membrane adenosine A2B receptor | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
| Design, synthesis, and biological evaluation of C9- and C2-substituted pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists. |
AID34890 | Displacement of specific [3H]MRE3008-F20 binding at human adenosine A3 receptor expressed in CHO cells. | 2002 | Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
| 7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility. |
AID1873116 | Antagonist activity at adenosine A1 receptor (unknown origin) | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Discovery of small-molecule compounds and natural products against Parkinson's disease: Pathological mechanism and structural modification. |
AID1871385 | Effect of compound in haloperidol-induced catalepsy in Swiss albino male mouse assessed as catalepsy score after 120 mins | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Adenosine receptor antagonists: Recent advances and therapeutic perspective. |
AID30442 | Binding affinity against adenosine A1 receptor in human cortical membranes using [3H]CHA as radioligand | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
| Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives. |
AID637450 | Displacement of [3H]-DPCPX from human adenosine A1 receptor expressed in CHO cells after 120 mins by liquid scintillation counting | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
| Pyrrolo- and pyrazolo-[3,4-e][1,2,4]triazolo[1,5-c]pyrimidines as adenosine receptor antagonists. |
AID1810014 | Displacement of [3H]DPCPX from human adenosine A2B receptor membrane (unknown origin) measured after 60 mins by scintillation counting analysis | | | |
AID343727 | Antagonist activity at human adenosine A2A receptor | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Biaryl and heteroaryl derivatives of SCH 58261 as potent and selective adenosine A2A receptor antagonists. |
AID33931 | Displacement [3H]-CGS-21,680 from Adenosine A2A receptor in rat striatal membrane. | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
| Tetrahydrobenzothiophenone derivatives as a novel class of adenosine receptor antagonists. |
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. |
AID234767 | Selectivity for A1 and A2A adenosine receptors in rat | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
| Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists. |
AID239479 | Binding affinity against Adenosine A2a receptor from rat brain tissue was determined using [3H]ZM-241385 as radioligand | 2004 | Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19
| Studies on adenosine A2a receptor antagonists: comparison of three core heterocycles. |
AID32887 | Displacement of [3H]-CGS- 21680 from rat striatal membrane Adenosine A2A receptor | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
| Design, synthesis, and biological evaluation of C9- and C2-substituted pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists. |
AID33296 | Displacement of specific [3H]DPCPX binding at human adenosine A2B receptor expressed in HEK293 cells. | 2002 | Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
| 7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility. |
AID767603 | Inhibition of haloperidol-induced catalepsy in Swiss albino mouse at 10 mg/kg, ip administered 30 mins prior haloperidol challenge measured after 120 mins | 2013 | Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
| Design and synthesis of (4E)-4-(4-substitutedbenzylideneamino)-3-substituted-2,3-dihydro-2-thioxothiazole-5-carbonitrile as novel A2A receptor antagonists. |
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. |
AID239096 | Inhibition of [3H]ZM-241,385 binding to rat brain adenosine A2a receptor | 2004 | Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
| Piperazine derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists. |
AID239189 | Inhibition of [3H]ZM-241385 binding to adenosine A2a receptor of rat brain tissue | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Novel diamino derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists. |
AID31077 | Displacement of [3H]CHA from human Adenosine A1 receptor expressed in CHO cells | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
| Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists. |
AID32350 | Inhibition of [3H]-CHA binding to Adenosine A1 receptor in rat whole brain homogenates. | 1996 | Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5
| Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives: potent and selective A(2A) adenosine antagonists. |
AID33059 | Selectivity ratio of human adenosine A3 receptor to human adenosine A2A receptor. | 2002 | Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
| 7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility. |
AID763042 | Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting analysis | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Fluorescent ligands for adenosine receptors. |
AID476444 | Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced intracellular cAMP accumulation at 100 nM after 24 hrs (Rvb= 0.40 pmol/ml) | 2010 | Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
| Novel 8-(furan-2-yl)-3-substituted thiazolo [5,4-e][1,2,4] triazolo[1,5-c] pyrimidine-2(3H)-thione derivatives as potential adenosine A(2A) receptor antagonists. |
AID343334 | Selectivity for human adenosine A2A receptor over human adenosine A1 receptor | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Design, synthesis, and evaluation of fused heterocyclic analogs of SCH 58261 as adenosine A2A receptor antagonists. |
AID32340 | Displacement of [3H]CHA from rat cortical membrane Adenosine A1 receptor | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
| Design, synthesis, and biological evaluation of C9- and C2-substituted pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists. |
AID343728 | Selectivity for human adenosine A2A receptor over human adenosine A1 receptor | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Biaryl and heteroaryl derivatives of SCH 58261 as potent and selective adenosine A2A receptor antagonists. |
AID33603 | Selectivity ratio of human adenosine A2B receptor to human adenosine A2A receptor. | 2002 | Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
| 7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility. |
AID231273 | Ratio of binding affinity against bovine adenosine A1 to that of A2 receptor | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
| Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives. |
AID1810049 | Antiproliferative activity against mouse CT26 cells measured after 72 hrs by CCK8 assay | | | |
AID239503 | Inhibition constant against human Adenosine A2a receptor using [3H]-SCH- 58261 as radioligand expressed in HEK cell membranes | 2005 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
| 6-(2-Furanyl)-9H-purin-2-amine derivatives as A2A adenosine antagonists. |
AID34235 | Binding affinity against human Adenosine A2a receptor (hA2a) | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
| Comparison of inhibitory activity of isomeric triazolopyridine derivatives towards adenosine receptor subtypes or do similar structures reveal similar bioactivities? |
AID1871353 | Effect of compound in haloperidol and NECA-induced catalepsy in mouse assessed as catalepsy score at 10 mg/kg measured after 120 mins | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Adenosine receptor antagonists: Recent advances and therapeutic perspective. |
AID239213 | Inhibition of [3H]DPCPX binding to rat cerebral cortex adenosine A1 receptor | 2004 | Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
| Piperazine derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists. |
AID224014 | Inhibition of the effects of NECA on ADP (5 uM)-induced rabbit platelet aggregation. | 1996 | Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5
| Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives: potent and selective A(2A) adenosine antagonists. |
AID239464 | Binding affinity against Adenosine A1 receptor from rat cerebral cortex was determined using [3H]DPCPX as radioligand | 2004 | Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19
| Studies on adenosine A2a receptor antagonists: comparison of three core heterocycles. |
AID235153 | Selectivity for A1 and A2A receptors | 1996 | Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5
| Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives: potent and selective A(2A) adenosine antagonists. |
AID234927 | Selectivity for human A3 adenosine receptor and human A2A adenosine receptor | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
| Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists. |
AID1696176 | Inhibition of human adenosine 2B receptor | | | |
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. |
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. |
AID1810012 | Displacement of [3H]DPCPX from human adenosine A3 receptor membrane (unknown origin) measured after 60 mins by scintillation counting analysis | | | |
AID234926 | Selectivity for human A1 adenosine receptor and human A2A adenosine receptor | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
| Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists. |
AID343333 | Antagonist activity at human adenosine A2A receptor | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Design, synthesis, and evaluation of fused heterocyclic analogs of SCH 58261 as adenosine A2A receptor antagonists. |
AID1696175 | Antagonist activity at human adenosine 2A receptor | | | |
AID31085 | Selectivity ratio of human adenosine A1 receptor to human adenosine A2A receptor. | 2002 | Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
| 7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility. |
AID32516 | Displacement of [3H]CHA from rat cortical membrane Adenosine A1 receptor. Parenthesis indicate 95% confidence limit. | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
| Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists. |
AID30443 | Binding affinity against human Adenosine A1 receptor | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
| Comparison of inhibitory activity of isomeric triazolopyridine derivatives towards adenosine receptor subtypes or do similar structures reveal similar bioactivities? |
AID476443 | Selectivity ratio of Ki for human adenosine A1 receptor to Ki for human adenosine A2A receptor | 2010 | Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
| Novel 8-(furan-2-yl)-3-substituted thiazolo [5,4-e][1,2,4] triazolo[1,5-c] pyrimidine-2(3H)-thione derivatives as potential adenosine A(2A) receptor antagonists. |
AID763043 | Competitive binding affinity to human adenosine A2A receptor expressed in HEK293 cells after 60 mins by fluorescence polarization assay in presence of MRS5346 | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Fluorescent ligands for adenosine receptors. |
AID244230 | Selectivity as the ratio of inhibition constants of human adenosine A1 receptor to that of human adenosine A2A receptor | 2005 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
| 6-(2-Furanyl)-9H-purin-2-amine derivatives as A2A adenosine antagonists. |
AID281574 | Displacement of [3H]ZM241385 from adenosine A2A receptor in rat brain membrane | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
| Novel bicyclic piperazine derivatives of triazolotriazine and triazolopyrimidines as highly potent and selective adenosine A2A receptor antagonists. |
AID34373 | Displacement of specific [3H]-SCH- 58261 binding at human Adenosine A2A receptor expressed in HEK293 cells. | 2002 | Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
| 7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility. |
AID33934 | Inhibition of [3H]-CGS- 21680 binding to Adenosine A2A receptor in rat striatal homogenates. | 1996 | Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5
| Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives: potent and selective A(2A) adenosine antagonists. |
AID30795 | Binding affinity against adenosine A2 receptor in human striatal membranes using [3H]CGS-21680 as radioligand | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
| Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives. |
AID239020 | Binding affinity towards Adenosine A2A receptor of rat brain tissues using [3H]ZM-241385 as radioligand | 2005 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3
| Synthesis of alkyne derivatives of a novel triazolopyrazine as A(2A) adenosine receptor antagonists. |
AID1873115 | Antagonist activity at adenosine A2A receptor (unknown origin) | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Discovery of small-molecule compounds and natural products against Parkinson's disease: Pathological mechanism and structural modification. |
AID31983 | Binding affinity against adenosine A1 receptor in bovine cortical membranes using [3H]CHA as radioligand | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
| Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives. |
AID30473 | Displacement of specific [3H]DPCPX binding at human Adenosine A1 receptor expressed in CHO cells. | 2002 | Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
| 7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility. |
AID767609 | Antagonist activity at human A2A receptor expressed in HEK293 cells assessed as decrease in NECA-induced cAMP release at 1 uM after 15 mins | 2013 | Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
| Design and synthesis of (4E)-4-(4-substitutedbenzylideneamino)-3-substituted-2,3-dihydro-2-thioxothiazole-5-carbonitrile as novel A2A receptor antagonists. |
AID254299 | Binding affinity towards adenosine A2A receptor | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
| Synthesis of [1,2,4]triazolo[1,5-a]pyrazines as adenosine A2A receptor antagonists. |
AID239210 | Inhibition of [3H]DPCPX binding to adenosine A1 receptor of rat cerebral cortex | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Novel diamino derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists. |
AID34881 | Displacement of [3H]-AB MECA from human Adenosine A3 receptor expressed in HEK293 cells | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
| Design, synthesis, and biological evaluation of C9- and C2-substituted pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists. |
AID1810050 | Antiproliferative activity against mouse MC38 cells measured after 72 hrs by CCK8 assay | | | |
AID239133 | Binding affinity against Adenosine A2a receptor determined using [3H]ZM-241385 as radioligand | 2004 | Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19
| Triamino derivatives of triazolotriazine and triazolopyrimidine as adenosine A2a receptor antagonists. |
AID1810053 | Displacement of [3H]SCH58261 from adenosine A2A receptor membrane (unknown origin) measured after 60 mins by scintillation counting analysis | | | |
AID637479 | Displacement of [3H]-MRE-3008-F20 from human adenosine A3 receptor expressed in CHO cells after 120 mins by liquid scintillation counting | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
| Pyrrolo- and pyrazolo-[3,4-e][1,2,4]triazolo[1,5-c]pyrimidines as adenosine receptor antagonists. |
AID33046 | Displacement of [125I]AB-MECA from human Adenosine A3 receptor expressed in HEK293 cells | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
| Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists. |
AID1138081 | Binding affinity to adenosine receptor A2a in rat striatum | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
| Adenosine A2A receptor as a drug discovery target. |
AID1810052 | Inhibition of HDAC6 (unknown origin) assessed as release of 7-amino-4-methylcoumarin incubated in room temperature for 15 min measured by Spectra max microtitre plate reader | | | |
AID365580 | Binding affinity to human adenosine A2A receptor | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| 2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists. |
AID476442 | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in HEK293 cells after 60 mins by rapid filtration assay | 2010 | Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
| Novel 8-(furan-2-yl)-3-substituted thiazolo [5,4-e][1,2,4] triazolo[1,5-c] pyrimidine-2(3H)-thione derivatives as potential adenosine A(2A) receptor antagonists. |
AID637491 | Displacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
| Pyrrolo- and pyrazolo-[3,4-e][1,2,4]triazolo[1,5-c]pyrimidines as adenosine receptor antagonists. |
AID767604 | Inhibition of haloperidol-induced catalepsy in Swiss albino mouse at 5 to 20 mg/kg, ip administered 30 mins prior haloperidol challenge measured after 120 mins | 2013 | Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
| Design and synthesis of (4E)-4-(4-substitutedbenzylideneamino)-3-substituted-2,3-dihydro-2-thioxothiazole-5-carbonitrile as novel A2A receptor antagonists. |
AID436525 | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
| Combining selectivity and affinity predictions using an integrated Support Vector Machine (SVM) approach: An alternative tool to discriminate between the human adenosine A(2A) and A(3) receptor pyrazolo-triazolo-pyrimidine antagonists binding sites. |
AID637451 | Displacement of [3H]-ZM 241385 from human adenosine A2A receptor expressed in CHO cells after 60 mins by liquid scintillation counting | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
| Pyrrolo- and pyrazolo-[3,4-e][1,2,4]triazolo[1,5-c]pyrimidines as adenosine receptor antagonists. |
AID93148 | Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
| Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists. |
AID34843 | Displacement of [3H]-SCH- 58261 from human Adenosine A2A receptor expressed in CHO cells | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
| Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists. |
AID234928 | Selectivity for human A3 adenosine receptor and rat A2A adenosine receptor | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
| Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists. |
AID238943 | Binding affinity towards Adenosine A1 receptor of rat cerebral cortex using [3H]-DPCPX as radioligand | 2005 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3
| Synthesis of alkyne derivatives of a novel triazolopyrazine as A(2A) adenosine receptor antagonists. |
AID30487 | Binding affinity against adenosine A2 receptor in bovine striatal membranes using [3H]-CGS-21,680 as radioligand | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
| Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives. |
AID239465 | Binding affinity against Adenosine A1 receptor from rat cerebral cortex was determined using [3H]DPCPX as radioligand | 2004 | Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19
| Triamino derivatives of triazolotriazine and triazolopyrimidine as adenosine A2a receptor antagonists. |
AID33015 | Displacement of [3H]-CGS- 21680 from rat striatal membranes Adenosine A2A receptor. Parenthesis indicate 95% confidence limits. | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
| Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists. |
AID231277 | Ratio of binding affinity against human adenosine A1 to that of A2 receptor | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
| Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives. |
AID436526 | Displacement of [3H]NECA from human adenosine A3 receptor expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
| Combining selectivity and affinity predictions using an integrated Support Vector Machine (SVM) approach: An alternative tool to discriminate between the human adenosine A(2A) and A(3) receptor pyrazolo-triazolo-pyrimidine antagonists binding sites. |
AID1347154 | Primary screen GU AMC 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. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6
| A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | | | |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |