| Assay ID | Title | Year | Journal | Article |
|---|
| 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. |
| 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. |
| AID706388 | Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in CHO cells after 60 mins by gamma counter | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications. |
| AID229549 | Relative binding to rat A1 and human A3 adenosine receptors (ratio of IC50) | 1996 | Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
| Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype. |
| AID1880710 | Cytotoxicity against human WI-38 cells assessed as cell viability incubated for 72 to 96 hrs by MTT assay | | | |
| AID1880699 | Antagonist activity at human wild type A1R expressed in CHO-K1 cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay | | | |
| AID1880702 | Displacement of CA200645 from NLuc human A1 receptor expressed in HEK293 cells assessed as inhibition constant by NanoBRET binding assay | | | |
| AID1857129 | Binding affinity to Nluc-A3R (unknown origin) expressed in HEK293 cells by nanoBRET assay | | | |
| AID1819771 | Displacement of [3H]HMRS7799 from human adenosine A3 receptor expressed in HEK293 cells by radioligand binding assay | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective A |
| AID1857121 | Binding affinity to wild type A1R (unknown origin) expressed in CHO-K1 cells assessed as dissociation constant by by Schild analysis | | | |
| AID32175 | Displacement of [3H]-(R)-PIA from Adenosine A1 receptor of rat cerebral cortex membranes | 1996 | Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
| Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype. |
| AID32884 | Displacement of [3H]-SCH- 58261 from Adenosine A2A receptor in rat striatal membranes | 1999 | Journal of medicinal chemistry, Nov-04, Volume: 42, Issue:22
| Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists. |
| AID1857128 | Binding affinity to Nluc-A3R (unknown origin) expressed in HEK293 cells assessed as dissociation constant (koff) by nanoBRET assay | | | |
| AID229550 | Relative binding to rat A2A and human A3 adenosine receptors (ratio of IC50) | 1996 | Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
| Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype. |
| AID1819775 | Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in HEK293 cells by radioligand binding assay | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective A |
| AID268110 | Displacement of [3H]MRE 3008F20 from human adenosine A3 receptor expressed in CHO cells | 2006 | Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
| Pharmacophore based receptor modeling: the case of adenosine A3 receptor antagonists. An approach to the optimization of protein models. |
| AID1814734 | Antagonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
| Development of Covalent, Clickable Probes for Adenosine A |
| AID1857122 | Binding affinity to wild type A1R (unknown origin) expressed in CHO-K1 cells assessed as equilibrium binding affinity constant by nanoBRET assay | | | |
| AID706380 | Selectivity ratio of Ki for human recombinant adenosine A2A receptor to Ki for human recombinant adenosine A3 receptor expressed in CHO cells | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications. |
| AID706387 | Displacement of [3H]CCPA from rat adenosine A1 receptor expressed in CHO cells after 60 mins by gamma counter | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications. |
| AID706382 | Selectivity ratio of Ki for human recombinant adenosine A1 receptor to Ki for human recombinant adenosine A3 receptor expressed in CHO cells | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications. |
| AID34716 | In vitro binding affinity at human Adenosine A3 receptor from HEK293 cells by [125I]AB-MECA displacement. | 1996 | Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
| Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype. |
| AID1857116 | Antagonist activity at wild type A3R (unknown origin) expressed in Flp-In-CHO cells assessed as inhibition of NECA reduced forskolin stimulated cAMP accumulation incubated for 30 mins | | | |
| AID32174 | Binding affinity was determined in radioligand binding assay at rat brain adenosine A1 receptor vs [3H]R-PIA | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
| Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes. |
| AID1880711 | Cytotoxicity against human PC-3 cells assessed as cell viability incubated for 72 to 96 hrs by MTT assay | | | |
| AID706386 | Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells after 60 mins by gamma counter | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications. |
| AID34860 | Displacement of [125]AB-MECA from human Adenosine A3 receptor expressed in HEK293 cells | 1999 | Journal of medicinal chemistry, Nov-04, Volume: 42, Issue:22
| Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists. |
| AID1880712 | Cytotoxicity against human HCT-116 cells assessed as cell viability incubated for 72 to 96 hrs by MTT assay | | | |
| AID1857131 | Binding affinity to Nluc-A1R (unknown origin) expressed in HEK293 cells assessed as association constant (kon) by nanoBRET assay | | | |
| AID1880722 | Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 10 uM incubated with NECA for 30 mins by LANCE cAMP detection as | | | |
| AID706376 | Antagonist activity at human adenosine A3 receptor expressed in CHO cells by [S35]GTPgammaS binding assay | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications. |
| AID706384 | Displacement of [125I]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counter | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications. |
| AID32888 | Displacement of specific [3H]-CGS- 21680 binding at Adenosine A2A receptor in rat striatal membranes. | 1997 | Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16
| Structure-activity relationships of 4-(phenylethynyl)-6-phenyl-1,4-dihydropyridines as highly selective A3 adenosine receptor antagonists. |
| AID32341 | Displacement of specific [3H](R)-PIA binding at adenosine A1 receptor from rat brain membranes. | 1997 | Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16
| Structure-activity relationships of 4-(phenylethynyl)-6-phenyl-1,4-dihydropyridines as highly selective A3 adenosine receptor antagonists. |
| AID32871 | Binding affinity was determined in radioligand binding assay at rat striatal Adenosine A2A receptor vs [3H]-CGS- 21680 | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
| Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes. |
| AID34733 | Bnding affinity in membrane of CHO cell stably expressing recombinant human Adenosine A3 receptor using [3H]8-ethyl-4-methyl-2-phenyl-(8R)-4,5,7,8-tetrahydro-1H-imidazo[2,1-i]-purin-5-one as radioligand | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
| Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary. |
| AID1880703 | Displacement of CA200645 from NLuc human A3 receptor expressed in HEK293 cells assessed as inhibition constant by NanoBRET binding assay | | | |
| AID32763 | Inhibition of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK cells | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
| 1,2,4-Triazolo[5,1-i]purine derivatives as highly potent and selective human adenosine A(3) receptor ligands. |
| AID231550 | Ratio of binding affinity for rat adenosine A1 and human adenosine A3 receptors expressed in HEK293 cells | 1999 | Journal of medicinal chemistry, Nov-04, Volume: 42, Issue:22
| Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists. |
| AID706377 | Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation by scintillation counter | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications. |
| AID34710 | Binding affinity at cloned human adenosine A3 receptor expressed in HEK293 cells was determined using [125I]AB-MECA as radioligand | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
| Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes. |
| AID231552 | Ratio of binding affinity for rat adenosine A2A of striatal membranes and human adenosine A3 receptors expressed in HEK293 cells | 1999 | Journal of medicinal chemistry, Nov-04, Volume: 42, Issue:22
| Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists. |
| AID33009 | Inhibition of [3H]CGS-21680 binding to rat Adenosine A2A receptor expressed in HEK293 cells | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
| 1,2,4-Triazolo[5,1-i]purine derivatives as highly potent and selective human adenosine A(3) receptor ligands. |
| AID235716 | Ratio against rat A1 receptor and Human A3 receptor | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
| Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes. |
| AID235717 | Ratio against rat A2A receptor and Human A3 receptor | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
| Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes. |
| AID1857132 | Binding affinity to Nluc-A1R (unknown origin) expressed in HEK293 cells assessed as dissociation constant (koff) by nanoBRET assay | | | |
| AID593980 | Antagonist activity at human adenosine A3 receptor | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| Pharmacophore elucidation for a new series of 2-aryl-pyrazolo-triazolo-pyrimidines as potent human A3 adenosine receptor antagonists. |
| AID1857135 | Binding affinity to Nluc-A1R (unknown origin) expressed in HEK293 cells assessed as residence time by nanoBRET assay | | | |
| AID462600 | Displacement of [3H]NECA from human recombinant adenosine A3 receptor expressed in human HeLa cell membrane | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
| Synthesis of theophylline derivatives and study of their activity as antagonists at adenosine receptors. |
| AID33796 | Displacement of [3H]-CGH 21680 from Adenosine A2A receptor of rat striatal membranes | 1996 | Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
| Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype. |
| AID34706 | Binding affinity in membrane of CHO cell stably expressing recombinant human Adenosine A3 receptor in the presence of GTPgammaS using [3H]8-ethyl-4-methyl-2-phenyl-(8R)-4,5,7,8-tetrahydro-1H-imidazo[2,1-i]-purin-5-one as radioligand | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
| Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary. |
| AID763040 | Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells after 90 mins by gamma counting analysis | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Fluorescent ligands for adenosine receptors. |
| AID234654 | Selectivity ratio of affinity at rat A2A and A3 receptors | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
| 1,2,4-Triazolo[5,1-i]purine derivatives as highly potent and selective human adenosine A(3) receptor ligands. |
| AID33175 | Inhibition at 50 uM on cAMP production induced by 50 uM 5`-(N-ethylcarboxamido)adenosine in CHO cell line transfected with human Adenosine A2B receptor cDNA | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
| Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes. |
| AID33489 | Binding affinity of adenosine derivative for endogenous rat Adenosine A3 receptor of RBL-2H3; Not determined | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
| Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary. |
| AID763041 | Competitive binding affinity to human adenosine A3 receptor expressed in CHO cells after 90 mins by flow cytometric analysis in presence of MRS5449 | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Fluorescent ligands for adenosine receptors. |
| AID1857133 | Binding affinity to Nluc-A1R (unknown origin) expressed in HEK293 cells by nanoBRET assay | | | |
| AID1857119 | Binding affinity to wild type A3R (unknown origin) expressed in CHO-K1 cells assessed as equilibrium binding affinity constant by nanoBRET assay | | | |
| AID1267443 | Displacement of CA200645 from human adenosine A3 receptor expressed in CHO CRE-SPAP cells at 1 uM incubated for 1 hr by fluorescence analysis | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
| Fragment-Based Discovery of Subtype-Selective Adenosine Receptor Ligands from Homology Models. |
| AID33338 | Binding affinity of adenosine derivative for endogenous rat Adenosine A3 receptor expressed on CHO cell | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
| Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary. |
| AID1857118 | Binding affinity to wild type A3R (unknown origin) expressed in Flp-In-CHO cells assessed as dissociation constant by by Schild analysis | | | |
| AID1813859 | Displacement of [3H]NECA from human adenosine A3 receptor expressed in human HeLa cells incubated for 30 mins by fluorescence polarization binding assay | 2022 | ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2
| Exploring Non-orthosteric Interactions with a Series of Potent and Selective A |
| AID1857120 | Antagonist activity at wild type A1R (unknown origin) expressed in CHO-K1 cells assessed as inhibition of NECA reduced forskolin stimulated cAMP accumulation incubated for 30 mins | | | |
| AID234653 | Selectivity ratio of affinity at rat A1 and A3 receptors | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
| 1,2,4-Triazolo[5,1-i]purine derivatives as highly potent and selective human adenosine A(3) receptor ligands. |
| AID32332 | Displacement of [3H]DPCPX from Adenosine A1 receptor of rat brain membranes | 1999 | Journal of medicinal chemistry, Nov-04, Volume: 42, Issue:22
| Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists. |
| AID32504 | Inhibition of [3H]DPCPX binding to rat Adenosine A1 receptor expressed in CHO cells | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
| 1,2,4-Triazolo[5,1-i]purine derivatives as highly potent and selective human adenosine A(3) receptor ligands. |
| AID34872 | Displacement of specific [125I]AB-MECA binding at human adenosine A3 receptor. | 1997 | Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16
| Structure-activity relationships of 4-(phenylethynyl)-6-phenyl-1,4-dihydropyridines as highly selective A3 adenosine receptor antagonists. |
| AID1176084 | Antagonist activity at human recombinant adenosine A3 receptor | 2015 | Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1
| 1,2,4-triazolo[1,5-a]quinoxaline derivatives and their simplified analogues as adenosine A₃ receptor antagonists. Synthesis, structure-affinity relationships and molecular modeling studies. |
| AID34861 | In vitro binding affinity against human Adenosine A3 receptor | 2000 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 10, Issue:1
| The utilization of a unified pharmacophore query in the discovery of new antagonists of the adenosine receptor family. |
| AID1857130 | Binding affinity to Nluc-A3R (unknown origin) expressed in HEK293 cells assessed as residence time by nanoBRET assay | | | |
| AID1857127 | Binding affinity to Nluc-A3R (unknown origin) expressed in HEK293 cells assessed as association constant (kon) by nanoBRET assay | | | |
| AID1813860 | Displacement of CELT-228 from human adenosine A3 receptor expressed in human HeLa cells incubated for 30 mins by fluorescence polarization binding assay | 2022 | ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2
| Exploring Non-orthosteric Interactions with a Series of Potent and Selective A |
| AID1345822 | Human A3 receptor (Adenosine receptors) | 2006 | Autonomic & autacoid pharmacology, Apr, Volume: 26, Issue:2
| Radioligand binding and functional responses of ligands for human recombinant adenosine A(3) receptors. |
| AID1345822 | Human A3 receptor (Adenosine receptors) | 2001 | British journal of pharmacology, Mar, Volume: 132, Issue:5
| Cyclic AMP-dependent inhibition of human neutrophil oxidative activity by substituted 2-propynylcyclohexyl adenosine A(2A) receptor agonists. |
| AID1345822 | Human A3 receptor (Adenosine receptors) | 1996 | Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
| Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype. |
| AID1345721 | Human A2B receptor (Adenosine receptors) | 2004 | Biochemical pharmacology, Jul-15, Volume: 68, Issue:2
| [3H]OSIP339391, a selective, novel, and high affinity antagonist radioligand for adenosine A2B receptors. |
| AID1345822 | Human A3 receptor (Adenosine receptors) | 1997 | Neuropharmacology, Sep, Volume: 36, Issue:9
| Pharmacological characterization of novel A3 adenosine receptor-selective antagonists. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |