| Assay ID | Title | Year | Journal | Article |
|---|
| 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. |
| 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. |
| AID1162465 | Allosteric enhancer activity at human adenosine A1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production at 100 nM in presence of 1 pM CCPA | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Synthesis and biological evaluation of novel allosteric enhancers of the A1 adenosine receptor based on 2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene. |
| AID390613 | Antagonist activity at human adenosine A1 receptor expressed in FlpIn-CHO cells assessed as inhibition of R-PIA-mediated ERK1/2 phosphorylation | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| 2-aminothienopyridazines as novel adenosine A1 receptor allosteric modulators and antagonists. |
| AID474665 | Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells by scintillation counting | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Hybrid ortho/allosteric ligands for the adenosine A(1) receptor. |
| AID31087 | Percent remaining of radioligand [3H]CCPA binding to human adenosine A1 receptor at 10 uM | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Synthesis and biological evaluation of 2,3,5-substituted [1,2,4]thiadiazoles as allosteric modulators of adenosine receptors. |
| AID1162477 | Allosteric enhancer activity at human adenosine A1 receptor expressed in CHO cell membranes assessed as shift in [3H}NECA binding affinity level at 1 uM | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Synthesis and biological evaluation of novel allosteric enhancers of the A1 adenosine receptor based on 2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene. |
| AID637820 | Displacement of [3H]DPCPX from recombinant human A1 adenosine receptor expressed in CHO-K1 cells at 100 uM | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
| Structure-activity relationships of 2-amino-3-aroyl-4-[(4-arylpiperazin-1-yl)methyl]thiophenes. Part 2: Probing the influence of diverse substituents at the phenyl of the arylpiperazine moiety on allosteric enhancer activity at the A₁ adenosine receptor. |
| AID363478 | Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells relative to untreated control | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor. |
| AID243350 | Allosteric enhancer activity against adenosine A1 receptor | 2005 | Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
| 6-aryl-8H-indeno[1,2-d]thiazol-2-ylamines: A1 adenosine receptor agonist allosteric enhancers having improved potency. |
| AID321391 | Displacement of [3H]CPX from human adenosine A1 receptor expressed in CHOK1 cells at 10 uM relative to control | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| 5-Substituted 2-aminothiophenes as A1 adenosine receptor allosteric enhancers. |
| AID637819 | Binding affinity to recombinant human A1 adenosine receptor allosteric site expressed in CHO cells assessed as potentiation of CCPA-induced [3H]DPCPX displacement at 10 uM after 90 mins relative to control | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
| Structure-activity relationships of 2-amino-3-aroyl-4-[(4-arylpiperazin-1-yl)methyl]thiophenes. Part 2: Probing the influence of diverse substituents at the phenyl of the arylpiperazine moiety on allosteric enhancer activity at the A₁ adenosine receptor. |
| AID321390 | Activity at human adenosine A1 receptor expressed in CHOK1 cells assessed as agonist-receptor ternary complex remaining by [35S]GTPgammaS binding assay | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| 5-Substituted 2-aminothiophenes as A1 adenosine receptor allosteric enhancers. |
| AID637812 | Allosteric enhancer activity at recombinant human A1 adenosine receptor expressed in CHO cells assessed as change in forskolin-induced cAMP production at 1 uM after 6 mins by radioimmunoassay | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
| Structure-activity relationships of 2-amino-3-aroyl-4-[(4-arylpiperazin-1-yl)methyl]thiophenes. Part 2: Probing the influence of diverse substituents at the phenyl of the arylpiperazine moiety on allosteric enhancer activity at the A₁ adenosine receptor. |
| AID703964 | Allosteric enhancing activity at human adenosine A1 receptor expressed in CHO cells assessed as increase in [3H]-2-chloro-N6-cyclopentyladenosine Bmax at 10 uM after 90 mins relative to control | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[(4-arylpiperazin-1-yl)methyl]-5-substituted-thiophenes. effect of the 5-modification on allosteric enhancer activity at the A1 adenosine receptor. |
| AID452545 | Allosteric modulatory activity at human adenosine A1 receptor expressed in CHOk1 cells assessed as drug level causing half maximal allosteric effect on [125I]-ABA dissociation from receptor-G protein ternary complex by dissociation kinetic binding assay | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
| 3- and 6-Substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists. |
| AID1061869 | Potentiation of CCPA-induced displacement of [3H]-DPCPX from human adenosine A1 receptor expressed in CHO cell membranes at 10 uM after 90 mins relative to CCPA-treated control | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Synthesis and biological evaluation of novel 2-amino-3-aroyl-4-neopentyl-5-substituted thiophene derivatives as allosteric enhancers of the A₁ adenosine receptor. |
| AID1162469 | Displacement of [3H]DPCPX from adenosine A1 receptor in rat membranes | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Synthesis and biological evaluation of novel allosteric enhancers of the A1 adenosine receptor based on 2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene. |
| AID1061877 | Allosteric enhancement of human adenosine A1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production at 10 uM preincubated for 10 mins followed by forskolin challenge measured after 5 mins by scintillation counting a | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Synthesis and biological evaluation of novel 2-amino-3-aroyl-4-neopentyl-5-substituted thiophene derivatives as allosteric enhancers of the A₁ adenosine receptor. |
| AID703967 | Displacement of [3H]MRE-3008-F20 from human adenosine A3 receptor expressed in CHO cells at 10 uM after 120 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[(4-arylpiperazin-1-yl)methyl]-5-substituted-thiophenes. effect of the 5-modification on allosteric enhancer activity at the A1 adenosine receptor. |
| AID1162473 | Allosteric enhancer activity at human adenosine A1 receptor expressed in CHO cell membranes assessed as shift in CCPA binding Ki level at 10 uM by [3H]DPCPX competition binding assay | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Synthesis and biological evaluation of novel allosteric enhancers of the A1 adenosine receptor based on 2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene. |
| AID363474 | Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in CHO cells at 10 uM | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor. |
| AID474666 | Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells by scintillation counting relative to control | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Hybrid ortho/allosteric ligands for the adenosine A(1) receptor. |
| AID390610 | Modulation of human adenosine A1 receptor expressed in CHO-K1 cells assessed as stabilization of [125I]ABA-receptor-G protein ternary complex at 50 uM by dissociation kinetic assay | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| 2-aminothienopyridazines as novel adenosine A1 receptor allosteric modulators and antagonists. |
| AID363471 | Activity at human recombinant adenosine A1 receptor expressed in CHO cells assessed as cAMP level at 1 uM | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor. |
| AID1061876 | Allosteric enhancement of human adenosine A1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production at 100 nM preincubated for 10 mins followed by forskolin challenge measured after 5 mins by scintillation counting | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Synthesis and biological evaluation of novel 2-amino-3-aroyl-4-neopentyl-5-substituted thiophene derivatives as allosteric enhancers of the A₁ adenosine receptor. |
| AID703966 | Displacement of [3H]DPCPX from adenosine A1 receptor in rat membrane | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[(4-arylpiperazin-1-yl)methyl]-5-substituted-thiophenes. effect of the 5-modification on allosteric enhancer activity at the A1 adenosine receptor. |
| AID31089 | Percent remaining of radioligand [3H]DPCPX binding to human adenosine A1 receptor at 10 uM | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Synthesis and biological evaluation of 2,3,5-substituted [1,2,4]thiadiazoles as allosteric modulators of adenosine receptors. |
| AID276227 | Activity at human recombinant adenosine A1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation in presence of CPA at 1 uM relative to control | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
| Microwave-assisted synthesis of thieno[2,3-c]pyridine derivatives as a new series of allosteric enhancers at the adenosine A(1) receptor. |
| AID30314 | Inhibition of [3H]CPX binding to CHO-K cell membrane expressing human Adenosine A1 receptor | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
| 2-Amino-3-aroyl-4,5-alkylthiophenes: agonist allosteric enhancers at human A(1) adenosine receptors. |
| AID363477 | Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells assessed for per milligram of protein | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor. |
| AID30312 | Ability to displace the binding of [3H]DPCPX to the ligand binding site of CHO:hA1 (human Adenosine A1 receptor) at concentration of 10 uM | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Synthesis and biological effects of novel 2-amino-3-naphthoylthiophenes as allosteric enhancers of the A1 adenosine receptor. |
| AID363480 | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells assessed for per milligram of protein | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor. |
| AID703963 | Allosteric enhancing activity at human adenosine A1 receptor expressed in CHO cells assessed as increase in CCPA-induced [3H]DPCPX displacement at 10 uM after 90 mins relative to control | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[(4-arylpiperazin-1-yl)methyl]-5-substituted-thiophenes. effect of the 5-modification on allosteric enhancer activity at the A1 adenosine receptor. |
| AID637814 | Displacement of [3H]DPCPX from recombinant human A1 adenosine receptor expressed in CHO cells at 10 uM after 120 mins by scintillation counting | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
| Structure-activity relationships of 2-amino-3-aroyl-4-[(4-arylpiperazin-1-yl)methyl]thiophenes. Part 2: Probing the influence of diverse substituents at the phenyl of the arylpiperazine moiety on allosteric enhancer activity at the A₁ adenosine receptor. |
| AID1243881 | Increase of [3H]-NECA affinity to human adenosine A1 receptor expressed in CHO cells at 1 uM after 45 mins by scintillation spectrometry analysis relative to control | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and biological evaluation of a new series of 2-amino-3-aroyl thiophene derivatives as agonist allosteric modulators of the A1 adenosine receptor. A position-dependent effect study. |
| AID276224 | Displacement of [3H]MRE-3008F20 from human adenosine A3 receptor expressed in CHO cells at 10 uM | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
| Microwave-assisted synthesis of thieno[2,3-c]pyridine derivatives as a new series of allosteric enhancers at the adenosine A(1) receptor. |
| AID1243884 | Displacement of [3H]DPCPX from adenosine A1 receptor in rat membranes | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and biological evaluation of a new series of 2-amino-3-aroyl thiophene derivatives as agonist allosteric modulators of the A1 adenosine receptor. A position-dependent effect study. |
| AID1061871 | Displacement of [3H]-DPCPX from human adenosine A1 receptor expressed in CHO-K1 cell membranes at 100 uM relative to control | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Synthesis and biological evaluation of novel 2-amino-3-aroyl-4-neopentyl-5-substituted thiophene derivatives as allosteric enhancers of the A₁ adenosine receptor. |
| AID363479 | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor. |
| AID321389 | Activity at human adenosine A1 receptor expressed in CHOK1 cells assessed as agonist-receptor ternary complex remaining by [35S]GTPgammaS binding assay after 10 mins | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| 5-Substituted 2-aminothiophenes as A1 adenosine receptor allosteric enhancers. |
| AID637811 | Allosteric enhancer activity at recombinant human A1 adenosine receptor expressed in CHO cells assessed as change in forskolin-induced cAMP production at 0.1 uM after 6 mins by radioimmunoassay | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
| Structure-activity relationships of 2-amino-3-aroyl-4-[(4-arylpiperazin-1-yl)methyl]thiophenes. Part 2: Probing the influence of diverse substituents at the phenyl of the arylpiperazine moiety on allosteric enhancer activity at the A₁ adenosine receptor. |
| AID637818 | Binding affinity to recombinant human A1 adenosine receptor allosteric site expressed in CHO cells assessed as [3H]DPCPX Bmax shift at 10 uM after 90 mins relative to control | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
| Structure-activity relationships of 2-amino-3-aroyl-4-[(4-arylpiperazin-1-yl)methyl]thiophenes. Part 2: Probing the influence of diverse substituents at the phenyl of the arylpiperazine moiety on allosteric enhancer activity at the A₁ adenosine receptor. |
| AID9630 | Percentage of response to 10 uM of PD-81723 on CHO cells expressing the cloned human A1-adenosine receptor at 10 uM concentration | 2000 | Bioorganic & medicinal chemistry letters, Sep-04, Volume: 10, Issue:17
| Synthesis and biological effects of a new series of 2-amino-3-benzoylthiophenes as allosteric enhancers of A1-adenosine receptor. |
| AID1243872 | Positive allosteric enhancement of human cloned adenosine A1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation at 100 nM using [3H]-cAMP by scintillation counting relative to control in presence of 1 pM of CCPA | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and biological evaluation of a new series of 2-amino-3-aroyl thiophene derivatives as agonist allosteric modulators of the A1 adenosine receptor. A position-dependent effect study. |
| AID240175 | Antagonist activity against adenosine A1 receptor | 2005 | Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
| 6-aryl-8H-indeno[1,2-d]thiazol-2-ylamines: A1 adenosine receptor agonist allosteric enhancers having improved potency. |
| AID34083 | Ability to displace the binding of [3H]-ZM 241385, to the ligand binding site of CHO:hA2A (human Adenosine A2A receptor) at concentration of 10 uM | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Synthesis and biological effects of novel 2-amino-3-naphthoylthiophenes as allosteric enhancers of the A1 adenosine receptor. |
| AID276229 | Activity at human recombinant adenosine A1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation in the presence of CPA relative to control | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
| Microwave-assisted synthesis of thieno[2,3-c]pyridine derivatives as a new series of allosteric enhancers at the adenosine A(1) receptor. |
| AID766683 | Allosteric enhancement of human adenosine A1 receptor expressed in CHO cells assessed as inhibition of CCPA-induced cAMP production at 100 nM after 10 mins | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and biological effects of novel 2-amino-3-(4-chlorobenzoyl)-4-substituted thiophenes as allosteric enhancers of the A1 adenosine receptor. |
| AID1061875 | Displacement of [3H]-DPCPX from human adenosine A1 receptor expressed in CHO cell membranes at 10 uM by scintillation counting analysis relative to control | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Synthesis and biological evaluation of novel 2-amino-3-aroyl-4-neopentyl-5-substituted thiophene derivatives as allosteric enhancers of the A₁ adenosine receptor. |
| AID31108 | Dissociation rate of [3H]CCPA from Adenosine A1 receptor expressing CHO cells at 10 uM as percent t1/2 | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Synthesis and biological effects of novel 2-amino-3-naphthoylthiophenes as allosteric enhancers of the A1 adenosine receptor. |
| AID19109 | Half life by its biological oxidation in presence of horse radish peroxide | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4
| Regioselective oxidation of 2-amino-3-aroyl-4,5-dialkylthiophenes by DMSO. |
| AID452549 | Agonist activity at human adenosine A1 receptor expressed in CHOk1 cells assessed as induction of ERK1/2 phosphorylation at 10 uM relative to R-PIA | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
| 3- and 6-Substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists. |
| AID363469 | Activity at human recombinant adenosine A1 receptor expressed in CHO cells assessed as cAMP level at 0.01 uM | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor. |
| AID766678 | Allosteric enhancement of human adenosine A1 receptor expressed in CHO cells assessed as increase of CCPA Ki at 10 uM after 90 mins by [3H]DPCPX radioligand binding assay | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and biological effects of novel 2-amino-3-(4-chlorobenzoyl)-4-substituted thiophenes as allosteric enhancers of the A1 adenosine receptor. |
| AID19110 | Half life by its biological oxidation in presence of human liver microsomes | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4
| Regioselective oxidation of 2-amino-3-aroyl-4,5-dialkylthiophenes by DMSO. |
| AID452547 | Agonist activity at human adenosine A1 receptor expressed in CHOk1 cells assessed as potentiation of R-PIA-induced ERK1/2 phosphorylation at 10 uM | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
| 3- and 6-Substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists. |
| AID637810 | Allosteric enhancer activity at recombinant human A1 adenosine receptor expressed in CHO cells assessed as change in forskolin-induced cAMP production at 0.01 uM after 6 mins by radioimmunoassay | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
| Structure-activity relationships of 2-amino-3-aroyl-4-[(4-arylpiperazin-1-yl)methyl]thiophenes. Part 2: Probing the influence of diverse substituents at the phenyl of the arylpiperazine moiety on allosteric enhancer activity at the A₁ adenosine receptor. |
| AID31088 | Percent remaining of radioligand [3H]DPCPX binding to human adenosine A1 receptor at 1 uM | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Synthesis and biological evaluation of 2,3,5-substituted [1,2,4]thiadiazoles as allosteric modulators of adenosine receptors. |
| AID703968 | Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in CHO cells at 10 uM after 120 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[(4-arylpiperazin-1-yl)methyl]-5-substituted-thiophenes. effect of the 5-modification on allosteric enhancer activity at the A1 adenosine receptor. |
| AID1243880 | Effect on dissociation binding rate constant of [3H]-NECA to human adenosine A1 receptor expressed in CHO cells at 1 uM after 45 mins by scintillation spectrometry analysis relative to control | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and biological evaluation of a new series of 2-amino-3-aroyl thiophene derivatives as agonist allosteric modulators of the A1 adenosine receptor. A position-dependent effect study. |
| AID32625 | Percent change in cAMP content of CHO (Chinese hamster ovary) cells expressing human Adenosine A1 receptor at 0.01 uM | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Synthesis and biological effects of novel 2-amino-3-naphthoylthiophenes as allosteric enhancers of the A1 adenosine receptor. |
| AID363473 | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells at 10 uM | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor. |
| AID766682 | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells at 10 uM after 60 mins by scintillation counting | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and biological effects of novel 2-amino-3-(4-chlorobenzoyl)-4-substituted thiophenes as allosteric enhancers of the A1 adenosine receptor. |
| AID7698 | Ability to displace the binding of [3H]-MRE 3008-F20 to the ligand binding site of CHO:hA3 (human Adenosine receptor) at concentration of 10 uM | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Synthesis and biological effects of novel 2-amino-3-naphthoylthiophenes as allosteric enhancers of the A1 adenosine receptor. |
| AID276222 | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells at 10 uM | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
| Microwave-assisted synthesis of thieno[2,3-c]pyridine derivatives as a new series of allosteric enhancers at the adenosine A(1) receptor. |
| AID363483 | Displacement of [3H]DPCPX from adenosine A1 receptor in rat membranes | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor. |
| AID1162476 | Allosteric enhancer activity at human adenosine A1 receptor expressed in CHO cell membranes assessed as [3H]NECA affinity constant at 1 uM (Kd = 0.87 +/- 0.04 nM) | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Synthesis and biological evaluation of novel allosteric enhancers of the A1 adenosine receptor based on 2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene. |
| AID363484 | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells at 100 uM | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor. |
| AID1243879 | Effect on association binding rate constant of [3H]-NECA to human adenosine A1 receptor expressed in CHO cells at 1 uM after 45 mins by scintillation spectrometry analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and biological evaluation of a new series of 2-amino-3-aroyl thiophene derivatives as agonist allosteric modulators of the A1 adenosine receptor. A position-dependent effect study. |
| AID31093 | Inhibition of antagonist [3H]CPX binding to Adenosine A1 receptor membrane at 100 uM | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10
| 2-Amino-3-benzoylthiophene allosteric enhancers of A1 adenosine agonist binding: new 3, 4-, and 5-modifications. |
| AID244459 | In vitro allosteric enhancer (AE) activity for adenosine A2A receptor at 50 uM | 2005 | Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
| 6-aryl-8H-indeno[1,2-d]thiazol-2-ylamines: A1 adenosine receptor agonist allosteric enhancers having improved potency. |
| AID703971 | Allosteric enhancing activity at human adenosine A1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation at 10 uM incubated for 10 mins prior to forskolin-stimulation measured after 5 mins by competition protein | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[(4-arylpiperazin-1-yl)methyl]-5-substituted-thiophenes. effect of the 5-modification on allosteric enhancer activity at the A1 adenosine receptor. |
| AID30319 | Dissociation of [3H]CCPA from Adenosine A1 receptor in CHO cells at 10 uM as percent K-1 | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Synthesis and biological effects of novel 2-amino-3-naphthoylthiophenes as allosteric enhancers of the A1 adenosine receptor. |
| AID32626 | Percent change in cAMP content of CHO (Chinese hamster ovary) cells expressing human Adenosine A1 receptor at 0.1 uM | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Synthesis and biological effects of novel 2-amino-3-naphthoylthiophenes as allosteric enhancers of the A1 adenosine receptor. |
| AID363476 | Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor. |
| AID766681 | Displacement of [3H]ZM 241385 from human adenosine A2A receptor expressed in CHO cells at 10 uM after 60 mins by scintillation counting | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and biological effects of novel 2-amino-3-(4-chlorobenzoyl)-4-substituted thiophenes as allosteric enhancers of the A1 adenosine receptor. |
| AID1162474 | Allosteric enhancer activity at human adenosine A1 receptor expressed in CHO cell membranes assessed as [3H]NECA association rate at 1 uM (Rvb = 0.0183 +/- 0.0008 /nM/min) | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Synthesis and biological evaluation of novel allosteric enhancers of the A1 adenosine receptor based on 2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene. |
| AID9624 | Percentage of response to 10 uM of PD-81723 on CHO cells expressing the cloned human A1-adenosine receptor at 1 uM concentration | 2000 | Bioorganic & medicinal chemistry letters, Sep-04, Volume: 10, Issue:17
| Synthesis and biological effects of a new series of 2-amino-3-benzoylthiophenes as allosteric enhancers of A1-adenosine receptor. |
| AID1162467 | Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in CHO cell membranes at 10 uM | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Synthesis and biological evaluation of novel allosteric enhancers of the A1 adenosine receptor based on 2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene. |
| AID276226 | Activity at human recombinant adenosine A1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation in presence of CPA at 0.1 uM relative to control | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
| Microwave-assisted synthesis of thieno[2,3-c]pyridine derivatives as a new series of allosteric enhancers at the adenosine A(1) receptor. |
| AID31241 | Antagonistic activity expressed as percent displacement of 0.4 nM of [3H]DPCPX from adenosine A1 receptors in rat brain cortex membranes at 10 uM | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Allosteric modulation of the adenosine A(1) receptor. Synthesis and biological evaluation of novel 2-amino-3-benzoylthiophenes as allosteric enhancers of agonist binding. |
| AID32624 | Dissociation of [3H]N6-cyclohexyladenosine ([3H]CHA) from CHO-K1 membrane expressing human adenosine A1 receptor after treatment with allosteric enhancer at 100 uM and (R)-PIA | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10
| 2-Amino-3-benzoylthiophene allosteric enhancers of A1 adenosine agonist binding: new 3, 4-, and 5-modifications. |
| AID766680 | Displacement of [3H]MRE-3008-F20 from human adenosine A3 receptor expressed in CHO cells at 10 uM after 60 mins by scintillation counting | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and biological effects of novel 2-amino-3-(4-chlorobenzoyl)-4-substituted thiophenes as allosteric enhancers of the A1 adenosine receptor. |
| AID31270 | Enhancing activity at 10 uM PD 81,723 (100%) at Adenosine A1 receptor in rat brain cortex membranes | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Allosteric modulation of the adenosine A(1) receptor. Synthesis and biological evaluation of novel 2-amino-3-benzoylthiophenes as allosteric enhancers of agonist binding. |
| AID452544 | Allosteric modulatory activity at human adenosine A1 receptor expressed in CHOk1 cells assessed as [125I]-ABA-receptor-G protein ternary complex remaining after 10 mins of radioligand dissociation at 50 uM by dissociation kinetic binding assay | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
| 3- and 6-Substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists. |
| AID1162466 | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes at 10 uM | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Synthesis and biological evaluation of novel allosteric enhancers of the A1 adenosine receptor based on 2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene. |
| AID1061873 | Displacement of [3H]-MRE-3008-F20 from human adenosine A3 receptor expressed in CHO cell membranes at 10 uM by scintillation counting analysis relative to control | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Synthesis and biological evaluation of novel 2-amino-3-aroyl-4-neopentyl-5-substituted thiophene derivatives as allosteric enhancers of the A₁ adenosine receptor. |
| AID32628 | Percent change in cAMP content of CHO (Chinese hamster ovary) cells expressing human Adenosine A1 receptor at 1 uM | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Synthesis and biological effects of novel 2-amino-3-naphthoylthiophenes as allosteric enhancers of the A1 adenosine receptor. |
| AID637813 | Allosteric enhancer activity at recombinant human A1 adenosine receptor expressed in CHO cells assessed as change in forskolin-induced cAMP production at 10 uM after 6 mins by radioimmunoassay | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
| Structure-activity relationships of 2-amino-3-aroyl-4-[(4-arylpiperazin-1-yl)methyl]thiophenes. Part 2: Probing the influence of diverse substituents at the phenyl of the arylpiperazine moiety on allosteric enhancer activity at the A₁ adenosine receptor. |
| AID1243876 | Displacement of [3H]-MRE-3008-F20 from human adenosine A3 receptor expressed in CHO cells at 10 uM after 120 mins by scintillation counting | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and biological evaluation of a new series of 2-amino-3-aroyl thiophene derivatives as agonist allosteric modulators of the A1 adenosine receptor. A position-dependent effect study. |
| AID390611 | Modulation of human adenosine A1 receptor expressed in CHO-K1 cells assessed as allosteric effect on [125I]ABA dissociation | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| 2-aminothienopyridazines as novel adenosine A1 receptor allosteric modulators and antagonists. |
| AID9617 | Percentage of response to 10 uM of PD-81723 on CHO cells expressing the cloned human A1-adenosine receptor at 0.1 uM concentration | 2000 | Bioorganic & medicinal chemistry letters, Sep-04, Volume: 10, Issue:17
| Synthesis and biological effects of a new series of 2-amino-3-benzoylthiophenes as allosteric enhancers of A1-adenosine receptor. |
| AID363481 | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells relative to untreated control | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor. |
| AID1061872 | Displacement of [3H]-DPCPX from rat brain membrane adenosine A1 receptor | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Synthesis and biological evaluation of novel 2-amino-3-aroyl-4-neopentyl-5-substituted thiophene derivatives as allosteric enhancers of the A₁ adenosine receptor. |
| AID1162470 | Allosteric enhancer activity at human adenosine A1 receptor expressed in CHO cell membranes assessed as shift in [3H]CCPA Bmax level at 10 uM by saturation binding assay | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Synthesis and biological evaluation of novel allosteric enhancers of the A1 adenosine receptor based on 2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene. |
| AID363475 | Displacement of [3H]MRE3008F20 from human adenosine A3 receptor expressed in CHO cells at 10 uM | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor. |
| AID766684 | Allosteric enhancement of human adenosine A1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production at 10 uM after 10 mins | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and biological effects of novel 2-amino-3-(4-chlorobenzoyl)-4-substituted thiophenes as allosteric enhancers of the A1 adenosine receptor. |
| AID1162468 | Displacement of [3H]MRE-3008-F20 from human adenosine 3 receptor expressed in CHO cell membranes at 10 uM | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Synthesis and biological evaluation of novel allosteric enhancers of the A1 adenosine receptor based on 2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene. |
| AID363472 | Activity at human recombinant adenosine A1 receptor expressed in CHO cells assessed as cAMP level at 10 uM | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor. |
| AID1162464 | Allosteric enhancer activity at human adenosine A1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production at 10 uM | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Synthesis and biological evaluation of novel allosteric enhancers of the A1 adenosine receptor based on 2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene. |
| AID1162475 | Allosteric enhancer activity at human adenosine A1 receptor expressed in CHO cell membranes assessed as [3H]NECA dissociation rate at 1 uM (Rvb = 0.0159 +/- 0.0004 /min) | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Synthesis and biological evaluation of novel allosteric enhancers of the A1 adenosine receptor based on 2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene. |
| AID703969 | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells at 10 uM after 120 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[(4-arylpiperazin-1-yl)methyl]-5-substituted-thiophenes. effect of the 5-modification on allosteric enhancer activity at the A1 adenosine receptor. |
| AID244458 | In vitro allosteric enhancer (AE) activity for adenosine A3 receptor at 50 uM | 2005 | Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
| 6-aryl-8H-indeno[1,2-d]thiazol-2-ylamines: A1 adenosine receptor agonist allosteric enhancers having improved potency. |
| AID276225 | Activity at human recombinant adenosine A1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation in presence of CPA at 0.01 uM relative to control | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
| Microwave-assisted synthesis of thieno[2,3-c]pyridine derivatives as a new series of allosteric enhancers at the adenosine A(1) receptor. |
| AID276228 | Activity at human recombinant adenosine A1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation in presence of CPA at 10 uM relative to control | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
| Microwave-assisted synthesis of thieno[2,3-c]pyridine derivatives as a new series of allosteric enhancers at the adenosine A(1) receptor. |
| AID703965 | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHOK1 cells at 100 uM | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[(4-arylpiperazin-1-yl)methyl]-5-substituted-thiophenes. effect of the 5-modification on allosteric enhancer activity at the A1 adenosine receptor. |
| AID1243875 | Displacement of [3H]-ZM241385 from human adenosine A2 receptor expressed in CHO cells at 10 uM after 120 mins by scintillation counting | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and biological evaluation of a new series of 2-amino-3-aroyl thiophene derivatives as agonist allosteric modulators of the A1 adenosine receptor. A position-dependent effect study. |
| AID1162472 | Allosteric enhancer activity at human adenosine A1 receptor expressed in CHO cell membranes assessed as shift in [3H]CCPA Kd level at 10 uM by saturation binding assay | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Synthesis and biological evaluation of novel allosteric enhancers of the A1 adenosine receptor based on 2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene. |
| AID637815 | Displacement of [3H]ZM241385 from recombinant human A2A adenosine receptor expressed in CHO cells at 10 uM after 60 mins by scintillation counting | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
| Structure-activity relationships of 2-amino-3-aroyl-4-[(4-arylpiperazin-1-yl)methyl]thiophenes. Part 2: Probing the influence of diverse substituents at the phenyl of the arylpiperazine moiety on allosteric enhancer activity at the A₁ adenosine receptor. |
| AID30293 | Effective dose as dissociation of [3H]N6-cyclohexyladenosine ([3H]CHA) from CHO-K1 membrane after treatment with allosteric enhancer and (R)-PIA | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10
| 2-Amino-3-benzoylthiophene allosteric enhancers of A1 adenosine agonist binding: new 3, 4-, and 5-modifications. |
| AID32618 | Allosteric enhancer activity score measured by its ability to stabilize the agonist-receptor-G protein ternary complex at a concentration of 100 uM | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
| 2-Amino-3-aroyl-4,5-alkylthiophenes: agonist allosteric enhancers at human A(1) adenosine receptors. |
| AID390612 | Displacement of [3H]CPX from human adenosine A1 receptor expressed in CHO-K1 cells at 50 uM | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| 2-aminothienopyridazines as novel adenosine A1 receptor allosteric modulators and antagonists. |
| AID703970 | Allosteric enhancing activity at human adenosine A1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation at 100 nM incubated for 10 mins prior to forskolin-stimulation measured after 5 mins by competition protei | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[(4-arylpiperazin-1-yl)methyl]-5-substituted-thiophenes. effect of the 5-modification on allosteric enhancer activity at the A1 adenosine receptor. |
| AID276223 | Displacement of [3H]ZM 241385 from human adenosine A2 receptor expressed in CHO cells at 10 uM | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
| Microwave-assisted synthesis of thieno[2,3-c]pyridine derivatives as a new series of allosteric enhancers at the adenosine A(1) receptor. |
| AID637816 | Displacement of [3H]MRE3008F20 from recombinant human A3 adenosine receptor expressed in CHO cells at 10 uM after 120 mins by scintillation counting | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
| Structure-activity relationships of 2-amino-3-aroyl-4-[(4-arylpiperazin-1-yl)methyl]thiophenes. Part 2: Probing the influence of diverse substituents at the phenyl of the arylpiperazine moiety on allosteric enhancer activity at the A₁ adenosine receptor. |
| AID637817 | Binding affinity to recombinant human A1 adenosine receptor allosteric site expressed in CHO cells assessed as [3H]CCPA Bmax shift at 10 uM after 90 mins relative to control | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
| Structure-activity relationships of 2-amino-3-aroyl-4-[(4-arylpiperazin-1-yl)methyl]thiophenes. Part 2: Probing the influence of diverse substituents at the phenyl of the arylpiperazine moiety on allosteric enhancer activity at the A₁ adenosine receptor. |
| AID452546 | Agonist activity at human adenosine A1 receptor expressed in CHOk1 cells assessed as potentiation of R-PIA-induced ERK1/2 phosphorylation at 3 uM | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
| 3- and 6-Substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists. |
| AID766679 | Allosteric enhancement of human adenosine A1 receptor expressed in CHO cells assessed as increase of [3H]CCPA Bmax at 10 uM after 90 mins | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and biological effects of novel 2-amino-3-(4-chlorobenzoyl)-4-substituted thiophenes as allosteric enhancers of the A1 adenosine receptor. |
| AID244462 | In vitro allosteric enhancer (AE) activity for adenosine A1 receptor at 50 uM; ND is not determined | 2005 | Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
| 6-aryl-8H-indeno[1,2-d]thiazol-2-ylamines: A1 adenosine receptor agonist allosteric enhancers having improved potency. |
| AID244457 | In vitro allosteric enhancer (AE) activity for adenosine A1 receptor at 50 uM | 2005 | Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
| 6-aryl-8H-indeno[1,2-d]thiazol-2-ylamines: A1 adenosine receptor agonist allosteric enhancers having improved potency. |
| AID1243871 | Positive allosteric enhancement of human cloned adenosine A1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation at 10 uM using [3H]-cAMP by scintillation counting relative to control | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and biological evaluation of a new series of 2-amino-3-aroyl thiophene derivatives as agonist allosteric modulators of the A1 adenosine receptor. A position-dependent effect study. |
| AID1243878 | Binding affinity to human adenosine A1 receptor expressed in CHO cells assessed as fold Ki shift of CCPA at 10 uM after 90 mins by [3H]-CCPA displacement assay relative to control | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and biological evaluation of a new series of 2-amino-3-aroyl thiophene derivatives as agonist allosteric modulators of the A1 adenosine receptor. A position-dependent effect study. |
| AID1243874 | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells at 10 uM after 120 mins by scintillation counting | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and biological evaluation of a new series of 2-amino-3-aroyl thiophene derivatives as agonist allosteric modulators of the A1 adenosine receptor. A position-dependent effect study. |
| AID1061870 | Potentiation of [3H]CCPA binding to human adenosine A1 receptor expressed in CHO cell membranes at 10 uM after 90 mins relative to [3H]CCPA-treated control | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Synthesis and biological evaluation of novel 2-amino-3-aroyl-4-neopentyl-5-substituted thiophene derivatives as allosteric enhancers of the A₁ adenosine receptor. |
| AID1061874 | Displacement of [3H]-ZM241385 from human adenosine A2A receptor expressed in CHO cell membranes at 10 uM by scintillation counting analysis relative to control | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Synthesis and biological evaluation of novel 2-amino-3-aroyl-4-neopentyl-5-substituted thiophene derivatives as allosteric enhancers of the A₁ adenosine receptor. |
| AID363470 | Activity at human recombinant adenosine A1 receptor expressed in CHO cells assessed as of cAMP level at 0.1 uM | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor. |
| AID32629 | Percent change in cAMP content of CHO (Chinese hamster ovary) cells expressing human Adenosine A1 receptor at 10 uM | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Synthesis and biological effects of novel 2-amino-3-naphthoylthiophenes as allosteric enhancers of the A1 adenosine receptor. |
| AID1243877 | Binding affinity to human adenosine A1 receptor expressed in CHO cells assessed as fold Bmax shift of [3H]-CCPA at 10 uM after 90 mins by [3H]-CCPA binding assay relative to control | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and biological evaluation of a new series of 2-amino-3-aroyl thiophene derivatives as agonist allosteric modulators of the A1 adenosine receptor. A position-dependent effect study. |
| AID637821 | Displacement of [3H]DPCPX from A1 adenosine receptor in rat membranes | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
| Structure-activity relationships of 2-amino-3-aroyl-4-[(4-arylpiperazin-1-yl)methyl]thiophenes. Part 2: Probing the influence of diverse substituents at the phenyl of the arylpiperazine moiety on allosteric enhancer activity at the A₁ adenosine receptor. |
| AID31264 | Enhanced 0.5 nM [3H]CCPA dissociation from adenosine A1 receptor of rat brain cortex membranes compared to 100 uM CPA | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Allosteric modulation of the adenosine A(1) receptor. Synthesis and biological evaluation of novel 2-amino-3-benzoylthiophenes as allosteric enhancers of agonist binding. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6
| A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| AID1345685 | Human A1 receptor (Adenosine receptors) | 1990 | Molecular pharmacology, Dec, Volume: 38, Issue:6
| Allosteric enhancement of adenosine A1 receptor binding and function by 2-amino-3-benzoylthiophenes. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |