| AID1604529 | Binding affinity to GABA-A alpha1 (unknown origin) | | | |
| AID1551057 | Inverse agonist activity at recombinant human GABA-A alpha5beta3gamma2 receptor expressed in mouse L(tk-) cells by radioligand binding assay | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | GABA allosteric modulators: An overview of recent developments in non-benzodiazepine modulators. |
| AID239700 | Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-2-beta-3-gamma-2 expressed in L(tk-) cells | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties. |
| AID260505 | Efficacy against human GABA alpha-3 receptor expressed in mouse fibroblast L(tk-) cells by whole cell patch clamp method | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
| Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction. |
| AID726073 | Positive allosteric modulation of GABAA alpha5 (unknown origin) relative to control | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Ion channels as therapeutic targets: a drug discovery perspective. |
| AID235954 | Oral bioavailability in rat | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties. |
| AID1604581 | Negative allosteric modulation of GABA-A alpha1 (unknown origin) assessed as reduction in DMCM induced current relative to DMCM | | | |
| AID1551055 | Inverse agonist activity at recombinant human GABA-A alpha5beta3gamma2 receptor expressed in mouse L(tk-) cells by whole-cell patch-Clamp method | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | GABA allosteric modulators: An overview of recent developments in non-benzodiazepine modulators. |
| AID1604528 | Binding affinity to GABA-A alpha2 (unknown origin) | | | |
| AID243406 | In vitro percent efficacy against human gamma-aminobutyric-acid A receptor alpha-3-beta-3-gamma-2 expressed in L(tk-) cells | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties. |
| AID238554 | Binding affinity towards gamma-aminobutyric-acid GABA-A receptor alpha-4-beta-3-gamma-2 | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties. |
| AID243407 | In vitro percent efficacy against human gamma-aminobutyric-acid A receptor alpha-5-beta-3-gamma-2 expressed in L(tk-) cells | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties. |
| AID260507 | Receptor occupancy in vivo by displacement of [3H]Ro 15-1788 binding from rat brain GABAA receptor at 3 mg/kg, ip | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
| Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction. |
| AID260500 | Clearance in rhesus | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
| Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction. |
| AID1604530 | Binding affinity to GABA-A alpha3 (unknown origin) | | | |
| AID260504 | Efficacy against human GABA alpha-2 receptor expressed in mouse fibroblast L(tk-) cells by whole cell patch clamp method | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
| Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction. |
| AID243445 | Concentration required to occupy 50% of gamma-aminobutyric-acid GABA-A receptor alpha subtype at 0.75 hr after dose | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties. |
| AID726074 | Positive allosteric modulation of GABAA alpha3 (unknown origin) relative to control | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Ion channels as therapeutic targets: a drug discovery perspective. |
| AID1551056 | Displacement of [3H]Ro15-1788 from recombinant human GABA-A alpha5beta3gamma2 receptor expressed in mouse L(tk-) cells by radioligand binding assay | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | GABA allosteric modulators: An overview of recent developments in non-benzodiazepine modulators. |
| AID1604598 | In vivo receptor occupancy at GABAA receptor in iv dosed rhesus monkey assessed as plasma concentration causing 50% reduction in [11C]-flumazenil receptor labeling by PET method | | | |
| AID243404 | In vitro percent efficacy against human gamma-aminobutyric-acid A receptor alpha-1-beta-3-gamma-2 expressed in L(tk-) cells | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties. |
| AID726075 | Positive allosteric modulation of GABAA alpha2 (unknown origin) relative to control | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Ion channels as therapeutic targets: a drug discovery perspective. |
| AID260495 | Oral bioavailability in rat | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
| Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction. |
| AID1604597 | In vivo receptor occupancy at GABAA receptor in po dosed Sprague-Dawley rat assessed as plasma concentration causing 50% reduction in [3H]-flumazenil receptor labeling after 0.5 hrs | | | |
| AID260493 | Half life in rat | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
| Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction. |
| AID239699 | Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-1-beta-3-gamma-2 expressed in L(tk-) cells | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties. |
| AID260497 | Clearance in dog | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
| Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction. |
| AID260503 | Efficacy against human GABA alpha-1 receptor expressed in mouse fibroblast L(tk-) cells by whole cell patch clamp method | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
| Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction. |
| AID260499 | Half life in rhesus | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
| Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction. |
| AID243405 | In vitro percent efficacy against human gamma-aminobutyric-acid A receptor alpha-2-beta-3-gamma-2 expressed in L(tk-) cells | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties. |
| AID238555 | Binding affinity towards gamma-aminobutyric-acid GABA-A receptor alpha-6-beta-3-gamma-2 | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties. |
| AID260494 | Clearance in rat | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
| Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction. |
| AID726244 | Positive allosteric modulation of GABAA alpha5 (unknown origin) | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Ion channels as therapeutic targets: a drug discovery perspective. |
| AID1604582 | Binding affinity to GABA-A alpha2 (unknown origin) assessed as reduction in DMCM induced current relative to DMCM | | | |
| AID726072 | Positive allosteric modulation of GABAA alpha1 (unknown origin) relative to control | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Ion channels as therapeutic targets: a drug discovery perspective. |
| AID726245 | Positive allosteric modulation of GABAA alpha2 (unknown origin) | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Ion channels as therapeutic targets: a drug discovery perspective. |
| AID239702 | Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-5-beta-3-gamma-2 expressed in L(tk-) cells | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties. |
| AID260496 | Half life in dog | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
| Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction. |
| AID1604583 | Binding affinity to GABA-A alpha3 (unknown origin) assessed as reduction in DMCM induced current relative to DMCM | | | |
| AID235953 | Oral bioavailability in dog | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties. |
| AID260501 | Oral bioavailability in rhesus | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
| Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction. |
| AID1604599 | Invivo receptor occupancy at GABAA receptor in human at 5 mg, po relative to control | | | |
| AID260506 | Efficacy against human GABA alpha-5 receptor expressed in mouse fibroblast L(tk-) cells by whole cell patch clamp method | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
| Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction. |
| AID1604596 | In vivo receptor occupancy at GABAA receptor in po dosed Sprague-Dawley rat assessed as brain concentration causing 50% reduction in [3H]-flumazenil receptor labeling after 0.5 hrs | | | |
| AID1604584 | Binding affinity to GABA-A alpha5 (unknown origin) assessed as reduction in DMCM induced current relative to DMCM | | | |
| AID239701 | Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-3-beta-3-gamma-2 expressed in L(tk-) cells | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties. |
| AID1604531 | Binding affinity to GABA-A alpha5 (unknown origin) | | | |
| AID726246 | Positive allosteric modulation of GABAA alpha3 (unknown origin) | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Ion channels as therapeutic targets: a drug discovery perspective. |
| AID260498 | Oral bioavailability in dog | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
| Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction. |
| AID260502 | Binding affinity to GABA alpha5 receptor | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
| Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction. |
| AID726242 | Positive allosteric modulation of GABAA alpha1 (unknown origin) | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Ion channels as therapeutic targets: a drug discovery perspective. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |