| Assay ID | Title | Year | Journal | Article |
|---|
| AID1695086 | Displacement of [3H]PK11195 from wild-type human TSPO expressed in HEK293 cell membranes after 90 mins by scintillation counting method | 2020 | RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4
| Reversing binding sensitivity to A147T translocator protein. |
| AID1256255 | Potentiation of antiproliferative activity of PK11195 at 100 uM against human T98G cells incubated for 48 hrs by BrdU enzyme-linked immunosorbent assay | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
| First Demonstration of Positive Allosteric-like Modulation at the Human Wild Type Translocator Protein (TSPO). |
| AID1506535 | Displacement of [3H]PK11195 from human TSPO A147T mutant expressed in HEK293T cell membranes after 90 mins by scintillation counting method | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1
| Determination and reduction of translocator protein (TSPO) ligand rs6971 discrimination. |
| AID516406 | Displacement of [3H]Ro151788 from CBR in rat kidney | 2010 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19
| Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO). |
| AID1256257 | Cytotoxicity against human T98G cells assessed as cell viability after 48 hrs by cell titer blue staining based fluorescence method | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
| First Demonstration of Positive Allosteric-like Modulation at the Human Wild Type Translocator Protein (TSPO). |
| AID1256249 | Displacement of [3H]PK11195 from TSPO in human HEK293T cell membranes incubated for 90 mins by competition radioligand binding assay | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
| First Demonstration of Positive Allosteric-like Modulation at the Human Wild Type Translocator Protein (TSPO). |
| AID1695085 | Displacement of [3H]PK11195 from human TSPO A147T mutant expressed in HEK293 cells after 90 mins by scintillation counting method | 2020 | RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4
| Reversing binding sensitivity to A147T translocator protein. |
| AID1256256 | Cytotoxicity against human T98G cells assessed as cell viability in the presence of PK11195 after 48 hrs by cell titer blue staining based fluorescence method | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
| First Demonstration of Positive Allosteric-like Modulation at the Human Wild Type Translocator Protein (TSPO). |
| AID1705620 | Displacement of [3H]-PK11195 from wild type TSPO (unknown origin) expressed in human HEK293T cells assessed as inhibitory constant incubated for 90 mins by microbeta scintillation counting method | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Tricyclic heterocycles display diverse sensitivity to the A147T TSPO polymorphism. |
| AID1506533 | Selectivity ratio of Ki for human TSPO A147T mutant to Ki for human wild type TSPO | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1
| Determination and reduction of translocator protein (TSPO) ligand rs6971 discrimination. |
| AID516405 | Displacement of [3H]PK11195 from TSPO in rat kidney | 2010 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19
| Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO). |
| AID1506534 | Displacement of [3H]PK11195 from human wild type TSPO expressed in HEK293T cell membranes after 90 mins by scintillation counting method | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1
| Determination and reduction of translocator protein (TSPO) ligand rs6971 discrimination. |
| AID1506536 | Cytotoxicity against HEK293T cells expressing human TSPO A147T mutant assessed as decrease in cell viability after 48 hrs by CellTiter blue assay | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1
| Determination and reduction of translocator protein (TSPO) ligand rs6971 discrimination. |
| AID1695087 | Selectivity index, ratio of Ki for human TSPO A147T mutant expressed in HEK293 cell membranes to Ki for human TSPO expressed in HEK293 cell membranes | 2020 | RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4
| Reversing binding sensitivity to A147T translocator protein. |
| AID1705621 | Selectivity index, ratio of Ki for TSPO A147T mutant (unknown origin) to Ki for wild type TSPO (unknown origin) | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Tricyclic heterocycles display diverse sensitivity to the A147T TSPO polymorphism. |
| AID1506538 | Antiproliferative activity against HEK293T cells expressing human wild type TSPO after 48 hrs by BrdU incorporation assay | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1
| Determination and reduction of translocator protein (TSPO) ligand rs6971 discrimination. |
| AID1705619 | Displacement of [3H]-PK11195 from TSPO A147T mutant (unknown origin) expressed in human HEK293T cells assessed as inhibitory constant incubated for 90 mins by microbeta scintillation counting method | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Tricyclic heterocycles display diverse sensitivity to the A147T TSPO polymorphism. |
| AID368144 | Displacement of [3H]PK11195 from TSPO in rat kidney membrane | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
| The translocator protein (18 kDa): central nervous system disease and drug design. |
| AID1506532 | Cytotoxicity against HEK293T cells expressing human wild type TSPO assessed as decrease in cell viability after 48 hrs by CellTiter blue assay | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1
| Determination and reduction of translocator protein (TSPO) ligand rs6971 discrimination. |
| AID733338 | Lipophilicity, log P of the compound at pH 7.5 by reversed phase HPLC analysis | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| Synthesis and structure-activity relationships of 5,6,7-substituted pyrazolopyrimidines: discovery of a novel TSPO PET ligand for cancer imaging. |
| AID1256250 | Displacement of [3H]PK11195 from TSPO in human T98G cell membranes incubated for 90 mins by competition radioligand binding assay | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
| First Demonstration of Positive Allosteric-like Modulation at the Human Wild Type Translocator Protein (TSPO). |
| AID1256251 | Antiproliferative activity against human T98G cells at 1 to 100 uM incubated for 48 hrs by BrdU enzyme-linked immunosorbent assay | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
| First Demonstration of Positive Allosteric-like Modulation at the Human Wild Type Translocator Protein (TSPO). |
| AID1506541 | Ratio of Ki for displacement of [3H]PK11195 from human brain TSPO isolated from low affinity binder patient to Ki for [3H]PK11195 from human brain TSPO isolated from high affinity binder patient | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1
| Determination and reduction of translocator protein (TSPO) ligand rs6971 discrimination. |
| AID1506539 | Antiproliferative activity against HEK293T cells expressing human TSPO A147T mutant after 48 hrs by BrdU incorporation assay | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1
| Determination and reduction of translocator protein (TSPO) ligand rs6971 discrimination. |
| AID733339 | Displacement of [3H]-PK 11195 from TSPO in rat C6 cell lysates after 2 hrs by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| Synthesis and structure-activity relationships of 5,6,7-substituted pyrazolopyrimidines: discovery of a novel TSPO PET ligand for cancer imaging. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |