PK 11195 [Ligand Id: 8703] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL481537 (PK-11195) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907607] [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14] | ||||||||
| ChEMBL | In vitro inhibition of [11C]flumazenil binding to GABA-A central benzodiazepine receptor of rat brain | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2004) 47: 2228-2235 [PMID:15084121] |
| ChEMBL | Displacement of [11C]Flumazenil from Sprague-Dawley rat brain CBR | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2006) 49: 2735-2742 [PMID:16640334] |
| ChEMBL | Affinity benzodiazepine receptor as ability to displace [3H]flunitrazepam from binding to membrane preparations from rat cerebral cortex. | B | 4.67 | pIC50 | 21379.62 | nM | IC50 | J Med Chem (1999) 42: 3934-3941 [PMID:10508441] |
| ChEMBL | In vitro displacement of [11C]Flumazenil from (CBR) central GABA-A benzodiazepine receptor of rat brain | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 201-204 [PMID:12482423] |
| Constitutive androstane receptor/Nuclear receptor subfamily 1 group I member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5503] [GtoPdb: 607] [UniProtKB: Q14994] | ||||||||
| ChEMBL | Inverse agonist activity at GST tagged-human CAR-LBD assessed as reduction in fluorescein-PGC1 alpha coactivator recruitment after 1 hr by TR-FRET assay | B | 6.41 | pIC50 | 390 | nM | IC50 | Eur J Med Chem (2016) 108: 505-528 [PMID:26717202] |
| Translocator protein in Human [GtoPdb: 2879] [UniProtKB: P30536] | ||||||||
| GtoPdb | - | - | 8.15 | pKi | 7.11 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4819-22 [PMID:21741237] |
| Translocator protein/Peripheral-type benzodiazepine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4552] [GtoPdb: 2879] [UniProtKB: P16257] | ||||||||
| ChEMBL | Binding affinity constant for peripheral (mitochondrial) Benzodiazepine receptor | B | 8.7 | pKd | 2 | nM | Kd | J Med Chem (1995) 38: 4730-4738 [PMID:7473601] |
| ChEMBL | Displacement of [3H]PK11195 from TSPO in rat cortex | B | 9.22 | pKd | 0.6 | nM | Kd | J Med Chem (2009) 52: 581-592 [PMID:19133775] |
| ChEMBL | Displacement of [3H]PK11195 from PBR in rat kidney mitochondrial membrane | B | 7.54 | pKi | 28.8 | nM | Ki | Bioorg Med Chem (2008) 16: 6145-6155 [PMID:18472268] |
| ChEMBL | Displacement of [3H]-PK11195 from TSPO in Sprague-Dawley rat brain homogenates after 90 mins by liquid scintillation counting analysis | B | 8 | pKi | 10 | nM | Ki | Medchemcomm (2013) 4: 1461-1466 |
| ChEMBL | Displacement of [3H]PK11195 from TSPO in Sprague-Dawley rat brain homogenates by liquid scintillation counting | B | 8.01 | pKi | 9.8 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 954-957 [PMID:20045646] |
| ChEMBL | Displacement of [3H]PK 11195 from peripheral-type benzodiazepine receptor in rat kidney mitochondrial membranes | B | 8.03 | pKi | 9.3 | nM | Ki | J Med Chem (2007) 50: 404-407 [PMID:17228885] |
| ChEMBL | Displacement of [3H]PK11195 from translocator protein in rat kidney mitochondrial membrane | B | 8.03 | pKi | 9.3 | nM | Ki | J Med Chem (2008) 51: 5798-5806 [PMID:18729350] |
| ChEMBL | Displacement of [3H]PK11195 from TSPO in rat kidney mitochondrial membranes | B | 8.03 | pKi | 9.3 | nM | Ki | J Med Chem (2014) 57: 2413-2428 [PMID:24580635] |
| ChEMBL | Displacement of [3H]PK11195 from TSPO receptor in rat kidney membranes | B | 8.03 | pKi | 9.3 | nM | Ki | Eur J Med Chem (2011) 46: 4506-4520 [PMID:21824692] |
| ChEMBL | Binding affinity to peripheral benzodiazepine receptors using [3H]-PK11195 radioligand in rat kidney mitochondrial membrane | B | 8.03 | pKi | 9.3 | nM | Ki | J Med Chem (2004) 47: 1852-1855 [PMID:15027878] |
| ChEMBL | Inhibition of [3H]PK11195 binding to TSPO in rat kidney mitochondrial membranes | B | 8.03 | pKi | 9.3 | nM | Ki | J Med Chem (2015) 58: 6081-6092 [PMID:26177193] |
| ChEMBL | Displacement of [3H]PK11195 from TSPO in rat kidney mitochondrial membranes by competitive binding assay | B | 8.03 | pKi | 9.3 | nM | Ki | J Med Chem (2012) 55: 4506-4510 [PMID:22489952] |
| ChEMBL | Displacement of [3H]PK11195 from TSPO in rat kidney mitochondrial fraction | B | 8.03 | pKi | 9.3 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4819-4822 [PMID:21741237] |
| ChEMBL | Displacement of [3H]PK11195 from TSPO in rat kidney | B | 8.03 | pKi | 9.3 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 5799-5802 [PMID:20727749] |
| ChEMBL | Displacement of [11C]PK11195 from TSPO in rat kidney mitochondrial membrane | B | 8.03 | pKi | 9.3 | nM | Ki | J Med Chem (2011) 54: 366-373 [PMID:21133364] |
| ChEMBL | Displacement of [3H]PK11195 from TSPO in Sprague-Dawley rat cerebral cortex membranes after 60 mins by microbeta liquid scintillation counting method | B | 8.05 | pKi | 8.85 | nM | Ki | Eur J Med Chem (2017) 125: 1172-1192 [PMID:27855359] |
| ChEMBL | Inhibition of rat TSPO | B | 8.52 | pKi | 3 | nM | Ki | Eur J Med Chem (2015) 93: 392-400 [PMID:25725375] |
| ChEMBL | Displacement of [3H]PK11195 from TSPO in rat heart membrane homogenate | B | 8.74 | pKi | 1.8 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4819-4822 [PMID:21741237] |
| ChEMBL | Displacement of [3H]PK11195 from TSPO receptor in rat Sprague-Dawley kidney membranes after 1 hr by liquid scintillation counting | B | 8.77 | pKi | 1.7 | nM | Ki | Bioorg Med Chem (2012) 20: 5568-5582 [PMID:22884355] |
| ChEMBL | Displacement of [3H]PK11195 from TSPO in Sprague-Dawley rat kidney mitochondria after 1 hr by liquid scintillation counting analysis | B | 8.77 | pKi | 1.7 | nM | Ki | Bioorg Med Chem (2013) 21: 1257-1267 [PMID:23352481] |
| ChEMBL | Displacement of [3H]PK11195 from Sprague-Dawley rat kidney TSPO after 1 hr by liquid scintillation counting analysis | B | 8.77 | pKi | 1.7 | nM | Ki | J Med Chem (2013) 56: 8191-8195 [PMID:24050790] |
| ChEMBL | Displacement of [3H]PK11195 from TSPO in Wistar rat heart incubated for 15 mins | B | 8.91 | pKi | 1.24 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 5795-5800 [PMID:22902658] |
| ChEMBL | Displacement of [3H]PK11195 from peripheral benzodiazepine receptor in Sprague-Dawley rat cerebral cortex membrane by liquid scintillation counting | B | 8.94 | pKi | 1.14 | nM | Ki | J Med Chem (2008) 51: 6876-6888 [PMID:18834105] |
| ChEMBL | Displacement of [3H]PK11195 from TSPO receptor in rat kidney membranes | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2011) 54: 2961-2970 [PMID:21428406] |
| ChEMBL | In vitro inhibition of [11C]2 binding to Peripheral benzodiazepine receptor (PBR) in rat brain | B | 9.08 | pKi | 0.83 | nM | Ki | J Med Chem (2004) 47: 2228-2235 [PMID:15084121] |
| ChEMBL | Displacement of [11C]DAA1106 from Sprague-Dawley rat brain PBR | B | 9.09 | pKi | 0.82 | nM | Ki | J Med Chem (2006) 49: 2735-2742 [PMID:16640334] |
| ChEMBL | Binding affinity against peripheral-type benzodiazepine receptor (PBR) from rat cortex homogenate using [3H]-PK 11195 as radioligand | B | 9.11 | pKi | 0.78 | nM | Ki | J Med Chem (1996) 39: 3435-3450 [PMID:8784441] |
| ChEMBL | Displacement of [11C](R)-PK1119 from Sprague-Dawley rat brain PBR | B | 9.27 | pKi | 0.54 | nM | Ki | J Med Chem (2006) 49: 2735-2742 [PMID:16640334] |
| ChEMBL | Displacement of [3H]PK11195 from TSPO in rat C6 cell membrane after 90 mins by radioligand binding assay | B | 9.4 | pKi | 0.4 | nM | Ki | ACS Med Chem Lett (2014) 5: 685-689 [PMID:24944744] |
| ChEMBL | Displacement of [11C]PK11195 from PBR receptor in rat brain membrane | B | 9.51 | pKi | 0.31 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 1707-1710 [PMID:19217778] |
| ChEMBL | Displacement of [3H]PK11195 from TSPO receptor in Sprague-Dawley rat cerebral cortex membrane by radiometric competitive assay | B | 7.91 | pIC50 | 12.3 | nM | IC50 | Eur J Med Chem (2015) 103: 210-222 [PMID:26355532] |
| ChEMBL | Displacement of [11C]PK-11195 from PBR in Sprague-Dawley rat brain | B | 8.04 | pIC50 | 9.2 | nM | IC50 | J Med Chem (2007) 50: 848-855 [PMID:17300167] |
| ChEMBL | Test in vitro, for potential ability to displace [3H]1 from PBR in rat brain cortex | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2001) 44: 1134-1150 [PMID:11312914] |
| ChEMBL | Inhibitory activity against specific binding of [3H]-CB 34 to peripheral benzodiazepine receptor in rat cortical membranes was evaluated | B | 8.08 | pIC50 | 8.4 | nM | IC50 | J Med Chem (2003) 46: 3568-3571 [PMID:12904061] |
| ChEMBL | Displacement of [11C]DAA1106 from PBR in Sprague-Dawley rat brain | B | 8.08 | pIC50 | 8.3 | nM | IC50 | J Med Chem (2007) 50: 848-855 [PMID:17300167] |
| ChEMBL | In vitro displacement of [11C]DAA1106 from PBR (peripheral benzodiazepine receptor) of rat brain | B | 8.08 | pIC50 | 8.26 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 201-204 [PMID:12482423] |
| ChEMBL | Displacement of [3H]PK11195 from TSPO in Sprague-Dawley rat cerebral cortex membranes after 60 mins by liquid scintillation counting analysis | B | 8.12 | pIC50 | 7.5 | nM | IC50 | Eur J Med Chem (2017) 141: 240-256 [PMID:29031071] |
| ChEMBL | Test in vitro, for potential ability to displace [3H]1 from PBR in rat brain cortex | B | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (2001) 44: 1134-1150 [PMID:11312914] |
| ChEMBL | In vitro displacement of [3H]PK11195 from the peripheral benzodiazepine receptor (PBR) in rat cortex | B | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (1997) 40: 2910-2921 [PMID:9288173] |
| ChEMBL | In vitro binding affinity (pIC50) was tested against peripheral benzodiazepine receptor (PBR) in rat. | B | 8.66 | pIC50 | 2.19 | nM | IC50 | J Med Chem (1997) 40: 2910-2921 [PMID:9288173] |
| ChEMBL | Displacement of [3H]PK115 from peripheral benzodiazepine receptor in Sprague-Dawley rat cortical membrane | B | 8.68 | pIC50 | 2.1 | nM | IC50 | Bioorg Med Chem (2008) 16: 3428-3437 [PMID:18294852] |
| ChEMBL | Displacement of [3H]-PK 11195 from rat peripheral (mitochondrial) benzodiazepine receptor | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1994) 37: 4100-4108 [PMID:7990110] |
| ChEMBL | Displacement of [3H]-PK 11195 from peripheral (mitochondrial) benzodiazepine receptor | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1994) 37: 1427-1438 [PMID:8182701] |
| ChEMBL | Ability to inhibit [3H]-PK 11195 binding to peripheral-type benzodiazepine receptor(PBR) in rat cerebral cortex homogenate. | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1996) 39: 2922-2938 [PMID:8709127] |
| ChEMBL | Inhibition of binding of [3H]-PK 11195 to peripheral-type benzodiazepine receptor (PBR) from rat cortex homogenate | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1996) 39: 3435-3450 [PMID:8784441] |
| ChEMBL | Displacement of [3H]-PK 11195 from peripheral-type benzodiazepine receptor of rat ovary membranes | B | 8.74 | pIC50 | 1.82 | nM | IC50 | J Med Chem (1999) 42: 3934-3941 [PMID:10508441] |
| ChEMBL | Binding affinity against peripheral benzodiazepine receptor( PBR). | B | 8.74 | pIC50 | 1.8 | nM | IC50 | J Med Chem (1996) 39: 4275-4284 [PMID:8863805] |
| ChEMBL | Displacement of [3H]PK 11195 from rat heart Peripheral-type benzodiazepine receptor | B | 8.8 | pIC50 | 1.6 | nM | IC50 | Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801] |
| ChEMBL | Displacement of [3H]PK 11195 from rat heart peripheral-type benzodiazepine receptor measured after 15 mins by scintillation counting method | B | 8.8 | pIC50 | 1.6 | nM | IC50 | Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250] |
| ChEMBL | Displacement of [3H]-PK 11195 from peripheral-type benzodiazepine receptor of rat cerebral cortex membranes | B | 8.85 | pIC50 | 1.41 | nM | IC50 | J Med Chem (1999) 42: 3934-3941 [PMID:10508441] |
| ChEMBL | Displacement of [3H]PK11195 from TSPO in Sprague-Dawley rat cerebral cortex membranes after 60 mins by microbeta liquid scintillation counting method | B | 8.88 | pIC50 | 1.32 | nM | IC50 | Eur J Med Chem (2017) 125: 1172-1192 [PMID:27855359] |
| ChEMBL | Displacement of [3H]PK11195 from TSPO in Sprague-Dawley rat brain homogenates after 90 mins by liquid scintillation spectrometry | B | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (2011) 54: 7165-7175 [PMID:21916402] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5.2 | pIC50 | 6309.57 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| Translocator protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5742] [GtoPdb: 2879] [UniProtKB: P30536] | ||||||||
| ChEMBL | Binding affinity to recombinant human TSPO by SPR assay | B | 7.95 | pKd | 11.1 | nM | Kd | Eur J Med Chem (2017) 125: 1172-1192 [PMID:27855359] |
| ChEMBL | Binding affinity to C-terminal DDK-tagged human recombinant full-length TSPO expressed in HEK293 cells by SPR assay | B | 7.95 | pKd | 11.1 | nM | Kd | Eur J Med Chem (2017) 141: 240-256 [PMID:29031071] |
| ChEMBL | Binding affinity to human PBR | B | 8.7 | pKd | 2 | nM | Kd | Bioorg Med Chem (2008) 16: 6145-6155 [PMID:18472268] |
| ChEMBL | Displacement of [3H]PK11195 from human TSPO A147T mutant expressed in HEK293T cell membranes after 90 mins by scintillation counting method | B | 7.44 | pKi | 36 | nM | Ki | Medchemcomm (2017) 8: 202-210 [PMID:30108706] |
| ChEMBL | Displacement of [3H]PK11195 from human TSPO A147T mutant expressed in HEK293 cells after 90 mins by scintillation counting method | B | 7.44 | pKi | 36 | nM | Ki | RSC Med Chem (2020) 11: 511-517 [PMID:33479652] |
| ChEMBL | Displacement of [3H]PK11195 from human wild type TSPO expressed in HEK293T cell membranes after 90 mins by scintillation counting method | B | 7.53 | pKi | 29.2 | nM | Ki | Medchemcomm (2017) 8: 202-210 [PMID:30108706] |
| ChEMBL | Displacement of [3H]PK11195 from wild-type human TSPO expressed in HEK293 cell membranes after 90 mins by scintillation counting method | B | 7.53 | pKi | 29.2 | nM | Ki | RSC Med Chem (2020) 11: 511-517 [PMID:33479652] |
| ChEMBL | Displacement of [3H]PK11195 from TSPO in human HEK293 mitochondrial fraction | B | 8.15 | pKi | 7.11 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4819-4822 [PMID:21741237] |
| GtoPdb | - | - | 8.15 | pKi | 7.11 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4819-22 [PMID:21741237] |
| ChEMBL | Inhibition of human TSPO | B | 8.35 | pKi | 4.5 | nM | Ki | Eur J Med Chem (2015) 93: 392-400 [PMID:25725375] |
| ChEMBL | Displacement of radiolabeled PK 11195 from peripheral-type benzodiazepine receptor | B | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| ChEMBL | Displacement of [3H]-PK11195 from PBR after 1 hr by scintillation counting | B | 6.31 | pIC50 | 490 | nM | IC50 | ACS Med Chem Lett (2011) 2: 136-141 [PMID:24900292] |
| ChEMBL | Displacement of radiolabeled PK 11195 from peripheral-type benzodiazepine receptor | B | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| ChEMBL | Inhibition of TSPO (unknown origin) | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Eur J Med Chem (2017) 125: 1172-1192 [PMID:27855359] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
