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ChEMBL ligand: CHEMBL481537 (PK-11195) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]-PK11195 from rat kidney mitochondrial membrane TSPO receptor assessed as inhibition constant | B | 8.03 | pKi | 9.3 | nM | Ki | J Med Chem (2021) 64: 3508-3545 [PMID:33764065] |
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 | 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 | 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 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 receptor in rat kidney membranes | B | 8.03 | pKi | 9.3 | nM | Ki | Eur J Med Chem (2011) 46: 4506-4520 [PMID:21824692] |
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 membranes | B | 8.03 | pKi | 9.3 | nM | Ki | J Med Chem (2014) 57: 2413-2428 [PMID:24580635] |
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 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 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 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 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]-flunitrazepam from TSPO receptor in Wistar rat brain without cerebellum incubated for 90 mins by liquid scintillation counter analysis | B | 8.94 | pKi | 1.14 | nM | Ki | Eur J Med Chem (2021) 209: 112924-112924 [PMID:33081988] |
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 | Displacement of [3H]CB34 from TSPO receptor in rat brain cortex membrane by liquid scintillation spectrometer method | B | 8.08 | pIC50 | 8.4 | nM | IC50 | J Med Chem (2021) 64: 9649-9676 [PMID:34254805] |
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 | 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 | 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 | 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 (mitochondrial) benzodiazepine receptor | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1994) 37: 1427-1438 [PMID:8182701] |
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]PK11195 from TSPO receptor in rat brain cortex membrane incubated for 120 mins by liquid scintillation spectrometer method | B | 8.74 | pIC50 | 1.8 | nM | IC50 | J Med Chem (2021) 64: 9649-9676 [PMID:34254805] |
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 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 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]