ifenprodil [Ligand Id: 5472] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL305187 (Ifenprodil, Ifenprodil hemitartrate, Ifenprodil tartrate, NP-120, RC 61-91, RC-61-91, Vadilex) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 3-beta-hydroxysteroid-delta(8),delta(7)-isomerase in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5525] [UniProtKB: Q60490] | ||||||||
| ChEMBL | Displacement of [3H]emopamil from Delta-(8)-Delta-(7) sterol isomerase in guinea pig liver membrane | B | 7.7 | pKi | 19.8 | nM | Ki | J Med Chem (2007) 50: 4648-4655 [PMID:17713896] |
| ChEMBL | Displacement of [3H](-)-(S)-emopamil from EBP in guinea pig liver membrane | B | 7.79 | pKi | 16.4 | nM | Ki | J Med Chem (2008) 51: 7523-7531 [PMID:19053780] |
| ChEMBL | Displacement of [3H]-emopamil from delta(8)-delta(7) sterol isomerase in guinea pig liver membranes | B | 7.82 | pKi | 15 | nM | Ki | Bioorg Med Chem (2011) 19: 7612-7622 [PMID:22075234] |
| ChEMBL | Displacement of [3H](+/-)-emopamil from EBP in Dunkin guinea pig liver membrane by radioreceptor binding assay | B | 7.99 | pKi | 10.2 | nM | Ki | J Med Chem (2009) 52: 7817-7828 [PMID:19842660] |
| ChEMBL | Displacement of [3H](+/-)-emopamil from delta8-delta7 sterol isomerase (SI) site in guinea pig liver membranes | B | 8.33 | pKi | 4.7 | nM | Ki | J Med Chem (2005) 48: 8237-8244 [PMID:16366605] |
| ChEMBL | Inhibition of [3H]-emopamil binding to Sterol delta 8-delta 7 isomerase in guinea pig liver membrane | B | 8.57 | pKi | 2.71 | nM | Ki | J Med Chem (2003) 46: 2117-2124 [PMID:12747784] |
| D1 receptor/Dopamine D1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3071] [GtoPdb: 214] [UniProtKB: Q61616] | ||||||||
| ChEMBL | Compound was tested for the binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1991) 34: 3085-3090 [PMID:1681106] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Compound was tested for the binding affinity against dopamine receptor D2 by using [3H]spiperone as radioligand | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1991) 34: 3085-3090 [PMID:1681106] |
| GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7] | ||||||||
| ChEMBL | N-methyl-D-aspartate glutamate receptor antagonistic activity in cell culture(CC)model | F | 6.58 | pIC50 | 263 | nM | IC50 | J Med Chem (1991) 34: 3085-3090 [PMID:1681106] |
| GluN1/GluN2B/Glutamate NMDA receptor; GRIN1/GRIN2B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907603] [GtoPdb: 455, 457] [UniProtKB: Q05586, Q13224] | ||||||||
| ChEMBL | Displacement of [3H]ifenprodil from human recombinant NR1-1a/NR2B receptor expressed in mouse L(tk-) cells after 120 mins by scintillation counting | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem (2010) 18: 8005-8015 [PMID:20965739] |
| ChEMBL | Displacement of [3H]-ifenprodil from GluN1a/GluN2B (unknown origin) expressed in L(tk-) cell membranes after 120 mins by scintillation counting analysis | B | 8 | pKi | 10 | nM | Ki | Eur J Med Chem (2018) 157: 397-404 [PMID:30103189] |
| ChEMBL | Antagonist activity against NR1/NR2B receptor expressed in xenopus oocytes assessed as inhibition of NMDA induced Ca2+ influx | F | 6.47 | pIC50 | 340 | nM | IC50 | Eur J Med Chem (2011) 46: 2295-2309 [PMID:21453995] |
| ChEMBL | Inhibition of GluN1/GluN2B receptor (unknown origin) expressed in Xenopus oocytes by voltage clamp assay | B | 6.47 | pIC50 | 340 | nM | IC50 | J Med Chem (2013) 56: 3121-3147 [PMID:23458846] |
| ChEMBL | Antagonist activity at wild type NR1/NR2B receptor expressed in Xenopus oocytes assessed as inhibition of agonist-induced current amplitude by two-electrode voltage-clamp method | F | 6.72 | pIC50 | 190 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 5552-5558 [PMID:20692832] |
| ChEMBL | Antagonist activity against NR1a/NR2B receptor transfected in human HEK293 cells assessed as inhibition of NMDA-induced Ca2+ influx | F | 6.75 | pIC50 | 177.4 | nM | IC50 | Eur J Med Chem (2011) 46: 2295-2309 [PMID:21453995] |
| ChEMBL | Inhibition of NR1/NR2B receptor expressed in xenopus oocytes assessed as effect on L-glutamate and glycine-induced current response | B | 6.96 | pIC50 | 110 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 2765-2770 [PMID:18434149] |
| ChEMBL | Antagonist activity at NR1/NR2B receptor assessed as inhibition of Glu/Gly induced Ca2+ influx | F | 7.18 | pIC50 | 66 | nM | IC50 | Eur J Med Chem (2011) 46: 2295-2309 [PMID:21453995] |
| GluN1/GluN2B/Glutamate NMDA receptor; Grin1/Grin2b in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096666] [GtoPdb: 455, 457] [UniProtKB: P35439, Q00960] | ||||||||
| ChEMBL | Inhibition of rat recombinant NR1/NR2B receptor expressed in Xenopus oocytes assessed as inhibition of glutamate and glycine-induced evoked current by two electrode voltage clamp method | B | 7.14 | pIC50 | 73 | nM | IC50 | J Med Chem (2008) 51: 5506-5521 [PMID:18800760] |
| GluN2A/Glutamate [NMDA] receptor subunit epsilon 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1972] [GtoPdb: 456] [UniProtKB: Q12879] | ||||||||
| ChEMBL | Negative allosteric modulation of human GluN2A receptor expressed in xenopus laevis oocytes assessed as reduction in 3 uM glycine-induced channel current at -40 mV holding potential by two electrode voltage clamp method | B | 4.4 | pIC50 | 39500 | nM | IC50 | J Med Chem (2018) 62: 3-23 [PMID:29446949] |
| GluN2B/Glutamate [NMDA] receptor subunit epsilon 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1904] [GtoPdb: 457] [UniProtKB: Q13224] | ||||||||
| ChEMBL | Displacement of [3H]ifenprodil from human GluN2B expressed in mouse L(tk-) cells co-expressing GluN1a after 120 mins by scintillation counting method | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem (2014) 22: 6638-6646 [PMID:25458498] |
| ChEMBL | Displacement of [3H]Ifenprodil from GluN2B receptor (unknown origin) expressed in mouse L(tk-) cell membranes incubated for 120 mins measured for 5 mins by scintillation counting method | B | 8 | pKi | 10 | nM | Ki | Eur J Med Chem (2018) 144: 672-681 [PMID:29289890] |
| ChEMBL | Displacement of [3H]-ifenprodil from GluN2B receptor (unknown origin) expressed in mouse L (tk-) cell membranes after 120 mins by scintillation counting method | B | 8 | pKi | 10 | nM | Ki | Medchemcomm (2017) 8: 975-981 [PMID:30108812] |
| ChEMBL | Displacement of [3H]-ifenprodil from GluN2B (unknown origin) expressed in rat L(tk) cells measured after 120 mins by scintillation counting analysis | B | 8 | pKi | 10 | nM | Ki | Medchemcomm (2019) 10: 315-325 [PMID:30881618] |
| ChEMBL | Displacement of [3H]ifenprodil from human recombinant GluN2B expressed in mouse L(tk-) cell membranes co-expressing GluN1a incubated for 120 mins by scintillation counting method | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem (2020) 28: 115245-115245 [PMID:31843460] |
| ChEMBL | Displacement of [3H]ifenprodil from GluN2B (unknown origin) expressed in mouse L(tk-) cell membranes co-expressing GluN1a incubated for 120 mins by scintillation counting method | B | 8 | pKi | 10 | nM | Ki | ACS Med Chem Lett (2020) 11: 651-656 [PMID:32435366] |
| ChEMBL | Displacement of [3H]ifenprodil from human GluN2B expressed in mouse L(tk-) cell membranes co-expressing GluN1a incubated for 2 hrs by scintillation counting method | B | 8 | pKi | 10 | nM | Ki | Eur J Med Chem (2020) 190: 112138-112138 [PMID:32070917] |
| ChEMBL | Negative allosteric modulation of human GluN2B receptor expressed in xenopus laevis oocytes assessed as reduction in 3 uM glycine-induced channel current at -40 mV holding potential by two electrode voltage clamp method | B | 6.96 | pIC50 | 110 | nM | IC50 | J Med Chem (2018) 62: 3-23 [PMID:29446949] |
| ChEMBL | Inhibition of NMDA receptor GluN2B subunit (unknown origin) | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem (2014) 22: 1040-1048 [PMID:24411196] |
| ChEMBL | Displacement of [3H]-ifenprodil from GluN2B (unknown origin) expressed in mouse L(tk) cells after 120 mins by MicroBeta scintillation counting analysis | B | 7.88 | pIC50 | 13.3 | nM | IC50 | Medchemcomm (2019) 10: 315-325 [PMID:30881618] |
| GluN2B/Glutamate [NMDA] receptor subunit epsilon 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL311] [GtoPdb: 457] [UniProtKB: Q00960] | ||||||||
| ChEMBL | Displacement of [3H]Ifenprodil from NMDAR-2B in Sprague-Dawley rat frontal cortex homogenates after 2 hrs by liquid scintillation counting | B | 7.54 | pKi | 29 | nM | Ki | J Med Chem (2012) 55: 9708-9721 [PMID:23033965] |
| ChEMBL | Displacement of [3H]ifenprodil from NR2B receptor in rat cortical synaptic membranes | B | 7.7 | pKi | 20 | nM | Ki | Bioorg Med Chem (2010) 18: 7497-7506 [PMID:20875744] |
| ChEMBL | Displacement of [3H]ifenprodil from Wistar rat cerebral cortex glutamate NMDA receptor GluN2B subunit after 120 mins by scintillation counting analysis | B | 7.72 | pKi | 19 | nM | Ki | Bioorg Med Chem (2014) 22: 393-397 [PMID:24290063] |
| ChEMBL | Displacement of [3H]ifenprodil from rat brain membrane NR2B receptor | B | 7.96 | pKi | 11 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2765-2770 [PMID:18434149] |
| ChEMBL | Displacement of [3H]ifenprodil from Wistar rat cerebral cortex GluN2B receptor after 120 mins | B | 7.33 | pIC50 | 47 | nM | IC50 | Bioorg Med Chem (2016) 24: 1513-1519 [PMID:26912202] |
| ChEMBL | Displacement of [3H]ifenprodil from NMDA NR2B receptor in Wistar rat cerebral cortex membrane | B | 7.69 | pIC50 | 20.5 | nM | IC50 | Bioorg Med Chem (2009) 17: 1640-1647 [PMID:19157884] |
| ChEMBL | Displacement of [3H]ifenprodil from NMDA receptor GluN2B subunit in Wistar rat cerebral cortex after 120 mins | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2012) 55: 10532-10539 [PMID:23140383] |
| ChEMBL | Displacement of [3H]Ifenprodil from NMDA receptor GluN2B subunit in Wistar rat cerebral cortex | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem (2014) 22: 1040-1048 [PMID:24411196] |
| GluN2C/Glutamate [NMDA] receptor subunit epsilon 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4109] [GtoPdb: 458] [UniProtKB: Q14957] | ||||||||
| ChEMBL | Negative allosteric modulation of human GluN2C receptor expressed in xenopus laevis oocytes assessed as reduction in 3 uM glycine-induced channel current at -40 mV holding potential by two electrode voltage clamp method | B | 4.54 | pIC50 | 29100 | nM | IC50 | J Med Chem (2018) 62: 3-23 [PMID:29446949] |
| GluN2D/Glutamate [NMDA] receptor subunit epsilon 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2591] [GtoPdb: 459] [UniProtKB: O15399] | ||||||||
| ChEMBL | Negative allosteric modulation of human GluN2D receptor expressed in xenopus laevis oocytes assessed as reduction in 3 uM glycine-induced channel current at -40 mV holding potential by two electrode voltage clamp method | B | 4.12 | pIC50 | 75900 | nM | IC50 | J Med Chem (2018) 62: 3-23 [PMID:29446949] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG | B | 7 | pIC50 | 100 | nM | IC50 | Eur J Med Chem (2011) 46: 618-630 [PMID:21185626] |
| H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| ChEMBL | Compound was tested for the binding affinity against histamine H1 receptor by using [3H]mepyramine as radioligand | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (1991) 34: 3085-3090 [PMID:1681106] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Compound was tested for the binding affinity against opioid receptor mu by using [3H]naloxone as radioligand | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1991) 34: 3085-3090 [PMID:1681106] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483] | ||||||||
| ChEMBL |
Compound was tested for the binding affinity against muscarinic acetylcholine receptor by using [3H]QNB as radioligand |
B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1991) 34: 3085-3090 [PMID:1681106] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264] | ||||||||
| ChEMBL | Compound was tested for the binding affinity against 5-hydroxytryptamine 1A receptor by using [3H]DPAT as radioligand | B | 6.62 | pIC50 | 238 | nM | IC50 | J Med Chem (1991) 34: 3085-3090 [PMID:1681106] |
| Serotonin 2a (5-HT2a) receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3446] [UniProtKB: Q75Z89] | ||||||||
| ChEMBL | Compound was tested for the binding affinity against 5-hydroxytryptamine 2 receptor by using [3H]ketanserin as radioligand | B | 6.21 | pIC50 | 610 | nM | IC50 | J Med Chem (1991) 34: 3085-3090 [PMID:1681106] |
| Sigma-1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4153] [UniProtKB: Q60492] | ||||||||
| ChEMBL | Displacement of [3H]-(+)-pentazocine from Sigma1 receptor in guinea pig cortex membranes incubated for 120 mins by scintillation counting method | B | 6.9 | pKi | 125 | nM | Ki | Eur J Med Chem (2020) 190: 112138-112138 [PMID:32070917] |
| ChEMBL | Displacement of [3H](+)-pentazocine from sigma1 receptor guinea pig brain after 180 mins scintillation counting | B | 6.9 | pKi | 125 | nM | Ki | Bioorg Med Chem (2010) 18: 8005-8015 [PMID:20965739] |
| ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membranes incubated for 120 mins by scintillation counting method | B | 6.9 | pKi | 125 | nM | Ki | Bioorg Med Chem (2020) 28: 115245-115245 [PMID:31843460] |
| ChEMBL | Displacement of [3H]-(+)pentazocine from sigma-1 receptor in guinea pig brain membranes after 120 mins by scintillation counting method | B | 6.9 | pKi | 125 | nM | Ki | ACS Med Chem Lett (2020) 11: 651-656 [PMID:32435366] |
| ChEMBL | Displacement of [3H](+)-pentazocine from sigma1 receptor in guinea pig brain membranes after 180 mins by scintillation counting method | B | 6.9 | pKi | 125 | nM | Ki | Bioorg Med Chem (2014) 22: 6638-6646 [PMID:25458498] |
| ChEMBL | Displacement of [3H]-(+)-Pentazocine from sigma 1 receptor in guinea pig brain cortex membranes after 120 mins by scintillation counting analysis | B | 6.9 | pKi | 125 | nM | Ki | Bioorg Med Chem (2018) 26: 501-508 [PMID:29254894] |
| ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain cortex membranes incubated for 120 mins measured for 5 mins by scintillation counting method | B | 6.9 | pKi | 125 | nM | Ki | Eur J Med Chem (2018) 144: 672-681 [PMID:29289890] |
| ChEMBL | Displacement of [3H](+)-Pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis | B | 6.9 | pKi | 125 | nM | Ki | Medchemcomm (2017) 8: 975-981 [PMID:30108812] |
| ChEMBL | Displacement of [3H](+)-pentazocine from S1R in guinea pig brain cortex membranes after 120 mins by scintillation counting assay | B | 6.9 | pKi | 125 | nM | Ki | Eur J Med Chem (2018) 158: 353-370 [PMID:30223122] |
| ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membrane after 120 mins by scintillation counting method | B | 6.9 | pKi | 125 | nM | Ki | Eur J Med Chem (2018) 157: 397-404 [PMID:30103189] |
| ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes incubated for 120 mins by solid scintillation counting method | B | 6.9 | pKi | 125 | nM | Ki | Bioorg Med Chem (2019) 27: 115146-115146 [PMID:31648876] |
| ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes measured after 120 mins by scintillation counting analysis | B | 6.9 | pKi | 125 | nM | Ki | Medchemcomm (2019) 10: 315-325 [PMID:30881618] |
| ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane without cerebellum | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2008) 51: 7523-7531 [PMID:19053780] |
| ChEMBL | Displacement of [3H]-(+)-pentazocine from guinea pig brain sigma1 receptor after 150 mins by scintillation counting analysis | B | 8.99 | pKi | 1.02 | nM | Ki | Bioorg Med Chem (2014) 22: 393-397 [PMID:24290063] |
| σ2/Sigma intracellular receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105864] [GtoPdb: 2553] [UniProtKB: Q5U3Y7] | ||||||||
| ChEMBL | Displacement of [3H]-DTG from sigma 2 receptor in rat liver membranes after 120 mins by scintillation counting analysis | B | 7.01 | pKi | 98 | nM | Ki | Bioorg Med Chem (2018) 26: 501-508 [PMID:29254894] |
| ChEMBL | Displacement of [3H]-di-o-tolylguanidine from sigma-2 receptor in rat liver membranes incubated for 120 mins measured for 5 mins by scintillation counting method | B | 7.01 | pKi | 98 | nM | Ki | Eur J Med Chem (2018) 144: 672-681 [PMID:29289890] |
| ChEMBL | Displacement of [3H]-DTG from S2R in rat liver membranes after 120 mins by scintillation counting assay | B | 7.01 | pKi | 98 | nM | Ki | Eur J Med Chem (2018) 158: 353-370 [PMID:30223122] |
| ChEMBL | Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membranes incubated for 120 mins by scintillation counting method | B | 7.01 | pKi | 98 | nM | Ki | Eur J Med Chem (2018) 157: 397-404 [PMID:30103189] |
| ChEMBL | Displacement of [3H]di-o-tolylguanidine from sigma2 receptor in rat liver membranes measured after 120 mins by solid scintillation counting method | B | 7.01 | pKi | 98 | nM | Ki | Bioorg Med Chem (2019) 27: 115146-115146 [PMID:31648876] |
| ChEMBL | Displacement of [3H]di-o-tolylguanidine from sigma2 receptor in rat liver membranes measured after 120 mins by scintillation counting analysis | B | 7.01 | pKi | 98 | nM | Ki | Medchemcomm (2019) 10: 315-325 [PMID:30881618] |
| ChEMBL | Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membranes incubated for 120 mins in the presence of sigma1 receptor ligand (+)-pentazocine by scintillation counting method | B | 7.01 | pKi | 98 | nM | Ki | Bioorg Med Chem (2020) 28: 115245-115245 [PMID:31843460] |
| ChEMBL | Displacement of [3H]-Di-o-tolylguanidine from sigma-2 receptor in rat liver membranes after 120 mins by scintillation counting method | B | 7.01 | pKi | 98 | nM | Ki | ACS Med Chem Lett (2020) 11: 651-656 [PMID:32435366] |
| ChEMBL | Displacement of [3H]DTG from sigma 2 receptor in rat liver membranes incubated for 120 mins by scintillation counting method | B | 7.01 | pKi | 98 | nM | Ki | Eur J Med Chem (2020) 190: 112138-112138 [PMID:32070917] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | Compound was tested for the binding affinity against sigma receptor by using [3H]-+3PPP as radioligand | B | 8.41 | pIC50 | 3.9 | nM | IC50 | J Med Chem (1991) 34: 3085-3090 [PMID:1681106] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9] | ||||||||
| ChEMBL | Inhibition of [3H]- ifenprodil binding against Sigma opioid receptor type 2 from rat brain | B | 8.31 | pKi | 4.9 | nM | Ki | J Med Chem (1999) 42: 5181-5187 [PMID:10602703] |
| ChEMBL | Displacement of [3H](+)-pentazocine from sigma1 receptor in rat liver membrane by liquid scintillation counting | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2009) 52: 5380-5393 [PMID:19673530] |
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]
