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 | Displacement of [3H] ifenprodil from Wistar rat glutamate NMDA receptor incubated for 2 hrs by scintillation counting method | B | 6.84 | pKi | 143.2 | nM | Ki | Eur J Med Chem (2022) 227: 113876-113876 [PMID:34710748] |
| 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 recombinant human GluN2B NMDA receptor (unknown origin) expressed in dexamethasone-induced mouse L-M(TK-) cell after 120 mins by microbeta scintillation counting method | B | 8 | pKi | 10.07 | nM | Ki | J Med Chem (2022) 65: 12292-12318 [PMID:36084304] |
| 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 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 (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 | 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 | 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 brain membrane measured after 120 mins by scintillation counting method | B | 6.9 | pKi | 125 | nM | Ki | J Med Chem (2022) 65: 12292-12318 [PMID:36084304] |
| 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 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 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 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 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 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] |
| ChEMBL | Displacement of [3H]DTG from sigma 2 receptor in rat liver membranes measured after 120 mins by scintillation counting method | B | 7.01 | pKi | 98 | nM | Ki | J Med Chem (2022) 65: 12292-12318 [PMID:36084304] |
| 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 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]
