endomorphin-2 [Ligand Id: 3668] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL333357 (Endomorphin 2) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| ChEMBL | Displacement of [3H]deltrophin-2 from human recombinant DOR expressed in CHO cell membranes incubated for 2 hrs by liquid scintillation counting method | B | 5.1 | pKi | 7899 | nM | Ki | Eur J Med Chem (2019) 179: 527-536 [PMID:31276897] |
| ChEMBL | Displacement of [3H]DPDPE from Myc-tagged delta opioid receptor expressed in HEK293 cells after 60 mins by liquid scintillation counter | B | 5.19 | pKi | 6420 | nM | Ki | J Med Chem (2012) 55: 6224-6236 [PMID:22724433] |
| ChEMBL | Binding affinity to delta opioid receptor (unknown origin) | B | 5.22 | pKi | 6085 | nM | Ki | Bioorg Med Chem (2014) 22: 2208-2219 [PMID:24613457] |
| ChEMBL | Displacement of [3H]DPDPE from delta opioid receptor (unknown origin) expressed in CHO cells after 90 mins by liquid scintillation counting | B | 5.47 | pKi | 3385 | nM | Ki | ACS Med Chem Lett (2013) 4: 795-799 [PMID:24900748] |
| ChEMBL | Activity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay | F | 6 | pEC50 | >1000 | nM | EC50 | J Med Chem (2007) 50: 512-520 [PMID:17266203] |
| ChEMBL | Antagonist activity at delta opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assay | F | 6 | pEC50 | >1000 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 1350-1353 [PMID:18207400] |
| δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300] | ||||||||
| ChEMBL | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | F | 6.29 | pIC50 | 510 | nM | IC50 | Eur J Med Chem (2010) 45: 4594-4600 [PMID:20692738] |
| ChEMBL | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically evoked contraction | F | 6.29 | pIC50 | 510 | nM | IC50 | J Med Chem (2010) 53: 4550-4554 [PMID:20476738] |
| ChEMBL | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically evoked muscle contractions | F | 6.46 | pIC50 | 344 | nM | IC50 | Bioorg Med Chem (2007) 15: 1237-1251 [PMID:17142049] |
| ChEMBL | In vitro inhibition of opioid receptor delta using mouse vas deferens | B | 6.46 | pIC50 | 344 | nM | IC50 | J Med Chem (2005) 48: 586-592 [PMID:15658871] |
| ChEMBL | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | F | 6.46 | pIC50 | 344 | nM | IC50 | J Med Chem (2007) 50: 2753-2766 [PMID:17497839] |
| ChEMBL | In vitro inhibitory concentration against Opioid receptor delta 1 was measured using mouse vas deferens assay | B | 7.32 | pIC50 | 48.2 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1847-1850 [PMID:15780619] |
| ChEMBL | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated contraction | F | 7.59 | pIC50 | 25.8 | nM | IC50 | Bioorg Med Chem (2008) 16: 6415-6422 [PMID:18490168] |
| ChEMBL | Agonist activity at delta opioid receptor in Kunming mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | F | 7.67 | pIC50 | 21.6 | nM | IC50 | J Med Chem (2012) 55: 6224-6236 [PMID:22724433] |
| ChEMBL | Agonist activity at delta opioid receptor by inhibition of electrically evoked muscle contraction in isolated mouse vas deferens | F | 7.82 | pIC50 | 15.3 | nM | IC50 | J Med Chem (2007) 50: 512-520 [PMID:17266203] |
| δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
| ChEMBL | Displacement of [3H]Ile5,6deltorphin-2 from delta opioid receptor in Wistar rat brain membranes by liquid scintillation counting | B | 5 | pKi | >10000 | nM | Ki | Eur J Med Chem (2013) 68: 167-177 [PMID:23974016] |
| ChEMBL | Displacement of [3H]-DPDPE from Wistar rat delta opioid receptor incubated for 3 hrs by liquid scintillation counting method | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2020) 28: 115438-115438 [PMID:32199689] |
| ChEMBL | Displacement of [3H][Ile5,6]deltorphin-2 from DOR in Wistar rat brain homogenates by liquid scintillation counting analysis | B | 5.02 | pKi | 9614.7 | nM | Ki | Eur J Med Chem (2016) 109: 276-286 [PMID:26785295] |
| ChEMBL | Binding affinity against rat brain opioid receptor delta 1 using [3H]DPDPE radioligand | B | 5.03 | pKi | 9230 | nM | Ki | J Med Chem (2004) 47: 3591-3599 [PMID:15214786] |
| ChEMBL | Inhibition of [3H]DPDPE binding to delta-Opioid receptor | B | 5.03 | pKi | 9230 | nM | Ki | J Med Chem (2005) 48: 586-592 [PMID:15658871] |
| ChEMBL | Displacement of [3H][Ile5,6]deltorphin2 from delta opioid receptor in rat brain membrane homogenate by liquid scintillation counting | B | 5.06 | pKi | 8771 | nM | Ki | J Med Chem (2011) 54: 1462-1472 [PMID:21287991] |
| ChEMBL | Displacement of [3H]DPDPE from DOR in Wistar rat brain membranes measured after 3 hrs by scintillation counting method | B | 5.06 | pKi | 8770 | nM | Ki | J Med Chem (2021) 64: 16801-16819 [PMID:34781680] |
| ChEMBL | Displacement of [3H][Ile5,6]deltorphin 2 from delta opioid receptor in Wistar rat brain membranes | B | 5.07 | pKi | 8495 | nM | Ki | J Med Chem (2012) 55: 8418-8428 [PMID:22957923] |
| ChEMBL | Displacement of [3H]DPDPE from delta opioid receptor in rat brain membrane | B | 5.08 | pKi | 8360 | nM | Ki | Bioorg Med Chem (2008) 16: 6415-6422 [PMID:18490168] |
| ChEMBL | Displacement of [3H]DPDPE from delta opioid receptor in Wistar rat brain | B | 5.08 | pKi | 8360 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 3688-3692 [PMID:16682191] |
| ChEMBL | Displacement of [3H]DPDPE from rat cortex delta opioid receptor after 2.5 hrs by liquid scintillation counting analysis | B | 5.17 | pKi | 6804 | nM | Ki | Eur J Med Chem (2015) 92: 270-281 [PMID:25559207] |
| ChEMBL | Displacement of [3H]deltorphin 2 from delta opioid receptor in Sprague-Dawley rat brain P2 synaptosome membrane | B | 5.22 | pKi | 6085 | nM | Ki | J Med Chem (2007) 50: 2753-2766 [PMID:17497839] |
| ChEMBL | Displacement of [3H]deltorphin 2 from delta opioid receptor in rat brain P2 synaptosome | B | 5.22 | pKi | 6080 | nM | Ki | Bioorg Med Chem (2007) 15: 1237-1251 [PMID:17142049] |
| ChEMBL | Displacement of [3H]Ile5,6deltorphin-2 from delta opioid receptor in Wistar rat brain | B | 5.25 | pKi | 5652 | nM | Ki | J Med Chem (2008) 51: 4270-4279 [PMID:18572932] |
| ChEMBL | Binding affinity towards delta receptor in rat brain using [3H]DSLET | B | 5.4 | pKi | 3940 | nM | Ki | J Med Chem (2001) 44: 3896-3903 [PMID:11689075] |
| ChEMBL | Displacement of [3H]Ile5,6-deltorphin II from opioid receptor delta 1 of rat brain membranes | B | 5.58 | pKi | 2650 | nM | Ki | J Med Chem (2004) 47: 735-743 [PMID:14736254] |
| ChEMBL | Inhibition of [3H]naloxone binding to rat brain homogenate Opioid receptor delta | B | 5.64 | pKi | 2300 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 2467-2469 [PMID:15863298] |
| ChEMBL | Displacement of [3H]deltorphin2 from delta opioid receptor in rat brain membrane | B | 4.99 | pIC50 | 10300 | nM | IC50 | Bioorg Med Chem (2007) 15: 3883-3888 [PMID:17395470] |
| ChEMBL | Displacement of [3H]naltrindole from delta opioid receptor in rat brain membranes | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1350-1353 [PMID:18207400] |
| ChEMBL | Displacement of [3H][Ile5,6]deltorphin-2 from delta opioid receptor in Wistar rat brain membrane | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2009) 17: 3789-3794 [PMID:19435668] |
| ChEMBL | Displacement of [3H][Ile5,6]deltorphin 2 from delta opioid receptor in Wistar rat brain membrane by liquid scintillation counting | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2011) 19: 6977-6981 [PMID:22047797] |
| ChEMBL | Displacement of [3H][Ile5,6]deltorphin-2 from DOR in Wistar rat brain membranes by liquid scintillation counting method | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2014) 22: 6545-6551 [PMID:25456075] |
| ChEMBL | Displacement of [3H](Ile5,6)deltorphin-2 from DOR in rat brain membranes | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2014) 22: 4803-4809 [PMID:25047937] |
| ChEMBL | Displacement of [3H][Ile5,6]deltorphin-2 from delta opioid receptor in Wistar rat brain membranes after 120 mins by scintillation counting analysis | B | 6 | pIC50 | >1000 | nM | IC50 | ACS Med Chem Lett (2015) 6: 579-583 [PMID:26005537] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | Displacement of [3H]U-69593 from human recombinant KOR expressed in CHO cell membranes incubated for 2 hrs by liquid scintillation counting method | B | 5.94 | pKi | 1136 | nM | Ki | Eur J Med Chem (2019) 179: 527-536 [PMID:31276897] |
| ChEMBL | Displacement of [3H]U69593 from human kappa opioid receptor expressed in CHO cells after 60 mins by liquid scintillation counter | B | 6.3 | pKi | >500 | nM | Ki | J Med Chem (2012) 55: 8477-8482 [PMID:22966938] |
| κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975] | ||||||||
| ChEMBL | Displacement of[3H]-U69,593 from Wistar rat kappa opioid receptor incubated for 1.5 hrs by liquid scintillation counting method | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2020) 28: 115438-115438 [PMID:32199689] |
| ChEMBL | Displacement of [3H]-U69593 from KOR in Wistar rat brain membranes measured after 1 hr by scintillation counting method | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2021) 64: 16801-16819 [PMID:34781680] |
| ChEMBL | Displacement of [3H]dynorphin A from Opioid receptor kappa 1 of rat brain membranes (DAMGO/DADLE quenching of mu/delta receptor binding) | B | 7.97 | pKi | 10.6 | nM | Ki | J Med Chem (2004) 47: 735-743 [PMID:14736254] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Displacement of [3H]nor-BNI from KOR in Dunkin Hartley guinea pig brain homogenates by liquid scintillation counting analysis | B | 5.11 | pKi | 7827.67 | nM | Ki | Eur J Med Chem (2016) 109: 276-286 [PMID:26785295] |
| ChEMBL | Displacement of [3H]U-69593 from kappa opioid receptor in Hartley guinea pig cerebellum P2 synaptosome membrane | B | 5.4 | pKi | >4000 | nM | Ki | J Med Chem (2007) 50: 2753-2766 [PMID:17497839] |
| ChEMBL | Displacement of [3H]U69,593 from guinea pig cortex/cerebella kappa opioid receptor after 2 hrs by liquid scintillation counting analysis | B | 5.57 | pKi | 2708 | nM | Ki | Eur J Med Chem (2015) 92: 270-281 [PMID:25559207] |
| ChEMBL | Displacement of [3H]nor-BNI from KOR in Dunkin Hartley guinea pig membranes by liquid scintillation counting method | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2014) 22: 6545-6551 [PMID:25456075] |
| ChEMBL | Displacement of [3H]nor-BNI from KOR in guinea pig brain membranes | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2014) 22: 4803-4809 [PMID:25047937] |
| ChEMBL | Displacement of [3H]nor-BNI from kappa opioid receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis | B | 6 | pIC50 | >1000 | nM | IC50 | ACS Med Chem Lett (2015) 6: 579-583 [PMID:26005537] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Binding affinity to human mu opioid receptor | B | 8.08 | pKi | 8.23 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 5387-5391 [PMID:19679474] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor (unknown origin) expressed in CHO cells after 90 mins by liquid scintillation counting | B | 8.28 | pKi | 5.3 | nM | Ki | ACS Med Chem Lett (2013) 4: 795-799 [PMID:24900748] |
| ChEMBL | Displacement of [3H]DAMGO from FLAG-tagged mu opioid receptor expressed in HEK293 cells after 60 mins by liquid scintillation counter | B | 8.49 | pKi | 3.2 | nM | Ki | J Med Chem (2012) 55: 6224-6236 [PMID:22724433] |
| ChEMBL | Displacement of [3H]DAMGO from human recombinant MOR expressed in CHO cell membranes incubated for 2 hrs by liquid scintillation counting method | B | 8.53 | pKi | 2.95 | nM | Ki | Eur J Med Chem (2019) 179: 527-536 [PMID:31276897] |
| ChEMBL | Binding affinity to mu opioid receptor (unknown origin) | B | 8.88 | pKi | 1.33 | nM | Ki | Bioorg Med Chem (2014) 22: 2208-2219 [PMID:24613457] |
| ChEMBL | Binding affinity to mu opioid receptor | B | 9.16 | pKi | 0.69 | nM | Ki | J Med Chem (2006) 49: 3990-3993 [PMID:16789756] |
| ChEMBL | Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins | F | 7.2 | pEC50 | 63.1 | nM | EC50 | Bioorg Med Chem (2019) 27: 630-643 [PMID:30626554] |
| ChEMBL | Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method | F | 7.26 | pEC50 | 55.5 | nM | EC50 | Bioorg Med Chem (2020) 28: 115438-115438 [PMID:32199689] |
| ChEMBL | Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins | F | 7.3 | pEC50 | 50 | nM | EC50 | Bioorg Med Chem (2019) 27: 630-643 [PMID:30626554] |
| ChEMBL | Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISA | F | 7.8 | pEC50 | 15.7 | nM | EC50 | J Med Chem (2021) 64: 16801-16819 [PMID:34781680] |
| ChEMBL | Agonist activity at human recombinant mu opioid receptor expressed in CHO cells co-expressing C-terminally modified GGalphaqi5 assessed as stimulation of calcium release by Fluo-4 AM dye-based fluorescence assay | F | 7.86 | pEC50 | 13.8 | nM | EC50 | ACS Med Chem Lett (2015) 6: 579-583 [PMID:26005537] |
| ChEMBL | Agonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis | F | 7.88 | pEC50 | 13.18 | nM | EC50 | Eur J Med Chem (2016) 109: 276-286 [PMID:26785295] |
| ChEMBL | Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter | F | 7.93 | pEC50 | 11.8 | nM | EC50 | J Med Chem (2012) 55: 6224-6236 [PMID:22724433] |
| ChEMBL | Agonist activity at human recombinant MOR expressed in CHO cells co-expressing C-terminally modified Galphaqi5 assessed as induction of calcium mobilization by Fluo-4AM dye-based fluorescence assay | F | 8.24 | pEC50 | 5.75 | nM | EC50 | Eur J Med Chem (2019) 179: 527-536 [PMID:31276897] |
| ChEMBL | Antagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assay | F | 10.4 | pEC50 | 0.04 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 1350-1353 [PMID:18207400] |
| ChEMBL | Activity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay | F | 10.4 | pEC50 | 0.04 | nM | EC50 | J Med Chem (2007) 50: 512-520 [PMID:17266203] |
| μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866] | ||||||||
| ChEMBL | Inhibition of Mu opioid receptor of mouse vas deferens | B | 7.62 | pIC50 | 24.1 | nM | IC50 | J Med Chem (2004) 47: 735-743 [PMID:14736254] |
| ChEMBL | Agonist activity at mu opioid receptor in NMRI mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | F | 7.77 | pIC50 | 16.79 | nM | IC50 | J Med Chem (2008) 51: 173-177 [PMID:18062664] |
| μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | Displacement of [3H]-DAMGO from Wistar rat mu opioid receptor incubated for 1 hr by liquid scintillation counting method | B | 7.72 | pKi | 19.2 | nM | Ki | Bioorg Med Chem (2020) 28: 115438-115438 [PMID:32199689] |
| ChEMBL | Displacement of [3H]nalocone from mu opioid receptor in rat brain membranes | B | 8.02 | pKi | 9.6 | nM | Ki | J Med Chem (2010) 53: 4550-4554 [PMID:20476738] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane by liquid scintillation counting | B | 8.02 | pKi | 9.56 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 4115-4118 [PMID:19560919] |
| ChEMBL | Displacement of [3H]DAMGO from Opioid receptor mu 1 of rat brain membranes | B | 8.02 | pKi | 9.53 | nM | Ki | J Med Chem (2004) 47: 735-743 [PMID:14736254] |
| ChEMBL | Inhibition of DAMGO (Tyr-[D-Ala]-Gly-[NMe-Phe]-Gly-ol) binding to rat brain mu opioid receptor | B | 8.02 | pKi | 9.53 | nM | Ki | J Med Chem (2005) 48: 3239-3250 [PMID:15857130] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane | B | 8.08 | pKi | 8.23 | nM | Ki | Bioorg Med Chem (2008) 16: 6415-6422 [PMID:18490168] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain | B | 8.08 | pKi | 8.23 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 3688-3692 [PMID:16682191] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane after 3 hrs by liquid scintillation counting | B | 8.08 | pKi | 8.23 | nM | Ki | Eur J Med Chem (2010) 45: 4594-4600 [PMID:20692738] |
| ChEMBL | Displacement of [3H]DAMGO from MOR in Wistar rat brain membranes measured after 1 hr by scintillation counting method | B | 8.21 | pKi | 6.12 | nM | Ki | J Med Chem (2021) 64: 16801-16819 [PMID:34781680] |
| ChEMBL | Displacement of [3H]endomorphin-2 from Opioid receptor mu 1 of rat brain membranes | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2004) 47: 735-743 [PMID:14736254] |
| ChEMBL | Inhibition of [3H]naloxone binding to rat brain homogenate Opioid receptor mu | B | 8.43 | pKi | 3.7 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 2467-2469 [PMID:15863298] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membranes by liquid scintillation counting | B | 8.45 | pKi | 3.56 | nM | Ki | Eur J Med Chem (2013) 68: 167-177 [PMID:23974016] |
| GtoPdb | - | - | 8.5 | pKi | 3.24 | nM | Ki | Nature (1997) 386: 499-502 [PMID:9087409] |
| ChEMBL | Displacement of [3H]DAMGO from rat cortex mu opioid receptor after 30 mins by liquid scintillation counting analysis | B | 8.52 | pKi | 3 | nM | Ki | Eur J Med Chem (2015) 92: 270-281 [PMID:25559207] |
| ChEMBL | Binding affinity towards mu receptor in rat brain using [3H]DAMGO | B | 8.69 | pKi | 2.06 | nM | Ki | J Med Chem (2001) 44: 3896-3903 [PMID:11689075] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membranes | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2012) 55: 8418-8428 [PMID:22957923] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane homogenate by liquid scintillation counting | B | 8.87 | pKi | 1.35 | nM | Ki | J Med Chem (2011) 54: 1462-1472 [PMID:21287991] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat brain P2 synaptosome | B | 8.88 | pKi | 1.33 | nM | Ki | Bioorg Med Chem (2007) 15: 1237-1251 [PMID:17142049] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in Sprague-Dawley rat brain P2 synaptosome membrane | B | 8.88 | pKi | 1.33 | nM | Ki | J Med Chem (2007) 50: 2753-2766 [PMID:17497839] |
| ChEMBL | Displacement of [3H]endomorphin-2 from mu opioid receptor in Wistar rat brain | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2008) 51: 4270-4279 [PMID:18572932] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2008) 51: 4270-4279 [PMID:18572932] |
| ChEMBL | Inhibition of [3H]DAMGO binding to mu-Opioid receptor | B | 9.16 | pKi | 0.69 | nM | Ki | J Med Chem (2005) 48: 586-592 [PMID:15658871] |
| ChEMBL | Binding affinity against rat brain Opioid receptor mu 1 using [3H]DAMGO radioligand | B | 9.16 | pKi | 0.69 | nM | Ki | J Med Chem (2004) 47: 3591-3599 [PMID:15214786] |
| ChEMBL | Displacement of [3H]DAMGO from MOR in Wistar rat brain homogenates by liquid scintillation counting analysis | B | 9.31 | pKi | 0.49 | nM | Ki | Eur J Med Chem (2016) 109: 276-286 [PMID:26785295] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membranes by liquid scintillation counting | B | 8.33 | pIC50 | 8.33 | - | logIC50 | Eur J Med Chem (2013) 68: 167-177 [PMID:23974016] |
| ChEMBL | Displacement of [3H]DAGO from mu opioid receptor in rat brain membrane | B | 8.46 | pIC50 | 3.46 | nM | IC50 | Bioorg Med Chem (2007) 15: 3883-3888 [PMID:17395470] |
| ChEMBL | Displacement of [3H]DAMGO from Wistar rat mu opioid receptor by liquid scintillation counting | B | 9 | pIC50 | 0.99 | nM | IC50 | Bioorg Med Chem (2011) 19: 6977-6981 [PMID:22047797] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membranes | B | 9.1 | pIC50 | 0.79 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1350-1353 [PMID:18207400] |
| ChEMBL | Displacement of [3H]DAMGO from MOR in Wistar rat brain membranes by liquid scintillation counting method | B | 9.1 | pIC50 | 0.79 | nM | IC50 | Bioorg Med Chem (2014) 22: 6545-6551 [PMID:25456075] |
| ChEMBL | Displacement of [3H]DAMGO from MOR in rat brain membranes | B | 9.1 | pIC50 | 0.79 | nM | IC50 | Bioorg Med Chem (2014) 22: 4803-4809 [PMID:25047937] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membranes after 120 mins by scintillation counting analysis | B | 9.1 | pIC50 | 0.79 | nM | IC50 | ACS Med Chem Lett (2015) 6: 579-583 [PMID:26005537] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membrane | B | 9.16 | pIC50 | 0.69 | nM | IC50 | Bioorg Med Chem (2009) 17: 3789-3794 [PMID:19435668] |
| ChEMBL | Agonist activity at mu opioid receptor in Wistar rat brain membranes after 60 mins by [35S]GTPgammaS binding assay | F | 6.42 | pEC50 | 383 | nM | EC50 | J Med Chem (2012) 55: 8418-8428 [PMID:22957923] |
| ChEMBL | Agonist activity at mu opioid receptor in rat brain membrane by [35S]GTPgammaS binding assay | F | 6.67 | pEC50 | 212 | nM | EC50 | J Med Chem (2011) 54: 1462-1472 [PMID:21287991] |
| ChEMBL | Activity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS binding | F | 7.11 | pEC50 | 78 | nM | EC50 | J Med Chem (2008) 51: 4270-4279 [PMID:18572932] |
| Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
| ChEMBL | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated contraction | F | 4.82 | pIC50 | 15000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4115-4118 [PMID:19560919] |
| ChEMBL | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction | F | 7.82 | pIC50 | 15 | nM | IC50 | Eur J Med Chem (2010) 45: 4594-4600 [PMID:20692738] |
| ChEMBL | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction | F | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2010) 53: 4550-4554 [PMID:20476738] |
| ChEMBL | In vitro inhibitory concentration against Opioid receptor mu 1 was measured using guinea pig ileum assay | B | 7.83 | pIC50 | 14.7 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1847-1850 [PMID:15780619] |
| ChEMBL | Agonist activity at mu opioid receptor assessed as inhibition of electrically-evoked contraction of guinea pig ileum | F | 7.86 | pIC50 | 13.7 | nM | IC50 | J Med Chem (2006) 49: 5610-5617 [PMID:16942034] |
| ChEMBL | Agonist activity at mu opioid receptor by guinea pig ileum assay | F | 7.86 | pIC50 | 13.7 | nM | IC50 | J Med Chem (2006) 49: 3990-3993 [PMID:16789756] |
| ChEMBL | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction | F | 8.03 | pIC50 | 9.33 | nM | IC50 | J Med Chem (2012) 55: 6224-6236 [PMID:22724433] |
| ChEMBL | Inhibition of Opioid receptor mu 1 of guinea pig ileum | B | 8.04 | pIC50 | 9.22 | nM | IC50 | J Med Chem (2004) 47: 735-743 [PMID:14736254] |
| ChEMBL | In vitro inhibition of opioid receptor mu using isolated guinea pig ileum | B | 8.1 | pIC50 | 7.96 | nM | IC50 | J Med Chem (2005) 48: 586-592 [PMID:15658871] |
| ChEMBL | Agonist activity at mu opioid receptor by inhibition of electrically evoked muscle contraction in guinea pig ileum | F | 8.11 | pIC50 | 7.71 | nM | IC50 | J Med Chem (2007) 50: 512-520 [PMID:17266203] |
| ChEMBL | Agonist activity at mu opioid receptor in Hartley guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction | F | 8.16 | pIC50 | 6.9 | nM | IC50 | J Med Chem (2007) 50: 2753-2766 [PMID:17497839] |
| ChEMBL | Agonist activity at mu opioid receptor in Hartley guinea pig intestine assessed as inhibition of electrically evoked myenteric plexus longitudinal muscle contractions | F | 8.16 | pIC50 | 6.88 | nM | IC50 | Bioorg Med Chem (2007) 15: 1237-1251 [PMID:17142049] |
| ChEMBL | Agonist activity at mu opioid receptor in guinea pig ileum | B | 8.33 | pIC50 | 4.7 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 6673-6676 [PMID:24220171] |
| Mu-opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5430] [UniProtKB: Q8CGM4] | ||||||||
| ChEMBL | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated contraction | F | 8.01 | pIC50 | 9.67 | nM | IC50 | Bioorg Med Chem (2008) 16: 6415-6422 [PMID:18490168] |
| NK1 receptor/Neurokinin 1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4027] [GtoPdb: 360] [UniProtKB: P14600] | ||||||||
| ChEMBL | Displacement of [3H]SP1-7 from NK1 receptor in Sprague-Dawley rat spinal cord membrane | B | 8.06 | pKi | 8.7 | nM | Ki | J Med Chem (2010) 53: 2383-2389 [PMID:20178322] |
| ChEMBL | Displacement of [3H]SP1-7 from NK1 receptor in Sprague-Dawley rat spinal cord membranes after 60 mins by scintillation counting method | B | 8.06 | pKi | 8.7 | nM | Ki | Bioorg Med Chem Lett (2018) 28: 2446-2450 [PMID:29929882] |
| Uncharacterized protein in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2169734] [UniProtKB: F1N083] | ||||||||
| ChEMBL | Displacement of [3H]DPDPE from delta opioid receptor in calf frontal cortex after 1 hr by gamma counter | B | 6.3 | pKi | >500 | nM | Ki | J Med Chem (2012) 55: 8477-8482 [PMID:22966938] |
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]
