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]-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]Ile5,6deltorphin-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][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 | Displacement of [3H]-[Ile5,6]-deltorphin-2 from Wistar rat brain membrane DOP | B | 5.03 | pKi | 9233 | nM | Ki | J Med Chem (2022) 65: 1612-1661 [PMID:34995453] |
| 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 | Binding affinity to KOP (unknown origin) | B | 5.28 | pKi | 5240 | nM | Ki | J Med Chem (2022) 65: 1612-1661 [PMID:34995453] |
| 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 human MOP assessed as forskolin stimulated cAMP accumulation | F | 7.92 | pEC50 | 12 | nM | EC50 | J Med Chem (2022) 65: 1612-1661 [PMID:34995453] |
| 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 | Agonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assay | F | 8.81 | pEC50 | 1.55 | nM | EC50 | J Med Chem (2022) 65: 1612-1661 [PMID:34995453] |
| 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 | 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 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 | 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 Wistar rat brain membrane MOP | B | 9.16 | pKi | 0.69 | nM | Ki | J Med Chem (2022) 65: 1612-1661 [PMID:34995453] |
| 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 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]
