endomorphin-2 [Ligand Id: 3668] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL333357 (Endomorphin 2)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
  • δ receptor/Delta opioid receptor in Mouse [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
  • δ receptor/Delta opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
1 CHEMBL333357_lig_chart_1 Delta opioid receptor HumanMouseRat
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
  • κ receptor/Kappa opioid receptor in Rat [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975]
  • Kappa opioid receptor in Guinea pig [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
2 CHEMBL333357_lig_chart_2 Kappa opioid receptor HumanRatGuinea pig
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
  • μ receptor/Mu opioid receptor in Mouse [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866]
  • μ receptor/Mu opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
  • Mu opioid receptor in Guinea pig [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
3 CHEMBL333357_lig_chart_3 Mu opioid receptor HumanMouseRatGuinea pig
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  • Mu-opioid receptor in Guinea pig [ChEMBL: CHEMBL5430] [UniProtKB: Q8CGM4]
  • This target only has 0 pki data point
4 CHEMBL333357_lig_chart_4 Mu-opioid receptor Guinea pig
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  • NK1 receptor/Neurokinin 1 receptor in Rat [ChEMBL: CHEMBL4027] [GtoPdb: 360] [UniProtKB: P14600]
5 CHEMBL333357_lig_chart_5 Neurokinin 1 receptor Rat
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  • Uncharacterized protein in Bovine [ChEMBL: CHEMBL2169734] [UniProtKB: F1N083]
  • This target only has 1 pki data point
6 CHEMBL333357_lig_chart_6 Uncharacterized protein Bovine
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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]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][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][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 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 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 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]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]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 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 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 B 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 B 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 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]
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]
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]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 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 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]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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]