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ChEMBL ligand: CHEMBL38874 (DAMGO) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
ChEMBL | Binding affinity to adenosine receptor A1 | B | 4 | pKi | >100000 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6736-6739 [PMID:19836950] |
CCK2 receptor/Cholecystokinin B receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL298] [GtoPdb: 77] [UniProtKB: P32239] | ||||||||
ChEMBL | Displacement of [3H]DAMGO from CCK2R-MOPR coexpressed in CHO cells | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2009) 52: 247-258 [PMID:19113864] |
ChEMBL | Activity at CCK2R-MOPR coexpressed in CHO cells co-transfected with delta-6-Galphaqi4-myr assessed as intracellular calcium release by FLIPR | F | 8.58 | pEC50 | 2.66 | nM | EC50 | J Med Chem (2009) 52: 247-258 [PMID:19113864] |
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
ChEMBL | Binding affinity against Delta opioid receptor in using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 20 nM NTI | F | 5.73 | pKd | 1850 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3053-3056 [PMID:10571174] |
ChEMBL | Binding affinity against Delta opioid receptor in using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 20 nM NTI | F | 5.73 | pKd | 1850 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3347-3350 [PMID:10612597] |
ChEMBL | In vitro potency was measured against human Opioid receptor delta 1 | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1998) 41: 2631-2635 [PMID:9651168] |
ChEMBL | Inhibition of [3H]naltrindole binding to human Opioid receptor delta 1 | B | 5.7 | pKi | >2000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5045-5050 [PMID:15380196] |
ChEMBL | Displacement of [3H]-DADLE from human delta opioid receptor expressed in CHO cells membrane after 2 hrs by liquid scintillation counting | B | 5.82 | pKi | 1500 | nM | Ki | Eur J Med Chem (2012) 50: 44-54 [PMID:22341895] |
ChEMBL | Displacement of [3H]DADLE from human recombinant opioid delta receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method | B | 5.82 | pKi | 1500 | nM | Ki | Eur J Med Chem (2015) 92: 531-539 [PMID:25599950] |
ChEMBL | Displacement of [3H]DADLE from human delta opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting | B | 5.82 | pKi | 1500 | nM | Ki | Eur J Med Chem (2013) 67: 335-343 [PMID:23880358] |
ChEMBL | Displacement of [3H]DADLE from human recombinant delta opioid receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting analysis | B | 5.82 | pKi | 1500 | nM | Ki | Bioorg Med Chem (2013) 21: 3298-3309 [PMID:23618710] |
ChEMBL | Displacement of [3H]-naltrindole from human delta opioid receptor expressed in CHO cells after 3 hrs by scintillation counting analysis | B | 6 | pKi | 990 | nM | Ki | J Med Chem (2015) 58: 5728-5741 [PMID:26125201] |
ChEMBL | Binding affinity against Opioid receptor delta 1 | B | 6.25 | pKi | 567 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2681-2684 [PMID:9873602] |
ChEMBL | Displacement of [3H]Cl-DPDPE from human DOP receptor expressed in CHO cells after 60 mins by scintillation counting | B | 6.52 | pKi | 300 | nM | Ki | J Med Chem (2011) 54: 6531-6537 [PMID:21866885] |
ChEMBL | Displacement of [3H]C1-DPDPE from human recombinant Opioid receptor delta 1 on CHO cell membranes. | B | 6.52 | pKi | 300 | nM | Ki | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
ChEMBL | Binding affinity for delta opioid receptor | B | 6.54 | pKi | 290 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 1585-1589 [PMID:12699761] |
ChEMBL | Displacement of radiolabeled DPDPE-Cl from delta opioid receptor in Hartley guinea pig brain | B | 6.9 | pKi | 127 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416] |
ChEMBL | Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 cells | B | 9.18 | pKi | 0.66 | nM | Ki | Bioorg Med Chem (2009) 17: 7337-7343 [PMID:19762245] |
ChEMBL | Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 cells | B | 8.84 | pIC50 | 1.45 | nM | IC50 | Bioorg Med Chem (2009) 17: 7337-7343 [PMID:19762245] |
ChEMBL | Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells. | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
ChEMBL | Agonist activity at human DOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | F | 6.4 | pEC50 | 400 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4870-4874 [PMID:23880538] |
ChEMBL | Partial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting | F | 8.16 | pEC50 | 6.86 | nM | EC50 | J Med Chem (2011) 54: 6531-6537 [PMID:21866885] |
δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300] | ||||||||
ChEMBL | Displacement of [125I]-Deltorphin 2 from mouse Flag-tagged delta-opioid receptor expressed in HEK293 cell membranes after 60 mins by gamma counting | B | 5.81 | pIC50 | 1533 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2320-2323 [PMID:29853330] |
ChEMBL | Agonist activity at delta-opioid receptor in mouse vasa deferens assessed as inhibition of electrically induced contractions | F | 6.02 | pIC50 | 950 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2320-2323 [PMID:29853330] |
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 Sprague-Dawley rat delta opioid receptor by liquid scintillation counting | B | 5.57 | pKi | 2670 | nM | Ki | Bioorg Med Chem (2010) 18: 4975-4982 [PMID:20599386] |
ChEMBL | Binding affinity against Opioid receptor delta 1 by displacement of radioligand [3H]DSLET in rat brain membrane | B | 5.89 | pKi | 1280 | nM | Ki | J Med Chem (1989) 32: 698-703 [PMID:2537427] |
ChEMBL | Ability to inhibit the binding of [3H]DSLET to Opioid receptor delta 1 in rat brain membranes | B | 6.15 | pKi | 700 | nM | Ki | J Med Chem (1988) 31: 374-383 [PMID:2828622] |
ChEMBL | Binding affinity to opioid receptor delta was determined in rat brain using [3H]DSTBULET as radioligand | B | 6.2 | pKi | 629 | nM | Ki | J Med Chem (1991) 34: 2430-2438 [PMID:1714957] |
ChEMBL | Binding affinity at opioid receptor delta 1 by displacement of [3H]DADLE in rat brain membrane | B | 6.33 | pKi | 469 | nM | Ki | J Med Chem (2004) 47: 1400-1412 [PMID:14998329] |
ChEMBL | Binding affinity against Opioid receptor delta 1 in P2 membrane preparation of rat brain by [3H]DADLE displacement. | B | 6.74 | pKi | 180.4 | nM | Ki | J Med Chem (1991) 34: 1350-1355 [PMID:1849997] |
ChEMBL | Displacement of [3H]deltorphin2 from delta opioid receptor in rat brain membrane | B | 6.14 | pIC50 | 727 | nM | IC50 | Bioorg Med Chem (2007) 15: 3883-3888 [PMID:17395470] |
ChEMBL | Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay | F | 7.31 | pEC50 | 49 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 2320-2323 [PMID:29853330] |
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
ChEMBL | In vitro potency was measured against human Opioid receptor kappa 1 | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1998) 41: 2631-2635 [PMID:9651168] |
ChEMBL | Inhibition of [3H]U-69593 binding to human Opioid receptor kappa 1 | B | 5.7 | pKi | >2000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5045-5050 [PMID:15380196] |
ChEMBL | Binding affinity for kappa opioid receptor | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 1585-1589 [PMID:12699761] |
GtoPdb | - | - | 6.5 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
ChEMBL | Displacement of [3H]U69593 from human KOP receptor expressed in CHO cells after 60 mins by scintillation counting | B | 6.51 | pKi | 306 | nM | Ki | J Med Chem (2011) 54: 6531-6537 [PMID:21866885] |
ChEMBL | Displacement of [3H]U-69593 from human recombinant Opioid receptor kappa 1 on CHO cell membranes. | B | 6.52 | pKi | 305 | nM | Ki | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
ChEMBL | Displacement of [3H]-U69593 from human kappa opioid receptor expressed in CHO cells after 60 mins by scintillation counting analysis | B | 6.57 | pKi | 270 | nM | Ki | J Med Chem (2015) 58: 5728-5741 [PMID:26125201] |
ChEMBL | Agonist activity at human kappa opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2016) 59: 11027-11038 [PMID:27958743] |
ChEMBL | Stimulation of U-69,593 binding at human recombinant Opioid receptor kappa 1 transfected into CHO cells. | B | 5.36 | pEC50 | 4365 | nM | EC50 | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
ChEMBL | Agonist activity at human KOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | F | 5.4 | pEC50 | 4000 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4870-4874 [PMID:23880538] |
κ receptor/Kappa opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534] | ||||||||
ChEMBL | Agonist activity at mouse KOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | F | 5.4 | pEC50 | 4000 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4870-4874 [PMID:23880538] |
κ receptor in Rat [GtoPdb: 318] [UniProtKB: P34975] | ||||||||
GtoPdb | - | - | 5.9 | pKi | - | - | - | Proc Natl Acad Sci USA (1993) 90: 9954-8 [PMID:8234341] |
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
ChEMBL | Binding affinity against kappa opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 6 nM nor-BNI | F | 6.29 | pKd | 509 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3053-3056 [PMID:10571174] |
ChEMBL | Binding affinity against kappa opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 6 nM nor-BNI | F | 6.29 | pKd | 509 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3347-3350 [PMID:10612597] |
ChEMBL | Binding affinity at Opioid receptor kappa 1 by displacement of [3H]U-69593 in guinea pig brain membranes | B | 5.24 | pKi | 5820 | nM | Ki | J Med Chem (2004) 47: 1400-1412 [PMID:14998329] |
ChEMBL | Displacement of [3H]U69593 from Sprague-Dawley rat kappa opioid receptor in guinea pig cerebella by liquid scintillation counting | B | 5.3 | pKi | >5000 | nM | Ki | Bioorg Med Chem (2010) 18: 4975-4982 [PMID:20599386] |
ChEMBL | Displacement of radiolabeled U69593 from kappa1 opioid receptor in Hartley guinea pig brain | B | 5.73 | pKi | 1841 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416] |
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
ChEMBL | Displacement of [3H]diprenorphine from human MOR expressed in CHO-FlpIn cell membranes after 1 hr by liquid scintillation counting analysis | B | 5.66 | pKi | 2187.76 | nM | Ki | J Med Chem (2015) 58: 9754-9767 [PMID:26632862] |
ChEMBL | Displacement of 2-((1E,3E,5E)-5-(1-Ethyl-3,3-dimethyl-5-sulfoindolin-2-ylidene)-penta-1,3-dien-1-yl)-1-(6-((6-((6S,7R,7aR,12bS)-9-hydroxy-7-methoxy-3-methyl-1,2,3,4,5,6,7,7a-octahydro-4a,7-ethano-4,12-methanobenzofuro[3,2-e]isoquinoline-6-carboxamido)hexyl)-amino)-6-oxohexyl)-3,3-dimethyl-3H-indol-1-ium-5-sulfonate,2,2,2-Trifluoroacetate Salt from human MOR expressed in HEK293 cells by Cheng-Prusoff analysis | B | 7.06 | pKi | 87.1 | nM | Ki | J Med Chem (2015) 58: 9754-9767 [PMID:26632862] |
ChEMBL | Inhibition of [3H]diprenorphine binding to human Opioid receptor mu 1 | B | 7.44 | pKi | 36.7 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5045-5050 [PMID:15380196] |
ChEMBL | In vitro potency was measured against human Opioid receptor mu 1 | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (1998) 41: 2631-2635 [PMID:9651168] |
ChEMBL | Displacement of [3H]Diprenorphine from human recombinant mu opioid receptor expressed in CHOK1 cells after 60 mins | B | 8.09 | pKi | 8.1 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor expressed in CHO cells | B | 8.17 | pKi | 6.7 | nM | Ki | J Med Chem (2009) 52: 247-258 [PMID:19113864] |
ChEMBL | Binding affinity to mu opioid receptor | B | 8.42 | pKi | 3.8 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6736-6739 [PMID:19836950] |
ChEMBL | Displacement of [3H]diprenorphine from human recombinant mu opioid receptor expressed in in CHO cells | B | 8.43 | pKi | 3.71 | nM | Ki | Bioorg Med Chem (2007) 15: 4434-4443 [PMID:17490886] |
ChEMBL | Displacement of [125I]-IBNtxA from MOR-1 expressed in CHO cells | B | 8.48 | pKi | 3.34 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410] |
ChEMBL | Displacement of [3H]-DAMGO from human MOR expressed in CHO-K1 cell membranes incubated for 90 mins measured by MicroBeta scintillation counter method | B | 8.49 | pKi | 3.2 | nM | Ki | Eur J Med Chem (2022) 241: 114649-114649 [PMID:35961067] |
ChEMBL | Displacement of [3H]DAMGO from human mu opioid receptor transfected in CHO cell membranes after 60 mins | B | 8.53 | pKi | 2.96 | nM | Ki | Bioorg Med Chem (2014) 22: 2508-2516 [PMID:24657054] |
ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor (unknown origin) expressed in HEK293T cells after 1.5 hrs by radioligand binding assay | B | 8.64 | pKi | 2.3 | nM | Ki | Eur J Med Chem (2014) 85: 818-829 [PMID:25193297] |
ChEMBL | Displacement of [3H]DAMGO from human MOP receptor expressed in CHO cells after 60 mins by scintillation counting | B | 8.8 | pKi | 1.59 | nM | Ki | J Med Chem (2011) 54: 6531-6537 [PMID:21866885] |
ChEMBL | Displacement of [125I]-IBOxyA from MOR-1 expressed in CHO cells | B | 8.81 | pKi | 1.55 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410] |
ChEMBL | Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK293 cells by scintillation counting | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2014) 57: 6861-6866 [PMID:25051243] |
ChEMBL | Displacement of [3H]DAMGO from human MOR expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2016) 59: 9255-9261 [PMID:27607020] |
ChEMBL | Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK293 cell membranes after 2 hrs by liquid scintillation spectrometry | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2018) 61: 5751-5757 [PMID:29901392] |
ChEMBL | Displacement of [3H]DAMGO from human MOR expressed in CHO cells | B | 8.82 | pKi | 1.5 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 666-669 [PMID:28011222] |
ChEMBL | Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells after 2 hrs by liquid scintillation counting | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2012) 55: 10292-10296 [PMID:22995061] |
ChEMBL | Binding affinity to MOR (unknown origin) assessed as inhibition constant by radioligand binding assay | B | 8.83 | pKi | 1.49 | nM | Ki | Bioorg Med Chem Lett (2022) 72: 128860-128860 [PMID:35724925] |
ChEMBL | Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells preincubated for 1 hr followed by radioligand addition measured after 1 hr by liquid scintillation counting analysis | B | 8.9 | pKi | 1.26 | nM | Ki | J Med Chem (2015) 58: 9754-9767 [PMID:26632862] |
ChEMBL | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting analysis | B | 8.92 | pKi | 1.2 | nM | Ki | Bioorg Med Chem (2013) 21: 3298-3309 [PMID:23618710] |
ChEMBL | Displacement of [3H]DAMGO from human recombinant opioid mu receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method | B | 8.92 | pKi | 1.2 | nM | Ki | Eur J Med Chem (2015) 92: 531-539 [PMID:25599950] |
ChEMBL | Displacement of [3H]-DAMGO from human mu opioid receptor expressed in CHO cells membrane after 2 hrs by liquid scintillation counting | B | 8.92 | pKi | 1.2 | nM | Ki | Eur J Med Chem (2012) 50: 44-54 [PMID:22341895] |
ChEMBL | Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting | B | 8.92 | pKi | 1.2 | nM | Ki | Eur J Med Chem (2013) 67: 335-343 [PMID:23880358] |
ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor (unknown origin) assessed as inhibition constant incubated for 180 mins by competitive radioligand binding assay | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2023) 66: 3312-3326 [PMID:36827198] |
ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor expressed in HEK293 cells by visible spectrophotometry | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449] |
ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor (unknown origin) | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 2860-2862 [PMID:23587424] |
ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor (unknown origin) assessed as inhibition constant incubated for 180 mins by competitive radioligand binding assay | B | 9.1 | pKi | 0.79 | nM | Ki | J Med Chem (2023) 66: 3312-3326 [PMID:36827198] |
ChEMBL | Displacement of [3H]-Diprenorphine from human mu opiod receptor expressed in CHO cells incubated for 1 hr by competition binding assay | B | 9.19 | pKi | 0.64 | nM | Ki | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
ChEMBL | Displacement of [3H]DAMGO from MOR in HEK293 cells | B | 9.22 | pKi | 0.6 | nM | Ki | Bioorg Med Chem (2016) 24: 5280-5290 [PMID:27624520] |
ChEMBL | Displacement of [3H]-DAMGO from human mu opioid receptor expressed in CHO cells after 60 mins by scintillation counting analysis | B | 9.25 | pKi | 0.56 | nM | Ki | J Med Chem (2015) 58: 5728-5741 [PMID:26125201] |
ChEMBL | Binding affinity for mu opioid receptor | B | 9.28 | pKi | 0.53 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 1585-1589 [PMID:12699761] |
GtoPdb | - | - | 9.3 | pKi | - | - | - |
NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]; Eur J Pharmacol (1981) 70: 531-40 [PMID:6263640] |
ChEMBL | Displacement of [3H]DAMGO from human recombinant Opioid receptor mu 1 on CHO cell membranes. | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
ChEMBL | Displacement of [125I]-IBNalA from MOR-1 expressed in CHO cells | B | 9.35 | pKi | 0.45 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410] |
ChEMBL | Displacement of radiolabeled DAMGO from human mu-type opioid receptor agonist site | F | 9.36 | pKi | 0.44 | nM | Ki | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
ChEMBL | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in HEK293 cell membranes incubated for 60 mins | B | 9.39 | pKi | 0.41 | nM | Ki | J Med Chem (2020) 63: 433-439 [PMID:31834797] |
ChEMBL | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in HEK293 cells incubated for 120 mins by radiometric scintillation analysis | B | 9.39 | pKi | 0.4 | nM | Ki | J Nat Prod (2021) 84: 1034-1043 [PMID:33635670] |
ChEMBL | Displacement of [3H]-DAMGO from human mu opioid receptor expressed in CHO-K1 cells by radioligand binding assay | B | 9.46 | pKi | 0.35 | nM | Ki | J Nat Prod (2021) 84: 71-80 [PMID:33326237] |
ChEMBL | Displacement of [3H]-DAMGO from human mu opioid receptor expressed in CHO-K1 cells by radioligand binding assay | B | 9.5 | pKi | 0.32 | nM | Ki | J Nat Prod (2021) 84: 71-80 [PMID:33326237] |
ChEMBL | Binding affinity to human mu-type opioid receptor by radioligand displacement assay | B | 9.55 | pKi | 0.28 | nM | Ki | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
ChEMBL | Displacement of [3H]Diprenorphine from human recombinant mu opioid receptor expressed in CHOK1 cells after 60 mins | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
ChEMBL | Agonist activity at human MOR expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by EIA method | F | 7.71 | pIC50 | 19.3 | nM | IC50 | J Med Chem (2016) 59: 9255-9261 [PMID:27607020] |
ChEMBL | Agonist activity at human MOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay | F | 8.29 | pIC50 | 5.1 | nM | IC50 | Eur J Med Chem (2017) 126: 202-217 [PMID:27776274] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production after 30 mins by HTRF assay | F | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem (2014) 22: 4694-4703 [PMID:25087049] |
ChEMBL | Agonist activity at mu opioid expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation | F | 8.5 | pIC50 | 3.18 | nM | IC50 | Bioorg Med Chem (2010) 18: 4975-4982 [PMID:20599386] |
ChEMBL | Agonist activity at human MOR expressed in CHO cells assessed as induction of membrane potential change measured every 3 secs for 30 secs by fluorescent membrane potential assay | B | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (2016) 59: 1239-1245 [PMID:26789491] |
ChEMBL | Inhibition of human mu opioid receptor | B | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (2008) 51: 4150-4169 [PMID:18588282] |
ChEMBL | Displacement of [3H]naloxone from mu opioid receptor expressed in CHO cell membrane | B | 8.7 | pIC50 | 2 | nM | IC50 | J Nat Prod (2010) 73: 988-991 [PMID:20426456] |
ChEMBL | Agonist activity at Gi-coupled mu opioid receptor (unknown origin) expressed in HEK293T cells assessed as inhibition of cAMP production at pH 6.5 measured after 15 mins by Glo-Sensor assay | F | 8.71 | pIC50 | 1.95 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1353-1356 [PMID:31531209] |
ChEMBL | Binding activity against human Opioid receptor mu 1 using [3H]DAMGO as a radioligand | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2002) 45: 1395-1398 [PMID:11906279] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in HEK293 assessed as inhibition forskolin-induced cAMP accumulation after 15 mins by EIA | F | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2018) 61: 5751-5757 [PMID:29901392] |
ChEMBL | Displacement of radiolabeled DAMGO from human mu-type opioid receptor agonist site | F | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
ChEMBL | Agonist activity at Gi-coupled mu opioid receptor (unknown origin) expressed in HEK293T cells assessed as inhibition of cAMP production at pH 7.4 measured after 15 mins by Glo-Sensor assay | F | 9.1 | pIC50 | 0.79 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1353-1356 [PMID:31531209] |
ChEMBL | Binding affinity to mu opioid receptor (unknown origin) by radioligand displacement assay | B | 9.13 | pIC50 | 0.74 | nM | IC50 | Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449] |
ChEMBL | Binding affinity to human mu-type opioid receptor by radioligand displacement assay | B | 9.17 | pIC50 | 0.68 | nM | IC50 | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
ChEMBL | Displacement of [3H]DAMGO from human recombinant mu-opioid receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method | B | 9.37 | pIC50 | 0.43 | nM | IC50 | Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250] |
ChEMBL | Displacement of [3H]DAMGO from human recombinant Mu-type opioid receptor expressed in CHO cells | B | 9.37 | pIC50 | 0.43 | nM | IC50 | Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in human USOS-beta-arrestin-hMOR-PathHunter cells incubated for 90 mins by beta-arrestin-2 enzyme fragment complementation assay | F | 6.66 | pEC50 | 220 | nM | EC50 | J Med Chem (2018) 61: 8895-8907 [PMID:30199635] |
ChEMBL | Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor mu 1 | B | 6.69 | pEC50 | 202 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 5045-5050 [PMID:15380196] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO-K1 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay | F | 6.7 | pEC50 | 199.53 | nM | EC50 | J Nat Prod (2021) 84: 71-80 [PMID:33326237] |
ChEMBL | Agonist activity at human MOR receptor expressed in HTLA cells co-expressing TEV-fused-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment by Tango assay | F | 6.74 | pEC50 | 182.04 | nM | EC50 | J Med Chem (2021) 64: 13873-13892 [PMID:34505767] |
ChEMBL | Agonist activity at human MOR receptor expressed in HTLA cells co-expressing TEV-fused-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment by Tango assay | F | 6.74 | pEC50 | 181.97 | nM | EC50 | J Med Chem (2021) 64: 13873-13892 [PMID:34505767] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins | F | 6.96 | pEC50 | 110 | nM | EC50 | Bioorg Med Chem (2007) 15: 4106-4112 [PMID:17433695] |
ChEMBL | Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding | F | 6.96 | pEC50 | 110 | nM | EC50 | J Med Chem (2007) 50: 2254-2258 [PMID:17407276] |
ChEMBL | Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | F | 6.96 | pEC50 | 110 | nM | EC50 | J Med Chem (2006) 49: 256-262 [PMID:16392810] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding | F | 6.96 | pEC50 | 110 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 1508-1511 [PMID:17276685] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting | F | 6.96 | pEC50 | 110 | nM | EC50 | J Med Chem (2011) 54: 1903-1913 [PMID:21351746] |
ChEMBL | Agonist activity at MOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay | F | 7.19 | pEC50 | 64.9 | nM | EC50 | J Med Chem (2023) 66: 17138-17154 [PMID:38095323] |
ChEMBL | Agonist activity at mu opioid receptor (unknown origin) assessed as beta arrestin-2 recruitment incubated for 3 days by PathHunter assay | F | 7.22 | pEC50 | 60.9 | nM | EC50 | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cell membrane assessed as stimulation of [35S]GTPgammaS binding after 60 mins by liquid scintillation counting | F | 7.26 | pEC50 | 55 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 2128-2133 [PMID:23434225] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding | F | 7.26 | pEC50 | 55 | nM | EC50 | J Med Chem (2006) 49: 5635-5639 [PMID:16942039] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assay | F | 7.26 | pEC50 | 55 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 6516-6520 [PMID:17935988] |
ChEMBL | Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 7.26 | pEC50 | 55 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293] |
ChEMBL | Activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.26 | pEC50 | 55 | nM | EC50 | Bioorg Med Chem (2008) 16: 5653-5664 [PMID:18417347] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.26 | pEC50 | 55 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 2289-2294 [PMID:19282177] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.26 | pEC50 | 55 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 365-368 [PMID:19091564] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting | F | 7.26 | pEC50 | 55 | nM | EC50 | J Med Chem (2012) 55: 3878-3890 [PMID:22439881] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting | F | 7.26 | pEC50 | 55 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 7340-7344 [PMID:23142613] |
ChEMBL | Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation [35S]GTPgammaS binding relative to basal level | F | 7.35 | pEC50 | 45.1 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 1825-1829 [PMID:19217280] |
ChEMBL | Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 7.35 | pEC50 | 45.06 | nM | EC50 | J Med Chem (2009) 52: 1416-1427 [PMID:19199782] |
ChEMBL | Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | F | 7.4 | pEC50 | 40 | nM | EC50 | J Med Chem (2008) 51: 2421-2431 [PMID:18380425] |
ChEMBL | Partial agonist activity at human MOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting | F | 7.45 | pEC50 | 35.3 | nM | EC50 | J Med Chem (2011) 54: 6531-6537 [PMID:21866885] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by scintillation counting method | F | 7.48 | pEC50 | 33 | nM | EC50 | J Med Chem (2018) 61: 8895-8907 [PMID:30199635] |
ChEMBL | Agonist activity at human mu opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis | F | 7.49 | pEC50 | 32.6 | nM | EC50 | Bioorg Med Chem (2014) 22: 2508-2516 [PMID:24657054] |
ChEMBL | Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay | B | 7.52 | pEC50 | 30 | nM | EC50 | ACS Med Chem Lett (2016) 7: 391-396 [PMID:27096047] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay | F | 7.59 | pEC50 | 25.5 | nM | EC50 | J Med Chem (2020) 63: 7663-7694 [PMID:32530286] |
ChEMBL | Agonist activity at human MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay | F | 7.64 | pEC50 | 23 | nM | EC50 | ACS Med Chem Lett (2020) 11: 720-726 [PMID:32435376] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay | F | 7.71 | pEC50 | 19.7 | nM | EC50 | ACS Med Chem Lett (2019) 10: 450-456 [PMID:30996778] |
ChEMBL | Agonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | F | 7.82 | pEC50 | 15 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4870-4874 [PMID:23880538] |
ChEMBL | Stimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells | F | 7.86 | pEC50 | 13.7 | nM | EC50 | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
ChEMBL | Agonist activity at human MOR expressed in CHO cells assessed as increase in intracellular Ca2+ level after 30 mins by cytosensor micrometer | F | 8.02 | pEC50 | 9.61 | nM | EC50 | Bioorg Med Chem (2015) 23: 1701-1715 [PMID:25783191] |
ChEMBL | Activity at mu opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding | F | 8.09 | pEC50 | 8.2 | nM | EC50 | Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449] |
ChEMBL | Agonist activity at MOR (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 60 mins by liquid scintillation counting analysis | B | 8.09 | pEC50 | 8.1 | nM | EC50 | J Med Chem (2021) 64: 9458-9483 [PMID:34152138] |
ChEMBL | Agonist activity at human MOR expressed in CHO cells by [35S]GTPgammaS binding assay | F | 8.12 | pEC50 | 7.57 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4895-4898 [PMID:25248680] |
ChEMBL | Agonist activity at human MOR expressed in CHO cells assessed as increase in intracellular Ca2+ level after 30 mins by microplate reader analysis | F | 8.12 | pEC50 | 7.5 | nM | EC50 | Bioorg Med Chem (2015) 23: 1701-1715 [PMID:25783191] |
ChEMBL | Agonist activity at human MOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay | F | 8.14 | pEC50 | 7.2 | nM | EC50 | J Med Chem (2020) 63: 2673-2687 [PMID:31834798] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assay | F | 8.2 | pEC50 | 6.38 | nM | EC50 | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
ChEMBL | Agonist activity at human MOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Glo-sensor cAMP assay | F | 8.23 | pEC50 | 5.89 | nM | EC50 | J Med Chem (2021) 64: 13873-13892 [PMID:34505767] |
ChEMBL | Agonist activity at human MOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation counting | F | 8.5 | pEC50 | 3.18 | nM | EC50 | J Med Chem (2011) 54: 7848-7859 [PMID:21978284] |
ChEMBL | Agonist activity at FLAG-tagged mu-type opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by liquid scintillation counting analysis | F | 8.52 | pEC50 | 3.04 | nM | EC50 | J Med Chem (2013) 56: 3102-3114 [PMID:23477419] |
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 | 8.52 | pEC50 | 3.04 | nM | EC50 | J Med Chem (2012) 55: 6224-6236 [PMID:22724433] |
ChEMBL | Agonist activity at human MOR expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 45 mins by cAMP HTRF assay | F | 8.7 | pEC50 | 2 | nM | EC50 | Eur J Med Chem (2022) 241: 114649-114649 [PMID:35961067] |
ChEMBL | Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry | F | 8.71 | pEC50 | 1.97 | nM | EC50 | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 8.77 | pEC50 | 1.7 | nM | EC50 | J Med Chem (2008) 51: 4404-4411 [PMID:18637671] |
ChEMBL | Activation of human mu opioid receptor expressed in HEK293a cells coexpressing YFP-labelled alphai1 and CFP-labelled beta-1-gamma-2 Gi subunits assessed as decrease in fluorescence resonance energy transfer signal at 10 uM | B | 9 | pEC50 | 1 | nM | EC50 | J Biol Chem (2007) 282: 27126-27132 [PMID:17616524] |
ChEMBL | Activation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assay | F | 9 | pEC50 | 1 | nM | EC50 | J Biol Chem (2007) 282: 27126-27132 [PMID:17616524] |
ChEMBL | Agonist activity at human mu opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay | F | 9.22 | pEC50 | 0.6 | nM | EC50 | J Med Chem (2016) 59: 11027-11038 [PMID:27958743] |
ChEMBL | Agonist activity at human MOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Glo-sensor cAMP assay | F | 9.31 | pEC50 | 0.49 | nM | EC50 | J Med Chem (2021) 64: 13873-13892 [PMID:34505767] |
ChEMBL | Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay | F | 9.52 | pEC50 | 0.3 | nM | EC50 | RSC Med Chem (2020) 11: 896-904 [PMID:33479684] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as decrease in intracellular cAMP level measured after 1 hr by LANCE ultra cAMP assay | F | 9.68 | pEC50 | 0.21 | nM | EC50 | Eur J Med Chem (2022) 243: 114728-114728 [PMID:36084534] |
μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866] | ||||||||
ChEMBL | Displacement of [3H] DAMGO from mouse MOR expressed in CHO cell membrane incubated for 90 mins by scintillation method | B | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (2021) 64: 9458-9483 [PMID:34152138] |
ChEMBL | Displacement of [3H]DAMGO from mouse whole brain MOR | B | 9.08 | pKi | 0.83 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4895-4898 [PMID:25248680] |
ChEMBL | Agonist activity at mu opioid receptor in NMRI mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | F | 7.12 | pIC50 | 75.55 | nM | IC50 | J Med Chem (2008) 51: 173-177 [PMID:18062664] |
ChEMBL | Agonist activity at mouse HA-tagged mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 15 mins by Glo-sensor reagent based assay | F | 8.18 | pIC50 | 6.6 | nM | IC50 | J Nat Prod (2021) 84: 71-80 [PMID:33326237] |
ChEMBL | Agonist activity at mouse HA-tagged mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 15 mins by Glo-sensor reagent based assay | F | 8.2 | pIC50 | 6.31 | nM | IC50 | J Nat Prod (2021) 84: 71-80 [PMID:33326237] |
ChEMBL | Displacement of [125I]-DAMGO from mouse Flag-tagged mu-opioid receptor expressed in HEK293 cell membranes after 60 mins by gamma counting | B | 8.86 | pIC50 | 1.39 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2320-2323 [PMID:29853330] |
ChEMBL | Agonist activity at Rluc8 fused mouse MOR transfected in HEK293T cells assessed as Nb33 recruitment using coelenterazine as substrate incubated for 40 mins by BRET assay | F | 6.61 | pEC50 | 248 | nM | EC50 | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
ChEMBL | Agonist activity at Rluc8 fused mouse MOR transfected in HEK293T cells assessed as Nb33 recruitment using coelenterazine as substrate incubated for 40 mins by BRET assay | F | 6.61 | pEC50 | 245.47 | nM | EC50 | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
ChEMBL | Agonist activity at Rluc8 fused mouse MOR transfected in HEK293T cells coexpressing wild type GRK2 assessed as arrestin-3 recruitment using coelenterazine as substrate incubated for 40 mins by BRET assay | F | 7.26 | pEC50 | 54.95 | nM | EC50 | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
ChEMBL | Agonist activity at Rluc8 fused mouse MOR transfected in HEK293T cells coexpressing wild type GRK2 assessed as arrestin-3 recruitment using coelenterazine as substrate incubated for 40 mins by BRET assay | F | 7.26 | pEC50 | 54.4 | nM | EC50 | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
ChEMBL | Agonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopy | F | 7.72 | pEC50 | 19 | nM | EC50 | Medchemcomm (2017) 8: 152-157 [PMID:28603600] |
ChEMBL | Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP formation incubated for 8 min followed by forskolin stimulation by ELISA | F | 7.72 | pEC50 | 19 | nM | EC50 | J Med Chem (2019) 62: 11399-11415 [PMID:31782922] |
ChEMBL | Agonist activity at mouse mu opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis | F | 7.72 | pEC50 | 19 | nM | EC50 | J Med Chem (2016) 59: 8381-8397 [PMID:27556704] |
ChEMBL | Agonist activity at HA-tagged mouse mu opioid receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by Glo Sensor assay | B | 8.15 | pEC50 | 7 | nM | EC50 | J Med Chem (2023) 66: 3312-3326 [PMID:36827198] |
ChEMBL | Agonist activity at HA-tagged mouse mu opioid receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by Glo Sensor assay | B | 8.2 | pEC50 | 6.31 | nM | EC50 | J Med Chem (2023) 66: 3312-3326 [PMID:36827198] |
ChEMBL | Agonist activity at mouse cloned mu opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay | F | 8.25 | pEC50 | 5.6 | nM | EC50 | Eur J Med Chem (2013) 69: 786-789 [PMID:24103580] |
ChEMBL | Agonist activity at mouse MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay | F | 8.3 | pEC50 | 5 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4870-4874 [PMID:23880538] |
ChEMBL | Agonist activity at SNAP-tagged mouse MOR transfected in HEK293T cells coexpressing wild type Galpha-i2, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-i2 activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay | F | 8.48 | pEC50 | 3.31 | nM | EC50 | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
ChEMBL | Agonist activity at SNAP-tagged mouse MOR transfected in HEK293T cells coexpressing wild type Galpha-i2, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-i2 activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay | F | 8.48 | pEC50 | 3.28 | nM | EC50 | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
ChEMBL | Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem (2009) 17: 7337-7343 [PMID:19762245] |
ChEMBL | Binding affinity at Opioid receptor mu 1 by displacement of [3H]DAMGO in rat brain membrane | B | 8.21 | pKi | 6.1 | nM | Ki | J Med Chem (2004) 47: 1400-1412 [PMID:14998329] |
ChEMBL | Compound was evaluated for binding affinity towards mu-specific opiate receptor from combinatorial peptoid library | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (1994) 37: 2678-2685 [PMID:8064796] |
ChEMBL | Inhibition of [3H]DAGO binding to mu 1 opioid receptor in rat brain membranes | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (1988) 31: 374-383 [PMID:2828622] |
ChEMBL | Binding affinity to opioid receptor mu was determined in rat brain using [3H]DAGO as radioligand | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (1991) 34: 2430-2438 [PMID:1714957] |
ChEMBL | Displacement of [3H]-DAMGO from rat mu opioid receptor expressed in CHO cells incubated for 30 mins by liquid scintillation counting method | B | 8.64 | pKi | 2.3 | nM | Ki | Eur J Med Chem (2020) 189: 112070-112070 [PMID:31982651] |
GtoPdb | - | - | 8.7 | pKi | - | - | - | Mol Pharmacol (1994) 45: 330-4 [PMID:8114680] |
ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membranes by liquid scintillation counting | B | 8.77 | pKi | 1.7 | nM | Ki | Eur J Med Chem (2013) 68: 167-177 [PMID:23974016] |
ChEMBL | Binding affinity towards Opioid receptor mu 1 | B | 8.79 | pKi | 1.64 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 2755-2758 [PMID:11133084] |
ChEMBL | Inhibition of [3H]-DAMGO binding to Opioid receptor mu 1 of rat brain membranes | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (2004) 47: 5198-5203 [PMID:15456262] |
ChEMBL | Binding affinity towards Opioid receptor mu 1 by displacing [3H]DAMGO in rat brain membranes. | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (2002) 45: 2571-2578 [PMID:12036366] |
ChEMBL | Displacement of [3H]-DAMGO from Sprague-Dawley rat brain membrane mu opioid receptor incubated for 45 mins by liquid scintillation counting analysis | B | 8.83 | pKi | 1.49 | nM | Ki | Eur J Med Chem (2022) 230: 114091-114091 [PMID:35016113] |
ChEMBL | Binding affinity against Opioid receptor mu 1 by displacement of radioligand [3H]-DAGO in rat brain membrane | B | 8.91 | pKi | 1.22 | nM | Ki | J Med Chem (1989) 32: 698-703 [PMID:2537427] |
ChEMBL | Displacement of [3H]-DAMGO from MOR in rat brain membranes incubated for 45 mins by liquid scintillation counting | B | 8.94 | pKi | 1.16 | nM | Ki | Eur J Med Chem (2019) 168: 189-198 [PMID:30822708] |
ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membranes by liquid scintillation counting based competition binding assay | B | 9 | pKi | 1 | nM | Ki | ACS Med Chem Lett (2014) 5: 1032-1036 [PMID:25221662] |
ChEMBL | Displacement of [3H]-DAMGO from MOR in rat brain membranes incubated for 45 mins by liquid scintillation counting | B | 9.05 | pKi | 0.9 | nM | Ki | ACS Med Chem Lett (2020) 11: 678-685 [PMID:32435370] |
ChEMBL | Displacement of [3H]DAMGO from Sprague-Dawley rat mu opioid receptor by liquid scintillation counting | B | 9.06 | pKi | 0.87 | nM | Ki | Bioorg Med Chem (2010) 18: 4975-4982 [PMID:20599386] |
ChEMBL | Displacement of [3H]DPDPE from rat mu opioid receptor | B | 9.07 | pKi | 0.85 | nM | Ki | J Med Chem (2010) 53: 5491-5501 [PMID:20617791] |
ChEMBL | Binding affinity against Opioid receptor mu 1 in P2 membrane preparation of rat brain by [3H]DAGO displacement. | B | 9.18 | pKi | 0.66 | nM | Ki | J Med Chem (1991) 34: 1350-1355 [PMID:1849997] |
ChEMBL | Compound was evaluated for the binding affinity of Opioid receptor mu 1 by displacing the radioligand [3H]DAMGO from rat brain membrane | B | 9.28 | pKi | 0.53 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1185-1188 [PMID:10866377] |
ChEMBL | Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells | B | 7.44 | pIC50 | 36.31 | nM | IC50 | Bioorg Med Chem (2009) 17: 7337-7343 [PMID:19762245] |
ChEMBL | Inhibitory activity against [3H]DAMGO binding to Opioid receptor mu 1 in rat brain membranes | B | 8 | pIC50 | 9.9 | nM | IC50 | J Med Chem (2002) 45: 2571-2578 [PMID:12036366] |
ChEMBL | Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 of rat brain membranes | B | 8 | pIC50 | 9.9 | nM | IC50 | J Med Chem (2004) 47: 5198-5203 [PMID:15456262] |
ChEMBL | Concentration required for inhibition of [3H]DAMGO binding to Opioid receptor mu 1 in rat brain membranes | B | 8 | pIC50 | 9.89 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2755-2758 [PMID:11133084] |
ChEMBL | The compound was tested for binding affinity towards rat Opioid receptor mu 1 by displacing [3H]DAMGO. | B | 8.46 | pIC50 | 3.5 | nM | IC50 | J Med Chem (1999) 42: 4331-4342 [PMID:10543877] |
ChEMBL | Binding affinity against rat mu-opioid receptor expressed in CHO cells by competitive inhibition of 1 nM [3H]DAMGO | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 2027-2032 [PMID:9873480] |
ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membranes by liquid scintillation counting | B | 8.62 | pIC50 | 8.62 | - | 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 | 8.95 | pIC50 | 1.13 | nM | IC50 | Bioorg Med Chem (2007) 15: 3883-3888 [PMID:17395470] |
ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat brain | B | 9 | pIC50 | 1.01 | nM | IC50 | Bioorg Med Chem (2009) 17: 5782-5790 [PMID:19640720] |
ChEMBL | Agonist activity at mu opioid receptor in Wistar rat brain membranes after 60 mins by [35S]GTPgammaS binding assay | F | 6.31 | pEC50 | 485 | 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 | 214 | nM | EC50 | J Med Chem (2011) 54: 1462-1472 [PMID:21287991] |
ChEMBL | Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method | F | 6.84 | pEC50 | 146 | nM | EC50 | Bioorg Med Chem (2017) 25: 2406-2422 [PMID:28314512] |
ChEMBL | Activity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS binding | F | 6.84 | pEC50 | 145 | nM | EC50 | J Med Chem (2008) 51: 4270-4279 [PMID:18572932] |
ChEMBL | Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 7.09 | pEC50 | 81 | nM | EC50 | ACS Med Chem Lett (2014) 5: 1032-1036 [PMID:25221662] |
ChEMBL | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assay | F | 7.4 | pEC50 | 7.4 | nM | pEC50 | J Med Chem (2008) 51: 6334-6347 [PMID:18821747] |
ChEMBL | Agonist activity at rat mu opioid receptor by [35S]GTP-gamma-S binding assay | F | 7.4 | pEC50 | -7.4 | - | logEC50 | J Med Chem (2008) 51: 1369-1376 [PMID:18266313] |
ChEMBL | Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells | F | 7.43 | pEC50 | 37 | nM | EC50 | J Med Chem (2006) 49: 2868-2875 [PMID:16686530] |
ChEMBL | Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells | F | 7.43 | pEC50 | 37 | nM | EC50 | J Med Chem (2006) 49: 1773-1780 [PMID:16509592] |
ChEMBL | Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.43 | pEC50 | 37 | nM | EC50 | Bioorg Med Chem (2009) 17: 7337-7343 [PMID:19762245] |
ChEMBL | Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay | F | 7.43 | pEC50 | 37 | nM | EC50 | J Med Chem (2007) 50: 2779-2786 [PMID:17516639] |
ChEMBL | Agonist activity at rat mu opioid receptor by [35S]GTP-gamma-S binding assay | F | 7.43 | pEC50 | 37 | nM | EC50 | J Med Chem (2008) 51: 1369-1376 [PMID:18266313] |
ChEMBL | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding | F | 7.43 | pEC50 | 37 | nM | EC50 | J Med Chem (2010) 53: 5491-5501 [PMID:20617791] |
ChEMBL | Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.43 | pEC50 | 37 | nM | EC50 | J Med Chem (2011) 54: 382-386 [PMID:21128594] |
ChEMBL | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assay | F | 7.43 | pEC50 | 37 | nM | EC50 | J Med Chem (2008) 51: 6334-6347 [PMID:18821747] |
ChEMBL | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding | F | 7.43 | pEC50 | 37 | nM | EC50 | J Med Chem (2011) 54: 2029-2038 [PMID:21366266] |
ChEMBL | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay | F | 7.43 | pEC50 | 37 | nM | EC50 | J Med Chem (2009) 52: 5164-5175 [PMID:20560643] |
ChEMBL | Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells | F | 7.44 | pEC50 | 36.31 | nM | EC50 | J Med Chem (2006) 49: 1773-1780 [PMID:16509592] |
ChEMBL | Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells | F | 7.44 | pEC50 | 36.31 | nM | EC50 | J Med Chem (2006) 49: 2868-2875 [PMID:16686530] |
ChEMBL | Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay | F | 7.44 | pEC50 | 36.31 | nM | EC50 | J Med Chem (2007) 50: 2779-2786 [PMID:17516639] |
ChEMBL | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay | F | 7.44 | pEC50 | 36.31 | nM | EC50 | J Med Chem (2009) 52: 5164-5175 [PMID:20560643] |
ChEMBL | Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.44 | pEC50 | 36.31 | nM | EC50 | Bioorg Med Chem (2009) 17: 7337-7343 [PMID:19762245] |
ChEMBL | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding | F | 7.44 | pEC50 | 36.31 | nM | EC50 | J Med Chem (2010) 53: 5491-5501 [PMID:20617791] |
ChEMBL | Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.44 | pEC50 | 36.31 | nM | EC50 | J Med Chem (2011) 54: 382-386 [PMID:21128594] |
ChEMBL | Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding | F | 7.44 | pEC50 | 36.31 | nM | EC50 | J Med Chem (2011) 54: 2029-2038 [PMID:21366266] |
ChEMBL | Agonist activity at rat mu opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method | F | 8.09 | pEC50 | 8.06 | nM | EC50 | Eur J Med Chem (2020) 189: 112070-112070 [PMID:31982651] |
ChEMBL | Agonist activity at rat mu-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay | F | 9.59 | pEC50 | 0.26 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 2320-2323 [PMID:29853330] |
Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
ChEMBL | Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes in unblocked condition | F | 6.23 | pKd | 592 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3053-3056 [PMID:10571174] |
ChEMBL | Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes in unblocked condition | F | 6.23 | pKd | 592 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3347-3350 [PMID:10612597] |
ChEMBL | Displacement of radiolabeled DAMGO from mu opioid receptor in Hartley guinea pig brain | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416] |
ChEMBL | Binding affinity against mu opioid receptor | B | 9 | pKi | 0.99 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2681-2684 [PMID:9873602] |
ChEMBL | Agonist activity at mu-opioid receptor in guinea pig ileum assessed as inhibition of electrically induced contractions | F | 7.55 | pIC50 | 28.3 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2320-2323 [PMID:29853330] |
ChEMBL | Inhibition of electrically evoked contraction of guinea pig ileum (myenteric plexus:longitudinal muscle preparation) by antagonist action at mu 1 opioid receptors | F | 7.94 | pIC50 | 11.5 | nM | IC50 | J Med Chem (1988) 31: 374-383 [PMID:2828622] |
ChEMBL | Agonist activity at MOR in Dunkin-Hartley guinea pig ileum assessed as inhibition of EFS-induced contractions incubated for 60 mins | B | 6.8 | pEC50 | 158.49 | nM | EC50 | Bioorg Med Chem (2016) 24: 2832-2842 [PMID:27234885] |
NK1 receptor/Neurokinin 1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4027] [GtoPdb: 360] [UniProtKB: P14600] | ||||||||
ChEMBL | Affinity for rat Tachykinin receptor 1 determined in displacement screening by using radioligand 3,4-[3H]-(L-Pro e2) SP. | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1999) 42: 4331-4342 [PMID:10543877] |
NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146] | ||||||||
ChEMBL | Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2011) 54: 6531-6537 [PMID:21866885] |
Nociceptin receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5492] [UniProtKB: P47748] | ||||||||
ChEMBL | Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain | B | 7.57 | pKi | 26.9 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416] |
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]