ChEMBL ligand: CHEMBL31421
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] There should be some charts here, you may need to enable JavaScript!
κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] There should be some charts here, you may need to enable JavaScript!
μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] There should be some charts here, you may need to enable JavaScript!

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]-Diprenorphine from human DOP receptor expressed in HEK293 cells by scintillation counting method	B	7.24	pKi	57.1	nM	Ki	J Med Chem (2021) 64: 7555-7564 [PMID:34008968]
ChEMBL	Displacement of [3H]diprenorphine from human DOR expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting	B	8.48	pKi	3.3	nM	Ki	J Med Chem (2016) 59: 9255-9261 [PMID:27607020]
ChEMBL	Displacement of [3H]diprenorphine from human delta opioid receptor expressed in HEK293 cell membranes after 2 hrs by liquid scintillation spectrometry	B	8.48	pKi	3.3	nM	Ki	J Med Chem (2018) 61: 5751-5757 [PMID:29901392]
ChEMBL	Displacement of [3H]diprenorphine from human cloned delta opioid receptor	B	8.49	pKi	3.2	nM	Ki	Bioorg Med Chem Lett (2007) 17: 2656-2660 [PMID:17350835]
ChEMBL	Displacement of [3H]DPDPE from human DOR expressed in CHO cells	B	8.62	pKi	2.4	nM	Ki	Bioorg Med Chem Lett (2017) 27: 666-669 [PMID:28011222]
ChEMBL	Displacement of [3H]-DPDPE from human DOR expressed in CHO cell membranes measured after 2 hrs by microbeta scintillation counting method	B	8.64	pKi	2.3	nM	Ki	J Med Chem (2021) 64: 9458-9483 [PMID:34152138]
ChEMBL	Displacement of [3H]DPDPE from human DOR expressed in CHO cells	B	8.77	pKi	1.7	nM	Ki	Bioorg Med Chem (2016) 24: 5280-5290 [PMID:27624520]
GtoPdb	-	-	8.8	pKi	-	-	-	NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]; Proc Natl Acad Sci USA (1983) 80: 5871-4 [PMID:6310598]
ChEMBL	Displacement of [3H]DADLE from human recombinant delta opioid receptor expressed in rat Chem-1 (RBL) cell membranes incubated for 60 mins	B	8.88	pKi	1.32	nM	Ki	J Med Chem (2020) 63: 433-439 [PMID:31834797]
ChEMBL	Agonist activity at human DOR expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by EIA method	F	8.8	pIC50	1.6	nM	IC50	J Med Chem (2016) 59: 9255-9261 [PMID:27607020]
ChEMBL	Displacement of [3H]DADLE from human recombinant delta opioid receptor expressed in CHO cells measured after 120 mins by scintillation counting method	B	8.89	pIC50	1.3	nM	IC50	Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
ChEMBL	Agonist activity at human DOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay	F	9.52	pIC50	0.3	nM	IC50	Eur J Med Chem (2017) 126: 202-217 [PMID:27776274]
ChEMBL	Agonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay	F	6.9	pEC50	125.4	nM	EC50	J Med Chem (2023) 66: 17138-17154 [PMID:38095323]
ChEMBL	Agonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis	F	7.57	pEC50	26.92	nM	EC50	Eur J Med Chem (2016) 109: 276-286 [PMID:26785295]
ChEMBL	Agonist activity at human cloned delta opioid receptor assessed as stimulation of [35S]GTP-gamma-S binding	F	7.68	pEC50	21	nM	EC50	Bioorg Med Chem Lett (2007) 17: 2656-2660 [PMID:17350835]
ChEMBL	Agonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assay	F	7.77	pEC50	16.98	nM	EC50	Bioorg Med Chem (2016) 24: 1582-1588 [PMID:26944625]
ChEMBL	Agonist activity at human delta opioid receptor over-expressed in CHO cell membrane after 1 hr by [35S]GTPgammaS binding assay	F	7.88	pEC50	13.2	nM	EC50	Bioorg Med Chem Lett (2015) 25: 5532-5535 [PMID:26525865]
ChEMBL	Inverse agonist activity at human DOR expressed in CHO cell membranes by [35S]GTPgammaS binding assay	F	8.1	pEC50	8.01	nM	EC50	Bioorg Med Chem Lett (2015) 25: 2927-2930 [PMID:26048798]
ChEMBL	Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay	F	8.19	pEC50	6.4	nM	EC50	J Med Chem (2021) 64: 13394-13409 [PMID:34465090]
ChEMBL	Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay	F	8.34	pEC50	4.57	nM	EC50	J Med Chem (2021) 64: 13394-13409 [PMID:34465090]
ChEMBL	Agonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 2 hrs by scintillation counting method	F	8.36	pEC50	4.32	nM	EC50	Bioorg Med Chem (2022) 53: 116552-116552 [PMID:34894610]
ChEMBL	Agonist activity at human delta opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assay	F	8.6	pEC50	2.49	nM	EC50	Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839]
ChEMBL	Agonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay	B	9.92	pEC50	0.12	nM	EC50	ACS Med Chem Lett (2016) 7: 391-396 [PMID:27096047]
ChEMBL	Agonist activity at DOR (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 60 mins by liquid scintillation counting analysis	B	10	pEC50	0.1	nM	EC50	J Med Chem (2021) 64: 9458-9483 [PMID:34152138]
δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
GtoPdb	-	-	7.9	pKi	-	-	-	Mol Pharmacol (1994) 45: 330-4 [PMID:8114680]
ChEMBL	Agonist activity at DOR in CD1 mouse vas deferens assessed as inhibition of EFS-induced contractions incubated for 60 mins	B	6.9	pEC50	125.89	nM	EC50	Bioorg Med Chem (2016) 24: 2832-2842 [PMID:27234885]
ChEMBL	Agonist activity at mouse delta opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis	F	8	pEC50	10	nM	EC50	J Med Chem (2016) 59: 8381-8397 [PMID:27556704]
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
ChEMBL	Displacement of [3H]lleDelt2 from delta opioid receptor in Wistar rat brain membranes after 45 mins by liquid scintillation counting method	B	8.35	pKi	4.5	nM	Ki	ACS Med Chem Lett (2017) 8: 449-454 [PMID:28435535]
ChEMBL	Displacement of [3H]-DPDPE from rat delta 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]
ChEMBL	Agonist activity at rat delta 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	6.43	pEC50	368	nM	EC50	Bioorg Med Chem (2017) 25: 2406-2422 [PMID:28314512]
ChEMBL	Agonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method	F	8.84	pEC50	1.43	nM	EC50	Eur J Med Chem (2020) 189: 112070-112070 [PMID:31982651]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL	Displacement of [3H]diprenorphine from human cloned kappa opioid receptor	B	5	pKi	>10000	nM	Ki	Bioorg Med Chem Lett (2007) 17: 2656-2660 [PMID:17350835]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL	Displacement of [3H]diprenorphine from human cloned mu opioid receptor	B	5	pKi	>10000	nM	Ki	Bioorg Med Chem Lett (2007) 17: 2656-2660 [PMID:17350835]
ChEMBL	Agonist activity at human MOR expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by EIA method	F	8.8	pIC50	1.6	nM	IC50	J Med Chem (2016) 59: 9255-9261 [PMID:27607020]

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]