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 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 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 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 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 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 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]
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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]