GPCRdb

Ligand source activities (1 row/activity)

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Ligands (move mouse cursor over ligand name to see structure)					Receptor	Activity									Chemical information
Sel. page	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
	3826	178897	None	57	Human	Functional	pAC50	=	8.9	8.9	13182	2	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	255	3	1	3	2.3	O=C(c1ccccc1)c1ccc2n1CCC2C(=O)O	10.1038/s41467-023-40064-9
	CHEMBL469	178897	None	57	Human	Functional	pAC50	=	8.9	8.9	13182	2	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	255	3	1	3	2.3	O=C(c1ccccc1)c1ccc2n1CCC2C(=O)O	10.1038/s41467-023-40064-9
	319	1324	None	32	Human	Functional	pAC50	=	6	6.0	-794	18	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	426	7	1	3	4.0	NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2	10.1038/s41467-023-40064-9
	321	1324	None	32	Human	Functional	pAC50	=	6	6.0	-794	18	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	426	7	1	3	4.0	NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2	10.1038/s41467-023-40064-9
	444031	1324	None	32	Human	Functional	pAC50	=	6	6.0	-794	18	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	426	7	1	3	4.0	NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2	10.1038/s41467-023-40064-9
	444031.0	1324	None	32	Human	Functional	pAC50	=	6	6.0	-794	18	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	426	7	1	3	4.0	NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2	10.1038/s41467-023-40064-9
	784	1324	None	32	Human	Functional	pAC50	=	6	6.0	-794	18	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	426	7	1	3	4.0	NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2	10.1038/s41467-023-40064-9
	CHEMBL1346	1324	None	32	Human	Functional	pAC50	=	6	6.0	-794	18	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	426	7	1	3	4.0	NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2	10.1038/s41467-023-40064-9
	DB00496	1324	None	32	Human	Functional	pAC50	=	6	6.0	-794	18	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	426	7	1	3	4.0	NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2	10.1038/s41467-023-40064-9
	1353	1911	None	63	Human	Functional	pAC50	=	5.0	5.0	-676	39	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
	3559	1911	None	63	Human	Functional	pAC50	=	5.0	5.0	-676	39	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
	3559.0	1911	None	63	Human	Functional	pAC50	=	5.0	5.0	-676	39	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
	86	1911	None	63	Human	Functional	pAC50	=	5.0	5.0	-676	39	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
	CHEMBL54	1911	None	63	Human	Functional	pAC50	=	5.0	5.0	-676	39	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
	DB00502	1911	None	63	Human	Functional	pAC50	=	5.0	5.0	-676	39	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
	16351	102785	None	36	Human	Functional	pAC50	=	5.0	5.0	-562	17	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	343	0	0	4	4.1	CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1	10.1038/s41467-023-40064-9
	16351.0	102785	None	36	Human	Functional	pAC50	=	5.0	5.0	-562	17	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	343	0	0	4	4.1	CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1	10.1038/s41467-023-40064-9
	CHEMBL304902	102785	None	36	Human	Functional	pAC50	=	5.0	5.0	-562	17	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	343	0	0	4	4.1	CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1	10.1038/s41467-023-40064-9
	DB13256	102785	None	36	Human	Functional	pAC50	=	5.0	5.0	-562	17	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	343	0	0	4	4.1	CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1	10.1038/s41467-023-40064-9
	2318	154946	None	18	Human	Functional	pAC50	=	5.0	5.0	-19	15	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	351	7	1	3	4.1	CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL400599	154946	None	18	Human	Functional	pAC50	=	5.0	5.0	-19	15	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	351	7	1	3	4.1	CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1	10.1038/s41467-023-40064-9
	2165	206241	None	47	Human	Functional	pAC50	=	5.0	5.0	-7	8	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	355	6	2	4	5.2	CCN(CC)Cc1cc(Nc2ccnc3cc(Cl)ccc23)ccc1O	10.1038/s41467-023-40064-9
	3647519	206241	None	47	Human	Functional	pAC50	=	5.0	5.0	-7	8	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	355	6	2	4	5.2	CCN(CC)Cc1cc(Nc2ccnc3cc(Cl)ccc23)ccc1O	10.1038/s41467-023-40064-9
	CHEMBL682	206241	None	47	Human	Functional	pAC50	=	5.0	5.0	-7	8	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	355	6	2	4	5.2	CCN(CC)Cc1cc(Nc2ccnc3cc(Cl)ccc23)ccc1O	10.1038/s41467-023-40064-9
	1673	962	None	12	Human	Functional	pAC50	=	6.0	6.0	1	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	299	1	1	4	1.5	COc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@@H]4C=C[C@@H]1O)C	10.1038/s41467-023-40064-9
	5284371	962	None	12	Human	Functional	pAC50	=	6.0	6.0	1	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	299	1	1	4	1.5	COc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@@H]4C=C[C@@H]1O)C	10.1038/s41467-023-40064-9
	5284371.0	962	None	12	Human	Functional	pAC50	=	6.0	6.0	1	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	299	1	1	4	1.5	COc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@@H]4C=C[C@@H]1O)C	10.1038/s41467-023-40064-9
	725	962	None	12	Human	Functional	pAC50	=	6.0	6.0	1	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	299	1	1	4	1.5	COc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@@H]4C=C[C@@H]1O)C	10.1038/s41467-023-40064-9
	CHEMBL485	962	None	12	Human	Functional	pAC50	=	6.0	6.0	1	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	299	1	1	4	1.5	COc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@@H]4C=C[C@@H]1O)C	10.1038/s41467-023-40064-9
	DB00318	962	None	12	Human	Functional	pAC50	=	6.0	6.0	1	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	299	1	1	4	1.5	COc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@@H]4C=C[C@@H]1O)C	10.1038/s41467-023-40064-9
	31640	210407	None	7	Human	Functional	pAC50	=	5.9	5.9	16	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	352	2	0	2	4.1	O=C1CN=C(c2ccccc2)c2cc(Cl)ccc2N1CC(F)(F)F	10.1038/s41467-023-40064-9
	CHEMBL970	210407	None	7	Human	Functional	pAC50	=	5.9	5.9	16	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	352	2	0	2	4.1	O=C1CN=C(c2ccccc2)c2cc(Cl)ccc2N1CC(F)(F)F	10.1038/s41467-023-40064-9
	4528	98179	None	50	Human	Functional	pAC50	=	5.9	5.9	-34	5	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	238	1	1	2	2.8	CN1Cc2c(N)cccc2C(c2ccccc2)C1	10.1038/s41467-023-40064-9
	CHEMBL273575	98179	None	50	Human	Functional	pAC50	=	5.9	5.9	-34	5	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	238	1	1	2	2.8	CN1Cc2c(N)cccc2C(c2ccccc2)C1	10.1038/s41467-023-40064-9
	1690	3058	None	10	Human	Functional	pAC50	=	5.8	5.8	1	4	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	247	3	0	3	2.2	CCOC(=O)C1(CCN(CC1)C)c1ccccc1	10.1038/s41467-023-40064-9
	4058	3058	None	10	Human	Functional	pAC50	=	5.8	5.8	1	4	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	247	3	0	3	2.2	CCOC(=O)C1(CCN(CC1)C)c1ccccc1	10.1038/s41467-023-40064-9
	4058.0	3058	None	10	Human	Functional	pAC50	=	5.8	5.8	1	4	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	247	3	0	3	2.2	CCOC(=O)C1(CCN(CC1)C)c1ccccc1	10.1038/s41467-023-40064-9
	5750	3058	None	10	Human	Functional	pAC50	=	5.8	5.8	1	4	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	247	3	0	3	2.2	CCOC(=O)C1(CCN(CC1)C)c1ccccc1	10.1038/s41467-023-40064-9
	7221	3058	None	10	Human	Functional	pAC50	=	5.8	5.8	1	4	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	247	3	0	3	2.2	CCOC(=O)C1(CCN(CC1)C)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL607	3058	None	10	Human	Functional	pAC50	=	5.8	5.8	1	4	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	247	3	0	3	2.2	CCOC(=O)C1(CCN(CC1)C)c1ccccc1	10.1038/s41467-023-40064-9
	DB00454	3058	None	10	Human	Functional	pAC50	=	5.8	5.8	1	4	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	247	3	0	3	2.2	CCOC(=O)C1(CCN(CC1)C)c1ccccc1	10.1038/s41467-023-40064-9
	9417	133581	None	40	Human	Functional	pAC50	=	4.8	4.8	-208	15	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	363	6	1	4	3.3	OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1	10.1038/s41467-023-40064-9
	CHEMBL1524185	133581	None	40	Human	Functional	pAC50	=	4.8	4.8	-208	15	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	363	6	1	4	3.3	OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1	10.1038/s41467-023-40064-9
	CHEMBL370753	133581	None	40	Human	Functional	pAC50	=	4.8	4.8	-208	15	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	363	6	1	4	3.3	OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1	10.1038/s41467-023-40064-9
	4020	207608	None	20	Human	Functional	pAC50	=	4.8	4.8	-2	4	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	284	1	1	3	2.6	OC1(c2ccc(Cl)cc2)c2ccccc2C2=NCCN21	10.1038/s41467-023-40064-9
	CHEMBL781	207608	None	20	Human	Functional	pAC50	=	4.8	4.8	-2	4	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	284	1	1	3	2.6	OC1(c2ccc(Cl)cc2)c2ccccc2C2=NCCN21	10.1038/s41467-023-40064-9
	10100	15300	None	4	Human	Functional	pAC50	=	6.8	6.8	2	7	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	339	8	0	3	4.3	CCC(=O)O[C@](Cc1ccccc1)(c1ccccc1)[C@H](C)CN(C)C	10.1038/s41467-023-40064-9
	CHEMBL1213351	15300	None	4	Human	Functional	pAC50	=	6.8	6.8	2	7	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	339	8	0	3	4.3	CCC(=O)O[C@](Cc1ccccc1)(c1ccccc1)[C@H](C)CN(C)C	10.1038/s41467-023-40064-9
	2351	4301	None	35	Human	Functional	pAC50	=	4.8	4.8	-7	22	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	366	10	0	3	4.8	CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1	10.1038/s41467-023-40064-9
	CHEMBL1008	4301	None	35	Human	Functional	pAC50	=	4.8	4.8	-7	22	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	366	10	0	3	4.8	CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1	10.1038/s41467-023-40064-9
	CHEMBL1257078	4301	None	35	Human	Functional	pAC50	=	4.8	4.8	-7	22	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	366	10	0	3	4.8	CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1	10.1038/s41467-023-40064-9
	54841	205585	None	33	Human	Functional	pAC50	=	4.8	4.8	-10	11	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	255	6	1	2	3.7	CNCC[C@@H](Oc1ccccc1C)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL641	205585	None	33	Human	Functional	pAC50	=	4.8	4.8	-10	11	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	255	6	1	2	3.7	CNCC[C@@H](Oc1ccccc1C)c1ccccc1	10.1038/s41467-023-40064-9
	1385580	29284	None	49	Human	Functional	pAC50	=	5.8	5.8	-173	19	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	426	7	1	4	4.1	O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1	10.1038/s41467-023-40064-9
	4615	29284	None	49	Human	Functional	pAC50	=	5.8	5.8	-173	19	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	426	7	1	4	4.1	O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1	10.1038/s41467-023-40064-9
	4615.0	29284	None	49	Human	Functional	pAC50	=	5.8	5.8	-173	19	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	426	7	1	4	4.1	O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1	10.1038/s41467-023-40064-9
	CHEMBL13828	29284	None	49	Human	Functional	pAC50	=	5.8	5.8	-173	19	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	426	7	1	4	4.1	O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1	10.1038/s41467-023-40064-9
	DB12877	29284	None	49	Human	Functional	pAC50	=	5.8	5.8	-173	19	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	426	7	1	4	4.1	O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1	10.1038/s41467-023-40064-9
	2337	3256	None	51	Human	Functional	pAC50	=	5.7	5.7	-134	29	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	10.1038/s41467-023-40064-9
	50	3256	None	51	Human	Functional	pAC50	=	5.7	5.7	-134	29	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	10.1038/s41467-023-40064-9
	5002	3256	None	51	Human	Functional	pAC50	=	5.7	5.7	-134	29	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	10.1038/s41467-023-40064-9
	5002.0	3256	None	51	Human	Functional	pAC50	=	5.7	5.7	-134	29	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	10.1038/s41467-023-40064-9
	CHEMBL716	3256	None	51	Human	Functional	pAC50	=	5.7	5.7	-134	29	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	10.1038/s41467-023-40064-9
	DB01224	3256	None	51	Human	Functional	pAC50	=	5.7	5.7	-134	29	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	10.1038/s41467-023-40064-9
	156419	938	None	48	Human	Functional	pAC50	=	5.7	5.7	-51	20	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	357	6	1	1	6.1	C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F	10.1038/s41467-023-40064-9
	156419.0	938	None	48	Human	Functional	pAC50	=	5.7	5.7	-51	20	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	357	6	1	1	6.1	C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F	10.1038/s41467-023-40064-9
	3308	938	None	48	Human	Functional	pAC50	=	5.7	5.7	-51	20	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	357	6	1	1	6.1	C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F	10.1038/s41467-023-40064-9
	647	938	None	48	Human	Functional	pAC50	=	5.7	5.7	-51	20	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	357	6	1	1	6.1	C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F	10.1038/s41467-023-40064-9
	CHEMBL1201284	938	None	48	Human	Functional	pAC50	=	5.7	5.7	-51	20	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	357	6	1	1	6.1	C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F	10.1038/s41467-023-40064-9
	DB01012	938	None	48	Human	Functional	pAC50	=	5.7	5.7	-51	20	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	357	6	1	1	6.1	C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F	10.1038/s41467-023-40064-9
	5573	67602	None	59	Human	Functional	pAC50	=	6.7	6.7	-1	6	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	387	9	0	6	3.7	CCC(COC(=O)c1cc(OC)c(OC)c(OC)c1)(c1ccccc1)N(C)C	10.1038/s41467-023-40064-9
	5573.0	67602	None	59	Human	Functional	pAC50	=	6.7	6.7	-1	6	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	387	9	0	6	3.7	CCC(COC(=O)c1cc(OC)c(OC)c(OC)c1)(c1ccccc1)N(C)C	10.1038/s41467-023-40064-9
	CHEMBL1325297	67602	None	59	Human	Functional	pAC50	=	6.7	6.7	-1	6	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	387	9	0	6	3.7	CCC(COC(=O)c1cc(OC)c(OC)c(OC)c1)(c1ccccc1)N(C)C	10.1038/s41467-023-40064-9
	CHEMBL190044	67602	None	59	Human	Functional	pAC50	=	6.7	6.7	-1	6	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	387	9	0	6	3.7	CCC(COC(=O)c1cc(OC)c(OC)c(OC)c1)(c1ccccc1)N(C)C	10.1038/s41467-023-40064-9
	DB09089	67602	None	59	Human	Functional	pAC50	=	6.7	6.7	-1	6	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	387	9	0	6	3.7	CCC(COC(=O)c1cc(OC)c(OC)c(OC)c1)(c1ccccc1)N(C)C	10.1038/s41467-023-40064-9
	3151	1462	None	65	Human	Functional	pAC50	=	5.7	5.7	-1230	24	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	425	5	2	5	3.4	Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	3151.0	1462	None	65	Human	Functional	pAC50	=	5.7	5.7	-1230	24	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	425	5	2	5	3.4	Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	945	1462	None	65	Human	Functional	pAC50	=	5.7	5.7	-1230	24	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	425	5	2	5	3.4	Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	965	1462	None	65	Human	Functional	pAC50	=	5.7	5.7	-1230	24	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	425	5	2	5	3.4	Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	CHEMBL219916	1462	None	65	Human	Functional	pAC50	=	5.7	5.7	-1230	24	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	425	5	2	5	3.4	Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	DB01184	1462	None	65	Human	Functional	pAC50	=	5.7	5.7	-1230	24	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	425	5	2	5	3.4	Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	2448	99377	None	50	Human	Functional	pAC50	=	5.7	5.7	-91	15	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	419	6	1	3	4.5	O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1	10.1038/s41467-023-40064-9
	2448.0	99377	None	50	Human	Functional	pAC50	=	5.7	5.7	-91	15	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	419	6	1	3	4.5	O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1	10.1038/s41467-023-40064-9
	CHEMBL28218	99377	None	50	Human	Functional	pAC50	=	5.7	5.7	-91	15	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	419	6	1	3	4.5	O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1	10.1038/s41467-023-40064-9
	DB12401	99377	None	50	Human	Functional	pAC50	=	5.7	5.7	-91	15	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	419	6	1	3	4.5	O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1	10.1038/s41467-023-40064-9
	5284603	205871	None	8	Human	Functional	pAC50	=	6.6	6.6	-19	6	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	315	1	1	5	1.0	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(O)[C@@H](C2)N(C)CC[C@]314	10.1038/s41467-023-40064-9
	CHEMBL656	205871	None	8	Human	Functional	pAC50	=	6.6	6.6	-19	6	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	315	1	1	5	1.0	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(O)[C@@H](C2)N(C)CC[C@]314	10.1038/s41467-023-40064-9
	1224	1432	None	51	Human	Functional	pAC50	=	4.6	4.6	-4786	22	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1038/s41467-023-40064-9
	3100	1432	None	51	Human	Functional	pAC50	=	4.6	4.6	-4786	22	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1038/s41467-023-40064-9
	3100.0	1432	None	51	Human	Functional	pAC50	=	4.6	4.6	-4786	22	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1038/s41467-023-40064-9
	8980	1432	None	51	Human	Functional	pAC50	=	4.6	4.6	-4786	22	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1038/s41467-023-40064-9
	916	1432	None	51	Human	Functional	pAC50	=	4.6	4.6	-4786	22	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1038/s41467-023-40064-9
	CHEMBL657	1432	None	51	Human	Functional	pAC50	=	4.6	4.6	-4786	22	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1038/s41467-023-40064-9
	DB01075	1432	None	51	Human	Functional	pAC50	=	4.6	4.6	-4786	22	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1038/s41467-023-40064-9
	4418	34231	None	58	Human	Functional	pAC50	=	4.6	4.6	-89	18	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	392	7	1	5	3.4	COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1	10.1038/s41467-023-40064-9
	4418.0	34231	None	58	Human	Functional	pAC50	=	4.6	4.6	-89	18	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	392	7	1	5	3.4	COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1	10.1038/s41467-023-40064-9
	CHEMBL142635	34231	None	58	Human	Functional	pAC50	=	4.6	4.6	-89	18	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	392	7	1	5	3.4	COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1	10.1038/s41467-023-40064-9
	DB12092	34231	None	58	Human	Functional	pAC50	=	4.6	4.6	-89	18	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	392	7	1	5	3.4	COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1	10.1038/s41467-023-40064-9
	68870	19101	None	51	Human	Functional	pAC50	=	5.6	5.6	7	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	436	8	2	4	4.2	CN1c2ccccc2C(NCCCCCCC(=O)O)c2ccc(Cl)cc2S1(=O)=O	10.1038/s41467-023-40064-9
	68870.0	19101	None	51	Human	Functional	pAC50	=	5.6	5.6	7	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	436	8	2	4	4.2	CN1c2ccccc2C(NCCCCCCC(=O)O)c2ccc(Cl)cc2S1(=O)=O	10.1038/s41467-023-40064-9
	CHEMBL1289110	19101	None	51	Human	Functional	pAC50	=	5.6	5.6	7	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	436	8	2	4	4.2	CN1c2ccccc2C(NCCCCCCC(=O)O)c2ccc(Cl)cc2S1(=O)=O	10.1038/s41467-023-40064-9
	DB09289	19101	None	51	Human	Functional	pAC50	=	5.6	5.6	7	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	436	8	2	4	4.2	CN1c2ccccc2C(NCCCCCCC(=O)O)c2ccc(Cl)cc2S1(=O)=O	10.1038/s41467-023-40064-9
	2286	3183	None	36	Human	Functional	pAC50	=	5.6	5.6	-602	28	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
	4927	3183	None	36	Human	Functional	pAC50	=	5.6	5.6	-602	28	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
	4927.0	3183	None	36	Human	Functional	pAC50	=	5.6	5.6	-602	28	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
	7282	3183	None	36	Human	Functional	pAC50	=	5.6	5.6	-602	28	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
	CHEMBL643	3183	None	36	Human	Functional	pAC50	=	5.6	5.6	-602	28	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
	DB01069	3183	None	36	Human	Functional	pAC50	=	5.6	5.6	-602	28	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
	100	3805	None	44	Human	Functional	pAC50	=	5.6	5.6	-1071	38	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
	2637	3805	None	44	Human	Functional	pAC50	=	5.6	5.6	-1071	38	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
	5452	3805	None	44	Human	Functional	pAC50	=	5.6	5.6	-1071	38	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
	CHEMBL479	3805	None	44	Human	Functional	pAC50	=	5.6	5.6	-1071	38	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
	DB00679	3805	None	44	Human	Functional	pAC50	=	5.6	5.6	-1071	38	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
	1427	2013	None	42	Human	Functional	pAC50	=	4.6	4.6	-19498	30	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	357	2013	None	42	Human	Functional	pAC50	=	4.6	4.6	-19498	30	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	3696	2013	None	42	Human	Functional	pAC50	=	4.6	4.6	-19498	30	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	CHEMBL11	2013	None	42	Human	Functional	pAC50	=	4.6	4.6	-19498	30	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	DB00458	2013	None	42	Human	Functional	pAC50	=	4.6	4.6	-19498	30	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	4872633	104397	None	70	Human	Functional	pAC50	=	4.6	4.6	-	1	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	375	4	2	6	2.0	COc1c(N2CCNC(C)C2)c(F)cc2c(=O)c(C(=O)O)cn(C3CC3)c12	10.1038/s41467-023-40064-9
	5379	104397	None	70	Human	Functional	pAC50	=	4.6	4.6	-	1	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	375	4	2	6	2.0	COc1c(N2CCNC(C)C2)c(F)cc2c(=O)c(C(=O)O)cn(C3CC3)c12	10.1038/s41467-023-40064-9
	CHEMBL31	104397	None	70	Human	Functional	pAC50	=	4.6	4.6	-	1	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	375	4	2	6	2.0	COc1c(N2CCNC(C)C2)c(F)cc2c(=O)c(C(=O)O)cn(C3CC3)c12	10.1038/s41467-023-40064-9
	2284	3182	None	26	Human	Functional	pAC50	=	5.5	5.5	-524	34	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	10.1038/s41467-023-40064-9
	4926	3182	None	26	Human	Functional	pAC50	=	5.5	5.5	-524	34	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	10.1038/s41467-023-40064-9
	7281	3182	None	26	Human	Functional	pAC50	=	5.5	5.5	-524	34	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	10.1038/s41467-023-40064-9
	CHEMBL564	3182	None	26	Human	Functional	pAC50	=	5.5	5.5	-524	34	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	10.1038/s41467-023-40064-9
	DB00420	3182	None	26	Human	Functional	pAC50	=	5.5	5.5	-524	34	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	10.1038/s41467-023-40064-9
	5365247	138516	None	29	Human	Functional	pAC50	=	5.5	5.5	-53	10	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	316	4	0	2	3.8	CN(C)C/C=C(/c1ccc(Br)cc1)c1cccnc1	10.1038/s41467-023-40064-9
	CHEMBL37744	138516	None	29	Human	Functional	pAC50	=	5.5	5.5	-53	10	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	316	4	0	2	3.8	CN(C)C/C=C(/c1ccc(Br)cc1)c1cccnc1	10.1038/s41467-023-40064-9
	1574	2313	None	6	Human	Functional	pAC50	=	5.5	5.5	-6	5	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	257	0	1	2	3.1	Oc1ccc2c(c1)[C@]13CCCC[C@H]3[C@@H](C2)N(CC1)C	10.1038/s41467-023-40064-9
	5359272	2313	None	6	Human	Functional	pAC50	=	5.5	5.5	-6	5	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	257	0	1	2	3.1	Oc1ccc2c(c1)[C@]13CCCC[C@H]3[C@@H](C2)N(CC1)C	10.1038/s41467-023-40064-9
	5359272.0	2313	None	6	Human	Functional	pAC50	=	5.5	5.5	-6	5	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	257	0	1	2	3.1	Oc1ccc2c(c1)[C@]13CCCC[C@H]3[C@@H](C2)N(CC1)C	10.1038/s41467-023-40064-9
	7595	2313	None	6	Human	Functional	pAC50	=	5.5	5.5	-6	5	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	257	0	1	2	3.1	Oc1ccc2c(c1)[C@]13CCCC[C@H]3[C@@H](C2)N(CC1)C	10.1038/s41467-023-40064-9
	CHEMBL592	2313	None	6	Human	Functional	pAC50	=	5.5	5.5	-6	5	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	257	0	1	2	3.1	Oc1ccc2c(c1)[C@]13CCCC[C@H]3[C@@H](C2)N(CC1)C	10.1038/s41467-023-40064-9
	DB00854	2313	None	6	Human	Functional	pAC50	=	5.5	5.5	-6	5	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	257	0	1	2	3.1	Oc1ccc2c(c1)[C@]13CCCC[C@H]3[C@@H](C2)N(CC1)C	10.1038/s41467-023-40064-9
	118422671	2757	None	41	Human	Functional	pAC50	=	5.5	5.5	-1096	23	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	405	6	3	5	2.4	OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O	10.1038/s41467-023-40064-9
	1887	2757	None	41	Human	Functional	pAC50	=	5.5	5.5	-1096	23	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	405	6	3	5	2.4	OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O	10.1038/s41467-023-40064-9
	189562	2757	None	41	Human	Functional	pAC50	=	5.5	5.5	-1096	23	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	405	6	3	5	2.4	OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O	10.1038/s41467-023-40064-9
	189562.0	2757	None	41	Human	Functional	pAC50	=	5.5	5.5	-1096	23	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	405	6	3	5	2.4	OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O	10.1038/s41467-023-40064-9
	71301	2757	None	41	Human	Functional	pAC50	=	5.5	5.5	-1096	23	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	405	6	3	5	2.4	OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O	10.1038/s41467-023-40064-9
	71301.0	2757	None	41	Human	Functional	pAC50	=	5.5	5.5	-1096	23	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	405	6	3	5	2.4	OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O	10.1038/s41467-023-40064-9
	7246	2757	None	41	Human	Functional	pAC50	=	5.5	5.5	-1096	23	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	405	6	3	5	2.4	OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O	10.1038/s41467-023-40064-9
	9844194	2757	None	41	Human	Functional	pAC50	=	5.5	5.5	-1096	23	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	405	6	3	5	2.4	OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O	10.1038/s41467-023-40064-9
	9844194.0	2757	None	41	Human	Functional	pAC50	=	5.5	5.5	-1096	23	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	405	6	3	5	2.4	OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O	10.1038/s41467-023-40064-9
	CHEMBL2365658	2757	None	41	Human	Functional	pAC50	=	5.5	5.5	-1096	23	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	405	6	3	5	2.4	OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O	10.1038/s41467-023-40064-9
	CHEMBL3526436	2757	None	41	Human	Functional	pAC50	=	5.5	5.5	-1096	23	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	405	6	3	5	2.4	OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O	10.1038/s41467-023-40064-9
	CHEMBL434394	2757	None	41	Human	Functional	pAC50	=	5.5	5.5	-1096	23	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	405	6	3	5	2.4	OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O	10.1038/s41467-023-40064-9
	DB04861	2757	None	41	Human	Functional	pAC50	=	5.5	5.5	-1096	23	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	405	6	3	5	2.4	OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O	10.1038/s41467-023-40064-9
	3949	100668	None	35	Human	Functional	pAC50	=	5.5	5.5	-6	16	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	468	8	0	5	4.9	COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC	10.1038/s41467-023-40064-9
	CHEMBL29188	100668	None	35	Human	Functional	pAC50	=	5.5	5.5	-6	16	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	468	8	0	5	4.9	COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC	10.1038/s41467-023-40064-9
	1386	1954	None	8	Human	Functional	pAC50	=	6.5	6.5	3	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	299	1	0	4	1.9	COc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@@H]4CCC1=O)C	10.1038/s41467-023-40064-9
	5284569	1954	None	8	Human	Functional	pAC50	=	6.5	6.5	3	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	299	1	0	4	1.9	COc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@@H]4CCC1=O)C	10.1038/s41467-023-40064-9
	5284569.0	1954	None	8	Human	Functional	pAC50	=	6.5	6.5	3	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	299	1	0	4	1.9	COc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@@H]4CCC1=O)C	10.1038/s41467-023-40064-9
	7081	1954	None	8	Human	Functional	pAC50	=	6.5	6.5	3	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	299	1	0	4	1.9	COc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@@H]4CCC1=O)C	10.1038/s41467-023-40064-9
	CHEMBL1457	1954	None	8	Human	Functional	pAC50	=	6.5	6.5	3	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	299	1	0	4	1.9	COc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@@H]4CCC1=O)C	10.1038/s41467-023-40064-9
	DB00956	1954	None	8	Human	Functional	pAC50	=	6.5	6.5	3	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	299	1	0	4	1.9	COc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@@H]4CCC1=O)C	10.1038/s41467-023-40064-9
	4942	5720	None	27	Human	Functional	pAC50	=	5.4	5.4	-1	11	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	367	7	0	4	4.0	CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	4942.0	5720	None	27	Human	Functional	pAC50	=	5.4	5.4	-1	11	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	367	7	0	4	4.0	CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL1078261	5720	None	27	Human	Functional	pAC50	=	5.4	5.4	-1	11	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	367	7	0	4	4.0	CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	DB12278	5720	None	27	Human	Functional	pAC50	=	5.4	5.4	-1	11	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	367	7	0	4	4.0	CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	2583	3776	None	69	Human	Functional	pAC50	=	5.4	5.4	-2630	16	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	514	7	1	5	7.3	CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2	10.1038/s41467-023-40064-9
	592	3776	None	69	Human	Functional	pAC50	=	5.4	5.4	-2630	16	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	514	7	1	5	7.3	CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2	10.1038/s41467-023-40064-9
	65999	3776	None	69	Human	Functional	pAC50	=	5.4	5.4	-2630	16	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	514	7	1	5	7.3	CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2	10.1038/s41467-023-40064-9
	65999.0	3776	None	69	Human	Functional	pAC50	=	5.4	5.4	-2630	16	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	514	7	1	5	7.3	CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2	10.1038/s41467-023-40064-9
	CHEMBL1017	3776	None	69	Human	Functional	pAC50	=	5.4	5.4	-2630	16	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	514	7	1	5	7.3	CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2	10.1038/s41467-023-40064-9
	DB00966	3776	None	69	Human	Functional	pAC50	=	5.4	5.4	-2630	16	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	514	7	1	5	7.3	CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2	10.1038/s41467-023-40064-9
	4450	178333	None	41	Human	Functional	pAC50	=	5.4	5.4	-5	11	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	253	1	0	2	3.2	CN1CCOC(c2ccccc2)c2ccccc2C1	10.1038/s41467-023-40064-9
	CHEMBL465026	178333	None	41	Human	Functional	pAC50	=	5.4	5.4	-5	11	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	253	1	0	2	3.2	CN1CCOC(c2ccccc2)c2ccccc2C1	10.1038/s41467-023-40064-9
	129211	3749	None	48	Human	Functional	pAC50	=	5.4	5.4	-9772	14	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	408	11	2	6	2.3	CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C	10.1038/s41467-023-40064-9
	129211.0	3749	None	48	Human	Functional	pAC50	=	5.4	5.4	-9772	14	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	408	11	2	6	2.3	CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C	10.1038/s41467-023-40064-9
	2562	3749	None	48	Human	Functional	pAC50	=	5.4	5.4	-9772	14	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	408	11	2	6	2.3	CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C	10.1038/s41467-023-40064-9
	488	3749	None	48	Human	Functional	pAC50	=	5.4	5.4	-9772	14	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	408	11	2	6	2.3	CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C	10.1038/s41467-023-40064-9
	CHEMBL836	3749	None	48	Human	Functional	pAC50	=	5.4	5.4	-9772	14	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	408	11	2	6	2.3	CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C	10.1038/s41467-023-40064-9
	DB00706	3749	None	48	Human	Functional	pAC50	=	5.4	5.4	-9772	14	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	408	11	2	6	2.3	CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C	10.1038/s41467-023-40064-9
	16231	209968	None	39	Human	Functional	pAC50	=	5.4	5.4	-1	5	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	229	1	5	6	-1.1	N=C(N)NC(=O)c1nc(Cl)c(N)nc1N	10.1038/s41467-023-40064-9
	CHEMBL945	209968	None	39	Human	Functional	pAC50	=	5.4	5.4	-1	5	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	229	1	5	6	-1.1	N=C(N)NC(=O)c1nc(Cl)c(N)nc1N	10.1038/s41467-023-40064-9
	10831	117027	None	19	Human	Functional	pAC50	=	5.4	5.4	-3	6	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	397	7	2	5	4.3	O=C(Nc1ccccc1)OCC(CN1CCCCC1)OC(=O)Nc1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL338667	117027	None	19	Human	Functional	pAC50	=	5.4	5.4	-3	6	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	397	7	2	5	4.3	O=C(Nc1ccccc1)OCC(CN1CCCCC1)OC(=O)Nc1ccccc1	10.1038/s41467-023-40064-9
	146570	43468	None	43	Human	Functional	pAC50	=	5.4	5.4	-1	7	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	324	5	0	3	3.8	CN(C)CCC[C@@]1(c2ccc(F)cc2)OCc2cc(C#N)ccc21	10.1038/s41467-023-40064-9
	CHEMBL1508	43468	None	43	Human	Functional	pAC50	=	5.4	5.4	-1	7	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	324	5	0	3	3.8	CN(C)CCC[C@@]1(c2ccc(F)cc2)OCc2cc(C#N)ccc21	10.1038/s41467-023-40064-9
	3883	183641	None	69	Human	Functional	pAC50	=	5.4	5.4	-72	14	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	369	5	1	4	3.5	Cc1c(OCC(F)(F)F)ccnc1C[S+]([O-])c1nc2ccccc2[nH]1	10.1038/s41467-023-40064-9
	CHEMBL480	183641	None	69	Human	Functional	pAC50	=	5.4	5.4	-72	14	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	369	5	1	4	3.5	Cc1c(OCC(F)(F)F)ccnc1C[S+]([O-])c1nc2ccccc2[nH]1	10.1038/s41467-023-40064-9
	2131	57423	None	16	Human	Functional	pAC50	=	5.4	5.4	-6	7	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	536	14	2	2	4.6	CC[N+](CC)(CCNC(=O)C(=O)NCC[N+](CC)(CC)Cc1ccccc1Cl)Cc1ccccc1Cl	10.1038/s41467-023-40064-9
	CHEMBL1652	57423	None	16	Human	Functional	pAC50	=	5.4	5.4	-6	7	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	536	14	2	2	4.6	CC[N+](CC)(CCNC(=O)C(=O)NCC[N+](CC)(CC)Cc1ccccc1Cl)Cc1ccccc1Cl	10.1038/s41467-023-40064-9
	2726	919	None	48	Human	Functional	pAC50	=	5.3	5.3	-3890	42	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	2726.0	919	None	48	Human	Functional	pAC50	=	5.3	5.3	-3890	42	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	621	919	None	48	Human	Functional	pAC50	=	5.3	5.3	-3890	42	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	83	919	None	48	Human	Functional	pAC50	=	5.3	5.3	-3890	42	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	CHEMBL71	919	None	48	Human	Functional	pAC50	=	5.3	5.3	-3890	42	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	DB00477	919	None	48	Human	Functional	pAC50	=	5.3	5.3	-3890	42	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	2585	803	None	59	Human	Functional	pAC50	=	5.3	5.3	-3801	33	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
	2585.0	803	None	59	Human	Functional	pAC50	=	5.3	5.3	-3801	33	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
	522	803	None	59	Human	Functional	pAC50	=	5.3	5.3	-3801	33	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
	551	803	None	59	Human	Functional	pAC50	=	5.3	5.3	-3801	33	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
	CHEMBL723	803	None	59	Human	Functional	pAC50	=	5.3	5.3	-3801	33	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
	DB01136	803	None	59	Human	Functional	pAC50	=	5.3	5.3	-3801	33	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
	2247	505	None	55	Human	Functional	pAC50	=	6.3	6.3	-97	42	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1038/s41467-023-40064-9
	249	505	None	55	Human	Functional	pAC50	=	6.3	6.3	-97	42	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1038/s41467-023-40064-9
	2603	505	None	55	Human	Functional	pAC50	=	6.3	6.3	-97	42	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1038/s41467-023-40064-9
	CHEMBL296419	505	None	55	Human	Functional	pAC50	=	6.3	6.3	-97	42	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1038/s41467-023-40064-9
	DB00637	505	None	55	Human	Functional	pAC50	=	6.3	6.3	-97	42	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1038/s41467-023-40064-9
	1201549	597	None	17	Human	Functional	pAC50	=	5.3	5.3	-2884	26	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	1201549.0	597	None	17	Human	Functional	pAC50	=	5.3	5.3	-2884	26	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	333	597	None	17	Human	Functional	pAC50	=	5.3	5.3	-2884	26	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	7601	597	None	17	Human	Functional	pAC50	=	5.3	5.3	-2884	26	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL1201203	597	None	17	Human	Functional	pAC50	=	5.3	5.3	-2884	26	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL438151	597	None	17	Human	Functional	pAC50	=	5.3	5.3	-2884	26	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	DB00245	597	None	17	Human	Functional	pAC50	=	5.3	5.3	-2884	26	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	454	748	None	11	Human	Functional	pAC50	=	8.2	8.2	-1	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	327	2	2	3	3.4	Oc1ccc2c(c1)[C@]13CCCC[C@]3([C@@H](C2)N(CC1)CC1CCC1)O	10.1038/s41467-023-40064-9
	5361092	748	None	11	Human	Functional	pAC50	=	8.2	8.2	-1	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	327	2	2	3	3.4	Oc1ccc2c(c1)[C@]13CCCC[C@]3([C@@H](C2)N(CC1)CC1CCC1)O	10.1038/s41467-023-40064-9
	5361092.0	748	None	11	Human	Functional	pAC50	=	8.2	8.2	-1	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	327	2	2	3	3.4	Oc1ccc2c(c1)[C@]13CCCC[C@]3([C@@H](C2)N(CC1)CC1CCC1)O	10.1038/s41467-023-40064-9
	6916249	748	None	11	Human	Functional	pAC50	=	8.2	8.2	-1	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	327	2	2	3	3.4	Oc1ccc2c(c1)[C@]13CCCC[C@]3([C@@H](C2)N(CC1)CC1CCC1)O	10.1038/s41467-023-40064-9
	6916249.0	748	None	11	Human	Functional	pAC50	=	8.2	8.2	-1	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	327	2	2	3	3.4	Oc1ccc2c(c1)[C@]13CCCC[C@]3([C@@H](C2)N(CC1)CC1CCC1)O	10.1038/s41467-023-40064-9
	7591	748	None	11	Human	Functional	pAC50	=	8.2	8.2	-1	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	327	2	2	3	3.4	Oc1ccc2c(c1)[C@]13CCCC[C@]3([C@@H](C2)N(CC1)CC1CCC1)O	10.1038/s41467-023-40064-9
	CHEMBL33986	748	None	11	Human	Functional	pAC50	=	8.2	8.2	-1	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	327	2	2	3	3.4	Oc1ccc2c(c1)[C@]13CCCC[C@]3([C@@H](C2)N(CC1)CC1CCC1)O	10.1038/s41467-023-40064-9
	DB00611	748	None	11	Human	Functional	pAC50	=	8.2	8.2	-1	3	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	327	2	2	3	3.4	Oc1ccc2c(c1)[C@]13CCCC[C@]3([C@@H](C2)N(CC1)CC1CCC1)O	10.1038/s41467-023-40064-9
	68617	207985	None	33	Human	Functional	pAC50	=	5.2	5.2	-28	30	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	305	2	1	1	5.2	CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21	10.1038/s41467-023-40064-9
	CHEMBL1709	207985	None	33	Human	Functional	pAC50	=	5.2	5.2	-28	30	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	305	2	1	1	5.2	CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21	10.1038/s41467-023-40064-9
	CHEMBL809	207985	None	33	Human	Functional	pAC50	=	5.2	5.2	-28	30	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	305	2	1	1	5.2	CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21	10.1038/s41467-023-40064-9
	191	403	None	60	Human	Functional	pAC50	=	5.2	5.2	-1174	36	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	201	403	None	60	Human	Functional	pAC50	=	5.2	5.2	-1174	36	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	2170	403	None	60	Human	Functional	pAC50	=	5.2	5.2	-1174	36	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	2170.0	403	None	60	Human	Functional	pAC50	=	5.2	5.2	-1174	36	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	CHEMBL1113	403	None	60	Human	Functional	pAC50	=	5.2	5.2	-1174	36	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	DB00543	403	None	60	Human	Functional	pAC50	=	5.2	5.2	-1174	36	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	1890	2759	None	31	Human	Functional	pAC50	=	5.1	5.1	-41	28	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	469	10	0	7	3.6	CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl	10.1038/s41467-023-40064-9
	4449	2759	None	31	Human	Functional	pAC50	=	5.1	5.1	-41	28	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	469	10	0	7	3.6	CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl	10.1038/s41467-023-40064-9
	7247	2759	None	31	Human	Functional	pAC50	=	5.1	5.1	-41	28	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	469	10	0	7	3.6	CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl	10.1038/s41467-023-40064-9
	CHEMBL623	2759	None	31	Human	Functional	pAC50	=	5.1	5.1	-41	28	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	469	10	0	7	3.6	CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl	10.1038/s41467-023-40064-9
	DB01149	2759	None	31	Human	Functional	pAC50	=	5.1	5.1	-41	28	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	469	10	0	7	3.6	CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl	10.1038/s41467-023-40064-9
	31729	208242	None	9	Human	Functional	pAC50	=	5.1	5.1	-407	8	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	287	6	4	4	2.4	CC(NCCc1ccc(O)cc1)C(O)c1ccc(O)cc1	10.1038/s41467-023-40064-9
	CHEMBL83063	208242	None	9	Human	Functional	pAC50	=	5.1	5.1	-407	8	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	287	6	4	4	2.4	CC(NCCc1ccc(O)cc1)C(O)c1ccc(O)cc1	10.1038/s41467-023-40064-9
	146015366	210861	None	45	Human	Functional	pAC50	=	5.1	5.1	-1	2	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	319	9	5	4	0.5	CCCCCN(C)CCC(O)(P(=O)(O)O)P(=O)(O)O	10.1038/s41467-023-40064-9
	60852	210861	None	45	Human	Functional	pAC50	=	5.1	5.1	-1	2	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	319	9	5	4	0.5	CCCCCN(C)CCC(O)(P(=O)(O)O)P(=O)(O)O	10.1038/s41467-023-40064-9
	CHEMBL997	210861	None	45	Human	Functional	pAC50	=	5.1	5.1	-1	2	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	319	9	5	4	0.5	CCCCCN(C)CCC(O)(P(=O)(O)O)P(=O)(O)O	10.1038/s41467-023-40064-9
	2470	3653	None	40	Human	Functional	pAC50	=	6.0	6.0	-15488	23	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	3300	3653	None	40	Human	Functional	pAC50	=	6.0	6.0	-15488	23	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	5265	3653	None	40	Human	Functional	pAC50	=	6.0	6.0	-15488	23	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	99	3653	None	40	Human	Functional	pAC50	=	6.0	6.0	-15488	23	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL267930	3653	None	40	Human	Functional	pAC50	=	6.0	6.0	-15488	23	Agonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assayAgonist activity at human OPRM1 in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	145953986	161453	None	0	Rat	Functional	pEC50	=	10.9	10.9	11	4	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 assayAgonist 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	ChEMBL	484	11	6	6	0.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1016/j.bmcl.2018.05.015
	CHEMBL4126050	161453	None	0	Rat	Functional	pEC50	=	10.9	10.9	11	4	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 assayAgonist 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	ChEMBL	484	11	6	6	0.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1016/j.bmcl.2018.05.015
	145961883	161459	None	0	Rat	Functional	pEC50	=	10.9	10.9	38	4	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 assayAgonist 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	ChEMBL	594	16	9	7	-0.4	C=Cc1ccccc1C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(N)=O	10.1016/j.bmcl.2018.05.015
	CHEMBL4126102	161459	None	0	Rat	Functional	pEC50	=	10.9	10.9	38	4	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 assayAgonist 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	ChEMBL	594	16	9	7	-0.4	C=Cc1ccccc1C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(N)=O	10.1016/j.bmcl.2018.05.015
	155567284	176076	None	0	Human	Functional	pEC50	=	10.9	10.9	-	1	Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay	ChEMBL	410	7	1	5	3.4	CCC(=O)N(c1ccccc1)C1(C(=O)OC)CCN(CCc2cccc(O)c2)CC1	10.1021/acsmedchemlett.9b00404
	CHEMBL4588535	176076	None	0	Human	Functional	pEC50	=	10.9	10.9	-	1	Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay	ChEMBL	410	7	1	5	3.4	CCC(=O)N(c1ccccc1)C1(C(=O)OC)CCN(CCc2cccc(O)c2)CC1	10.1021/acsmedchemlett.9b00404
	162676173	183557	None	0	Human	Functional	pEC50	=	10.8	10.8	8	3	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL	337	4	2	3	3.5	Oc1cccc([C@@]23CCC[C@H]([C@H]2O)N(CCc2ccccc2)CC3)c1	10.1039/d0md00104j
	CHEMBL4798954	183557	None	0	Human	Functional	pEC50	=	10.8	10.8	8	3	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL	337	4	2	3	3.5	Oc1cccc([C@@]23CCC[C@H]([C@H]2O)N(CCc2ccccc2)CC3)c1	10.1039/d0md00104j
	155564874	175631	None	1	Human	Functional	pEC50	=	10.6	10.6	-	1	Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay	ChEMBL	410	7	1	5	3.4	CCC(=O)N(c1ccccc1)C1(C(=O)OC)CCN(CCc2ccc(O)cc2)CC1	10.1021/acsmedchemlett.9b00404
	CHEMBL4578287	175631	None	1	Human	Functional	pEC50	=	10.6	10.6	-	1	Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay	ChEMBL	410	7	1	5	3.4	CCC(=O)N(c1ccccc1)C1(C(=O)OC)CCN(CCc2ccc(O)cc2)CC1	10.1021/acsmedchemlett.9b00404
	168282272	191135	None	0	Human	Functional	pEC50	=	10.5	10.5	-	1	Agonist activity at human MOP stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human MOP stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation	ChEMBL	524	5	1	9	3.8	COC(=O)[C@@H]1C[C@H](OC(=O)c2ccc(CO)cc2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@]21C	10.1021/acs.jmedchem.0c01915
	CHEMBL5186887	191135	None	0	Human	Functional	pEC50	=	10.5	10.5	-	1	Agonist activity at human MOP stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human MOP stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation	ChEMBL	524	5	1	9	3.8	COC(=O)[C@@H]1C[C@H](OC(=O)c2ccc(CO)cc2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@]21C	10.1021/acs.jmedchem.0c01915
	60168107	81743	None	0	Human	Functional	pEC50	=	10.5	10.5	478	2	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL	612	12	6	7	2.0	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1	10.1021/jm300664y
	CHEMBL2163916	81743	None	0	Human	Functional	pEC50	=	10.5	10.5	478	2	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL	612	12	6	7	2.0	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1	10.1021/jm300664y
	60170775	81744	None	0	Human	Functional	pEC50	=	10.5	10.5	301	2	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL	612	12	6	7	2.0	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccoc1	10.1021/jm300664y
	CHEMBL2163917	81744	None	0	Human	Functional	pEC50	=	10.5	10.5	301	2	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL	612	12	6	7	2.0	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccoc1	10.1021/jm300664y
	71605418	87531	None	0	Human	Functional	pEC50	=	10.4	10.4	57	2	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 analysisAgonist 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	ChEMBL	622	12	6	6	2.2	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCN(C(=O)[C@@H](N)Cc2ccc(O)cc2)C1)c1ccccc1	10.1021/jm400195y
	CHEMBL2334770	87531	None	0	Human	Functional	pEC50	=	10.4	10.4	57	2	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 analysisAgonist 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	ChEMBL	622	12	6	6	2.2	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCN(C(=O)[C@@H](N)Cc2ccc(O)cc2)C1)c1ccccc1	10.1021/jm400195y
	3668	1561	None	36	Human	Functional	pEC50	=	10.4	10.4	1	5	Activity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assayActivity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay	ChEMBL		None	None	None		None	10.1021/jm060998u
	5311081	1561	None	36	Human	Functional	pEC50	=	10.4	10.4	1	5	Activity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assayActivity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay	ChEMBL		None	None	None		None	10.1021/jm060998u
	CHEMBL333357	1561	None	36	Human	Functional	pEC50	=	10.4	10.4	1	5	Activity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assayActivity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay	ChEMBL		None	None	None		None	10.1021/jm060998u
	CHEMBL589982	1561	None	36	Human	Functional	pEC50	=	10.4	10.4	1	5	Activity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assayActivity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay	ChEMBL		None	None	None		None	10.1021/jm060998u
	145961816	161705	None	0	Rat	Functional	pEC50	=	10.4	10.4	36	4	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 assayAgonist 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	ChEMBL	650	16	9	8	0.7	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1-c1ccsc1)C(=O)NCC(N)=O	10.1016/j.bmcl.2018.05.015
	CHEMBL4129689	161705	None	0	Rat	Functional	pEC50	=	10.4	10.4	36	4	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 assayAgonist 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	ChEMBL	650	16	9	8	0.7	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1-c1ccsc1)C(=O)NCC(N)=O	10.1016/j.bmcl.2018.05.015
	3668	1561	None	36	Human	Functional	pEC50	=	10.4	10.4	1	5	Antagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assayAntagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assay	ChEMBL		None	None	None		None	10.1016/j.bmcl.2008.01.009
	5311081	1561	None	36	Human	Functional	pEC50	=	10.4	10.4	1	5	Antagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assayAntagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assay	ChEMBL		None	None	None		None	10.1016/j.bmcl.2008.01.009
	CHEMBL333357	1561	None	36	Human	Functional	pEC50	=	10.4	10.4	1	5	Antagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assayAntagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assay	ChEMBL		None	None	None		None	10.1016/j.bmcl.2008.01.009
	CHEMBL589982	1561	None	36	Human	Functional	pEC50	=	10.4	10.4	1	5	Antagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assayAntagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assay	ChEMBL		None	None	None		None	10.1016/j.bmcl.2008.01.009
	71456262	79488	None	0	Human	Functional	pEC50	=	10.4	10.4	2	3	Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR	ChEMBL	448	3	1	4	3.5	CN1CC[C@]23c4c5cccc4O[C@H]2C(=O)CC[C@@]3(NC(=O)/C=C/c2ccccc2Cl)[C@H]1C5	10.1021/jm0604777
	CHEMBL2113666	79488	None	0	Human	Functional	pEC50	=	10.4	10.4	2	3	Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR	ChEMBL	448	3	1	4	3.5	CN1CC[C@]23c4c5cccc4O[C@H]2C(=O)CC[C@@]3(NC(=O)/C=C/c2ccccc2Cl)[C@H]1C5	10.1021/jm0604777
	11849285	204307	None	0	Human	Functional	pEC50	=	10.4	10.4	5	3	Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR	ChEMBL	444	3	2	5	2.9	Cc1ccccc1/C=C/C(=O)N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5	10.1021/jm0604777
	CHEMBL607125	204307	None	0	Human	Functional	pEC50	=	10.4	10.4	5	3	Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR	ChEMBL	444	3	2	5	2.9	Cc1ccccc1/C=C/C(=O)N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5	10.1021/jm0604777
	71605420	87529	None	0	Human	Functional	pEC50	=	10.2	10.2	85	2	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 analysisAgonist 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	ChEMBL	622	12	6	6	2.2	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CCN(C(=O)[C@@H](N)Cc2ccc(O)cc2)C1)c1ccccc1	10.1021/jm400195y
	CHEMBL2334768	87529	None	0	Human	Functional	pEC50	=	10.2	10.2	85	2	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 analysisAgonist 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	ChEMBL	622	12	6	6	2.2	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CCN(C(=O)[C@@H](N)Cc2ccc(O)cc2)C1)c1ccccc1	10.1021/jm400195y
	50994602	57239	None	0	Rat	Functional	pEC50	=	10.2	10.2	2	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	820	13	4	7	4.8	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	CHEMBL1649948	57239	None	0	Rat	Functional	pEC50	=	10.2	10.2	2	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	820	13	4	7	4.8	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	50994602	57239	None	0	Rat	Functional	pEC50	=	10.2	10.2	2	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	820	13	4	7	4.8	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	CHEMBL1649948	57239	None	0	Rat	Functional	pEC50	=	10.2	10.2	2	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	820	13	4	7	4.8	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	122194218	124049	None	0	Human	Functional	pEC50	=	10.2	10.2	-	1	Agonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production	ChEMBL	628	12	6	7	2.4	C=C(C(N)=O)[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1cccs1	10.1016/j.bmcl.2015.09.025
	CHEMBL3629337	124049	None	0	Human	Functional	pEC50	=	10.2	10.2	-	1	Agonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production	ChEMBL	628	12	6	7	2.4	C=C(C(N)=O)[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1cccs1	10.1016/j.bmcl.2015.09.025
	122194219	123957	None	0	Human	Functional	pEC50	=	10.2	10.2	-	1	Agonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production	ChEMBL	628	12	6	7	2.4	C=C(C(N)=O)[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccsc1	10.1016/j.bmcl.2015.09.025
	CHEMBL3627737	123957	None	0	Human	Functional	pEC50	=	10.2	10.2	-	1	Agonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production	ChEMBL	628	12	6	7	2.4	C=C(C(N)=O)[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccsc1	10.1016/j.bmcl.2015.09.025
	CHEMBL5074742	216816	None	0	Human	Functional	pEC50	=	10.2	10.2	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL		None	None	None		Fc1ccc([C@]2(CCNCc3scc4c3CCC4)CCOC3(CCOC3)C2)cc1	10.1016/j.ejmech.2021.113986
	CHEMBL2151734	211749	None	0	Human	Functional	pEC50	=	10.1	10.1	3	4	Agonist activity at human MOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation countingAgonist activity at human MOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation counting	ChEMBL		None	None	None		Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N(C)[C@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(C)CC(N)=O	10.1021/jm200894e
	54757387	65678	None	0	Human	Functional	pEC50	=	10.1	10.1	2	3	Agonist activity at human MOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation countingAgonist activity at human MOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation counting	ChEMBL	495	8	5	6	-0.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@H]1Cc2ccccc2CN(CC(N)=O)C1=O	10.1021/jm200894e
	CHEMBL1834247	65678	None	0	Human	Functional	pEC50	=	10.1	10.1	2	3	Agonist activity at human MOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation countingAgonist activity at human MOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation counting	ChEMBL	495	8	5	6	-0.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@H]1Cc2ccccc2CN(CC(N)=O)C1=O	10.1021/jm200894e
	25232542	187727	None	0	Human	Functional	pEC50	=	10.1	10.1	-	1	Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	497	4	3	6	3.3	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccccc2n1	10.1021/jm801272c
	CHEMBL494853	187727	None	0	Human	Functional	pEC50	=	10.1	10.1	-	1	Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	497	4	3	6	3.3	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccccc2n1	10.1021/jm801272c
	71605421	87530	None	0	Human	Functional	pEC50	=	10.0	10.0	52	2	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 analysisAgonist 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	ChEMBL	612	12	6	7	1.8	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CCN(C(=O)[C@@H](N)Cc2ccc(O)cc2)C1)c1ccco1	10.1021/jm400195y
	CHEMBL2334769	87530	None	0	Human	Functional	pEC50	=	10.0	10.0	52	2	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 analysisAgonist 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	ChEMBL	612	12	6	7	1.8	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CCN(C(=O)[C@@H](N)Cc2ccc(O)cc2)C1)c1ccco1	10.1021/jm400195y
	71625280	87921	None	0	Rat	Functional	pEC50	=	10.0	10.0	-3	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	493	6	2	5	4.9	CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338726	87921	None	0	Rat	Functional	pEC50	=	10.0	10.0	-3	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	493	6	2	5	4.9	CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	118731120	118240	None	0	Human	Functional	pEC50	=	10	10.0	-3	3	Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	594	13	8	7	-0.4	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(N)=O)C1=O	10.1021/acs.jmedchem.8b01282
	CHEMBL3408737	118240	None	0	Human	Functional	pEC50	=	10	10.0	-3	3	Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	594	13	8	7	-0.4	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(N)=O)C1=O	10.1021/acs.jmedchem.8b01282
	53233475	166916	None	0	Human	Functional	pEC50	=	10	10.0	-	1	Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	630	17	7	7	1.4	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.8b01282
	CHEMBL4284813	166916	None	0	Human	Functional	pEC50	=	10	10.0	-	1	Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	630	17	7	7	1.4	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.8b01282
	CHEMBL331325	213821	None	2	Human	Functional	pEC50	=	10	10.0	1	2	Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL		None	None	None		Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.8b01282
	CHEMBL412923	215494	None	0	Human	Functional	pEC50	=	10	10.0	-	1	Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL		None	None	None		Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.8b01282
	118731120	118240	None	0	Human	Functional	pEC50	=	10	10.0	-3	3	Agonist activity at human MOR stably expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by liquid scintillation counting assayAgonist activity at human MOR stably expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by liquid scintillation counting assay	ChEMBL	594	13	8	7	-0.4	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(N)=O)C1=O	10.1021/acs.jmedchem.0c01376
	CHEMBL3408737	118240	None	0	Human	Functional	pEC50	=	10	10.0	-3	3	Agonist activity at human MOR stably expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by liquid scintillation counting assayAgonist activity at human MOR stably expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by liquid scintillation counting assay	ChEMBL	594	13	8	7	-0.4	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(N)=O)C1=O	10.1021/acs.jmedchem.0c01376
	CHEMBL5082714	217310	None	0	Human	Functional	pEC50	=	10	10.0	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL		None	None	None		FC1(F)Cc2csc(CNCC[C@@]3(c4ccccn4)CCOC4(CCCC4)C3)c2C1	10.1016/j.ejmech.2021.113986
	145961895	161477	None	0	Rat	Functional	pEC50	=	10	10.0	5	4	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 assayAgonist 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	ChEMBL	622	16	9	7	0.4	CC(C)=Cc1ccccc1C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(N)=O	10.1016/j.bmcl.2018.05.015
	CHEMBL4126322	161477	None	0	Rat	Functional	pEC50	=	10	10.0	5	4	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 assayAgonist 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	ChEMBL	622	16	9	7	0.4	CC(C)=Cc1ccccc1C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(N)=O	10.1016/j.bmcl.2018.05.015
	9848990	189274	None	0	Human	Functional	pEC50	=	10.0	10.0	-3	7	Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1016/j.bmcl.2008.10.134
	9848990.0	189274	None	0	Human	Functional	pEC50	=	10.0	10.0	-3	7	Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1016/j.bmcl.2008.10.134
	CHEMBL2368861	189274	None	0	Human	Functional	pEC50	=	10.0	10.0	-3	7	Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1016/j.bmcl.2008.10.134
	CHEMBL511142	189274	None	0	Human	Functional	pEC50	=	10.0	10.0	-3	7	Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1016/j.bmcl.2008.10.134
	50994380	57229	None	0	Rat	Functional	pEC50	=	10.0	10.0	-1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	740	17	5	7	3.8	CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1	10.1021/jm100982d
	CHEMBL1649938	57229	None	0	Rat	Functional	pEC50	=	10.0	10.0	-1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	740	17	5	7	3.8	CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1	10.1021/jm100982d
	50994380	57229	None	0	Rat	Functional	pEC50	=	10.0	10.0	-1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	740	17	5	7	3.8	CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1	10.1021/jm100982d
	CHEMBL1649938	57229	None	0	Rat	Functional	pEC50	=	10.0	10.0	-1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	740	17	5	7	3.8	CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1	10.1021/jm100982d
	155545412	176694	None	0	Rat	Functional	pEC50	=	9.9	9.9	371	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	562	7	3	6	3.5	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(CN3CCc4ccccc4C3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4548498	176694	None	0	Rat	Functional	pEC50	=	9.9	9.9	371	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	562	7	3	6	3.5	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(CN3CCc4ccccc4C3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4597549	176694	None	0	Rat	Functional	pEC50	=	9.9	9.9	371	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	562	7	3	6	3.5	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(CN3CCc4ccccc4C3)cc21	10.1021/acs.jmedchem.9b00378
	145961040	161489	None	0	Rat	Functional	pEC50	=	9.9	9.9	2	4	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 assayAgonist 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	ChEMBL	559	12	6	6	1.4	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1-c1ccccc1)C(=O)NCC(N)=O	10.1016/j.bmcl.2018.05.015
	CHEMBL4126470	161489	None	0	Rat	Functional	pEC50	=	9.9	9.9	2	4	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 assayAgonist 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	ChEMBL	559	12	6	6	1.4	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1-c1ccccc1)C(=O)NCC(N)=O	10.1016/j.bmcl.2018.05.015
	145961135	161662	None	0	Rat	Functional	pEC50	=	9.9	9.9	-1	4	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 assayAgonist 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	ChEMBL	636	15	9	7	-0.0	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(C(F)(F)F)cc1)C(=O)NCC(N)=O	10.1016/j.bmcl.2018.05.015
	CHEMBL4128945	161662	None	0	Rat	Functional	pEC50	=	9.9	9.9	-1	4	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 assayAgonist 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	ChEMBL	636	15	9	7	-0.0	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(C(F)(F)F)cc1)C(=O)NCC(N)=O	10.1016/j.bmcl.2018.05.015
	71625279	87920	None	0	Rat	Functional	pEC50	=	9.9	9.9	-	1	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	479	5	2	5	4.6	CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)C1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338725	87920	None	0	Rat	Functional	pEC50	=	9.9	9.9	-	1	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	479	5	2	5	4.6	CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)C1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	137657725	159708	None	0	Human	Functional	pEC50	=	9.9	9.9	-	1	Agonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	377	3	1	4	3.8	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2CCC[C@@]3(OCc2ccccc2)[C@H]1C5	10.1021/acs.jmedchem.7b01363
	CHEMBL4103328	159708	None	0	Human	Functional	pEC50	=	9.9	9.9	-	1	Agonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	377	3	1	4	3.8	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2CCC[C@@]3(OCc2ccccc2)[C@H]1C5	10.1021/acs.jmedchem.7b01363
	50994459	57232	None	0	Rat	Functional	pEC50	=	9.9	9.9	-1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	774	17	5	7	4.5	CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1	10.1021/jm100982d
	CHEMBL1649941	57232	None	0	Rat	Functional	pEC50	=	9.9	9.9	-1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	774	17	5	7	4.5	CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1	10.1021/jm100982d
	50994459	57232	None	0	Rat	Functional	pEC50	=	9.9	9.9	-1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	774	17	5	7	4.5	CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1	10.1021/jm100982d
	CHEMBL1649941	57232	None	0	Rat	Functional	pEC50	=	9.9	9.9	-1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	774	17	5	7	4.5	CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1	10.1021/jm100982d
	58443234	84208	None	0	Human	Functional	pEC50	=	9.8	9.8	-3	3	Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	522	7	1	4	6.0	CC1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccc6c(c5)OCO6)cc4)cc3C1(C)CCN2CC1CC1	10.1016/j.bmcl.2012.10.081
	CHEMBL2208351	84208	None	0	Human	Functional	pEC50	=	9.8	9.8	-3	3	Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	522	7	1	4	6.0	CC1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccc6c(c5)OCO6)cc4)cc3C1(C)CCN2CC1CC1	10.1016/j.bmcl.2012.10.081
	1639	2726	None	32	Mouse	Functional	pEC50	=	9.8	9.8	-3	9	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1016/j.bmcl.2013.07.043
	1765	2726	None	32	Mouse	Functional	pEC50	=	9.8	9.8	-3	9	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1016/j.bmcl.2013.07.043
	5360515	2726	None	32	Mouse	Functional	pEC50	=	9.8	9.8	-3	9	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1016/j.bmcl.2013.07.043
	5360515.0	2726	None	32	Mouse	Functional	pEC50	=	9.8	9.8	-3	9	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1016/j.bmcl.2013.07.043
	CHEMBL19019	2726	None	32	Mouse	Functional	pEC50	=	9.8	9.8	-3	9	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1016/j.bmcl.2013.07.043
	DB00704	2726	None	32	Mouse	Functional	pEC50	=	9.8	9.8	-3	9	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1016/j.bmcl.2013.07.043
	60170609	81749	None	0	Human	Functional	pEC50	=	9.8	9.8	47	2	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL	622	12	6	6	2.4	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccccc1	10.1021/jm300664y
	CHEMBL2163921	81749	None	0	Human	Functional	pEC50	=	9.8	9.8	47	2	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL	622	12	6	6	2.4	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccccc1	10.1021/jm300664y
	71625152	87916	None	0	Rat	Functional	pEC50	=	9.8	9.8	-	1	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	467	7	2	5	4.4	CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CCC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338721	87916	None	0	Rat	Functional	pEC50	=	9.8	9.8	-	1	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	467	7	2	5	4.4	CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CCC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	71625277	87918	None	0	Rat	Functional	pEC50	=	9.8	9.8	-	1	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	479	6	2	5	4.6	CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CC1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338723	87918	None	0	Rat	Functional	pEC50	=	9.8	9.8	-	1	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	479	6	2	5	4.6	CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CC1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	71625278	87919	None	0	Rat	Functional	pEC50	=	9.8	9.8	-	1	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	493	7	2	5	4.9	CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CCC1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338724	87919	None	0	Rat	Functional	pEC50	=	9.8	9.8	-	1	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	493	7	2	5	4.9	CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CCC1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	1639	2726	None	32	Mouse	Functional	pEC50	=	9.8	9.8	-3	9	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1016/j.bmc.2015.02.055
	1765	2726	None	32	Mouse	Functional	pEC50	=	9.8	9.8	-3	9	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1016/j.bmc.2015.02.055
	5360515	2726	None	32	Mouse	Functional	pEC50	=	9.8	9.8	-3	9	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1016/j.bmc.2015.02.055
	5360515.0	2726	None	32	Mouse	Functional	pEC50	=	9.8	9.8	-3	9	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1016/j.bmc.2015.02.055
	CHEMBL19019	2726	None	32	Mouse	Functional	pEC50	=	9.8	9.8	-3	9	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1016/j.bmc.2015.02.055
	DB00704	2726	None	32	Mouse	Functional	pEC50	=	9.8	9.8	-3	9	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1016/j.bmc.2015.02.055
	25259490	174005	None	0	Rat	Functional	pEC50	=	9.7	9.7	-1	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	517	6	3	7	3.1	O=C(/C=C/c1cccc([N+](=O)[O-])c1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/jm8015552
	CHEMBL454018	174005	None	0	Rat	Functional	pEC50	=	9.7	9.7	-1	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	517	6	3	7	3.1	O=C(/C=C/c1cccc([N+](=O)[O-])c1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/jm8015552
	44323614	168110	None	0	Rat	Functional	pEC50	=	9.7	9.7	-	1	Compound was tested for its ability to stimulate [35S]GTP-gamma-S, binding to membranes from C6 glioma cells stably expressing rat mu opioid receptor.Compound was tested for its ability to stimulate [35S]GTP-gamma-S, binding to membranes from C6 glioma cells stably expressing rat mu opioid receptor.	ChEMBL	429	6	4	4	4.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NC1CCNc2ccc(Cc3ccccc3)cc21	10.1016/s0960-894x(98)00472-7
	CHEMBL432045	168110	None	0	Rat	Functional	pEC50	=	9.7	9.7	-	1	Compound was tested for its ability to stimulate [35S]GTP-gamma-S, binding to membranes from C6 glioma cells stably expressing rat mu opioid receptor.Compound was tested for its ability to stimulate [35S]GTP-gamma-S, binding to membranes from C6 glioma cells stably expressing rat mu opioid receptor.	ChEMBL	429	6	4	4	4.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NC1CCNc2ccc(Cc3ccccc3)cc21	10.1016/s0960-894x(98)00472-7
	145984911	166493	None	0	Human	Functional	pEC50	=	9.7	9.7	-	1	Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	658	17	9	7	0.6	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.8b01282
	CHEMBL4276875	166493	None	0	Human	Functional	pEC50	=	9.7	9.7	-	1	Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	658	17	9	7	0.6	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.8b01282
	71624447	87941	None	0	Rat	Functional	pEC50	=	9.7	9.7	-2	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	481	7	2	5	4.8	CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CCC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338745	87941	None	0	Rat	Functional	pEC50	=	9.7	9.7	-2	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	481	7	2	5	4.8	CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CCC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	155559128	176351	None	0	Mouse	Functional	pEC50	=	9.7	9.7	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2sccc2c1	10.1021/acs.jmedchem.9b01767
	CHEMBL4562210	176351	None	0	Mouse	Functional	pEC50	=	9.7	9.7	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2sccc2c1	10.1021/acs.jmedchem.9b01767
	CHEMBL4594861	176351	None	0	Mouse	Functional	pEC50	=	9.7	9.7	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2sccc2c1	10.1021/acs.jmedchem.9b01767
	155548948	174330	None	1	Human	Functional	pEC50	=	9.7	9.7	-	1	Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay	ChEMBL	408	7	0	5	3.3	CCC(=O)N(c1ccccc1)C1(C(=O)OC)CCN(CC(=O)c2ccccc2)CC1	10.1021/acsmedchemlett.9b00404
	CHEMBL4548662	174330	None	1	Human	Functional	pEC50	=	9.7	9.7	-	1	Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay	ChEMBL	408	7	0	5	3.3	CCC(=O)N(c1ccccc1)C1(C(=O)OC)CCN(CC(=O)c2ccccc2)CC1	10.1021/acsmedchemlett.9b00404
	118562375	169696	None	0	Human	Functional	pEC50	=	9.7	9.7	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	392	5	0	3	4.2	CC(C)C1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccc2)C1=O	10.1021/acs.jmedchem.9b01256
	CHEMBL4436170	169696	None	0	Human	Functional	pEC50	=	9.7	9.7	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	392	5	0	3	4.2	CC(C)C1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccc2)C1=O	10.1021/acs.jmedchem.9b01256
	11956520	120629	None	0	Human	Functional	pEC50	=	9.7	9.7	6	2	Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	359	2	2	2	4.5	CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)NCCc1c3ccccc3[nH]c12	10.1021/ml500117c
	CHEMBL3326228	120629	None	0	Human	Functional	pEC50	=	9.7	9.7	6	2	Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	359	2	2	2	4.5	CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)NCCc1c3ccccc3[nH]c12	10.1021/ml500117c
	CHEMBL3545629	120629	None	0	Human	Functional	pEC50	=	9.7	9.7	6	2	Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	359	2	2	2	4.5	CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)NCCc1c3ccccc3[nH]c12	10.1021/ml500117c
	CHEMBL5084800	217424	None	0	Human	Functional	pEC50	=	9.7	9.7	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL		None	None	None		Fc1ccc([C@]2(CCNCc3scc4c3CCCC4)CCO[C@]3(CCOC3)C2)nc1	10.1016/j.ejmech.2021.113986
	CHEMBL2387215	212863	None	0	Rat	Functional	pEC50	=	9.7	9.7	1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL		None	None	None		Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)NCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCNC(=O)NCCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)C(=O)O	10.1016/j.bmcl.2013.03.065
	71625281	87922	None	0	Rat	Functional	pEC50	=	9.7	9.7	-4	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	507	7	2	5	5.3	CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CCC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338727	87922	None	0	Rat	Functional	pEC50	=	9.7	9.7	-4	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	507	7	2	5	5.3	CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CCC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	1647	1313	None	34	Human	Functional	pEC50	=	9.7	9.7	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1016/j.ejmech.2022.114728
	5462471	1313	None	34	Human	Functional	pEC50	=	9.7	9.7	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1016/j.ejmech.2022.114728
	CHEMBL113995	1313	None	34	Human	Functional	pEC50	=	9.7	9.7	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1016/j.ejmech.2022.114728
	CHEMBL38874	1313	None	34	Human	Functional	pEC50	=	9.7	9.7	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1016/j.ejmech.2022.114728
	155517331	176352	None	0	Mouse	Functional	pEC50	=	9.7	9.7	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccsc2c1	10.1021/acs.jmedchem.9b01767
	CHEMBL4444746	176352	None	0	Mouse	Functional	pEC50	=	9.7	9.7	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccsc2c1	10.1021/acs.jmedchem.9b01767
	CHEMBL4594862	176352	None	0	Mouse	Functional	pEC50	=	9.7	9.7	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccsc2c1	10.1021/acs.jmedchem.9b01767
	122179053	121461	None	0	Rat	Functional	pEC50	=	9.7	9.7	33	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	503	5	2	5	4.7	CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccc(F)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/acs.jmedchem.5b00130
	CHEMBL3581743	121461	None	0	Rat	Functional	pEC50	=	9.7	9.7	33	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	503	5	2	5	4.7	CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccc(F)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/acs.jmedchem.5b00130
	24873473	84214	None	0	Human	Functional	pEC50	=	9.7	9.7	-1	3	Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	508	8	1	3	6.3	COc1cccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)c1	10.1016/j.bmcl.2012.10.081
	CHEMBL2208358	84214	None	0	Human	Functional	pEC50	=	9.7	9.7	-1	3	Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	508	8	1	3	6.3	COc1cccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)c1	10.1016/j.bmcl.2012.10.081
	164616054	188620	None	0	Mouse	Functional	pEC50	=	9.7	9.7	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based scintillation counting method	ChEMBL	483	4	4	5	3.0	O=C(N[C@@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2ccccc12	10.1016/j.bmcl.2021.127953
	CHEMBL4860525	188620	None	0	Mouse	Functional	pEC50	=	9.7	9.7	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based scintillation counting method	ChEMBL	483	4	4	5	3.0	O=C(N[C@@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2ccccc12	10.1016/j.bmcl.2021.127953
	CHEMBL5028355	188620	None	0	Mouse	Functional	pEC50	=	9.7	9.7	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based scintillation counting method	ChEMBL	483	4	4	5	3.0	O=C(N[C@@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2ccccc12	10.1016/j.bmcl.2021.127953
	172439036	195311	None	0	Human	Functional	pEC50	=	9.6	9.6	-17	3	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 assayAgonist 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	ChEMBL	338	5	1	3	4.2	Cc1ccc(C(CNC(=O)c2cc3ccccc3s2)N(C)C)cc1	10.1016/j.ejmech.2022.114728
	CHEMBL5400535	195311	None	0	Human	Functional	pEC50	=	9.6	9.6	-17	3	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 assayAgonist 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	ChEMBL	338	5	1	3	4.2	Cc1ccc(C(CNC(=O)c2cc3ccccc3s2)N(C)C)cc1	10.1016/j.ejmech.2022.114728
	155542413	176400	None	0	Rat	Functional	pEC50	=	9.6	9.6	52	3	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	507	7	3	5	3.5	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3ccccc3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4521319	176400	None	0	Rat	Functional	pEC50	=	9.6	9.6	52	3	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	507	7	3	5	3.5	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3ccccc3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4595172	176400	None	0	Rat	Functional	pEC50	=	9.6	9.6	52	3	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	507	7	3	5	3.5	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3ccccc3)cc21	10.1021/acs.jmedchem.9b00378
	155567469	176664	None	0	Rat	Functional	pEC50	=	9.6	9.6	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	557	7	3	5	4.7	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3ccc4ccccc4c3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4588807	176664	None	0	Rat	Functional	pEC50	=	9.6	9.6	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	557	7	3	5	4.7	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3ccc4ccccc4c3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4597299	176664	None	0	Rat	Functional	pEC50	=	9.6	9.6	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	557	7	3	5	4.7	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3ccc4ccccc4c3)cc21	10.1021/acs.jmedchem.9b00378
	71625394	87923	None	0	Rat	Functional	pEC50	=	9.6	9.6	-3	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	487	6	2	5	4.2	CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)Cc1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338728	87923	None	0	Rat	Functional	pEC50	=	9.6	9.6	-3	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	487	6	2	5	4.2	CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)Cc1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	162649449	180159	None	0	Human	Functional	pEC50	=	9.6	9.6	21	3	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL	421	8	1	4	5.1	CCOC(=O)CC[C@H]1[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1	10.1039/d0md00104j
	CHEMBL4747769	180159	None	0	Human	Functional	pEC50	=	9.6	9.6	21	3	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL	421	8	1	4	5.1	CCOC(=O)CC[C@H]1[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1	10.1039/d0md00104j
	71583725	86880	None	0	Rat	Functional	pEC50	=	9.6	9.6	281	2	Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	469	6	4	4	4.5	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(CC3Cc4ccccc4C3)cc21	10.1021/jm400050y
	CHEMBL2322563	86880	None	0	Rat	Functional	pEC50	=	9.6	9.6	281	2	Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	469	6	4	4	4.5	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(CC3Cc4ccccc4C3)cc21	10.1021/jm400050y
	71230156	121460	None	0	Rat	Functional	pEC50	=	9.6	9.6	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	499	5	2	5	4.8	CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccc(C)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/acs.jmedchem.5b00130
	CHEMBL3581742	121460	None	0	Rat	Functional	pEC50	=	9.6	9.6	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	499	5	2	5	4.8	CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccc(C)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/acs.jmedchem.5b00130
	71583725	86880	None	0	Rat	Functional	pEC50	=	9.6	9.6	281	2	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	469	6	4	4	4.5	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(CC3Cc4ccccc4C3)cc21	10.1021/acs.jmedchem.5b01270
	CHEMBL2322563	86880	None	0	Rat	Functional	pEC50	=	9.6	9.6	281	2	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	469	6	4	4	4.5	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(CC3Cc4ccccc4C3)cc21	10.1021/acs.jmedchem.5b01270
	118709689	113551	None	0	Mouse	Functional	pEC50	=	9.6	9.6	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2s1	10.1021/acs.jmedchem.9b01767
	CHEMBL3319616	113551	None	0	Mouse	Functional	pEC50	=	9.6	9.6	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2s1	10.1021/acs.jmedchem.9b01767
	CHEMBL4458688	113551	None	0	Mouse	Functional	pEC50	=	9.6	9.6	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2s1	10.1021/acs.jmedchem.9b01767
	71449133	79170	None	0	Human	Functional	pEC50	=	9.6	9.6	-	1	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	500	5	2	5	4.0	CO[C@@]12CC[C@@]3(C[C@@H]1CNC(=O)/C=C/c1ccccc1C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1021/jm070255o
	CHEMBL2113304	79170	None	0	Human	Functional	pEC50	=	9.6	9.6	-	1	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	500	5	2	5	4.0	CO[C@@]12CC[C@@]3(C[C@@H]1CNC(=O)/C=C/c1ccccc1C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1021/jm070255o
	155535194	176420	None	0	Rat	Functional	pEC50	=	9.6	9.6	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	558	7	3	6	4.0	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3cnc4ccccc4c3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4471560	176420	None	0	Rat	Functional	pEC50	=	9.6	9.6	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	558	7	3	6	4.0	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3cnc4ccccc4c3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4595286	176420	None	0	Rat	Functional	pEC50	=	9.6	9.6	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	558	7	3	6	4.0	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3cnc4ccccc4c3)cc21	10.1021/acs.jmedchem.9b00378
	1647	1313	None	34	Rat	Functional	pEC50	=	9.6	9.6	-5	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1016/j.bmcl.2018.05.015
	5462471	1313	None	34	Rat	Functional	pEC50	=	9.6	9.6	-5	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1016/j.bmcl.2018.05.015
	CHEMBL113995	1313	None	34	Rat	Functional	pEC50	=	9.6	9.6	-5	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1016/j.bmcl.2018.05.015
	CHEMBL38874	1313	None	34	Rat	Functional	pEC50	=	9.6	9.6	-5	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1016/j.bmcl.2018.05.015
	71625026	87937	None	0	Rat	Functional	pEC50	=	9.6	9.6	-4	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	479	5	2	5	4.6	CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)C1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338741	87937	None	0	Rat	Functional	pEC50	=	9.6	9.6	-4	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	479	5	2	5	4.6	CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)C1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	25233083	192771	None	0	Human	Functional	pEC50	=	9.6	9.6	-	1	Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	497	4	3	6	3.3	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2cn1	10.1021/jm801272c
	CHEMBL521854	192771	None	0	Human	Functional	pEC50	=	9.6	9.6	-	1	Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	497	4	3	6	3.3	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2cn1	10.1021/jm801272c
	9848990	189274	None	0	Rat	Functional	pEC50	=	9.6	9.6	2	7	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	9848990.0	189274	None	0	Rat	Functional	pEC50	=	9.6	9.6	2	7	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2368861	189274	None	0	Rat	Functional	pEC50	=	9.6	9.6	2	7	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL511142	189274	None	0	Rat	Functional	pEC50	=	9.6	9.6	2	7	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	145992101	167126	None	0	Human	Functional	pEC50	=	9.6	9.6	-	1	Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	787	22	11	9	-0.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)O	10.1021/acs.jmedchem.8b01282
	CHEMBL4288649	167126	None	0	Human	Functional	pEC50	=	9.6	9.6	-	1	Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	787	22	11	9	-0.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)O	10.1021/acs.jmedchem.8b01282
	155520187	173341	None	1	Human	Functional	pEC50	=	9.6	9.6	-	1	Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay	ChEMBL	410	8	1	5	2.7	COC(=O)C1(N(C(=O)CCO)c2ccccc2)CCN(CCc2ccccc2)CC1	10.1021/acsmedchemlett.9b00404
	CHEMBL4524446	173341	None	1	Human	Functional	pEC50	=	9.6	9.6	-	1	Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay	ChEMBL	410	8	1	5	2.7	COC(=O)C1(N(C(=O)CCO)c2ccccc2)CCN(CCc2ccccc2)CC1	10.1021/acsmedchemlett.9b00404
	50994460	57233	None	0	Rat	Functional	pEC50	=	9.5	9.5	1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	758	17	5	7	4.0	CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1	10.1021/jm100982d
	CHEMBL1649942	57233	None	0	Rat	Functional	pEC50	=	9.5	9.5	1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	758	17	5	7	4.0	CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1	10.1021/jm100982d
	71625393	87917	None	0	Rat	Functional	pEC50	=	9.5	9.5	-14	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	465	5	2	5	4.2	CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)C1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338722	87917	None	0	Rat	Functional	pEC50	=	9.5	9.5	-14	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	465	5	2	5	4.2	CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)C1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	50994460	57233	None	0	Rat	Functional	pEC50	=	9.5	9.5	1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	758	17	5	7	4.0	CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1	10.1021/jm100982d
	CHEMBL1649942	57233	None	0	Rat	Functional	pEC50	=	9.5	9.5	1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	758	17	5	7	4.0	CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1	10.1021/jm100982d
	1647	1313	None	34	Human	Functional	pEC50	=	9.5	9.5	-3	9	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL		None	None	None		None	10.1039/d0md00104j
	5462471	1313	None	34	Human	Functional	pEC50	=	9.5	9.5	-3	9	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL		None	None	None		None	10.1039/d0md00104j
	CHEMBL113995	1313	None	34	Human	Functional	pEC50	=	9.5	9.5	-3	9	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL		None	None	None		None	10.1039/d0md00104j
	CHEMBL38874	1313	None	34	Human	Functional	pEC50	=	9.5	9.5	-3	9	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL		None	None	None		None	10.1039/d0md00104j
	71461666	79171	None	0	Human	Functional	pEC50	=	9.5	9.5	3	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	520	5	2	5	4.3	CO[C@@]12CC[C@@]3(C[C@@H]1CNC(=O)/C=C/c1ccccc1Cl)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1021/jm070255o
	CHEMBL2113305	79171	None	0	Human	Functional	pEC50	=	9.5	9.5	3	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	520	5	2	5	4.3	CO[C@@]12CC[C@@]3(C[C@@H]1CNC(=O)/C=C/c1ccccc1Cl)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1021/jm070255o
	25233081	187545	None	2	Human	Functional	pEC50	=	9.5	9.5	-	1	Agonist activity at human mu-opioid receptor expressed in HEK293 cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human mu-opioid receptor expressed in HEK293 cell membranes after 1 hr by [35S]-GTPgammaS binding assay	ChEMBL	496	4	3	5	3.9	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccccc2c1	10.1021/acs.jmedchem.6b01807
	CHEMBL493846	187545	None	2	Human	Functional	pEC50	=	9.5	9.5	-	1	Agonist activity at human mu-opioid receptor expressed in HEK293 cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human mu-opioid receptor expressed in HEK293 cell membranes after 1 hr by [35S]-GTPgammaS binding assay	ChEMBL	496	4	3	5	3.9	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccccc2c1	10.1021/acs.jmedchem.6b01807
	118988707	146004	None	0	Human	Functional	pEC50	=	9.5	9.5	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	467	4	2	5	4.3	CO[C@@H]1C([C@](C)(O)C(C)(C)C)[C@H]2CC[C@@]13Oc1c(O)ccc4c1[C@@]31CCN(CC3CC3)[C@H](C4)C21	nan
	CHEMBL3917891	146004	None	0	Human	Functional	pEC50	=	9.5	9.5	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	467	4	2	5	4.3	CO[C@@H]1C([C@](C)(O)C(C)(C)C)[C@H]2CC[C@@]13Oc1c(O)ccc4c1[C@@]31CCN(CC3CC3)[C@H](C4)C21	nan
	50925450	57234	None	0	Rat	Functional	pEC50	=	9.5	9.5	-1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	732	14	5	7	3.3	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	CHEMBL1649943	57234	None	0	Rat	Functional	pEC50	=	9.5	9.5	-1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	732	14	5	7	3.3	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	71625029	87911	None	0	Rat	Functional	pEC50	=	9.5	9.5	-4	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	487	6	2	5	4.2	CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)Cc1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338717	87911	None	0	Rat	Functional	pEC50	=	9.5	9.5	-4	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	487	6	2	5	4.2	CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)Cc1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	11773726	204344	None	0	Human	Functional	pEC50	=	9.5	9.5	4	2	Agonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	391	3	1	5	3.0	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2C(=O)CC[C@@]3(OCc2ccccc2)[C@H]1C5	10.1021/acs.jmedchem.7b01363
	CHEMBL607351	204344	None	0	Human	Functional	pEC50	=	9.5	9.5	4	2	Agonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	391	3	1	5	3.0	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2C(=O)CC[C@@]3(OCc2ccccc2)[C@H]1C5	10.1021/acs.jmedchem.7b01363
	155564088	176786	None	0	Mouse	Functional	pEC50	=	9.5	9.5	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2sccc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4575933	176786	None	0	Mouse	Functional	pEC50	=	9.5	9.5	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2sccc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4598304	176786	None	0	Mouse	Functional	pEC50	=	9.5	9.5	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2sccc12	10.1021/acs.jmedchem.9b01767
	25232539	179366	None	0	Human	Functional	pEC50	=	9.5	9.5	-	1	Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	447	4	3	6	2.2	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccnc1	10.1021/jm801272c
	CHEMBL472937	179366	None	0	Human	Functional	pEC50	=	9.5	9.5	-	1	Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	447	4	3	6	2.2	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccnc1	10.1021/jm801272c
	139568842	195841	None	0	Human	Functional	pEC50	=	9.5	9.5	-	1	Agonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assayAgonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assay	ChEMBL	366	7	2	3	3.3	Cc1cc(O)ccc1C[C@@H](CNC(=O)[C@@H]1C[C@@]1(C)c1ccccc1)N(C)C	10.1016/j.bmcl.2023.129405
	CHEMBL5411716	195841	None	0	Human	Functional	pEC50	=	9.5	9.5	-	1	Agonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assayAgonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assay	ChEMBL	366	7	2	3	3.3	Cc1cc(O)ccc1C[C@@H](CNC(=O)[C@@H]1C[C@@]1(C)c1ccccc1)N(C)C	10.1016/j.bmcl.2023.129405
	155527203	176401	None	0	Rat	Functional	pEC50	=	9.5	9.5	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	547	7	3	6	4.2	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3cc4ccccc4o3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4459271	176401	None	0	Rat	Functional	pEC50	=	9.5	9.5	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	547	7	3	6	4.2	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3cc4ccccc4o3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4595173	176401	None	0	Rat	Functional	pEC50	=	9.5	9.5	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	547	7	3	6	4.2	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3cc4ccccc4o3)cc21	10.1021/acs.jmedchem.9b00378
	155538529	176633	None	0	Rat	Functional	pEC50	=	9.5	9.5	2	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	548	7	3	5	5.0	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3cnc4ccccc4c3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4476818	176633	None	0	Rat	Functional	pEC50	=	9.5	9.5	2	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	548	7	3	5	5.0	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3cnc4ccccc4c3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4597054	176633	None	0	Rat	Functional	pEC50	=	9.5	9.5	2	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	548	7	3	5	5.0	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3cnc4ccccc4c3)cc21	10.1021/acs.jmedchem.9b00378
	50925450	57234	None	0	Rat	Functional	pEC50	=	9.5	9.5	-1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	732	14	5	7	3.3	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	CHEMBL1649943	57234	None	0	Rat	Functional	pEC50	=	9.5	9.5	-1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	732	14	5	7	3.3	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	CHEMBL5083403	217347	None	3	Human	Functional	pEC50	=	9.5	9.5	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL		None	None	None		Fc1ccc([C@]2(CCNCc3cccc(Cl)c3)CCO[C@]3(CCOC3)C2)nc1	10.1016/j.ejmech.2021.113986
	155524410	176571	None	0	Mouse	Functional	pEC50	=	9.4	9.4	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1csc2ccccc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4455793	176571	None	0	Mouse	Functional	pEC50	=	9.4	9.4	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1csc2ccccc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4596517	176571	None	0	Mouse	Functional	pEC50	=	9.4	9.4	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1csc2ccccc12	10.1021/acs.jmedchem.9b01767
	127053153	141145	None	0	Rat	Functional	pEC50	=	9.4	9.4	-	1	Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay	ChEMBL	537	6	3	5	5.5	COC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccc4ccccc4c3)ccc21	10.1021/acs.jmedchem.6b00308
	CHEMBL3824356	141145	None	0	Rat	Functional	pEC50	=	9.4	9.4	-	1	Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay	ChEMBL	537	6	3	5	5.5	COC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccc4ccccc4c3)ccc21	10.1021/acs.jmedchem.6b00308
	118709690	113552	None	0	Mouse	Functional	pEC50	=	9.4	9.4	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2o1	10.1021/acs.jmedchem.9b01767
	CHEMBL3319617	113552	None	0	Mouse	Functional	pEC50	=	9.4	9.4	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2o1	10.1021/acs.jmedchem.9b01767
	CHEMBL4570108	113552	None	0	Mouse	Functional	pEC50	=	9.4	9.4	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2o1	10.1021/acs.jmedchem.9b01767
	86291189	150546	None	0	Human	Functional	pEC50	=	9.4	9.4	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	368	3	2	4	2.5	NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@@H]1CCC(=O)C3	nan
	CHEMBL3954177	150546	None	0	Human	Functional	pEC50	=	9.4	9.4	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	368	3	2	4	2.5	NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@@H]1CCC(=O)C3	nan
	118716009	114845	None	0	Human	Functional	pEC50	=	9.4	9.4	-12	3	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	485	5	3	6	2.5	O=C(NCc1ccccc1)C1=N[C@@]23CC[C@]1(O)C1Oc4c(O)ccc5c4C12CCN(CC1CC1)C3C5	10.1016/j.bmcl.2014.09.029
	CHEMBL3339378	114845	None	0	Human	Functional	pEC50	=	9.4	9.4	-12	3	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	485	5	3	6	2.5	O=C(NCc1ccccc1)C1=N[C@@]23CC[C@]1(O)C1Oc4c(O)ccc5c4C12CCN(CC1CC1)C3C5	10.1016/j.bmcl.2014.09.029
	16720749	85410	None	0	Human	Functional	pEC50	=	9.4	9.4	-7	3	Agonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	367	2	2	5	3.1	Nc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CC1)C2	10.1021/jm0701674
	CHEMBL226217	85410	None	0	Human	Functional	pEC50	=	9.4	9.4	-7	3	Agonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	367	2	2	5	3.1	Nc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CC1)C2	10.1021/jm0701674
	CHEMBL3086304	85410	None	0	Human	Functional	pEC50	=	9.4	9.4	-7	3	Agonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	367	2	2	5	3.1	Nc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CC1)C2	10.1021/jm0701674
	155532589	176735	None	0	Rat	Functional	pEC50	=	9.4	9.4	223	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	484	6	4	5	4.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(CN3CCc4ccccc4C3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4467875	176735	None	0	Rat	Functional	pEC50	=	9.4	9.4	223	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	484	6	4	5	4.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(CN3CCc4ccccc4C3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4597899	176735	None	0	Rat	Functional	pEC50	=	9.4	9.4	223	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	484	6	4	5	4.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(CN3CCc4ccccc4C3)cc21	10.1021/acs.jmedchem.9b00378
	155528038	176435	None	0	Mouse	Functional	pEC50	=	9.4	9.4	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2occc2c1	10.1021/acs.jmedchem.9b01767
	CHEMBL4460495	176435	None	0	Mouse	Functional	pEC50	=	9.4	9.4	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2occc2c1	10.1021/acs.jmedchem.9b01767
	CHEMBL4595439	176435	None	0	Mouse	Functional	pEC50	=	9.4	9.4	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2occc2c1	10.1021/acs.jmedchem.9b01767
	134338859	176504	None	0	Rat	Functional	pEC50	=	9.4	9.4	4	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	547	7	3	4	5.6	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3ccc4ccccc4c3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4446945	176504	None	0	Rat	Functional	pEC50	=	9.4	9.4	4	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	547	7	3	4	5.6	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3ccc4ccccc4c3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4595985	176504	None	0	Rat	Functional	pEC50	=	9.4	9.4	4	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	547	7	3	4	5.6	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3ccc4ccccc4c3)cc21	10.1021/acs.jmedchem.9b00378
	56596877	191847	None	0	Human	Functional	pEC50	=	9.4	9.4	-	1	Agonist activity at human MOP expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS bindingAgonist activity at human MOP expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS binding	ChEMBL	752	9	9	8	0.7	NC(=O)[C@@H]1CCC(=O)NCCCC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1	10.1021/acs.jmedchem.0c01915
	CHEMBL5197271	191847	None	0	Human	Functional	pEC50	=	9.4	9.4	-	1	Agonist activity at human MOP expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS bindingAgonist activity at human MOP expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS binding	ChEMBL	752	9	9	8	0.7	NC(=O)[C@@H]1CCC(=O)NCCCC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1	10.1021/acs.jmedchem.0c01915
	71624776	87927	None	0	Rat	Functional	pEC50	=	9.4	9.4	-2	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	481	7	2	5	4.8	CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)CCC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338731	87927	None	0	Rat	Functional	pEC50	=	9.4	9.4	-2	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	481	7	2	5	4.8	CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)CCC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	71624554	87945	None	0	Rat	Functional	pEC50	=	9.4	9.4	-13	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	493	5	2	5	4.9	CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338749	87945	None	0	Rat	Functional	pEC50	=	9.4	9.4	-13	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	493	5	2	5	4.9	CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	44427178	152475	None	0	Human	Functional	pEC50	=	9.4	9.4	-4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	ChEMBL	416	4	1	3	5.8	O=C(Nc1ccccc1)Oc1ccc2c(c1)C13CCCCC1C(C2)N(CC1CC1)CC3	10.1016/j.bmcl.2007.01.013
	CHEMBL397035	152475	None	0	Human	Functional	pEC50	=	9.4	9.4	-4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	ChEMBL	416	4	1	3	5.8	O=C(Nc1ccccc1)Oc1ccc2c(c1)C13CCCCC1C(C2)N(CC1CC1)CC3	10.1016/j.bmcl.2007.01.013
	CHEMBL5084538	218035	None	2	Mouse	Functional	pEC50	=	9.4	9.4	3	3	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccs1	10.1021/acs.jmedchem.2c00087
	CHEMBL5095817	218035	None	2	Mouse	Functional	pEC50	=	9.4	9.4	3	3	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccs1	10.1021/acs.jmedchem.2c00087
	CHEMBL208479	211658	None	0	Rat	Functional	pEC50	=	9.3	9.3	-1	5	Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCC)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/jm050921q
	CHEMBL208479	211658	None	0	Rat	Functional	pEC50	=	9.3	9.3	-1	5	Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCC)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/jm050921q
	162654878	180696	None	0	Human	Functional	pEC50	=	9.3	9.3	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL	407	7	1	4	4.7	COC(=O)CC[C@H]1[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1	10.1039/d0md00104j
	CHEMBL4754352	180696	None	0	Human	Functional	pEC50	=	9.3	9.3	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL	407	7	1	4	4.7	COC(=O)CC[C@H]1[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1	10.1039/d0md00104j
	CHEMBL5075300	216855	None	0	Human	Functional	pEC50	=	9.3	9.3	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL		None	None	None		c1ccc([C@]2(CCNCc3scc4c3CCC4)CCO[C@]3(CCOC3)C2)nc1	10.1016/j.ejmech.2021.113986
	155531530	176584	None	0	Mouse	Functional	pEC50	=	9.3	9.3	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1coc2ccccc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4466064	176584	None	0	Mouse	Functional	pEC50	=	9.3	9.3	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1coc2ccccc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4596625	176584	None	0	Mouse	Functional	pEC50	=	9.3	9.3	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1coc2ccccc12	10.1021/acs.jmedchem.9b01767
	122195960	124281	None	0	Rat	Functional	pEC50	=	9.3	9.3	-	1	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	521	6	3	4	5.2	CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cccc4ccccc34)ccc21	10.1021/acs.jmedchem.5b01270
	CHEMBL3634254	124281	None	0	Rat	Functional	pEC50	=	9.3	9.3	-	1	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	521	6	3	4	5.2	CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cccc4ccccc34)ccc21	10.1021/acs.jmedchem.5b01270
	71625151	87915	None	0	Rat	Functional	pEC50	=	9.3	9.3	-37	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	453	6	2	5	4.0	CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338720	87915	None	0	Rat	Functional	pEC50	=	9.3	9.3	-37	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	453	6	2	5	4.0	CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	13149	2545	None	18	Human	Functional	pEC50	=	9.3	9.3	8	4	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 assayAgonist 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	ChEMBL	398	5	1	5	3.8	CC[C@@H]1CN2CCC3=C([C@@H]2C[C@@H]1/C(=C\OC)/C(=O)OC)NC4=C3C(=CC=C4)OC	10.1021/acs.jmedchem.1c01273
	3034396	2545	None	18	Human	Functional	pEC50	=	9.3	9.3	8	4	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 assayAgonist 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	ChEMBL	398	5	1	5	3.8	CC[C@@H]1CN2CCC3=C([C@@H]2C[C@@H]1/C(=C\OC)/C(=O)OC)NC4=C3C(=CC=C4)OC	10.1021/acs.jmedchem.1c01273
	CHEMBL299031	2545	None	18	Human	Functional	pEC50	=	9.3	9.3	8	4	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 assayAgonist 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	ChEMBL	398	5	1	5	3.8	CC[C@@H]1CN2CCC3=C([C@@H]2C[C@@H]1/C(=C\OC)/C(=O)OC)NC4=C3C(=CC=C4)OC	10.1021/acs.jmedchem.1c01273
	1647	1313	None	34	Human	Functional	pEC50	=	9.3	9.3	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01273
	5462471	1313	None	34	Human	Functional	pEC50	=	9.3	9.3	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01273
	CHEMBL113995	1313	None	34	Human	Functional	pEC50	=	9.3	9.3	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01273
	CHEMBL38874	1313	None	34	Human	Functional	pEC50	=	9.3	9.3	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01273
	164628752	188722	None	0	Human	Functional	pEC50	=	9.3	9.3	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1n[nH]c2ccccc12	10.1016/j.bmcl.2021.127953
	CHEMBL4878281	188722	None	0	Human	Functional	pEC50	=	9.3	9.3	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1n[nH]c2ccccc12	10.1016/j.bmcl.2021.127953
	CHEMBL5029073	188722	None	0	Human	Functional	pEC50	=	9.3	9.3	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1n[nH]c2ccccc12	10.1016/j.bmcl.2021.127953
	CHEMBL5082522	217296	None	0	Human	Functional	pEC50	=	9.3	9.3	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL		None	None	None		FC1(F)CCc2c(csc2CNCC[C@@]2(c3ccccn3)CCOC3(CCOC3)C2)C1	10.1016/j.ejmech.2021.113986
	71454361	84204	None	0	Human	Functional	pEC50	=	9.3	9.3	-5	3	Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	494	7	2	3	6.0	C[C@H]1[C@H]2Cc3ccc(C(=O)NCCc4ccc(-c5ccc(O)cc5)cc4)cc3[C@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2012.10.081
	CHEMBL2208347	84204	None	0	Human	Functional	pEC50	=	9.3	9.3	-5	3	Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	494	7	2	3	6.0	C[C@H]1[C@H]2Cc3ccc(C(=O)NCCc4ccc(-c5ccc(O)cc5)cc4)cc3[C@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2012.10.081
	11849361	204279	None	0	Human	Functional	pEC50	=	9.3	9.3	4	3	Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR	ChEMBL	478	4	1	5	3.5	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccccc5Cl)[C@@H](C2)N(C)CC[C@]314	10.1021/jm0604777
	CHEMBL607016	204279	None	0	Human	Functional	pEC50	=	9.3	9.3	4	3	Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR	ChEMBL	478	4	1	5	3.5	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccccc5Cl)[C@@H](C2)N(C)CC[C@]314	10.1021/jm0604777
	11849284	204280	None	0	Human	Functional	pEC50	=	9.3	9.3	9	3	Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR	ChEMBL	458	4	1	5	3.2	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccccc5C)[C@@H](C2)N(C)CC[C@]314	10.1021/jm0604777
	CHEMBL607017	204280	None	0	Human	Functional	pEC50	=	9.3	9.3	9	3	Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR	ChEMBL	458	4	1	5	3.2	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccccc5C)[C@@H](C2)N(C)CC[C@]314	10.1021/jm0604777
	1164	1630	None	10	Human	Functional	pEC50	=	9.3	9.3	-1	13	Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acsmedchemlett.9b00404
	1626	1630	None	10	Human	Functional	pEC50	=	9.3	9.3	-1	13	Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acsmedchemlett.9b00404
	3345	1630	None	10	Human	Functional	pEC50	=	9.3	9.3	-1	13	Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acsmedchemlett.9b00404
	3345.0	1630	None	10	Human	Functional	pEC50	=	9.3	9.3	-1	13	Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acsmedchemlett.9b00404
	CHEMBL596	1630	None	10	Human	Functional	pEC50	=	9.3	9.3	-1	13	Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acsmedchemlett.9b00404
	DB00813	1630	None	10	Human	Functional	pEC50	=	9.3	9.3	-1	13	Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acsmedchemlett.9b00404
	72711408	103637	None	0	Human	Functional	pEC50	=	9.3	9.3	1	2	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis	ChEMBL	409	3	2	5	3.5	CC(=O)Nc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CC1)C2	10.1021/jm401290y
	CHEMBL3086305	103637	None	0	Human	Functional	pEC50	=	9.3	9.3	1	2	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis	ChEMBL	409	3	2	5	3.5	CC(=O)Nc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CC1)C2	10.1021/jm401290y
	72711412	106463	None	0	Human	Functional	pEC50	=	9.3	9.3	-1	2	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis	ChEMBL	381	3	2	5	3.6	CNc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CC1)C2	10.1021/jm401290y
	CHEMBL3086308	106463	None	0	Human	Functional	pEC50	=	9.3	9.3	-1	2	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis	ChEMBL	381	3	2	5	3.6	CNc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CC1)C2	10.1021/jm401290y
	CHEMBL3139481	106463	None	0	Human	Functional	pEC50	=	9.3	9.3	-1	2	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis	ChEMBL	381	3	2	5	3.6	CNc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CC1)C2	10.1021/jm401290y
	155555694	176566	None	0	Rat	Functional	pEC50	=	9.3	9.3	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	552	7	3	5	4.4	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(CN3CCc4ccccc4C3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4553931	176566	None	0	Rat	Functional	pEC50	=	9.3	9.3	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	552	7	3	5	4.4	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(CN3CCc4ccccc4C3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4596478	176566	None	0	Rat	Functional	pEC50	=	9.3	9.3	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	552	7	3	5	4.4	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(CN3CCc4ccccc4C3)cc21	10.1021/acs.jmedchem.9b00378
	71583625	86879	None	0	Rat	Functional	pEC50	=	9.3	9.3	-	1	Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	479	6	4	4	5.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccc4ccccc4c3)cc21	10.1021/jm400050y
	CHEMBL2322562	86879	None	0	Rat	Functional	pEC50	=	9.3	9.3	-	1	Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	479	6	4	4	5.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccc4ccccc4c3)cc21	10.1021/jm400050y
	71583625	86879	None	0	Rat	Functional	pEC50	=	9.3	9.3	-	1	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	479	6	4	4	5.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccc4ccccc4c3)cc21	10.1021/acs.jmedchem.5b01270
	CHEMBL2322562	86879	None	0	Rat	Functional	pEC50	=	9.3	9.3	-	1	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	479	6	4	4	5.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccc4ccccc4c3)cc21	10.1021/acs.jmedchem.5b01270
	153536692	173600	None	0	Mouse	Functional	pEC50	=	9.3	9.3	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	492	5	3	8	2.1	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1[N+](=O)[O-]	10.1021/acs.jmedchem.8b01158
	CHEMBL4530500	173600	None	0	Mouse	Functional	pEC50	=	9.3	9.3	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	492	5	3	8	2.1	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1[N+](=O)[O-]	10.1021/acs.jmedchem.8b01158
	86582596	149926	None	0	Human	Functional	pEC50	=	9.3	9.3	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	366	3	2	3	3.5	C=C1CC[C@H]2[C@H]3Cc4ccc(C(N)=O)c(O)c4[C@@]2(CCN3CC2CCC2)C1	nan
	CHEMBL3948892	149926	None	0	Human	Functional	pEC50	=	9.3	9.3	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	366	3	2	3	3.5	C=C1CC[C@H]2[C@H]3Cc4ccc(C(N)=O)c(O)c4[C@@]2(CCN3CC2CCC2)C1	nan
	CHEMBL5075108	218018	None	2	Mouse	Functional	pEC50	=	9.3	9.3	13	3	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccs1	10.1021/acs.jmedchem.2c00087
	CHEMBL5095555	218018	None	2	Mouse	Functional	pEC50	=	9.3	9.3	13	3	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccs1	10.1021/acs.jmedchem.2c00087
	122195962	124283	None	0	Rat	Functional	pEC50	=	9.3	9.3	1096	2	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	511	6	3	4	4.5	CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(CC3Cc4ccccc4C3)ccc21	10.1021/acs.jmedchem.5b01270
	CHEMBL3634256	124283	None	0	Rat	Functional	pEC50	=	9.3	9.3	1096	2	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	511	6	3	4	4.5	CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(CC3Cc4ccccc4C3)ccc21	10.1021/acs.jmedchem.5b01270
	71625027	87938	None	0	Rat	Functional	pEC50	=	9.3	9.3	-2	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	493	6	2	5	4.9	CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)CC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338742	87938	None	0	Rat	Functional	pEC50	=	9.3	9.3	-2	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	493	6	2	5	4.9	CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)CC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	71624552	87943	None	0	Rat	Functional	pEC50	=	9.3	9.3	-51	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	493	6	2	5	4.9	CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338747	87943	None	0	Rat	Functional	pEC50	=	9.3	9.3	-51	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	493	6	2	5	4.9	CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	44177570	61280	None	0	Rat	Functional	pEC50	=	9.2	9.2	-7	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding	ChEMBL	1219	27	10	10	6.0	CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1021/jm101023r
	CHEMBL1766204	61280	None	0	Rat	Functional	pEC50	=	9.2	9.2	-7	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding	ChEMBL	1219	27	10	10	6.0	CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1021/jm101023r
	44177570	61280	None	0	Rat	Functional	pEC50	=	9.2	9.2	-7	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding	ChEMBL	1219	27	10	10	6.0	CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1021/jm101023r
	CHEMBL1766204	61280	None	0	Rat	Functional	pEC50	=	9.2	9.2	-7	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding	ChEMBL	1219	27	10	10	6.0	CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1021/jm101023r
	71625601	90598	None	0	Rat	Functional	pEC50	=	9.2	9.2	10	3	Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	888	22	7	9	3.0	CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1	10.1016/j.bmcl.2013.03.065
	CHEMBL2387341	90598	None	0	Rat	Functional	pEC50	=	9.2	9.2	10	3	Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	888	22	7	9	3.0	CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1	10.1016/j.bmcl.2013.03.065
	155526174	176572	None	0	Mouse	Functional	pEC50	=	9.2	9.2	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccoc2c1	10.1021/acs.jmedchem.9b01767
	CHEMBL4457013	176572	None	0	Mouse	Functional	pEC50	=	9.2	9.2	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccoc2c1	10.1021/acs.jmedchem.9b01767
	CHEMBL4596531	176572	None	0	Mouse	Functional	pEC50	=	9.2	9.2	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccoc2c1	10.1021/acs.jmedchem.9b01767
	155544776	176585	None	0	Mouse	Functional	pEC50	=	9.2	9.2	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2occc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4565323	176585	None	0	Mouse	Functional	pEC50	=	9.2	9.2	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2occc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4596626	176585	None	0	Mouse	Functional	pEC50	=	9.2	9.2	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2occc12	10.1021/acs.jmedchem.9b01767
	1639	2726	None	32	Human	Functional	pEC50	=	9.2	9.2	-4	9	Effective concentration agonistic activity towards Opioid receptor mu 1Effective concentration agonistic activity towards Opioid receptor mu 1	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1021/jm030801n
	1765	2726	None	32	Human	Functional	pEC50	=	9.2	9.2	-4	9	Effective concentration agonistic activity towards Opioid receptor mu 1Effective concentration agonistic activity towards Opioid receptor mu 1	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1021/jm030801n
	5360515	2726	None	32	Human	Functional	pEC50	=	9.2	9.2	-4	9	Effective concentration agonistic activity towards Opioid receptor mu 1Effective concentration agonistic activity towards Opioid receptor mu 1	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1021/jm030801n
	5360515.0	2726	None	32	Human	Functional	pEC50	=	9.2	9.2	-4	9	Effective concentration agonistic activity towards Opioid receptor mu 1Effective concentration agonistic activity towards Opioid receptor mu 1	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1021/jm030801n
	CHEMBL19019	2726	None	32	Human	Functional	pEC50	=	9.2	9.2	-4	9	Effective concentration agonistic activity towards Opioid receptor mu 1Effective concentration agonistic activity towards Opioid receptor mu 1	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1021/jm030801n
	DB00704	2726	None	32	Human	Functional	pEC50	=	9.2	9.2	-4	9	Effective concentration agonistic activity towards Opioid receptor mu 1Effective concentration agonistic activity towards Opioid receptor mu 1	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1021/jm030801n
	1647	1313	None	34	Human	Functional	pEC50	=	9.2	9.2	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b01235
	5462471	1313	None	34	Human	Functional	pEC50	=	9.2	9.2	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b01235
	CHEMBL113995	1313	None	34	Human	Functional	pEC50	=	9.2	9.2	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b01235
	CHEMBL38874	1313	None	34	Human	Functional	pEC50	=	9.2	9.2	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b01235
	169494201	196019	None	2	Human	Functional	pEC50	=	9.2	9.2	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	365	7	0	3	4.5	CCC(=O)N(CC(CC)N1CCC(c2ccccc2)CC1)c1ccccn1	10.1021/acs.jmedchem.3c01637
	CHEMBL5415173	196019	None	2	Human	Functional	pEC50	=	9.2	9.2	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	365	7	0	3	4.5	CCC(=O)N(CC(CC)N1CCC(c2ccccc2)CC1)c1ccccn1	10.1021/acs.jmedchem.3c01637
	25256965	179300	None	0	Rat	Functional	pEC50	=	9.2	9.2	-7	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	512	8	2	5	4.4	C=CCO[C@@]12CC[C@@H](NC(=O)/C=C/c3ccccc3)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5	10.1021/jm8015552
	CHEMBL472410	179300	None	0	Rat	Functional	pEC50	=	9.2	9.2	-7	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	512	8	2	5	4.4	C=CCO[C@@]12CC[C@@H](NC(=O)/C=C/c3ccccc3)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5	10.1021/jm8015552
	71625025	87936	None	0	Rat	Functional	pEC50	=	9.2	9.2	-2	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	465	5	2	5	4.2	CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)C1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338740	87936	None	0	Rat	Functional	pEC50	=	9.2	9.2	-2	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	465	5	2	5	4.2	CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)C1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	58443217	84209	None	0	Human	Functional	pEC50	=	9.2	9.2	-6	3	Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	522	8	1	3	6.6	COc1ccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)cc1C	10.1016/j.bmcl.2012.10.081
	CHEMBL2208352	84209	None	0	Human	Functional	pEC50	=	9.2	9.2	-6	3	Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	522	8	1	3	6.6	COc1ccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)cc1C	10.1016/j.bmcl.2012.10.081
	122195956	124277	None	0	Rat	Functional	pEC50	=	9.2	9.2	22	3	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	477	6	3	4	4.6	CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(CC3CCCCC3)ccc21	10.1021/acs.jmedchem.5b01270
	CHEMBL3634250	124277	None	0	Rat	Functional	pEC50	=	9.2	9.2	22	3	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	477	6	3	4	4.6	CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(CC3CCCCC3)ccc21	10.1021/acs.jmedchem.5b01270
	155539282	172937	None	0	Human	Functional	pEC50	=	9.2	9.2	-	1	Agonist activity at human recombinant MOR expressed in CHO cells co-expressing C-terminally modified Galphaqi5 assessed as induction of calcium mobilization by Fluo-4AM dye-based fluorescence assayAgonist activity at human recombinant MOR expressed in CHO cells co-expressing C-terminally modified Galphaqi5 assessed as induction of calcium mobilization by Fluo-4AM dye-based fluorescence assay	ChEMBL	633	12	5	6	2.5	Cc1cc(O)c(Cl)c(C)c1C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.ejmech.2019.06.077
	CHEMBL4514319	172937	None	0	Human	Functional	pEC50	=	9.2	9.2	-	1	Agonist activity at human recombinant MOR expressed in CHO cells co-expressing C-terminally modified Galphaqi5 assessed as induction of calcium mobilization by Fluo-4AM dye-based fluorescence assayAgonist activity at human recombinant MOR expressed in CHO cells co-expressing C-terminally modified Galphaqi5 assessed as induction of calcium mobilization by Fluo-4AM dye-based fluorescence assay	ChEMBL	633	12	5	6	2.5	Cc1cc(O)c(Cl)c(C)c1C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.ejmech.2019.06.077
	56945125	159963	None	0	Human	Functional	pEC50	=	9.2	9.2	1	2	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	514	8	1	5	4.2	CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(C(N)=O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	nan
	CHEMBL4106746	159963	None	0	Human	Functional	pEC50	=	9.2	9.2	1	2	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	514	8	1	5	4.2	CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(C(N)=O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	nan
	CHEMBL5089829	218049	None	0	Mouse	Functional	pEC50	=	9.2	9.2	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(CCc1ccoc1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	CHEMBL5095916	218049	None	0	Mouse	Functional	pEC50	=	9.2	9.2	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(CCc1ccoc1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	44408526	137032	None	0	Rat	Functional	pEC50	=	9.2	9.2	1	5	Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells	ChEMBL	1148	30	11	15	3.0	CCCC[C@@H](C(=O)N[C@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O	10.1021/jm050851n
	CHEMBL374325	137032	None	0	Rat	Functional	pEC50	=	9.2	9.2	1	5	Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells	ChEMBL	1148	30	11	15	3.0	CCCC[C@@H](C(=O)N[C@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O	10.1021/jm050851n
	44408526	137032	None	0	Rat	Functional	pEC50	=	9.2	9.2	1	5	Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells	ChEMBL	1148	30	11	15	3.0	CCCC[C@@H](C(=O)N[C@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O	10.1021/jm050851n
	CHEMBL374325	137032	None	0	Rat	Functional	pEC50	=	9.2	9.2	1	5	Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells	ChEMBL	1148	30	11	15	3.0	CCCC[C@@H](C(=O)N[C@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O	10.1021/jm050851n
	25232543	187728	None	0	Human	Functional	pEC50	=	9.2	9.2	-	1	Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	497	4	3	6	3.3	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccccc2n1	10.1021/jm801272c
	CHEMBL494854	187728	None	0	Human	Functional	pEC50	=	9.2	9.2	-	1	Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	497	4	3	6	3.3	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccccc2n1	10.1021/jm801272c
	51003219	60134	None	0	Human	Functional	pEC50	=	9.2	9.2	-1	3	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 minsAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins	ChEMBL	518	10	3	6	3.7	O=C(O)CN[C@H]1CC[C@@]2(OCCCc3ccccc3)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/jm101211p
	CHEMBL1739441	60134	None	0	Human	Functional	pEC50	=	9.2	9.2	-1	3	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 minsAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins	ChEMBL	518	10	3	6	3.7	O=C(O)CN[C@H]1CC[C@@]2(OCCCc3ccccc3)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/jm101211p
	CHEMBL3216476	60134	None	0	Human	Functional	pEC50	=	9.2	9.2	-1	3	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 minsAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins	ChEMBL	518	10	3	6	3.7	O=C(O)CN[C@H]1CC[C@@]2(OCCCc3ccccc3)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/jm101211p
	50994530	57237	None	0	Rat	Functional	pEC50	=	9.2	9.2	-1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	716	14	5	7	2.8	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	CHEMBL1649946	57237	None	0	Rat	Functional	pEC50	=	9.2	9.2	-1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	716	14	5	7	2.8	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	25259489	172563	None	0	Rat	Functional	pEC50	=	9.2	9.2	2	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	517	6	3	7	3.1	O=C(/C=C/c1ccccc1[N+](=O)[O-])N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/jm8015552
	CHEMBL448145	172563	None	0	Rat	Functional	pEC50	=	9.2	9.2	2	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	517	6	3	7	3.1	O=C(/C=C/c1ccccc1[N+](=O)[O-])N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/jm8015552
	50994530	57237	None	0	Rat	Functional	pEC50	=	9.2	9.2	-1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	716	14	5	7	2.8	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	CHEMBL1649946	57237	None	0	Rat	Functional	pEC50	=	9.2	9.2	-1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	716	14	5	7	2.8	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	155520861	170596	None	0	Mouse	Functional	pEC50	=	9.2	9.2	102	3	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 analysisAgonist 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	ChEMBL	409	4	1	7	2.7	CC[C@@H]1CN2CC[C@]3(Nc4cccc(C#N)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.6b00748
	CHEMBL4449284	170596	None	0	Mouse	Functional	pEC50	=	9.2	9.2	102	3	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 analysisAgonist 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	ChEMBL	409	4	1	7	2.7	CC[C@@H]1CN2CC[C@]3(Nc4cccc(C#N)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.6b00748
	9848990	189274	None	0	Rat	Functional	pEC50	=	9.2	9.2	2	7	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/acs.jmedchem.5b00130
	9848990.0	189274	None	0	Rat	Functional	pEC50	=	9.2	9.2	2	7	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/acs.jmedchem.5b00130
	CHEMBL2368861	189274	None	0	Rat	Functional	pEC50	=	9.2	9.2	2	7	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/acs.jmedchem.5b00130
	CHEMBL511142	189274	None	0	Rat	Functional	pEC50	=	9.2	9.2	2	7	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/acs.jmedchem.5b00130
	24768353	97801	None	0	Rat	Functional	pEC50	=	9.2	9.2	18	3	Agonist activity at rat mu opioid receptor by [35S]GTP-gamma-S binding assayAgonist activity at rat mu opioid receptor by [35S]GTP-gamma-S binding assay	ChEMBL	941	22	9	9	2.7	CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccccc1	10.1021/jm070332f
	CHEMBL271619	97801	None	0	Rat	Functional	pEC50	=	9.2	9.2	18	3	Agonist activity at rat mu opioid receptor by [35S]GTP-gamma-S binding assayAgonist activity at rat mu opioid receptor by [35S]GTP-gamma-S binding assay	ChEMBL	941	22	9	9	2.7	CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccccc1	10.1021/jm070332f
	1651	2719	None	23	Human	Functional	pEC50	=	9.1	9.1	-18	5	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	476	5	2	6	3.1	CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1	10.1016/j.bmcl.2014.09.029
	4673	2719	None	23	Human	Functional	pEC50	=	9.1	9.1	-18	5	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	476	5	2	6	3.1	CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1	10.1016/j.bmcl.2014.09.029
	6445230	2719	None	23	Human	Functional	pEC50	=	9.1	9.1	-18	5	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	476	5	2	6	3.1	CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1	10.1016/j.bmcl.2014.09.029
	CHEMBL267495	2719	None	23	Human	Functional	pEC50	=	9.1	9.1	-18	5	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	476	5	2	6	3.1	CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1	10.1016/j.bmcl.2014.09.029
	DB13471	2719	None	23	Human	Functional	pEC50	=	9.1	9.1	-18	5	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	476	5	2	6	3.1	CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1	10.1016/j.bmcl.2014.09.029
	60170689	81739	None	0	Human	Functional	pEC50	=	9.1	9.1	95	2	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL	656	12	6	6	3.0	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1cccc(Cl)c1	10.1021/jm300664y
	CHEMBL2163912	81739	None	0	Human	Functional	pEC50	=	9.1	9.1	95	2	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL	656	12	6	6	3.0	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1cccc(Cl)c1	10.1021/jm300664y
	50994531	57238	None	0	Rat	Functional	pEC50	=	9.1	9.1	-25	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	804	13	4	7	4.2	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	CHEMBL1649947	57238	None	0	Rat	Functional	pEC50	=	9.1	9.1	-25	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	804	13	4	7	4.2	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	54581461	61283	None	0	Rat	Functional	pEC50	=	9.1	9.1	-1	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding	ChEMBL	1143	29	10	12	4.0	CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccc(OC)c(OC)c1	10.1021/jm101023r
	CHEMBL1766207	61283	None	0	Rat	Functional	pEC50	=	9.1	9.1	-1	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding	ChEMBL	1143	29	10	12	4.0	CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccc(OC)c(OC)c1	10.1021/jm101023r
	71624778	87929	None	0	Rat	Functional	pEC50	=	9.1	9.1	-2	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	507	6	2	5	5.3	CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)CC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338733	87929	None	0	Rat	Functional	pEC50	=	9.1	9.1	-2	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	507	6	2	5	5.3	CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)CC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	50994531	57238	None	0	Rat	Functional	pEC50	=	9.1	9.1	-25	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	804	13	4	7	4.2	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	CHEMBL1649947	57238	None	0	Rat	Functional	pEC50	=	9.1	9.1	-25	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	804	13	4	7	4.2	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	CHEMBL5087973	217622	None	0	Human	Functional	pEC50	=	9.1	9.1	-	1	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 assayAgonist 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	ChEMBL		None	None	None		CCC(=O)N(C[C@H](C)N1CCC(Cc2ccccc2)CC1)c1ccccc1	10.1016/j.ejmech.2022.114649
	CHEMBL5087973	217622	None	0	Human	Functional	pEC50	=	9.1	9.1	-	1	Agonist activity at human MOR expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 60 mins by cAMP HTRF assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 60 mins by cAMP HTRF assay	ChEMBL		None	None	None		CCC(=O)N(C[C@H](C)N1CCC(Cc2ccccc2)CC1)c1ccccc1	10.1016/j.ejmech.2021.113879
	164627377	188712	None	0	Human	Functional	pEC50	=	9.1	9.1	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2ncccc12	10.1016/j.bmcl.2021.127953
	CHEMBL4874437	188712	None	0	Human	Functional	pEC50	=	9.1	9.1	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2ncccc12	10.1016/j.bmcl.2021.127953
	CHEMBL5028994	188712	None	0	Human	Functional	pEC50	=	9.1	9.1	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2ncccc12	10.1016/j.bmcl.2021.127953
	132961503	161132	None	0	Rat	Functional	pEC50	=	9.1	9.1	851	2	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 methodAgonist 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	ChEMBL	382	5	2	5	3.4	O=[N+]([O-])c1ccc(CCN2CC[C@@]3(c4cccc(O)c4)CCC[C@@H]2[C@H]3O)cc1	10.1016/j.bmc.2017.02.064
	CHEMBL4085431	161132	None	0	Rat	Functional	pEC50	=	9.1	9.1	851	2	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 methodAgonist 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	ChEMBL	382	5	2	5	3.4	O=[N+]([O-])c1ccc(CCN2CC[C@@]3(c4cccc(O)c4)CCC[C@@H]2[C@H]3O)cc1	10.1016/j.bmc.2017.02.064
	CHEMBL4116456	161132	None	0	Rat	Functional	pEC50	=	9.1	9.1	851	2	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 methodAgonist 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	ChEMBL	382	5	2	5	3.4	O=[N+]([O-])c1ccc(CCN2CC[C@@]3(c4cccc(O)c4)CCC[C@@H]2[C@H]3O)cc1	10.1016/j.bmc.2017.02.064
	155538317	176402	None	0	Mouse	Functional	pEC50	=	9.1	9.1	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2occc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4476318	176402	None	0	Mouse	Functional	pEC50	=	9.1	9.1	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2occc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4595175	176402	None	0	Mouse	Functional	pEC50	=	9.1	9.1	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2occc12	10.1021/acs.jmedchem.9b01767
	127049274	141105	None	0	Rat	Functional	pEC50	=	9.1	9.1	18	3	Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay	ChEMBL	487	6	3	5	4.3	COC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccccc3)ccc21	10.1021/acs.jmedchem.6b00308
	CHEMBL3823830	141105	None	0	Rat	Functional	pEC50	=	9.1	9.1	18	3	Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay	ChEMBL	487	6	3	5	4.3	COC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccccc3)ccc21	10.1021/acs.jmedchem.6b00308
	5359966	187361	None	3	Human	Functional	pEC50	=	9.1	9.1	-6	2	Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	297	2	1	2	3.9	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3	10.1021/jm050577x
	CHEMBL49269	187361	None	3	Human	Functional	pEC50	=	9.1	9.1	-6	2	Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	297	2	1	2	3.9	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3	10.1021/jm050577x
	5359966	187361	None	3	Human	Functional	pEC50	=	9.1	9.1	-6	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting	ChEMBL	297	2	1	2	3.9	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3	10.1021/jm101542c
	CHEMBL49269	187361	None	3	Human	Functional	pEC50	=	9.1	9.1	-6	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting	ChEMBL	297	2	1	2	3.9	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3	10.1021/jm101542c
	5359966	187361	None	3	Human	Functional	pEC50	=	9.1	9.1	-6	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	ChEMBL	297	2	1	2	3.9	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3	10.1016/j.bmcl.2007.01.013
	CHEMBL49269	187361	None	3	Human	Functional	pEC50	=	9.1	9.1	-6	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	ChEMBL	297	2	1	2	3.9	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3	10.1016/j.bmcl.2007.01.013
	5359966	187361	None	3	Human	Functional	pEC50	=	9.1	9.1	-6	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	297	2	1	2	3.9	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3	10.1021/jm3001086
	CHEMBL49269	187361	None	3	Human	Functional	pEC50	=	9.1	9.1	-6	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	297	2	1	2	3.9	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3	10.1021/jm3001086
	5359966	187361	None	3	Human	Functional	pEC50	=	9.1	9.1	-6	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 minsAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins	ChEMBL	297	2	1	2	3.9	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3	10.1016/j.bmc.2007.03.076
	CHEMBL49269	187361	None	3	Human	Functional	pEC50	=	9.1	9.1	-6	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 minsAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins	ChEMBL	297	2	1	2	3.9	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3	10.1016/j.bmc.2007.03.076
	CHEMBL2419542	212902	None	0	Rat	Functional	pEC50	=	9.1	9.1	1	3	Agonist activity at rat MOR expressed in HN9.10 cell membranes by [35S]GTPgammaS binding assayAgonist activity at rat MOR expressed in HN9.10 cell membranes by [35S]GTPgammaS binding assay	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1016/j.bmcl.2013.06.065
	5359966	187361	None	3	Human	Functional	pEC50	=	9.1	9.1	-6	2	Agonistic activity against Opioid receptor mu 1 in Chinese hamster ovary membranesAgonistic activity against Opioid receptor mu 1 in Chinese hamster ovary membranes	ChEMBL	297	2	1	2	3.9	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3	10.1021/jm049978n
	CHEMBL49269	187361	None	3	Human	Functional	pEC50	=	9.1	9.1	-6	2	Agonistic activity against Opioid receptor mu 1 in Chinese hamster ovary membranesAgonistic activity against Opioid receptor mu 1 in Chinese hamster ovary membranes	ChEMBL	297	2	1	2	3.9	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3	10.1021/jm049978n
	44279594	107170	None	0	Human	Functional	pEC50	=	9.1	9.1	1	3	GTPgammaS binding in cloned human Opioid receptor mu 1 transfected into hamster ovary cellsGTPgammaS binding in cloned human Opioid receptor mu 1 transfected into hamster ovary cells	ChEMBL	423	1	2	5	3.2	CO[C@]12C=CC3(CC14CCC(C)(C)[C@H]4O)C1Cc4ccc(O)c5c4C3(CCN1C)[C@@H]2O5	10.1021/jm991165p
	CHEMBL31605	107170	None	0	Human	Functional	pEC50	=	9.1	9.1	1	3	GTPgammaS binding in cloned human Opioid receptor mu 1 transfected into hamster ovary cellsGTPgammaS binding in cloned human Opioid receptor mu 1 transfected into hamster ovary cells	ChEMBL	423	1	2	5	3.2	CO[C@]12C=CC3(CC14CCC(C)(C)[C@H]4O)C1Cc4ccc(O)c5c4C3(CCN1C)[C@@H]2O5	10.1021/jm991165p
	CHEMBL5094608	218042	None	0	Mouse	Functional	pEC50	=	9.1	9.1	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(Cc1ccc[nH]1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	CHEMBL5095870	218042	None	0	Mouse	Functional	pEC50	=	9.1	9.1	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(Cc1ccc[nH]1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	CHEMBL5092405	218040	None	0	Mouse	Functional	pEC50	=	9.1	9.1	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(CCc1ccsc1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	CHEMBL5095853	218040	None	0	Mouse	Functional	pEC50	=	9.1	9.1	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(CCc1ccsc1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	56668839	66658	None	0	Human	Functional	pEC50	=	9.1	9.1	-	1	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	481	4	3	6	2.8	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccnc(Cl)c1	10.1016/j.bmcl.2011.06.135
	CHEMBL1824509	66658	None	0	Human	Functional	pEC50	=	9.1	9.1	-	1	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	481	4	3	6	2.8	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccnc(Cl)c1	10.1016/j.bmcl.2011.06.135
	CHEMBL1852788	66658	None	0	Human	Functional	pEC50	=	9.1	9.1	-	1	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	481	4	3	6	2.8	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccnc(Cl)c1	10.1016/j.bmcl.2011.06.135
	44177670	61282	None	0	Rat	Functional	pEC50	=	9.1	9.1	-1	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding	ChEMBL	1151	27	10	10	5.0	CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cccc(C(F)(F)F)c1	10.1021/jm101023r
	CHEMBL1766206	61282	None	0	Rat	Functional	pEC50	=	9.1	9.1	-1	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding	ChEMBL	1151	27	10	10	5.0	CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cccc(C(F)(F)F)c1	10.1021/jm101023r
	44177670	61282	None	0	Rat	Functional	pEC50	=	9.1	9.1	-1	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding	ChEMBL	1151	27	10	10	5.0	CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cccc(C(F)(F)F)c1	10.1021/jm101023r
	CHEMBL1766206	61282	None	0	Rat	Functional	pEC50	=	9.1	9.1	-1	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding	ChEMBL	1151	27	10	10	5.0	CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cccc(C(F)(F)F)c1	10.1021/jm101023r
	71453373	81740	None	0	Human	Functional	pEC50	=	9.1	9.1	436	2	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL	656	12	6	6	3.0	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccccc1Cl	10.1021/jm300664y
	CHEMBL2163913	81740	None	0	Human	Functional	pEC50	=	9.1	9.1	436	2	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL	656	12	6	6	3.0	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccccc1Cl	10.1021/jm300664y
	71720457	86878	None	0	Rat	Functional	pEC50	=	9.1	9.1	83	2	Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	479	6	4	4	5.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3cccc4ccccc34)cc21	10.1021/jm400050y
	CHEMBL2322561	86878	None	0	Rat	Functional	pEC50	=	9.1	9.1	83	2	Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	479	6	4	4	5.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3cccc4ccccc34)cc21	10.1021/jm400050y
	71720457	86878	None	0	Rat	Functional	pEC50	=	9.1	9.1	83	2	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	479	6	4	4	5.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3cccc4ccccc34)cc21	10.1021/acs.jmedchem.5b01270
	CHEMBL2322561	86878	None	0	Rat	Functional	pEC50	=	9.1	9.1	83	2	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	479	6	4	4	5.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3cccc4ccccc34)cc21	10.1021/acs.jmedchem.5b01270
	71624892	87926	None	0	Rat	Functional	pEC50	=	9.1	9.1	-4	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	467	6	2	5	4.4	CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)CC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338730	87926	None	0	Rat	Functional	pEC50	=	9.1	9.1	-4	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	467	6	2	5	4.4	CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)CC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	57900041	88197	None	0	Human	Functional	pEC50	=	9.1	9.1	1	2	Partial 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 countingPartial 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	ChEMBL	479	7	1	3	5.7	C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(-c5cccnc5)cc4)cc3[C@@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2013.01.117
	CHEMBL2347236	88197	None	0	Human	Functional	pEC50	=	9.1	9.1	1	2	Partial 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 countingPartial 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	ChEMBL	479	7	1	3	5.7	C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(-c5cccnc5)cc4)cc3[C@@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2013.01.117
	44592015	189350	None	0	Human	Functional	pEC50	=	9.1	9.1	1	3	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	386	3	4	5	1.4	NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@]1(O)CC[C@@H](O)C3	10.1016/j.bmcl.2009.02.078
	CHEMBL511645	189350	None	0	Human	Functional	pEC50	=	9.1	9.1	1	3	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	386	3	4	5	1.4	NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@]1(O)CC[C@@H](O)C3	10.1016/j.bmcl.2009.02.078
	139569022	196368	None	3	Human	Functional	pEC50	=	9.1	9.1	-	1	Agonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assayAgonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assay	ChEMBL	352	7	2	3	3.0	CN(C)[C@H](CNC(=O)[C@@H]1C[C@@]1(C)c1ccccc1)Cc1ccc(O)cc1	10.1016/j.bmcl.2023.129405
	CHEMBL5422389	196368	None	3	Human	Functional	pEC50	=	9.1	9.1	-	1	Agonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assayAgonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assay	ChEMBL	352	7	2	3	3.0	CN(C)[C@H](CNC(=O)[C@@H]1C[C@@]1(C)c1ccccc1)Cc1ccc(O)cc1	10.1016/j.bmcl.2023.129405
	24768397	146506	None	0	Rat	Functional	pEC50	=	9.1	9.1	-4	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	698	14	5	7	2.7	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	CHEMBL392185	146506	None	0	Rat	Functional	pEC50	=	9.1	9.1	-4	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	698	14	5	7	2.7	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	44436084	88542	None	0	Rat	Functional	pEC50	=	9.1	9.1	-1	3	Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay	ChEMBL	845	18	6	8	3.4	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm061465o
	CHEMBL235109	88542	None	0	Rat	Functional	pEC50	=	9.1	9.1	-1	3	Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay	ChEMBL	845	18	6	8	3.4	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm061465o
	86582908	160148	None	0	Human	Functional	pEC50	=	9.1	9.1	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	324	3	1	2	3.3	NC(=O)c1ccc2c(c1)[C@@]13CCCCC1[C@@H](C2)N(CC1CC1)CC3	nan
	CHEMBL4108288	160148	None	0	Human	Functional	pEC50	=	9.1	9.1	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	324	3	1	2	3.3	NC(=O)c1ccc2c(c1)[C@@]13CCCCC1[C@@H](C2)N(CC1CC1)CC3	nan
	24768397	146506	None	0	Rat	Functional	pEC50	=	9.1	9.1	-4	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	698	14	5	7	2.7	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	CHEMBL392185	146506	None	0	Rat	Functional	pEC50	=	9.1	9.1	-4	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	698	14	5	7	2.7	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	44436084	88542	None	0	Rat	Functional	pEC50	=	9.1	9.1	-1	3	Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay	ChEMBL	845	18	6	8	3.4	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm061465o
	CHEMBL235109	88542	None	0	Rat	Functional	pEC50	=	9.1	9.1	-1	3	Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay	ChEMBL	845	18	6	8	3.4	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm061465o
	127050834	141114	None	0	Rat	Functional	pEC50	=	9.1	9.1	-	1	Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay	ChEMBL	549	8	3	4	6.0	CCCC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccc4ccccc4c3)ccc21	10.1021/acs.jmedchem.6b00308
	CHEMBL3823891	141114	None	0	Rat	Functional	pEC50	=	9.1	9.1	-	1	Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay	ChEMBL	549	8	3	4	6.0	CCCC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccc4ccccc4c3)ccc21	10.1021/acs.jmedchem.6b00308
	73355099	91662	None	0	Rat	Functional	pEC50	=	9.1	9.1	3	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 90 mins by liquid scintillation counting analysisAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 90 mins by liquid scintillation counting analysis	ChEMBL	729	11	3	6	5.0	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/ml400115n
	CHEMBL2408014	91662	None	0	Rat	Functional	pEC50	=	9.1	9.1	3	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 90 mins by liquid scintillation counting analysisAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 90 mins by liquid scintillation counting analysis	ChEMBL	729	11	3	6	5.0	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/ml400115n
	155522441	176598	None	0	Rat	Functional	pEC50	=	9.1	9.1	4	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	537	7	3	5	5.2	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3cc4ccccc4o3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4451910	176598	None	0	Rat	Functional	pEC50	=	9.1	9.1	4	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	537	7	3	5	5.2	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3cc4ccccc4o3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4596711	176598	None	0	Rat	Functional	pEC50	=	9.1	9.1	4	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	537	7	3	5	5.2	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3cc4ccccc4o3)cc21	10.1021/acs.jmedchem.9b00378
	11849360	204296	None	0	Human	Functional	pEC50	=	9.1	9.1	5	3	Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR	ChEMBL	478	4	1	5	3.5	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccc(Cl)cc5)[C@@H](C2)N(C)CC[C@]314	10.1021/jm0604777
	CHEMBL607069	204296	None	0	Human	Functional	pEC50	=	9.1	9.1	5	3	Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR	ChEMBL	478	4	1	5	3.5	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccc(Cl)cc5)[C@@H](C2)N(C)CC[C@]314	10.1021/jm0604777
	CHEMBL5081715	218025	None	0	Mouse	Functional	pEC50	=	9.0	9.0	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(Cc1ccoc1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	CHEMBL5095670	218025	None	0	Mouse	Functional	pEC50	=	9.0	9.0	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(Cc1ccoc1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	73355099	91662	None	0	Rat	Functional	pEC50	=	9.0	9.0	3	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 90 mins by liquid scintillation counting analysisAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 90 mins by liquid scintillation counting analysis	ChEMBL	729	11	3	6	5.0	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/ml400115n
	CHEMBL2408014	91662	None	0	Rat	Functional	pEC50	=	9.0	9.0	3	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 90 mins by liquid scintillation counting analysisAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 90 mins by liquid scintillation counting analysis	ChEMBL	729	11	3	6	5.0	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/ml400115n
	122195958	124279	None	0	Rat	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	521	6	3	4	5.2	CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccc4ccccc4c3)ccc21	10.1021/acs.jmedchem.5b01270
	CHEMBL3634252	124279	None	0	Rat	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	521	6	3	4	5.2	CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccc4ccccc4c3)ccc21	10.1021/acs.jmedchem.5b01270
	50994458	57231	None	0	Rat	Functional	pEC50	=	9.0	9.0	6	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	641	12	4	6	3.5	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	CHEMBL1649940	57231	None	0	Rat	Functional	pEC50	=	9.0	9.0	6	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	641	12	4	6	3.5	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	56596903	190141	None	0	Human	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at human MOP expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS bindingAgonist activity at human MOP expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS binding	ChEMBL	738	9	9	8	0.3	NC(=O)[C@@H]1CC(=O)NCCCC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1	10.1021/acs.jmedchem.0c01915
	CHEMBL5171745	190141	None	0	Human	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at human MOP expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS bindingAgonist activity at human MOP expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS binding	ChEMBL	738	9	9	8	0.3	NC(=O)[C@@H]1CC(=O)NCCCC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1	10.1021/acs.jmedchem.0c01915
	50994458	57231	None	0	Rat	Functional	pEC50	=	9.0	9.0	6	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	641	12	4	6	3.5	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	CHEMBL1649940	57231	None	0	Rat	Functional	pEC50	=	9.0	9.0	6	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	641	12	4	6	3.5	CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1	10.1021/jm100982d
	12732	1534	None	0	Human	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL	363	6	1	2	5.5	C(CC1=CC=CC=C1)N2[C@H]3CCC[C@@](CC2)([C@H]3CCC)C=4C=C(C=CC4)O	10.1039/d0md00104j
	155771777	1534	None	0	Human	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL	363	6	1	2	5.5	C(CC1=CC=CC=C1)N2[C@H]3CCC[C@@](CC2)([C@H]3CCC)C=4C=C(C=CC4)O	10.1039/d0md00104j
	CHEMBL4781853	1534	None	0	Human	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL	363	6	1	2	5.5	C(CC1=CC=CC=C1)N2[C@H]3CCC[C@@](CC2)([C@H]3CCC)C=4C=C(C=CC4)O	10.1039/d0md00104j
	155567281	176738	None	0	Mouse	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2ccoc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4588474	176738	None	0	Mouse	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2ccoc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4597924	176738	None	0	Mouse	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2ccoc12	10.1021/acs.jmedchem.9b01767
	CHEMBL5088056	218060	None	0	Mouse	Functional	pEC50	=	9.0	9.0	1	3	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccsc1	10.1021/acs.jmedchem.2c00087
	CHEMBL5096013	218060	None	0	Mouse	Functional	pEC50	=	9.0	9.0	1	3	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccsc1	10.1021/acs.jmedchem.2c00087
	54581461	61283	None	0	Rat	Functional	pEC50	=	9.0	9.0	-1	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding	ChEMBL	1143	29	10	12	4.0	CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccc(OC)c(OC)c1	10.1021/jm101023r
	CHEMBL1766207	61283	None	0	Rat	Functional	pEC50	=	9.0	9.0	-1	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding	ChEMBL	1143	29	10	12	4.0	CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccc(OC)c(OC)c1	10.1021/jm101023r
	164610091	188573	None	0	Human	Functional	pEC50	=	9.0	9.0	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2cccnc12	10.1016/j.bmcl.2021.127953
	CHEMBL4852470	188573	None	0	Human	Functional	pEC50	=	9.0	9.0	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2cccnc12	10.1016/j.bmcl.2021.127953
	CHEMBL5027998	188573	None	0	Human	Functional	pEC50	=	9.0	9.0	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2cccnc12	10.1016/j.bmcl.2021.127953
	155515704	176770	None	0	Mouse	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2ccoc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4442161	176770	None	0	Mouse	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2ccoc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4598179	176770	None	0	Mouse	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2ccoc12	10.1021/acs.jmedchem.9b01767
	CHEMBL5085221	218065	None	0	Mouse	Functional	pEC50	=	9.0	9.0	13	3	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(Cc1ccco1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	CHEMBL5096025	218065	None	0	Mouse	Functional	pEC50	=	9.0	9.0	13	3	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(Cc1ccco1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	44592015	189350	None	0	Human	Functional	pEC50	=	9.0	9.0	1	3	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	386	3	4	5	1.4	NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@]1(O)CC[C@@H](O)C3	nan
	CHEMBL511645	189350	None	0	Human	Functional	pEC50	=	9.0	9.0	1	3	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	386	3	4	5	1.4	NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@]1(O)CC[C@@H](O)C3	nan
	CHEMBL5083695	218030	None	0	Mouse	Functional	pEC50	=	9.0	9.0	6	3	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccco1	10.1021/acs.jmedchem.2c00087
	CHEMBL5095764	218030	None	0	Mouse	Functional	pEC50	=	9.0	9.0	6	3	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccco1	10.1021/acs.jmedchem.2c00087
	1647	1313	None	34	Human	Functional	pEC50	=	9	9.0	-3	9	Activation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assayActivation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assay	ChEMBL		None	None	None		None	10.1074/jbc.m703272200
	5462471	1313	None	34	Human	Functional	pEC50	=	9	9.0	-3	9	Activation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assayActivation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assay	ChEMBL		None	None	None		None	10.1074/jbc.m703272200
	CHEMBL113995	1313	None	34	Human	Functional	pEC50	=	9	9.0	-3	9	Activation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assayActivation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assay	ChEMBL		None	None	None		None	10.1074/jbc.m703272200
	CHEMBL38874	1313	None	34	Human	Functional	pEC50	=	9	9.0	-3	9	Activation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assayActivation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assay	ChEMBL		None	None	None		None	10.1074/jbc.m703272200
	9839245	101476	None	0	Human	Functional	pEC50	=	9	9.0	1	2	Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	298	3	1	2	2.7	CC1C2Cc3ccc(C(N)=O)cc3C1(C)CCN2CC1CC1	10.1016/j.bmcl.2008.10.134
	CHEMBL297428	101476	None	0	Human	Functional	pEC50	=	9	9.0	1	2	Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	298	3	1	2	2.7	CC1C2Cc3ccc(C(N)=O)cc3C1(C)CCN2CC1CC1	10.1016/j.bmcl.2008.10.134
	118567608	170816	None	0	Human	Functional	pEC50	=	9	9.0	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	398	4	0	3	4.2	CC1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccc2Cl)C1=O	10.1021/acs.jmedchem.9b01256
	CHEMBL4452042	170816	None	0	Human	Functional	pEC50	=	9	9.0	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	398	4	0	3	4.2	CC1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccc2Cl)C1=O	10.1021/acs.jmedchem.9b01256
	118562510	172997	None	0	Human	Functional	pEC50	=	9	9.0	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	378	5	0	3	3.9	CCC1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccc2)C1=O	10.1021/acs.jmedchem.9b01256
	CHEMBL4515812	172997	None	0	Human	Functional	pEC50	=	9	9.0	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	378	5	0	3	3.9	CCC1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccc2)C1=O	10.1021/acs.jmedchem.9b01256
	11250029	1549	None	30	Human	Functional	pEC50	=	9	9.0	1584	2	Agonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay	ChEMBL	569	11	4	6	4.2	COc1ccc(cc1C(=O)O)CN([C@H](c1ncc([nH]1)c1ccccc1)C)C(=O)[C@H](Cc1c(C)cc(cc1C)C(=O)N)N	10.1016/j.bmcl.2012.05.042
	11250029.0	1549	None	30	Human	Functional	pEC50	=	9	9.0	1584	2	Agonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay	ChEMBL	569	11	4	6	4.2	COc1ccc(cc1C(=O)O)CN([C@H](c1ncc([nH]1)c1ccccc1)C)C(=O)[C@H](Cc1c(C)cc(cc1C)C(=O)N)N	10.1016/j.bmcl.2012.05.042
	130406582	1549	None	30	Human	Functional	pEC50	=	9	9.0	1584	2	Agonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay	ChEMBL	569	11	4	6	4.2	COc1ccc(cc1C(=O)O)CN([C@H](c1ncc([nH]1)c1ccccc1)C)C(=O)[C@H](Cc1c(C)cc(cc1C)C(=O)N)N	10.1016/j.bmcl.2012.05.042
	5001	1549	None	30	Human	Functional	pEC50	=	9	9.0	1584	2	Agonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay	ChEMBL	569	11	4	6	4.2	COc1ccc(cc1C(=O)O)CN([C@H](c1ncc([nH]1)c1ccccc1)C)C(=O)[C@H](Cc1c(C)cc(cc1C)C(=O)N)N	10.1016/j.bmcl.2012.05.042
	7691	1549	None	30	Human	Functional	pEC50	=	9	9.0	1584	2	Agonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay	ChEMBL	569	11	4	6	4.2	COc1ccc(cc1C(=O)O)CN([C@H](c1ncc([nH]1)c1ccccc1)C)C(=O)[C@H](Cc1c(C)cc(cc1C)C(=O)N)N	10.1016/j.bmcl.2012.05.042
	CHEMBL2159122	1549	None	30	Human	Functional	pEC50	=	9	9.0	1584	2	Agonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay	ChEMBL	569	11	4	6	4.2	COc1ccc(cc1C(=O)O)CN([C@H](c1ncc([nH]1)c1ccccc1)C)C(=O)[C@H](Cc1c(C)cc(cc1C)C(=O)N)N	10.1016/j.bmcl.2012.05.042
	DB09272	1549	None	30	Human	Functional	pEC50	=	9	9.0	1584	2	Agonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay	ChEMBL	569	11	4	6	4.2	COc1ccc(cc1C(=O)O)CN([C@H](c1ncc([nH]1)c1ccccc1)C)C(=O)[C@H](Cc1c(C)cc(cc1C)C(=O)N)N	10.1016/j.bmcl.2012.05.042
	25256967	179322	None	0	Rat	Functional	pEC50	=	9	9.0	2	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	514	6	2	6	3.7	CC(=O)O[C@@]12CC[C@@H](NC(=O)/C=C/c3ccccc3)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5	10.1021/jm8015552
	CHEMBL472583	179322	None	0	Rat	Functional	pEC50	=	9	9.0	2	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	514	6	2	6	3.7	CC(=O)O[C@@]12CC[C@@H](NC(=O)/C=C/c3ccccc3)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5	10.1021/jm8015552
	155551874	176666	None	0	Rat	Functional	pEC50	=	9	9.0	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	584	7	3	5	5.9	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)c2ccccc2)c2ccc(Cc3cnc4ccccc4c3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4569709	176666	None	0	Rat	Functional	pEC50	=	9	9.0	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	584	7	3	5	5.9	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)c2ccccc2)c2ccc(Cc3cnc4ccccc4c3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4597300	176666	None	0	Rat	Functional	pEC50	=	9	9.0	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	584	7	3	5	5.9	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)c2ccccc2)c2ccc(Cc3cnc4ccccc4c3)cc21	10.1021/acs.jmedchem.9b00378
	71717732	87908	None	0	Rat	Functional	pEC50	=	9	9.0	-19	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	479	7	2	5	4.6	CO[C@]12C=C[C@@]3(C[C@@H]1[C@](C)(O)CCC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338714	87908	None	0	Rat	Functional	pEC50	=	9	9.0	-19	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	479	7	2	5	4.6	CO[C@]12C=C[C@@]3(C[C@@H]1[C@](C)(O)CCC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	71624777	87928	None	0	Rat	Functional	pEC50	=	9	9.0	-12	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	479	5	2	5	4.6	CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)C1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338732	87928	None	0	Rat	Functional	pEC50	=	9	9.0	-12	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	479	5	2	5	4.6	CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)C1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	71624894	87933	None	0	Rat	Functional	pEC50	=	9	9.0	-1	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	439	5	2	5	3.6	CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)C(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338737	87933	None	0	Rat	Functional	pEC50	=	9	9.0	-1	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	439	5	2	5	3.6	CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)C(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	44401457	132826	None	0	Human	Functional	pEC50	=	9	9.0	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	384	3	3	5	1.6	NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@]1(O)CCC(=O)C3	nan
	CHEMBL370029	132826	None	0	Human	Functional	pEC50	=	9	9.0	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	384	3	3	5	1.6	NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@]1(O)CCC(=O)C3	nan
	164618692	188639	None	0	Mouse	Functional	pEC50	=	9	9.0	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based scintillation counting method	ChEMBL	483	4	4	5	3.0	O=C(N[C@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2ccccc12	10.1016/j.bmcl.2021.127953
	CHEMBL4872376	188639	None	0	Mouse	Functional	pEC50	=	9	9.0	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based scintillation counting method	ChEMBL	483	4	4	5	3.0	O=C(N[C@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2ccccc12	10.1016/j.bmcl.2021.127953
	CHEMBL5028511	188639	None	0	Mouse	Functional	pEC50	=	9	9.0	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based scintillation counting method	ChEMBL	483	4	4	5	3.0	O=C(N[C@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2ccccc12	10.1016/j.bmcl.2021.127953
	25232367	189713	None	0	Human	Functional	pEC50	=	9	9.0	-	1	Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	447	4	3	6	2.2	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccnc1	10.1021/jm801272c
	CHEMBL514769	189713	None	0	Human	Functional	pEC50	=	9	9.0	-	1	Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	447	4	3	6	2.2	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccnc1	10.1021/jm801272c
	56596878	191947	None	0	Human	Functional	pEC50	=	9	9.0	-	1	Agonist activity at human MOP expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS bindingAgonist activity at human MOP expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS binding	ChEMBL	809	11	10	9	-0.2	NC(=O)CNC(=O)[C@@H]1CCC(=O)NCCCC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1	10.1021/acs.jmedchem.0c01915
	CHEMBL5198915	191947	None	0	Human	Functional	pEC50	=	9	9.0	-	1	Agonist activity at human MOP expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS bindingAgonist activity at human MOP expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS binding	ChEMBL	809	11	10	9	-0.2	NC(=O)CNC(=O)[C@@H]1CCC(=O)NCCCC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1	10.1021/acs.jmedchem.0c01915
	155530151	176642	None	0	Mouse	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2sccc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4463978	176642	None	0	Mouse	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2sccc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4597107	176642	None	0	Mouse	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2sccc12	10.1021/acs.jmedchem.9b01767
	72164177	92045	None	0	Mouse	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	ChEMBL	513	4	4	7	3.0	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ncc2ccccc2c1O	10.1016/j.bmcl.2013.07.043
	CHEMBL2417568	92045	None	0	Mouse	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	ChEMBL	513	4	4	7	3.0	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ncc2ccccc2c1O	10.1016/j.bmcl.2013.07.043
	72164177	92045	None	0	Mouse	Functional	pEC50	=	9.0	9.0	-	1	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	513	4	4	7	3.0	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ncc2ccccc2c1O	10.1016/j.bmc.2015.02.055
	CHEMBL2417568	92045	None	0	Mouse	Functional	pEC50	=	9.0	9.0	-	1	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	513	4	4	7	3.0	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ncc2ccccc2c1O	10.1016/j.bmc.2015.02.055
	CHEMBL5074403	218061	None	2	Mouse	Functional	pEC50	=	9.0	9.0	15	3	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccsc1	10.1021/acs.jmedchem.2c00087
	CHEMBL5096015	218061	None	2	Mouse	Functional	pEC50	=	9.0	9.0	15	3	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccsc1	10.1021/acs.jmedchem.2c00087
	118716010	114846	None	0	Human	Functional	pEC50	=	9.0	9.0	-6	2	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	499	6	3	6	2.5	O=C(NCCc1ccccc1)C1=N[C@@]23CC[C@]1(O)C1Oc4c(O)ccc5c4C12CCN(CC1CC1)C3C5	10.1016/j.bmcl.2014.09.029
	CHEMBL3339379	114846	None	0	Human	Functional	pEC50	=	9.0	9.0	-6	2	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	499	6	3	6	2.5	O=C(NCCc1ccccc1)C1=N[C@@]23CC[C@]1(O)C1Oc4c(O)ccc5c4C12CCN(CC1CC1)C3C5	10.1016/j.bmcl.2014.09.029
	57412942	75871	None	0	Human	Functional	pEC50	=	9.0	9.0	-3	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	445	6	1	4	6.1	O=[N+]([O-])c1cccc(CNc2ccc3c(c2)[C@@]24CCCC[C@H]2[C@@H](C3)N(CC2CCC2)CC4)c1	10.1021/jm3001086
	CHEMBL2048767	75871	None	0	Human	Functional	pEC50	=	9.0	9.0	-3	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	445	6	1	4	6.1	O=[N+]([O-])c1cccc(CNc2ccc3c(c2)[C@@]24CCCC[C@H]2[C@@H](C3)N(CC2CCC2)CC4)c1	10.1021/jm3001086
	168272069	190389	None	0	Human	Functional	pEC50	=	9.0	9.0	-13	3	Agonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assay	ChEMBL	713	7	8	8	1.0	Cc1cccc([C@@H]2NC(=O)[C@H](c3ccccc3)NC(=O)[C@H](NC(=O)[C@@H](N)Cc3c(C)cc(O)cc3C)CCCCNC(=O)C[C@@H](C(N)=O)NC2=O)c1	10.1021/acs.jmedchem.0c01915
	CHEMBL5175678	190389	None	0	Human	Functional	pEC50	=	9.0	9.0	-13	3	Agonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assay	ChEMBL	713	7	8	8	1.0	Cc1cccc([C@@H]2NC(=O)[C@H](c3ccccc3)NC(=O)[C@H](NC(=O)[C@@H](N)Cc3c(C)cc(O)cc3C)CCCCNC(=O)C[C@@H](C(N)=O)NC2=O)c1	10.1021/acs.jmedchem.0c01915
	71583623	86877	None	0	Rat	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	443	7	4	4	4.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(CCc3ccccc3)cc21	10.1021/jm400050y
	CHEMBL2322560	86877	None	0	Rat	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	443	7	4	4	4.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(CCc3ccccc3)cc21	10.1021/jm400050y
	134345539	176649	None	0	Rat	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	469	6	4	5	4.9	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3cc4ccccc4o3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4529363	176649	None	0	Rat	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	469	6	4	5	4.9	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3cc4ccccc4o3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4597172	176649	None	0	Rat	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	469	6	4	5	4.9	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3cc4ccccc4o3)cc21	10.1021/acs.jmedchem.9b00378
	155555053	176667	None	0	Rat	Functional	pEC50	=	9.0	9.0	5	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	522	6	3	5	4.6	CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cnc4ccccc4c3)ccc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4550332	176667	None	0	Rat	Functional	pEC50	=	9.0	9.0	5	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	522	6	3	5	4.6	CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cnc4ccccc4c3)ccc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4597317	176667	None	0	Rat	Functional	pEC50	=	9.0	9.0	5	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	522	6	3	5	4.6	CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cnc4ccccc4c3)ccc21	10.1021/acs.jmedchem.9b00378
	86582595	160210	None	0	Human	Functional	pEC50	=	9.0	9.0	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	382	3	3	4	2.6	C=C1CC[C@@]2(O)[C@H]3Cc4ccc(C(N)=O)c(O)c4[C@@]2(CCN3CC2CCC2)C1	nan
	CHEMBL4108846	160210	None	0	Human	Functional	pEC50	=	9.0	9.0	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	382	3	3	4	2.6	C=C1CC[C@@]2(O)[C@H]3Cc4ccc(C(N)=O)c(O)c4[C@@]2(CCN3CC2CCC2)C1	nan
	156015003	177643	None	0	Human	Functional	pEC50	=	9.0	9.0	1	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	586	8	2	6	6.5	Oc1cccc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)c1	10.1021/acs.jmedchem.0c00503
	CHEMBL4640139	177643	None	0	Human	Functional	pEC50	=	9.0	9.0	1	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	586	8	2	6	6.5	Oc1cccc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)c1	10.1021/acs.jmedchem.0c00503
	56672310	66607	None	0	Human	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	461	4	3	6	2.5	Cc1cc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)ccn1	10.1016/j.bmcl.2011.06.135
	CHEMBL1824512	66607	None	0	Human	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	461	4	3	6	2.5	Cc1cc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)ccn1	10.1016/j.bmcl.2011.06.135
	CHEMBL1852558	66607	None	0	Human	Functional	pEC50	=	9.0	9.0	-	1	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	461	4	3	6	2.5	Cc1cc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)ccn1	10.1016/j.bmcl.2011.06.135
	25232540	192909	None	2	Human	Functional	pEC50	=	8.9	8.9	4	3	Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	447	4	3	6	2.2	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1	10.1021/jm801272c
	CHEMBL522143	192909	None	2	Human	Functional	pEC50	=	8.9	8.9	4	3	Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	447	4	3	6	2.2	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1	10.1021/jm801272c
	72164055	92095	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	ChEMBL	525	6	3	6	3.6	O=C(CCc1cc2ccccc2cn1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2013.07.043
	CHEMBL2419119	92095	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	ChEMBL	525	6	3	6	3.6	O=C(CCc1cc2ccccc2cn1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2013.07.043
	72164055	92095	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	525	6	3	6	3.6	O=C(CCc1cc2ccccc2cn1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmc.2015.02.055
	CHEMBL2419119	92095	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	525	6	3	6	3.6	O=C(CCc1cc2ccccc2cn1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmc.2015.02.055
	CHEMBL375068	214671	None	0	Human	Functional	pEC50	=	8.9	8.9	-	1	Activity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assayActivity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay	ChEMBL		None	None	None		Cc1cc(C[C@H](N)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](Cc2cccc3ccccc23)C(N)=O)cc(C)c1O	10.1021/jm060998u
	CHEMBL5086477	217522	None	2	Mouse	Functional	pEC50	=	8.9	8.9	10	3	Antagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method	ChEMBL		None	None	None		O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cnc[nH]1	10.1021/acs.jmedchem.1c02185
	24822965	169609	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	466	5	3	6	2.7	O=C(Cc1cccs1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	CHEMBL443326	169609	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	466	5	3	6	2.7	O=C(Cc1cccs1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	CHEMBL5082679	169609	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	466	5	3	6	2.7	O=C(Cc1cccs1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	CHEMBL5085865	218055	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(Cc1cc[nH]c1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	CHEMBL5095975	218055	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(Cc1cc[nH]c1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	56679008	66548	None	0	Human	Functional	pEC50	=	8.9	8.9	-	1	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	525	4	3	6	2.9	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccnc(Br)c1	10.1016/j.bmcl.2011.06.135
	CHEMBL1824510	66548	None	0	Human	Functional	pEC50	=	8.9	8.9	-	1	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	525	4	3	6	2.9	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccnc(Br)c1	10.1016/j.bmcl.2011.06.135
	CHEMBL1852385	66548	None	0	Human	Functional	pEC50	=	8.9	8.9	-	1	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	525	4	3	6	2.9	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccnc(Br)c1	10.1016/j.bmcl.2011.06.135
	72735760	106372	None	0	Human	Functional	pEC50	=	8.9	8.9	1	2	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay	ChEMBL	438	2	2	5	4.1	Oc1ccc2c(c1)[C@]13CCN(Cc4ccco4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3	10.1016/j.bmc.2013.10.032
	CHEMBL3139108	106372	None	0	Human	Functional	pEC50	=	8.9	8.9	1	2	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay	ChEMBL	438	2	2	5	4.1	Oc1ccc2c(c1)[C@]13CCN(Cc4ccco4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3	10.1016/j.bmc.2013.10.032
	CHEMBL4296726	106372	None	0	Human	Functional	pEC50	=	8.9	8.9	1	2	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay	ChEMBL	438	2	2	5	4.1	Oc1ccc2c(c1)[C@]13CCN(Cc4ccco4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3	10.1016/j.bmc.2013.10.032
	44380504	59085	None	0	Human	Functional	pEC50	=	8.9	8.9	1	3	Activity was evaluated in human mu opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assayActivity was evaluated in human mu opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assay	ChEMBL	427	2	2	5	3.6	CO[C@@]12CCC3(C[C@H]1[C@@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4C3(CCN1C)[C@H]2O5	10.1016/s0960-894x(99)00085-2
	CHEMBL169552	59085	None	0	Human	Functional	pEC50	=	8.9	8.9	1	3	Activity was evaluated in human mu opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assayActivity was evaluated in human mu opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assay	ChEMBL	427	2	2	5	3.6	CO[C@@]12CCC3(C[C@H]1[C@@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4C3(CCN1C)[C@H]2O5	10.1016/s0960-894x(99)00085-2
	172450838	195593	None	0	Human	Functional	pEC50	=	8.9	8.9	7	4	Agonist activity at MOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at MOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay	ChEMBL	1150	24	13	13	-0.4	CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C/CC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1	10.1021/acs.jmedchem.3c02093
	CHEMBL5406732	195593	None	0	Human	Functional	pEC50	=	8.9	8.9	7	4	Agonist activity at MOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at MOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay	ChEMBL	1150	24	13	13	-0.4	CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C/CC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1	10.1021/acs.jmedchem.3c02093
	156043182	183244	None	0	Human	Functional	pEC50	=	8.9	8.9	67	2	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL	379	7	2	3	4.5	OCCC[C@H]1[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1	10.1039/d0md00104j
	CHEMBL4795160	183244	None	0	Human	Functional	pEC50	=	8.9	8.9	67	2	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL	379	7	2	3	4.5	OCCC[C@H]1[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1	10.1039/d0md00104j
	132079904	182575	None	0	Human	Functional	pEC50	=	8.9	8.9	5	2	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 assayAgonist 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	ChEMBL	492	4	0	8	4.4	COC(=O)[C@@H]1C=C(OC(=O)c2ccccc2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@@]12C	10.1021/acs.jmedchem.6b01235
	CHEMBL4786506	182575	None	0	Human	Functional	pEC50	=	8.9	8.9	5	2	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 assayAgonist 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	ChEMBL	492	4	0	8	4.4	COC(=O)[C@@H]1C=C(OC(=O)c2ccccc2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@@]12C	10.1021/acs.jmedchem.6b01235
	54580938	62097	None	0	Human	Functional	pEC50	=	8.9	8.9	-1	2	Agonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	805	15	1	7	10.2	O=C(CCCCCCCCC(=O)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3)Oc1ccc2c(c1)[C@@]13CCCC[C@@]1(O)[C@@H](C2)N(CC1CCC1)CC3	10.1016/j.bmc.2011.03.052
	CHEMBL1774949	62097	None	0	Human	Functional	pEC50	=	8.9	8.9	-1	2	Agonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	805	15	1	7	10.2	O=C(CCCCCCCCC(=O)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3)Oc1ccc2c(c1)[C@@]13CCCC[C@@]1(O)[C@@H](C2)N(CC1CCC1)CC3	10.1016/j.bmc.2011.03.052
	11848225	877	None	42	Human	Functional	pEC50	=	8.9	8.9	10	2	Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	378	2	1	2	5.1	Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1	10.1021/ml500117c
	11848225.0	877	None	42	Human	Functional	pEC50	=	8.9	8.9	10	2	Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	378	2	1	2	5.1	Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1	10.1021/ml500117c
	8866	877	None	42	Human	Functional	pEC50	=	8.9	8.9	10	2	Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	378	2	1	2	5.1	Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1	10.1021/ml500117c
	CHEMBL2364605	877	None	42	Human	Functional	pEC50	=	8.9	8.9	10	2	Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	378	2	1	2	5.1	Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1	10.1021/ml500117c
	CHEMBL3545616	877	None	42	Human	Functional	pEC50	=	8.9	8.9	10	2	Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	378	2	1	2	5.1	Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1	10.1021/ml500117c
	CHEMBL3962932	877	None	42	Human	Functional	pEC50	=	8.9	8.9	10	2	Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	378	2	1	2	5.1	Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1	10.1021/ml500117c
	DB12830	877	None	42	Human	Functional	pEC50	=	8.9	8.9	10	2	Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	378	2	1	2	5.1	Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1	10.1021/ml500117c
	11956680	120622	None	0	Human	Functional	pEC50	=	8.9	8.9	100	2	Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	376	2	2	3	4.7	CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(O)ccc3[nH]c12	10.1021/ml500117c
	CHEMBL3325961	120622	None	0	Human	Functional	pEC50	=	8.9	8.9	100	2	Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	376	2	2	3	4.7	CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(O)ccc3[nH]c12	10.1021/ml500117c
	CHEMBL3545622	120622	None	0	Human	Functional	pEC50	=	8.9	8.9	100	2	Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	376	2	2	3	4.7	CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(O)ccc3[nH]c12	10.1021/ml500117c
	44598284	200311	None	0	Rat	Functional	pEC50	=	8.9	8.9	10	3	Agonist activity at rat mu opioid receptor expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at rat mu opioid receptor expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting	ChEMBL	742	9	7	9	1.8	NC(=O)[C@@H]1CSCSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1	10.1021/jm9007483
	CHEMBL572525	200311	None	0	Rat	Functional	pEC50	=	8.9	8.9	10	3	Agonist activity at rat mu opioid receptor expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at rat mu opioid receptor expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting	ChEMBL	742	9	7	9	1.8	NC(=O)[C@@H]1CSCSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1	10.1021/jm9007483
	71624446	87940	None	0	Rat	Functional	pEC50	=	8.9	8.9	-20	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	467	6	2	5	4.4	CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338744	87940	None	0	Rat	Functional	pEC50	=	8.9	8.9	-20	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	467	6	2	5	4.4	CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	146408960	173942	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	465	4	3	6	2.3	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1F	10.1021/acs.jmedchem.8b01158
	CHEMBL4538841	173942	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	465	4	3	6	2.3	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1F	10.1021/acs.jmedchem.8b01158
	5486554	31444	None	23	Human	Functional	pEC50	=	8.9	8.9	3	3	Inverse agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 3 hrs by [35S]GTPgammaS binding assayInverse agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 3 hrs by [35S]GTPgammaS binding assay	ChEMBL	343	2	3	5	1.3	Oc1ccc2c3c1O[C@H]1[C@H](O)CC[C@@]4(O)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1016/j.bmcl.2012.06.056
	CHEMBL140278	31444	None	23	Human	Functional	pEC50	=	8.9	8.9	3	3	Inverse agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 3 hrs by [35S]GTPgammaS binding assayInverse agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 3 hrs by [35S]GTPgammaS binding assay	ChEMBL	343	2	3	5	1.3	Oc1ccc2c3c1O[C@H]1[C@H](O)CC[C@@]4(O)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1016/j.bmcl.2012.06.056
	CHEMBL558140	31444	None	23	Human	Functional	pEC50	=	8.9	8.9	3	3	Inverse agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 3 hrs by [35S]GTPgammaS binding assayInverse agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 3 hrs by [35S]GTPgammaS binding assay	ChEMBL	343	2	3	5	1.3	Oc1ccc2c3c1O[C@H]1[C@H](O)CC[C@@]4(O)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1016/j.bmcl.2012.06.056
	CHEMBL285479	213322	None	0	Human	Functional	pEC50	=	8.9	8.9	89	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human mu opioid receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay	ChEMBL		None	None	None		C[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O	10.1021/acs.jmedchem.0c02062
	CHEMBL5070150	218014	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(Cc1ccsc1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	CHEMBL5095511	218014	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(Cc1ccsc1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	CHEMBL5080352	218028	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(CCc1ccc[nH]1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	CHEMBL5095701	218028	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(CCc1ccc[nH]1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	72164176	92098	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	ChEMBL	547	4	4	7	3.7	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1nc(Cl)c2ccccc2c1O	10.1016/j.bmcl.2013.07.043
	CHEMBL2419122	92098	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	ChEMBL	547	4	4	7	3.7	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1nc(Cl)c2ccccc2c1O	10.1016/j.bmcl.2013.07.043
	72164176	92098	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	547	4	4	7	3.7	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1nc(Cl)c2ccccc2c1O	10.1016/j.bmc.2015.02.055
	CHEMBL2419122	92098	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	547	4	4	7	3.7	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1nc(Cl)c2ccccc2c1O	10.1016/j.bmc.2015.02.055
	CHEMBL5085703	217471	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Antagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method	ChEMBL		None	None	None		O=C(CCc1ncc[nH]1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.1c02185
	CHEMBL5086878	217542	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Antagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method	ChEMBL		None	None	None		O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cn[nH]c1	10.1021/acs.jmedchem.1c02185
	25233258	189852	None	0	Human	Functional	pEC50	=	8.9	8.9	-	1	Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	447	4	3	6	2.2	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1	10.1021/jm801272c
	CHEMBL515864	189852	None	0	Human	Functional	pEC50	=	8.9	8.9	-	1	Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	447	4	3	6	2.2	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1	10.1021/jm801272c
	156010967	177199	None	0	Human	Functional	pEC50	=	8.9	8.9	-1	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	570	8	1	5	6.8	Oc1ccc2c3c1O[C@H]1c4ncc(-c5ccccc5)cc4C[C@@]4(OCCCc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/acs.jmedchem.0c00503
	CHEMBL4633209	177199	None	0	Human	Functional	pEC50	=	8.9	8.9	-1	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	570	8	1	5	6.8	Oc1ccc2c3c1O[C@H]1c4ncc(-c5ccccc5)cc4C[C@@]4(OCCCc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/acs.jmedchem.0c00503
	71624665	87952	None	0	Rat	Functional	pEC50	=	8.9	8.9	-2	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	453	5	2	5	4.0	CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)C(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338756	87952	None	0	Rat	Functional	pEC50	=	8.9	8.9	-2	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	453	5	2	5	4.0	CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)C(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	146405163	173998	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	472	4	3	7	2.0	N#Cc1cnccc1C(=O)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.8b01158
	CHEMBL4540013	173998	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	472	4	3	7	2.0	N#Cc1cnccc1C(=O)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.8b01158
	16100408	141878	None	0	Rat	Functional	pEC50	=	8.9	8.9	2	4	Activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	1132	28	13	13	1.7	CCCC[C@@H](NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)OC(C)(C)C)C(=O)N[C@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm061268p
	CHEMBL386186	141878	None	0	Rat	Functional	pEC50	=	8.9	8.9	2	4	Activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	1132	28	13	13	1.7	CCCC[C@@H](NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)OC(C)(C)C)C(=O)N[C@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm061268p
	168290722	191987	None	0	Human	Functional	pEC50	=	8.9	8.9	-	1	Agonist activity at MOP in human SH-SY5Y cells assessed as forskolin stimulated cAMP accumulation incubated for 30 mins by Biotrak-EIA kit methodAgonist activity at MOP in human SH-SY5Y cells assessed as forskolin stimulated cAMP accumulation incubated for 30 mins by Biotrak-EIA kit method	ChEMBL	807	21	7	7	4.5	CCCCCCCCC(N)C(=O)N[C@@H](Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.0c01915
	CHEMBL5199625	191987	None	0	Human	Functional	pEC50	=	8.9	8.9	-	1	Agonist activity at MOP in human SH-SY5Y cells assessed as forskolin stimulated cAMP accumulation incubated for 30 mins by Biotrak-EIA kit methodAgonist activity at MOP in human SH-SY5Y cells assessed as forskolin stimulated cAMP accumulation incubated for 30 mins by Biotrak-EIA kit method	ChEMBL	807	21	7	7	4.5	CCCCCCCCC(N)C(=O)N[C@@H](Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.0c01915
	2491	3699	None	10	Human	Functional	pEC50	=	8.9	8.9	-6	3	Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay	ChEMBL	386	8	0	4	4.2	COCC1(CCN(CC1)CCc1cccs1)N(c1ccccc1)C(=O)CC	10.1021/acs.jmedchem.8b00435
	3534	3699	None	10	Human	Functional	pEC50	=	8.9	8.9	-6	3	Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay	ChEMBL	386	8	0	4	4.2	COCC1(CCN(CC1)CCc1cccs1)N(c1ccccc1)C(=O)CC	10.1021/acs.jmedchem.8b00435
	41693	3699	None	10	Human	Functional	pEC50	=	8.9	8.9	-6	3	Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay	ChEMBL	386	8	0	4	4.2	COCC1(CCN(CC1)CCc1cccs1)N(c1ccccc1)C(=O)CC	10.1021/acs.jmedchem.8b00435
	41693.0	3699	None	10	Human	Functional	pEC50	=	8.9	8.9	-6	3	Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay	ChEMBL	386	8	0	4	4.2	COCC1(CCN(CC1)CCc1cccs1)N(c1ccccc1)C(=O)CC	10.1021/acs.jmedchem.8b00435
	CHEMBL658	3699	None	10	Human	Functional	pEC50	=	8.9	8.9	-6	3	Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay	ChEMBL	386	8	0	4	4.2	COCC1(CCN(CC1)CCc1cccs1)N(c1ccccc1)C(=O)CC	10.1021/acs.jmedchem.8b00435
	DB00708	3699	None	10	Human	Functional	pEC50	=	8.9	8.9	-6	3	Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay	ChEMBL	386	8	0	4	4.2	COCC1(CCN(CC1)CCc1cccs1)N(c1ccccc1)C(=O)CC	10.1021/acs.jmedchem.8b00435
	44427183	92172	None	0	Human	Functional	pEC50	=	8.9	8.9	-2	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	ChEMBL	430	4	1	3	6.2	O=C(Nc1ccccc1)Oc1ccc2c(c1)C13CCCCC1C(C2)N(CC1CCC1)CC3	10.1016/j.bmcl.2007.01.013
	CHEMBL242048	92172	None	0	Human	Functional	pEC50	=	8.9	8.9	-2	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	ChEMBL	430	4	1	3	6.2	O=C(Nc1ccccc1)Oc1ccc2c(c1)C13CCCCC1C(C2)N(CC1CCC1)CC3	10.1016/j.bmcl.2007.01.013
	71454514	79174	None	0	Human	Functional	pEC50	=	8.9	8.9	1	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	531	6	2	7	3.6	CO[C@@]12CC[C@@]3(C[C@@H]1CNC(=O)/C=C/c1ccc([N+](=O)[O-])cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1021/jm070255o
	CHEMBL2113308	79174	None	0	Human	Functional	pEC50	=	8.9	8.9	1	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	531	6	2	7	3.6	CO[C@@]12CC[C@@]3(C[C@@H]1CNC(=O)/C=C/c1ccc([N+](=O)[O-])cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1021/jm070255o
	9897164	39697	None	0	Human	Functional	pEC50	=	8.9	8.9	-5	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	789	15	0	6	11.0	O=C(CCCCCCCCC(=O)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	10.1021/jm900379p
	CHEMBL147511	39697	None	0	Human	Functional	pEC50	=	8.9	8.9	-5	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	789	15	0	6	11.0	O=C(CCCCCCCCC(=O)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	10.1021/jm900379p
	1613	2297	None	29	Human	Functional	pEC50	=	8.9	8.9	-51	7	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c00530
	3903	2297	None	29	Human	Functional	pEC50	=	8.9	8.9	-51	7	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c00530
	461776	2297	None	29	Human	Functional	pEC50	=	8.9	8.9	-51	7	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c00530
	CHEMBL15038	2297	None	29	Human	Functional	pEC50	=	8.9	8.9	-51	7	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c00530
	CHEMBL8234	2297	None	29	Human	Functional	pEC50	=	8.9	8.9	-51	7	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c00530
	25259957	188736	None	0	Rat	Functional	pEC50	=	8.9	8.9	-2	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	590	8	2	6	4.9	O=C(/C=C/c1ccccc1)N[C@@H]1CC[C@@]2(OC(=O)Cc3ccccc3)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/jm8015552
	CHEMBL503017	188736	None	0	Rat	Functional	pEC50	=	8.9	8.9	-2	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	590	8	2	6	4.9	O=C(/C=C/c1ccccc1)N[C@@H]1CC[C@@]2(OC(=O)Cc3ccccc3)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/jm8015552
	71624662	87948	None	0	Rat	Functional	pEC50	=	8.9	8.9	-18	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	501	6	2	5	4.6	CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)Cc1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338752	87948	None	0	Rat	Functional	pEC50	=	8.9	8.9	-18	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	501	6	2	5	4.6	CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)Cc1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	86291190	160879	None	0	Human	Functional	pEC50	=	8.9	8.9	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	338	3	1	2	3.6	C[C@H](C1CC1)N1CC[C@]23CCCC[C@H]2[C@H]1Cc1ccc(C(N)=O)cc13	nan
	CHEMBL4114285	160879	None	0	Human	Functional	pEC50	=	8.9	8.9	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	338	3	1	2	3.6	C[C@H](C1CC1)N1CC[C@]23CCCC[C@H]2[C@H]1Cc1ccc(C(N)=O)cc13	nan
	9897164	39697	None	0	Human	Functional	pEC50	=	8.9	8.9	-5	2	Partial agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS bindingPartial agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding	ChEMBL	789	15	0	6	11.0	O=C(CCCCCCCCC(=O)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	10.1016/j.ejmech.2015.11.028
	CHEMBL147511	39697	None	0	Human	Functional	pEC50	=	8.9	8.9	-5	2	Partial agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS bindingPartial agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding	ChEMBL	789	15	0	6	11.0	O=C(CCCCCCCCC(=O)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	10.1016/j.ejmech.2015.11.028
	56675713	66616	None	0	Human	Functional	pEC50	=	8.9	8.9	-	1	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	525	4	3	6	2.9	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1Br	10.1016/j.bmcl.2011.06.135
	CHEMBL1824513	66616	None	0	Human	Functional	pEC50	=	8.9	8.9	-	1	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	525	4	3	6	2.9	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1Br	10.1016/j.bmcl.2011.06.135
	CHEMBL1852602	66616	None	0	Human	Functional	pEC50	=	8.9	8.9	-	1	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	525	4	3	6	2.9	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1Br	10.1016/j.bmcl.2011.06.135
	CHEMBL5090637	218053	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(CCc1ccco1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	CHEMBL5095967	218053	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(CCc1ccco1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	137633728	156398	None	0	Human	Functional	pEC50	=	8.9	8.9	-	1	Agonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	301	1	1	4	2.2	CO[C@@]12CCC[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5	10.1021/acs.jmedchem.7b01363
	CHEMBL4065490	156398	None	0	Human	Functional	pEC50	=	8.9	8.9	-	1	Agonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	301	1	1	4	2.2	CO[C@@]12CCC[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5	10.1021/acs.jmedchem.7b01363
	73330543	92862	None	0	Mouse	Functional	pEC50	=	8.9	8.9	6	3	Agonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopyAgonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopy	ChEMBL	414	3	2	4	3.0	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@H](NC(=O)/C=C/c2ccccc2)C=C[C@H]3[C@H]1C5	10.1039/C6MD00450D
	CHEMBL2437063	92862	None	0	Mouse	Functional	pEC50	=	8.9	8.9	6	3	Agonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopyAgonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopy	ChEMBL	414	3	2	4	3.0	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@H](NC(=O)/C=C/c2ccccc2)C=C[C@H]3[C@H]1C5	10.1039/C6MD00450D
	73330543	92862	None	0	Mouse	Functional	pEC50	=	8.9	8.9	6	3	Agonist activity at mouse cloned mu opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at mouse cloned mu opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	414	3	2	4	3.0	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@H](NC(=O)/C=C/c2ccccc2)C=C[C@H]3[C@H]1C5	10.1016/j.ejmech.2013.09.031
	CHEMBL2437063	92862	None	0	Mouse	Functional	pEC50	=	8.9	8.9	6	3	Agonist activity at mouse cloned mu opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at mouse cloned mu opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	414	3	2	4	3.0	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@H](NC(=O)/C=C/c2ccccc2)C=C[C@H]3[C@H]1C5	10.1016/j.ejmech.2013.09.031
	146408970	172021	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	515	4	3	6	3.2	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1C(F)(F)F	10.1021/acs.jmedchem.8b01158
	CHEMBL4469986	172021	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	515	4	3	6	3.2	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1C(F)(F)F	10.1021/acs.jmedchem.8b01158
	CHEMBL382051	214753	None	0	Rat	Functional	pEC50	=	8.9	8.9	-8	5	Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/jm050921q
	155523378	170925	None	0	Mouse	Functional	pEC50	=	8.9	8.9	138	3	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 analysisAgonist 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	ChEMBL	384	4	1	6	2.9	CC[C@@H]1CN2CC[C@]3(Nc4ccccc4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.6b00748
	CHEMBL4453504	170925	None	0	Mouse	Functional	pEC50	=	8.9	8.9	138	3	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 analysisAgonist 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	ChEMBL	384	4	1	6	2.9	CC[C@@H]1CN2CC[C@]3(Nc4ccccc4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.6b00748
	155526934	171235	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-1	6	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 analysisAgonist 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	ChEMBL	460	5	1	6	4.5	CC[C@@H]1CN2CC[C@]3(Nc4cccc(-c5ccccc5)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.6b00748
	CHEMBL4458337	171235	None	0	Mouse	Functional	pEC50	=	8.9	8.9	-1	6	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 analysisAgonist 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	ChEMBL	460	5	1	6	4.5	CC[C@@H]1CN2CC[C@]3(Nc4cccc(-c5ccccc5)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.6b00748
	CHEMBL2387216	212864	None	0	Rat	Functional	pEC50	=	8.9	8.9	5	3	Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)NCCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2013.03.065
	122179052	121459	None	0	Rat	Functional	pEC50	=	8.9	8.9	10	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	499	5	2	5	4.8	CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/acs.jmedchem.5b00130
	CHEMBL3581741	121459	None	0	Rat	Functional	pEC50	=	8.9	8.9	10	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	499	5	2	5	4.8	CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/acs.jmedchem.5b00130
	56847097	161055	None	0	Human	Functional	pEC50	=	8.9	8.9	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	370	3	3	4	2.5	NC(=O)c1ccc2c(c1O)[C@@]13CCCC[C@@]1(O)[C@@H](C2)N(CC1CCC1)CC3	nan
	CHEMBL4115660	161055	None	0	Human	Functional	pEC50	=	8.9	8.9	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	370	3	3	4	2.5	NC(=O)c1ccc2c(c1O)[C@@]13CCCC[C@@]1(O)[C@@H](C2)N(CC1CCC1)CC3	nan
	155526934	171235	None	0	Human	Functional	pEC50	=	8.9	8.9	-1	6	Inhibition of mu opioid receptor (unknown origin) in presence of DAMGO by [35S]-GTPgammaS binding assayInhibition of mu opioid receptor (unknown origin) in presence of DAMGO by [35S]-GTPgammaS binding assay	ChEMBL	460	5	1	6	4.5	CC[C@@H]1CN2CC[C@]3(Nc4cccc(-c5ccccc5)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1016/j.ejmech.2019.111701
	CHEMBL4458337	171235	None	0	Human	Functional	pEC50	=	8.9	8.9	-1	6	Inhibition of mu opioid receptor (unknown origin) in presence of DAMGO by [35S]-GTPgammaS binding assayInhibition of mu opioid receptor (unknown origin) in presence of DAMGO by [35S]-GTPgammaS binding assay	ChEMBL	460	5	1	6	4.5	CC[C@@H]1CN2CC[C@]3(Nc4cccc(-c5ccccc5)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1016/j.ejmech.2019.111701
	155526934	171235	None	0	Human	Functional	pEC50	=	8.9	8.9	-1	6	Inhibition of mu opioid receptor (unknown origin) in presence of DPDPE by [35S]-GTPgammaS binding assayInhibition of mu opioid receptor (unknown origin) in presence of DPDPE by [35S]-GTPgammaS binding assay	ChEMBL	460	5	1	6	4.5	CC[C@@H]1CN2CC[C@]3(Nc4cccc(-c5ccccc5)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1016/j.ejmech.2019.111701
	CHEMBL4458337	171235	None	0	Human	Functional	pEC50	=	8.9	8.9	-1	6	Inhibition of mu opioid receptor (unknown origin) in presence of DPDPE by [35S]-GTPgammaS binding assayInhibition of mu opioid receptor (unknown origin) in presence of DPDPE by [35S]-GTPgammaS binding assay	ChEMBL	460	5	1	6	4.5	CC[C@@H]1CN2CC[C@]3(Nc4cccc(-c5ccccc5)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1016/j.ejmech.2019.111701
	CHEMBL382051	214753	None	0	Rat	Functional	pEC50	=	8.8	8.8	-8	5	Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/jm050921q
	168294718	192577	None	0	Human	Functional	pEC50	=	8.8	8.8	-	1	Agonist activity at MOP (unknown origin) stably expressed in HEK293 cells assessed as forskolin stimulated cAMP accumulation incubated for 30 mins by radioactivity based scintillation counter analysisAgonist activity at MOP (unknown origin) stably expressed in HEK293 cells assessed as forskolin stimulated cAMP accumulation incubated for 30 mins by radioactivity based scintillation counter analysis	ChEMBL	600	13	6	7	1.8	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](C)N(C)C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1	10.1021/acs.jmedchem.0c01915
	CHEMBL5208747	192577	None	0	Human	Functional	pEC50	=	8.8	8.8	-	1	Agonist activity at MOP (unknown origin) stably expressed in HEK293 cells assessed as forskolin stimulated cAMP accumulation incubated for 30 mins by radioactivity based scintillation counter analysisAgonist activity at MOP (unknown origin) stably expressed in HEK293 cells assessed as forskolin stimulated cAMP accumulation incubated for 30 mins by radioactivity based scintillation counter analysis	ChEMBL	600	13	6	7	1.8	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](C)N(C)C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1	10.1021/acs.jmedchem.0c01915
	13559325	204355	None	1	Human	Functional	pEC50	=	8.8	8.8	12	4	Agonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	315	1	1	5	1.4	CO[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5	10.1021/acs.jmedchem.7b01363
	CHEMBL607405	204355	None	1	Human	Functional	pEC50	=	8.8	8.8	12	4	Agonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	315	1	1	5	1.4	CO[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5	10.1021/acs.jmedchem.7b01363
	56665405	66604	None	0	Human	Functional	pEC50	=	8.8	8.8	-	1	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	475	6	3	6	2.5	O=C(CCc1ccncc1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2011.06.135
	CHEMBL1824511	66604	None	0	Human	Functional	pEC50	=	8.8	8.8	-	1	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	475	6	3	6	2.5	O=C(CCc1ccncc1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2011.06.135
	CHEMBL1852555	66604	None	0	Human	Functional	pEC50	=	8.8	8.8	-	1	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	475	6	3	6	2.5	O=C(CCc1ccncc1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2011.06.135
	146408932	172606	None	0	Mouse	Functional	pEC50	=	8.8	8.8	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	523	5	3	6	3.8	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1-c1ccccc1	10.1021/acs.jmedchem.8b01158
	CHEMBL4483410	172606	None	0	Mouse	Functional	pEC50	=	8.8	8.8	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	523	5	3	6	3.8	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1-c1ccccc1	10.1021/acs.jmedchem.8b01158
	121427906	191776	None	0	Human	Functional	pEC50	=	8.8	8.8	-	1	Agonist activity at human MOP expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS bindingAgonist activity at human MOP expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS binding	ChEMBL	713	9	8	8	0.3	NC(=O)[C@@H]1CCCCNC(=O)CC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1	10.1021/acs.jmedchem.0c01915
	CHEMBL5196331	191776	None	0	Human	Functional	pEC50	=	8.8	8.8	-	1	Agonist activity at human MOP expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS bindingAgonist activity at human MOP expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS binding	ChEMBL	713	9	8	8	0.3	NC(=O)[C@@H]1CCCCNC(=O)CC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1	10.1021/acs.jmedchem.0c01915
	156009540	177254	None	0	Human	Functional	pEC50	=	8.8	8.8	2	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	613	9	1	6	6.9	CN(C)c1cccc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)c1	10.1021/acs.jmedchem.0c00503
	CHEMBL4634021	177254	None	0	Human	Functional	pEC50	=	8.8	8.8	2	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	613	9	1	6	6.9	CN(C)c1cccc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)c1	10.1021/acs.jmedchem.0c00503
	155515067	170043	None	0	Mouse	Functional	pEC50	=	8.8	8.8	25	3	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 analysisAgonist 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	ChEMBL	450	5	1	7	4.1	CC[C@@H]1CN2CC[C@]3(Nc4cccc(-c5ccoc5)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.6b00748
	CHEMBL4441457	170043	None	0	Mouse	Functional	pEC50	=	8.8	8.8	25	3	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 analysisAgonist 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	ChEMBL	450	5	1	7	4.1	CC[C@@H]1CN2CC[C@]3(Nc4cccc(-c5ccoc5)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.6b00748
	127050830	141141	None	0	Rat	Functional	pEC50	=	8.8	8.8	177	3	Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay	ChEMBL	486	8	4	5	3.0	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(CC(N)=O)c2ccc(Cc3ccccc3)cc21	10.1021/acs.jmedchem.6b00308
	CHEMBL3824309	141141	None	0	Rat	Functional	pEC50	=	8.8	8.8	177	3	Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay	ChEMBL	486	8	4	5	3.0	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(CC(N)=O)c2ccc(Cc3ccccc3)cc21	10.1021/acs.jmedchem.6b00308
	CHEMBL2387214	212862	None	0	Rat	Functional	pEC50	=	8.8	8.8	-6	3	Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL		None	None	None		CC(C)C[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)NCCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)C(=O)O	10.1016/j.bmcl.2013.03.065
	71625148	87935	None	0	Rat	Functional	pEC50	=	8.8	8.8	-36	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	467	7	2	5	4.4	CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)CCC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338739	87935	None	0	Rat	Functional	pEC50	=	8.8	8.8	-36	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	467	7	2	5	4.4	CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)CCC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	86582597	160909	None	0	Human	Functional	pEC50	=	8.8	8.8	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	370	3	3	4	2.3	NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@@H]1CC[C@@H](O)C3	nan
	CHEMBL4114524	160909	None	0	Human	Functional	pEC50	=	8.8	8.8	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	370	3	3	4	2.3	NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@@H]1CC[C@@H](O)C3	nan
	71456106	84206	None	0	Human	Functional	pEC50	=	8.8	8.8	-114	3	Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	494	7	2	3	6.0	CC1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccccc5O)cc4)cc3C1(C)CCN2CC1CC1	10.1016/j.bmcl.2012.10.081
	CHEMBL2208349	84206	None	0	Human	Functional	pEC50	=	8.8	8.8	-114	3	Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	494	7	2	3	6.0	CC1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccccc5O)cc4)cc3C1(C)CCN2CC1CC1	10.1016/j.bmcl.2012.10.081
	53388149	66555	None	1	Human	Functional	pEC50	=	8.8	8.8	17	3	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	461	4	3	6	2.5	Cc1cnccc1C(=O)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2011.06.135
	CHEMBL1824515	66555	None	1	Human	Functional	pEC50	=	8.8	8.8	17	3	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	461	4	3	6	2.5	Cc1cnccc1C(=O)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2011.06.135
	CHEMBL1852393	66555	None	1	Human	Functional	pEC50	=	8.8	8.8	17	3	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	461	4	3	6	2.5	Cc1cnccc1C(=O)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2011.06.135
	CHEMBL5094575	217992	None	0	Mouse	Functional	pEC50	=	8.8	8.8	-	1	Antagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method	ChEMBL		None	None	None		O=C(Cc1cn[nH]c1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.1c02185
	CHEMBL5076910	218021	None	0	Mouse	Functional	pEC50	=	8.8	8.8	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(CCc1cccs1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	CHEMBL5095595	218021	None	0	Mouse	Functional	pEC50	=	8.8	8.8	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(CCc1cccs1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	90306849	111018	None	0	Human	Functional	pEC50	=	8.8	8.8	-4	3	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysis	ChEMBL	473	5	2	5	4.4	CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm401964y
	CHEMBL3262092	111018	None	0	Human	Functional	pEC50	=	8.8	8.8	-4	3	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysis	ChEMBL	473	5	2	5	4.4	CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm401964y
	3668	1561	None	36	Human	Functional	pEC50	=	8.8	8.8	1	5	Agonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01915
	5311081	1561	None	36	Human	Functional	pEC50	=	8.8	8.8	1	5	Agonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01915
	CHEMBL333357	1561	None	36	Human	Functional	pEC50	=	8.8	8.8	1	5	Agonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01915
	CHEMBL589982	1561	None	36	Human	Functional	pEC50	=	8.8	8.8	1	5	Agonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01915
	155513830	176557	None	0	Mouse	Functional	pEC50	=	8.8	8.8	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1coc2ccccc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4439476	176557	None	0	Mouse	Functional	pEC50	=	8.8	8.8	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1coc2ccccc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4596411	176557	None	0	Mouse	Functional	pEC50	=	8.8	8.8	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1coc2ccccc12	10.1021/acs.jmedchem.9b01767
	164623602	188684	None	0	Human	Functional	pEC50	=	8.8	8.8	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1n[nH]c2ccccc12	10.1016/j.bmcl.2021.127953
	CHEMBL4862035	188684	None	0	Human	Functional	pEC50	=	8.8	8.8	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1n[nH]c2ccccc12	10.1016/j.bmcl.2021.127953
	CHEMBL5028768	188684	None	0	Human	Functional	pEC50	=	8.8	8.8	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1n[nH]c2ccccc12	10.1016/j.bmcl.2021.127953
	9804450	101996	None	2	Human	Functional	pEC50	=	8.8	8.8	-4	2	Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	311	2	1	2	4.3	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	10.1021/jm050577x
	CHEMBL301160	101996	None	2	Human	Functional	pEC50	=	8.8	8.8	-4	2	Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	311	2	1	2	4.3	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	10.1021/jm050577x
	9804450	101996	None	2	Human	Functional	pEC50	=	8.8	8.8	-4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	ChEMBL	311	2	1	2	4.3	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	10.1016/j.bmcl.2007.01.013
	CHEMBL301160	101996	None	2	Human	Functional	pEC50	=	8.8	8.8	-4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	ChEMBL	311	2	1	2	4.3	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	10.1016/j.bmcl.2007.01.013
	9804450	101996	None	2	Human	Functional	pEC50	=	8.8	8.8	-4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	311	2	1	2	4.3	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	10.1021/jm3001086
	CHEMBL301160	101996	None	2	Human	Functional	pEC50	=	8.8	8.8	-4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	311	2	1	2	4.3	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	10.1021/jm3001086
	9804450	101996	None	2	Human	Functional	pEC50	=	8.8	8.8	-4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 minsAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins	ChEMBL	311	2	1	2	4.3	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	10.1016/j.bmc.2007.03.076
	CHEMBL301160	101996	None	2	Human	Functional	pEC50	=	8.8	8.8	-4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 minsAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins	ChEMBL	311	2	1	2	4.3	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	10.1016/j.bmc.2007.03.076
	9804450	101996	None	2	Human	Functional	pEC50	=	8.8	8.8	-4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	311	2	1	2	4.3	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	10.1021/jm900379p
	CHEMBL301160	101996	None	2	Human	Functional	pEC50	=	8.8	8.8	-4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	311	2	1	2	4.3	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	10.1021/jm900379p
	44592088	179116	None	0	Human	Functional	pEC50	=	8.8	8.8	2	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	314	1	2	4	1.4	CN1CC[C@]23CC(=O)CC[C@H]2[C@H]1Cc1ccc(C(N)=O)c(O)c13	10.1016/j.bmcl.2009.02.078
	CHEMBL471048	179116	None	0	Human	Functional	pEC50	=	8.8	8.8	2	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	314	1	2	4	1.4	CN1CC[C@]23CC(=O)CC[C@H]2[C@H]1Cc1ccc(C(N)=O)c(O)c13	10.1016/j.bmcl.2009.02.078
	9804450	101996	None	2	Human	Functional	pEC50	=	8.8	8.8	-4	2	Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	311	2	1	2	4.3	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	10.1021/jm061327z
	CHEMBL301160	101996	None	2	Human	Functional	pEC50	=	8.8	8.8	-4	2	Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	311	2	1	2	4.3	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	10.1021/jm061327z
	10320450	86885	None	0	Rat	Functional	pEC50	=	8.8	8.8	69	3	Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	429	6	4	4	4.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21	10.1021/jm400050y
	CHEMBL2322568	86885	None	0	Rat	Functional	pEC50	=	8.8	8.8	69	3	Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	429	6	4	4	4.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21	10.1021/jm400050y
	CHEMBL4444479	86885	None	0	Rat	Functional	pEC50	=	8.8	8.8	69	3	Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	429	6	4	4	4.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21	10.1021/jm400050y
	10320450	86885	None	0	Rat	Functional	pEC50	=	8.8	8.8	69	3	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	429	6	4	4	4.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL2322568	86885	None	0	Rat	Functional	pEC50	=	8.8	8.8	69	3	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	429	6	4	4	4.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4444479	86885	None	0	Rat	Functional	pEC50	=	8.8	8.8	69	3	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	429	6	4	4	4.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21	10.1021/acs.jmedchem.9b00378
	122187724	123132	None	0	Rat	Functional	pEC50	=	8.8	8.8	7	3	Agonist activity at rat mu opioid receptor transfected in HN9.10 cells by [35S]GTPgammaS binding assayAgonist activity at rat mu opioid receptor transfected in HN9.10 cells by [35S]GTPgammaS binding assay	ChEMBL	692	11	5	6	5.4	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1016/j.bmcl.2015.06.030
	CHEMBL3609620	123132	None	0	Rat	Functional	pEC50	=	8.8	8.8	7	3	Agonist activity at rat mu opioid receptor transfected in HN9.10 cells by [35S]GTPgammaS binding assayAgonist activity at rat mu opioid receptor transfected in HN9.10 cells by [35S]GTPgammaS binding assay	ChEMBL	692	11	5	6	5.4	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1016/j.bmcl.2015.06.030
	10320450	86885	None	0	Rat	Functional	pEC50	=	8.8	8.8	69	3	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	429	6	4	4	4.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21	10.1021/acs.jmedchem.5b01270
	CHEMBL2322568	86885	None	0	Rat	Functional	pEC50	=	8.8	8.8	69	3	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	429	6	4	4	4.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21	10.1021/acs.jmedchem.5b01270
	CHEMBL4444479	86885	None	0	Rat	Functional	pEC50	=	8.8	8.8	69	3	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	429	6	4	4	4.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21	10.1021/acs.jmedchem.5b01270
	9804450	101996	None	2	Human	Functional	pEC50	=	8.8	8.8	-4	2	Agonistic activity against Opioid receptor mu 1 in Chinese hamster ovary membranesAgonistic activity against Opioid receptor mu 1 in Chinese hamster ovary membranes	ChEMBL	311	2	1	2	4.3	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	10.1021/jm049978n
	CHEMBL301160	101996	None	2	Human	Functional	pEC50	=	8.8	8.8	-4	2	Agonistic activity against Opioid receptor mu 1 in Chinese hamster ovary membranesAgonistic activity against Opioid receptor mu 1 in Chinese hamster ovary membranes	ChEMBL	311	2	1	2	4.3	Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	10.1021/jm049978n
	71454362	84207	None	0	Human	Functional	pEC50	=	8.8	8.8	-2	3	Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	538	9	1	4	6.3	COc1ccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)cc1OC	10.1016/j.bmcl.2012.10.081
	CHEMBL2208350	84207	None	0	Human	Functional	pEC50	=	8.8	8.8	-2	3	Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	538	9	1	4	6.3	COc1ccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)cc1OC	10.1016/j.bmcl.2012.10.081
	CHEMBL5088671	218051	None	0	Mouse	Functional	pEC50	=	8.8	8.8	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(CCc1cc[nH]c1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	CHEMBL5095948	218051	None	0	Mouse	Functional	pEC50	=	8.8	8.8	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(CCc1cc[nH]c1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	156010419	177260	None	0	Human	Functional	pEC50	=	8.8	8.8	-1	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	559	8	1	6	5.9	Oc1ccc2c3c1O[C@H]1c4ncc(-n5cccc5)cc4C[C@@]4(OCCCc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/acs.jmedchem.0c00503
	CHEMBL4634079	177260	None	0	Human	Functional	pEC50	=	8.8	8.8	-1	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	559	8	1	6	5.9	Oc1ccc2c3c1O[C@H]1c4ncc(-n5cccc5)cc4C[C@@]4(OCCCc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/acs.jmedchem.0c00503
	CHEMBL331325	213821	None	2	Human	Functional	pEC50	=	8.8	8.8	1	2	Agonist activity at human recombinant MOR expressed in CHO cells co-expressing C-terminally modified Galphaqi5 assessed as induction of calcium mobilization by Fluo-4AM dye-based fluorescence assayAgonist activity at human recombinant MOR expressed in CHO cells co-expressing C-terminally modified Galphaqi5 assessed as induction of calcium mobilization by Fluo-4AM dye-based fluorescence assay	ChEMBL		None	None	None		Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.ejmech.2019.06.077
	CHEMBL3580749	214236	None	0	Human	Functional	pEC50	=	8.8	8.8	-5	6	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 assayAgonist 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	ChEMBL		None	None	None		Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(F)cc2F)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.5b00056
	1647	1313	None	34	Human	Functional	pEC50	=	8.8	8.8	-3	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL		None	None	None		None	10.1021/jm701440h
	5462471	1313	None	34	Human	Functional	pEC50	=	8.8	8.8	-3	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL		None	None	None		None	10.1021/jm701440h
	CHEMBL113995	1313	None	34	Human	Functional	pEC50	=	8.8	8.8	-3	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL		None	None	None		None	10.1021/jm701440h
	CHEMBL38874	1313	None	34	Human	Functional	pEC50	=	8.8	8.8	-3	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL		None	None	None		None	10.1021/jm701440h
	16720551	85358	None	0	Human	Functional	pEC50	=	8.8	8.8	-18	3	Agonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	398	3	1	2	4.9	COc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@@H]1Cc1c([nH]c2ccccc12)C3	10.1021/jm0701674
	CHEMBL226113	85358	None	0	Human	Functional	pEC50	=	8.8	8.8	-18	3	Agonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	398	3	1	2	4.9	COc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@@H]1Cc1c([nH]c2ccccc12)C3	10.1021/jm0701674
	54584041	61804	None	0	Human	Functional	pEC50	=	8.8	8.8	1	2	Agonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	615	15	0	6	8.1	CO[C@@]12CCCC[C@@]13CCN(CC1CCC1)[C@@H]2Cc1ccc(OC(=O)CCCCCCCCC(=O)OCc2ccccc2)cc13	10.1016/j.bmc.2011.03.052
	CHEMBL1773091	61804	None	0	Human	Functional	pEC50	=	8.8	8.8	1	2	Agonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	615	15	0	6	8.1	CO[C@@]12CCCC[C@@]13CCN(CC1CCC1)[C@@H]2Cc1ccc(OC(=O)CCCCCCCCC(=O)OCc2ccccc2)cc13	10.1016/j.bmc.2011.03.052
	44301701	201281	None	4	Mouse	Functional	pEC50	=	8.8	8.8	-1	6	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 analysisAgonist 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	ChEMBL	414	5	1	7	2.9	CC[C@@H]1CN2CC[C@]3(Nc4cccc(OC)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.6b00748
	CHEMBL58362	201281	None	4	Mouse	Functional	pEC50	=	8.8	8.8	-1	6	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 analysisAgonist 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	ChEMBL	414	5	1	7	2.9	CC[C@@H]1CN2CC[C@]3(Nc4cccc(OC)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.6b00748
	71624555	87946	None	0	Rat	Functional	pEC50	=	8.8	8.8	-100	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	507	6	2	5	5.3	CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338750	87946	None	0	Rat	Functional	pEC50	=	8.8	8.8	-100	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	507	6	2	5	5.3	CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	44301701	201281	None	4	Human	Functional	pEC50	=	8.8	8.8	-2	6	Inhibition of mu opioid receptor (unknown origin) in presence of DAMGO by [35S]-GTPgammaS binding assayInhibition of mu opioid receptor (unknown origin) in presence of DAMGO by [35S]-GTPgammaS binding assay	ChEMBL	414	5	1	7	2.9	CC[C@@H]1CN2CC[C@]3(Nc4cccc(OC)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1016/j.ejmech.2019.111701
	CHEMBL58362	201281	None	4	Human	Functional	pEC50	=	8.8	8.8	-2	6	Inhibition of mu opioid receptor (unknown origin) in presence of DAMGO by [35S]-GTPgammaS binding assayInhibition of mu opioid receptor (unknown origin) in presence of DAMGO by [35S]-GTPgammaS binding assay	ChEMBL	414	5	1	7	2.9	CC[C@@H]1CN2CC[C@]3(Nc4cccc(OC)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1016/j.ejmech.2019.111701
	44301701	201281	None	4	Human	Functional	pEC50	=	8.8	8.8	-2	6	Inhibition of mu opioid receptor (unknown origin) in presence of DPDPE by [35S]-GTPgammaS binding assayInhibition of mu opioid receptor (unknown origin) in presence of DPDPE by [35S]-GTPgammaS binding assay	ChEMBL	414	5	1	7	2.9	CC[C@@H]1CN2CC[C@]3(Nc4cccc(OC)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1016/j.ejmech.2019.111701
	CHEMBL58362	201281	None	4	Human	Functional	pEC50	=	8.8	8.8	-2	6	Inhibition of mu opioid receptor (unknown origin) in presence of DPDPE by [35S]-GTPgammaS binding assayInhibition of mu opioid receptor (unknown origin) in presence of DPDPE by [35S]-GTPgammaS binding assay	ChEMBL	414	5	1	7	2.9	CC[C@@H]1CN2CC[C@]3(Nc4cccc(OC)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1016/j.ejmech.2019.111701
	44240972	88198	None	0	Human	Functional	pEC50	=	8.8	8.8	-6	2	Partial 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 countingPartial 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	ChEMBL	479	7	1	3	5.7	C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccccn5)cc4)cc3[C@@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2013.01.117
	CHEMBL2347237	88198	None	0	Human	Functional	pEC50	=	8.8	8.8	-6	2	Partial 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 countingPartial 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	ChEMBL	479	7	1	3	5.7	C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccccn5)cc4)cc3[C@@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2013.01.117
	168269196	190117	None	0	Human	Functional	pEC50	=	8.8	8.8	-6	3	Agonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assay	ChEMBL	699	7	8	8	0.7	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](c2ccccc2)NC(=O)[C@H](c2ccccc2)NC1=O	10.1021/acs.jmedchem.0c01915
	CHEMBL5171420	190117	None	0	Human	Functional	pEC50	=	8.8	8.8	-6	3	Agonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assay	ChEMBL	699	7	8	8	0.7	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](c2ccccc2)NC(=O)[C@H](c2ccccc2)NC1=O	10.1021/acs.jmedchem.0c01915
	71460942	82740	None	0	Human	Functional	pEC50	=	8.8	8.8	1	3	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting analysisAgonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting analysis	ChEMBL	604	8	1	5	7.5	Oc1ccc2c3c1O[C@H]1c4ncc(-c5ccc(Cl)cc5)cc4C[C@@]4(OCCCc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/jm300686p
	CHEMBL2179652	82740	None	0	Human	Functional	pEC50	=	8.8	8.8	1	3	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting analysisAgonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting analysis	ChEMBL	604	8	1	5	7.5	Oc1ccc2c3c1O[C@H]1c4ncc(-c5ccc(Cl)cc5)cc4C[C@@]4(OCCCc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/jm300686p
	72164175	92097	None	0	Mouse	Functional	pEC50	=	8.8	8.8	13	4	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	ChEMBL	561	5	3	7	4.0	COc1c(C(=O)N[C@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)nc(Cl)c2ccccc12	10.1016/j.bmcl.2013.07.043
	CHEMBL2419121	92097	None	0	Mouse	Functional	pEC50	=	8.8	8.8	13	4	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	ChEMBL	561	5	3	7	4.0	COc1c(C(=O)N[C@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)nc(Cl)c2ccccc12	10.1016/j.bmcl.2013.07.043
	CHEMBL5073556	216786	None	0	Mouse	Functional	pEC50	=	8.8	8.8	-	1	Antagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method	ChEMBL		None	None	None		O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ncc[nH]1	10.1021/acs.jmedchem.1c02185
	72164175	92097	None	0	Mouse	Functional	pEC50	=	8.8	8.8	13	4	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	561	5	3	7	4.0	COc1c(C(=O)N[C@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)nc(Cl)c2ccccc12	10.1016/j.bmc.2015.02.055
	CHEMBL2419121	92097	None	0	Mouse	Functional	pEC50	=	8.8	8.8	13	4	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	561	5	3	7	4.0	COc1c(C(=O)N[C@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)nc(Cl)c2ccccc12	10.1016/j.bmc.2015.02.055
	CHEMBL5093110	217897	None	0	Mouse	Functional	pEC50	=	8.8	8.8	-	1	Antagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method	ChEMBL		None	None	None		O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cn[nH]c1	10.1021/acs.jmedchem.1c02185
	71454517	79179	None	0	Human	Functional	pEC50	=	8.7	8.7	1	2	Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	510	3	1	5	3.7	CO[C@@]12C=C[C@@]3([C@@H]4CN(C(=O)/C=C/c5ccccc5C)C[C@@H]41)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1021/jm070255o
	CHEMBL2113313	79179	None	0	Human	Functional	pEC50	=	8.7	8.7	1	2	Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	510	3	1	5	3.7	CO[C@@]12C=C[C@@]3([C@@H]4CN(C(=O)/C=C/c5ccccc5C)C[C@@H]41)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1021/jm070255o
	54586810	62095	None	0	Human	Functional	pEC50	=	8.7	8.7	-3	2	Agonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	849	17	0	8	10.6	CO[C@@]12CCCC[C@@]13CCN(CC1CCC1)[C@@H]2Cc1ccc(OC(=O)CCCCCCCCC(=O)Oc2ccc4c(c2)[C@@]25CCCC[C@@]2(OC)[C@@H](C4)N(CC2CCC2)CC5)cc13	10.1016/j.bmc.2011.03.052
	CHEMBL1774947	62095	None	0	Human	Functional	pEC50	=	8.7	8.7	-3	2	Agonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	849	17	0	8	10.6	CO[C@@]12CCCC[C@@]13CCN(CC1CCC1)[C@@H]2Cc1ccc(OC(=O)CCCCCCCCC(=O)Oc2ccc4c(c2)[C@@]25CCCC[C@@]2(OC)[C@@H](C4)N(CC2CCC2)CC5)cc13	10.1016/j.bmc.2011.03.052
	66553195	93198	None	26	Human	Functional	pEC50	=	8.7	8.7	-1	5	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL	386	7	1	5	4.7	COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1	10.1016/j.ejmech.2021.113986
	66553195.0	93198	None	26	Human	Functional	pEC50	=	8.7	8.7	-1	5	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL	386	7	1	5	4.7	COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1	10.1016/j.ejmech.2021.113986
	CHEMBL2443262	93198	None	26	Human	Functional	pEC50	=	8.7	8.7	-1	5	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL	386	7	1	5	4.7	COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1	10.1016/j.ejmech.2021.113986
	DB14881	93198	None	26	Human	Functional	pEC50	=	8.7	8.7	-1	5	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL	386	7	1	5	4.7	COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1	10.1016/j.ejmech.2021.113986
	CHEMBL5078909	217081	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL		None	None	None		FC1(F)CCc2csc(CNCC[C@@]3(c4ccccn4)CCOC4(CCCC4)C3)c2C1	10.1016/j.ejmech.2021.113986
	127049272	141059	None	0	Rat	Functional	pEC50	=	8.7	8.7	5	3	Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay	ChEMBL	497	7	3	4	4.5	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3ccccc3)cc21	10.1021/acs.jmedchem.6b00308
	CHEMBL3823231	141059	None	0	Rat	Functional	pEC50	=	8.7	8.7	5	3	Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay	ChEMBL	497	7	3	4	4.5	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3ccccc3)cc21	10.1021/acs.jmedchem.6b00308
	24822299	179421	None	0	Rat	Functional	pEC50	=	8.7	8.7	-15	4	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	472	5	3	5	3.2	O=C(/C=C/c1ccccc1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/jm8015552
	CHEMBL473362	179421	None	0	Rat	Functional	pEC50	=	8.7	8.7	-15	4	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	472	5	3	5	3.2	O=C(/C=C/c1ccccc1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/jm8015552
	CHEMBL5092377	217854	None	0	Mouse	Functional	pEC50	=	8.7	8.7	-	1	Antagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method	ChEMBL		None	None	None		O=C(Cc1ncc[nH]1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.1c02185
	146408971	174630	None	0	Mouse	Functional	pEC50	=	8.7	8.7	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	491	5	4	7	1.8	O=C(O)c1cnccc1C(=O)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.8b01158
	CHEMBL4555537	174630	None	0	Mouse	Functional	pEC50	=	8.7	8.7	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	491	5	4	7	1.8	O=C(O)c1cnccc1C(=O)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.8b01158
	CHEMBL5069828	216709	None	0	Mouse	Functional	pEC50	=	8.7	8.7	-	1	Antagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method	ChEMBL		None	None	None		O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc[nH]n1	10.1021/acs.jmedchem.1c02185
	155563764	176458	None	0	Mouse	Functional	pEC50	=	8.7	8.7	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1csc2ccccc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4572619	176458	None	0	Mouse	Functional	pEC50	=	8.7	8.7	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1csc2ccccc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4595660	176458	None	0	Mouse	Functional	pEC50	=	8.7	8.7	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1csc2ccccc12	10.1021/acs.jmedchem.9b01767
	146408966	175735	None	0	Mouse	Functional	pEC50	=	8.7	8.7	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	515	5	3	6	3.8	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1C1CCCC1	10.1021/acs.jmedchem.8b01158
	CHEMBL4580789	175735	None	0	Mouse	Functional	pEC50	=	8.7	8.7	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	515	5	3	6	3.8	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1C1CCCC1	10.1021/acs.jmedchem.8b01158
	50994381	57230	None	0	Rat	Functional	pEC50	=	8.7	8.7	1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	683	15	4	6	4.7	CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1	10.1021/jm100982d
	CHEMBL1649939	57230	None	0	Rat	Functional	pEC50	=	8.7	8.7	1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	683	15	4	6	4.7	CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1	10.1021/jm100982d
	156019450	178039	None	0	Human	Functional	pEC50	=	8.7	8.7	-4	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	585	8	1	6	6.5	Cc1cc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)ccn1	10.1021/acs.jmedchem.0c00503
	CHEMBL4645508	178039	None	0	Human	Functional	pEC50	=	8.7	8.7	-4	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	585	8	1	6	6.5	Cc1cc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)ccn1	10.1021/acs.jmedchem.0c00503
	16100411	137531	None	0	Rat	Functional	pEC50	=	8.7	8.7	3	3	Activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	1031	27	13	12	0.2	CCCC[C@@H](NC(=O)[C@@H](N)Cc1cc2ccccc2[nH]1)C(=O)N[C@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm061268p
	CHEMBL375359	137531	None	0	Rat	Functional	pEC50	=	8.7	8.7	3	3	Activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	1031	27	13	12	0.2	CCCC[C@@H](NC(=O)[C@@H](N)Cc1cc2ccccc2[nH]1)C(=O)N[C@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm061268p
	70693567	78406	None	0	Human	Functional	pEC50	=	8.7	8.7	10	3	Activity was evaluated in human mu opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assayActivity was evaluated in human mu opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assay	ChEMBL	395	0	1	4	4.0	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@]24CC[C@@]3(C[C@H]2C(C)(C)C(C)(C)O4)C1C5	10.1016/s0960-894x(99)00085-2
	CHEMBL2110315	78406	None	0	Human	Functional	pEC50	=	8.7	8.7	10	3	Activity was evaluated in human mu opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assayActivity was evaluated in human mu opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assay	ChEMBL	395	0	1	4	4.0	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@]24CC[C@@]3(C[C@H]2C(C)(C)C(C)(C)O4)C1C5	10.1016/s0960-894x(99)00085-2
	155514662	176336	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	487	9	3	5	4.2	CCOc1ccc(CN2CCc3ccccc3C2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b01818
	CHEMBL4440537	176336	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	487	9	3	5	4.2	CCOc1ccc(CN2CCc3ccccc3C2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b01818
	CHEMBL4594673	176336	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	487	9	3	5	4.2	CCOc1ccc(CN2CCc3ccccc3C2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b01818
	1164	1630	None	10	Human	Functional	pEC50	=	8.7	8.7	-1	13	Agonist activity at mu-opioid receptor (unknown origin)Agonist activity at mu-opioid receptor (unknown origin)	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.3c01637
	1626	1630	None	10	Human	Functional	pEC50	=	8.7	8.7	-1	13	Agonist activity at mu-opioid receptor (unknown origin)Agonist activity at mu-opioid receptor (unknown origin)	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.3c01637
	3345	1630	None	10	Human	Functional	pEC50	=	8.7	8.7	-1	13	Agonist activity at mu-opioid receptor (unknown origin)Agonist activity at mu-opioid receptor (unknown origin)	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.3c01637
	3345.0	1630	None	10	Human	Functional	pEC50	=	8.7	8.7	-1	13	Agonist activity at mu-opioid receptor (unknown origin)Agonist activity at mu-opioid receptor (unknown origin)	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.3c01637
	CHEMBL596	1630	None	10	Human	Functional	pEC50	=	8.7	8.7	-1	13	Agonist activity at mu-opioid receptor (unknown origin)Agonist activity at mu-opioid receptor (unknown origin)	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.3c01637
	DB00813	1630	None	10	Human	Functional	pEC50	=	8.7	8.7	-1	13	Agonist activity at mu-opioid receptor (unknown origin)Agonist activity at mu-opioid receptor (unknown origin)	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.3c01637
	1164	1630	None	10	Human	Functional	pEC50	=	8.7	8.7	-1	13	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.3c01637
	1626	1630	None	10	Human	Functional	pEC50	=	8.7	8.7	-1	13	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.3c01637
	3345	1630	None	10	Human	Functional	pEC50	=	8.7	8.7	-1	13	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.3c01637
	3345.0	1630	None	10	Human	Functional	pEC50	=	8.7	8.7	-1	13	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.3c01637
	CHEMBL596	1630	None	10	Human	Functional	pEC50	=	8.7	8.7	-1	13	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.3c01637
	DB00813	1630	None	10	Human	Functional	pEC50	=	8.7	8.7	-1	13	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.3c01637
	50994381	57230	None	0	Rat	Functional	pEC50	=	8.7	8.7	1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	683	15	4	6	4.7	CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1	10.1021/jm100982d
	CHEMBL1649939	57230	None	0	Rat	Functional	pEC50	=	8.7	8.7	1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	683	15	4	6	4.7	CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1	10.1021/jm100982d
	137630442	161160	None	0	Rat	Functional	pEC50	=	8.7	8.7	131	2	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 methodAgonist 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	ChEMBL	349	4	2	3	4.0	Oc1cccc([C@@]23CCC[C@@H]([C@@H]2O)N(C/C=C/c2ccccc2)CC3)c1	10.1016/j.bmc.2017.02.064
	CHEMBL4078283	161160	None	0	Rat	Functional	pEC50	=	8.7	8.7	131	2	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 methodAgonist 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	ChEMBL	349	4	2	3	4.0	Oc1cccc([C@@]23CCC[C@@H]([C@@H]2O)N(C/C=C/c2ccccc2)CC3)c1	10.1016/j.bmc.2017.02.064
	CHEMBL4116647	161160	None	0	Rat	Functional	pEC50	=	8.7	8.7	131	2	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 methodAgonist 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	ChEMBL	349	4	2	3	4.0	Oc1cccc([C@@]23CCC[C@@H]([C@@H]2O)N(C/C=C/c2ccccc2)CC3)c1	10.1016/j.bmc.2017.02.064
	155522549	176342	None	0	Rat	Functional	pEC50	=	8.7	8.7	-1	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	511	6	3	5	4.8	CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cc4ccccc4o3)ccc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4453526	176342	None	0	Rat	Functional	pEC50	=	8.7	8.7	-1	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	511	6	3	5	4.8	CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cc4ccccc4o3)ccc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4594713	176342	None	0	Rat	Functional	pEC50	=	8.7	8.7	-1	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	511	6	3	5	4.8	CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cc4ccccc4o3)ccc21	10.1021/acs.jmedchem.9b00378
	1647	1313	None	34	Human	Functional	pEC50	=	8.7	8.7	-3	9	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL		None	None	None		None	10.1016/j.ejmech.2021.113986
	5462471	1313	None	34	Human	Functional	pEC50	=	8.7	8.7	-3	9	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL		None	None	None		None	10.1016/j.ejmech.2021.113986
	CHEMBL113995	1313	None	34	Human	Functional	pEC50	=	8.7	8.7	-3	9	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL		None	None	None		None	10.1016/j.ejmech.2021.113986
	CHEMBL38874	1313	None	34	Human	Functional	pEC50	=	8.7	8.7	-3	9	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL		None	None	None		None	10.1016/j.ejmech.2021.113986
	44339521	9229	None	0	Human	Functional	pEC50	=	8.7	8.7	10	2	Concentration necessary to produce 50% of the Emax value, i.e. to stimulate [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cellsConcentration necessary to produce 50% of the Emax value, i.e. to stimulate [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells	ChEMBL	459	8	0	4	5.1	COc1cccc2c1C13CCN(CC4CC4)[C@H](C2)[C@]1(OCCCc1ccccc1)CCC(=O)C3	10.1021/jm031126k
	CHEMBL110640	9229	None	0	Human	Functional	pEC50	=	8.7	8.7	10	2	Concentration necessary to produce 50% of the Emax value, i.e. to stimulate [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cellsConcentration necessary to produce 50% of the Emax value, i.e. to stimulate [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells	ChEMBL	459	8	0	4	5.1	COc1cccc2c1C13CCN(CC4CC4)[C@H](C2)[C@]1(OCCCc1ccccc1)CCC(=O)C3	10.1021/jm031126k
	164628212	188719	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2cccnc12	10.1016/j.bmcl.2021.127953
	CHEMBL4875882	188719	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2cccnc12	10.1016/j.bmcl.2021.127953
	CHEMBL5029040	188719	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2cccnc12	10.1016/j.bmcl.2021.127953
	46887089	8554	None	0	Mouse	Functional	pEC50	=	8.7	8.7	-15	3	Agonist activity at mu opioid receptor in Swiss albino mouse ileum assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at mu opioid receptor in Swiss albino mouse ileum assessed as inhibition of electrically-stimulated muscle contraction	ChEMBL	409	3	1	4	4.4	CCCO[C@]12C=C[C@@]3(C[C@@H]1C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1016/j.bmc.2010.03.068
	CHEMBL1094469	8554	None	0	Mouse	Functional	pEC50	=	8.7	8.7	-15	3	Agonist activity at mu opioid receptor in Swiss albino mouse ileum assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at mu opioid receptor in Swiss albino mouse ileum assessed as inhibition of electrically-stimulated muscle contraction	ChEMBL	409	3	1	4	4.4	CCCO[C@]12C=C[C@@]3(C[C@@H]1C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1016/j.bmc.2010.03.068
	CHEMBL336381	214042	None	0	Rat	Functional	pEC50	=	8.7	8.7	-2	4	Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm050921q
	9848990	189274	None	0	Human	Functional	pEC50	=	8.7	8.7	-3	7	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm4010829
	9848990.0	189274	None	0	Human	Functional	pEC50	=	8.7	8.7	-3	7	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm4010829
	CHEMBL2368861	189274	None	0	Human	Functional	pEC50	=	8.7	8.7	-3	7	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm4010829
	CHEMBL511142	189274	None	0	Human	Functional	pEC50	=	8.7	8.7	-3	7	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm4010829
	137541816	156820	None	0	Human	Functional	pEC50	=	8	8.0	1	3	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	308	4	1	2	3.2	CCc1ccc(C(=O)NCC2c3ccccc3CCN2C)cc1	10.1016/j.ejmech.2016.09.003
	CHEMBL4070288	156820	None	0	Human	Functional	pEC50	=	8	8.0	1	3	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	308	4	1	2	3.2	CCc1ccc(C(=O)NCC2c3ccccc3CCN2C)cc1	10.1016/j.ejmech.2016.09.003
	137541810	156926	None	0	Human	Functional	pEC50	=	8	8.0	2	2	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	308	3	1	2	3.3	Cc1ccc(C(=O)NCC2c3ccccc3CCN2C)cc1C	10.1016/j.ejmech.2016.09.003
	CHEMBL4071332	156926	None	0	Human	Functional	pEC50	=	8	8.0	2	2	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	308	3	1	2	3.3	Cc1ccc(C(=O)NCC2c3ccccc3CCN2C)cc1C	10.1016/j.ejmech.2016.09.003
	137541784	158695	None	23	Human	Functional	pEC50	=	8	8.0	19	2	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	348	3	1	2	4.0	CN1CCc2ccccc2C1CNC(=O)c1ccc(Cl)c(Cl)c1	10.1016/j.ejmech.2016.09.003
	CHEMBL4092125	158695	None	23	Human	Functional	pEC50	=	8	8.0	19	2	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	348	3	1	2	4.0	CN1CCc2ccccc2C1CNC(=O)c1ccc(Cl)c(Cl)c1	10.1016/j.ejmech.2016.09.003
	118561099	181806	None	0	Human	Functional	pEC50	=	8	8.0	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	352	4	0	3	2.6	CCN1CC2(CCN(CCc3cccc(F)c3F)CC2)O[C@H](C)C1=O	10.1021/acs.jmedchem.0c01127
	CHEMBL4776743	181806	None	0	Human	Functional	pEC50	=	8	8.0	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	352	4	0	3	2.6	CCN1CC2(CCN(CCc3cccc(F)c3F)CC2)O[C@H](C)C1=O	10.1021/acs.jmedchem.0c01127
	1627	2594	None	9	Human	Functional	pEC50	=	8	8.0	-1	9	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmc.2014.07.012
	1845	2594	None	9	Human	Functional	pEC50	=	8	8.0	-1	9	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmc.2014.07.012
	5288826	2594	None	9	Human	Functional	pEC50	=	8	8.0	-1	9	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmc.2014.07.012
	5288826.0	2594	None	9	Human	Functional	pEC50	=	8	8.0	-1	9	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmc.2014.07.012
	CHEMBL70	2594	None	9	Human	Functional	pEC50	=	8	8.0	-1	9	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmc.2014.07.012
	DB00295	2594	None	9	Human	Functional	pEC50	=	8	8.0	-1	9	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmc.2014.07.012
	44592086	179015	None	0	Human	Functional	pEC50	=	8	8.0	-1	3	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	356	3	3	4	2.1	NC(=O)c1ccc2c(c1O)[C@@]13CCCC[C@@]1(O)[C@@H](C2)N(CC1CC1)CC3	10.1016/j.bmcl.2009.02.078
	CHEMBL470005	179015	None	0	Human	Functional	pEC50	=	8	8.0	-1	3	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	356	3	3	4	2.1	NC(=O)c1ccc2c(c1O)[C@@]13CCCC[C@@]1(O)[C@@H](C2)N(CC1CC1)CC3	10.1016/j.bmcl.2009.02.078
	72712155	93207	None	0	Human	Functional	pEC50	=	8	8.0	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	384	6	1	3	5.3	Clc1ccccc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1	10.1021/jm4010829
	CHEMBL2443271	93207	None	0	Human	Functional	pEC50	=	8	8.0	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	384	6	1	3	5.3	Clc1ccccc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1	10.1021/jm4010829
	54585844	62096	None	0	Human	Functional	pEC50	=	8	8.0	-1	2	Agonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	834	16	1	10	7.9	C=CCN1CC[C@]23c4c5ccc(OC(=O)CCCCCCCCC(=O)Oc6ccc7c(c6)[C@@]68CCCC[C@@]6(OC)[C@@H](C7)N(CC6CCC6)CC8)c4O[C@H]2C(=O)CC[C@@]3(O)[C@H]1C5	10.1016/j.bmc.2011.03.052
	CHEMBL1774948	62096	None	0	Human	Functional	pEC50	=	8	8.0	-1	2	Agonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	834	16	1	10	7.9	C=CCN1CC[C@]23c4c5ccc(OC(=O)CCCCCCCCC(=O)Oc6ccc7c(c6)[C@@]68CCCC[C@@]6(OC)[C@@H](C7)N(CC6CCC6)CC8)c4O[C@H]2C(=O)CC[C@@]3(O)[C@H]1C5	10.1016/j.bmc.2011.03.052
	89435275	156586	None	0	Human	Functional	pEC50	=	8	8.0	-2	3	Agonist activity at human recombinant MOR expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant MOR expressed in CHO cells assessed as cAMP accumulation	ChEMBL	426	3	1	3	5.0	Oc1ccc2c(c1)C13CCN(CC4CC4)C(C2)C12CCC1C3[C@@H](CN1c1ccccc1)C2	10.1016/j.bmcl.2017.05.072
	CHEMBL4067629	156586	None	0	Human	Functional	pEC50	=	8	8.0	-2	3	Agonist activity at human recombinant MOR expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant MOR expressed in CHO cells assessed as cAMP accumulation	ChEMBL	426	3	1	3	5.0	Oc1ccc2c(c1)C13CCN(CC4CC4)C(C2)C12CCC1C3[C@@H](CN1c1ccccc1)C2	10.1016/j.bmcl.2017.05.072
	71819401	92084	None	0	Mouse	Functional	pEC50	=	8	8.0	1	5	Agonist activity at mouse MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assayAgonist activity at mouse MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay	ChEMBL	301	0	2	4	1.7	C[C@@H]1C[C@H]2[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3C)[C@@H](O5)[C@H]1O	10.1016/j.bmcl.2013.06.084
	CHEMBL2418739	92084	None	0	Mouse	Functional	pEC50	=	8	8.0	1	5	Agonist activity at mouse MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assayAgonist activity at mouse MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay	ChEMBL	301	0	2	4	1.7	C[C@@H]1C[C@H]2[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3C)[C@@H](O5)[C@H]1O	10.1016/j.bmcl.2013.06.084
	CHEMBL5082714	217310	None	0	Human	Functional	pEC50	=	8	8.0	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as beta arrestin-2 recruitment incubated for 3 days by PathHunter assayAgonist activity at mu opioid receptor (unknown origin) assessed as beta arrestin-2 recruitment incubated for 3 days by PathHunter assay	ChEMBL		None	None	None		FC1(F)Cc2csc(CNCC[C@@]3(c4ccccn4)CCOC4(CCCC4)C3)c2C1	10.1016/j.ejmech.2021.113986
	121596705	3246	None	34	Human	Functional	pEC50	=	8	8.0	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL	361	8	3	4	2.9	C[C@@H](Cc1cscc1)NC(=O)NC[C@@H](N(C)C)Cc1ccc(cc1)O	10.1016/j.ejmech.2021.113986
	9286	3246	None	34	Human	Functional	pEC50	=	8	8.0	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL	361	8	3	4	2.9	C[C@@H](Cc1cscc1)NC(=O)NC[C@@H](N(C)C)Cc1ccc(cc1)O	10.1016/j.ejmech.2021.113986
	CHEMBL4467777	3246	None	34	Human	Functional	pEC50	=	8	8.0	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL	361	8	3	4	2.9	C[C@@H](Cc1cscc1)NC(=O)NC[C@@H](N(C)C)Cc1ccc(cc1)O	10.1016/j.ejmech.2021.113986
	DB14030	3246	None	34	Human	Functional	pEC50	=	8	8.0	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL	361	8	3	4	2.9	C[C@@H](Cc1cscc1)NC(=O)NC[C@@H](N(C)C)Cc1ccc(cc1)O	10.1016/j.ejmech.2021.113986
	CHEMBL2419544	212904	None	0	Rat	Functional	pEC50	=	8	8.0	2	3	Agonist activity at rat MOR expressed in HN9.10 cell membranes by [35S]GTPgammaS binding assayAgonist activity at rat MOR expressed in HN9.10 cell membranes by [35S]GTPgammaS binding assay	ChEMBL		None	None	None		C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1016/j.bmcl.2013.06.065
	44408632	158329	None	0	Rat	Functional	pEC50	=	8	8.0	-4	5	Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells	ChEMBL	1212	31	12	15	3.8	CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@H](Cc1cn(C(=O)OC23CC4CC(CC(C4)C2)C3)c2ccccc12)C(=O)O	10.1021/jm050851n
	CHEMBL408832	158329	None	0	Rat	Functional	pEC50	=	8	8.0	-4	5	Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells	ChEMBL	1212	31	12	15	3.8	CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@H](Cc1cn(C(=O)OC23CC4CC(CC(C4)C2)C3)c2ccccc12)C(=O)O	10.1021/jm050851n
	9848990	189274	None	0	Human	Functional	pEC50	=	8.0	8.0	-3	7	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysis	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm401964y
	9848990.0	189274	None	0	Human	Functional	pEC50	=	8.0	8.0	-3	7	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysis	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm401964y
	CHEMBL2368861	189274	None	0	Human	Functional	pEC50	=	8.0	8.0	-3	7	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysis	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm401964y
	CHEMBL511142	189274	None	0	Human	Functional	pEC50	=	8.0	8.0	-3	7	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysis	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm401964y
	9848990	189274	None	0	Human	Functional	pEC50	=	8.0	8.0	-3	7	Partial agonist activity at human MOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human MOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm2003238
	9848990.0	189274	None	0	Human	Functional	pEC50	=	8.0	8.0	-3	7	Partial agonist activity at human MOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human MOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm2003238
	CHEMBL2368861	189274	None	0	Human	Functional	pEC50	=	8.0	8.0	-3	7	Partial agonist activity at human MOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human MOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm2003238
	CHEMBL511142	189274	None	0	Human	Functional	pEC50	=	8.0	8.0	-3	7	Partial agonist activity at human MOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human MOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm2003238
	137662101	159375	None	0	Human	Functional	pEC50	=	8.0	8.0	-	1	Agonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysisAgonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis	ChEMBL	727	10	7	8	0.5	CN[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)N(C)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1016/j.bmcl.2017.03.016
	CHEMBL4099423	159375	None	0	Human	Functional	pEC50	=	8.0	8.0	-	1	Agonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysisAgonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis	ChEMBL	727	10	7	8	0.5	CN[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)N(C)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1016/j.bmcl.2017.03.016
	71230334	111016	None	0	Human	Functional	pEC50	=	8.0	8.0	-9	3	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysis	ChEMBL	473	5	2	5	4.4	CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm401964y
	CHEMBL3262090	111016	None	0	Human	Functional	pEC50	=	8.0	8.0	-9	3	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysis	ChEMBL	473	5	2	5	4.4	CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm401964y
	CHEMBL235743	212033	None	1	Rat	Functional	pEC50	=	8.0	8.0	7	4	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL		None	None	None		C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/jm100982d
	CHEMBL235743	212033	None	1	Rat	Functional	pEC50	=	8.0	8.0	7	4	Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay	ChEMBL		None	None	None		C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/jm061465o
	5485199	213293	None	26	Human	Functional	pEC50	=	8.0	8.0	-3	6	Antagonist activity at human recombinant mu opioid receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of dermorphin-induced intracellular calcium mobilizationAntagonist activity at human recombinant mu opioid receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of dermorphin-induced intracellular calcium mobilization	ChEMBL		None	None	None		C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O	10.1021/jm900604g
	CHEMBL278789	213293	None	26	Human	Functional	pEC50	=	8.0	8.0	-3	6	Antagonist activity at human recombinant mu opioid receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of dermorphin-induced intracellular calcium mobilizationAntagonist activity at human recombinant mu opioid receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of dermorphin-induced intracellular calcium mobilization	ChEMBL		None	None	None		C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O	10.1021/jm900604g
	44408632	158329	None	0	Rat	Functional	pEC50	=	8.0	8.0	-4	5	Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells	ChEMBL	1212	31	12	15	3.8	CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@H](Cc1cn(C(=O)OC23CC4CC(CC(C4)C2)C3)c2ccccc12)C(=O)O	10.1021/jm050851n
	CHEMBL408832	158329	None	0	Rat	Functional	pEC50	=	8.0	8.0	-4	5	Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells	ChEMBL	1212	31	12	15	3.8	CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@H](Cc1cn(C(=O)OC23CC4CC(CC(C4)C2)C3)c2ccccc12)C(=O)O	10.1021/jm050851n
	71459947	79162	None	0	Human	Functional	pEC50	=	8.0	8.0	1	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	534	6	1	5	4.6	COc1ccc2c3c1O[C@H]1[C@]4(OC)CC[C@@]5(C[C@@H]4CNC(=O)/C=C/c4ccccc4Cl)[C@@H](C2)N(C)CC[C@]315	10.1021/jm070255o
	CHEMBL2113296	79162	None	0	Human	Functional	pEC50	=	8.0	8.0	1	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	534	6	1	5	4.6	COc1ccc2c3c1O[C@H]1[C@]4(OC)CC[C@@]5(C[C@@H]4CNC(=O)/C=C/c4ccccc4Cl)[C@@H](C2)N(C)CC[C@]315	10.1021/jm070255o
	60170774	81742	None	0	Human	Functional	pEC50	=	8.0	8.0	39	2	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL	666	12	6	8	2.1	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccc2c(c1)OCO2	10.1021/jm300664y
	CHEMBL2163915	81742	None	0	Human	Functional	pEC50	=	8.0	8.0	39	2	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL	666	12	6	8	2.1	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccc2c(c1)OCO2	10.1021/jm300664y
	58296565	145772	None	0	Human	Functional	pEC50	=	8.0	8.0	-2	3	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	501	8	0	5	5.1	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2	nan
	CHEMBL3916122	145772	None	0	Human	Functional	pEC50	=	8.0	8.0	-2	3	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	501	8	0	5	5.1	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2	nan
	60170691	81741	None	0	Human	Functional	pEC50	=	8.0	8.0	27	2	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL	652	13	6	7	2.4	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccc(OC)cc1	10.1021/jm300664y
	CHEMBL2163914	81741	None	0	Human	Functional	pEC50	=	8.0	8.0	27	2	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL	652	13	6	7	2.4	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccc(OC)cc1	10.1021/jm300664y
	23634921	146536	None	0	Rat	Functional	pEC50	=	8.0	8.0	10	3	Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay	ChEMBL	832	19	7	9	2.3	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)CCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1	10.1021/jm061465o
	CHEMBL392206	146536	None	0	Rat	Functional	pEC50	=	8.0	8.0	10	3	Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay	ChEMBL	832	19	7	9	2.3	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)CCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1	10.1021/jm061465o
	CHEMBL1627325	211270	None	0	Human	Functional	pEC50	=	8.0	8.0	-323	8	Antagonist activity at human recombinant mu opioid receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of dermorphin-induced intracellular calcium mobilizationAntagonist activity at human recombinant mu opioid receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of dermorphin-induced intracellular calcium mobilization	ChEMBL		None	None	None		CSCC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(C)(C)C)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)O)[C@@H](C)O	10.1021/jm900604g
	118711209	113990	None	0	Human	Functional	pEC50	=	7	7.0	1	2	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	412	1	1	3	4.7	Cc1nn(-c2ccc(Br)cc2Br)c2c1C(O)CC(C)(C)C2	10.1016/j.bmc.2014.07.012
	CHEMBL3325841	113990	None	0	Human	Functional	pEC50	=	7	7.0	1	2	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	412	1	1	3	4.7	Cc1nn(-c2ccc(Br)cc2Br)c2c1C(O)CC(C)(C)C2	10.1016/j.bmc.2014.07.012
	CHEMBL2419539	212899	None	0	Rat	Functional	pEC50	=	7	7.0	-18	3	Agonist activity at rat MOR expressed in HN9.10 cell membranes by [35S]GTPgammaS binding assayAgonist activity at rat MOR expressed in HN9.10 cell membranes by [35S]GTPgammaS binding assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NC(C)(C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1016/j.bmcl.2013.06.065
	CHEMBL3609616	214290	None	0	Rat	Functional	pEC50	=	7	7.0	-2	3	Agonist activity at rat mu opioid receptor transfected in HN9.10 cells by [35S]GTPgammaS binding assayAgonist activity at rat mu opioid receptor transfected in HN9.10 cells by [35S]GTPgammaS binding assay	ChEMBL		None	None	None		C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1016/j.bmcl.2015.06.030
	10406239	120624	None	0	Human	Functional	pEC50	=	6	6.0	10	2	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay	ChEMBL	360	2	1	2	5.0	CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12	10.1021/ml500116x
	CHEMBL3326224	120624	None	0	Human	Functional	pEC50	=	6	6.0	10	2	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay	ChEMBL	360	2	1	2	5.0	CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12	10.1021/ml500116x
	CHEMBL3326226	120624	None	0	Human	Functional	pEC50	=	6	6.0	10	2	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay	ChEMBL	360	2	1	2	5.0	CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12	10.1021/ml500116x
	CHEMBL3545624	120624	None	0	Human	Functional	pEC50	=	6	6.0	10	2	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay	ChEMBL	360	2	1	2	5.0	CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12	10.1021/ml500116x
	72711954	93203	None	0	Human	Functional	pEC50	=	6	6.0	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	381	6	1	2	5.9	C[C@@H](NCC[C@@]1(c2ccc(F)cc2)CCOC2(CCCC2)C1)c1ccccc1	10.1021/jm4010829
	CHEMBL2443267	93203	None	0	Human	Functional	pEC50	=	6	6.0	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	381	6	1	2	5.9	C[C@@H](NCC[C@@]1(c2ccc(F)cc2)CCOC2(CCCC2)C1)c1ccccc1	10.1021/jm4010829
	137541792	158727	None	0	Human	Functional	pEC50	=	5	5.0	-	1	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	286	3	2	2	2.8	CC1CCCCC1C(=O)NCC1NCCc2ccccc21	10.1016/j.ejmech.2016.09.003
	CHEMBL4092452	158727	None	0	Human	Functional	pEC50	=	5	5.0	-	1	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	286	3	2	2	2.8	CC1CCCCC1C(=O)NCC1NCCc2ccccc21	10.1016/j.ejmech.2016.09.003
	4247619	113940	None	0	Human	Functional	pEC50	=	5	5.0	-	1	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	312	2	0	5	3.1	COC(=O)c1ccc(-n2nc(C)c3c2CC(C)(C)CC3=O)cc1	10.1016/j.bmc.2014.07.012
	CHEMBL3325706	113940	None	0	Human	Functional	pEC50	=	5	5.0	-	1	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	312	2	0	5	3.1	COC(=O)c1ccc(-n2nc(C)c3c2CC(C)(C)CC3=O)cc1	10.1016/j.bmc.2014.07.012
	118711131	113943	None	0	Human	Functional	pEC50	=	5	5.0	-	1	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	282	1	0	3	4.0	Cc1ccc(C)c(-n2nc(C)c3c2CC(C)(C)CC3=O)c1	10.1016/j.bmc.2014.07.012
	CHEMBL3325709	113943	None	0	Human	Functional	pEC50	=	5	5.0	-	1	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	282	1	0	3	4.0	Cc1ccc(C)c(-n2nc(C)c3c2CC(C)(C)CC3=O)c1	10.1016/j.bmc.2014.07.012
	25207946	191407	None	0	Human	Functional	pEC50	=	5	5.0	-1737	3	Agonist activity at human mu opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS binding	ChEMBL	469	3	0	3	7.9	CC1(N2CCC(n3c(-c4cccc(C(F)(F)F)c4)nc4ccccc43)CC2)CCCCCCC1	10.1021/jm7012979
	CHEMBL519100	191407	None	0	Human	Functional	pEC50	=	5	5.0	-1737	3	Agonist activity at human mu opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS binding	ChEMBL	469	3	0	3	7.9	CC1(N2CCC(n3c(-c4cccc(C(F)(F)F)c4)nc4ccccc43)CC2)CCCCCCC1	10.1021/jm7012979
	72711945	93217	None	0	Human	Functional	pEC50	=	5	5.0	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	325	6	2	3	3.9	Cc1ccc(C2(CCNCc3ccccc3O)CCOCC2)cc1	10.1021/jm4010829
	CHEMBL2443281	93217	None	0	Human	Functional	pEC50	=	5	5.0	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	325	6	2	3	3.9	Cc1ccc(C2(CCNCc3ccccc3O)CCOCC2)cc1	10.1021/jm4010829
	99941396	156253	None	10	Human	Functional	pEC50	=	5	5.0	-776	2	Agonist activity at human mu-type opioid receptor expressed in CHO-K1 cells assessed as cAMP accumulation by HTRF assayAgonist activity at human mu-type opioid receptor expressed in CHO-K1 cells assessed as cAMP accumulation by HTRF assay	ChEMBL	329	4	0	6	2.7	CC(C)(C)C[C@@H]1COCc2nc(OCc3ccccn3)cc(=O)n21	10.1021/acs.jmedchem.7b00604
	CHEMBL4063837	156253	None	10	Human	Functional	pEC50	=	5	5.0	-776	2	Agonist activity at human mu-type opioid receptor expressed in CHO-K1 cells assessed as cAMP accumulation by HTRF assayAgonist activity at human mu-type opioid receptor expressed in CHO-K1 cells assessed as cAMP accumulation by HTRF assay	ChEMBL	329	4	0	6	2.7	CC(C)(C)C[C@@H]1COCc2nc(OCc3ccccn3)cc(=O)n21	10.1021/acs.jmedchem.7b00604
	118725843	117232	None	0	Human	Functional	pEC50	=	4	4.0	-1445	3	Agonist activity at human mu opioid receptor expressed in COS7 cells after 60 mins IP1 assayAgonist activity at human mu opioid receptor expressed in COS7 cells after 60 mins IP1 assay	ChEMBL	349	5	1	5	3.1	Cc1ccc(C(=O)Nc2nc3ccccc3n2CCN2CCCC2)nc1	10.1016/j.bmcl.2014.12.064
	CHEMBL3393993	117232	None	0	Human	Functional	pEC50	=	4	4.0	-1445	3	Agonist activity at human mu opioid receptor expressed in COS7 cells after 60 mins IP1 assayAgonist activity at human mu opioid receptor expressed in COS7 cells after 60 mins IP1 assay	ChEMBL	349	5	1	5	3.1	Cc1ccc(C(=O)Nc2nc3ccccc3n2CCN2CCCC2)nc1	10.1016/j.bmcl.2014.12.064
	118725849	117237	None	0	Human	Functional	pEC50	=	4	4.0	-812	3	Agonist activity at human mu opioid receptor expressed in COS7 cells after 60 mins IP1 assayAgonist activity at human mu opioid receptor expressed in COS7 cells after 60 mins IP1 assay	ChEMBL	391	5	1	6	4.0	O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1nc2ccccc2s1	10.1016/j.bmcl.2014.12.064
	CHEMBL3393999	117237	None	0	Human	Functional	pEC50	=	4	4.0	-812	3	Agonist activity at human mu opioid receptor expressed in COS7 cells after 60 mins IP1 assayAgonist activity at human mu opioid receptor expressed in COS7 cells after 60 mins IP1 assay	ChEMBL	391	5	1	6	4.0	O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1nc2ccccc2s1	10.1016/j.bmcl.2014.12.064
	16190821	45898	None	5	Human	Functional	pEC50	=	5	5.0	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	385	8	1	5	4.5	Cc1ccc(C)c(-n2cc(CNCCCn3cccn3)c(-c3ccccc3)n2)c1	nan
	CHEMBL1531675	45898	None	5	Human	Functional	pEC50	=	5	5.0	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	385	8	1	5	4.5	Cc1ccc(C)c(-n2cc(CNCCCn3cccn3)c(-c3ccccc3)n2)c1	nan
	44570027	176681	None	0	Human	Functional	pEC50	=	7	7.0	1	2	Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	328	3	1	3	2.5	C[C@@H]1[C@@H]2Cc3ccc(C(N)=O)cc3[C@@]1(C)CCN2C[C@H]1CCCO1	10.1016/j.bmcl.2008.10.134
	CHEMBL459746	176681	None	0	Human	Functional	pEC50	=	7	7.0	1	2	Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	328	3	1	3	2.5	C[C@@H]1[C@@H]2Cc3ccc(C(N)=O)cc3[C@@]1(C)CCN2C[C@H]1CCCO1	10.1016/j.bmcl.2008.10.134
	126619429	174872	None	0	Human	Functional	pEC50	=	5	5.0	-	1	Agonist activity at human mu opioid receptor expressed in CHOK1 cells coexpressing Galpha15 assessed as increase in intracellular calcium flux in presence of mu opioid receptor antagonist naloxone and incubated for 1 hr measured for 90 secs at 1.5 sec interval by FLIPR assayAgonist activity at human mu opioid receptor expressed in CHOK1 cells coexpressing Galpha15 assessed as increase in intracellular calcium flux in presence of mu opioid receptor antagonist naloxone and incubated for 1 hr measured for 90 secs at 1.5 sec interval by FLIPR assay	ChEMBL	319	3	1	5	5.1	Cc1nc(C)c(-c2csc(Nc3cccc(F)c3C)n2)s1	10.1016/j.ejmech.2019.01.063
	CHEMBL4561162	174872	None	0	Human	Functional	pEC50	=	5	5.0	-	1	Agonist activity at human mu opioid receptor expressed in CHOK1 cells coexpressing Galpha15 assessed as increase in intracellular calcium flux in presence of mu opioid receptor antagonist naloxone and incubated for 1 hr measured for 90 secs at 1.5 sec interval by FLIPR assayAgonist activity at human mu opioid receptor expressed in CHOK1 cells coexpressing Galpha15 assessed as increase in intracellular calcium flux in presence of mu opioid receptor antagonist naloxone and incubated for 1 hr measured for 90 secs at 1.5 sec interval by FLIPR assay	ChEMBL	319	3	1	5	5.1	Cc1nc(C)c(-c2csc(Nc3cccc(F)c3C)n2)s1	10.1016/j.ejmech.2019.01.063
	44337645	5414	None	0	Human	Functional	pEC50	=	6.0	6.0	-4	3	Effective concentration agonistic activity towards Opioid receptor mu 1Effective concentration agonistic activity towards Opioid receptor mu 1	ChEMBL	440	1	2	3	5.4	COc1ccc2c(c1O)[C@]13CCN(C)C(C2)[C@@]12CC(=C(C)C)[C@@H]3c1[nH]c3ccccc3c1C2	10.1021/jm030801n
	CHEMBL107207	5414	None	0	Human	Functional	pEC50	=	6.0	6.0	-4	3	Effective concentration agonistic activity towards Opioid receptor mu 1Effective concentration agonistic activity towards Opioid receptor mu 1	ChEMBL	440	1	2	3	5.4	COc1ccc2c(c1O)[C@]13CCN(C)C(C2)[C@@]12CC(=C(C)C)[C@@H]3c1[nH]c3ccccc3c1C2	10.1021/jm030801n
	24892627	55669	None	4	Human	Functional	pEC50	=	5.0	5.0	5	2	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	548	8	0	6	5.0	Cc1ccc2nc(N(CCCN(C)C)C(=O)c3ccc(S(=O)(=O)N4CCc5ccccc5C4)cc3)sc2c1	nan
	CHEMBL1460676	55669	None	4	Human	Functional	pEC50	=	5.0	5.0	5	2	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	548	8	0	6	5.0	Cc1ccc2nc(N(CCCN(C)C)C(=O)c3ccc(S(=O)(=O)N4CCc5ccccc5C4)cc3)sc2c1	nan
	CHEMBL1621632	55669	None	4	Human	Functional	pEC50	=	5.0	5.0	5	2	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	548	8	0	6	5.0	Cc1ccc2nc(N(CCCN(C)C)C(=O)c3ccc(S(=O)(=O)N4CCc5ccccc5C4)cc3)sc2c1	nan
	21262767	163917	None	5	Human	Functional	pEC50	=	7.0	7.0	-	1	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 methodAgonist 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	ChEMBL	321	3	1	3	3.7	CC(c1ccccc1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4206287	163917	None	5	Human	Functional	pEC50	=	7.0	7.0	-	1	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 methodAgonist 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	ChEMBL	321	3	1	3	3.7	CC(c1ccccc1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1	10.1021/acs.jmedchem.8b01136
	86711645	160901	None	0	Human	Functional	pEC50	=	7.0	7.0	-7	3	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	474	6	1	5	3.4	CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(C(N)=O)c5c4[C@@]3(CCN1C)[C@H]2O5	nan
	CHEMBL4114477	160901	None	0	Human	Functional	pEC50	=	7.0	7.0	-7	3	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	474	6	1	5	3.4	CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(C(N)=O)c5c4[C@@]3(CCN1C)[C@H]2O5	nan
	155554576	176548	None	0	Human	Functional	pEC50	=	6.0	6.0	-	1	Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	441	9	3	6	2.4	CCOc1ccc(CN2CCOCC2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b01818
	CHEMBL4557264	176548	None	0	Human	Functional	pEC50	=	6.0	6.0	-	1	Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	441	9	3	6	2.4	CCOc1ccc(CN2CCOCC2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b01818
	CHEMBL4596319	176548	None	0	Human	Functional	pEC50	=	6.0	6.0	-	1	Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	441	9	3	6	2.4	CCOc1ccc(CN2CCOCC2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b01818
	71460828	82581	None	0	Rat	Functional	pEC50	=	6.0	6.0	-	1	Agonist activity at mu opioid receptor in Wistar rat brain membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at mu opioid receptor in Wistar rat brain membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	597	13	6	6	1.7	NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H]1CC=CC[C@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm300836n
	CHEMBL2178087	82581	None	0	Rat	Functional	pEC50	=	6.0	6.0	-	1	Agonist activity at mu opioid receptor in Wistar rat brain membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at mu opioid receptor in Wistar rat brain membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	597	13	6	6	1.7	NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H]1CC=CC[C@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm300836n
	1177949	34298	None	10	Human	Functional	pEC50	=	5.0	5.0	-1	3	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	429	6	0	7	5.3	COc1ccc2c(Cl)c(-c3nnc(SCC(=O)c4ccccc4)n3C)sc2c1	nan
	CHEMBL1426979	34298	None	10	Human	Functional	pEC50	=	5.0	5.0	-1	3	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	429	6	0	7	5.3	COc1ccc2c(Cl)c(-c3nnc(SCC(=O)c4ccccc4)n3C)sc2c1	nan
	118711133	113945	None	0	Human	Functional	pEC50	=	5.0	5.0	-	1	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	290	1	0	3	3.6	Cc1nn(-c2ccc(F)cc2F)c2c1C(=O)CC(C)(C)C2	10.1016/j.bmc.2014.07.012
	CHEMBL3325711	113945	None	0	Human	Functional	pEC50	=	5.0	5.0	-	1	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	290	1	0	3	3.6	Cc1nn(-c2ccc(F)cc2F)c2c1C(=O)CC(C)(C)C2	10.1016/j.bmc.2014.07.012
	1623	1560	None	36	Rat	Functional	pEC50	=	7.0	7.0	2	6	Activity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS bindingActivity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS binding	ChEMBL		None	None	None		None	10.1021/jm800223t
	5311080	1560	None	36	Rat	Functional	pEC50	=	7.0	7.0	2	6	Activity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS bindingActivity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS binding	ChEMBL		None	None	None		None	10.1021/jm800223t
	CHEMBL316446	1560	None	36	Rat	Functional	pEC50	=	7.0	7.0	2	6	Activity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS bindingActivity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS binding	ChEMBL		None	None	None		None	10.1021/jm800223t
	172450600	195903	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assayAgonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assay	ChEMBL	367	8	3	3	3.3	CN(C)[C@H](CNC(=O)N[C@@H](c1ccccc1)C1CC1)Cc1ccc(O)cc1	10.1016/j.bmcl.2023.129405
	CHEMBL5412978	195903	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assayAgonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assay	ChEMBL	367	8	3	3	3.3	CN(C)[C@H](CNC(=O)N[C@@H](c1ccccc1)C1CC1)Cc1ccc(O)cc1	10.1016/j.bmcl.2023.129405
	CHEMBL5075279	216853	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	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 assayAgonist 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	ChEMBL		None	None	None		CC[C@@H]1CN2CC[C@@]3(O)C(=Nc4ccc(-c5ccccc5)c(OC)c43)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.1c01273
	172464127	196667	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	379	7	0	3	4.8	CCC(=O)N(CC(CC)N1CCC(c2ccccc2)CC1)c1cccc(C)n1	10.1021/acs.jmedchem.3c01637
	CHEMBL5429304	196667	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	379	7	0	3	4.8	CCC(=O)N(CC(CC)N1CCC(c2ccccc2)CC1)c1cccc(C)n1	10.1021/acs.jmedchem.3c01637
	CHEMBL5075279	216853	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	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 assayAgonist 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	ChEMBL		None	None	None		CC[C@@H]1CN2CC[C@@]3(O)C(=Nc4ccc(-c5ccccc5)c(OC)c43)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.1c01273
	CHEMBL5074977	216834	None	0	Human	Functional	pEC50	=	5.0	5.0	-	1	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 assayAgonist 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	ChEMBL		None	None	None		CC[C@@H]1CN2CC[C@@]3(O)C(=Nc4cccc(C)c43)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.1c01273
	5702288	93312	None	0	Human	Functional	pEC50	=	5.0	5.0	-	1	HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.	ChEMBL	299	1	1	4	1.5	COc1ccc2c3c1O[C@H]1[C@@H](O)C=CC4[C@@H](C2)N(C)CC[C@@]341	nan
	CHEMBL2448883	93312	None	0	Human	Functional	pEC50	=	5.0	5.0	-	1	HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.	ChEMBL	299	1	1	4	1.5	COc1ccc2c3c1O[C@H]1[C@@H](O)C=CC4[C@@H](C2)N(C)CC[C@@]341	nan
	CHEMBL5074977	216834	None	0	Human	Functional	pEC50	=	5.0	5.0	-	1	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 assayAgonist 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	ChEMBL		None	None	None		CC[C@@H]1CN2CC[C@@]3(O)C(=Nc4cccc(C)c43)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.1c01273
	CHEMBL5089655	217710	None	0	Human	Functional	pEC50	=	5.0	5.0	-63	2	Agonist activity at human mu opioid receptor expressed in HEK293T cells assessed as Galphai2 activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human mu opioid receptor expressed in HEK293T cells assessed as Galphai2 activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay	ChEMBL		None	None	None		N#CC(CCNCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1	10.1021/acs.jmedchem.1c00611
	134563655	174322	None	4	Human	Functional	pEC50	=	7.0	7.0	-1	2	Agonist activity at human MOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay	ChEMBL	353	4	1	3	5.0	CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN)c4ccccc43)CC2)CC1	10.1021/acs.jmedchem.9b02134
	CHEMBL4548515	174322	None	4	Human	Functional	pEC50	=	7.0	7.0	-1	2	Agonist activity at human MOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay	ChEMBL	353	4	1	3	5.0	CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN)c4ccccc43)CC2)CC1	10.1021/acs.jmedchem.9b02134
	71459947	79162	None	0	Human	Functional	pEC50	=	7.0	7.0	1	2	Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	534	6	1	5	4.6	COc1ccc2c3c1O[C@H]1[C@]4(OC)CC[C@@]5(C[C@@H]4CNC(=O)/C=C/c4ccccc4Cl)[C@@H](C2)N(C)CC[C@]315	10.1021/jm070255o
	CHEMBL2113296	79162	None	0	Human	Functional	pEC50	=	7.0	7.0	1	2	Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	534	6	1	5	4.6	COc1ccc2c3c1O[C@H]1[C@]4(OC)CC[C@@]5(C[C@@H]4CNC(=O)/C=C/c4ccccc4Cl)[C@@H](C2)N(C)CC[C@]315	10.1021/jm070255o
	146025598	170733	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay	ChEMBL	379	3	1	5	3.5	CC(c1ccc2c(c1)OCCO2)N1CCC(n2c(=O)[nH]c3ccccc32)CC1	10.1021/acs.jmedchem.8b00435
	CHEMBL4451128	170733	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay	ChEMBL	379	3	1	5	3.5	CC(c1ccc2c(c1)OCCO2)N1CCC(n2c(=O)[nH]c3ccccc32)CC1	10.1021/acs.jmedchem.8b00435
	72735204	106369	None	0	Human	Functional	pEC50	=	7.0	7.0	-97	2	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay	ChEMBL	386	1	2	4	3.4	CCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13	10.1016/j.bmc.2013.10.032
	CHEMBL3139097	106369	None	0	Human	Functional	pEC50	=	7.0	7.0	-97	2	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay	ChEMBL	386	1	2	4	3.4	CCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13	10.1016/j.bmc.2013.10.032
	CHEMBL4296733	106369	None	0	Human	Functional	pEC50	=	7.0	7.0	-97	2	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay	ChEMBL	386	1	2	4	3.4	CCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13	10.1016/j.bmc.2013.10.032
	172443869	195196	None	0	Human	Functional	pEC50	=	6.0	6.0	-	1	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assay	ChEMBL	342	5	1	3	4.1	CN(C)C(CNC(=O)c1sccc1Cl)c1ccccc1Cl	10.1016/j.ejmech.2022.114728
	CHEMBL5398541	195196	None	0	Human	Functional	pEC50	=	6.0	6.0	-	1	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assay	ChEMBL	342	5	1	3	4.1	CN(C)C(CNC(=O)c1sccc1Cl)c1ccccc1Cl	10.1016/j.ejmech.2022.114728
	124037297	160173	None	0	Human	Functional	pEC50	=	6.0	6.0	4	2	HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.	ChEMBL	713	28	2	14	1.3	COCCOCCOCCOCCOCCOCCOCCOCCOCCO[C@H]1CC[C@@]2(O)C3Cc4ccc(O)c5c4[C@@]2(CCN3C)[C@H]1O5	nan
	CHEMBL4108525	160173	None	0	Human	Functional	pEC50	=	6.0	6.0	4	2	HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.	ChEMBL	713	28	2	14	1.3	COCCOCCOCCOCCOCCOCCOCCOCCOCCO[C@H]1CC[C@@]2(O)C3Cc4ccc(O)c5c4[C@@]2(CCN3C)[C@H]1O5	nan
	118562576	173541	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	470	8	0	4	4.7	O=C1C(COCc2ccccc2)OC2(CCN(CCc3ccccc3)CC2)CN1c1ccccc1	10.1021/acs.jmedchem.9b01256
	CHEMBL4528962	173541	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	470	8	0	4	4.7	O=C1C(COCc2ccccc2)OC2(CCN(CCc3ccccc3)CC2)CN1c1ccccc1	10.1021/acs.jmedchem.9b01256
	155526412	176591	None	0	Rat	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method	ChEMBL	494	10	3	4	5.4	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCc1cc(Cc2ccccc2)ccc1OCc1ccccc1	10.1021/acs.jmedchem.9b00219
	CHEMBL4459283	176591	None	0	Rat	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method	ChEMBL	494	10	3	4	5.4	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCc1cc(Cc2ccccc2)ccc1OCc1ccccc1	10.1021/acs.jmedchem.9b00219
	CHEMBL4596662	176591	None	0	Rat	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method	ChEMBL	494	10	3	4	5.4	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCc1cc(Cc2ccccc2)ccc1OCc1ccccc1	10.1021/acs.jmedchem.9b00219
	71761637	91434	None	0	Rat	Functional	pEC50	=	6.0	6.0	1	2	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	635	7	8	10	-2.4	NC(=O)[C@@H]1C/N=C(/N2CCCC2)NC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1	10.1021/jm4008592
	CHEMBL2402929	91434	None	0	Rat	Functional	pEC50	=	6.0	6.0	1	2	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	635	7	8	10	-2.4	NC(=O)[C@@H]1C/N=C(/N2CCCC2)NC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1	10.1021/jm4008592
	145973938	164682	None	0	Human	Functional	pEC50	=	6.0	6.0	-	1	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 assayAgonist 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	ChEMBL	365	5	1	4	4.1	CCOc1ccc(C(C)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)cc1	10.1021/acs.jmedchem.8b01136
	CHEMBL4215601	164682	None	0	Human	Functional	pEC50	=	6.0	6.0	-	1	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 assayAgonist 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	ChEMBL	365	5	1	4	4.1	CCOc1ccc(C(C)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)cc1	10.1021/acs.jmedchem.8b01136
	4368841	51961	None	1	Human	Functional	pEC50	=	5.0	5.0	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	531	4	0	8	4.1	Cc1nc(N2CCN(c3ccccn3)CC2)c2c(C)c(C(=O)N3CCN(c4ccc(F)cc4)CC3)sc2n1	nan
	CHEMBL1586285	51961	None	1	Human	Functional	pEC50	=	5.0	5.0	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	531	4	0	8	4.1	Cc1nc(N2CCN(c3ccccn3)CC2)c2c(C)c(C(=O)N3CCN(c4ccc(F)cc4)CC3)sc2n1	nan
	162669410	182744	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	334	4	0	3	2.5	CCN1CC2(CCN(CCc3ccc(F)cc3)CC2)O[C@H](C)C1=O	10.1021/acs.jmedchem.0c01127
	CHEMBL4788650	182744	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	334	4	0	3	2.5	CCN1CC2(CCN(CCc3ccc(F)cc3)CC2)O[C@H](C)C1=O	10.1021/acs.jmedchem.0c01127
	23661598	94092	None	0	Human	Functional	pEC50	=	6.0	6.0	-67	2	Activity at mu opioid receptor assessed as stimulation of [35S]GTP-gamma-S bindingActivity at mu opioid receptor assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	392	0	3	4	2.9	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccc(F)cc4c2C[C@@]3(O)[C@H]1C5	10.1016/j.bmcl.2007.07.098
	CHEMBL248839	94092	None	0	Human	Functional	pEC50	=	6.0	6.0	-67	2	Activity at mu opioid receptor assessed as stimulation of [35S]GTP-gamma-S bindingActivity at mu opioid receptor assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	392	0	3	4	2.9	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccc(F)cc4c2C[C@@]3(O)[C@H]1C5	10.1016/j.bmcl.2007.07.098
	CHEMBL408330	215165	None	0	Rat	Functional	pEC50	=	7.0	7.0	-9	4	Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCC)NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm050921q
	44246590	59319	None	0	Human	Functional	pEC50	=	5.0	5.0	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	591	12	2	5	5.6	CC[C@@H](C)[C@@H]1CN([C@@H](CN2CCC[C@H]2CN2C(N)=NC[C@H]2C(C)C)C(C)C)C(=N)N1CCc1ccc(Cl)c(Cl)c1	nan
	CHEMBL1705302	59319	None	0	Human	Functional	pEC50	=	5.0	5.0	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	591	12	2	5	5.6	CC[C@@H](C)[C@@H]1CN([C@@H](CN2CCC[C@H]2CN2C(N)=NC[C@H]2C(C)C)C(C)C)C(=N)N1CCc1ccc(Cl)c(Cl)c1	nan
	CHEMBL5073754	216793	None	0	Human	Functional	pEC50	=	6.0	6.0	-41	2	Agonist activity at human mu opioid receptor expressed in HEK293T cells assessed as Galphai2 activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human mu opioid receptor expressed in HEK293T cells assessed as Galphai2 activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay	ChEMBL		None	None	None		CN(C)C(=O)C(CCNCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1	10.1021/acs.jmedchem.1c00611
	CHEMBL5071286	216744	None	3	Human	Functional	pEC50	=	5.0	5.0	-	1	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 assayAgonist 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	ChEMBL		None	None	None		CC[C@@H]1CN2CC[C@@]3(O)C(=Nc4cccc(-c5ccoc5)c43)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.1c01273
	118562538	169845	None	0	Human	Functional	pEC50	=	8.0	8.0	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	376	4	0	3	3.7	O=C1N(c2ccccc2)CC2(CCN(CCc3ccccc3)CC2)OC12CC2	10.1021/acs.jmedchem.9b01256
	CHEMBL4438550	169845	None	0	Human	Functional	pEC50	=	8.0	8.0	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	376	4	0	3	3.7	O=C1N(c2ccccc2)CC2(CCN(CCc3ccccc3)CC2)OC12CC2	10.1021/acs.jmedchem.9b01256
	132079918	179967	None	0	Human	Functional	pEC50	=	8.0	8.0	13	2	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 assayAgonist 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	ChEMBL	522	5	0	9	4.4	COC(=O)[C@@H]1C=C(OC(=O)c2cccc(OC)c2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@@]12C	10.1021/acs.jmedchem.6b01235
	CHEMBL4745430	179967	None	0	Human	Functional	pEC50	=	8.0	8.0	13	2	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 assayAgonist 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	ChEMBL	522	5	0	9	4.4	COC(=O)[C@@H]1C=C(OC(=O)c2cccc(OC)c2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@@]12C	10.1021/acs.jmedchem.6b01235
	44444601	94283	None	0	Human	Functional	pEC50	=	8.0	8.0	-23	3	Agonist activity at human mu opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assay	ChEMBL	508	8	1	3	6.3	COc1ccc(-c2ccc(CCNC(=O)c3ccc4c(c3)[C@@]3(C)CCN(CC5CC5)C(C4)[C@@H]3C)cc2)cc1	10.1016/j.bmcl.2007.09.082
	CHEMBL249985	94283	None	0	Human	Functional	pEC50	=	8.0	8.0	-23	3	Agonist activity at human mu opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assay	ChEMBL	508	8	1	3	6.3	COc1ccc(-c2ccc(CCNC(=O)c3ccc4c(c3)[C@@]3(C)CCN(CC5CC5)C(C4)[C@@H]3C)cc2)cc1	10.1016/j.bmcl.2007.09.082
	44427180	92170	None	0	Human	Functional	pEC50	=	8.0	8.0	-1	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	ChEMBL	368	3	1	3	4.3	CNC(=O)Oc1ccc2c(c1)C13CCCCC1C(C2)N(CC1CCC1)CC3	10.1016/j.bmcl.2007.01.013
	CHEMBL242046	92170	None	0	Human	Functional	pEC50	=	8.0	8.0	-1	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	ChEMBL	368	3	1	3	4.3	CNC(=O)Oc1ccc2c(c1)C13CCCCC1C(C2)N(CC1CCC1)CC3	10.1016/j.bmcl.2007.01.013
	44597714	201395	None	0	Human	Functional	pEC50	=	8.0	8.0	-4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	845	15	0	6	12.3	CC(C)(CCCCCCC(C)(C)C(=O)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3)C(=O)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	10.1021/jm900379p
	CHEMBL584790	201395	None	0	Human	Functional	pEC50	=	8.0	8.0	-4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	845	15	0	6	12.3	CC(C)(CCCCCCC(C)(C)C(=O)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3)C(=O)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	10.1021/jm900379p
	CHEMBL5078909	217081	None	0	Human	Functional	pEC50	=	8.0	8.0	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as beta arrestin-2 recruitment incubated for 3 days by PathHunter assayAgonist activity at mu opioid receptor (unknown origin) assessed as beta arrestin-2 recruitment incubated for 3 days by PathHunter assay	ChEMBL		None	None	None		FC1(F)CCc2csc(CNCC[C@@]3(c4ccccn4)CCOC4(CCCC4)C3)c2C1	10.1016/j.ejmech.2021.113986
	23634921	146536	None	0	Rat	Functional	pEC50	=	8.0	8.0	10	3	Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay	ChEMBL	832	19	7	9	2.3	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)CCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1	10.1021/jm061465o
	CHEMBL392206	146536	None	0	Rat	Functional	pEC50	=	8.0	8.0	10	3	Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay	ChEMBL	832	19	7	9	2.3	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)CCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1	10.1021/jm061465o
	CHEMBL5081106	217210	None	0	Human	Functional	pEC50	=	8.0	8.0	-	1	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 assayAgonist 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	ChEMBL		None	None	None		CC[C@@H]1CN2CC[C@@]3(O)C(=Nc4c(C)ccc(OC)c43)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.1c01273
	CHEMBL5081106	217210	None	0	Human	Functional	pEC50	=	8.0	8.0	-	1	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 assayAgonist 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	ChEMBL		None	None	None		CC[C@@H]1CN2CC[C@@]3(O)C(=Nc4c(C)ccc(OC)c43)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.1c01273
	71454514	79174	None	0	Human	Functional	pEC50	=	8.0	8.0	1	2	Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	531	6	2	7	3.6	CO[C@@]12CC[C@@]3(C[C@@H]1CNC(=O)/C=C/c1ccc([N+](=O)[O-])cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1021/jm070255o
	CHEMBL2113308	79174	None	0	Human	Functional	pEC50	=	8.0	8.0	1	2	Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	531	6	2	7	3.6	CO[C@@]12CC[C@@]3(C[C@@H]1CNC(=O)/C=C/c1ccc([N+](=O)[O-])cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1021/jm070255o
	86711652	160116	None	0	Human	Functional	pEC50	=	7.9	7.9	-7	3	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	489	7	0	4	5.3	CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(F)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	nan
	CHEMBL4108017	160116	None	0	Human	Functional	pEC50	=	7.9	7.9	-7	3	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	489	7	0	4	5.3	CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(F)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	nan
	117738996	117797	None	0	Mouse	Functional	pEC50	=	7.9	7.9	-	1	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	558	5	3	7	2.6	CN(C)c1ccc2c(c1)CN(C)C(C(=O)N[C@H]1CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]1O6)C2	10.1016/j.bmc.2015.02.055
	CHEMBL3401558	117797	None	0	Mouse	Functional	pEC50	=	7.9	7.9	-	1	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	558	5	3	7	2.6	CN(C)c1ccc2c(c1)CN(C)C(C(=O)N[C@H]1CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]1O6)C2	10.1016/j.bmc.2015.02.055
	CHEMBL3759981	214699	None	0	Human	Functional	pEC50	=	7.9	7.9	147	2	Agonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysisAgonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis	ChEMBL		None	None	None		Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC1=O	10.1016/j.ejmech.2015.12.012
	127032210	139280	None	0	Human	Functional	pEC50	=	7.9	7.9	-1	3	Agonist activity at human mu opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay	ChEMBL	426	2	2	4	4.1	Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(O)CCc1cc2ccccc2nc1C3	10.1016/j.bmc.2016.03.040
	CHEMBL3787663	139280	None	0	Human	Functional	pEC50	=	7.9	7.9	-1	3	Agonist activity at human mu opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay	ChEMBL	426	2	2	4	4.1	Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(O)CCc1cc2ccccc2nc1C3	10.1016/j.bmc.2016.03.040
	CHEMBL5079835	217135	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL		None	None	None		Cc1cc(C)cc(CNCC[C@@]2(c3ccccn3)CCOC3(CCOC3)C2)c1	10.1016/j.ejmech.2021.113986
	71459949	79167	None	0	Human	Functional	pEC50	=	7.9	7.9	3	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	530	7	1	6	4.0	COc1ccccc1/C=C/C(=O)NC[C@H]1C[C@@]23CC[C@@]1(OC)[C@@H]1Oc4c(OC)ccc5c4[C@@]12CCN(C)[C@@H]3C5	10.1021/jm070255o
	CHEMBL2113301	79167	None	0	Human	Functional	pEC50	=	7.9	7.9	3	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	530	7	1	6	4.0	COc1ccccc1/C=C/C(=O)NC[C@H]1C[C@@]23CC[C@@]1(OC)[C@@H]1Oc4c(OC)ccc5c4[C@@]12CCN(C)[C@@H]3C5	10.1021/jm070255o
	CHEMBL262172	212987	None	0	Rat	Functional	pEC50	=	7.9	7.9	-7	5	Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/jm050921q
	3668	1561	None	36	Human	Functional	pEC50	=	7.9	7.9	1	5	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL		None	None	None		None	10.1021/jm300664y
	5311081	1561	None	36	Human	Functional	pEC50	=	7.9	7.9	1	5	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL		None	None	None		None	10.1021/jm300664y
	CHEMBL333357	1561	None	36	Human	Functional	pEC50	=	7.9	7.9	1	5	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL		None	None	None		None	10.1021/jm300664y
	CHEMBL589982	1561	None	36	Human	Functional	pEC50	=	7.9	7.9	1	5	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL		None	None	None		None	10.1021/jm300664y
	46887087	8552	None	0	Mouse	Functional	pEC50	=	7.9	7.9	-22	3	Agonist activity at mu opioid receptor in Swiss albino mouse ileum assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at mu opioid receptor in Swiss albino mouse ileum assessed as inhibition of electrically-stimulated muscle contraction	ChEMBL	381	1	1	4	3.7	CO[C@]12C=C[C@@]3(C[C@@H]1C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1016/j.bmc.2010.03.068
	CHEMBL1094466	8552	None	0	Mouse	Functional	pEC50	=	7.9	7.9	-22	3	Agonist activity at mu opioid receptor in Swiss albino mouse ileum assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at mu opioid receptor in Swiss albino mouse ileum assessed as inhibition of electrically-stimulated muscle contraction	ChEMBL	381	1	1	4	3.7	CO[C@]12C=C[C@@]3(C[C@@H]1C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1016/j.bmc.2010.03.068
	CHEMBL408330	215165	None	0	Rat	Functional	pEC50	=	7.0	7.0	-9	4	Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCC)NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm050921q
	1647	1313	None	34	Human	Functional	pEC50	=	7.0	7.0	-3	9	Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL		None	None	None		None	10.1021/jm050577x
	5462471	1313	None	34	Human	Functional	pEC50	=	7.0	7.0	-3	9	Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL		None	None	None		None	10.1021/jm050577x
	CHEMBL113995	1313	None	34	Human	Functional	pEC50	=	7.0	7.0	-3	9	Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL		None	None	None		None	10.1021/jm050577x
	CHEMBL38874	1313	None	34	Human	Functional	pEC50	=	7.0	7.0	-3	9	Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL		None	None	None		None	10.1021/jm050577x
	137541811	158459	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	336	5	1	2	4.0	Cc1ccc(C(=O)NCC2c3ccccc3CCN2CC(C)C)cc1	10.1016/j.ejmech.2016.09.003
	CHEMBL4089738	158459	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	336	5	1	2	4.0	Cc1ccc(C(=O)NCC2c3ccccc3CCN2CC(C)C)cc1	10.1016/j.ejmech.2016.09.003
	55433787	164356	None	1	Human	Functional	pEC50	=	7.0	7.0	-	1	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 methodAgonist 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	ChEMBL	403	3	1	3	4.1	O=c1[nH]c2ccccc2n1C1CCN(Cc2ccc(Br)cc2F)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4211596	164356	None	1	Human	Functional	pEC50	=	7.0	7.0	-	1	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 methodAgonist 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	ChEMBL	403	3	1	3	4.1	O=c1[nH]c2ccccc2n1C1CCN(Cc2ccc(Br)cc2F)CC1	10.1021/acs.jmedchem.8b01136
	1647	1313	None	34	Human	Functional	pEC50	=	7.0	7.0	-3	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting	ChEMBL		None	None	None		None	10.1021/jm101542c
	5462471	1313	None	34	Human	Functional	pEC50	=	7.0	7.0	-3	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting	ChEMBL		None	None	None		None	10.1021/jm101542c
	CHEMBL113995	1313	None	34	Human	Functional	pEC50	=	7.0	7.0	-3	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting	ChEMBL		None	None	None		None	10.1021/jm101542c
	CHEMBL38874	1313	None	34	Human	Functional	pEC50	=	7.0	7.0	-3	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting	ChEMBL		None	None	None		None	10.1021/jm101542c
	1647	1313	None	34	Human	Functional	pEC50	=	7.0	7.0	-3	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	ChEMBL		None	None	None		None	10.1016/j.bmcl.2007.01.013
	5462471	1313	None	34	Human	Functional	pEC50	=	7.0	7.0	-3	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	ChEMBL		None	None	None		None	10.1016/j.bmcl.2007.01.013
	CHEMBL113995	1313	None	34	Human	Functional	pEC50	=	7.0	7.0	-3	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	ChEMBL		None	None	None		None	10.1016/j.bmcl.2007.01.013
	CHEMBL38874	1313	None	34	Human	Functional	pEC50	=	7.0	7.0	-3	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	ChEMBL		None	None	None		None	10.1016/j.bmcl.2007.01.013
	1647	1313	None	34	Human	Functional	pEC50	=	7.0	7.0	-3	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 minsAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins	ChEMBL		None	None	None		None	10.1016/j.bmc.2007.03.076
	5462471	1313	None	34	Human	Functional	pEC50	=	7.0	7.0	-3	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 minsAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins	ChEMBL		None	None	None		None	10.1016/j.bmc.2007.03.076
	CHEMBL113995	1313	None	34	Human	Functional	pEC50	=	7.0	7.0	-3	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 minsAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins	ChEMBL		None	None	None		None	10.1016/j.bmc.2007.03.076
	CHEMBL38874	1313	None	34	Human	Functional	pEC50	=	7.0	7.0	-3	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 minsAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins	ChEMBL		None	None	None		None	10.1016/j.bmc.2007.03.076
	44592089	179117	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	312	1	1	4	1.0	CN1CC[C@]23c4c5ccc(C(N)=O)c4O[C@H]2C(=O)CC[C@H]3[C@H]1C5	10.1016/j.bmcl.2009.02.078
	CHEMBL471049	179117	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	312	1	1	4	1.0	CN1CC[C@]23c4c5ccc(C(N)=O)c4O[C@H]2C(=O)CC[C@H]3[C@H]1C5	10.1016/j.bmcl.2009.02.078
	16720646	137674	None	0	Human	Functional	pEC50	=	7.0	7.0	-158	3	Agonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	398	2	2	2	5.0	Oc1ccc2c(c1)[C@]13CCN(CC4CCC4)[C@H](C2)[C@@H]1Cc1c([nH]c2ccccc12)C3	10.1021/jm0701674
	CHEMBL375504	137674	None	0	Human	Functional	pEC50	=	7.0	7.0	-158	3	Agonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	398	2	2	2	5.0	Oc1ccc2c(c1)[C@]13CCN(CC4CCC4)[C@H](C2)[C@@H]1Cc1c([nH]c2ccccc12)C3	10.1021/jm0701674
	1614	2495	None	37	Human	Functional	pEC50	=	7.0	7.0	-95	5	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as reduction in beta-arrestin 2 recruitment measured after 1.5 hrs by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as reduction in beta-arrestin 2 recruitment measured after 1.5 hrs by PathHunter assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2022.114728
	443363	2495	None	37	Human	Functional	pEC50	=	7.0	7.0	-95	5	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as reduction in beta-arrestin 2 recruitment measured after 1.5 hrs by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as reduction in beta-arrestin 2 recruitment measured after 1.5 hrs by PathHunter assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2022.114728
	CHEMBL13786	2495	None	37	Human	Functional	pEC50	=	7.0	7.0	-95	5	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as reduction in beta-arrestin 2 recruitment measured after 1.5 hrs by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as reduction in beta-arrestin 2 recruitment measured after 1.5 hrs by PathHunter assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2022.114728
	DB12668	2495	None	37	Human	Functional	pEC50	=	7.0	7.0	-95	5	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as reduction in beta-arrestin 2 recruitment measured after 1.5 hrs by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as reduction in beta-arrestin 2 recruitment measured after 1.5 hrs by PathHunter assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2022.114728
	137631684	156456	None	0	Human	Functional	pEC50	=	7.0	7.0	-3890	2	Agonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assayAgonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assay	ChEMBL	508	5	3	7	3.0	CN(C(=O)/C=C/c1ccsc1)[C@@H]1CC[C@@]2(O)[C@H]3[C@@H](O)c4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2017.06.017
	CHEMBL4066058	156456	None	0	Human	Functional	pEC50	=	7.0	7.0	-3890	2	Agonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assayAgonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assay	ChEMBL	508	5	3	7	3.0	CN(C(=O)/C=C/c1ccsc1)[C@@H]1CC[C@@]2(O)[C@H]3[C@@H](O)c4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2017.06.017
	1647	1313	None	34	Human	Functional	pEC50	=	7.0	7.0	-3	9	Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL		None	None	None		None	10.1021/jm061327z
	5462471	1313	None	34	Human	Functional	pEC50	=	7.0	7.0	-3	9	Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL		None	None	None		None	10.1021/jm061327z
	CHEMBL113995	1313	None	34	Human	Functional	pEC50	=	7.0	7.0	-3	9	Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL		None	None	None		None	10.1021/jm061327z
	CHEMBL38874	1313	None	34	Human	Functional	pEC50	=	7.0	7.0	-3	9	Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL		None	None	None		None	10.1021/jm061327z
	44570025	176951	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	312	3	1	2	3.3	CC(C)=CCN1CC[C@@]2(C)c3cc(C(N)=O)ccc3C[C@@H]1[C@@H]2C	nan
	CHEMBL461227	176951	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	312	3	1	2	3.3	CC(C)=CCN1CC[C@@]2(C)c3cc(C(N)=O)ccc3C[C@@H]1[C@@H]2C	nan
	44341722	9983	None	0	Human	Functional	pEC50	=	7.0	7.0	-1	3	Agonistic activity against human opioid Mu receptor transfected into Chinese hamster ovary (CHO) cells using [3H]-DAMGO as radioligandAgonistic activity against human opioid Mu receptor transfected into Chinese hamster ovary (CHO) cells using [3H]-DAMGO as radioligand	ChEMBL	353	0	3	7	0.8	CN1CCC23c4c5ccc(O)c4OC2c2nc(O)ncc2CC3(O)C1C5	10.1016/s0960-894x(99)00608-3
	CHEMBL114803	9983	None	0	Human	Functional	pEC50	=	7.0	7.0	-1	3	Agonistic activity against human opioid Mu receptor transfected into Chinese hamster ovary (CHO) cells using [3H]-DAMGO as radioligandAgonistic activity against human opioid Mu receptor transfected into Chinese hamster ovary (CHO) cells using [3H]-DAMGO as radioligand	ChEMBL	353	0	3	7	0.8	CN1CCC23c4c5ccc(O)c4OC2c2nc(O)ncc2CC3(O)C1C5	10.1016/s0960-894x(99)00608-3
	172470340	197126	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	380	6	0	4	2.7	CCC(=O)N(CC(C)N1CCN(C(=O)c2ccccc2)CC1)c1ccccn1	10.1021/acs.jmedchem.3c01637
	CHEMBL5439322	197126	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	380	6	0	4	2.7	CCC(=O)N(CC(C)N1CCN(C(=O)c2ccccc2)CC1)c1ccccn1	10.1021/acs.jmedchem.3c01637
	11179386	159753	None	5	Human	Functional	pEC50	=	6.0	6.0	-43651	2	Agonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assayAgonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assay	ChEMBL	492	5	3	7	2.6	CN(C(=O)/C=C/c1ccoc1)[C@@H]1CC[C@@]2(O)[C@H]3[C@@H](O)c4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2017.06.017
	CHEMBL4103819	159753	None	5	Human	Functional	pEC50	=	6.0	6.0	-43651	2	Agonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assayAgonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assay	ChEMBL	492	5	3	7	2.6	CN(C(=O)/C=C/c1ccoc1)[C@@H]1CC[C@@]2(O)[C@H]3[C@@H](O)c4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2017.06.017
	3132840	201121	None	4	Human	Functional	pEC50	=	6.0	6.0	3	2	Inhibition of mu-opioid receptor (unknown origin) by [35S]-GTPgammaS binding assayInhibition of mu-opioid receptor (unknown origin) by [35S]-GTPgammaS binding assay	ChEMBL	383	8	2	4	4.8	CCC1(C)CC(CCNCc2ccccc2O)(c2ccccc2OC)CCO1	10.1016/j.ejmech.2019.111701
	CHEMBL579408	201121	None	4	Human	Functional	pEC50	=	6.0	6.0	3	2	Inhibition of mu-opioid receptor (unknown origin) by [35S]-GTPgammaS binding assayInhibition of mu-opioid receptor (unknown origin) by [35S]-GTPgammaS binding assay	ChEMBL	383	8	2	4	4.8	CCC1(C)CC(CCNCc2ccccc2O)(c2ccccc2OC)CCO1	10.1016/j.ejmech.2019.111701
	CHEMBL5071286	216744	None	3	Human	Functional	pEC50	=	5.0	5.0	-	1	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 assayAgonist 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	ChEMBL		None	None	None		CC[C@@H]1CN2CC[C@@]3(O)C(=Nc4cccc(-c5ccoc5)c43)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.1c01273
	145965538	164417	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	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 methodAgonist 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	ChEMBL	359	3	1	3	4.0	O=c1[nH]c2cc(F)ccc2n1C1CCN(Cc2ccccc2Cl)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4212370	164417	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	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 methodAgonist 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	ChEMBL	359	3	1	3	4.0	O=c1[nH]c2cc(F)ccc2n1C1CCN(Cc2ccccc2Cl)CC1	10.1021/acs.jmedchem.8b01136
	155551877	176628	None	0	Rat	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method	ChEMBL	402	7	3	3	4.1	Cc1ccc(Cc2ccccc2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b00219
	CHEMBL4569796	176628	None	0	Rat	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method	ChEMBL	402	7	3	3	4.1	Cc1ccc(Cc2ccccc2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b00219
	CHEMBL4597010	176628	None	0	Rat	Functional	pEC50	=	7.0	7.0	-	1	Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method	ChEMBL	402	7	3	3	4.1	Cc1ccc(Cc2ccccc2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b00219
	172466088	196858	None	0	Human	Functional	pEC50	=	5.0	5.0	-	1	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assay	ChEMBL	330	5	1	3	4.1	CN(C)C(CNC(=O)c1cc2ccccc2s1)C1CCCCC1	10.1016/j.ejmech.2022.114728
	CHEMBL5433534	196858	None	0	Human	Functional	pEC50	=	5.0	5.0	-	1	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assay	ChEMBL	330	5	1	3	4.1	CN(C)C(CNC(=O)c1cc2ccccc2s1)C1CCCCC1	10.1016/j.ejmech.2022.114728
	CHEMBL5093143	217902	None	0	Human	Functional	pEC50	=	6.0	6.0	-	1	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 assayAgonist 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	ChEMBL		None	None	None		CC[C@@H]1CN2CCc3c([nH]c4c(-c5ccccc5)ccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.1c01273
	145963594	161508	None	0	Human	Functional	pEC50	=	7.0	7.0	-3	3	Agonist activity at MOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assayAgonist activity at MOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assay	ChEMBL	1080	12	10	14	0.5	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCN(CC2)C(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O	10.1016/j.bmc.2018.05.045
	CHEMBL4126803	161508	None	0	Human	Functional	pEC50	=	7.0	7.0	-3	3	Agonist activity at MOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assayAgonist activity at MOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assay	ChEMBL	1080	12	10	14	0.5	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCN(CC2)C(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O	10.1016/j.bmc.2018.05.045
	134563420	195891	None	0	Human	Functional	pEC50	=	7.0	7.0	-2	3	Agonist activity at human MOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 minsAgonist activity at human MOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 mins	ChEMBL	395	5	1	3	5.1	CC(=O)NCc1cc2ccccc2n1C1CCN([C@H]2CC[C@@H](C(C)C)CC2)CC1	10.1016/j.bmc.2023.117421
	CHEMBL5412738	195891	None	0	Human	Functional	pEC50	=	7.0	7.0	-2	3	Agonist activity at human MOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 minsAgonist activity at human MOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 mins	ChEMBL	395	5	1	3	5.1	CC(=O)NCc1cc2ccccc2n1C1CCN([C@H]2CC[C@@H](C(C)C)CC2)CC1	10.1016/j.bmc.2023.117421
	145963594	161508	None	0	Human	Functional	pEC50	=	7.0	7.0	-3	3	Agonist activity at MOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assayAgonist activity at MOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assay	ChEMBL	1080	12	10	14	0.5	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCN(CC2)C(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O	10.1016/j.bmc.2018.05.045
	CHEMBL4126803	161508	None	0	Human	Functional	pEC50	=	7.0	7.0	-3	3	Agonist activity at MOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assayAgonist activity at MOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assay	ChEMBL	1080	12	10	14	0.5	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCN(CC2)C(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O	10.1016/j.bmc.2018.05.045
	121684957	159438	None	0	Human	Functional	pEC50	=	6.0	6.0	-	1	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	300	4	2	2	3.2	CCC1CCC(C(=O)NCC2NCCc3ccccc32)CC1	10.1016/j.ejmech.2016.09.003
	CHEMBL4100195	159438	None	0	Human	Functional	pEC50	=	6.0	6.0	-	1	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	300	4	2	2	3.2	CCC1CCC(C(=O)NCC2NCCc3ccccc32)CC1	10.1016/j.ejmech.2016.09.003
	5030548	159655	None	0	Human	Functional	pEC50	=	6.0	6.0	-	1	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	574	6	1	4	5.3	O=C(NCC1c2ccccc2CCN1S(=O)(=O)c1ccc(Br)cc1OC(F)(F)F)C1CCCCC1	10.1016/j.ejmech.2016.09.003
	CHEMBL4102638	159655	None	0	Human	Functional	pEC50	=	6.0	6.0	-	1	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	574	6	1	4	5.3	O=C(NCC1c2ccccc2CCN1S(=O)(=O)c1ccc(Br)cc1OC(F)(F)F)C1CCCCC1	10.1016/j.ejmech.2016.09.003
	715224	113934	None	9	Human	Functional	pEC50	=	6.0	6.0	-	1	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	332	1	0	3	4.1	Cc1nn(-c2ccccc2Br)c2c1C(=O)CC(C)(C)C2	10.1016/j.bmc.2014.07.012
	CHEMBL3325700	113934	None	9	Human	Functional	pEC50	=	6.0	6.0	-	1	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	332	1	0	3	4.1	Cc1nn(-c2ccccc2Br)c2c1C(=O)CC(C)(C)C2	10.1016/j.bmc.2014.07.012
	CHEMBL5093143	217902	None	0	Human	Functional	pEC50	=	6.0	6.0	-	1	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 assayAgonist 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	ChEMBL		None	None	None		CC[C@@H]1CN2CCc3c([nH]c4c(-c5ccccc5)ccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.1c01273
	156014251	177304	None	0	Human	Functional	pEC50	=	6.0	6.0	-	1	Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting methodAgonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method	ChEMBL	643	17	8	8	1.6	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1	10.1016/j.bmc.2020.115438
	CHEMBL4635184	177304	None	0	Human	Functional	pEC50	=	6.0	6.0	-	1	Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting methodAgonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method	ChEMBL	643	17	8	8	1.6	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1	10.1016/j.bmc.2020.115438
	86711654	160589	None	0	Human	Functional	pEC50	=	7.0	7.0	-1	3	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	578	9	0	6	4.4	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CN(Cc1ccccc1)S(C)(=O)=O)C2	nan
	CHEMBL4112051	160589	None	0	Human	Functional	pEC50	=	7.0	7.0	-1	3	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	578	9	0	6	4.4	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CN(Cc1ccccc1)S(C)(=O)=O)C2	nan
	89978667	161042	None	0	Human	Functional	pEC50	=	6.0	6.0	1	2	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	468	8	1	6	2.4	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCC(N)=O)C2	nan
	CHEMBL4115536	161042	None	0	Human	Functional	pEC50	=	6.0	6.0	1	2	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	468	8	1	6	2.4	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCC(N)=O)C2	nan
	172449716	195885	None	0	Mouse	Functional	pEC50	=	5.9	5.9	-8	2	Partial 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 assayPartial 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	ChEMBL	682	13	1	6	5.0	CN(C)C(=O)C(CCN1C[C@H](F)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(C(F)(F)F)n2)CC1)(c1ccccc1)c1ccccc1	10.1021/acs.jmedchem.3c00417
	CHEMBL5412606	195885	None	0	Mouse	Functional	pEC50	=	5.9	5.9	-8	2	Partial 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 assayPartial 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	ChEMBL	682	13	1	6	5.0	CN(C)C(=O)C(CCN1C[C@H](F)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(C(F)(F)F)n2)CC1)(c1ccccc1)c1ccccc1	10.1021/acs.jmedchem.3c00417
	72735386	106425	None	0	Human	Functional	pEC50	=	6.9	6.9	-81	2	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay	ChEMBL	404	2	2	4	3.3	Oc1ccc2c(c1)[C@]13CCN(CCF)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3	10.1016/j.bmc.2013.10.032
	CHEMBL3139248	106425	None	0	Human	Functional	pEC50	=	6.9	6.9	-81	2	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay	ChEMBL	404	2	2	4	3.3	Oc1ccc2c(c1)[C@]13CCN(CCF)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3	10.1016/j.bmc.2013.10.032
	CHEMBL4296731	106425	None	0	Human	Functional	pEC50	=	6.9	6.9	-81	2	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay	ChEMBL	404	2	2	4	3.3	Oc1ccc2c(c1)[C@]13CCN(CCF)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3	10.1016/j.bmc.2013.10.032
	11562400	96851	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	500	4	0	9	4.4	COC(=O)[C@@H]1C[C@H](OC(=O)c2cccs2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@]21C	10.1021/jm701162g
	CHEMBL264967	96851	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	500	4	0	9	4.4	COC(=O)[C@@H]1C[C@H](OC(=O)c2cccs2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@]21C	10.1021/jm701162g
	24735767	163634	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	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 methodAgonist 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	ChEMBL	337	4	1	4	3.2	COc1cccc(CN2CCC(n3c(=O)[nH]c4ccccc43)CC2)c1	10.1021/acs.jmedchem.8b01136
	CHEMBL4202891	163634	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	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 methodAgonist 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	ChEMBL	337	4	1	4	3.2	COc1cccc(CN2CCC(n3c(=O)[nH]c4ccccc43)CC2)c1	10.1021/acs.jmedchem.8b01136
	172449716	195885	None	0	Mouse	Functional	pEC50	=	5.9	5.9	-8	2	Partial 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 assayPartial 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	ChEMBL	682	13	1	6	5.0	CN(C)C(=O)C(CCN1C[C@H](F)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(C(F)(F)F)n2)CC1)(c1ccccc1)c1ccccc1	10.1021/acs.jmedchem.3c00417
	CHEMBL5412606	195885	None	0	Mouse	Functional	pEC50	=	5.9	5.9	-8	2	Partial 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 assayPartial 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	ChEMBL	682	13	1	6	5.0	CN(C)C(=O)C(CCN1C[C@H](F)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(C(F)(F)F)n2)CC1)(c1ccccc1)c1ccccc1	10.1021/acs.jmedchem.3c00417
	CHEMBL5082661	217305	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	Agonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assay	ChEMBL		None	None	None		CN1CCN(C2(CNC(=O)C(C)(c3ccccc3)c3ccccc3)CCCCC2)CC1	10.1021/acs.jmedchem.1c00417
	156018208	177981	None	0	Human	Functional	pEC50	=	6.9	6.9	-3	3	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	588	8	1	5	7.0	Oc1ccc2c3c1O[C@H]1c4ncc(-c5ccc(F)cc5)cc4C[C@@]4(OCCCc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/acs.jmedchem.0c00503
	CHEMBL4644543	177981	None	0	Human	Functional	pEC50	=	6.9	6.9	-3	3	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	588	8	1	5	7.0	Oc1ccc2c3c1O[C@H]1c4ncc(-c5ccc(F)cc5)cc4C[C@@]4(OCCCc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/acs.jmedchem.0c00503
	155536262	176451	None	0	Rat	Functional	pEC50	=	6.9	6.9	-	1	Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method	ChEMBL	445	8	4	4	3.7	CC(=O)Nc1ccc(Cc2ccccc2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b00219
	CHEMBL4473111	176451	None	0	Rat	Functional	pEC50	=	6.9	6.9	-	1	Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method	ChEMBL	445	8	4	4	3.7	CC(=O)Nc1ccc(Cc2ccccc2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b00219
	CHEMBL4595573	176451	None	0	Rat	Functional	pEC50	=	6.9	6.9	-	1	Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method	ChEMBL	445	8	4	4	3.7	CC(=O)Nc1ccc(Cc2ccccc2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b00219
	46227360	205039	None	0	Rat	Functional	pEC50	=	6.9	6.9	-25	5	Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	1210	18	10	12	4.6	CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1016/j.bmc.2009.08.035
	CHEMBL611924	205039	None	0	Rat	Functional	pEC50	=	6.9	6.9	-25	5	Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	1210	18	10	12	4.6	CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1016/j.bmc.2009.08.035
	73212368	104525	None	0	Rat	Functional	pEC50	=	6.9	6.9	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cells assessed as stimulation of [35S]-GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat mu opioid receptor expressed in rat C6 cells assessed as stimulation of [35S]-GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	394	7	2	3	4.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CCC(CCCc2ccccc2)CC1	10.1016/j.bmcl.2013.12.021
	CHEMBL3104107	104525	None	0	Rat	Functional	pEC50	=	6.9	6.9	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cells assessed as stimulation of [35S]-GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat mu opioid receptor expressed in rat C6 cells assessed as stimulation of [35S]-GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	394	7	2	3	4.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CCC(CCCc2ccccc2)CC1	10.1016/j.bmcl.2013.12.021
	71624270	90498	None	0	Human	Functional	pEC50	=	6.9	6.9	-2	2	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis	ChEMBL	354	3	0	2	4.8	CC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21	10.1016/j.bmcl.2013.03.101
	CHEMBL2387194	90498	None	0	Human	Functional	pEC50	=	6.9	6.9	-2	2	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis	ChEMBL	354	3	0	2	4.8	CC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21	10.1016/j.bmcl.2013.03.101
	168277465	190698	None	0	Rat	Functional	pEC50	=	5.9	5.9	-4	2	Agonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay	ChEMBL	499	6	0	5	5.2	COc1ccc2c3c1O[C@H]1[C@@]4(OC)CC[C@@]5(C[C@@]4(C)C(=O)c4ccccc4)[C@@H](C2)N(CC2CC2)CC[C@]315	10.1021/acs.jmedchem.2c00014
	CHEMBL5180450	190698	None	0	Rat	Functional	pEC50	=	5.9	5.9	-4	2	Agonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay	ChEMBL	499	6	0	5	5.2	COc1ccc2c3c1O[C@H]1[C@@]4(OC)CC[C@@]5(C[C@@]4(C)C(=O)c4ccccc4)[C@@H](C2)N(CC2CC2)CC[C@]315	10.1021/acs.jmedchem.2c00014
	CHEMBL262172	212987	None	0	Rat	Functional	pEC50	=	7.9	7.9	-7	5	Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/jm050921q
	44406657	132805	None	0	Human	Functional	pEC50	=	7.9	7.9	-7	2	Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	821	15	0	8	9.8	O=C(CCCCCCCCC(=O)Oc1ccc2c(c1)[C@@]13CCCCC1[C@@H](C2)N(C[C@@H]1CCCO1)CC3)Oc1ccc2c(c1)[C@@]13CCCCC1[C@@H](C2)N(C[C@@H]1CCCO1)CC3	10.1021/jm050577x
	CHEMBL369919	132805	None	0	Human	Functional	pEC50	=	7.9	7.9	-7	2	Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	821	15	0	8	9.8	O=C(CCCCCCCCC(=O)Oc1ccc2c(c1)[C@@]13CCCCC1[C@@H](C2)N(C[C@@H]1CCCO1)CC3)Oc1ccc2c(c1)[C@@]13CCCCC1[C@@H](C2)N(C[C@@H]1CCCO1)CC3	10.1021/jm050577x
	3668	1561	None	36	Human	Functional	pEC50	=	7.9	7.9	1	5	Agonist activity at human MOP assessed as forskolin stimulated cAMP accumulationAgonist activity at human MOP assessed as forskolin stimulated cAMP accumulation	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01915
	5311081	1561	None	36	Human	Functional	pEC50	=	7.9	7.9	1	5	Agonist activity at human MOP assessed as forskolin stimulated cAMP accumulationAgonist activity at human MOP assessed as forskolin stimulated cAMP accumulation	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01915
	CHEMBL333357	1561	None	36	Human	Functional	pEC50	=	7.9	7.9	1	5	Agonist activity at human MOP assessed as forskolin stimulated cAMP accumulationAgonist activity at human MOP assessed as forskolin stimulated cAMP accumulation	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01915
	CHEMBL589982	1561	None	36	Human	Functional	pEC50	=	7.9	7.9	1	5	Agonist activity at human MOP assessed as forskolin stimulated cAMP accumulationAgonist activity at human MOP assessed as forskolin stimulated cAMP accumulation	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01915
	CHEMBL5094899	218008	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assay	ChEMBL		None	None	None		CCC(=O)N(CC1(N2CCN(Cc3ccccc3)CC2)CC1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00417
	16049012	154735	None	0	Human	Functional	pEC50	=	7.9	7.9	3	2	Agonist activity at human mu opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assay	ChEMBL	478	7	1	2	6.3	C[C@H]1C2Cc3ccc(C(=O)NCCc4ccccc4-c4ccccc4)cc3[C@@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2007.09.082
	CHEMBL399465	154735	None	0	Human	Functional	pEC50	=	7.9	7.9	3	2	Agonist activity at human mu opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assay	ChEMBL	478	7	1	2	6.3	C[C@H]1C2Cc3ccc(C(=O)NCCc4ccccc4-c4ccccc4)cc3[C@@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2007.09.082
	44433402	88572	None	0	Human	Functional	pEC50	=	7.9	7.9	4	3	Agonist activity at human mu opioid receptor expressed in CHO membrane by [35S]GTP-gamma-S binding assayAgonist activity at human mu opioid receptor expressed in CHO membrane by [35S]GTP-gamma-S binding assay	ChEMBL	387	2	3	6	1.2	CO[C@]12CC(O)[C@@]3(C[C@@H]1[C@@H](C)O)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1016/j.bmcl.2007.06.050
	CHEMBL235239	88572	None	0	Human	Functional	pEC50	=	7.9	7.9	4	3	Agonist activity at human mu opioid receptor expressed in CHO membrane by [35S]GTP-gamma-S binding assayAgonist activity at human mu opioid receptor expressed in CHO membrane by [35S]GTP-gamma-S binding assay	ChEMBL	387	2	3	6	1.2	CO[C@]12CC(O)[C@@]3(C[C@@H]1[C@@H](C)O)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1016/j.bmcl.2007.06.050
	162676940	183434	None	0	Human	Functional	pEC50	=	7.9	7.9	-35	5	Agonist activity at human mu-opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition in presence of IBMX by Glo-sensor cAMP assayAgonist activity at human mu-opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition in presence of IBMX by Glo-sensor cAMP assay	ChEMBL	897	23	13	10	-1.0	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)C1=O	10.1021/acs.jmedchem.0c00643
	CHEMBL4797394	183434	None	0	Human	Functional	pEC50	=	7.9	7.9	-35	5	Agonist activity at human mu-opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition in presence of IBMX by Glo-sensor cAMP assayAgonist activity at human mu-opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition in presence of IBMX by Glo-sensor cAMP assay	ChEMBL	897	23	13	10	-1.0	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)C1=O	10.1021/acs.jmedchem.0c00643
	66553195	93198	None	26	Human	Functional	pEC50	=	7.9	7.9	-1	5	Agonist activity at mu opioid receptor (unknown origin) assessed as beta arrestin-2 recruitment incubated for 3 days by PathHunter assayAgonist activity at mu opioid receptor (unknown origin) assessed as beta arrestin-2 recruitment incubated for 3 days by PathHunter assay	ChEMBL	386	7	1	5	4.7	COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1	10.1016/j.ejmech.2021.113986
	66553195.0	93198	None	26	Human	Functional	pEC50	=	7.9	7.9	-1	5	Agonist activity at mu opioid receptor (unknown origin) assessed as beta arrestin-2 recruitment incubated for 3 days by PathHunter assayAgonist activity at mu opioid receptor (unknown origin) assessed as beta arrestin-2 recruitment incubated for 3 days by PathHunter assay	ChEMBL	386	7	1	5	4.7	COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1	10.1016/j.ejmech.2021.113986
	CHEMBL2443262	93198	None	26	Human	Functional	pEC50	=	7.9	7.9	-1	5	Agonist activity at mu opioid receptor (unknown origin) assessed as beta arrestin-2 recruitment incubated for 3 days by PathHunter assayAgonist activity at mu opioid receptor (unknown origin) assessed as beta arrestin-2 recruitment incubated for 3 days by PathHunter assay	ChEMBL	386	7	1	5	4.7	COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1	10.1016/j.ejmech.2021.113986
	DB14881	93198	None	26	Human	Functional	pEC50	=	7.9	7.9	-1	5	Agonist activity at mu opioid receptor (unknown origin) assessed as beta arrestin-2 recruitment incubated for 3 days by PathHunter assayAgonist activity at mu opioid receptor (unknown origin) assessed as beta arrestin-2 recruitment incubated for 3 days by PathHunter assay	ChEMBL	386	7	1	5	4.7	COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1	10.1016/j.ejmech.2021.113986
	60170688	81738	None	0	Human	Functional	pEC50	=	7.9	7.9	3	2	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL	656	12	6	6	3.0	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccc(Cl)cc1	10.1021/jm300664y
	CHEMBL2163911	81738	None	0	Human	Functional	pEC50	=	7.9	7.9	3	2	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL	656	12	6	6	3.0	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccc(Cl)cc1	10.1021/jm300664y
	CHEMBL2387329	212867	None	0	Rat	Functional	pEC50	=	7.9	7.9	-4	3	Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)NCCCCCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)C(=O)N[C@@H](Cc1c(F)c(F)c(F)c(F)c1F)C(N)=O	10.1016/j.bmcl.2013.03.065
	5487663	72864	None	12	Rat	Functional	pEC50	=	7.9	7.9	-6	4	Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	908	22	12	12	-1.6	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/ml500241n
	CHEMBL200199	72864	None	12	Rat	Functional	pEC50	=	7.9	7.9	-6	4	Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	908	22	12	12	-1.6	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/ml500241n
	25257195	189352	None	0	Rat	Functional	pEC50	=	7.9	7.9	-30	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	506	5	3	5	3.8	O=C(/C=C/c1ccccc1Cl)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/jm8015552
	CHEMBL511655	189352	None	0	Rat	Functional	pEC50	=	7.9	7.9	-30	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	506	5	3	5	3.8	O=C(/C=C/c1ccccc1Cl)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/jm8015552
	155527041	176679	None	0	Rat	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	573	7	3	5	6.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)c2ccccc2)c2ccc(Cc3cc4ccccc4o3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4459439	176679	None	0	Rat	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	573	7	3	5	6.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)c2ccccc2)c2ccc(Cc3cc4ccccc4o3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4597424	176679	None	0	Rat	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	573	7	3	5	6.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)c2ccccc2)c2ccc(Cc3cc4ccccc4o3)cc21	10.1021/acs.jmedchem.9b00378
	1627	2594	None	9	Mouse	Functional	pEC50	=	7.9	7.9	-7	9	Partial 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 assayPartial 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	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.3c00417
	1845	2594	None	9	Mouse	Functional	pEC50	=	7.9	7.9	-7	9	Partial 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 assayPartial 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	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.3c00417
	5288826	2594	None	9	Mouse	Functional	pEC50	=	7.9	7.9	-7	9	Partial 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 assayPartial 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	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.3c00417
	5288826.0	2594	None	9	Mouse	Functional	pEC50	=	7.9	7.9	-7	9	Partial 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 assayPartial 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	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.3c00417
	CHEMBL70	2594	None	9	Mouse	Functional	pEC50	=	7.9	7.9	-7	9	Partial 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 assayPartial 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	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.3c00417
	DB00295	2594	None	9	Mouse	Functional	pEC50	=	7.9	7.9	-7	9	Partial 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 assayPartial 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	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.3c00417
	1627	2594	None	9	Mouse	Functional	pEC50	=	7.9	7.9	-7	9	Partial 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 assayPartial 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	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.3c00417
	1845	2594	None	9	Mouse	Functional	pEC50	=	7.9	7.9	-7	9	Partial 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 assayPartial 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	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.3c00417
	5288826	2594	None	9	Mouse	Functional	pEC50	=	7.9	7.9	-7	9	Partial 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 assayPartial 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	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.3c00417
	5288826.0	2594	None	9	Mouse	Functional	pEC50	=	7.9	7.9	-7	9	Partial 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 assayPartial 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	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.3c00417
	CHEMBL70	2594	None	9	Mouse	Functional	pEC50	=	7.9	7.9	-7	9	Partial 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 assayPartial 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	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.3c00417
	DB00295	2594	None	9	Mouse	Functional	pEC50	=	7.9	7.9	-7	9	Partial 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 assayPartial 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	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.3c00417
	CHEMBL5085974	217493	None	0	Human	Functional	pEC50	=	7.9	7.9	11	2	Agonist activity at human mu opioid receptor expressed in HEK293T cells assessed as Galphai2 activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human mu opioid receptor expressed in HEK293T cells assessed as Galphai2 activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay	ChEMBL		None	None	None		CN(C)C(=O)C(CCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1	10.1021/acs.jmedchem.1c00611
	CHEMBL5087771	217607	None	0	Mouse	Functional	pEC50	=	7.9	7.9	-	1	Antagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method	ChEMBL		None	None	None		O=C(CCc1cn[nH]c1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.1c02185
	89978762	160238	None	0	Human	Functional	pEC50	=	7.9	7.9	-5	3	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	544	10	1	6	4.0	CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(OCC(N)=O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	nan
	CHEMBL4109061	160238	None	0	Human	Functional	pEC50	=	7.9	7.9	-5	3	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	544	10	1	6	4.0	CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(OCC(N)=O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	nan
	72713191	93205	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	350	6	1	3	4.6	c1ccc(CNCC[C@@]2(c3ccccn3)CCOC3(CCCC3)C2)cc1	10.1021/jm4010829
	CHEMBL2443269	93205	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	350	6	1	3	4.6	c1ccc(CNCC[C@@]2(c3ccccn3)CCOC3(CCCC3)C2)cc1	10.1021/jm4010829
	72712589	93215	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	356	6	1	4	4.7	c1ccc([C@]2(CCNCc3ccsc3)CCOC3(CCCC3)C2)nc1	10.1021/jm4010829
	CHEMBL2443279	93215	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	356	6	1	4	4.7	c1ccc([C@]2(CCNCc3ccsc3)CCOC3(CCCC3)C2)nc1	10.1021/jm4010829
	162669697	182826	None	0	Human	Functional	pEC50	=	7.9	7.9	-549	4	Agonist activity at human MOR stably expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by liquid scintillation counting assayAgonist activity at human MOR stably expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by liquid scintillation counting assay	ChEMBL	1394	36	20	16	-0.8	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O	10.1021/acs.jmedchem.0c01376
	CHEMBL4789659	182826	None	0	Human	Functional	pEC50	=	7.9	7.9	-549	4	Agonist activity at human MOR stably expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by liquid scintillation counting assayAgonist activity at human MOR stably expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by liquid scintillation counting assay	ChEMBL	1394	36	20	16	-0.8	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O	10.1021/acs.jmedchem.0c01376
	CHEMBL5084268	217395	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL		None	None	None		Fc1ccc([C@]2(CCNCc3cncc(Cl)c3)CCOC3(CCOC3)C2)cc1	10.1016/j.ejmech.2021.113986
	121614490	159898	None	0	Human	Functional	pEC50	=	6.9	6.9	47	2	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	294	3	2	2	2.9	Cc1ccc(C(=O)NCC2NCCc3ccccc32)cc1C	10.1016/j.ejmech.2016.09.003
	CHEMBL4105599	159898	None	0	Human	Functional	pEC50	=	6.9	6.9	47	2	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	294	3	2	2	2.9	Cc1ccc(C(=O)NCC2NCCc3ccccc32)cc1C	10.1016/j.ejmech.2016.09.003
	9838803	31121	None	10	Human	Functional	pEC50	=	6.9	6.9	2	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assayAgonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assay	ChEMBL	249	3	2	3	2.3	CN(C)C[C@H]1CCCC[C@]1(O)c1cccc(O)c1	10.1021/ml200268w
	CHEMBL1400	31121	None	10	Human	Functional	pEC50	=	6.9	6.9	2	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assayAgonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assay	ChEMBL	249	3	2	3	2.3	CN(C)C[C@H]1CCCC[C@]1(O)c1cccc(O)c1	10.1021/ml200268w
	CHEMBL201556	31121	None	10	Human	Functional	pEC50	=	6.9	6.9	2	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assayAgonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assay	ChEMBL	249	3	2	3	2.3	CN(C)C[C@H]1CCCC[C@]1(O)c1cccc(O)c1	10.1021/ml200268w
	7362	2114	None	29	Human	Functional	pEC50	=	6.9	6.9	-19	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	465	6	4	5	3.6	Oc1ccc2c(c1)CN[C@H](C2)C(=O)N[C@@H](C(C)C)CN1CC[C@@]([C@H](C1)C)(C)c1cccc(c1)O	10.1021/jm1004978
	9956146	2114	None	29	Human	Functional	pEC50	=	6.9	6.9	-19	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	465	6	4	5	3.6	Oc1ccc2c(c1)CN[C@H](C2)C(=O)N[C@@H](C(C)C)CN1CC[C@@]([C@H](C1)C)(C)c1cccc(c1)O	10.1021/jm1004978
	CHEMBL415247	2114	None	29	Human	Functional	pEC50	=	6.9	6.9	-19	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	465	6	4	5	3.6	Oc1ccc2c(c1)CN[C@H](C2)C(=O)N[C@@H](C(C)C)CN1CC[C@@]([C@H](C1)C)(C)c1cccc(c1)O	10.1021/jm1004978
	1642	2859	None	17	Human	Functional	pEC50	=	6.9	6.9	-85	7	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	661	4	5	8	3.8	Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2C[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)CC1CC1	10.1021/jm1004978
	5480230	2859	None	17	Human	Functional	pEC50	=	6.9	6.9	-85	7	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	661	4	5	8	3.8	Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2C[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)CC1CC1	10.1021/jm1004978
	CHEMBL573214	2859	None	17	Human	Functional	pEC50	=	6.9	6.9	-85	7	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	661	4	5	8	3.8	Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2C[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)CC1CC1	10.1021/jm1004978
	46867404	6580	None	0	Human	Functional	pEC50	=	6.9	6.9	-19	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	460	6	3	4	5.3	CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)c1ccc2cc(O)ccc2c1	10.1021/jm1004978
	CHEMBL1083061	6580	None	0	Human	Functional	pEC50	=	6.9	6.9	-19	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	460	6	3	4	5.3	CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)c1ccc2cc(O)ccc2c1	10.1021/jm1004978
	CHEMBL1204084	6580	None	0	Human	Functional	pEC50	=	6.9	6.9	-19	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	460	6	3	4	5.3	CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)c1ccc2cc(O)ccc2c1	10.1021/jm1004978
	11712760	6581	None	0	Human	Functional	pEC50	=	6.9	6.9	-19	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	482	6	3	5	4.7	CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@H]1Cc2ccc(O)cc2CS1	10.1021/jm1004978
	CHEMBL1083062	6581	None	0	Human	Functional	pEC50	=	6.9	6.9	-19	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	482	6	3	5	4.7	CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@H]1Cc2ccc(O)cc2CS1	10.1021/jm1004978
	11540292	6654	None	0	Human	Functional	pEC50	=	6.9	6.9	-19	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	482	6	3	5	4.7	CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@@H]1Cc2ccc(O)cc2CS1	10.1021/jm1004978
	CHEMBL1083371	6654	None	0	Human	Functional	pEC50	=	6.9	6.9	-19	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	482	6	3	5	4.7	CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@@H]1Cc2ccc(O)cc2CS1	10.1021/jm1004978
	CHEMBL1204085	6654	None	0	Human	Functional	pEC50	=	6.9	6.9	-19	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	482	6	3	5	4.7	CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@@H]1Cc2ccc(O)cc2CS1	10.1021/jm1004978
	11562377	6655	None	0	Human	Functional	pEC50	=	6.9	6.9	-19	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	498	6	3	5	3.7	CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@H]1Cc2ccc(O)cc2C[S+]1[O-]	10.1021/jm1004978
	CHEMBL1083372	6655	None	0	Human	Functional	pEC50	=	6.9	6.9	-19	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	498	6	3	5	3.7	CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@H]1Cc2ccc(O)cc2C[S+]1[O-]	10.1021/jm1004978
	11619680	6958	None	0	Human	Functional	pEC50	=	6.9	6.9	-19	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	466	6	3	5	4.0	CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@@H]1Cc2ccc(O)cc2CO1	10.1021/jm1004978
	CHEMBL1084529	6958	None	0	Human	Functional	pEC50	=	6.9	6.9	-19	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	466	6	3	5	4.0	CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@@H]1Cc2ccc(O)cc2CO1	10.1021/jm1004978
	11698381	7081	None	0	Human	Functional	pEC50	=	6.9	6.9	-19	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	464	6	3	4	4.6	CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@@H]1CCc2cc(O)ccc2C1	10.1021/jm1004978
	CHEMBL1085023	7081	None	0	Human	Functional	pEC50	=	6.9	6.9	-19	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	464	6	3	4	4.6	CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@@H]1CCc2cc(O)ccc2C1	10.1021/jm1004978
	11496383	7082	None	0	Human	Functional	pEC50	=	6.9	6.9	-19	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	464	6	3	4	4.6	CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@H]1CCc2cc(O)ccc2C1	10.1021/jm1004978
	CHEMBL1085024	7082	None	0	Human	Functional	pEC50	=	6.9	6.9	-19	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	464	6	3	4	4.6	CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@H]1CCc2cc(O)ccc2C1	10.1021/jm1004978
	11698420	7083	None	0	Human	Functional	pEC50	=	6.9	6.9	-19	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	466	6	3	5	4.0	CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@H]1Cc2ccc(O)cc2CO1	10.1021/jm1004978
	CHEMBL1085025	7083	None	0	Human	Functional	pEC50	=	6.9	6.9	-19	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	466	6	3	5	4.0	CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@H]1Cc2ccc(O)cc2CO1	10.1021/jm1004978
	CHEMBL2419540	212900	None	0	Rat	Functional	pEC50	=	6.9	6.9	-14	3	Agonist activity at rat MOR expressed in HN9.10 cell membranes by [35S]GTPgammaS binding assayAgonist activity at rat MOR expressed in HN9.10 cell membranes by [35S]GTPgammaS binding assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1016/j.bmcl.2013.06.065
	46227360	205039	None	0	Rat	Functional	pEC50	=	6.9	6.9	-25	5	Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	1210	18	10	12	4.6	CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1016/j.bmc.2009.08.035
	CHEMBL611924	205039	None	0	Rat	Functional	pEC50	=	6.9	6.9	-25	5	Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	1210	18	10	12	4.6	CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1016/j.bmc.2009.08.035
	1627	2594	None	9	Mouse	Functional	pEC50	=	6.9	6.9	-7	9	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmc.2015.02.055
	1845	2594	None	9	Mouse	Functional	pEC50	=	6.9	6.9	-7	9	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmc.2015.02.055
	5288826	2594	None	9	Mouse	Functional	pEC50	=	6.9	6.9	-7	9	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmc.2015.02.055
	5288826.0	2594	None	9	Mouse	Functional	pEC50	=	6.9	6.9	-7	9	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmc.2015.02.055
	CHEMBL70	2594	None	9	Mouse	Functional	pEC50	=	6.9	6.9	-7	9	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmc.2015.02.055
	DB00295	2594	None	9	Mouse	Functional	pEC50	=	6.9	6.9	-7	9	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmc.2015.02.055
	12986253	120616	None	0	Human	Functional	pEC50	=	4.9	4.9	3	2	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay	ChEMBL	379	7	2	2	4.3	CN(C)[C@]1(c2ccccc2)CC[C@@H](NC(=O)NCCCc2ccccc2)CC1	10.1021/ml500116x
	CHEMBL3325881	120616	None	0	Human	Functional	pEC50	=	4.9	4.9	3	2	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay	ChEMBL	379	7	2	2	4.3	CN(C)[C@]1(c2ccccc2)CC[C@@H](NC(=O)NCCCc2ccccc2)CC1	10.1021/ml500116x
	CHEMBL3545610	120616	None	0	Human	Functional	pEC50	=	4.9	4.9	3	2	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay	ChEMBL	379	7	2	2	4.3	CN(C)[C@]1(c2ccccc2)CC[C@@H](NC(=O)NCCCc2ccccc2)CC1	10.1021/ml500116x
	44337642	109766	None	0	Human	Functional	pEC50	=	5.9	5.9	-13	3	Effective concentration agonistic activity towards Opioid receptor mu 1Effective concentration agonistic activity towards Opioid receptor mu 1	ChEMBL	440	2	2	3	5.6	CC(C)=CC[C@@]12Cc3c([nH]c4ccccc34)[C@]3(C)Oc4c(O)ccc5c4[C@@]31CCN(C)C2C5	10.1021/jm030801n
	CHEMBL322875	109766	None	0	Human	Functional	pEC50	=	5.9	5.9	-13	3	Effective concentration agonistic activity towards Opioid receptor mu 1Effective concentration agonistic activity towards Opioid receptor mu 1	ChEMBL	440	2	2	3	5.6	CC(C)=CC[C@@]12Cc3c([nH]c4ccccc34)[C@]3(C)Oc4c(O)ccc5c4[C@@]31CCN(C)C2C5	10.1021/jm030801n
	44686	59641	None	10	Human	Functional	pEC50	=	4.9	4.9	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	337	7	0	3	3.7	CCC(=O)C(CCN1CCOCC1)(c1ccccc1)c1ccccc1	nan
	CHEMBL1720091	59641	None	10	Human	Functional	pEC50	=	4.9	4.9	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	337	7	0	3	3.7	CCC(=O)C(CCN1CCOCC1)(c1ccccc1)c1ccccc1	nan
	164851917	190307	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	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 assayAgonist 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	ChEMBL	382	8	0	2	4.7	CCCC(=O)N(Cc1ccc(F)cc1)C1CCN(CCc2ccccc2)CC1	10.1016/j.ejmech.2022.114649
	CHEMBL5174391	190307	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	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 assayAgonist 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	ChEMBL	382	8	0	2	4.7	CCCC(=O)N(Cc1ccc(F)cc1)C1CCN(CCc2ccccc2)CC1	10.1016/j.ejmech.2022.114649
	137637659	156331	None	0	Human	Functional	pEC50	=	4.9	4.9	-467735	2	Agonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assayAgonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assay	ChEMBL	503	5	3	7	2.4	CN(C(=O)/C=C/c1ccncc1)[C@@H]1CC[C@@]2(O)[C@H]3[C@@H](O)c4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2017.06.017
	CHEMBL4064781	156331	None	0	Human	Functional	pEC50	=	4.9	4.9	-467735	2	Agonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assayAgonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assay	ChEMBL	503	5	3	7	2.4	CN(C(=O)/C=C/c1ccncc1)[C@@H]1CC[C@@]2(O)[C@H]3[C@@H](O)c4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2017.06.017
	53324890	57322	None	0	Human	Functional	pEC50	=	5.9	5.9	-138	2	Agonist activity at human MOP receptor expressed in CHO-K1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human MOP receptor expressed in CHO-K1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting	ChEMBL	469	4	1	4	6.6	OCC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCCCC1	10.1016/j.bmc.2010.07.034
	CHEMBL1650842	57322	None	0	Human	Functional	pEC50	=	5.9	5.9	-138	2	Agonist activity at human MOP receptor expressed in CHO-K1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human MOP receptor expressed in CHO-K1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting	ChEMBL	469	4	1	4	6.6	OCC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCCCC1	10.1016/j.bmc.2010.07.034
	1627	2594	None	9	Rat	Functional	pEC50	=	6.9	6.9	1	9	Agonist activity at rat MOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation countingAgonist activity at rat MOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.9b00857
	1845	2594	None	9	Rat	Functional	pEC50	=	6.9	6.9	1	9	Agonist activity at rat MOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation countingAgonist activity at rat MOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.9b00857
	5288826	2594	None	9	Rat	Functional	pEC50	=	6.9	6.9	1	9	Agonist activity at rat MOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation countingAgonist activity at rat MOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.9b00857
	5288826.0	2594	None	9	Rat	Functional	pEC50	=	6.9	6.9	1	9	Agonist activity at rat MOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation countingAgonist activity at rat MOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.9b00857
	CHEMBL70	2594	None	9	Rat	Functional	pEC50	=	6.9	6.9	1	9	Agonist activity at rat MOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation countingAgonist activity at rat MOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.9b00857
	DB00295	2594	None	9	Rat	Functional	pEC50	=	6.9	6.9	1	9	Agonist activity at rat MOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation countingAgonist activity at rat MOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.9b00857
	1627	2594	None	9	Rat	Functional	pEC50	=	6.9	6.9	1	9	Agonist activity at rat mu opioid receptor assessed as stimulation of [35]SGTPgammaS bindingAgonist activity at rat mu opioid receptor assessed as stimulation of [35]SGTPgammaS binding	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmcl.2009.07.119
	1845	2594	None	9	Rat	Functional	pEC50	=	6.9	6.9	1	9	Agonist activity at rat mu opioid receptor assessed as stimulation of [35]SGTPgammaS bindingAgonist activity at rat mu opioid receptor assessed as stimulation of [35]SGTPgammaS binding	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmcl.2009.07.119
	5288826	2594	None	9	Rat	Functional	pEC50	=	6.9	6.9	1	9	Agonist activity at rat mu opioid receptor assessed as stimulation of [35]SGTPgammaS bindingAgonist activity at rat mu opioid receptor assessed as stimulation of [35]SGTPgammaS binding	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmcl.2009.07.119
	5288826.0	2594	None	9	Rat	Functional	pEC50	=	6.9	6.9	1	9	Agonist activity at rat mu opioid receptor assessed as stimulation of [35]SGTPgammaS bindingAgonist activity at rat mu opioid receptor assessed as stimulation of [35]SGTPgammaS binding	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmcl.2009.07.119
	CHEMBL70	2594	None	9	Rat	Functional	pEC50	=	6.9	6.9	1	9	Agonist activity at rat mu opioid receptor assessed as stimulation of [35]SGTPgammaS bindingAgonist activity at rat mu opioid receptor assessed as stimulation of [35]SGTPgammaS binding	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmcl.2009.07.119
	DB00295	2594	None	9	Rat	Functional	pEC50	=	6.9	6.9	1	9	Agonist activity at rat mu opioid receptor assessed as stimulation of [35]SGTPgammaS bindingAgonist activity at rat mu opioid receptor assessed as stimulation of [35]SGTPgammaS binding	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmcl.2009.07.119
	1627	2594	None	9	Rat	Functional	pEC50	=	6.9	6.9	1	9	Agonist activity at rat mu opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat mu opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.1c01082
	1845	2594	None	9	Rat	Functional	pEC50	=	6.9	6.9	1	9	Agonist activity at rat mu opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat mu opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.1c01082
	5288826	2594	None	9	Rat	Functional	pEC50	=	6.9	6.9	1	9	Agonist activity at rat mu opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat mu opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.1c01082
	5288826.0	2594	None	9	Rat	Functional	pEC50	=	6.9	6.9	1	9	Agonist activity at rat mu opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat mu opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.1c01082
	CHEMBL70	2594	None	9	Rat	Functional	pEC50	=	6.9	6.9	1	9	Agonist activity at rat mu opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat mu opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.1c01082
	DB00295	2594	None	9	Rat	Functional	pEC50	=	6.9	6.9	1	9	Agonist activity at rat mu opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat mu opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.1c01082
	136239310	91438	None	0	Rat	Functional	pEC50	=	5.9	5.9	1	2	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	764	9	10	9	-1.2	C/N=C1/NCCC[C@@H](C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCN1	10.1021/jm4008592
	CHEMBL2402933	91438	None	0	Rat	Functional	pEC50	=	5.9	5.9	1	2	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	764	9	10	9	-1.2	C/N=C1/NCCC[C@@H](C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCN1	10.1021/jm4008592
	71765061	91446	None	0	Rat	Functional	pEC50	=	5.9	5.9	2	2	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	609	8	9	10	-2.9	CCN/C1=N/C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CN1	10.1021/jm4008592
	CHEMBL2402940	91446	None	0	Rat	Functional	pEC50	=	5.9	5.9	2	2	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	609	8	9	10	-2.9	CCN/C1=N/C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CN1	10.1021/jm4008592
	94156776	162199	None	0	Human	Functional	pEC50	=	4.9	4.9	-	1	Agonist activity at MOR (unknown origin) expressed in HEK293T assessed as intracellular cAMP accumulation after 15 mins by luciferase based GloSensor assayAgonist activity at MOR (unknown origin) expressed in HEK293T assessed as intracellular cAMP accumulation after 15 mins by luciferase based GloSensor assay	ChEMBL	324	5	2	4	1.3	CN(C)[C@H](CNC(=O)C1CCN(C(N)=O)CC1)c1cccs1	10.1021/acs.jmedchem.8b00718
	CHEMBL4161204	162199	None	0	Human	Functional	pEC50	=	4.9	4.9	-	1	Agonist activity at MOR (unknown origin) expressed in HEK293T assessed as intracellular cAMP accumulation after 15 mins by luciferase based GloSensor assayAgonist activity at MOR (unknown origin) expressed in HEK293T assessed as intracellular cAMP accumulation after 15 mins by luciferase based GloSensor assay	ChEMBL	324	5	2	4	1.3	CN(C)[C@H](CNC(=O)C1CCN(C(N)=O)CC1)c1cccs1	10.1021/acs.jmedchem.8b00718
	136239310	91438	None	0	Rat	Functional	pEC50	=	5.9	5.9	1	2	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	764	9	10	9	-1.2	C/N=C1/NCCC[C@@H](C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCN1	10.1021/jm4008592
	CHEMBL2402933	91438	None	0	Rat	Functional	pEC50	=	5.9	5.9	1	2	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	764	9	10	9	-1.2	C/N=C1/NCCC[C@@H](C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCN1	10.1021/jm4008592
	71765061	91446	None	0	Rat	Functional	pEC50	=	5.9	5.9	2	2	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	609	8	9	10	-2.9	CCN/C1=N/C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CN1	10.1021/jm4008592
	CHEMBL2402940	91446	None	0	Rat	Functional	pEC50	=	5.9	5.9	2	2	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	609	8	9	10	-2.9	CCN/C1=N/C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CN1	10.1021/jm4008592
	145975633	163872	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	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 methodAgonist 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	ChEMBL	425	4	1	4	4.7	O=c1[nH]c2cc(OC(F)(F)F)ccc2n1C1CCN(Cc2ccccc2Cl)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4205780	163872	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	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 methodAgonist 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	ChEMBL	425	4	1	4	4.7	O=c1[nH]c2cc(OC(F)(F)F)ccc2n1C1CCN(Cc2ccccc2Cl)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL5082031	217271	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	Agonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assay	ChEMBL		None	None	None		CCC(=O)N(CC1(N2CCNCC2)CCOCC1)c1cccc(C(F)(F)F)n1	10.1021/acs.jmedchem.1c00417
	172452364	195983	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assay	ChEMBL	342	5	1	3	4.1	CN(C)C(CNC(=O)c1cc2ccccc2s1)c1ccccc1F	10.1016/j.ejmech.2022.114728
	CHEMBL5414604	195983	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assay	ChEMBL	342	5	1	3	4.1	CN(C)C(CNC(=O)c1cc2ccccc2s1)c1ccccc1F	10.1016/j.ejmech.2022.114728
	5113115	20637	None	4	Human	Functional	pEC50	=	4.9	4.9	5	2	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	314	5	2	3	3.4	Cc1ccccc1NC(S)=NCC(c1cccnc1)N(C)C	nan
	CHEMBL1308389	20637	None	4	Human	Functional	pEC50	=	4.9	4.9	5	2	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	314	5	2	3	3.4	Cc1ccccc1NC(S)=NCC(c1cccnc1)N(C)C	nan
	118562362	171290	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	380	5	1	4	2.5	O=C1C(CO)OC2(CCN(CCc3ccccc3)CC2)CN1c1ccccc1	10.1021/acs.jmedchem.9b01256
	CHEMBL4459117	171290	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	380	5	1	4	2.5	O=C1C(CO)OC2(CCN(CCc3ccccc3)CC2)CN1c1ccccc1	10.1021/acs.jmedchem.9b01256
	23635163	88539	None	0	Rat	Functional	pEC50	=	6.9	6.9	2	3	Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay	ChEMBL	642	15	6	7	1.4	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NC1CCN(CCc2ccccc2)CC1	10.1021/jm061465o
	CHEMBL235106	88539	None	0	Rat	Functional	pEC50	=	6.9	6.9	2	3	Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay	ChEMBL	642	15	6	7	1.4	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NC1CCN(CCc2ccccc2)CC1	10.1021/jm061465o
	162643968	181889	None	0	Human	Functional	pEC50	=	6.9	6.9	-3	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1115	32	14	14	-2.5	CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.6b01181
	CHEMBL4777803	181889	None	0	Human	Functional	pEC50	=	6.9	6.9	-3	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1115	32	14	14	-2.5	CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.6b01181
	23635163	88539	None	0	Rat	Functional	pEC50	=	6.9	6.9	2	3	Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay	ChEMBL	642	15	6	7	1.4	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NC1CCN(CCc2ccccc2)CC1	10.1021/jm061465o
	CHEMBL235106	88539	None	0	Rat	Functional	pEC50	=	6.9	6.9	2	3	Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay	ChEMBL	642	15	6	7	1.4	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NC1CCN(CCc2ccccc2)CC1	10.1021/jm061465o
	53327534	160240	None	0	Human	Functional	pEC50	=	4.9	4.9	-	1	HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.	ChEMBL	595	20	1	11	1.6	COCCOCCOCCOCCOCCOCCO[C@H]1CC[C@@]2(O)C3Cc4ccc(OC)c5c4[C@@]2(CCN3C)[C@H]1O5	nan
	CHEMBL4109078	160240	None	0	Human	Functional	pEC50	=	4.9	4.9	-	1	HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.	ChEMBL	595	20	1	11	1.6	COCCOCCOCCOCCOCCOCCO[C@H]1CC[C@@]2(O)C3Cc4ccc(OC)c5c4[C@@]2(CCN3C)[C@H]1O5	nan
	68314366	93211	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	351	6	1	4	4.0	c1ccc([C@]2(CCNCc3ccncc3)CCOC3(CCCC3)C2)nc1	10.1021/jm4010829
	CHEMBL2443275	93211	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	351	6	1	4	4.0	c1ccc([C@]2(CCNCc3ccncc3)CCOC3(CCCC3)C2)nc1	10.1021/jm4010829
	162643968	181889	None	0	Human	Functional	pEC50	=	6.9	6.9	-3	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1115	32	14	14	-2.5	CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.6b01181
	CHEMBL4777803	181889	None	0	Human	Functional	pEC50	=	6.9	6.9	-3	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1115	32	14	14	-2.5	CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.6b01181
	172468454	196932	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assay	ChEMBL	358	5	1	3	4.6	CN(C)C(CNC(=O)c1cc2ccccc2s1)c1ccc(Cl)cc1	10.1016/j.ejmech.2022.114728
	CHEMBL5435116	196932	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assay	ChEMBL	358	5	1	3	4.6	CN(C)C(CNC(=O)c1cc2ccccc2s1)c1ccc(Cl)cc1	10.1016/j.ejmech.2022.114728
	130431390	163779	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	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 methodAgonist 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	ChEMBL	437	3	1	3	4.7	O=c1[nH]c2ccc(Cl)cc2n1C1CCN(Cc2ccc(Br)cc2F)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4204767	163779	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	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 methodAgonist 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	ChEMBL	437	3	1	3	4.7	O=c1[nH]c2ccc(Cl)cc2n1C1CCN(Cc2ccc(Br)cc2F)CC1	10.1021/acs.jmedchem.8b01136
	66828846	160639	None	0	Human	Functional	pEC50	=	6.9	6.9	-6	3	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	520	8	0	7	4.7	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1c(C)noc1C)C2	nan
	CHEMBL4112472	160639	None	0	Human	Functional	pEC50	=	6.9	6.9	-6	3	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	520	8	0	7	4.7	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1c(C)noc1C)C2	nan
	1613	2297	None	29	Human	Functional	pEC50	=	5.9	5.9	-51	7	Agonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay	ChEMBL		None	None	None		None	10.1039/D1MD00025J
	3903	2297	None	29	Human	Functional	pEC50	=	5.9	5.9	-51	7	Agonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay	ChEMBL		None	None	None		None	10.1039/D1MD00025J
	461776	2297	None	29	Human	Functional	pEC50	=	5.9	5.9	-51	7	Agonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay	ChEMBL		None	None	None		None	10.1039/D1MD00025J
	CHEMBL15038	2297	None	29	Human	Functional	pEC50	=	5.9	5.9	-51	7	Agonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay	ChEMBL		None	None	None		None	10.1039/D1MD00025J
	CHEMBL8234	2297	None	29	Human	Functional	pEC50	=	5.9	5.9	-51	7	Agonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay	ChEMBL		None	None	None		None	10.1039/D1MD00025J
	156017673	177989	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting methodAgonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method	ChEMBL	633	17	8	8	0.4	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1	10.1016/j.bmc.2020.115438
	CHEMBL4644694	177989	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting methodAgonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method	ChEMBL	633	17	8	8	0.4	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1	10.1016/j.bmc.2020.115438
	124037293	159932	None	0	Human	Functional	pEC50	=	6.9	6.9	23	2	HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.	ChEMBL	493	13	2	9	1.3	COCCOCCOCCOCCO[C@H]1CC[C@@]2(O)C3Cc4ccc(O)c5c4[C@@]2(CCN3C)[C@H]1O5	nan
	CHEMBL4106506	159932	None	0	Human	Functional	pEC50	=	6.9	6.9	23	2	HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.	ChEMBL	493	13	2	9	1.3	COCCOCCOCCOCCO[C@H]1CC[C@@]2(O)C3Cc4ccc(O)c5c4[C@@]2(CCN3C)[C@H]1O5	nan
	1613	2297	None	29	Human	Functional	pEC50	=	5.9	5.9	-51	7	Agonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay	ChEMBL		None	None	None		None	10.1039/D1MD00025J
	3903	2297	None	29	Human	Functional	pEC50	=	5.9	5.9	-51	7	Agonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay	ChEMBL		None	None	None		None	10.1039/D1MD00025J
	461776	2297	None	29	Human	Functional	pEC50	=	5.9	5.9	-51	7	Agonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay	ChEMBL		None	None	None		None	10.1039/D1MD00025J
	CHEMBL15038	2297	None	29	Human	Functional	pEC50	=	5.9	5.9	-51	7	Agonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay	ChEMBL		None	None	None		None	10.1039/D1MD00025J
	CHEMBL8234	2297	None	29	Human	Functional	pEC50	=	5.9	5.9	-51	7	Agonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay	ChEMBL		None	None	None		None	10.1039/D1MD00025J
	73350483	90497	None	0	Human	Functional	pEC50	=	6.9	6.9	-2	2	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis	ChEMBL	386	2	0	2	5.0	O=C1Cc2ccccc2N1C1CCN(C2CC[C@H]3CCCc4cccc2c43)CC1	10.1016/j.bmcl.2013.03.101
	CHEMBL2387193	90497	None	0	Human	Functional	pEC50	=	6.9	6.9	-2	2	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis	ChEMBL	386	2	0	2	5.0	O=C1Cc2ccccc2N1C1CCN(C2CC[C@H]3CCCc4cccc2c43)CC1	10.1016/j.bmcl.2013.03.101
	137639500	157009	None	0	Human	Functional	pEC50	=	4.9	4.9	-1698	2	Agonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assayAgonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assay	ChEMBL	518	7	3	6	3.3	CN(C(=O)CCCc1ccccc1)[C@@H]1CC[C@@]2(O)[C@H]3[C@@H](O)c4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2017.06.017
	CHEMBL4072327	157009	None	0	Human	Functional	pEC50	=	4.9	4.9	-1698	2	Agonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assayAgonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assay	ChEMBL	518	7	3	6	3.3	CN(C(=O)CCCc1ccccc1)[C@@H]1CC[C@@]2(O)[C@H]3[C@@H](O)c4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2017.06.017
	89978678	159931	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	602	11	2	7	4.0	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccc(C(=O)NCC(=O)O)cc1)C2	nan
	CHEMBL4106505	159931	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	602	11	2	7	4.0	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccc(C(=O)NCC(=O)O)cc1)C2	nan
	16188374	52194	None	5	Human	Functional	pEC50	=	4.9	4.9	3	2	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	403	6	1	5	4.9	Cc1ccc(-n2cc(CNC(C)c3cnn(C)c3C)c(-c3ccc(F)cc3)n2)cc1	nan
	CHEMBL1588202	52194	None	5	Human	Functional	pEC50	=	4.9	4.9	3	2	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	403	6	1	5	4.9	Cc1ccc(-n2cc(CNC(C)c3cnn(C)c3C)c(-c3ccc(F)cc3)n2)cc1	nan
	118562440	173744	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	382	4	0	3	3.7	CC1OC2(CCN(CCc3cccc(F)c3)CC2)CN(c2ccccc2)C1=O	10.1021/acs.jmedchem.9b01256
	CHEMBL4534193	173744	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	382	4	0	3	3.7	CC1OC2(CCN(CCc3cccc(F)c3)CC2)CN(c2ccccc2)C1=O	10.1021/acs.jmedchem.9b01256
	145963850	164279	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	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 methodAgonist 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	ChEMBL	351	4	1	4	3.7	COc1ccc(C(C)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)cc1	10.1021/acs.jmedchem.8b01136
	CHEMBL4210647	164279	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	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 methodAgonist 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	ChEMBL	351	4	1	4	3.7	COc1ccc(C(C)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)cc1	10.1021/acs.jmedchem.8b01136
	156010407	177242	None	0	Human	Functional	pEC50	=	7.9	7.9	-5	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	600	9	1	6	6.8	COc1cccc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)c1	10.1021/acs.jmedchem.0c00503
	CHEMBL4633907	177242	None	0	Human	Functional	pEC50	=	7.9	7.9	-5	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	600	9	1	6	6.8	COc1cccc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)c1	10.1021/acs.jmedchem.0c00503
	44597831	199266	None	0	Human	Functional	pEC50	=	7.9	7.9	-2	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	523	12	1	4	7.1	CC(CCCCCCC(C)C(=O)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3)C(=O)O	10.1021/jm900379p
	CHEMBL565679	199266	None	0	Human	Functional	pEC50	=	7.9	7.9	-2	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	523	12	1	4	7.1	CC(CCCCCCC(C)C(=O)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3)C(=O)O	10.1021/jm900379p
	121596705	3246	None	34	Human	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assayAgonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assay	ChEMBL	361	8	3	4	2.9	C[C@@H](Cc1cscc1)NC(=O)NC[C@@H](N(C)C)Cc1ccc(cc1)O	10.1016/j.bmcl.2023.129405
	9286	3246	None	34	Human	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assayAgonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assay	ChEMBL	361	8	3	4	2.9	C[C@@H](Cc1cscc1)NC(=O)NC[C@@H](N(C)C)Cc1ccc(cc1)O	10.1016/j.bmcl.2023.129405
	CHEMBL4467777	3246	None	34	Human	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assayAgonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assay	ChEMBL	361	8	3	4	2.9	C[C@@H](Cc1cscc1)NC(=O)NC[C@@H](N(C)C)Cc1ccc(cc1)O	10.1016/j.bmcl.2023.129405
	DB14030	3246	None	34	Human	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assayAgonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assay	ChEMBL	361	8	3	4	2.9	C[C@@H](Cc1cscc1)NC(=O)NC[C@@H](N(C)C)Cc1ccc(cc1)O	10.1016/j.bmcl.2023.129405
	127050833	141056	None	0	Rat	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay	ChEMBL	535	7	3	4	5.6	CCC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccc4ccccc4c3)ccc21	10.1021/acs.jmedchem.6b00308
	CHEMBL3823186	141056	None	0	Rat	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay	ChEMBL	535	7	3	4	5.6	CCC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccc4ccccc4c3)ccc21	10.1021/acs.jmedchem.6b00308
	CHEMBL235743	212033	None	1	Rat	Functional	pEC50	=	7.9	7.9	7	4	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL		None	None	None		C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/jm100982d
	155569441	176364	None	0	Rat	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	529	6	3	6	3.9	CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccc4c(c3)OCCO4)ccc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4593995	176364	None	0	Rat	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	529	6	3	6	3.9	CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccc4c(c3)OCCO4)ccc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4594956	176364	None	0	Rat	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	529	6	3	6	3.9	CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccc4c(c3)OCCO4)ccc21	10.1021/acs.jmedchem.9b00378
	CHEMBL235743	212033	None	1	Rat	Functional	pEC50	=	7.9	7.9	7	4	Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay	ChEMBL		None	None	None		C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/jm061465o
	117862196	160283	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	285	2	1	2	3.7	CC1C2Cc3ccc(O)cc3[C@]1(C)CCN2CC1(C)CC1	nan
	CHEMBL4109400	160283	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	285	2	1	2	3.7	CC1C2Cc3ccc(O)cc3[C@]1(C)CCN2CC1(C)CC1	nan
	3668	1561	None	36	Human	Functional	pEC50	=	7.9	7.9	1	5	Agonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysisAgonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis	ChEMBL		None	None	None		None	10.1016/j.ejmech.2015.12.012
	5311081	1561	None	36	Human	Functional	pEC50	=	7.9	7.9	1	5	Agonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysisAgonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis	ChEMBL		None	None	None		None	10.1016/j.ejmech.2015.12.012
	CHEMBL333357	1561	None	36	Human	Functional	pEC50	=	7.9	7.9	1	5	Agonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysisAgonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis	ChEMBL		None	None	None		None	10.1016/j.ejmech.2015.12.012
	CHEMBL589982	1561	None	36	Human	Functional	pEC50	=	7.9	7.9	1	5	Agonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysisAgonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis	ChEMBL		None	None	None		None	10.1016/j.ejmech.2015.12.012
	162660385	181310	None	0	Human	Functional	pEC50	=	7.9	7.9	-5	4	Agonist activity at human MOR stably expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by liquid scintillation counting assayAgonist activity at human MOR stably expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by liquid scintillation counting assay	ChEMBL	1358	40	14	15	3.0	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C	10.1021/acs.jmedchem.0c01376
	CHEMBL4761165	181310	None	0	Human	Functional	pEC50	=	7.9	7.9	-5	4	Agonist activity at human MOR stably expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by liquid scintillation counting assayAgonist activity at human MOR stably expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by liquid scintillation counting assay	ChEMBL	1358	40	14	15	3.0	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C	10.1021/acs.jmedchem.0c01376
	146408968	175890	None	0	Mouse	Functional	pEC50	=	7.9	7.9	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	505	5	3	8	1.9	COC(=O)c1cnccc1C(=O)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.8b01158
	CHEMBL4584097	175890	None	0	Mouse	Functional	pEC50	=	7.9	7.9	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	505	5	3	8	1.9	COC(=O)c1cnccc1C(=O)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.8b01158
	164626711	188704	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2cnccc12	10.1016/j.bmcl.2021.127953
	CHEMBL4879114	188704	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2cnccc12	10.1016/j.bmcl.2021.127953
	CHEMBL5028952	188704	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2cnccc12	10.1016/j.bmcl.2021.127953
	CHEMBL5076581	216939	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISAAgonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISA	ChEMBL		None	None	None		Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H]1CSSC[C@@H](C(=O)NCC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](CCCNC(=N)N)C(=O)O)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.1c01631
	1647	1313	None	34	Human	Functional	pEC50	=	7.9	7.9	-3	9	Stimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cellsStimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells	ChEMBL		None	None	None		None	10.1021/jm021073r
	5462471	1313	None	34	Human	Functional	pEC50	=	7.9	7.9	-3	9	Stimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cellsStimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells	ChEMBL		None	None	None		None	10.1021/jm021073r
	CHEMBL113995	1313	None	34	Human	Functional	pEC50	=	7.9	7.9	-3	9	Stimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cellsStimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells	ChEMBL		None	None	None		None	10.1021/jm021073r
	CHEMBL38874	1313	None	34	Human	Functional	pEC50	=	7.9	7.9	-3	9	Stimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cellsStimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells	ChEMBL		None	None	None		None	10.1021/jm021073r
	3668	1561	None	36	Human	Functional	pEC50	=	7.9	7.9	1	5	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.5b00056
	5311081	1561	None	36	Human	Functional	pEC50	=	7.9	7.9	1	5	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.5b00056
	CHEMBL333357	1561	None	36	Human	Functional	pEC50	=	7.9	7.9	1	5	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.5b00056
	CHEMBL589982	1561	None	36	Human	Functional	pEC50	=	7.9	7.9	1	5	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.5b00056
	44421412	84722	None	0	Human	Functional	pEC50	=	6.9	6.9	-10	3	Activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	474	2	2	5	4.6	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2c(c4c(n2CC2CCCCC2)CCCC4)C[C@@]3(O)C1C5	10.1021/jm040817t
	CHEMBL222579	84722	None	0	Human	Functional	pEC50	=	6.9	6.9	-10	3	Activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	474	2	2	5	4.6	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2c(c4c(n2CC2CCCCC2)CCCC4)C[C@@]3(O)C1C5	10.1021/jm040817t
	156013796	177382	None	0	Human	Functional	pEC50	=	6.9	6.9	-39	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	606	8	1	5	7.1	Oc1ccc2c3c1O[C@H]1c4ncc(-c5ccc(F)cc5F)cc4C[C@@]4(OCCCc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/acs.jmedchem.0c00503
	CHEMBL4636305	177382	None	0	Human	Functional	pEC50	=	6.9	6.9	-39	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	606	8	1	5	7.1	Oc1ccc2c3c1O[C@H]1c4ncc(-c5ccc(F)cc5F)cc4C[C@@]4(OCCCc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/acs.jmedchem.0c00503
	51356293	61227	None	0	Human	Functional	pEC50	=	6.9	6.9	-4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting	ChEMBL	359	3	1	4	4.3	Nc1nc2cc3c(cc2s1)C[C@@H]1[C@@H]2CCCC[C@]32CCN1CCCF	10.1021/jm101542c
	CHEMBL1766022	61227	None	0	Human	Functional	pEC50	=	6.9	6.9	-4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting	ChEMBL	359	3	1	4	4.3	Nc1nc2cc3c(cc2s1)C[C@@H]1[C@@H]2CCCC[C@]32CCN1CCCF	10.1021/jm101542c
	72713094	106411	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	418	8	2	3	5.1	C[C@@H]1CN(CCCc2ccccc2)[C@H]2C[C@H](NCC3CC3)C[C@]1(c1cccc(O)c1)C2	10.1021/jm401250s
	CHEMBL3139211	106411	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	418	8	2	3	5.1	C[C@@H]1CN(CCCc2ccccc2)[C@H]2C[C@H](NCC3CC3)C[C@]1(c1cccc(O)c1)C2	10.1021/jm401250s
	CHEMBL3217273	106411	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	418	8	2	3	5.1	C[C@@H]1CN(CCCc2ccccc2)[C@H]2C[C@H](NCC3CC3)C[C@]1(c1cccc(O)c1)C2	10.1021/jm401250s
	54582934	62099	None	0	Human	Functional	pEC50	=	6.9	6.9	-23	2	Agonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	872	15	2	8	11.5	O=C(CCCCCCCCC(=O)Nc1nc2cc3c(cc2s1)C[C@@H]1[C@@H]2CCCC[C@]32CCN1CC1CC1)Nc1nc2cc3c(cc2s1)C[C@@H]1[C@@H]2CCCC[C@]32CCN1CC1CC1	10.1016/j.bmc.2011.03.052
	CHEMBL1774951	62099	None	0	Human	Functional	pEC50	=	6.9	6.9	-23	2	Agonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	872	15	2	8	11.5	O=C(CCCCCCCCC(=O)Nc1nc2cc3c(cc2s1)C[C@@H]1[C@@H]2CCCC[C@]32CCN1CC1CC1)Nc1nc2cc3c(cc2s1)C[C@@H]1[C@@H]2CCCC[C@]32CCN1CC1CC1	10.1016/j.bmc.2011.03.052
	49863732	15337	None	0	Rat	Functional	pEC50	=	6.9	6.9	-1000	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding	ChEMBL	1266	18	10	12	6.1	CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(C)(C)SSC1(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1021/jm100157m
	CHEMBL1214025	15337	None	0	Rat	Functional	pEC50	=	6.9	6.9	-1000	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding	ChEMBL	1266	18	10	12	6.1	CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(C)(C)SSC1(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1021/jm100157m
	145984332	165968	None	0	Rat	Functional	pEC50	=	6.9	6.9	-131	3	Agonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis	ChEMBL	483	6	0	5	4.6	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42C=C[C@@]1(OC)[C@@H](C(=O)c1ccccc1)C2	10.1016/j.bmc.2018.07.020
	CHEMBL4249256	165968	None	0	Rat	Functional	pEC50	=	6.9	6.9	-131	3	Agonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis	ChEMBL	483	6	0	5	4.6	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42C=C[C@@]1(OC)[C@@H](C(=O)c1ccccc1)C2	10.1016/j.bmc.2018.07.020
	172464006	196593	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	367	7	0	4	3.3	COCC(=O)N(CC(C)N1CCC(c2ccccc2)CC1)c1ccccn1	10.1021/acs.jmedchem.3c01637
	CHEMBL5427406	196593	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	367	7	0	4	3.3	COCC(=O)N(CC(C)N1CCC(c2ccccc2)CC1)c1ccccn1	10.1021/acs.jmedchem.3c01637
	5523	3851	None	17	Human	Functional	pEC50	=	5.9	5.9	-2	3	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assayAgonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assay	ChEMBL	263	4	1	3	2.6	COc1cccc(c1)C1(O)CCCCC1CN(C)C	10.1021/ml200268w
	5523.0	3851	None	17	Human	Functional	pEC50	=	5.9	5.9	-2	3	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assayAgonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assay	ChEMBL	263	4	1	3	2.6	COc1cccc(c1)C1(O)CCCCC1CN(C)C	10.1021/ml200268w
	8286	3851	None	17	Human	Functional	pEC50	=	5.9	5.9	-2	3	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assayAgonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assay	ChEMBL	263	4	1	3	2.6	COc1cccc(c1)C1(O)CCCCC1CN(C)C	10.1021/ml200268w
	CHEMBL1237044	3851	None	17	Human	Functional	pEC50	=	5.9	5.9	-2	3	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assayAgonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assay	ChEMBL	263	4	1	3	2.6	COc1cccc(c1)C1(O)CCCCC1CN(C)C	10.1021/ml200268w
	DB00193	3851	None	17	Human	Functional	pEC50	=	5.9	5.9	-2	3	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assayAgonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assay	ChEMBL	263	4	1	3	2.6	COc1cccc(c1)C1(O)CCCCC1CN(C)C	10.1021/ml200268w
	162650094	180232	None	0	Human	Functional	pEC50	=	6.9	6.9	1	2	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL	405	6	1	4	4.5	COC(=O)/C=C/[C@H]1[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1	10.1039/d0md00104j
	CHEMBL4748689	180232	None	0	Human	Functional	pEC50	=	6.9	6.9	1	2	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL	405	6	1	4	4.5	COC(=O)/C=C/[C@H]1[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1	10.1039/d0md00104j
	CHEMBL5092587	217867	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	Agonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assay	ChEMBL		None	None	None		CCC(=O)N(CC1(N2CCN(CCOc3ccccc3)CC2)CCOCC1)c1cccc(C(F)(F)F)n1	10.1021/acs.jmedchem.1c00417
	126619377	176033	None	0	Human	Functional	pEC50	=	4.9	4.9	-	1	Agonist activity at human mu opioid receptor expressed in CHOK1 cells coexpressing Galpha15 assessed as increase in intracellular calcium flux in presence of mu opioid receptor antagonist naloxone and incubated for 1 hr measured for 90 secs at 1.5 sec interval by FLIPR assayAgonist activity at human mu opioid receptor expressed in CHOK1 cells coexpressing Galpha15 assessed as increase in intracellular calcium flux in presence of mu opioid receptor antagonist naloxone and incubated for 1 hr measured for 90 secs at 1.5 sec interval by FLIPR assay	ChEMBL	299	4	1	5	4.7	CCc1ccccc1Nc1ncc(-c2sc(C)nc2C)o1	10.1016/j.ejmech.2019.01.063
	CHEMBL4587559	176033	None	0	Human	Functional	pEC50	=	4.9	4.9	-	1	Agonist activity at human mu opioid receptor expressed in CHOK1 cells coexpressing Galpha15 assessed as increase in intracellular calcium flux in presence of mu opioid receptor antagonist naloxone and incubated for 1 hr measured for 90 secs at 1.5 sec interval by FLIPR assayAgonist activity at human mu opioid receptor expressed in CHOK1 cells coexpressing Galpha15 assessed as increase in intracellular calcium flux in presence of mu opioid receptor antagonist naloxone and incubated for 1 hr measured for 90 secs at 1.5 sec interval by FLIPR assay	ChEMBL	299	4	1	5	4.7	CCc1ccccc1Nc1ncc(-c2sc(C)nc2C)o1	10.1016/j.ejmech.2019.01.063
	172451116	195895	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	389	6	0	4	4.6	CC(CN(C(=O)c1ccco1)c1ccccn1)N1CCC(c2ccccc2)CC1	10.1021/acs.jmedchem.3c01637
	CHEMBL5412869	195895	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	389	6	0	4	4.6	CC(CN(C(=O)c1ccco1)c1ccccn1)N1CCC(c2ccccc2)CC1	10.1021/acs.jmedchem.3c01637
	49863732	15337	None	0	Rat	Functional	pEC50	=	6.9	6.9	-1000	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding	ChEMBL	1266	18	10	12	6.1	CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(C)(C)SSC1(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1021/jm100157m
	CHEMBL1214025	15337	None	0	Rat	Functional	pEC50	=	6.9	6.9	-1000	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding	ChEMBL	1266	18	10	12	6.1	CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(C)(C)SSC1(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1021/jm100157m
	49863734	15339	None	0	Rat	Functional	pEC50	=	6.9	6.9	-79	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding	ChEMBL	1477	21	11	14	6.8	CCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(C)(C)SSC(C)(C)[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm100157m
	CHEMBL1214027	15339	None	0	Rat	Functional	pEC50	=	6.9	6.9	-79	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding	ChEMBL	1477	21	11	14	6.8	CCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(C)(C)SSC(C)(C)[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm100157m
	145974614	164647	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	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 methodAgonist 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	ChEMBL	341	3	1	3	3.8	O=c1[nH]c2ccccc2n1C1CCN(Cc2cccc(Cl)c2)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4215165	164647	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	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 methodAgonist 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	ChEMBL	341	3	1	3	3.8	O=c1[nH]c2ccccc2n1C1CCN(Cc2cccc(Cl)c2)CC1	10.1021/acs.jmedchem.8b01136
	89978526	160267	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	721	23	0	10	5.2	COCCOCCOCCOCCOCCO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(OC)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	nan
	CHEMBL4109267	160267	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	721	23	0	10	5.2	COCCOCCOCCOCCOCCO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(OC)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	nan
	66826731	160306	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	633	17	0	8	5.2	COCCOCCOCCO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(OC)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	nan
	CHEMBL4109653	160306	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	633	17	0	8	5.2	COCCOCCOCCO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(OC)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	nan
	156014487	177318	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting methodAgonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method	ChEMBL	604	15	7	8	0.1	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CNC(C)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1	10.1016/j.bmc.2020.115438
	CHEMBL4635430	177318	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting methodAgonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method	ChEMBL	604	15	7	8	0.1	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CNC(C)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1	10.1016/j.bmc.2020.115438
	44367028	121071	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	The partial agonist activity tested in [35S]-GTP-gamma S Recombinant Human Opioid receptor mu 1 transfected in to CHO cells for the displacement of [3H]-DAMGO (mu)The partial agonist activity tested in [35S]-GTP-gamma S Recombinant Human Opioid receptor mu 1 transfected in to CHO cells for the displacement of [3H]-DAMGO (mu)	ChEMBL	544	5	2	5	5.9	Cc1ccc(-c2cn(Cc3ccccc3)c3c2C[C@@]2(O)C4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)cc1	10.1021/jm010841w
	CHEMBL356473	121071	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	The partial agonist activity tested in [35S]-GTP-gamma S Recombinant Human Opioid receptor mu 1 transfected in to CHO cells for the displacement of [3H]-DAMGO (mu)The partial agonist activity tested in [35S]-GTP-gamma S Recombinant Human Opioid receptor mu 1 transfected in to CHO cells for the displacement of [3H]-DAMGO (mu)	ChEMBL	544	5	2	5	5.9	Cc1ccc(-c2cn(Cc3ccccc3)c3c2C[C@@]2(O)C4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)cc1	10.1021/jm010841w
	16585103	113932	None	7	Human	Functional	pEC50	=	4.9	4.9	-	1	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	288	1	0	3	4.0	Cc1nn(-c2ccc(Cl)cc2)c2c1C(=O)CC(C)(C)C2	10.1016/j.bmc.2014.07.012
	CHEMBL3325699	113932	None	7	Human	Functional	pEC50	=	4.9	4.9	-	1	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	288	1	0	3	4.0	Cc1nn(-c2ccc(Cl)cc2)c2c1C(=O)CC(C)(C)C2	10.1016/j.bmc.2014.07.012
	118711136	113951	None	0	Human	Functional	pEC50	=	4.9	4.9	-	1	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	294	1	0	3	4.0	Cc1nn(-c2ccc(Cl)cc2Cl)c2c1C(=O)CCC2	10.1016/j.bmc.2014.07.012
	CHEMBL3325717	113951	None	0	Human	Functional	pEC50	=	4.9	4.9	-	1	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	294	1	0	3	4.0	Cc1nn(-c2ccc(Cl)cc2Cl)c2c1C(=O)CCC2	10.1016/j.bmc.2014.07.012
	66829015	160829	None	0	Human	Functional	pEC50	=	5.9	5.9	1	2	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	529	8	1	8	3.4	COc1ccc2c3c1O[C@@H]1[C@]34CCN(Cc3nn[nH]n3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2	nan
	CHEMBL4113890	160829	None	0	Human	Functional	pEC50	=	5.9	5.9	1	2	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	529	8	1	8	3.4	COc1ccc2c3c1O[C@@H]1[C@]34CCN(Cc3nn[nH]n3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2	nan
	24854177	96884	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	539	5	0	10	4.2	COC(=O)[C@@H]1C[C@H](OC(=O)c2ccc([N+](=O)[O-])cc2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@]21C	10.1021/jm701162g
	CHEMBL265195	96884	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	539	5	0	10	4.2	COC(=O)[C@@H]1C[C@H](OC(=O)c2ccc([N+](=O)[O-])cc2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@]21C	10.1021/jm701162g
	168679651	195904	None	2	Mouse	Functional	pEC50	=	5.9	5.9	-1	2	Partial 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 assayPartial 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	ChEMBL	428	9	1	3	4.6	COc1ccccc1[C@@H]1C[C@H]1NCCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	10.1021/acs.jmedchem.3c00417
	CHEMBL5412995	195904	None	2	Mouse	Functional	pEC50	=	5.9	5.9	-1	2	Partial 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 assayPartial 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	ChEMBL	428	9	1	3	4.6	COc1ccccc1[C@@H]1C[C@H]1NCCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	10.1021/acs.jmedchem.3c00417
	126619400	172173	None	0	Human	Functional	pEC50	=	4.9	4.9	-	1	Agonist activity at human mu opioid receptor expressed in CHOK1 cells coexpressing Galpha15 assessed as increase in intracellular calcium flux in presence of mu opioid receptor antagonist naloxone and incubated for 1 hr measured for 90 secs at 1.5 sec interval by FLIPR assayAgonist activity at human mu opioid receptor expressed in CHOK1 cells coexpressing Galpha15 assessed as increase in intracellular calcium flux in presence of mu opioid receptor antagonist naloxone and incubated for 1 hr measured for 90 secs at 1.5 sec interval by FLIPR assay	ChEMBL	433	3	1	5	6.4	Cc1nc(C)c(-c2csc(Nc3ccc(Br)cc3C(F)(F)F)n2)s1	10.1016/j.ejmech.2019.01.063
	CHEMBL4472177	172173	None	0	Human	Functional	pEC50	=	4.9	4.9	-	1	Agonist activity at human mu opioid receptor expressed in CHOK1 cells coexpressing Galpha15 assessed as increase in intracellular calcium flux in presence of mu opioid receptor antagonist naloxone and incubated for 1 hr measured for 90 secs at 1.5 sec interval by FLIPR assayAgonist activity at human mu opioid receptor expressed in CHOK1 cells coexpressing Galpha15 assessed as increase in intracellular calcium flux in presence of mu opioid receptor antagonist naloxone and incubated for 1 hr measured for 90 secs at 1.5 sec interval by FLIPR assay	ChEMBL	433	3	1	5	6.4	Cc1nc(C)c(-c2csc(Nc3ccc(Br)cc3C(F)(F)F)n2)s1	10.1016/j.ejmech.2019.01.063
	71761637	91434	None	0	Rat	Functional	pEC50	=	5.9	5.9	1	2	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	635	7	8	10	-2.4	NC(=O)[C@@H]1C/N=C(/N2CCCC2)NC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1	10.1021/jm4008592
	CHEMBL2402929	91434	None	0	Rat	Functional	pEC50	=	5.9	5.9	1	2	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	635	7	8	10	-2.4	NC(=O)[C@@H]1C/N=C(/N2CCCC2)NC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1	10.1021/jm4008592
	168679651	195904	None	2	Mouse	Functional	pEC50	=	5.9	5.9	-1	2	Partial 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 assayPartial 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	ChEMBL	428	9	1	3	4.6	COc1ccccc1[C@@H]1C[C@H]1NCCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	10.1021/acs.jmedchem.3c00417
	CHEMBL5412995	195904	None	2	Mouse	Functional	pEC50	=	5.9	5.9	-1	2	Partial 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 assayPartial 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	ChEMBL	428	9	1	3	4.6	COc1ccccc1[C@@H]1C[C@H]1NCCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	10.1021/acs.jmedchem.3c00417
	13787553	204266	None	0	Rat	Functional	pEC50	=	5.9	5.9	-8	2	Agonist activity against rat Opioid receptor mu 1 expressed in C6 cells in [35S]-GTP-gamma S binding assay Agonist activity against rat Opioid receptor mu 1 expressed in C6 cells in [35S]-GTP-gamma S binding assay	ChEMBL	581	0	5	8	2.3	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4c(c2C[C@@]3(O)[C@H]1C5)C[C@@]1(O)[C@H]2Cc3ccc(O)c5c3[C@@]1(CCN2C)[C@H]4O5	10.1021/jm049172n
	CHEMBL606959	204266	None	0	Rat	Functional	pEC50	=	5.9	5.9	-8	2	Agonist activity against rat Opioid receptor mu 1 expressed in C6 cells in [35S]-GTP-gamma S binding assay Agonist activity against rat Opioid receptor mu 1 expressed in C6 cells in [35S]-GTP-gamma S binding assay	ChEMBL	581	0	5	8	2.3	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4c(c2C[C@@]3(O)[C@H]1C5)C[C@@]1(O)[C@H]2Cc3ccc(O)c5c3[C@@]1(CCN2C)[C@H]4O5	10.1021/jm049172n
	71454515	79175	None	0	Human	Functional	pEC50	=	6.9	6.9	-1	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	486	7	1	5	4.4	COc1ccc2c3c1O[C@H]1[C@]4(OC)CC[C@@]5(C[C@@H]4CNC/C=C/c4ccccc4)[C@@H](C2)N(C)CC[C@]315	10.1021/jm070255o
	CHEMBL2113309	79175	None	0	Human	Functional	pEC50	=	6.9	6.9	-1	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	486	7	1	5	4.4	COc1ccc2c3c1O[C@H]1[C@]4(OC)CC[C@@]5(C[C@@H]4CNC/C=C/c4ccccc4)[C@@H](C2)N(C)CC[C@]315	10.1021/jm070255o
	44337800	5451	None	0	Human	Functional	pEC50	=	6.9	6.9	-1	3	Effective concentration agonistic activity towards Opioid receptor mu 1Effective concentration agonistic activity towards Opioid receptor mu 1	ChEMBL	502	2	2	3	6.6	COc1ccc2c(c1O)[C@]13CCN(C)C(C2)[C@@]12C/C(=C(/C)c1ccccc1)[C@@H]3c1[nH]c3ccccc3c1C2	10.1021/jm030801n
	CHEMBL107420	5451	None	0	Human	Functional	pEC50	=	6.9	6.9	-1	3	Effective concentration agonistic activity towards Opioid receptor mu 1Effective concentration agonistic activity towards Opioid receptor mu 1	ChEMBL	502	2	2	3	6.6	COc1ccc2c(c1O)[C@]13CCN(C)C(C2)[C@@]12C/C(=C(/C)c1ccccc1)[C@@H]3c1[nH]c3ccccc3c1C2	10.1021/jm030801n
	89978524	160667	None	0	Human	Functional	pEC50	=	6.9	6.9	-6	3	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	447	6	1	5	4.0	COc1ccc2c3c1O[C@@H]1[C@]34CCN[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2	nan
	CHEMBL4112656	160667	None	0	Human	Functional	pEC50	=	6.9	6.9	-6	3	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	447	6	1	5	4.0	COc1ccc2c3c1O[C@@H]1[C@]34CCN[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2	nan
	1623	1560	None	36	Human	Functional	pEC50	=	7.9	7.9	-2	6	Agonist activity at human MOP assessed as forskolin stimulated cAMP accumulationAgonist activity at human MOP assessed as forskolin stimulated cAMP accumulation	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01915
	5311080	1560	None	36	Human	Functional	pEC50	=	7.9	7.9	-2	6	Agonist activity at human MOP assessed as forskolin stimulated cAMP accumulationAgonist activity at human MOP assessed as forskolin stimulated cAMP accumulation	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01915
	CHEMBL316446	1560	None	36	Human	Functional	pEC50	=	7.9	7.9	-2	6	Agonist activity at human MOP assessed as forskolin stimulated cAMP accumulationAgonist activity at human MOP assessed as forskolin stimulated cAMP accumulation	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01915
	102004349	174050	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	364	4	0	3	3.5	CC1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccc2)C1=O	10.1021/acs.jmedchem.0c01127
	102004349	174050	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	364	4	0	3	3.5	CC1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccc2)C1=O	10.1021/acs.jmedchem.9b01256
	CHEMBL4541206	174050	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	364	4	0	3	3.5	CC1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccc2)C1=O	10.1021/acs.jmedchem.0c01127
	CHEMBL4541206	174050	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	364	4	0	3	3.5	CC1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccc2)C1=O	10.1021/acs.jmedchem.9b01256
	44427176	92052	None	0	Human	Functional	pEC50	=	7.9	7.9	1	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	ChEMBL	354	3	1	3	3.9	CNC(=O)Oc1ccc2c(c1)C13CCCCC1C(C2)N(CC1CC1)CC3	10.1016/j.bmcl.2007.01.013
	CHEMBL241824	92052	None	0	Human	Functional	pEC50	=	7.9	7.9	1	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	ChEMBL	354	3	1	3	3.9	CNC(=O)Oc1ccc2c(c1)C13CCCCC1C(C2)N(CC1CC1)CC3	10.1016/j.bmcl.2007.01.013
	1663	2717	None	11	Human	Functional	pEC50	=	7.9	7.9	-2	4	Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	357	2	3	5	1.7	O[C@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CCC2)ccc1O)O	10.1021/jm061327z
	1874	2717	None	11	Human	Functional	pEC50	=	7.9	7.9	-2	4	Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	357	2	3	5	1.7	O[C@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CCC2)ccc1O)O	10.1021/jm061327z
	5311304	2717	None	11	Human	Functional	pEC50	=	7.9	7.9	-2	4	Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	357	2	3	5	1.7	O[C@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CCC2)ccc1O)O	10.1021/jm061327z
	5311304.0	2717	None	11	Human	Functional	pEC50	=	7.9	7.9	-2	4	Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	357	2	3	5	1.7	O[C@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CCC2)ccc1O)O	10.1021/jm061327z
	CHEMBL895	2717	None	11	Human	Functional	pEC50	=	7.9	7.9	-2	4	Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	357	2	3	5	1.7	O[C@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CCC2)ccc1O)O	10.1021/jm061327z
	DB00844	2717	None	11	Human	Functional	pEC50	=	7.9	7.9	-2	4	Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	357	2	3	5	1.7	O[C@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CCC2)ccc1O)O	10.1021/jm061327z
	CHEMBL2419541	212901	None	0	Rat	Functional	pEC50	=	7.9	7.9	-2	3	Agonist activity at rat MOR expressed in HN9.10 cell membranes by [35S]GTPgammaS binding assayAgonist activity at rat MOR expressed in HN9.10 cell membranes by [35S]GTPgammaS binding assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1016/j.bmcl.2013.06.065
	122195961	124282	None	0	Rat	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	478	6	3	3	5.8	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCCc2ccc(Cc3cccc4ccccc34)cc21	10.1021/acs.jmedchem.5b01270
	CHEMBL3634255	124282	None	0	Rat	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	478	6	3	3	5.8	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCCc2ccc(Cc3cccc4ccccc34)cc21	10.1021/acs.jmedchem.5b01270
	72164056	92096	None	0	Mouse	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	ChEMBL	554	6	4	7	2.4	O=C(CNC(=O)c1cc2ccccc2cn1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2013.07.043
	CHEMBL2419120	92096	None	0	Mouse	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	ChEMBL	554	6	4	7	2.4	O=C(CNC(=O)c1cc2ccccc2cn1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2013.07.043
	CHEMBL5079983	217145	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL		None	None	None		c1ccc([C@]2(CCNCc3scc4c3COC4)CCOC3(CCOC3)C2)nc1	10.1016/j.ejmech.2021.113986
	72164056	92096	None	0	Mouse	Functional	pEC50	=	7.9	7.9	-	1	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	554	6	4	7	2.4	O=C(CNC(=O)c1cc2ccccc2cn1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmc.2015.02.055
	CHEMBL2419120	92096	None	0	Mouse	Functional	pEC50	=	7.9	7.9	-	1	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	554	6	4	7	2.4	O=C(CNC(=O)c1cc2ccccc2cn1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmc.2015.02.055
	71450926	79166	None	0	Human	Functional	pEC50	=	7.8	7.8	5	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	545	7	1	7	3.9	COc1ccc2c3c1O[C@H]1[C@]4(OC)CC[C@@]5(C[C@@H]4CNC(=O)/C=C/c4ccccc4[N+](=O)[O-])[C@@H](C2)N(C)CC[C@]315	10.1021/jm070255o
	CHEMBL2113300	79166	None	0	Human	Functional	pEC50	=	7.8	7.8	5	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	545	7	1	7	3.9	COc1ccc2c3c1O[C@H]1[C@]4(OC)CC[C@@]5(C[C@@H]4CNC(=O)/C=C/c4ccccc4[N+](=O)[O-])[C@@H](C2)N(C)CC[C@]315	10.1021/jm070255o
	CHEMBL5085104	217438	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISAAgonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISA	ChEMBL		None	None	None		Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H]1CSSC[C@@H](C(=O)NCC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](CCCNC(=N)N)C(=O)O)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.1c01631
	71458064	79180	None	0	Human	Functional	pEC50	=	7.8	7.8	-1	2	Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	510	3	1	5	3.7	CO[C@@]12C=C[C@@]3([C@@H]4CN(C(=O)/C=C/c5ccc(C)cc5)C[C@@H]41)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1021/jm070255o
	CHEMBL2113314	79180	None	0	Human	Functional	pEC50	=	7.8	7.8	-1	2	Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	510	3	1	5	3.7	CO[C@@]12C=C[C@@]3([C@@H]4CN(C(=O)/C=C/c5ccc(C)cc5)C[C@@H]41)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1021/jm070255o
	1623	1560	None	36	Human	Functional	pEC50	=	7.8	7.8	-2	6	Agonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production	ChEMBL		None	None	None		None	10.1016/j.bmcl.2015.09.025
	5311080	1560	None	36	Human	Functional	pEC50	=	7.8	7.8	-2	6	Agonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production	ChEMBL		None	None	None		None	10.1016/j.bmcl.2015.09.025
	CHEMBL316446	1560	None	36	Human	Functional	pEC50	=	7.8	7.8	-2	6	Agonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production	ChEMBL		None	None	None		None	10.1016/j.bmcl.2015.09.025
	1623	1560	None	36	Human	Functional	pEC50	=	7.8	7.8	-2	6	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL		None	None	None		None	10.1021/jm300664y
	5311080	1560	None	36	Human	Functional	pEC50	=	7.8	7.8	-2	6	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL		None	None	None		None	10.1021/jm300664y
	CHEMBL316446	1560	None	36	Human	Functional	pEC50	=	7.8	7.8	-2	6	Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter	ChEMBL		None	None	None		None	10.1021/jm300664y
	44408411	161404	None	0	Rat	Functional	pEC50	=	7.8	7.8	-6	5	Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells	ChEMBL	1242	31	11	15	4.4	CCCC[C@@H](C(=O)N[C@@H](Cc1cn(C(C)=O)c2ccccc12)C(=O)O)N(C(=O)Nc1ccccc1Cl)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)N(C)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O	10.1021/jm050851n
	CHEMBL412331	161404	None	0	Rat	Functional	pEC50	=	7.8	7.8	-6	5	Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells	ChEMBL	1242	31	11	15	4.4	CCCC[C@@H](C(=O)N[C@@H](Cc1cn(C(C)=O)c2ccccc12)C(=O)O)N(C(=O)Nc1ccccc1Cl)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)N(C)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O	10.1021/jm050851n
	165405557	196893	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	Agonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assayAgonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assay	ChEMBL	376	8	2	3	3.5	C[C@@H](CC(=O)NC[C@H](Cc1c(F)cc(O)cc1F)N(C)C)c1ccccc1	10.1016/j.bmcl.2023.129405
	CHEMBL5434293	196893	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	Agonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assayAgonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assay	ChEMBL	376	8	2	3	3.5	C[C@@H](CC(=O)NC[C@H](Cc1c(F)cc(O)cc1F)N(C)C)c1ccccc1	10.1016/j.bmcl.2023.129405
	9848990	189274	None	0	Human	Functional	pEC50	=	7.8	7.8	-3	7	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm070255o
	9848990.0	189274	None	0	Human	Functional	pEC50	=	7.8	7.8	-3	7	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm070255o
	CHEMBL2368861	189274	None	0	Human	Functional	pEC50	=	7.8	7.8	-3	7	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm070255o
	CHEMBL511142	189274	None	0	Human	Functional	pEC50	=	7.8	7.8	-3	7	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm070255o
	121614715	156862	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	280	3	2	2	2.6	Cc1ccc(C(=O)NCC2NCCc3ccccc32)cc1	10.1016/j.ejmech.2016.09.003
	CHEMBL4070750	156862	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	280	3	2	2	2.6	Cc1ccc(C(=O)NCC2NCCc3ccccc32)cc1	10.1016/j.ejmech.2016.09.003
	11250396	145733	None	0	Human	Functional	pEC50	=	6.9	6.9	-26	2	Agonist activity at human cloned mu opioid receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned mu opioid receptor assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	600	17	7	8	-1.1	CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(C(N)=O)cc1)C(=O)O	10.1016/j.bmcl.2007.01.092
	CHEMBL391580	145733	None	0	Human	Functional	pEC50	=	6.9	6.9	-26	2	Agonist activity at human cloned mu opioid receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned mu opioid receptor assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	600	17	7	8	-1.1	CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(C(N)=O)cc1)C(=O)O	10.1016/j.bmcl.2007.01.092
	51357420	61241	None	0	Human	Functional	pEC50	=	6.9	6.9	-3	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting	ChEMBL	381	3	0	4	4.8	CN(C)c1nc2cc3c(cc2s1)C[C@@H]1[C@@H]2CCCC[C@]32CCN1CC1CC1	10.1021/jm101542c
	CHEMBL1766036	61241	None	0	Human	Functional	pEC50	=	6.9	6.9	-3	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting	ChEMBL	381	3	0	4	4.8	CN(C)c1nc2cc3c(cc2s1)C[C@@H]1[C@@H]2CCCC[C@]32CCN1CC1CC1	10.1021/jm101542c
	16720649	85395	None	0	Human	Functional	pEC50	=	6.9	6.9	-16	3	Agonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	327	0	2	5	2.3	CN1CC[C@]23Cc4nc(N)sc4C[C@H]2[C@H]1Cc1ccc(O)cc13	10.1021/jm0701674
	CHEMBL226167	85395	None	0	Human	Functional	pEC50	=	6.9	6.9	-16	3	Agonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	327	0	2	5	2.3	CN1CC[C@]23Cc4nc(N)sc4C[C@H]2[C@H]1Cc1ccc(O)cc13	10.1021/jm0701674
	CHEMBL261390	212977	None	0	Rat	Functional	pEC50	=	6.9	6.9	-3	3	Agonist activity at rat mu opioid receptor by [35S]GTP-gamma-S binding assayAgonist activity at rat mu opioid receptor by [35S]GTP-gamma-S binding assay	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1021/jm070332f
	49863734	15339	None	0	Rat	Functional	pEC50	=	6.9	6.9	-79	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding	ChEMBL	1477	21	11	14	6.8	CCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(C)(C)SSC(C)(C)[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm100157m
	CHEMBL1214027	15339	None	0	Rat	Functional	pEC50	=	6.9	6.9	-79	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding	ChEMBL	1477	21	11	14	6.8	CCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(C)(C)SSC(C)(C)[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm100157m
	44366823	97057	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	Stimulation of [35S]GTP-gamma-S, binding using COS-human Opioid receptor mu 1 membranesStimulation of [35S]GTP-gamma-S, binding using COS-human Opioid receptor mu 1 membranes	ChEMBL	903	22	10	10	-1.0	CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@H]2SC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O	10.1021/jm020078l
	CHEMBL266609	97057	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	Stimulation of [35S]GTP-gamma-S, binding using COS-human Opioid receptor mu 1 membranesStimulation of [35S]GTP-gamma-S, binding using COS-human Opioid receptor mu 1 membranes	ChEMBL	903	22	10	10	-1.0	CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@H]2SC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O	10.1021/jm020078l
	126619369	170989	None	0	Human	Functional	pEC50	=	4.9	4.9	-	1	Agonist activity at human mu opioid receptor expressed in CHOK1 cells coexpressing Galpha15 assessed as increase in intracellular calcium flux in presence of mu opioid receptor antagonist naloxone and incubated for 1 hr measured for 90 secs at 1.5 sec interval by FLIPR assayAgonist activity at human mu opioid receptor expressed in CHOK1 cells coexpressing Galpha15 assessed as increase in intracellular calcium flux in presence of mu opioid receptor antagonist naloxone and incubated for 1 hr measured for 90 secs at 1.5 sec interval by FLIPR assay	ChEMBL	331	4	1	6	4.9	COc1ccc(Nc2nc(-c3sc(C)nc3C)cs2)c(C)c1	10.1016/j.ejmech.2019.01.063
	CHEMBL4454409	170989	None	0	Human	Functional	pEC50	=	4.9	4.9	-	1	Agonist activity at human mu opioid receptor expressed in CHOK1 cells coexpressing Galpha15 assessed as increase in intracellular calcium flux in presence of mu opioid receptor antagonist naloxone and incubated for 1 hr measured for 90 secs at 1.5 sec interval by FLIPR assayAgonist activity at human mu opioid receptor expressed in CHOK1 cells coexpressing Galpha15 assessed as increase in intracellular calcium flux in presence of mu opioid receptor antagonist naloxone and incubated for 1 hr measured for 90 secs at 1.5 sec interval by FLIPR assay	ChEMBL	331	4	1	6	4.9	COc1ccc(Nc2nc(-c3sc(C)nc3C)cs2)c(C)c1	10.1016/j.ejmech.2019.01.063
	145966009	164427	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	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 methodAgonist 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	ChEMBL	467	3	1	3	5.6	O=c1[nH]c2cc(Cl)c(Cl)cc2n1C1CCCN(Cc2ccc(Br)cc2)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4212478	164427	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	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 methodAgonist 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	ChEMBL	467	3	1	3	5.6	O=c1[nH]c2cc(Cl)c(Cl)cc2n1C1CCCN(Cc2ccc(Br)cc2)CC1	10.1021/acs.jmedchem.8b01136
	66826389	160849	None	0	Human	Functional	pEC50	=	5.9	5.9	-2	2	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	519	9	1	6	4.2	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CCC(=O)O)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2	nan
	CHEMBL4114011	160849	None	0	Human	Functional	pEC50	=	5.9	5.9	-2	2	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	519	9	1	6	4.2	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CCC(=O)O)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2	nan
	156020566	178168	None	0	Human	Functional	pEC50	=	6.9	6.9	-57	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	610	9	1	5	7.7	Oc1ccc2c3c1O[C@H]1c4ncc(-c5ccccc5C5CC5)cc4C[C@@]4(OCCCc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/acs.jmedchem.0c00503
	CHEMBL4647353	178168	None	0	Human	Functional	pEC50	=	6.9	6.9	-57	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	610	9	1	5	7.7	Oc1ccc2c3c1O[C@H]1c4ncc(-c5ccccc5C5CC5)cc4C[C@@]4(OCCCc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/acs.jmedchem.0c00503
	CHEMBL5085771	217476	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	Agonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assay	ChEMBL		None	None	None		CCC(=O)N(CC1(N2CCN(C(C)c3ccccc3)CC2)CCOCC1)c1cccc(C(F)(F)F)n1	10.1021/acs.jmedchem.1c00417
	16326480	59583	None	4	Human	Functional	pEC50	=	5.9	5.9	18	2	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	332	8	1	4	3.1	COc1ccc(C(CNC(=O)CCc2ccsc2)N(C)C)cc1	nan
	CHEMBL1717557	59583	None	4	Human	Functional	pEC50	=	5.9	5.9	18	2	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	332	8	1	4	3.1	COc1ccc(C(CNC(=O)CCc2ccsc2)N(C)C)cc1	nan
	137656339	158834	None	0	Human	Functional	pEC50	=	4.9	4.9	-114815	2	Agonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assayAgonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assay	ChEMBL	492	5	3	7	2.6	CN(C(=O)/C=C/c1ccco1)[C@@H]1CC[C@@]2(O)[C@H]3[C@@H](O)c4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2017.06.017
	CHEMBL4093632	158834	None	0	Human	Functional	pEC50	=	4.9	4.9	-114815	2	Agonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assayAgonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assay	ChEMBL	492	5	3	7	2.6	CN(C(=O)/C=C/c1ccco1)[C@@H]1CC[C@@]2(O)[C@H]3[C@@H](O)c4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2017.06.017
	118567672	170332	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	365	4	0	4	2.9	CC1OC2(CCN(CCc3ccncc3)CC2)CN(c2ccccc2)C1=O	10.1021/acs.jmedchem.9b01256
	CHEMBL4445578	170332	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	365	4	0	4	2.9	CC1OC2(CCN(CCc3ccncc3)CC2)CN(c2ccccc2)C1=O	10.1021/acs.jmedchem.9b01256
	155519089	170446	None	0	Rat	Functional	pEC50	=	5.9	5.9	-17	2	Agonist activity at rat MOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation countingAgonist activity at rat MOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting	ChEMBL	562	8	1	5	6.7	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](c1ccc(NCc3ccccc3)cc1)C2	10.1021/acs.jmedchem.9b00857
	CHEMBL4447249	170446	None	0	Rat	Functional	pEC50	=	5.9	5.9	-17	2	Agonist activity at rat MOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation countingAgonist activity at rat MOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting	ChEMBL	562	8	1	5	6.7	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](c1ccc(NCc3ccccc3)cc1)C2	10.1021/acs.jmedchem.9b00857
	53316969	57330	None	0	Human	Functional	pEC50	=	6.8	6.8	-3	3	Agonist activity at human MOP receptor expressed in CHO-K1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human MOP receptor expressed in CHO-K1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting	ChEMBL	357	3	2	4	3.4	O=c1[nH]c2ccccc2n1C1CCN(C2(CO)CCCCCCC2)CC1	10.1016/j.bmc.2010.07.034
	CHEMBL1650851	57330	None	0	Human	Functional	pEC50	=	6.8	6.8	-3	3	Agonist activity at human MOP receptor expressed in CHO-K1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human MOP receptor expressed in CHO-K1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting	ChEMBL	357	3	2	4	3.4	O=c1[nH]c2ccccc2n1C1CCN(C2(CO)CCCCCCC2)CC1	10.1016/j.bmc.2010.07.034
	118567744	173408	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	394	5	0	4	3.5	COc1ccccc1N1CC2(CCN(CCc3ccccc3)CC2)OC(C)C1=O	10.1021/acs.jmedchem.9b01256
	CHEMBL4526087	173408	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	394	5	0	4	3.5	COc1ccccc1N1CC2(CCN(CCc3ccccc3)CC2)OC(C)C1=O	10.1021/acs.jmedchem.9b01256
	71761638	91435	None	0	Rat	Functional	pEC50	=	5.8	5.8	-4	3	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	649	7	8	10	-2.0	NC(=O)[C@@H]1C/N=C(/N2CCCCC2)NC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1	10.1021/jm4008592
	CHEMBL2402930	91435	None	0	Rat	Functional	pEC50	=	5.8	5.8	-4	3	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	649	7	8	10	-2.0	NC(=O)[C@@H]1C/N=C(/N2CCCCC2)NC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1	10.1021/jm4008592
	16193242	41389	None	5	Human	Functional	pEC50	=	4.8	4.8	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	445	5	2	6	4.1	COc1ccc(-n2c3c(cc(C(=O)NNc4ccccc4C)c2=O)C(=O)CC(C)(C)C3)cc1	nan
	CHEMBL1490069	41389	None	5	Human	Functional	pEC50	=	4.8	4.8	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	445	5	2	6	4.1	COc1ccc(-n2c3c(cc(C(=O)NNc4ccccc4C)c2=O)C(=O)CC(C)(C)C3)cc1	nan
	1647	1313	None	34	Rat	Functional	pEC50	=	6.8	6.8	-5	9	Activity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS bindingActivity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS binding	ChEMBL		None	None	None		None	10.1021/jm800223t
	5462471	1313	None	34	Rat	Functional	pEC50	=	6.8	6.8	-5	9	Activity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS bindingActivity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS binding	ChEMBL		None	None	None		None	10.1021/jm800223t
	CHEMBL113995	1313	None	34	Rat	Functional	pEC50	=	6.8	6.8	-5	9	Activity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS bindingActivity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS binding	ChEMBL		None	None	None		None	10.1021/jm800223t
	CHEMBL38874	1313	None	34	Rat	Functional	pEC50	=	6.8	6.8	-5	9	Activity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS bindingActivity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS binding	ChEMBL		None	None	None		None	10.1021/jm800223t
	145982510	165503	None	0	Rat	Functional	pEC50	=	6.8	6.8	-2	3	Agonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis	ChEMBL	529	7	0	6	5.2	COc1ccc(C(=O)[C@@]2(C)C[C@@]34CC[C@]2(OC)[C@@H]2Oc5c(OC)ccc6c5[C@@]23CCN(CC2CC2)[C@@H]4C6)cc1	10.1016/j.bmc.2018.07.020
	CHEMBL4238289	165503	None	0	Rat	Functional	pEC50	=	6.8	6.8	-2	3	Agonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis	ChEMBL	529	7	0	6	5.2	COc1ccc(C(=O)[C@@]2(C)C[C@@]34CC[C@]2(OC)[C@@H]2Oc5c(OC)ccc6c5[C@@]23CCN(CC2CC2)[C@@H]4C6)cc1	10.1016/j.bmc.2018.07.020
	1647	1313	None	34	Rat	Functional	pEC50	=	6.8	6.8	-5	9	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 methodAgonist 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	ChEMBL		None	None	None		None	10.1016/j.bmc.2017.02.064
	5462471	1313	None	34	Rat	Functional	pEC50	=	6.8	6.8	-5	9	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 methodAgonist 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	ChEMBL		None	None	None		None	10.1016/j.bmc.2017.02.064
	CHEMBL113995	1313	None	34	Rat	Functional	pEC50	=	6.8	6.8	-5	9	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 methodAgonist 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	ChEMBL		None	None	None		None	10.1016/j.bmc.2017.02.064
	CHEMBL38874	1313	None	34	Rat	Functional	pEC50	=	6.8	6.8	-5	9	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 methodAgonist 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	ChEMBL		None	None	None		None	10.1016/j.bmc.2017.02.064
	CHEMBL5075152	216848	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assay	ChEMBL		None	None	None		COCC(=O)N(CC(C)(C)N1CCN(Cc2ccccc2)CC1)c1ccccc1	10.1021/acs.jmedchem.1c00417
	1627	2594	None	9	Human	Functional	pEC50	=	6.8	6.8	-1	9	Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.9b01818
	1845	2594	None	9	Human	Functional	pEC50	=	6.8	6.8	-1	9	Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.9b01818
	5288826	2594	None	9	Human	Functional	pEC50	=	6.8	6.8	-1	9	Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.9b01818
	5288826.0	2594	None	9	Human	Functional	pEC50	=	6.8	6.8	-1	9	Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.9b01818
	CHEMBL70	2594	None	9	Human	Functional	pEC50	=	6.8	6.8	-1	9	Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.9b01818
	DB00295	2594	None	9	Human	Functional	pEC50	=	6.8	6.8	-1	9	Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.9b01818
	155564196	175509	None	0	Rat	Functional	pEC50	=	5.8	5.8	-2	2	Agonist activity at MOR in Wistar rat brain membranes in presence of naloxone after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at MOR in Wistar rat brain membranes in presence of naloxone after 60 mins by [35S]-GTPgammaS binding assay	ChEMBL	851	21	7	9	4.1	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)NCCCCCn1cc(C(=O)c2cccc3ccccc23)c2ccccc21	10.1016/j.ejmech.2019.05.037
	CHEMBL4575678	175509	None	0	Rat	Functional	pEC50	=	5.8	5.8	-2	2	Agonist activity at MOR in Wistar rat brain membranes in presence of naloxone after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at MOR in Wistar rat brain membranes in presence of naloxone after 60 mins by [35S]-GTPgammaS binding assay	ChEMBL	851	21	7	9	4.1	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)NCCCCCn1cc(C(=O)c2cccc3ccccc23)c2ccccc21	10.1016/j.ejmech.2019.05.037
	145977533	163702	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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 methodAgonist 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	ChEMBL	375	3	1	3	4.5	O=c1[nH]c2ccc(Cl)cc2n1C1CCN(Cc2ccccc2Cl)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4203641	163702	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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 methodAgonist 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	ChEMBL	375	3	1	3	4.5	O=c1[nH]c2ccc(Cl)cc2n1C1CCN(Cc2ccccc2Cl)CC1	10.1021/acs.jmedchem.8b01136
	130431412	164816	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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 methodAgonist 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	ChEMBL	453	3	1	3	5.2	O=c1[nH]c2cc(Cl)c(Cl)cc2n1C1CCN(Cc2ccc(Br)cc2)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4217435	164816	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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 methodAgonist 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	ChEMBL	453	3	1	3	5.2	O=c1[nH]c2cc(Cl)c(Cl)cc2n1C1CCN(Cc2ccc(Br)cc2)CC1	10.1021/acs.jmedchem.8b01136
	71454516	79176	None	0	Human	Functional	pEC50	=	6.8	6.8	1	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	520	7	1	5	5.1	COc1ccc2c3c1O[C@H]1[C@]4(OC)CC[C@@]5(C[C@@H]4CNC/C=C/c4ccc(Cl)cc4)[C@@H](C2)N(C)CC[C@]315	10.1021/jm070255o
	CHEMBL2113310	79176	None	0	Human	Functional	pEC50	=	6.8	6.8	1	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	520	7	1	5	5.1	COc1ccc2c3c1O[C@H]1[C@]4(OC)CC[C@@]5(C[C@@H]4CNC/C=C/c4ccc(Cl)cc4)[C@@H](C2)N(C)CC[C@]315	10.1021/jm070255o
	71456258	79210	None	0	Human	Functional	pEC50	=	6.8	6.8	-44	3	Stimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cellsStimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells	ChEMBL	457	4	3	4	4.1	CCCCC(=O)N[C@@]12Cc3c([nH]c4ccccc34)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)C2C5	10.1021/jm021073r
	CHEMBL2113381	79210	None	0	Human	Functional	pEC50	=	6.8	6.8	-44	3	Stimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cellsStimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells	ChEMBL	457	4	3	4	4.1	CCCCC(=O)N[C@@]12Cc3c([nH]c4ccccc34)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)C2C5	10.1021/jm021073r
	172444704	194949	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assay	ChEMBL	342	5	1	3	4.1	CN(C)C(CNC(=O)c1cc2ccccc2s1)c1cccc(F)c1	10.1016/j.ejmech.2022.114728
	CHEMBL5393886	194949	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assay	ChEMBL	342	5	1	3	4.1	CN(C)C(CNC(=O)c1cc2ccccc2s1)c1cccc(F)c1	10.1016/j.ejmech.2022.114728
	118560889	180354	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	329	4	0	4	1.9	CCN1CC2(CCN(CCc3ccccn3)CC2)OC2(CC2)C1=O	10.1021/acs.jmedchem.0c01127
	CHEMBL4750243	180354	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	329	4	0	4	1.9	CCN1CC2(CCN(CCc3ccccn3)CC2)OC2(CC2)C1=O	10.1021/acs.jmedchem.0c01127
	1647	1313	None	34	Human	Functional	pEC50	=	7.8	7.8	-3	9	Agonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assayAgonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay	ChEMBL		None	None	None		None	10.1016/j.bmcl.2013.06.084
	5462471	1313	None	34	Human	Functional	pEC50	=	7.8	7.8	-3	9	Agonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assayAgonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay	ChEMBL		None	None	None		None	10.1016/j.bmcl.2013.06.084
	CHEMBL113995	1313	None	34	Human	Functional	pEC50	=	7.8	7.8	-3	9	Agonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assayAgonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay	ChEMBL		None	None	None		None	10.1016/j.bmcl.2013.06.084
	CHEMBL38874	1313	None	34	Human	Functional	pEC50	=	7.8	7.8	-3	9	Agonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assayAgonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay	ChEMBL		None	None	None		None	10.1016/j.bmcl.2013.06.084
	155516536	176687	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	487	8	3	5	3.8	CCOc1ccc(C(=O)N2Cc3ccccc3C2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b01818
	CHEMBL4443759	176687	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	487	8	3	5	3.8	CCOc1ccc(C(=O)N2Cc3ccccc3C2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b01818
	CHEMBL4597505	176687	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	487	8	3	5	3.8	CCOc1ccc(C(=O)N2Cc3ccccc3C2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b01818
	132079908	180880	None	0	Human	Functional	pEC50	=	7.8	7.8	4	3	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 assayAgonist 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	ChEMBL	510	4	0	8	4.6	COC(=O)[C@@H]1C=C(OC(=O)c2ccc(F)cc2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@@]12C	10.1021/acs.jmedchem.6b01235
	CHEMBL4756271	180880	None	0	Human	Functional	pEC50	=	7.8	7.8	4	3	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 assayAgonist 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	ChEMBL	510	4	0	8	4.6	COC(=O)[C@@H]1C=C(OC(=O)c2ccc(F)cc2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@@]12C	10.1021/acs.jmedchem.6b01235
	72713091	106486	None	0	Human	Functional	pEC50	=	7.8	7.8	-1	2	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	378	6	2	3	4.4	CN[C@H]1C[C@H]2C[C@@](c3cccc(O)c3)(C1)[C@H](C)CN2CCCc1ccccc1	10.1021/jm401250s
	CHEMBL3139588	106486	None	0	Human	Functional	pEC50	=	7.8	7.8	-1	2	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	378	6	2	3	4.4	CN[C@H]1C[C@H]2C[C@@](c3cccc(O)c3)(C1)[C@H](C)CN2CCCc1ccccc1	10.1021/jm401250s
	CHEMBL3217272	106486	None	0	Human	Functional	pEC50	=	7.8	7.8	-1	2	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	378	6	2	3	4.4	CN[C@H]1C[C@H]2C[C@@](c3cccc(O)c3)(C1)[C@H](C)CN2CCCc1ccccc1	10.1021/jm401250s
	44433399	89965	None	0	Human	Functional	pEC50	=	7.8	7.8	1	3	Agonist activity at human mu opioid receptor expressed in CHO membrane by [35S]GTP-gamma-S binding assayAgonist activity at human mu opioid receptor expressed in CHO membrane by [35S]GTP-gamma-S binding assay	ChEMBL	387	2	3	6	1.2	CO[C@]12C(O)C[C@@]3(C[C@@H]1[C@H](C)O)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1016/j.bmcl.2007.06.050
	CHEMBL238017	89965	None	0	Human	Functional	pEC50	=	7.8	7.8	1	3	Agonist activity at human mu opioid receptor expressed in CHO membrane by [35S]GTP-gamma-S binding assayAgonist activity at human mu opioid receptor expressed in CHO membrane by [35S]GTP-gamma-S binding assay	ChEMBL	387	2	3	6	1.2	CO[C@]12C(O)C[C@@]3(C[C@@H]1[C@H](C)O)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1016/j.bmcl.2007.06.050
	122195964	124285	None	0	Rat	Functional	pEC50	=	7.8	7.8	22	2	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	511	6	3	4	4.8	CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(CC3CCc4ccccc43)ccc21	10.1021/acs.jmedchem.5b01270
	CHEMBL3634258	124285	None	0	Rat	Functional	pEC50	=	7.8	7.8	22	2	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	511	6	3	4	4.8	CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(CC3CCc4ccccc43)ccc21	10.1021/acs.jmedchem.5b01270
	86582748	160928	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	382	3	3	4	2.8	C=C1CC[C@@]2(O)[C@H]3Cc4ccc(C(N)=O)c(O)c4[C@@]2(CCN3CC=C(C)C)C1	nan
	CHEMBL4114707	160928	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	382	3	3	4	2.8	C=C1CC[C@@]2(O)[C@H]3Cc4ccc(C(N)=O)c(O)c4[C@@]2(CCN3CC=C(C)C)C1	nan
	44408411	161404	None	0	Rat	Functional	pEC50	=	7.8	7.8	-6	5	Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells	ChEMBL	1242	31	11	15	4.4	CCCC[C@@H](C(=O)N[C@@H](Cc1cn(C(C)=O)c2ccccc12)C(=O)O)N(C(=O)Nc1ccccc1Cl)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)N(C)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O	10.1021/jm050851n
	CHEMBL412331	161404	None	0	Rat	Functional	pEC50	=	7.8	7.8	-6	5	Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells	ChEMBL	1242	31	11	15	4.4	CCCC[C@@H](C(=O)N[C@@H](Cc1cn(C(C)=O)c2ccccc12)C(=O)O)N(C(=O)Nc1ccccc1Cl)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)N(C)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O	10.1021/jm050851n
	71454513	79161	None	0	Human	Functional	pEC50	=	7.8	7.8	2	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	514	6	1	5	4.3	COc1ccc2c3c1O[C@H]1[C@]4(OC)CC[C@@]5(C[C@@H]4CNC(=O)/C=C/c4ccccc4C)[C@@H](C2)N(C)CC[C@]315	10.1021/jm070255o
	CHEMBL2113295	79161	None	0	Human	Functional	pEC50	=	7.8	7.8	2	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	514	6	1	5	4.3	COc1ccc2c3c1O[C@H]1[C@]4(OC)CC[C@@]5(C[C@@H]4CNC(=O)/C=C/c4ccccc4C)[C@@H](C2)N(C)CC[C@]315	10.1021/jm070255o
	CHEMBL5094655	217995	None	0	Human	Functional	pEC50	=	7.8	7.8	1	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis	ChEMBL		None	None	None		Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(N)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O	10.1021/acs.jmedchem.0c02062
	44337683	9163	None	0	Human	Functional	pEC50	=	7.8	7.8	-4	3	Effective concentration agonistic activity towards Opioid receptor mu 1Effective concentration agonistic activity towards Opioid receptor mu 1	ChEMBL	429	2	1	4	4.7	COc1ccc2c(c1O)[C@]13CCN(C)C(C2)[C@]12CCC(=O)[C@H]3/C(=C(\C)c1ccccc1)C2	10.1021/jm030801n
	CHEMBL110124	9163	None	0	Human	Functional	pEC50	=	7.8	7.8	-4	3	Effective concentration agonistic activity towards Opioid receptor mu 1Effective concentration agonistic activity towards Opioid receptor mu 1	ChEMBL	429	2	1	4	4.7	COc1ccc2c(c1O)[C@]13CCN(C)C(C2)[C@]12CCC(=O)[C@H]3/C(=C(\C)c1ccccc1)C2	10.1021/jm030801n
	72735758	106389	None	0	Human	Functional	pEC50	=	7.8	7.8	-11	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay	ChEMBL	442	2	2	5	3.5	Oc1ccc2c(c1)[C@]13CCN(C[C@@H]4CCCO4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3	10.1016/j.bmc.2013.10.032
	CHEMBL3139163	106389	None	0	Human	Functional	pEC50	=	7.8	7.8	-11	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay	ChEMBL	442	2	2	5	3.5	Oc1ccc2c(c1)[C@]13CCN(C[C@@H]4CCCO4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3	10.1016/j.bmc.2013.10.032
	CHEMBL4296737	106389	None	0	Human	Functional	pEC50	=	7.8	7.8	-11	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay	ChEMBL	442	2	2	5	3.5	Oc1ccc2c(c1)[C@]13CCN(C[C@@H]4CCCO4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3	10.1016/j.bmc.2013.10.032
	CHEMBL5087383	217581	None	0	Human	Functional	pEC50	=	7.8	7.8	7	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis	ChEMBL		None	None	None		Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O	10.1021/acs.jmedchem.0c02062
	130431397	170847	None	34	Human	Functional	pEC50	=	7.8	7.8	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL	409	3	1	3	5.1	O=c1[nH]c2cc(Cl)c(Cl)cc2n1C1CCN(Cc2ccc(Cl)cc2)CC1	10.1039/d0md00104j
	CHEMBL4452384	170847	None	34	Human	Functional	pEC50	=	7.8	7.8	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL	409	3	1	3	5.1	O=c1[nH]c2cc(Cl)c(Cl)cc2n1C1CCN(Cc2ccc(Cl)cc2)CC1	10.1039/d0md00104j
	1627	2594	None	9	Human	Functional	pEC50	=	7.8	7.8	-1	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm070255o
	1845	2594	None	9	Human	Functional	pEC50	=	7.8	7.8	-1	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm070255o
	5288826	2594	None	9	Human	Functional	pEC50	=	7.8	7.8	-1	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm070255o
	5288826.0	2594	None	9	Human	Functional	pEC50	=	7.8	7.8	-1	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm070255o
	CHEMBL70	2594	None	9	Human	Functional	pEC50	=	7.8	7.8	-1	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm070255o
	DB00295	2594	None	9	Human	Functional	pEC50	=	7.8	7.8	-1	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm070255o
	1627	2594	None	9	Human	Functional	pEC50	=	7.8	7.8	-1	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm8012272
	1845	2594	None	9	Human	Functional	pEC50	=	7.8	7.8	-1	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm8012272
	5288826	2594	None	9	Human	Functional	pEC50	=	7.8	7.8	-1	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm8012272
	5288826.0	2594	None	9	Human	Functional	pEC50	=	7.8	7.8	-1	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm8012272
	CHEMBL70	2594	None	9	Human	Functional	pEC50	=	7.8	7.8	-1	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm8012272
	DB00295	2594	None	9	Human	Functional	pEC50	=	7.8	7.8	-1	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm8012272
	1627	2594	None	9	Human	Functional	pEC50	=	7.8	7.8	-1	9	Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm0604777
	1845	2594	None	9	Human	Functional	pEC50	=	7.8	7.8	-1	9	Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm0604777
	5288826	2594	None	9	Human	Functional	pEC50	=	7.8	7.8	-1	9	Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm0604777
	5288826.0	2594	None	9	Human	Functional	pEC50	=	7.8	7.8	-1	9	Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm0604777
	CHEMBL70	2594	None	9	Human	Functional	pEC50	=	7.8	7.8	-1	9	Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm0604777
	DB00295	2594	None	9	Human	Functional	pEC50	=	7.8	7.8	-1	9	Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm0604777
	3668	1561	None	36	Human	Functional	pEC50	=	7.8	7.8	1	5	Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISAAgonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISA	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01631
	5311081	1561	None	36	Human	Functional	pEC50	=	7.8	7.8	1	5	Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISAAgonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISA	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01631
	CHEMBL333357	1561	None	36	Human	Functional	pEC50	=	7.8	7.8	1	5	Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISAAgonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISA	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01631
	CHEMBL589982	1561	None	36	Human	Functional	pEC50	=	7.8	7.8	1	5	Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISAAgonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISA	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01631
	CHEMBL5072270	216765	None	0	Human	Functional	pEC50	=	7.8	7.8	3	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis	ChEMBL		None	None	None		Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O	10.1021/acs.jmedchem.0c02062
	72712793	93193	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	370	6	1	4	5.0	Cc1ccc(CNCC[C@@]2(c3ccccn3)CCOC3(CCCC3)C2)s1	10.1021/jm4010829
	CHEMBL2443257	93193	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	370	6	1	4	5.0	Cc1ccc(CNCC[C@@]2(c3ccccn3)CCOC3(CCCC3)C2)s1	10.1021/jm4010829
	72712370	93214	None	2	Human	Functional	pEC50	=	7.8	7.8	12	3	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	356	6	1	4	4.7	c1ccc([C@]2(CCNCc3cccs3)CCOC3(CCCC3)C2)nc1	10.1021/jm4010829
	CHEMBL2443278	93214	None	2	Human	Functional	pEC50	=	7.8	7.8	12	3	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	356	6	1	4	4.7	c1ccc([C@]2(CCNCc3cccs3)CCOC3(CCCC3)C2)nc1	10.1021/jm4010829
	172467824	196974	None	0	Human	Functional	pEC50	=	7.8	7.8	2	4	Agonist activity at MOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at MOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay	ChEMBL	1136	24	13	13	-0.8	CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C/C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1	10.1021/acs.jmedchem.3c02093
	CHEMBL5435869	196974	None	0	Human	Functional	pEC50	=	7.8	7.8	2	4	Agonist activity at MOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at MOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay	ChEMBL	1136	24	13	13	-0.8	CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C/C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1	10.1021/acs.jmedchem.3c02093
	71458063	79172	None	0	Human	Functional	pEC50	=	7.8	7.8	-1	2	Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	500	5	2	5	4.0	CO[C@@]12CC[C@@]3(C[C@@H]1CNC(=O)/C=C/c1ccc(C)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1021/jm070255o
	CHEMBL2113306	79172	None	0	Human	Functional	pEC50	=	7.8	7.8	-1	2	Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	500	5	2	5	4.0	CO[C@@]12CC[C@@]3(C[C@@H]1CNC(=O)/C=C/c1ccc(C)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1021/jm070255o
	715222	113947	None	9	Human	Functional	pEC50	=	6.8	6.8	2	3	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	322	1	0	3	4.6	Cc1nn(-c2ccc(Cl)cc2Cl)c2c1C(=O)CC(C)(C)C2	10.1016/j.bmc.2014.07.012
	CHEMBL3325713	113947	None	9	Human	Functional	pEC50	=	6.8	6.8	2	3	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	322	1	0	3	4.6	Cc1nn(-c2ccc(Cl)cc2Cl)c2c1C(=O)CC(C)(C)C2	10.1016/j.bmc.2014.07.012
	172440894	195049	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assay	ChEMBL	402	5	1	3	4.7	CN(C)C(CNC(=O)c1cc2ccccc2s1)c1ccc(Br)cc1	10.1016/j.ejmech.2022.114728
	CHEMBL5395529	195049	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assay	ChEMBL	402	5	1	3	4.7	CN(C)C(CNC(=O)c1cc2ccccc2s1)c1ccc(Br)cc1	10.1016/j.ejmech.2022.114728
	118725855	117244	None	0	Human	Functional	pEC50	=	6.8	6.8	-75	3	Agonist activity at human mu opioid receptor expressed in COS7 cells after 60 mins IP1 assayAgonist activity at human mu opioid receptor expressed in COS7 cells after 60 mins IP1 assay	ChEMBL	373	5	2	4	3.9	O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1cc2ccccc2[nH]1	10.1016/j.bmcl.2014.12.064
	CHEMBL3394005	117244	None	0	Human	Functional	pEC50	=	6.8	6.8	-75	3	Agonist activity at human mu opioid receptor expressed in COS7 cells after 60 mins IP1 assayAgonist activity at human mu opioid receptor expressed in COS7 cells after 60 mins IP1 assay	ChEMBL	373	5	2	4	3.9	O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1cc2ccccc2[nH]1	10.1016/j.bmcl.2014.12.064
	CHEMBL387670	214871	None	0	Rat	Functional	pEC50	=	6.8	6.8	-72	4	Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assayAgonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)N(C)C(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm061369n
	73212369	104526	None	0	Rat	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cells assessed as stimulation of [35S]-GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat mu opioid receptor expressed in rat C6 cells assessed as stimulation of [35S]-GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	395	7	2	4	2.7	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CCN(CCCc2ccccc2)CC1	10.1016/j.bmcl.2013.12.021
	CHEMBL3104108	104526	None	0	Rat	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cells assessed as stimulation of [35S]-GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat mu opioid receptor expressed in rat C6 cells assessed as stimulation of [35S]-GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	395	7	2	4	2.7	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CCN(CCCc2ccccc2)CC1	10.1016/j.bmcl.2013.12.021
	16037800	77257	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assayAgonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assay	ChEMBL	447	9	2	6	5.1	CCOc1ccc(Cc2nc3cc(NC(=N)c4cccs4)ccc3n2CCN(C)C)cc1	10.1021/ml200268w
	CHEMBL2079501	77257	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assayAgonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assay	ChEMBL	447	9	2	6	5.1	CCOc1ccc(Cc2nc3cc(NC(=N)c4cccs4)ccc3n2CCN(C)C)cc1	10.1021/ml200268w
	CHEMBL3217000	77257	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assayAgonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assay	ChEMBL	447	9	2	6	5.1	CCOc1ccc(Cc2nc3cc(NC(=N)c4cccs4)ccc3n2CCN(C)C)cc1	10.1021/ml200268w
	156016960	177860	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting methodAgonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method	ChEMBL	562	14	7	8	-0.1	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CN)NC(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1	10.1016/j.bmc.2020.115438
	CHEMBL4642698	177860	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting methodAgonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method	ChEMBL	562	14	7	8	-0.1	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CN)NC(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1	10.1016/j.bmc.2020.115438
	90207338	160071	None	0	Human	Functional	pEC50	=	4.8	4.8	-19	2	GTPgammaS Functional Assay (mu): [35S]GTPgammaS functional assays were conducted using freshly thawed pt-receptor membranes prepared in-house from a cell line expressing recombinant mu opioid receptor in a HEK-293, CHO cell background, or purchased from a commercial source (Perkin Elmer, Shelton, Conn.; or DiscovRx, Fremont, Calif.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2,20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B.GTPgammaS Functional Assay (mu): [35S]GTPgammaS functional assays were conducted using freshly thawed pt-receptor membranes prepared in-house from a cell line expressing recombinant mu opioid receptor in a HEK-293, CHO cell background, or purchased from a commercial source (Perkin Elmer, Shelton, Conn.; or DiscovRx, Fremont, Calif.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2,20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B.	ChEMBL	619	10	2	6	5.5	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](C(N[C@@H](C(N)=O)c1ccccc1)c1ccccc1)C2	nan
	CHEMBL4107606	160071	None	0	Human	Functional	pEC50	=	4.8	4.8	-19	2	GTPgammaS Functional Assay (mu): [35S]GTPgammaS functional assays were conducted using freshly thawed pt-receptor membranes prepared in-house from a cell line expressing recombinant mu opioid receptor in a HEK-293, CHO cell background, or purchased from a commercial source (Perkin Elmer, Shelton, Conn.; or DiscovRx, Fremont, Calif.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2,20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B.GTPgammaS Functional Assay (mu): [35S]GTPgammaS functional assays were conducted using freshly thawed pt-receptor membranes prepared in-house from a cell line expressing recombinant mu opioid receptor in a HEK-293, CHO cell background, or purchased from a commercial source (Perkin Elmer, Shelton, Conn.; or DiscovRx, Fremont, Calif.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2,20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B.	ChEMBL	619	10	2	6	5.5	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](C(N[C@@H](C(N)=O)c1ccccc1)c1ccccc1)C2	nan
	CHEMBL387670	214871	None	0	Rat	Functional	pEC50	=	6.8	6.8	-72	4	Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assayAgonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)N(C)C(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm061369n
	66826814	160599	None	0	Human	Functional	pEC50	=	5.8	5.8	-29	2	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	518	9	1	6	3.6	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CCC(N)=O)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2	nan
	CHEMBL4112155	160599	None	0	Human	Functional	pEC50	=	5.8	5.8	-29	2	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	518	9	1	6	3.6	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CCC(N)=O)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2	nan
	71764841	91439	None	0	Rat	Functional	pEC50	=	5.8	5.8	-1	2	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	778	9	9	11	-0.8	CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCN/C(N(C)C)=N\CCC[C@@H](C(N)=O)NC1=O	10.1021/jm4008592
	CHEMBL2402934	91439	None	0	Rat	Functional	pEC50	=	5.8	5.8	-1	2	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	778	9	9	11	-0.8	CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCN/C(N(C)C)=N\CCC[C@@H](C(N)=O)NC1=O	10.1021/jm4008592
	145974455	164744	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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 methodAgonist 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	ChEMBL	355	3	1	3	4.1	Cc1cc(Cl)ccc1CN1CCC(n2c(=O)[nH]c3ccccc32)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4216570	164744	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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 methodAgonist 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	ChEMBL	355	3	1	3	4.1	Cc1cc(Cl)ccc1CN1CCC(n2c(=O)[nH]c3ccccc32)CC1	10.1021/acs.jmedchem.8b01136
	145966109	164194	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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 methodAgonist 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	ChEMBL	471	3	1	3	5.4	O=c1[nH]c2c(Cl)cc(Cl)cc2n1C1CCN(Cc2ccc(Br)cc2F)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4209633	164194	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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 methodAgonist 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	ChEMBL	471	3	1	3	5.4	O=c1[nH]c2c(Cl)cc(Cl)cc2n1C1CCN(Cc2ccc(Br)cc2F)CC1	10.1021/acs.jmedchem.8b01136
	137541772	158947	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	286	3	2	2	2.8	CC1CCC(C(=O)NCC2NCCc3ccccc32)CC1	10.1016/j.ejmech.2016.09.003
	CHEMBL4094890	158947	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	286	3	2	2	2.8	CC1CCC(C(=O)NCC2NCCc3ccccc32)CC1	10.1016/j.ejmech.2016.09.003
	CHEMBL235743	212033	None	1	Rat	Functional	pEC50	=	6.8	6.8	7	4	Agonist activity at MOR in Wistar rat brain membranes after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at MOR in Wistar rat brain membranes after 60 mins by [35S]-GTPgammaS binding assay	ChEMBL		None	None	None		C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.ejmech.2019.05.037
	CHEMBL5084034	217383	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISAAgonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISA	ChEMBL		None	None	None		N=C(N)NCCC[C@@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.1c01631
	CHEMBL5094439	217985	None	0	Human	Functional	pEC50	=	6.8	6.8	-5	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis	ChEMBL		None	None	None		C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O	10.1021/acs.jmedchem.0c02062
	118711137	113952	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	376	1	0	3	5.4	CC1(C)CC(=O)c2c(C(F)(F)F)nn(-c3ccc(Cl)cc3Cl)c2C1	10.1016/j.bmc.2014.07.012
	CHEMBL3325718	113952	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	376	1	0	3	5.4	CC1(C)CC(=O)c2c(C(F)(F)F)nn(-c3ccc(Cl)cc3Cl)c2C1	10.1016/j.bmc.2014.07.012
	CHEMBL5091971	217826	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	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 assayAgonist 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	ChEMBL		None	None	None		CC[C@@H]1CN2CC[C@@]3(O)C(=Nc4c(-c5ccoc5)ccc(OC)c43)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.1c01273
	162649206	180089	None	0	Human	Functional	pEC50	=	5.8	5.8	-61	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1118	31	16	15	-3.4	N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.0c01367
	CHEMBL4746919	180089	None	0	Human	Functional	pEC50	=	5.8	5.8	-61	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1118	31	16	15	-3.4	N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.0c01367
	71764841	91439	None	0	Rat	Functional	pEC50	=	5.8	5.8	-1	2	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	778	9	9	11	-0.8	CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCN/C(N(C)C)=N\CCC[C@@H](C(N)=O)NC1=O	10.1021/jm4008592
	CHEMBL2402934	91439	None	0	Rat	Functional	pEC50	=	5.8	5.8	-1	2	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	778	9	9	11	-0.8	CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCN/C(N(C)C)=N\CCC[C@@H](C(N)=O)NC1=O	10.1021/jm4008592
	16190489	30604	None	5	Human	Functional	pEC50	=	4.8	4.8	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	439	7	0	6	4.6	CCOC(=O)C1(CC2CCCCO2)CCN(Cc2c(C)cc(C)cc2-n2cccn2)CC1	nan
	CHEMBL1393837	30604	None	5	Human	Functional	pEC50	=	4.8	4.8	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	439	7	0	6	4.6	CCOC(=O)C1(CC2CCCCO2)CCN(Cc2c(C)cc(C)cc2-n2cccn2)CC1	nan
	130431412	164816	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay	ChEMBL	453	3	1	3	5.2	O=c1[nH]c2cc(Cl)c(Cl)cc2n1C1CCN(Cc2ccc(Br)cc2)CC1	10.1021/acs.jmedchem.8b00435
	CHEMBL4217435	164816	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay	ChEMBL	453	3	1	3	5.2	O=c1[nH]c2cc(Cl)c(Cl)cc2n1C1CCN(Cc2ccc(Br)cc2)CC1	10.1021/acs.jmedchem.8b00435
	137657032	159684	None	0	Human	Functional	pEC50	=	6.8	6.8	-676	3	Agonist activity at human recombinant MOR expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant MOR expressed in CHO cells assessed as cAMP accumulation	ChEMBL	444	3	1	4	4.2	O=C(c1ccoc1)N1C[C@H]2CC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21	10.1016/j.bmcl.2017.05.072
	CHEMBL4103044	159684	None	0	Human	Functional	pEC50	=	6.8	6.8	-676	3	Agonist activity at human recombinant MOR expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant MOR expressed in CHO cells assessed as cAMP accumulation	ChEMBL	444	3	1	4	4.2	O=C(c1ccoc1)N1C[C@H]2CC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21	10.1016/j.bmcl.2017.05.072
	162649206	180089	None	0	Human	Functional	pEC50	=	5.8	5.8	-61	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1118	31	16	15	-3.4	N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.0c01367
	CHEMBL4746919	180089	None	0	Human	Functional	pEC50	=	5.8	5.8	-61	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1118	31	16	15	-3.4	N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.0c01367
	155514602	176445	None	0	Rat	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method	ChEMBL	431	9	4	4	4.2	CCNc1ccc(Cc2ccccc2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b00219
	CHEMBL4440903	176445	None	0	Rat	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method	ChEMBL	431	9	4	4	4.2	CCNc1ccc(Cc2ccccc2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b00219
	CHEMBL4595539	176445	None	0	Rat	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method	ChEMBL	431	9	4	4	4.2	CCNc1ccc(Cc2ccccc2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b00219
	CHEMBL5091971	217826	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	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 assayAgonist 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	ChEMBL		None	None	None		CC[C@@H]1CN2CC[C@@]3(O)C(=Nc4c(-c5ccoc5)ccc(OC)c43)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.1c01273
	76331525	103402	None	0	Human	Functional	pEC50	=	5.8	5.8	-109	2	Agonist activity at human mu opioid assessed as stimulation of GTPgammaS bindingAgonist activity at human mu opioid assessed as stimulation of GTPgammaS binding	ChEMBL	542	6	1	3	7.7	COC(=O)N[C@@]1(Cc2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl	10.1016/j.bmcl.2009.03.057
	CHEMBL3084558	103402	None	0	Human	Functional	pEC50	=	5.8	5.8	-109	2	Agonist activity at human mu opioid assessed as stimulation of GTPgammaS bindingAgonist activity at human mu opioid assessed as stimulation of GTPgammaS binding	ChEMBL	542	6	1	3	7.7	COC(=O)N[C@@]1(Cc2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl	10.1016/j.bmcl.2009.03.057
	3600177	59619	None	4	Human	Functional	pEC50	=	4.8	4.8	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	314	5	2	3	3.4	Cc1cccc(NC(S)=NCC(c2cccnc2)N(C)C)c1	nan
	CHEMBL1719184	59619	None	4	Human	Functional	pEC50	=	4.8	4.8	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	314	5	2	3	3.4	Cc1cccc(NC(S)=NCC(c2cccnc2)N(C)C)c1	nan
	124037294	160193	None	0	Human	Functional	pEC50	=	6.8	6.8	14	2	HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.	ChEMBL	537	16	2	10	1.3	COCCOCCOCCOCCOCCO[C@H]1CC[C@@]2(O)C3Cc4ccc(O)c5c4[C@@]2(CCN3C)[C@H]1O5	nan
	CHEMBL4108649	160193	None	0	Human	Functional	pEC50	=	6.8	6.8	14	2	HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.	ChEMBL	537	16	2	10	1.3	COCCOCCOCCOCCOCCO[C@H]1CC[C@@]2(O)C3Cc4ccc(O)c5c4[C@@]2(CCN3C)[C@H]1O5	nan
	851992	35732	None	4	Human	Functional	pEC50	=	4.8	4.8	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	340	3	0	4	3.5	Cn1c(CN2CCN(c3cccc(Cl)c3)CC2)nc2ccccc21	nan
	CHEMBL1440652	35732	None	4	Human	Functional	pEC50	=	4.8	4.8	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	340	3	0	4	3.5	Cn1c(CN2CCN(c3cccc(Cl)c3)CC2)nc2ccccc21	nan
	CHEMBL5077829	217006	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assay	ChEMBL		None	None	None		CCC(=O)N(CC1(N2CCN(Cc3ccccc3)CC2)CCCCC1)c1ccccc1	10.1021/acs.jmedchem.1c00417
	72735390	106374	None	0	Human	Functional	pEC50	=	6.8	6.8	-69	2	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay	ChEMBL	402	2	3	5	2.3	OCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13	10.1016/j.bmc.2013.10.032
	CHEMBL3139110	106374	None	0	Human	Functional	pEC50	=	6.8	6.8	-69	2	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay	ChEMBL	402	2	3	5	2.3	OCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13	10.1016/j.bmc.2013.10.032
	CHEMBL4296735	106374	None	0	Human	Functional	pEC50	=	6.8	6.8	-69	2	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay	ChEMBL	402	2	3	5	2.3	OCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13	10.1016/j.bmc.2013.10.032
	155516762	176481	None	0	Rat	Functional	pEC50	=	6.8	6.8	13	2	Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method	ChEMBL	416	8	3	3	4.7	CC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)c1cccc(Cc2ccccc2)c1	10.1021/acs.jmedchem.9b00219
	CHEMBL4443946	176481	None	0	Rat	Functional	pEC50	=	6.8	6.8	13	2	Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method	ChEMBL	416	8	3	3	4.7	CC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)c1cccc(Cc2ccccc2)c1	10.1021/acs.jmedchem.9b00219
	CHEMBL4595821	176481	None	0	Rat	Functional	pEC50	=	6.8	6.8	13	2	Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method	ChEMBL	416	8	3	3	4.7	CC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)c1cccc(Cc2ccccc2)c1	10.1021/acs.jmedchem.9b00219
	164916997	196206	None	0	Mouse	Functional	pEC50	=	6.8	6.8	-8	2	Partial 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 assayPartial 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	ChEMBL	592	10	0	4	6.3	CN(C)C(=O)C(CCN1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)C1)(c1ccccc1)c1ccccc1	10.1021/acs.jmedchem.3c00417
	CHEMBL5418819	196206	None	0	Mouse	Functional	pEC50	=	6.8	6.8	-8	2	Partial 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 assayPartial 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	ChEMBL	592	10	0	4	6.3	CN(C)C(=O)C(CCN1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)C1)(c1ccccc1)c1ccccc1	10.1021/acs.jmedchem.3c00417
	68314562	93189	None	3	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	400	6	1	3	5.8	c1ccc([C@]2(CCNCc3ccc4ccccc4c3)CCOC3(CCCC3)C2)nc1	10.1021/jm4010829
	CHEMBL2443253	93189	None	3	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	400	6	1	3	5.8	c1ccc([C@]2(CCNCc3ccc4ccccc4c3)CCOC3(CCCC3)C2)nc1	10.1021/jm4010829
	68314457	93209	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	351	6	1	4	4.0	c1ccc(CNCC[C@@]2(c3ccccn3)CCOC3(CCCC3)C2)nc1	10.1021/jm4010829
	CHEMBL2443273	93209	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	351	6	1	4	4.0	c1ccc(CNCC[C@@]2(c3ccccn3)CCOC3(CCCC3)C2)nc1	10.1021/jm4010829
	164916997	196206	None	0	Mouse	Functional	pEC50	=	6.8	6.8	-8	2	Partial 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 assayPartial 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	ChEMBL	592	10	0	4	6.3	CN(C)C(=O)C(CCN1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)C1)(c1ccccc1)c1ccccc1	10.1021/acs.jmedchem.3c00417
	CHEMBL5418819	196206	None	0	Mouse	Functional	pEC50	=	6.8	6.8	-8	2	Partial 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 assayPartial 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	ChEMBL	592	10	0	4	6.3	CN(C)C(=O)C(CCN1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)C1)(c1ccccc1)c1ccccc1	10.1021/acs.jmedchem.3c00417
	168475887	195235	None	2	Mouse	Functional	pEC50	=	5.8	5.8	-10	2	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 assayAgonist 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	ChEMBL	419	5	0	4	4.6	Clc1cccc(N2CCN(CCC3(c4ccccn4)CCOCC3)CC2)c1Cl	10.1021/acs.jmedchem.3c00417
	CHEMBL5399270	195235	None	2	Mouse	Functional	pEC50	=	5.8	5.8	-10	2	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 assayAgonist 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	ChEMBL	419	5	0	4	4.6	Clc1cccc(N2CCN(CCC3(c4ccccn4)CCOCC3)CC2)c1Cl	10.1021/acs.jmedchem.3c00417
	68314329	93219	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	341	6	1	2	4.8	CC1(C)CC(CCNCc2ccccc2)(c2ccc(F)cc2)CCO1	10.1021/jm4010829
	CHEMBL2443283	93219	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	341	6	1	2	4.8	CC1(C)CC(CCNCc2ccccc2)(c2ccc(F)cc2)CCO1	10.1021/jm4010829
	155520785	170612	None	0	Human	Functional	pEC50	=	5.8	5.8	-6	4	Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 minsAgonist activity at mu-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins	ChEMBL	1165	30	12	11	2.7	N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O	10.1016/j.bmc.2019.01.003
	CHEMBL4449491	170612	None	0	Human	Functional	pEC50	=	5.8	5.8	-6	4	Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 minsAgonist activity at mu-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins	ChEMBL	1165	30	12	11	2.7	N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O	10.1016/j.bmc.2019.01.003
	168475887	195235	None	2	Mouse	Functional	pEC50	=	5.8	5.8	-10	2	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 assayAgonist 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	ChEMBL	419	5	0	4	4.6	Clc1cccc(N2CCN(CCC3(c4ccccn4)CCOCC3)CC2)c1Cl	10.1021/acs.jmedchem.3c00417
	CHEMBL5399270	195235	None	2	Mouse	Functional	pEC50	=	5.8	5.8	-10	2	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 assayAgonist 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	ChEMBL	419	5	0	4	4.6	Clc1cccc(N2CCN(CCC3(c4ccccn4)CCOCC3)CC2)c1Cl	10.1021/acs.jmedchem.3c00417
	66829005	160535	None	0	Human	Functional	pEC50	=	6.8	6.8	-1	2	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	549	8	0	6	4.5	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CS(=O)(=O)Cc1ccccc1)C2	nan
	CHEMBL4111594	160535	None	0	Human	Functional	pEC50	=	6.8	6.8	-1	2	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	549	8	0	6	4.5	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CS(=O)(=O)Cc1ccccc1)C2	nan
	136260442	91444	None	0	Rat	Functional	pEC50	=	5.8	5.8	-1	3	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	595	7	9	10	-3.3	CN/C1=N/C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CN1	10.1021/jm4008592
	CHEMBL2402939	91444	None	0	Rat	Functional	pEC50	=	5.8	5.8	-1	3	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	595	7	9	10	-3.3	CN/C1=N/C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CN1	10.1021/jm4008592
	145965998	164411	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	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 methodAgonist 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	ChEMBL	369	4	1	3	4.8	CCC(c1ccc(Cl)cc1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4212298	164411	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	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 methodAgonist 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	ChEMBL	369	4	1	3	4.8	CCC(c1ccc(Cl)cc1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1	10.1021/acs.jmedchem.8b01136
	145984702	165591	None	0	Rat	Functional	pEC50	=	5.8	5.8	-1	3	Agonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis	ChEMBL	499	6	0	5	5.2	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@](C)(C(=O)c1ccccc1)C2	10.1016/j.bmc.2018.07.020
	CHEMBL4240426	165591	None	0	Rat	Functional	pEC50	=	5.8	5.8	-1	3	Agonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis	ChEMBL	499	6	0	5	5.2	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@](C)(C(=O)c1ccccc1)C2	10.1016/j.bmc.2018.07.020
	46227963	14181	None	0	Human	Functional	pEC50	=	7.8	7.8	-3	4	Activity at mu opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at mu opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	514	4	3	5	3.8	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(C(F)(F)F)cc1	10.1016/j.bmc.2009.07.069
	CHEMBL1198701	14181	None	0	Human	Functional	pEC50	=	7.8	7.8	-3	4	Activity at mu opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at mu opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	514	4	3	5	3.8	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(C(F)(F)F)cc1	10.1016/j.bmc.2009.07.069
	CHEMBL611929	14181	None	0	Human	Functional	pEC50	=	7.8	7.8	-3	4	Activity at mu opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at mu opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	514	4	3	5	3.8	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(C(F)(F)F)cc1	10.1016/j.bmc.2009.07.069
	118562584	170696	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	364	4	0	3	3.5	C[C@H]1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccc2)C1=O	10.1021/acs.jmedchem.9b01256
	CHEMBL4450665	170696	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	364	4	0	3	3.5	C[C@H]1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccc2)C1=O	10.1021/acs.jmedchem.9b01256
	162655458	180883	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	352	4	0	3	2.6	CCN1CC2(CCN(CCc3c(F)cccc3F)CC2)O[C@H](C)C1=O	10.1021/acs.jmedchem.0c01127
	CHEMBL4756310	180883	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	352	4	0	3	2.6	CCN1CC2(CCN(CCc3c(F)cccc3F)CC2)O[C@H](C)C1=O	10.1021/acs.jmedchem.0c01127
	16048866	94224	None	0	Human	Functional	pEC50	=	7.8	7.8	1	3	Agonist activity at human mu opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assay	ChEMBL	480	6	1	2	5.4	C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(Br)cc4)cc3[C@@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2007.09.082
	CHEMBL249567	94224	None	0	Human	Functional	pEC50	=	7.8	7.8	1	3	Agonist activity at human mu opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assay	ChEMBL	480	6	1	2	5.4	C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(Br)cc4)cc3[C@@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2007.09.082
	60561198	164905	None	5	Human	Functional	pEC50	=	7.8	7.8	-	1	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 methodAgonist 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	ChEMBL	355	3	1	3	4.4	CC(c1ccc(Cl)cc1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4218547	164905	None	5	Human	Functional	pEC50	=	7.8	7.8	-	1	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 methodAgonist 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	ChEMBL	355	3	1	3	4.4	CC(c1ccc(Cl)cc1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1	10.1021/acs.jmedchem.8b01136
	1639	2726	None	32	Human	Functional	pEC50	=	7.8	7.8	-4	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1016/j.bmcl.2009.02.078
	1765	2726	None	32	Human	Functional	pEC50	=	7.8	7.8	-4	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1016/j.bmcl.2009.02.078
	5360515	2726	None	32	Human	Functional	pEC50	=	7.8	7.8	-4	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1016/j.bmcl.2009.02.078
	5360515.0	2726	None	32	Human	Functional	pEC50	=	7.8	7.8	-4	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1016/j.bmcl.2009.02.078
	CHEMBL19019	2726	None	32	Human	Functional	pEC50	=	7.8	7.8	-4	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1016/j.bmcl.2009.02.078
	DB00704	2726	None	32	Human	Functional	pEC50	=	7.8	7.8	-4	9	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	341	2	2	5	1.5	O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O	10.1016/j.bmcl.2009.02.078
	23634920	88540	None	0	Rat	Functional	pEC50	=	7.8	7.8	1	3	Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay	ChEMBL	756	18	8	9	0.4	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)CCC(=O)NC1CCN(CCc2ccccc2)CC1	10.1021/jm061465o
	CHEMBL235107	88540	None	0	Rat	Functional	pEC50	=	7.8	7.8	1	3	Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay	ChEMBL	756	18	8	9	0.4	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)CCC(=O)NC1CCN(CCc2ccccc2)CC1	10.1021/jm061465o
	CHEMBL26575	213121	None	0	Rat	Functional	pEC50	=	7.8	7.8	-158	4	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 assayAgonist 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	ChEMBL		None	None	None		CC(C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)NCC(=O)O)C(C)C	10.1016/j.bmcl.2018.05.015
	23634920	88540	None	0	Rat	Functional	pEC50	=	7.8	7.8	1	3	Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay	ChEMBL	756	18	8	9	0.4	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)CCC(=O)NC1CCN(CCc2ccccc2)CC1	10.1021/jm061465o
	CHEMBL235107	88540	None	0	Rat	Functional	pEC50	=	7.8	7.8	1	3	Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay	ChEMBL	756	18	8	9	0.4	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)CCC(=O)NC1CCN(CCc2ccccc2)CC1	10.1021/jm061465o
	44323614	168110	None	0	Rat	Functional	pEC50	=	7.8	7.8	-	1	Compound was tested for its ability to stimulate [35S]GTP-gamma-S, binding to membranes from C6 glioma cells stably expressing rat mu opioid receptorCompound was tested for its ability to stimulate [35S]GTP-gamma-S, binding to membranes from C6 glioma cells stably expressing rat mu opioid receptor	ChEMBL	429	6	4	4	4.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NC1CCNc2ccc(Cc3ccccc3)cc21	10.1016/s0960-894x(98)00472-7
	CHEMBL432045	168110	None	0	Rat	Functional	pEC50	=	7.8	7.8	-	1	Compound was tested for its ability to stimulate [35S]GTP-gamma-S, binding to membranes from C6 glioma cells stably expressing rat mu opioid receptorCompound was tested for its ability to stimulate [35S]GTP-gamma-S, binding to membranes from C6 glioma cells stably expressing rat mu opioid receptor	ChEMBL	429	6	4	4	4.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NC1CCNc2ccc(Cc3ccccc3)cc21	10.1016/s0960-894x(98)00472-7
	172439216	195376	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	351	6	0	3	4.1	CCC(=O)N(CC(C)N1CCC(c2ccccc2)CC1)c1ccccn1	10.1021/acs.jmedchem.3c01637
	CHEMBL5402310	195376	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	351	6	0	3	4.1	CCC(=O)N(CC(C)N1CCC(c2ccccc2)CC1)c1ccccn1	10.1021/acs.jmedchem.3c01637
	155569411	176766	None	0	Human	Functional	pEC50	=	7.8	7.8	-3	2	Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	461	11	4	5	3.9	CCOc1ccc(CNCc2ccccc2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b01818
	CHEMBL4592669	176766	None	0	Human	Functional	pEC50	=	7.8	7.8	-3	2	Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	461	11	4	5	3.9	CCOc1ccc(CNCc2ccccc2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b01818
	CHEMBL4598103	176766	None	0	Human	Functional	pEC50	=	7.8	7.8	-3	2	Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	461	11	4	5	3.9	CCOc1ccc(CNCc2ccccc2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b01818
	72735567	106394	None	0	Human	Functional	pEC50	=	7.8	7.8	-10	2	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay	ChEMBL	416	2	3	5	2.7	C[C@H](O)CN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13	10.1016/j.bmc.2013.10.032
	CHEMBL3139175	106394	None	0	Human	Functional	pEC50	=	7.8	7.8	-10	2	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay	ChEMBL	416	2	3	5	2.7	C[C@H](O)CN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13	10.1016/j.bmc.2013.10.032
	CHEMBL4296732	106394	None	0	Human	Functional	pEC50	=	7.8	7.8	-10	2	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay	ChEMBL	416	2	3	5	2.7	C[C@H](O)CN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13	10.1016/j.bmc.2013.10.032
	137541796	158827	None	0	Human	Functional	pEC50	=	6.8	6.8	1	2	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	336	6	1	2	4.1	CCCCN1CCc2ccccc2C1CNC(=O)c1ccc(C)cc1	10.1016/j.ejmech.2016.09.003
	CHEMBL4093524	158827	None	0	Human	Functional	pEC50	=	6.8	6.8	1	2	Agonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assayAgonist activity at human MOR expressed in CHO-K1 cells co-expressing Galpha 15 assessed as increase in intracellular calcium release incubated for 1 measured every 1.52 secs for 90 secs by FLIPR assay	ChEMBL	336	6	1	2	4.1	CCCCN1CCc2ccccc2C1CNC(=O)c1ccc(C)cc1	10.1016/j.ejmech.2016.09.003
	71450925	79160	None	0	Human	Functional	pEC50	=	6.8	6.8	1	2	Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	500	6	1	5	4.0	COc1ccc2c3c1O[C@H]1[C@]4(OC)CC[C@@]5(C[C@@H]4CNC(=O)/C=C/c4ccccc4)[C@@H](C2)N(C)CC[C@]315	10.1021/jm070255o
	CHEMBL2113294	79160	None	0	Human	Functional	pEC50	=	6.8	6.8	1	2	Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	500	6	1	5	4.0	COc1ccc2c3c1O[C@H]1[C@]4(OC)CC[C@@]5(C[C@@H]4CNC(=O)/C=C/c4ccccc4)[C@@H](C2)N(C)CC[C@]315	10.1021/jm070255o
	5284603	205871	None	8	Mouse	Functional	pEC50	=	6.8	6.8	-1	6	Agonist activity at mouse MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assayAgonist activity at mouse MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay	ChEMBL	315	1	1	5	1.0	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(O)[C@@H](C2)N(C)CC[C@]314	10.1016/j.bmcl.2013.06.084
	CHEMBL656	205871	None	8	Mouse	Functional	pEC50	=	6.8	6.8	-1	6	Agonist activity at mouse MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assayAgonist activity at mouse MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay	ChEMBL	315	1	1	5	1.0	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(O)[C@@H](C2)N(C)CC[C@]314	10.1016/j.bmcl.2013.06.084
	CHEMBL5080666	217188	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISAAgonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISA	ChEMBL		None	None	None		N=C(N)NCCC[C@@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.1c01631
	71819402	92085	None	0	Human	Functional	pEC50	=	4.8	4.8	-3	4	Agonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assayAgonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay	ChEMBL	331	2	1	5	1.4	COc1ccc2c3c1O[C@H]1[C@@H](O)[C@H](OC)C[C@H]4[C@@H](C2)N(C)CC[C@]314	10.1016/j.bmcl.2013.06.084
	CHEMBL2418740	92085	None	0	Human	Functional	pEC50	=	4.8	4.8	-3	4	Agonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assayAgonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay	ChEMBL	331	2	1	5	1.4	COc1ccc2c3c1O[C@H]1[C@@H](O)[C@H](OC)C[C@H]4[C@@H](C2)N(C)CC[C@]314	10.1016/j.bmcl.2013.06.084
	71819403	92086	None	0	Human	Functional	pEC50	=	4.8	4.8	-2	3	Agonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assayAgonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay	ChEMBL	317	1	2	5	0.7	COc1ccc2c3c1O[C@H]1[C@@H](O)[C@H](O)C[C@H]4[C@@H](C2)N(C)CC[C@]314	10.1016/j.bmcl.2013.06.084
	CHEMBL2418741	92086	None	0	Human	Functional	pEC50	=	4.8	4.8	-2	3	Agonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assayAgonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay	ChEMBL	317	1	2	5	0.7	COc1ccc2c3c1O[C@H]1[C@@H](O)[C@H](O)C[C@H]4[C@@H](C2)N(C)CC[C@]314	10.1016/j.bmcl.2013.06.084
	457967	173286	None	1	Human	Functional	pEC50	=	4.8	4.8	-16	2	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cells by [35S]-GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cells by [35S]-GTPgammaS binding assay	ChEMBL	296	1	2	2	3.6	CCC1CC2CC3c4[nH]c5ccc(O)cc5c4CCN(C2)C13	10.1016/j.ejmech.2019.111701
	CHEMBL4522339	173286	None	1	Human	Functional	pEC50	=	4.8	4.8	-16	2	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cells by [35S]-GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cells by [35S]-GTPgammaS binding assay	ChEMBL	296	1	2	2	3.6	CCC1CC2CC3c4[nH]c5ccc(O)cc5c4CCN(C2)C13	10.1016/j.ejmech.2019.111701
	156012397	177536	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting methodAgonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method	ChEMBL	615	15	8	8	0.8	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCN)NC(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1	10.1016/j.bmc.2020.115438
	CHEMBL4638662	177536	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting methodAgonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method	ChEMBL	615	15	8	8	0.8	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCN)NC(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1	10.1016/j.bmc.2020.115438
	10255149	166412	None	0	Human	Functional	pEC50	=	6.8	6.8	-7	3	Agonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay	ChEMBL	493	6	3	4	4.0	Cc1cc(C(N)=O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1	10.1016/j.bmcl.2012.05.042
	CHEMBL427214	166412	None	0	Human	Functional	pEC50	=	6.8	6.8	-7	3	Agonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay	ChEMBL	493	6	3	4	4.0	Cc1cc(C(N)=O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1	10.1016/j.bmcl.2012.05.042
	43843657	195074	None	7	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assay	ChEMBL	372	5	1	3	4.9	Cc1ccc2c(Cl)c(C(=O)NCC(c3ccccc3)N(C)C)sc2c1	10.1016/j.ejmech.2022.114728
	CHEMBL5396293	195074	None	7	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assay	ChEMBL	372	5	1	3	4.9	Cc1ccc2c(Cl)c(C(=O)NCC(c3ccccc3)N(C)C)sc2c1	10.1016/j.ejmech.2022.114728
	24735749	164329	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	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 methodAgonist 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	ChEMBL	391	4	1	4	4.1	O=c1[nH]c2ccccc2n1C1CCN(Cc2cccc(OC(F)(F)F)c2)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4211156	164329	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	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 methodAgonist 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	ChEMBL	391	4	1	4	4.1	O=c1[nH]c2ccccc2n1C1CCN(Cc2cccc(OC(F)(F)F)c2)CC1	10.1021/acs.jmedchem.8b01136
	136260442	91444	None	0	Rat	Functional	pEC50	=	5.8	5.8	-1	3	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	595	7	9	10	-3.3	CN/C1=N/C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CN1	10.1021/jm4008592
	CHEMBL2402939	91444	None	0	Rat	Functional	pEC50	=	5.8	5.8	-1	3	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	595	7	9	10	-3.3	CN/C1=N/C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CN1	10.1021/jm4008592
	102270007	112922	None	0	Human	Functional	pEC50	=	6.8	6.8	-13	2	Agonist activity at human recombinant mu opioid receptor expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	412	2	3	6	0.9	CN1C(=O)[C@H](CCO)CC2=C1[C@@H]1Oc3c(O)ccc4c3[C@@]13CCN(C)[C@H](C4)[C@]3(O)C2	10.1016/j.bmc.2014.05.065
	CHEMBL3309508	112922	None	0	Human	Functional	pEC50	=	6.8	6.8	-13	2	Agonist activity at human recombinant mu opioid receptor expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	412	2	3	6	0.9	CN1C(=O)[C@H](CCO)CC2=C1[C@@H]1Oc3c(O)ccc4c3[C@@]13CCN(C)[C@H](C4)[C@]3(O)C2	10.1016/j.bmc.2014.05.065
	71459949	79167	None	0	Human	Functional	pEC50	=	6.8	6.8	3	2	Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	530	7	1	6	4.0	COc1ccccc1/C=C/C(=O)NC[C@H]1C[C@@]23CC[C@@]1(OC)[C@@H]1Oc4c(OC)ccc5c4[C@@]12CCN(C)[C@@H]3C5	10.1021/jm070255o
	CHEMBL2113301	79167	None	0	Human	Functional	pEC50	=	6.8	6.8	3	2	Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	530	7	1	6	4.0	COc1ccccc1/C=C/C(=O)NC[C@H]1C[C@@]23CC[C@@]1(OC)[C@@H]1Oc4c(OC)ccc5c4[C@@]12CCN(C)[C@@H]3C5	10.1021/jm070255o
	156010475	177182	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting methodAgonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method	ChEMBL	672	17	9	8	0.9	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1	10.1016/j.bmc.2020.115438
	CHEMBL4633024	177182	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting methodAgonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method	ChEMBL	672	17	9	8	0.9	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1	10.1016/j.bmc.2020.115438
	145986165	165633	None	0	Rat	Functional	pEC50	=	6.8	6.8	1	3	Agonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis	ChEMBL	567	6	0	5	6.2	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@](C)(C(=O)c1ccc(C(F)(F)F)cc1)C2	10.1016/j.bmc.2018.07.020
	CHEMBL4241369	165633	None	0	Rat	Functional	pEC50	=	6.8	6.8	1	3	Agonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis	ChEMBL	567	6	0	5	6.2	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@](C)(C(=O)c1ccc(C(F)(F)F)cc1)C2	10.1016/j.bmc.2018.07.020
	145965538	164417	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	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 assayAgonist 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	ChEMBL	359	3	1	3	4.0	O=c1[nH]c2cc(F)ccc2n1C1CCN(Cc2ccccc2Cl)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4212370	164417	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	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 assayAgonist 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	ChEMBL	359	3	1	3	4.0	O=c1[nH]c2cc(F)ccc2n1C1CCN(Cc2ccccc2Cl)CC1	10.1021/acs.jmedchem.8b01136
	44337839	108630	None	0	Human	Functional	pEC50	=	5.8	5.8	-7	3	Effective concentration agonistic activity towards Opioid receptor mu 1Effective concentration agonistic activity towards Opioid receptor mu 1	ChEMBL	426	1	2	3	5.1	C/C=C1\C[C@@]23Cc4c([nH]c5ccccc45)[C@@H]1[C@@]21CCN(C)C3Cc2ccc(OC)c(O)c21	10.1021/jm030801n
	CHEMBL320306	108630	None	0	Human	Functional	pEC50	=	5.8	5.8	-7	3	Effective concentration agonistic activity towards Opioid receptor mu 1Effective concentration agonistic activity towards Opioid receptor mu 1	ChEMBL	426	1	2	3	5.1	C/C=C1\C[C@@]23Cc4c([nH]c5ccccc45)[C@@H]1[C@@]21CCN(C)C3Cc2ccc(OC)c(O)c21	10.1021/jm030801n
	172460655	196515	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	363	6	0	3	4.1	CC(CN(C(=O)C1CC1)c1ccccn1)N1CCC(c2ccccc2)CC1	10.1021/acs.jmedchem.3c01637
	CHEMBL5425711	196515	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	363	6	0	3	4.1	CC(CN(C(=O)C1CC1)c1ccccn1)N1CCC(c2ccccc2)CC1	10.1021/acs.jmedchem.3c01637
	CHEMBL5085013	217432	None	0	Human	Functional	pEC50	=	6.8	6.8	-2	4	Agonist activity at MOR (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 assayAgonist activity at MOR (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	ChEMBL		None	None	None		CN1C(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCCNC(=O)C[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1	10.1021/acs.jmedchem.1c00694
	CHEMBL5085090	217437	None	0	Human	Functional	pEC50	=	6.8	6.8	1	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis	ChEMBL		None	None	None		C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O	10.1021/acs.jmedchem.0c02062
	1623	1560	None	36	Rat	Functional	pEC50	=	6.8	6.8	2	6	Agonist activity at mu opioid receptor in rat brain membrane by [35S]GTPgammaS binding assayAgonist activity at mu opioid receptor in rat brain membrane by [35S]GTPgammaS binding assay	ChEMBL		None	None	None		None	10.1021/jm101515v
	5311080	1560	None	36	Rat	Functional	pEC50	=	6.8	6.8	2	6	Agonist activity at mu opioid receptor in rat brain membrane by [35S]GTPgammaS binding assayAgonist activity at mu opioid receptor in rat brain membrane by [35S]GTPgammaS binding assay	ChEMBL		None	None	None		None	10.1021/jm101515v
	CHEMBL316446	1560	None	36	Rat	Functional	pEC50	=	6.8	6.8	2	6	Agonist activity at mu opioid receptor in rat brain membrane by [35S]GTPgammaS binding assayAgonist activity at mu opioid receptor in rat brain membrane by [35S]GTPgammaS binding assay	ChEMBL		None	None	None		None	10.1021/jm101515v
	CHEMBL5085013	217432	None	0	Human	Functional	pEC50	=	6.8	6.8	-2	4	Agonist activity at MOR (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 assayAgonist activity at MOR (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	ChEMBL		None	None	None		CN1C(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCCNC(=O)C[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1	10.1021/acs.jmedchem.1c00694
	24854100	96195	None	0	Human	Functional	pEC50	=	5.8	5.8	2	2	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	524	5	0	9	4.3	COC(=O)[C@@H]1C[C@H](OC(=O)c2cccc(OC)c2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@]21C	10.1021/jm701162g
	CHEMBL260485	96195	None	0	Human	Functional	pEC50	=	5.8	5.8	2	2	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	524	5	0	9	4.3	COC(=O)[C@@H]1C[C@H](OC(=O)c2cccc(OC)c2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@]21C	10.1021/jm701162g
	145973500	164738	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	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 assayAgonist 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	ChEMBL	405	4	1	4	4.6	CC(c1ccc(OC(F)(F)F)cc1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4216374	164738	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	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 assayAgonist 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	ChEMBL	405	4	1	4	4.6	CC(c1ccc(OC(F)(F)F)cc1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL5094675	217999	None	0	Human	Functional	pEC50	=	6.8	6.8	-1	5	Agonist activity at MOR (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 assayAgonist activity at MOR (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	ChEMBL		None	None	None		CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1	10.1021/acs.jmedchem.1c00694
	155559679	176535	None	0	Human	Functional	pEC50	=	6.8	6.8	8	2	Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	425	9	3	5	3.2	CCOc1ccc(CN2CCCC2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b01818
	CHEMBL4564309	176535	None	0	Human	Functional	pEC50	=	6.8	6.8	8	2	Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	425	9	3	5	3.2	CCOc1ccc(CN2CCCC2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b01818
	CHEMBL4596196	176535	None	0	Human	Functional	pEC50	=	6.8	6.8	8	2	Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	425	9	3	5	3.2	CCOc1ccc(CN2CCCC2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C	10.1021/acs.jmedchem.9b01818
	24854180	96138	None	0	Human	Functional	pEC50	=	5.8	5.8	-1	2	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	534	4	0	9	5.0	COC(=O)[C@@H]1C[C@H](OC(=O)c2cc3ccccc3o2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@]21C	10.1021/jm701162g
	CHEMBL260121	96138	None	0	Human	Functional	pEC50	=	5.8	5.8	-1	2	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	534	4	0	9	5.0	COC(=O)[C@@H]1C[C@H](OC(=O)c2cc3ccccc3o2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@]21C	10.1021/jm701162g
	CHEMBL5094675	217999	None	0	Human	Functional	pEC50	=	6.8	6.8	-1	5	Agonist activity at MOR (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 assayAgonist activity at MOR (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	ChEMBL		None	None	None		CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1	10.1021/acs.jmedchem.1c00694
	162659824	181316	None	0	Human	Functional	pEC50	=	6.8	6.8	1	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1118	31	16	15	-3.4	N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.0c01367
	CHEMBL4761246	181316	None	0	Human	Functional	pEC50	=	6.8	6.8	1	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1118	31	16	15	-3.4	N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.0c01367
	46227361	205040	None	0	Rat	Functional	pEC50	=	6.8	6.8	-138	5	Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	1210	18	10	12	4.6	CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1016/j.bmc.2009.08.035
	CHEMBL611925	205040	None	0	Rat	Functional	pEC50	=	6.8	6.8	-138	5	Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	1210	18	10	12	4.6	CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1016/j.bmc.2009.08.035
	44574586	189432	None	0	Human	Functional	pEC50	=	5.8	5.8	-33	2	Agonist activity at human mu opioid assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human mu opioid assessed as stimulation of GDP-induced [35S]GTPgammaS binding	ChEMBL	453	4	1	4	5.7	Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(c2ccncn2)C3)c(Cl)c1	10.1016/j.bmcl.2009.03.031
	CHEMBL512411	189432	None	0	Human	Functional	pEC50	=	5.8	5.8	-33	2	Agonist activity at human mu opioid assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human mu opioid assessed as stimulation of GDP-induced [35S]GTPgammaS binding	ChEMBL	453	4	1	4	5.7	Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(c2ccncn2)C3)c(Cl)c1	10.1016/j.bmcl.2009.03.031
	16100406	83256	None	0	Rat	Functional	pEC50	=	7.8	7.8	-6	5	Activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	1132	28	13	13	1.7	CCCC[C@@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](Cc1cc2ccccc2[nH]1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm061268p
	CHEMBL218600	83256	None	0	Rat	Functional	pEC50	=	7.8	7.8	-6	5	Activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	1132	28	13	13	1.7	CCCC[C@@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](Cc1cc2ccccc2[nH]1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm061268p
	2724431	174934	None	20	Human	Functional	pEC50	=	7.8	7.8	17	2	Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay	ChEMBL	290	4	1	4	1.7	CCC(=O)N(c1ccccc1)C1(C(=O)OC)CCNCC1	10.1021/acsmedchemlett.9b00404
	CHEMBL4562635	174934	None	20	Human	Functional	pEC50	=	7.8	7.8	17	2	Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay	ChEMBL	290	4	1	4	1.7	CCC(=O)N(c1ccccc1)C1(C(=O)OC)CCNCC1	10.1021/acsmedchemlett.9b00404
	5284603	205871	None	8	Human	Functional	pEC50	=	7.8	7.8	-19	6	Agonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assay	ChEMBL	315	1	1	5	1.0	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(O)[C@@H](C2)N(C)CC[C@]314	10.1021/acs.jmedchem.1c00417
	CHEMBL656	205871	None	8	Human	Functional	pEC50	=	7.8	7.8	-19	6	Agonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assay	ChEMBL	315	1	1	5	1.0	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(O)[C@@H](C2)N(C)CC[C@]314	10.1021/acs.jmedchem.1c00417
	5284603	205871	None	8	Human	Functional	pEC50	=	7.8	7.8	-19	6	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	315	1	1	5	1.0	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(O)[C@@H](C2)N(C)CC[C@]314	10.1021/acs.jmedchem.0c01127
	5284603	205871	None	8	Human	Functional	pEC50	=	7.8	7.8	-19	6	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	315	1	1	5	1.0	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(O)[C@@H](C2)N(C)CC[C@]314	10.1021/acs.jmedchem.9b01256
	CHEMBL656	205871	None	8	Human	Functional	pEC50	=	7.8	7.8	-19	6	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	315	1	1	5	1.0	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(O)[C@@H](C2)N(C)CC[C@]314	10.1021/acs.jmedchem.0c01127
	CHEMBL656	205871	None	8	Human	Functional	pEC50	=	7.8	7.8	-19	6	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	315	1	1	5	1.0	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(O)[C@@H](C2)N(C)CC[C@]314	10.1021/acs.jmedchem.9b01256
	53318823	58982	None	0	Rat	Functional	pEC50	=	7.8	7.8	-	1	Agonist activity at mu opioid receptor in rat brain membrane by [35S]GTPgammaS binding assayAgonist activity at mu opioid receptor in rat brain membrane by [35S]GTPgammaS binding assay	ChEMBL	641	13	6	6	3.1	Cc1cc(CC(N)C(=O)N[C@@H]2CCCC[C@@H]2C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(N)=O)[C@@H](C)c2ccccc2)cc(C)c1O	10.1021/jm101515v
	CHEMBL1689548	58982	None	0	Rat	Functional	pEC50	=	7.8	7.8	-	1	Agonist activity at mu opioid receptor in rat brain membrane by [35S]GTPgammaS binding assayAgonist activity at mu opioid receptor in rat brain membrane by [35S]GTPgammaS binding assay	ChEMBL	641	13	6	6	3.1	Cc1cc(CC(N)C(=O)N[C@@H]2CCCC[C@@H]2C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(N)=O)[C@@H](C)c2ccccc2)cc(C)c1O	10.1021/jm101515v
	1164	1630	None	10	Human	Functional	pEC50	=	7.8	7.8	-1	13	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.0c01367
	1626	1630	None	10	Human	Functional	pEC50	=	7.8	7.8	-1	13	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.0c01367
	3345	1630	None	10	Human	Functional	pEC50	=	7.8	7.8	-1	13	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.0c01367
	3345.0	1630	None	10	Human	Functional	pEC50	=	7.8	7.8	-1	13	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.0c01367
	CHEMBL596	1630	None	10	Human	Functional	pEC50	=	7.8	7.8	-1	13	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.0c01367
	DB00813	1630	None	10	Human	Functional	pEC50	=	7.8	7.8	-1	13	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.0c01367
	1164	1630	None	10	Human	Functional	pEC50	=	7.8	7.8	-1	13	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.0c01367
	1626	1630	None	10	Human	Functional	pEC50	=	7.8	7.8	-1	13	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.0c01367
	3345	1630	None	10	Human	Functional	pEC50	=	7.8	7.8	-1	13	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.0c01367
	3345.0	1630	None	10	Human	Functional	pEC50	=	7.8	7.8	-1	13	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.0c01367
	CHEMBL596	1630	None	10	Human	Functional	pEC50	=	7.8	7.8	-1	13	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.0c01367
	DB00813	1630	None	10	Human	Functional	pEC50	=	7.8	7.8	-1	13	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1021/acs.jmedchem.0c01367
	156020668	178124	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	576	8	1	8	5.5	Cc1nnc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)o1	10.1021/acs.jmedchem.0c00503
	CHEMBL4646678	178124	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	576	8	1	8	5.5	Cc1nnc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)o1	10.1021/acs.jmedchem.0c00503
	155536594	176472	None	0	Human	Functional	pEC50	=	7.8	7.8	-48	3	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	932	12	12	12	-1.3	N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1C/C=C/C[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O	10.1021/acsmedchemlett.8b00495
	CHEMBL4473857	176472	None	0	Human	Functional	pEC50	=	7.8	7.8	-48	3	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	932	12	12	12	-1.3	N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1C/C=C/C[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O	10.1021/acsmedchemlett.8b00495
	CHEMBL4595743	176472	None	0	Human	Functional	pEC50	=	7.8	7.8	-48	3	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	932	12	12	12	-1.3	N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1C/C=C/C[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O	10.1021/acsmedchemlett.8b00495
	CHEMBL382349	214762	None	0	Rat	Functional	pEC50	=	7.8	7.8	-14	5	Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm050921q
	44233185	194934	None	0	Rat	Functional	pEC50	=	7.8	7.8	-97	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assayAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay	ChEMBL	1327	29	14	16	1.1	CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1021/jm900473p
	CHEMBL539193	194934	None	0	Rat	Functional	pEC50	=	7.8	7.8	-97	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assayAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay	ChEMBL	1327	29	14	16	1.1	CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1021/jm900473p
	44417373	141895	None	0	Human	Functional	pEC50	=	7.8	7.8	1	3	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	518	6	1	5	4.3	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccc(Cl)cc5)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/jm8012272
	CHEMBL386272	141895	None	0	Human	Functional	pEC50	=	7.8	7.8	1	3	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	518	6	1	5	4.3	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccc(Cl)cc5)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/jm8012272
	16036897	77197	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assayAgonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assay	ChEMBL	475	11	2	6	5.9	CCOc1ccc(Cc2nc3ccc(NC(=N)c4cccs4)cc3n2CCN(CC)CC)cc1	10.1021/ml200268w
	CHEMBL2078719	77197	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assayAgonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assay	ChEMBL	475	11	2	6	5.9	CCOc1ccc(Cc2nc3ccc(NC(=N)c4cccs4)cc3n2CCN(CC)CC)cc1	10.1021/ml200268w
	CHEMBL3217001	77197	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assayAgonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assay	ChEMBL	475	11	2	6	5.9	CCOc1ccc(Cc2nc3ccc(NC(=N)c4cccs4)cc3n2CCN(CC)CC)cc1	10.1021/ml200268w
	46227361	205040	None	0	Rat	Functional	pEC50	=	6.8	6.8	-138	5	Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	1210	18	10	12	4.6	CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1016/j.bmc.2009.08.035
	CHEMBL611925	205040	None	0	Rat	Functional	pEC50	=	6.8	6.8	-138	5	Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	1210	18	10	12	4.6	CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1016/j.bmc.2009.08.035
	CHEMBL3609619	214293	None	0	Rat	Functional	pEC50	=	6.8	6.8	-1	2	Agonist activity at rat mu opioid receptor transfected in HN9.10 cells by [35S]GTPgammaS binding assayAgonist activity at rat mu opioid receptor transfected in HN9.10 cells by [35S]GTPgammaS binding assay	ChEMBL		None	None	None		C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1016/j.bmcl.2015.06.030
	16312302	59484	None	3	Human	Functional	pEC50	=	4.8	4.8	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	351	6	1	4	2.5	CN(C)C(CNC(=O)CSC(=S)N1CCCC1)c1ccccc1	nan
	CHEMBL1713166	59484	None	3	Human	Functional	pEC50	=	4.8	4.8	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	351	6	1	4	2.5	CN(C)C(CNC(=O)CSC(=S)N1CCCC1)c1ccccc1	nan
	162659824	181316	None	0	Human	Functional	pEC50	=	6.8	6.8	1	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1118	31	16	15	-3.4	N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.0c01367
	CHEMBL4761246	181316	None	0	Human	Functional	pEC50	=	6.8	6.8	1	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1118	31	16	15	-3.4	N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.0c01367
	90207332	160449	None	0	Human	Functional	pEC50	=	6.8	6.8	3	2	GTPgammaS Functional Assay (U-2): [35S]GTPgammaS functional assays were conducted using freshly thawed pt-receptor membranes prepared in-house from a cell line expressing recombinant mu opioid receptor in a U-2 OS cell background, or purchased from a commercial source (Perkin Elmer, Shelton, Conn.; or DiscovRx, Fremont, Calif.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2,20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B.GTPgammaS Functional Assay (U-2): [35S]GTPgammaS functional assays were conducted using freshly thawed pt-receptor membranes prepared in-house from a cell line expressing recombinant mu opioid receptor in a U-2 OS cell background, or purchased from a commercial source (Perkin Elmer, Shelton, Conn.; or DiscovRx, Fremont, Calif.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2,20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B.	ChEMBL	558	9	2	6	4.7	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](C(NC(C)C(=O)O)c1ccccc1)C2	nan
	CHEMBL4110838	160449	None	0	Human	Functional	pEC50	=	6.8	6.8	3	2	GTPgammaS Functional Assay (U-2): [35S]GTPgammaS functional assays were conducted using freshly thawed pt-receptor membranes prepared in-house from a cell line expressing recombinant mu opioid receptor in a U-2 OS cell background, or purchased from a commercial source (Perkin Elmer, Shelton, Conn.; or DiscovRx, Fremont, Calif.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2,20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B.GTPgammaS Functional Assay (U-2): [35S]GTPgammaS functional assays were conducted using freshly thawed pt-receptor membranes prepared in-house from a cell line expressing recombinant mu opioid receptor in a U-2 OS cell background, or purchased from a commercial source (Perkin Elmer, Shelton, Conn.; or DiscovRx, Fremont, Calif.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2,20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B.	ChEMBL	558	9	2	6	4.7	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](C(NC(C)C(=O)O)c1ccccc1)C2	nan
	18574678	34557	None	7	Human	Functional	pEC50	=	4.8	4.8	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	383	5	1	6	2.6	COC(=O)NCC(c1ccc2c(c1)OCO2)N1CCN(c2ccccc2)CC1	nan
	CHEMBL1429212	34557	None	7	Human	Functional	pEC50	=	4.8	4.8	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	383	5	1	6	2.6	COC(=O)NCC(c1ccc2c(c1)OCO2)N1CCN(c2ccccc2)CC1	nan
	90207334	160972	None	0	Human	Functional	pEC50	=	6.8	6.8	4	2	GTPgammaS Functional Assay (mu): [35S]GTPgammaS functional assays were conducted using freshly thawed pt-receptor membranes prepared in-house from a cell line expressing recombinant mu opioid receptor in a HEK-293, CHO cell background, or purchased from a commercial source (Perkin Elmer, Shelton, Conn.; or DiscovRx, Fremont, Calif.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2,20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B.GTPgammaS Functional Assay (mu): [35S]GTPgammaS functional assays were conducted using freshly thawed pt-receptor membranes prepared in-house from a cell line expressing recombinant mu opioid receptor in a HEK-293, CHO cell background, or purchased from a commercial source (Perkin Elmer, Shelton, Conn.; or DiscovRx, Fremont, Calif.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2,20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B.	ChEMBL	544	9	2	6	4.3	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](C(NCC(=O)O)c1ccccc1)C2	nan
	CHEMBL4115057	160972	None	0	Human	Functional	pEC50	=	6.8	6.8	4	2	GTPgammaS Functional Assay (mu): [35S]GTPgammaS functional assays were conducted using freshly thawed pt-receptor membranes prepared in-house from a cell line expressing recombinant mu opioid receptor in a HEK-293, CHO cell background, or purchased from a commercial source (Perkin Elmer, Shelton, Conn.; or DiscovRx, Fremont, Calif.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2,20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B.GTPgammaS Functional Assay (mu): [35S]GTPgammaS functional assays were conducted using freshly thawed pt-receptor membranes prepared in-house from a cell line expressing recombinant mu opioid receptor in a HEK-293, CHO cell background, or purchased from a commercial source (Perkin Elmer, Shelton, Conn.; or DiscovRx, Fremont, Calif.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2,20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B.	ChEMBL	544	9	2	6	4.3	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](C(NCC(=O)O)c1ccccc1)C2	nan
	CHEMBL5081900	217262	None	0	Human	Functional	pEC50	=	6.8	6.8	-2	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis	ChEMBL		None	None	None		C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O	10.1021/acs.jmedchem.0c02062
	44233410	198050	None	0	Rat	Functional	pEC50	=	6.8	6.8	-64	4	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assayAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay	ChEMBL	1327	28	14	16	1.0	CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1021/jm900473p
	CHEMBL555504	198050	None	0	Rat	Functional	pEC50	=	6.8	6.8	-64	4	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assayAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay	ChEMBL	1327	28	14	16	1.0	CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1021/jm900473p
	44235488	198255	None	0	Human	Functional	pEC50	=	6.8	6.8	-2	3	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by scintillation counting	ChEMBL	358	0	1	3	3.8	CN1CC[C@]23Cc4c(c5ccccc5n4C)C[C@]2(Cc2ccc(O)cc23)C1	10.1016/j.bmcl.2009.06.093
	CHEMBL557937	198255	None	0	Human	Functional	pEC50	=	6.8	6.8	-2	3	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by scintillation counting	ChEMBL	358	0	1	3	3.8	CN1CC[C@]23Cc4c(c5ccccc5n4C)C[C@]2(Cc2ccc(O)cc23)C1	10.1016/j.bmcl.2009.06.093
	168292466	192150	None	0	Rat	Functional	pEC50	=	5.8	5.8	-16	3	Agonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay	ChEMBL	567	6	0	5	6.2	COc1ccc2c3c1O[C@H]1[C@@]4(OC)CC[C@@]5(C[C@@]4(C)C(=O)c4ccc(C(F)(F)F)cc4)[C@@H](C2)N(CC2CC2)CC[C@]315	10.1021/acs.jmedchem.2c00014
	CHEMBL5202222	192150	None	0	Rat	Functional	pEC50	=	5.8	5.8	-16	3	Agonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay	ChEMBL	567	6	0	5	6.2	COc1ccc2c3c1O[C@H]1[C@@]4(OC)CC[C@@]5(C[C@@]4(C)C(=O)c4ccc(C(F)(F)F)cc4)[C@@H](C2)N(CC2CC2)CC[C@]315	10.1021/acs.jmedchem.2c00014
	CHEMBL5079626	217117	None	0	Human	Functional	pEC50	=	4.8	4.8	-	1	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 assayAgonist 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	ChEMBL		None	None	None		CC[C@@H]1CN2CC[C@@]3(O)C(=Nc4c(-c5ccccc5)ccc(OC)c43)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.1c01273
	70552386	180785	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	330	4	0	3	2.6	CC(C)C1OC2(CCN(CCc3ccccc3)CC2)CN(C)C1=O	10.1021/acs.jmedchem.0c01127
	CHEMBL4755342	180785	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	330	4	0	3	2.6	CC(C)C1OC2(CCN(CCc3ccccc3)CC2)CN(C)C1=O	10.1021/acs.jmedchem.0c01127
	CHEMBL5092009	217830	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL		None	None	None		c1ccc([C@]2(CCNCc3ccc4ccccc4c3)CCOC3(CCOC3)C2)nc1	10.1016/j.ejmech.2021.113986
	44421408	84740	None	0	Human	Functional	pEC50	=	6.8	6.8	-16	3	Activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	406	1	2	5	3.0	CCn1c2c(c3c1[C@@H]1Oc4c(O)ccc5c4[C@@]14CCN(C)C(C5)[C@]4(O)C3)CCCC2	10.1021/jm040817t
	CHEMBL222704	84740	None	0	Human	Functional	pEC50	=	6.8	6.8	-16	3	Activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	406	1	2	5	3.0	CCn1c2c(c3c1[C@@H]1Oc4c(O)ccc5c4[C@@]14CCN(C)C(C5)[C@]4(O)C3)CCCC2	10.1021/jm040817t
	44421422	84760	None	0	Human	Functional	pEC50	=	6.8	6.8	-14	3	Activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	482	3	2	5	4.2	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2c(c4c(n2CCc2ccccc2)CCCC4)C[C@@]3(O)C1C5	10.1021/jm040817t
	CHEMBL222814	84760	None	0	Human	Functional	pEC50	=	6.8	6.8	-14	3	Activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	482	3	2	5	4.2	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2c(c4c(n2CCc2ccccc2)CCCC4)C[C@@]3(O)C1C5	10.1021/jm040817t
	118725856	117245	None	0	Human	Functional	pEC50	=	5.8	5.8	-173	3	Agonist activity at human mu opioid receptor expressed in COS7 cells after 60 mins IP1 assayAgonist activity at human mu opioid receptor expressed in COS7 cells after 60 mins IP1 assay	ChEMBL	384	5	2	5	3.0	O=C(Nc1nc2ccccc2n1CCN1CC[C@H](O)C1)c1ccc(Cl)cc1	10.1016/j.bmcl.2014.12.064
	CHEMBL3394006	117245	None	0	Human	Functional	pEC50	=	5.8	5.8	-173	3	Agonist activity at human mu opioid receptor expressed in COS7 cells after 60 mins IP1 assayAgonist activity at human mu opioid receptor expressed in COS7 cells after 60 mins IP1 assay	ChEMBL	384	5	2	5	3.0	O=C(Nc1nc2ccccc2n1CCN1CC[C@H](O)C1)c1ccc(Cl)cc1	10.1016/j.bmcl.2014.12.064
	CHEMBL5079626	217117	None	0	Human	Functional	pEC50	=	4.8	4.8	-	1	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 assayAgonist 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	ChEMBL		None	None	None		CC[C@@H]1CN2CC[C@@]3(O)C(=Nc4c(-c5ccccc5)ccc(OC)c43)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.1c01273
	16188233	29622	None	5	Human	Functional	pEC50	=	4.8	4.8	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	433	9	0	6	4.5	CCOC(=O)C1(CCOc2ccccc2)CCN(Cc2cccn2-c2cccnc2)CC1	nan
	CHEMBL1385823	29622	None	5	Human	Functional	pEC50	=	4.8	4.8	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	433	9	0	6	4.5	CCOC(=O)C1(CCOc2ccccc2)CCN(Cc2cccn2-c2cccnc2)CC1	nan
	145950456	162797	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as reduction in forskolin-induced intracellular cAMP increase after 45 mins by HTRF analysisAgonist activity at human MOR expressed in CHOK1 cells assessed as reduction in forskolin-induced intracellular cAMP increase after 45 mins by HTRF analysis	ChEMBL	414	4	0	3	5.1	FCC[C@@H]1Cc2ccccc2C2(CCC(N3CCN(C4CCCCC4)CC3)CC2)O1	10.1021/acs.jmedchem.8b01183
	CHEMBL4170683	162797	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as reduction in forskolin-induced intracellular cAMP increase after 45 mins by HTRF analysisAgonist activity at human MOR expressed in CHOK1 cells assessed as reduction in forskolin-induced intracellular cAMP increase after 45 mins by HTRF analysis	ChEMBL	414	4	0	3	5.1	FCC[C@@H]1Cc2ccccc2C2(CCC(N3CCN(C4CCCCC4)CC3)CC2)O1	10.1021/acs.jmedchem.8b01183
	134563704	176739	None	0	Human	Functional	pEC50	=	5.8	5.8	-7	2	Agonist activity at human MOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay	ChEMBL	381	6	1	3	5.4	CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCN)c4ccccc43)CC2)CC1	10.1021/acs.jmedchem.9b02134
	CHEMBL4451073	176739	None	0	Human	Functional	pEC50	=	5.8	5.8	-7	2	Agonist activity at human MOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay	ChEMBL	381	6	1	3	5.4	CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCN)c4ccccc43)CC2)CC1	10.1021/acs.jmedchem.9b02134
	CHEMBL4597933	176739	None	0	Human	Functional	pEC50	=	5.8	5.8	-7	2	Agonist activity at human MOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay	ChEMBL	381	6	1	3	5.4	CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCN)c4ccccc43)CC2)CC1	10.1021/acs.jmedchem.9b02134
	145974608	164625	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	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 methodAgonist 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	ChEMBL	505	3	1	3	6.0	O=c1[nH]c2c(Cl)c(Cl)cc(Cl)c2n1C1CCN(Cc2ccc(Br)cc2F)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4214973	164625	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	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 methodAgonist 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	ChEMBL	505	3	1	3	6.0	O=c1[nH]c2c(Cl)c(Cl)cc(Cl)c2n1C1CCN(Cc2ccc(Br)cc2F)CC1	10.1021/acs.jmedchem.8b01136
	168293279	192259	None	0	Human	Functional	pEC50	=	4.8	4.8	-41	4	Agonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay	ChEMBL	583	15	5	6	2.0	CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(=O)N(C)C	10.1039/D1MD00025J
	CHEMBL5203813	192259	None	0	Human	Functional	pEC50	=	4.8	4.8	-41	4	Agonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay	ChEMBL	583	15	5	6	2.0	CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(=O)N(C)C	10.1039/D1MD00025J
	162644880	179554	None	0	Human	Functional	pEC50	=	6.8	6.8	-2	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1118	31	16	15	-3.4	N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.0c01367
	CHEMBL4740521	179554	None	0	Human	Functional	pEC50	=	6.8	6.8	-2	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1118	31	16	15	-3.4	N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.0c01367
	155520785	170612	None	0	Human	Functional	pEC50	=	5.8	5.8	-6	4	Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 minsAgonist activity at mu-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins	ChEMBL	1165	30	12	11	2.7	N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O	10.1016/j.bmc.2019.01.003
	CHEMBL4449491	170612	None	0	Human	Functional	pEC50	=	5.8	5.8	-6	4	Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 minsAgonist activity at mu-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins	ChEMBL	1165	30	12	11	2.7	N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O	10.1016/j.bmc.2019.01.003
	53322245	57328	None	0	Human	Functional	pEC50	=	5.8	5.8	-46	3	Agonist activity at human MOP receptor expressed in CHO-K1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human MOP receptor expressed in CHO-K1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting	ChEMBL	439	4	2	6	3.9	CC1CN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CCN1	10.1016/j.bmc.2010.07.034
	CHEMBL1650848	57328	None	0	Human	Functional	pEC50	=	5.8	5.8	-46	3	Agonist activity at human MOP receptor expressed in CHO-K1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human MOP receptor expressed in CHO-K1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting	ChEMBL	439	4	2	6	3.9	CC1CN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CCN1	10.1016/j.bmc.2010.07.034
	168293279	192259	None	0	Human	Functional	pEC50	=	4.8	4.8	-41	4	Agonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay	ChEMBL	583	15	5	6	2.0	CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(=O)N(C)C	10.1039/D1MD00025J
	CHEMBL5203813	192259	None	0	Human	Functional	pEC50	=	4.8	4.8	-41	4	Agonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay	ChEMBL	583	15	5	6	2.0	CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(=O)N(C)C	10.1039/D1MD00025J
	CHEMBL5077091	216966	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL		None	None	None		Fc1ccc([C@]2(CCNCc3scc4c3CCC4)CCOC3(CCOCC3)C2)nc1	10.1016/j.ejmech.2021.113986
	162644880	179554	None	0	Human	Functional	pEC50	=	6.8	6.8	-2	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1118	31	16	15	-3.4	N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.0c01367
	CHEMBL4740521	179554	None	0	Human	Functional	pEC50	=	6.8	6.8	-2	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1118	31	16	15	-3.4	N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.0c01367
	162660406	181360	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	302	3	0	3	1.9	C[C@@H]1OC2(CCN(CCc3ccccc3)CC2)CN(C)C1=O	10.1021/acs.jmedchem.0c01127
	CHEMBL4761794	181360	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	302	3	0	3	1.9	C[C@@H]1OC2(CCN(CCc3ccccc3)CC2)CN(C)C1=O	10.1021/acs.jmedchem.0c01127
	46179067	125866	None	0	Human	Functional	pEC50	=	4.8	4.8	-9	2	Mu-Opioid GTPgammaS Binding Assay: [35S]GTP gamma S functional assays were conducted using freshly thawed mu-receptor membranes. Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTP gamma S (0.20 nM; NEN). The prepared membrane solution (1904/well) was transferred to 96-shallow well polypropylene plates containing 10 uL of 20x concentrated stock solutions of the agonist DAMGO ([D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin) prepared in DMSO. Plates were incubated for 30 min at about 25 C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Packard, Meriden, Conn.) using a 96-well tissue harvester (Brandel, Gaithersburg, Md.) followed by three filtration washes with 200 mL of ice-cold wash buffer.Mu-Opioid GTPgammaS Binding Assay: [35S]GTP gamma S functional assays were conducted using freshly thawed mu-receptor membranes. Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTP gamma S (0.20 nM; NEN). The prepared membrane solution (1904/well) was transferred to 96-shallow well polypropylene plates containing 10 uL of 20x concentrated stock solutions of the agonist DAMGO ([D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin) prepared in DMSO. Plates were incubated for 30 min at about 25 C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Packard, Meriden, Conn.) using a 96-well tissue harvester (Brandel, Gaithersburg, Md.) followed by three filtration washes with 200 mL of ice-cold wash buffer.	ChEMBL	451	3	1	5	5.5	O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CC[C@H](C2)N3C2CCCCCCCCCC2)c1=O	nan
	CHEMBL3647960	125866	None	0	Human	Functional	pEC50	=	4.8	4.8	-9	2	Mu-Opioid GTPgammaS Binding Assay: [35S]GTP gamma S functional assays were conducted using freshly thawed mu-receptor membranes. Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTP gamma S (0.20 nM; NEN). The prepared membrane solution (1904/well) was transferred to 96-shallow well polypropylene plates containing 10 uL of 20x concentrated stock solutions of the agonist DAMGO ([D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin) prepared in DMSO. Plates were incubated for 30 min at about 25 C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Packard, Meriden, Conn.) using a 96-well tissue harvester (Brandel, Gaithersburg, Md.) followed by three filtration washes with 200 mL of ice-cold wash buffer.Mu-Opioid GTPgammaS Binding Assay: [35S]GTP gamma S functional assays were conducted using freshly thawed mu-receptor membranes. Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTP gamma S (0.20 nM; NEN). The prepared membrane solution (1904/well) was transferred to 96-shallow well polypropylene plates containing 10 uL of 20x concentrated stock solutions of the agonist DAMGO ([D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin) prepared in DMSO. Plates were incubated for 30 min at about 25 C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Packard, Meriden, Conn.) using a 96-well tissue harvester (Brandel, Gaithersburg, Md.) followed by three filtration washes with 200 mL of ice-cold wash buffer.	ChEMBL	451	3	1	5	5.5	O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CC[C@H](C2)N3C2CCCCCCCCCC2)c1=O	nan
	130431384	172899	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay	ChEMBL	427	3	1	3	5.3	O=c1[nH]c2cc(Cl)c(Cl)cc2n1C1CCN(Cc2ccc(Cl)cc2F)CC1	10.1021/acs.jmedchem.8b00435
	CHEMBL4513533	172899	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay	ChEMBL	427	3	1	3	5.3	O=c1[nH]c2cc(Cl)c(Cl)cc2n1C1CCN(Cc2ccc(Cl)cc2F)CC1	10.1021/acs.jmedchem.8b00435
	44455966	155125	None	0	Mouse	Functional	pEC50	=	4.8	4.8	-	1	Agonist activity at mu opioid receptor in Swiss mouse vas deferens assessed as inhibition of electrically-stimulated twitchAgonist activity at mu opioid receptor in Swiss mouse vas deferens assessed as inhibition of electrically-stimulated twitch	ChEMBL	331	5	1	4	3.3	CCOC(=O)CCCN1CC[C@]2(C)c3cc(O)ccc3CC1[C@@H]2C	10.1016/j.bmc.2007.10.030
	CHEMBL401590	155125	None	0	Mouse	Functional	pEC50	=	4.8	4.8	-	1	Agonist activity at mu opioid receptor in Swiss mouse vas deferens assessed as inhibition of electrically-stimulated twitchAgonist activity at mu opioid receptor in Swiss mouse vas deferens assessed as inhibition of electrically-stimulated twitch	ChEMBL	331	5	1	4	3.3	CCOC(=O)CCCN1CC[C@]2(C)c3cc(O)ccc3CC1[C@@H]2C	10.1016/j.bmc.2007.10.030
	53327589	160144	None	0	Human	Functional	pEC50	=	4.8	4.8	-	1	HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.	ChEMBL	727	29	1	14	1.6	COCCOCCOCCOCCOCCOCCOCCOCCOCCO[C@H]1CC[C@@]2(O)C3Cc4ccc(OC)c5c4[C@@]2(CCN3C)[C@H]1O5	nan
	CHEMBL4108254	160144	None	0	Human	Functional	pEC50	=	4.8	4.8	-	1	HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.	ChEMBL	727	29	1	14	1.6	COCCOCCOCCOCCOCCOCCOCCOCCOCCO[C@H]1CC[C@@]2(O)C3Cc4ccc(OC)c5c4[C@@]2(CCN3C)[C@H]1O5	nan
	9504185	21460	None	2	Human	Functional	pEC50	=	4.8	4.8	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	345	4	1	5	4.0	CC(C)n1ncc2c(C(=O)Nc3cccc(C#N)c3)cc(C3CC3)nc21	nan
	CHEMBL1315401	21460	None	2	Human	Functional	pEC50	=	4.8	4.8	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	345	4	1	5	4.0	CC(C)n1ncc2c(C(=O)Nc3cccc(C#N)c3)cc(C3CC3)nc21	nan
	CHEMBL382349	214762	None	0	Rat	Functional	pEC50	=	7.8	7.8	-14	5	Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm050921q
	145965971	164348	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	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 methodAgonist 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	ChEMBL	417	3	1	3	4.6	CC(c1ccc(Br)cc1F)N1CCC(n2c(=O)[nH]c3ccccc32)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4211411	164348	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	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 methodAgonist 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	ChEMBL	417	3	1	3	4.6	CC(c1ccc(Br)cc1F)N1CCC(n2c(=O)[nH]c3ccccc32)CC1	10.1021/acs.jmedchem.8b01136
	44591193	179462	None	0	Human	Functional	pEC50	=	7.8	7.8	-75	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	309	2	1	2	3.8	Cc1nc2cc3c(cc2[nH]1)[C@@]1(C)CCN(CC2CC2)C(C3)[C@@H]1C	10.1016/j.bmcl.2008.11.076
	CHEMBL473699	179462	None	0	Human	Functional	pEC50	=	7.8	7.8	-75	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	309	2	1	2	3.8	Cc1nc2cc3c(cc2[nH]1)[C@@]1(C)CCN(CC2CC2)C(C3)[C@@H]1C	10.1016/j.bmcl.2008.11.076
	72713093	106410	None	0	Human	Functional	pEC50	=	7.8	7.8	16	2	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	406	8	2	3	5.1	CCCN[C@H]1C[C@H]2C[C@@](c3cccc(O)c3)(C1)[C@H](C)CN2CCCc1ccccc1	10.1021/jm401250s
	CHEMBL3139210	106410	None	0	Human	Functional	pEC50	=	7.8	7.8	16	2	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	406	8	2	3	5.1	CCCN[C@H]1C[C@H]2C[C@@](c3cccc(O)c3)(C1)[C@H](C)CN2CCCc1ccccc1	10.1021/jm401250s
	CHEMBL3215960	106410	None	0	Human	Functional	pEC50	=	7.8	7.8	16	2	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	406	8	2	3	5.1	CCCN[C@H]1C[C@H]2C[C@@](c3cccc(O)c3)(C1)[C@H](C)CN2CCCc1ccccc1	10.1021/jm401250s
	155461914	182927	None	0	Human	Functional	pEC50	=	7.8	7.8	-22	5	Agonist activity at human mu-opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition in presence of IBMX by Glo-sensor cAMP assayAgonist activity at human mu-opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition in presence of IBMX by Glo-sensor cAMP assay	ChEMBL	1014	25	10	10	2.5	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCN2CCC(Cc3ccccc3)CC2)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)C1=O	10.1021/acs.jmedchem.0c00643
	CHEMBL4790994	182927	None	0	Human	Functional	pEC50	=	7.8	7.8	-22	5	Agonist activity at human mu-opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition in presence of IBMX by Glo-sensor cAMP assayAgonist activity at human mu-opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition in presence of IBMX by Glo-sensor cAMP assay	ChEMBL	1014	25	10	10	2.5	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCN2CCC(Cc3ccccc3)CC2)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)C1=O	10.1021/acs.jmedchem.0c00643
	54757387	65678	None	0	Rat	Functional	pEC50	=	7.8	7.8	-213	3	Agonist activity at rat brain mu-opioid receptor assessed as [35S]GTPgammaS binding by liquid scintillation countingAgonist activity at rat brain mu-opioid receptor assessed as [35S]GTPgammaS binding by liquid scintillation counting	ChEMBL	495	8	5	6	-0.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@H]1Cc2ccccc2CN(CC(N)=O)C1=O	10.1021/jm2003574
	CHEMBL1834247	65678	None	0	Rat	Functional	pEC50	=	7.8	7.8	-213	3	Agonist activity at rat brain mu-opioid receptor assessed as [35S]GTPgammaS binding by liquid scintillation countingAgonist activity at rat brain mu-opioid receptor assessed as [35S]GTPgammaS binding by liquid scintillation counting	ChEMBL	495	8	5	6	-0.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@H]1Cc2ccccc2CN(CC(N)=O)C1=O	10.1021/jm2003574
	44233185	194934	None	0	Rat	Functional	pEC50	=	7.8	7.8	-97	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assayAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay	ChEMBL	1327	29	14	16	1.1	CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1021/jm900473p
	CHEMBL539193	194934	None	0	Rat	Functional	pEC50	=	7.8	7.8	-97	5	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assayAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay	ChEMBL	1327	29	14	16	1.1	CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1021/jm900473p
	44177145	198184	None	0	Rat	Functional	pEC50	=	7.8	7.8	-8	4	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assayAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay	ChEMBL	1191	27	10	10	5.4	CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1021/jm900473p
	CHEMBL557188	198184	None	0	Rat	Functional	pEC50	=	7.8	7.8	-8	4	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assayAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay	ChEMBL	1191	27	10	10	5.4	CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1021/jm900473p
	168277847	190548	None	0	Rat	Functional	pEC50	=	7.8	7.8	3	2	Agonist activity at recombinant rat MOP stably expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS bindingAgonist activity at recombinant rat MOP stably expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS binding	ChEMBL	434	5	2	7	2.6	CC[C@@H]1CN2CC[C@]3(O)c4c(ccc(F)c4OC)N[C@@H]3[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.0c01915
	CHEMBL5178271	190548	None	0	Rat	Functional	pEC50	=	7.8	7.8	3	2	Agonist activity at recombinant rat MOP stably expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS bindingAgonist activity at recombinant rat MOP stably expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS binding	ChEMBL	434	5	2	7	2.6	CC[C@@H]1CN2CC[C@]3(O)c4c(ccc(F)c4OC)N[C@@H]3[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.0c01915
	44177145	198184	None	0	Rat	Functional	pEC50	=	7.7	7.7	-8	4	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assayAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay	ChEMBL	1191	27	10	10	5.4	CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1021/jm900473p
	CHEMBL557188	198184	None	0	Rat	Functional	pEC50	=	7.7	7.7	-8	4	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assayAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay	ChEMBL	1191	27	10	10	5.4	CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1021/jm900473p
	CHEMBL2370163	212263	None	0	Rat	Functional	pEC50	=	7.7	7.7	-	1	Compound was tested for its ability to stimulate [35S]GTP-gamma-S, binding to membranes from C6 glioma cells stably expressing rat mu opioid receptorCompound was tested for its ability to stimulate [35S]GTP-gamma-S, binding to membranes from C6 glioma cells stably expressing rat mu opioid receptor	ChEMBL		None	None	None		CC1(C)SSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]1C(N)=O	10.1016/s0960-894x(98)00472-7
	89978695	160488	None	0	Human	Functional	pEC50	=	7.7	7.7	-4	3	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	505	8	1	6	4.0	CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1C)[C@H]1Cc4ccc(OCCO)c5c4[C@@]3(CCN1C)[C@H]2O5	nan
	CHEMBL4111224	160488	None	0	Human	Functional	pEC50	=	7.7	7.7	-4	3	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	505	8	1	6	4.0	CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1C)[C@H]1Cc4ccc(OCCO)c5c4[C@@]3(CCN1C)[C@H]2O5	nan
	90656668	111017	None	0	Human	Functional	pEC50	=	7.7	7.7	-2	3	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysis	ChEMBL	501	6	2	5	4.9	CC[C@@](O)(c1ccccc1)[C@H]1C[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5	10.1021/jm401964y
	CHEMBL3262091	111017	None	0	Human	Functional	pEC50	=	7.7	7.7	-2	3	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysis	ChEMBL	501	6	2	5	4.9	CC[C@@](O)(c1ccccc1)[C@H]1C[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5	10.1021/jm401964y
	89978582	161015	None	0	Human	Functional	pEC50	=	7.7	7.7	-2	3	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	457	6	0	4	5.0	C=Cc1ccc2c3c1O[C@@H]1[C@]34CCN(C)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2	nan
	CHEMBL4115338	161015	None	0	Human	Functional	pEC50	=	7.7	7.7	-2	3	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	457	6	0	4	5.0	C=Cc1ccc2c3c1O[C@@H]1[C@]34CCN(C)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2	nan
	71887675	170589	None	2	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at Gi/o coupled human mu opioid receptor expressed in HEK293T cells co-expressing luciferase based cAMP biosensor and GRK2 assessed as increase in cAMP accumulation after 15 mins by FLIPR assayAgonist activity at Gi/o coupled human mu opioid receptor expressed in HEK293T cells co-expressing luciferase based cAMP biosensor and GRK2 assessed as increase in cAMP accumulation after 15 mins by FLIPR assay	ChEMBL	345	8	2	3	3.2	CC(Cc1ccsc1)NC(=O)NCC(Cc1ccccc1)N(C)C	10.1021/acs.jmedchem.8b00435
	CHEMBL4449152	170589	None	2	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at Gi/o coupled human mu opioid receptor expressed in HEK293T cells co-expressing luciferase based cAMP biosensor and GRK2 assessed as increase in cAMP accumulation after 15 mins by FLIPR assayAgonist activity at Gi/o coupled human mu opioid receptor expressed in HEK293T cells co-expressing luciferase based cAMP biosensor and GRK2 assessed as increase in cAMP accumulation after 15 mins by FLIPR assay	ChEMBL	345	8	2	3	3.2	CC(Cc1ccsc1)NC(=O)NCC(Cc1ccccc1)N(C)C	10.1021/acs.jmedchem.8b00435
	CHEMBL5093051	217894	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assay	ChEMBL		None	None	None		CCCN1CCN(C2(CN(C(=O)CC)c3cccc(C(F)(F)F)n3)CCOCC2)CC1	10.1021/acs.jmedchem.1c00417
	44439880	93690	None	0	Human	Functional	pEC50	=	6.8	6.8	-43	2	Agonist activity at human cloned mu opioid receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned mu opioid receptor assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	610	16	7	7	-0.2	Cc1cc(C(N)=O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)O	10.1016/j.bmcl.2007.01.092
	CHEMBL246739	93690	None	0	Human	Functional	pEC50	=	6.8	6.8	-43	2	Agonist activity at human cloned mu opioid receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned mu opioid receptor assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	610	16	7	7	-0.2	Cc1cc(C(N)=O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)O	10.1016/j.bmcl.2007.01.092
	172452553	195727	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assayAgonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assay	ChEMBL	342	7	2	4	3.4	C[C@H](OC(=O)NC[C@H](Cc1ccc(O)cc1)N(C)C)c1ccccc1	10.1016/j.bmcl.2023.129405
	CHEMBL5409642	195727	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	Agonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assayAgonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assay	ChEMBL	342	7	2	4	3.4	C[C@H](OC(=O)NC[C@H](Cc1ccc(O)cc1)N(C)C)c1ccccc1	10.1016/j.bmcl.2023.129405
	44233410	198050	None	0	Rat	Functional	pEC50	=	6.8	6.8	-64	4	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assayAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay	ChEMBL	1327	28	14	16	1.0	CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1021/jm900473p
	CHEMBL555504	198050	None	0	Rat	Functional	pEC50	=	6.8	6.8	-64	4	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assayAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay	ChEMBL	1327	28	14	16	1.0	CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1021/jm900473p
	71887675	170589	None	2	Human	Functional	pEC50	=	6.8	6.8	-	1	Inhibition of mu opioid receptor (unknown origin) assessed as reduction in intracellular cAMP accumulationInhibition of mu opioid receptor (unknown origin) assessed as reduction in intracellular cAMP accumulation	ChEMBL	345	8	2	3	3.2	CC(Cc1ccsc1)NC(=O)NCC(Cc1ccccc1)N(C)C	10.1016/j.ejmech.2019.111701
	CHEMBL4449152	170589	None	2	Human	Functional	pEC50	=	6.8	6.8	-	1	Inhibition of mu opioid receptor (unknown origin) assessed as reduction in intracellular cAMP accumulationInhibition of mu opioid receptor (unknown origin) assessed as reduction in intracellular cAMP accumulation	ChEMBL	345	8	2	3	3.2	CC(Cc1ccsc1)NC(=O)NCC(Cc1ccccc1)N(C)C	10.1016/j.ejmech.2019.111701
	118725841	117230	None	0	Human	Functional	pEC50	=	5.8	5.8	-251	3	Agonist activity at human mu opioid receptor expressed in COS7 cells after 60 mins IP1 assayAgonist activity at human mu opioid receptor expressed in COS7 cells after 60 mins IP1 assay	ChEMBL	402	5	1	4	4.7	O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1ccc(Cl)c(Cl)c1	10.1016/j.bmcl.2014.12.064
	CHEMBL3393991	117230	None	0	Human	Functional	pEC50	=	5.8	5.8	-251	3	Agonist activity at human mu opioid receptor expressed in COS7 cells after 60 mins IP1 assayAgonist activity at human mu opioid receptor expressed in COS7 cells after 60 mins IP1 assay	ChEMBL	402	5	1	4	4.7	O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1ccc(Cl)c(Cl)c1	10.1016/j.bmcl.2014.12.064
	118562469	170378	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	422	6	0	5	3.1	COC(=O)CC1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccc2)C1=O	10.1021/acs.jmedchem.9b01256
	CHEMBL4446209	170378	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	422	6	0	5	3.1	COC(=O)CC1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccc2)C1=O	10.1021/acs.jmedchem.9b01256
	1647	1313	None	34	Human	Functional	pEC50	=	6.7	6.7	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01273
	5462471	1313	None	34	Human	Functional	pEC50	=	6.7	6.7	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01273
	CHEMBL113995	1313	None	34	Human	Functional	pEC50	=	6.7	6.7	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01273
	CHEMBL38874	1313	None	34	Human	Functional	pEC50	=	6.7	6.7	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01273
	CHEMBL5073561	216787	None	0	Human	Functional	pEC50	=	6.7	6.7	-107	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O	10.1021/acs.jmedchem.0c02062
	164916967	195989	None	2	Mouse	Functional	pEC50	=	5.7	5.7	-45	2	Partial 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 assayPartial 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	ChEMBL	679	13	2	6	4.9	CN(C)C(=O)C(CCN1C[C@H](O)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1	10.1021/acs.jmedchem.3c00417
	CHEMBL5414796	195989	None	2	Mouse	Functional	pEC50	=	5.7	5.7	-45	2	Partial 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 assayPartial 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	ChEMBL	679	13	2	6	4.9	CN(C)C(=O)C(CCN1C[C@H](O)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1	10.1021/acs.jmedchem.3c00417
	164916967	195989	None	2	Mouse	Functional	pEC50	=	5.7	5.7	-45	2	Partial 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 assayPartial 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	ChEMBL	679	13	2	6	4.9	CN(C)C(=O)C(CCN1C[C@H](O)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1	10.1021/acs.jmedchem.3c00417
	CHEMBL5414796	195989	None	2	Mouse	Functional	pEC50	=	5.7	5.7	-45	2	Partial 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 assayPartial 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	ChEMBL	679	13	2	6	4.9	CN(C)C(=O)C(CCN1C[C@H](O)C[C@H]1C(=O)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1	10.1021/acs.jmedchem.3c00417
	12956	730	None	4	Human	Functional	pEC50	=	6.7	6.7	-	1	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 assayAgonist 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	ChEMBL	399	3	1	3	4.5	CC(C1=CC=C(C=C1)Br)N2CCC(CC2)N3C4=CC=CC=C4NC3=O	10.1021/acs.jmedchem.8b01136
	145975294	730	None	4	Human	Functional	pEC50	=	6.7	6.7	-	1	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 assayAgonist 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	ChEMBL	399	3	1	3	4.5	CC(C1=CC=C(C=C1)Br)N2CCC(CC2)N3C4=CC=CC=C4NC3=O	10.1021/acs.jmedchem.8b01136
	CHEMBL4203403	730	None	4	Human	Functional	pEC50	=	6.7	6.7	-	1	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 assayAgonist 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	ChEMBL	399	3	1	3	4.5	CC(C1=CC=C(C=C1)Br)N2CCC(CC2)N3C4=CC=CC=C4NC3=O	10.1021/acs.jmedchem.8b01136
	1647	1313	None	34	Human	Functional	pEC50	=	6.7	6.7	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01273
	5462471	1313	None	34	Human	Functional	pEC50	=	6.7	6.7	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01273
	CHEMBL113995	1313	None	34	Human	Functional	pEC50	=	6.7	6.7	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01273
	CHEMBL38874	1313	None	34	Human	Functional	pEC50	=	6.7	6.7	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01273
	CHEMBL5086571	217525	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assay	ChEMBL		None	None	None		CCC(=O)N(CC1(N2CCN(CC(C)C)CC2)CCOCC1)c1cccc(C(F)(F)F)n1	10.1021/acs.jmedchem.1c00417
	CHEMBL5086571	217525	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at mu-opioid receptor (unknown origin)Agonist activity at mu-opioid receptor (unknown origin)	ChEMBL		None	None	None		CCC(=O)N(CC1(N2CCN(CC(C)C)CC2)CCOCC1)c1cccc(C(F)(F)F)n1	10.1021/acs.jmedchem.3c01637
	137659520	159359	None	0	Human	Functional	pEC50	=	4.7	4.7	-17378	2	Agonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assayAgonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assay	ChEMBL	504	6	3	6	2.9	CN(C(=O)CCc1ccccc1)[C@@H]1CC[C@@]2(O)[C@H]3[C@@H](O)c4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2017.06.017
	CHEMBL4099273	159359	None	0	Human	Functional	pEC50	=	4.7	4.7	-17378	2	Agonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assayAgonist activity at human mu opioid receptor expressed in CHO-dhfr(-) cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assay	ChEMBL	504	6	3	6	2.9	CN(C(=O)CCc1ccccc1)[C@@H]1CC[C@@]2(O)[C@H]3[C@@H](O)c4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2017.06.017
	71761636	91433	None	0	Rat	Functional	pEC50	=	5.7	5.7	1	2	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	609	7	8	10	-2.9	CN(C)/C1=N/C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CN1	10.1021/jm4008592
	CHEMBL2402928	91433	None	0	Rat	Functional	pEC50	=	5.7	5.7	1	2	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	609	7	8	10	-2.9	CN(C)/C1=N/C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CN1	10.1021/jm4008592
	24906068	172545	None	0	Rat	Functional	pEC50	=	5.7	5.7	-	1	Activity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS bindingActivity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	599	13	6	6	1.9	NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCC[C@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm800223t
	CHEMBL447871	172545	None	0	Rat	Functional	pEC50	=	5.7	5.7	-	1	Activity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS bindingActivity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	599	13	6	6	1.9	NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCC[C@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm800223t
	145978786	163886	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	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 methodAgonist 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	ChEMBL	375	3	1	3	4.5	O=c1[nH]c2cc(Cl)ccc2n1C1CCN(Cc2ccccc2Cl)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4205961	163886	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	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 methodAgonist 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	ChEMBL	375	3	1	3	4.5	O=c1[nH]c2cc(Cl)ccc2n1C1CCN(Cc2ccccc2Cl)CC1	10.1021/acs.jmedchem.8b01136
	60561198	164905	None	5	Human	Functional	pEC50	=	6.7	6.7	-	1	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 assayAgonist 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	ChEMBL	355	3	1	3	4.4	CC(c1ccc(Cl)cc1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4218547	164905	None	5	Human	Functional	pEC50	=	6.7	6.7	-	1	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 assayAgonist 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	ChEMBL	355	3	1	3	4.4	CC(c1ccc(Cl)cc1)N1CCC(n2c(=O)[nH]c3ccccc32)CC1	10.1021/acs.jmedchem.8b01136
	54757290	65653	None	0	Rat	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at rat brain mu-opioid receptor assessed as [35S]GTPgammaS binding by liquid scintillation countingAgonist activity at rat brain mu-opioid receptor assessed as [35S]GTPgammaS binding by liquid scintillation counting	ChEMBL	509	8	5	6	0.5	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@H]1C(=O)N(CC(N)=O)Cc2ccccc2[C@H]1C	10.1021/jm2003574
	CHEMBL1834219	65653	None	0	Rat	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at rat brain mu-opioid receptor assessed as [35S]GTPgammaS binding by liquid scintillation countingAgonist activity at rat brain mu-opioid receptor assessed as [35S]GTPgammaS binding by liquid scintillation counting	ChEMBL	509	8	5	6	0.5	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@H]1C(=O)N(CC(N)=O)Cc2ccccc2[C@H]1C	10.1021/jm2003574
	71452746	79212	None	0	Human	Functional	pEC50	=	6.7	6.7	-549	2	Stimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cellsStimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells	ChEMBL	401	2	3	4	3.4	CCN[C@@]12Cc3c([nH]c4ccccc34)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)C2C5	10.1021/jm021073r
	CHEMBL2113383	79212	None	0	Human	Functional	pEC50	=	6.7	6.7	-549	2	Stimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cellsStimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells	ChEMBL	401	2	3	4	3.4	CCN[C@@]12Cc3c([nH]c4ccccc34)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)C2C5	10.1021/jm021073r
	15185486	113938	None	1	Human	Functional	pEC50	=	4.7	4.7	-	1	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	284	2	0	4	3.3	COc1ccc(-n2nc(C)c3c2CC(C)(C)CC3=O)cc1	10.1016/j.bmc.2014.07.012
	CHEMBL3325704	113938	None	1	Human	Functional	pEC50	=	4.7	4.7	-	1	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	284	2	0	4	3.3	COc1ccc(-n2nc(C)c3c2CC(C)(C)CC3=O)cc1	10.1016/j.bmc.2014.07.012
	89978423	147629	None	0	Human	Functional	pEC50	=	6.7	6.7	-1	2	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	601	12	0	7	5.7	CCOC(=O)CC[C@H]1[C@H](COCc2ccccc2)[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(OC)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5	nan
	CHEMBL3930729	147629	None	0	Human	Functional	pEC50	=	6.7	6.7	-1	2	Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.	ChEMBL	601	12	0	7	5.7	CCOC(=O)CC[C@H]1[C@H](COCc2ccccc2)[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(OC)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5	nan
	4881395	59427	None	2	Human	Functional	pEC50	=	4.7	4.7	1	2	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	377	6	1	4	2.9	COc1ccc(C(CNC(=O)c2cncc(Br)c2)N(C)C)cc1	nan
	CHEMBL1709988	59427	None	2	Human	Functional	pEC50	=	4.7	4.7	1	2	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	377	6	1	4	2.9	COc1ccc(C(CNC(=O)c2cncc(Br)c2)N(C)C)cc1	nan
	118567545	173811	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	433	4	0	4	3.9	CC1OC2(CCN(CCc3ccccc3)CC2)CN(c2cccnc2C(F)(F)F)C1=O	10.1021/acs.jmedchem.9b01256
	CHEMBL4535897	173811	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	433	4	0	4	3.9	CC1OC2(CCN(CCc3ccccc3)CC2)CN(c2cccnc2C(F)(F)F)C1=O	10.1021/acs.jmedchem.9b01256
	CHEMBL5079202	217097	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	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 assayAgonist 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	ChEMBL		None	None	None		CC[C@@H]1CN2CCc3c([nH]c4c(-c5ccoc5)ccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.1c01273
	CHEMBL5079202	217097	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	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 assayAgonist 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	ChEMBL		None	None	None		CC[C@@H]1CN2CCc3c([nH]c4c(-c5ccoc5)ccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.1c01273
	71761636	91433	None	0	Rat	Functional	pEC50	=	5.7	5.7	1	2	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	609	7	8	10	-2.9	CN(C)/C1=N/C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CN1	10.1021/jm4008592
	CHEMBL2402928	91433	None	0	Rat	Functional	pEC50	=	5.7	5.7	1	2	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	609	7	8	10	-2.9	CN(C)/C1=N/C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CN1	10.1021/jm4008592
	11274203	79033	None	0	Rat	Functional	pEC50	=	6.7	6.7	10	2	Agonist activity against rat Opioid receptor mu 1 expressed in C6 cells in [35S]-GTP-gamma S binding assay Agonist activity against rat Opioid receptor mu 1 expressed in C6 cells in [35S]-GTP-gamma S binding assay	ChEMBL	751	6	4	9	5.3	Oc1ccc2c3c1O[C@H]1c4c(c5c(n4Cc4ccccc4)[C@@H]4Oc6c(O)ccc7c6[C@@]46CCN(CC4CC4)[C@H](C7)[C@]6(O)C5)C[C@@]4(O)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/jm049172n
	CHEMBL2113078	79033	None	0	Rat	Functional	pEC50	=	6.7	6.7	10	2	Agonist activity against rat Opioid receptor mu 1 expressed in C6 cells in [35S]-GTP-gamma S binding assay Agonist activity against rat Opioid receptor mu 1 expressed in C6 cells in [35S]-GTP-gamma S binding assay	ChEMBL	751	6	4	9	5.3	Oc1ccc2c3c1O[C@H]1c4c(c5c(n4Cc4ccccc4)[C@@H]4Oc6c(O)ccc7c6[C@@]46CCN(CC4CC4)[C@H](C7)[C@]6(O)C5)C[C@@]4(O)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/jm049172n
	5077003	55540	None	6	Human	Functional	pEC50	=	4.7	4.7	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	311	2	1	3	2.9	Cc1ccccc1[N+]1=C2SCCN2C(O)(c2ccccc2)C1	nan
	CHEMBL1425453	55540	None	6	Human	Functional	pEC50	=	4.7	4.7	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	311	2	1	3	2.9	Cc1ccccc1[N+]1=C2SCCN2C(O)(c2ccccc2)C1	nan
	CHEMBL1620357	55540	None	6	Human	Functional	pEC50	=	4.7	4.7	-	1	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	311	2	1	3	2.9	Cc1ccccc1[N+]1=C2SCCN2C(O)(c2ccccc2)C1	nan
	16189942	36569	None	5	Human	Functional	pEC50	=	4.7	4.7	1	2	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	419	8	1	6	4.5	CCn1cc(CNCc2cn(-c3ccccc3C)nc2-c2ccc(OC)c(F)c2)cn1	nan
	CHEMBL1448229	36569	None	5	Human	Functional	pEC50	=	4.7	4.7	1	2	PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory) PubChem BioAssay. Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRM1 homodimerization. (Class of assay: confirmatory)	ChEMBL	419	8	1	6	4.5	CCn1cc(CNCc2cn(-c3ccccc3C)nc2-c2ccc(OC)c(F)c2)cn1	nan
	145973938	164682	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	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 methodAgonist 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	ChEMBL	365	5	1	4	4.1	CCOc1ccc(C(C)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)cc1	10.1021/acs.jmedchem.8b01136
	CHEMBL4215601	164682	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	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 methodAgonist 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	ChEMBL	365	5	1	4	4.1	CCOc1ccc(C(C)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)cc1	10.1021/acs.jmedchem.8b01136
	71624266	90493	None	0	Human	Functional	pEC50	=	6.7	6.7	-2	2	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis	ChEMBL	368	4	0	2	5.0	CCC(C)(C)[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1	10.1016/j.bmcl.2013.03.101
	CHEMBL2387189	90493	None	0	Human	Functional	pEC50	=	6.7	6.7	-2	2	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis	ChEMBL	368	4	0	2	5.0	CCC(C)(C)[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1	10.1016/j.bmcl.2013.03.101
	CHEMBL5080233	217158	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISAAgonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISA	ChEMBL		None	None	None		N=C(N)NCCC[C@@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.1c01631
	CHEMBL5081955	217267	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at human MOR expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 60 mins by cAMP HTRF assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 60 mins by cAMP HTRF assay	ChEMBL		None	None	None		CCC(=O)N(C[C@@H](C)N1CCC(Cc2ccccc2)CC1)c1ccccc1	10.1016/j.ejmech.2021.113879
	172459209	196212	None	0	Human	Functional	pEC50	=	5.7	5.7	-	1	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assay	ChEMBL	372	5	1	3	4.9	Cc1ccc2cc(C(=O)NCC(c3ccccc3Cl)N(C)C)sc2c1	10.1016/j.ejmech.2022.114728
	CHEMBL5418969	196212	None	0	Human	Functional	pEC50	=	5.7	5.7	-	1	Agonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed in CHO-K1 cells coexpressing Galpha15 assessed as increase in fluorescence of [ca2+]i measured for 1.52 sec by FLIPR calcium assay	ChEMBL	372	5	1	3	4.9	Cc1ccc2cc(C(=O)NCC(c3ccccc3Cl)N(C)C)sc2c1	10.1016/j.ejmech.2022.114728
	44406695	140801	None	0	Human	Functional	pEC50	=	7.7	7.7	-1	2	Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	728	9	0	6	9.0	O=C(/C=C/C=C/C(=O)Oc1ccc2c(c1)[C@@]13CCCCC1[C@@H](C2)N(CC1CCC1)CC3)Oc1ccc2c(c1)[C@@]13CCCCC1[C@@H](C2)N(CC1CCC1)CC3	10.1021/jm050577x
	CHEMBL381750	140801	None	0	Human	Functional	pEC50	=	7.7	7.7	-1	2	Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	728	9	0	6	9.0	O=C(/C=C/C=C/C(=O)Oc1ccc2c(c1)[C@@]13CCCCC1[C@@H](C2)N(CC1CCC1)CC3)Oc1ccc2c(c1)[C@@]13CCCCC1[C@@H](C2)N(CC1CCC1)CC3	10.1021/jm050577x
	1647	1313	None	34	Mouse	Functional	pEC50	=	7.7	7.7	-4	9	Agonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopyAgonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopy	ChEMBL		None	None	None		None	10.1039/C6MD00450D
	5462471	1313	None	34	Mouse	Functional	pEC50	=	7.7	7.7	-4	9	Agonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopyAgonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopy	ChEMBL		None	None	None		None	10.1039/C6MD00450D
	CHEMBL113995	1313	None	34	Mouse	Functional	pEC50	=	7.7	7.7	-4	9	Agonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopyAgonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopy	ChEMBL		None	None	None		None	10.1039/C6MD00450D
	CHEMBL38874	1313	None	34	Mouse	Functional	pEC50	=	7.7	7.7	-4	9	Agonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopyAgonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopy	ChEMBL		None	None	None		None	10.1039/C6MD00450D
	1647	1313	None	34	Mouse	Functional	pEC50	=	7.7	7.7	-4	9	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 ELISAAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b01767
	5462471	1313	None	34	Mouse	Functional	pEC50	=	7.7	7.7	-4	9	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 ELISAAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b01767
	CHEMBL113995	1313	None	34	Mouse	Functional	pEC50	=	7.7	7.7	-4	9	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 ELISAAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b01767
	CHEMBL38874	1313	None	34	Mouse	Functional	pEC50	=	7.7	7.7	-4	9	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 ELISAAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b01767
	1647	1313	None	34	Mouse	Functional	pEC50	=	7.7	7.7	-4	9	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 analysisAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b00748
	5462471	1313	None	34	Mouse	Functional	pEC50	=	7.7	7.7	-4	9	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 analysisAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b00748
	CHEMBL113995	1313	None	34	Mouse	Functional	pEC50	=	7.7	7.7	-4	9	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 analysisAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b00748
	CHEMBL38874	1313	None	34	Mouse	Functional	pEC50	=	7.7	7.7	-4	9	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 analysisAgonist 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	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b00748
	50994461	57235	None	0	Rat	Functional	pEC50	=	7.7	7.7	2	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	717	15	4	6	5.4	CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1	10.1021/jm100982d
	CHEMBL1649944	57235	None	0	Rat	Functional	pEC50	=	7.7	7.7	2	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	717	15	4	6	5.4	CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1	10.1021/jm100982d
	137630443	161161	None	0	Rat	Functional	pEC50	=	7.7	7.7	39	3	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 methodAgonist 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	ChEMBL	405	4	2	3	4.5	Oc1cccc([C@]23CCC[C@H]([C@H]2O)N(CCc2ccc(C(F)(F)F)cc2)CC3)c1	10.1016/j.bmc.2017.02.064
	CHEMBL4102551	161161	None	0	Rat	Functional	pEC50	=	7.7	7.7	39	3	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 methodAgonist 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	ChEMBL	405	4	2	3	4.5	Oc1cccc([C@]23CCC[C@H]([C@H]2O)N(CCc2ccc(C(F)(F)F)cc2)CC3)c1	10.1016/j.bmc.2017.02.064
	CHEMBL4116648	161161	None	0	Rat	Functional	pEC50	=	7.7	7.7	39	3	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 methodAgonist 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	ChEMBL	405	4	2	3	4.5	Oc1cccc([C@]23CCC[C@H]([C@H]2O)N(CCc2ccc(C(F)(F)F)cc2)CC3)c1	10.1016/j.bmc.2017.02.064
	57900045	88200	None	0	Human	Functional	pEC50	=	7.7	7.7	-2	2	Partial 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 countingPartial 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	ChEMBL	479	7	1	3	5.7	C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccccc5)cn4)cc3[C@@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2013.01.117
	CHEMBL2347239	88200	None	0	Human	Functional	pEC50	=	7.7	7.7	-2	2	Partial 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 countingPartial 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	ChEMBL	479	7	1	3	5.7	C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccccc5)cn4)cc3[C@@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2013.01.117
	50994461	57235	None	0	Rat	Functional	pEC50	=	7.7	7.7	2	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	717	15	4	6	5.4	CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1	10.1021/jm100982d
	CHEMBL1649944	57235	None	0	Rat	Functional	pEC50	=	7.7	7.7	2	3	Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	717	15	4	6	5.4	CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1	10.1021/jm100982d
	127033967	139134	None	0	Human	Functional	pEC50	=	7.7	7.7	-10	3	Agonist activity at human mu opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay	ChEMBL	429	3	2	4	4.2	O=C1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]3(O)CC/C1=C/c1ccccc1	10.1016/j.bmc.2016.03.040
	CHEMBL3786083	139134	None	0	Human	Functional	pEC50	=	7.7	7.7	-10	3	Agonist activity at human mu opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay	ChEMBL	429	3	2	4	4.2	O=C1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]3(O)CC/C1=C/c1ccccc1	10.1016/j.bmc.2016.03.040
	9949205	9495	None	0	Human	Functional	pEC50	=	7.7	7.7	1	2	Agonistic activity against human opioid Mu receptor transfected into Chinese hamster ovary (CHO) cells using [3H]-DAMGO as radioligandAgonistic activity against human opioid Mu receptor transfected into Chinese hamster ovary (CHO) cells using [3H]-DAMGO as radioligand	ChEMBL	325	0	3	5	1.0	CN1CCC23c4c5ccc(O)c4OC2c2n[nH]cc2CC3(O)C1C5	10.1016/s0960-894x(99)00608-3
	CHEMBL112035	9495	None	0	Human	Functional	pEC50	=	7.7	7.7	1	2	Agonistic activity against human opioid Mu receptor transfected into Chinese hamster ovary (CHO) cells using [3H]-DAMGO as radioligandAgonistic activity against human opioid Mu receptor transfected into Chinese hamster ovary (CHO) cells using [3H]-DAMGO as radioligand	ChEMBL	325	0	3	5	1.0	CN1CCC23c4c5ccc(O)c4OC2c2n[nH]cc2CC3(O)C1C5	10.1016/s0960-894x(99)00608-3
	73350737	92093	None	0	Mouse	Functional	pEC50	=	7.7	7.7	-	1	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	ChEMBL	515	4	3	6	2.5	CN1Cc2ccccc2C[C@H]1C(=O)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2013.07.043
	CHEMBL2419117	92093	None	0	Mouse	Functional	pEC50	=	7.7	7.7	-	1	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	ChEMBL	515	4	3	6	2.5	CN1Cc2ccccc2C[C@H]1C(=O)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2013.07.043
	73350737	92093	None	0	Mouse	Functional	pEC50	=	7.7	7.7	-	1	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	515	4	3	6	2.5	CN1Cc2ccccc2C[C@H]1C(=O)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmc.2015.02.055
	CHEMBL2419117	92093	None	0	Mouse	Functional	pEC50	=	7.7	7.7	-	1	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	515	4	3	6	2.5	CN1Cc2ccccc2C[C@H]1C(=O)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmc.2015.02.055
	CHEMBL285479	213322	None	0	Human	Functional	pEC50	=	7.7	7.7	89	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis	ChEMBL		None	None	None		C[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O	10.1021/acs.jmedchem.0c02062
	11566769	112725	None	0	Human	Functional	pEC50	=	7.7	7.7	-2	2	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	364	5	2	3	4.1	C[C@@H]1CN(CCCc2ccccc2)[C@H]2C[C@H](N)C[C@]1(c1cccc(O)c1)C2	10.1021/jm401250s
	CHEMBL3216611	112725	None	0	Human	Functional	pEC50	=	7.7	7.7	-2	2	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	364	5	2	3	4.1	C[C@@H]1CN(CCCc2ccccc2)[C@H]2C[C@H](N)C[C@]1(c1cccc(O)c1)C2	10.1021/jm401250s
	CHEMBL3303515	112725	None	0	Human	Functional	pEC50	=	7.7	7.7	-2	2	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	364	5	2	3	4.1	C[C@@H]1CN(CCCc2ccccc2)[C@H]2C[C@H](N)C[C@]1(c1cccc(O)c1)C2	10.1021/jm401250s
	155510746	176340	None	0	Human	Functional	pEC50	=	7.7	7.7	2	3	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	932	12	12	12	-1.3	N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1C/C=C\C[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O	10.1021/acsmedchemlett.8b00495
	CHEMBL4434948	176340	None	0	Human	Functional	pEC50	=	7.7	7.7	2	3	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	932	12	12	12	-1.3	N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1C/C=C\C[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O	10.1021/acsmedchemlett.8b00495
	CHEMBL4594706	176340	None	0	Human	Functional	pEC50	=	7.7	7.7	2	3	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	932	12	12	12	-1.3	N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1C/C=C\C[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O	10.1021/acsmedchemlett.8b00495
	1647	1313	None	34	Human	Functional	pEC50	=	7.7	7.7	-3	9	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.8b00495
	5462471	1313	None	34	Human	Functional	pEC50	=	7.7	7.7	-3	9	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.8b00495
	CHEMBL113995	1313	None	34	Human	Functional	pEC50	=	7.7	7.7	-3	9	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.8b00495
	CHEMBL38874	1313	None	34	Human	Functional	pEC50	=	7.7	7.7	-3	9	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.8b00495
	155515241	170044	None	0	Mouse	Functional	pEC50	=	7.7	7.7	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	503	6	3	6	3.3	CC(C)Cc1cnccc1C(=O)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.8b01158
	CHEMBL4441484	170044	None	0	Mouse	Functional	pEC50	=	7.7	7.7	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	503	6	3	6	3.3	CC(C)Cc1cnccc1C(=O)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.8b01158
	CHEMBL5085321	217451	None	0	Human	Functional	pEC50	=	7.7	7.7	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL		None	None	None		Fc1ccc([C@]2(CCNCc3cccs3)CCOC3(CCOC3)C2)cc1	10.1016/j.ejmech.2021.113986
	CHEMBL205306	211627	None	0	Rat	Functional	pEC50	=	7.7	7.7	-8	4	Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCC)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/jm050921q
	CHEMBL5080654	217186	None	0	Human	Functional	pEC50	=	7.7	7.7	134	2	Agonist activity at human mu opioid receptor expressed in HEK293T cells assessed as arrestin-3 recruitment preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human mu opioid receptor expressed in HEK293T cells assessed as arrestin-3 recruitment preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay	ChEMBL		None	None	None		CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1	10.1021/acs.jmedchem.1c00611
	CHEMBL3758969	214687	None	0	Human	Functional	pEC50	=	7.7	7.7	64	2	Agonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysisAgonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis	ChEMBL		None	None	None		Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2cccc3ccccc23)NC1=O	10.1016/j.ejmech.2015.12.012
	162643991	181904	None	0	Human	Functional	pEC50	=	7.7	7.7	1	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1126	32	14	14	-3.6	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.6b01181
	CHEMBL4777999	181904	None	0	Human	Functional	pEC50	=	7.7	7.7	1	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1126	32	14	14	-3.6	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.6b01181
	86580802	152788	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	286	1	1	3	1.9	CN1CC[C@]23c4cccc(C(N)=O)c4O[C@H]2CCC[C@H]3C1	nan
	CHEMBL3972934	152788	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	286	1	1	3	1.9	CN1CC[C@]23c4cccc(C(N)=O)c4O[C@H]2CCC[C@H]3C1	nan
	145961131	161657	None	0	Human	Functional	pEC50	=	6.7	6.7	1	3	Agonist activity at MOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assayAgonist activity at MOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assay	ChEMBL	1080	12	10	14	0.8	CC1(C)SSC(C)(C)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCN(CC2)C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1016/j.bmc.2018.05.045
	CHEMBL4128853	161657	None	0	Human	Functional	pEC50	=	6.7	6.7	1	3	Agonist activity at MOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assayAgonist activity at MOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assay	ChEMBL	1080	12	10	14	0.8	CC1(C)SSC(C)(C)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCN(CC2)C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1016/j.bmc.2018.05.045
	155515973	170122	None	0	Human	Functional	pEC50	=	5.7	5.7	-10	3	Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 minsAgonist activity at mu-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins	ChEMBL	1165	30	12	11	2.7	N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O	10.1016/j.bmc.2019.01.003
	CHEMBL4442534	170122	None	0	Human	Functional	pEC50	=	5.7	5.7	-10	3	Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 minsAgonist activity at mu-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins	ChEMBL	1165	30	12	11	2.7	N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O	10.1016/j.bmc.2019.01.003
	118711127	113937	None	0	Human	Functional	pEC50	=	4.7	4.7	-	1	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	282	2	0	3	3.9	CCc1ccccc1-n1nc(C)c2c1CC(C)(C)CC2=O	10.1016/j.bmc.2014.07.012
	CHEMBL3325703	113937	None	0	Human	Functional	pEC50	=	4.7	4.7	-	1	Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assayAgonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay	ChEMBL	282	2	0	3	3.9	CCc1ccccc1-n1nc(C)c2c1CC(C)(C)CC2=O	10.1016/j.bmc.2014.07.012
	972358	40344	None	8	Human	Functional	pEC50	=	4.7	4.7	-	1	Agonist activity at human mu opioid receptor expressed in CHOK1 cells coexpressing Galpha15 assessed as increase in intracellular calcium flux in presence of mu opioid receptor antagonist naloxone and incubated for 1 hr measured for 90 secs at 1.5 sec interval by FLIPR assayAgonist activity at human mu opioid receptor expressed in CHOK1 cells coexpressing Galpha15 assessed as increase in intracellular calcium flux in presence of mu opioid receptor antagonist naloxone and incubated for 1 hr measured for 90 secs at 1.5 sec interval by FLIPR assay	ChEMBL	347	5	1	7	4.6	COc1ccc(Nc2nc(-c3sc(C)nc3C)cs2)c(OC)c1	10.1016/j.ejmech.2019.01.063
	CHEMBL1481328	40344	None	8	Human	Functional	pEC50	=	4.7	4.7	-	1	Agonist activity at human mu opioid receptor expressed in CHOK1 cells coexpressing Galpha15 assessed as increase in intracellular calcium flux in presence of mu opioid receptor antagonist naloxone and incubated for 1 hr measured for 90 secs at 1.5 sec interval by FLIPR assayAgonist activity at human mu opioid receptor expressed in CHOK1 cells coexpressing Galpha15 assessed as increase in intracellular calcium flux in presence of mu opioid receptor antagonist naloxone and incubated for 1 hr measured for 90 secs at 1.5 sec interval by FLIPR assay	ChEMBL	347	5	1	7	4.6	COc1ccc(Nc2nc(-c3sc(C)nc3C)cs2)c(OC)c1	10.1016/j.ejmech.2019.01.063
	CHEMBL5086786	217538	None	0	Human	Functional	pEC50	=	4.7	4.7	-	1	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 assayAgonist 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	ChEMBL		None	None	None		CC[C@@H]1CN2CC[C@@]3(O)C(=Nc4cccc(-c5ccccc5)c43)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.1c01273
	145961131	161657	None	0	Human	Functional	pEC50	=	6.7	6.7	1	3	Agonist activity at MOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assayAgonist activity at MOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assay	ChEMBL	1080	12	10	14	0.8	CC1(C)SSC(C)(C)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCN(CC2)C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1016/j.bmc.2018.05.045
	CHEMBL4128853	161657	None	0	Human	Functional	pEC50	=	6.7	6.7	1	3	Agonist activity at MOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assayAgonist activity at MOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assay	ChEMBL	1080	12	10	14	0.8	CC1(C)SSC(C)(C)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCN(CC2)C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1016/j.bmc.2018.05.045
	172449739	195892	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	351	7	0	3	4.1	CCC(=O)N(CCCN1CCC(c2ccccc2)CC1)c1ccccn1	10.1021/acs.jmedchem.3c01637
	CHEMBL5412750	195892	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	351	7	0	3	4.1	CCC(=O)N(CCCN1CCC(c2ccccc2)CC1)c1ccccn1	10.1021/acs.jmedchem.3c01637
	156014932	177654	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting methodAgonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method	ChEMBL	601	14	8	8	0.4	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CN)NC(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1	10.1016/j.bmc.2020.115438
	CHEMBL4640310	177654	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting methodAgonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method	ChEMBL	601	14	8	8	0.4	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CN)NC(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1	10.1016/j.bmc.2020.115438
	168296046	192410	None	0	Rat	Functional	pEC50	=	6.7	6.7	-3	3	Agonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay	ChEMBL	529	7	0	6	5.2	COc1cccc(C(=O)[C@]2(C)C[C@@]34CC[C@]2(OC)[C@@H]2Oc5c(OC)ccc6c5[C@@]23CCN(CC2CC2)[C@@H]4C6)c1	10.1021/acs.jmedchem.2c00014
	CHEMBL5206165	192410	None	0	Rat	Functional	pEC50	=	6.7	6.7	-3	3	Agonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay	ChEMBL	529	7	0	6	5.2	COc1cccc(C(=O)[C@]2(C)C[C@@]34CC[C@]2(OC)[C@@H]2Oc5c(OC)ccc6c5[C@@]23CCN(CC2CC2)[C@@H]4C6)c1	10.1021/acs.jmedchem.2c00014
	CHEMBL5086786	217538	None	0	Human	Functional	pEC50	=	4.7	4.7	-	1	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 assayAgonist 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	ChEMBL		None	None	None		CC[C@@H]1CN2CC[C@@]3(O)C(=Nc4cccc(-c5ccccc5)c43)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.1c01273
	24800107	191970	None	0	Human	Functional	pEC50	=	6.7	6.7	-32	3	Agonist activity at human mu opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS binding	ChEMBL	437	3	1	5	5.4	CC1CN(c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)CC(C)N1	10.1021/jm7012979
	CHEMBL519925	191970	None	0	Human	Functional	pEC50	=	6.7	6.7	-32	3	Agonist activity at human mu opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS binding	ChEMBL	437	3	1	5	5.4	CC1CN(c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)CC(C)N1	10.1021/jm7012979
	CHEMBL5090537	217758	None	0	Human	Functional	pEC50	=	5.7	5.7	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL		None	None	None		COc1ccsc1CNCC[C@@]1(c2ccccn2)CCO[C@@]2(CCOC2)C1	10.1016/j.ejmech.2021.113986
	76320665	103393	None	0	Human	Functional	pEC50	=	5.7	5.7	-102	2	Agonist activity at human mu opioid assessed as stimulation of GTPgammaS bindingAgonist activity at human mu opioid assessed as stimulation of GTPgammaS binding	ChEMBL	479	5	1	3	6.1	CC(=O)N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl	10.1016/j.bmcl.2009.03.057
	CHEMBL3084549	103393	None	0	Human	Functional	pEC50	=	5.7	5.7	-102	2	Agonist activity at human mu opioid assessed as stimulation of GTPgammaS bindingAgonist activity at human mu opioid assessed as stimulation of GTPgammaS binding	ChEMBL	479	5	1	3	6.1	CC(=O)N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl	10.1016/j.bmcl.2009.03.057
	1627	2594	None	9	Rat	Functional	pEC50	=	6.7	6.7	1	9	Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm400050y
	1845	2594	None	9	Rat	Functional	pEC50	=	6.7	6.7	1	9	Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm400050y
	5288826	2594	None	9	Rat	Functional	pEC50	=	6.7	6.7	1	9	Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm400050y
	5288826.0	2594	None	9	Rat	Functional	pEC50	=	6.7	6.7	1	9	Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm400050y
	CHEMBL70	2594	None	9	Rat	Functional	pEC50	=	6.7	6.7	1	9	Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm400050y
	DB00295	2594	None	9	Rat	Functional	pEC50	=	6.7	6.7	1	9	Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/jm400050y
	1627	2594	None	9	Rat	Functional	pEC50	=	6.7	6.7	1	9	Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.9b00219
	1845	2594	None	9	Rat	Functional	pEC50	=	6.7	6.7	1	9	Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.9b00219
	5288826	2594	None	9	Rat	Functional	pEC50	=	6.7	6.7	1	9	Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.9b00219
	5288826.0	2594	None	9	Rat	Functional	pEC50	=	6.7	6.7	1	9	Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.9b00219
	CHEMBL70	2594	None	9	Rat	Functional	pEC50	=	6.7	6.7	1	9	Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.9b00219
	DB00295	2594	None	9	Rat	Functional	pEC50	=	6.7	6.7	1	9	Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method	ChEMBL	285	0	2	4	1.2	O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1021/acs.jmedchem.9b00219
	CHEMBL5093399	217915	None	0	Human	Functional	pEC50	=	6.7	6.7	-10	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis	ChEMBL		None	None	None		Cc1cc(O)cc(C)c1C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O	10.1021/acs.jmedchem.0c02062
	162651091	180338	None	0	Human	Functional	pEC50	=	6.7	6.7	-1	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1116	23	14	15	-2.8	N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.0c01367
	CHEMBL4750006	180338	None	0	Human	Functional	pEC50	=	6.7	6.7	-1	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1116	23	14	15	-2.8	N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.0c01367
	162654268	180781	None	0	Human	Functional	pEC50	=	6.7	6.7	-1	4	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1126	33	15	14	-3.7	CN[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.6b01181
	CHEMBL4755334	180781	None	0	Human	Functional	pEC50	=	6.7	6.7	-1	4	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1126	33	15	14	-3.7	CN[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.6b01181
	71761638	91435	None	0	Rat	Functional	pEC50	=	5.7	5.7	-4	3	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	649	7	8	10	-2.0	NC(=O)[C@@H]1C/N=C(/N2CCCCC2)NC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1	10.1021/jm4008592
	CHEMBL2402930	91435	None	0	Rat	Functional	pEC50	=	5.7	5.7	-4	3	Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDPAgonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP	ChEMBL	649	7	8	10	-2.0	NC(=O)[C@@H]1C/N=C(/N2CCCCC2)NC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1	10.1021/jm4008592
	118567543	171471	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	463	4	0	4	4.2	O=C1N(c2cccnc2C(F)(F)F)CC2(CCN(CCc3ccccc3F)CC2)OC12CC2	10.1021/acs.jmedchem.0c01127
	118567543	171471	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	463	4	0	4	4.2	O=C1N(c2cccnc2C(F)(F)F)CC2(CCN(CCc3ccccc3F)CC2)OC12CC2	10.1021/acs.jmedchem.9b01256
	CHEMBL4461774	171471	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	463	4	0	4	4.2	O=C1N(c2cccnc2C(F)(F)F)CC2(CCN(CCc3ccccc3F)CC2)OC12CC2	10.1021/acs.jmedchem.0c01127
	CHEMBL4461774	171471	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	463	4	0	4	4.2	O=C1N(c2cccnc2C(F)(F)F)CC2(CCN(CCc3ccccc3F)CC2)OC12CC2	10.1021/acs.jmedchem.9b01256
	118567543	171471	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at mu-opioid receptor (unknown origin)Agonist activity at mu-opioid receptor (unknown origin)	ChEMBL	463	4	0	4	4.2	O=C1N(c2cccnc2C(F)(F)F)CC2(CCN(CCc3ccccc3F)CC2)OC12CC2	10.1021/acs.jmedchem.3c01637
	CHEMBL4461774	171471	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at mu-opioid receptor (unknown origin)Agonist activity at mu-opioid receptor (unknown origin)	ChEMBL	463	4	0	4	4.2	O=C1N(c2cccnc2C(F)(F)F)CC2(CCN(CCc3ccccc3F)CC2)OC12CC2	10.1021/acs.jmedchem.3c01637
	162651091	180338	None	0	Human	Functional	pEC50	=	6.7	6.7	-1	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1116	23	14	15	-2.8	N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.0c01367
	CHEMBL4750006	180338	None	0	Human	Functional	pEC50	=	6.7	6.7	-1	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1116	23	14	15	-2.8	N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.0c01367
	162654268	180781	None	0	Human	Functional	pEC50	=	6.7	6.7	-1	4	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1126	33	15	14	-3.7	CN[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.6b01181
	CHEMBL4755334	180781	None	0	Human	Functional	pEC50	=	6.7	6.7	-1	4	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1126	33	15	14	-3.7	CN[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.6b01181
	90199005	160061	None	0	Human	Functional	pEC50	=	6.7	6.7	-1	2	GTPgammaS Functional Assay (mu): [35S]GTPgammaS functional assays were conducted using freshly thawed pt-receptor membranes prepared in-house from a cell line expressing recombinant mu opioid receptor in a HEK-293, CHO cell background, or purchased from a commercial source (Perkin Elmer, Shelton, Conn.; or DiscovRx, Fremont, Calif.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2,20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B.GTPgammaS Functional Assay (mu): [35S]GTPgammaS functional assays were conducted using freshly thawed pt-receptor membranes prepared in-house from a cell line expressing recombinant mu opioid receptor in a HEK-293, CHO cell background, or purchased from a commercial source (Perkin Elmer, Shelton, Conn.; or DiscovRx, Fremont, Calif.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2,20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B.	ChEMBL	561	9	3	7	3.6	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H]([C@](O)(CC(O)CO)c1ccccc1)C2	nan
	CHEMBL4107541	160061	None	0	Human	Functional	pEC50	=	6.7	6.7	-1	2	GTPgammaS Functional Assay (mu): [35S]GTPgammaS functional assays were conducted using freshly thawed pt-receptor membranes prepared in-house from a cell line expressing recombinant mu opioid receptor in a HEK-293, CHO cell background, or purchased from a commercial source (Perkin Elmer, Shelton, Conn.; or DiscovRx, Fremont, Calif.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2,20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B.GTPgammaS Functional Assay (mu): [35S]GTPgammaS functional assays were conducted using freshly thawed pt-receptor membranes prepared in-house from a cell line expressing recombinant mu opioid receptor in a HEK-293, CHO cell background, or purchased from a commercial source (Perkin Elmer, Shelton, Conn.; or DiscovRx, Fremont, Calif.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2,20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B.	ChEMBL	561	9	3	7	3.6	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H]([C@](O)(CC(O)CO)c1ccccc1)C2	nan
	130431382	163985	None	0	Human	Functional	pEC50	=	5.7	5.7	-	1	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 assayAgonist 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	ChEMBL	375	3	1	3	4.5	O=c1[nH]c2c(Cl)cccc2n1C1CCN(Cc2ccccc2Cl)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4207047	163985	None	0	Human	Functional	pEC50	=	5.7	5.7	-	1	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 assayAgonist 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	ChEMBL	375	3	1	3	4.5	O=c1[nH]c2c(Cl)cccc2n1C1CCN(Cc2ccccc2Cl)CC1	10.1021/acs.jmedchem.8b01136
	81689720	111855	None	0	Human	Functional	pEC50	=	6.7	6.7	-77	3	Agonist activity at mu-opioid receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at mu-opioid receptor (unknown origin) by [35S]GTPgammaS binding assay	ChEMBL	396	2	1	3	4.6	Oc1ccc2c(c1)[C@]13CCN(CC4CC4)C[C@@]1(C2)Cc1cc2ccccc2nc1C3	10.1016/j.bmcl.2014.04.098
	CHEMBL3287467	111855	None	0	Human	Functional	pEC50	=	6.7	6.7	-77	3	Agonist activity at mu-opioid receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at mu-opioid receptor (unknown origin) by [35S]GTPgammaS binding assay	ChEMBL	396	2	1	3	4.6	Oc1ccc2c(c1)[C@]13CCN(CC4CC4)C[C@@]1(C2)Cc1cc2ccccc2nc1C3	10.1016/j.bmcl.2014.04.098
	124037299	148136	None	0	Human	Functional	pEC50	=	4.7	4.7	-	1	HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.	ChEMBL	445	11	0	7	2.2	COCCOCCOCCO[C@H]1C=CC2C3Cc4ccc(OC)c5c4[C@@]2(CCN3C)C1O5	nan
	CHEMBL3934684	148136	None	0	Human	Functional	pEC50	=	4.7	4.7	-	1	HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.HiRange Homogenous Time-Resolved Fluorescence (HTRF) Assay: Briefly, suspensions of cells expressing either the mu, kappa or delta opioid receptors were prepared in buffer containing 0.5 mM isobutyl-methyl xanthine (IBMX). Cells were incubated with varying concentrations of PEG-opioid conjugates and 3 uM forskolin for 30 minutes at room temperature. cAMP was detected following a two-step assay protocol per the manufacturer's instructions and time resolved fluorescence was measured with the following settings: 330 nm excitation; 620 nm and 665 nm emission; 380 nm dichroic mirror. The 665 nm/620 nm ratio is expressed as Delta F % and test compound-related data is expressed as a percentage of average maximum response in wells without forskolin. EC50 values were calculated for each compound from a sigmoidal dose-response plot of concentrations versus maximum response.	ChEMBL	445	11	0	7	2.2	COCCOCCOCCO[C@H]1C=CC2C3Cc4ccc(OC)c5c4[C@@]2(CCN3C)C1O5	nan
	3655995	108801	None	1	Human	Functional	pEC50	=	5.7	5.7	-11	2	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis	ChEMBL	306	3	0	2	3.2	O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1	10.1016/j.bmcl.2013.03.101
	CHEMBL320874	108801	None	1	Human	Functional	pEC50	=	5.7	5.7	-11	2	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis	ChEMBL	306	3	0	2	3.2	O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1	10.1016/j.bmcl.2013.03.101
	118567606	175665	None	0	Human	Functional	pEC50	=	5.7	5.7	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	365	4	0	4	2.9	CC1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccn2)C1=O	10.1021/acs.jmedchem.9b01256
	CHEMBL4578955	175665	None	0	Human	Functional	pEC50	=	5.7	5.7	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	365	4	0	4	2.9	CC1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccn2)C1=O	10.1021/acs.jmedchem.9b01256
	118567747	172631	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	383	4	0	4	3.1	CC1OC2(CCN(CCc3ccccc3)CC2)CN(c2ncccc2F)C1=O	10.1021/acs.jmedchem.9b01256
	CHEMBL4483643	172631	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	383	4	0	4	3.1	CC1OC2(CCN(CCc3ccccc3)CC2)CN(c2ncccc2F)C1=O	10.1021/acs.jmedchem.9b01256
	10832076	38062	None	0	Human	Functional	pEC50	=	6.7	6.7	-5	4	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 assayAgonist 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	ChEMBL	355	3	1	4	4.8	CC(c1ccccc1Cl)N1CCC(n2c(O)nc3ccccc32)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL146054	38062	None	0	Human	Functional	pEC50	=	6.7	6.7	-5	4	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 assayAgonist 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	ChEMBL	355	3	1	4	4.8	CC(c1ccccc1Cl)N1CCC(n2c(O)nc3ccccc32)CC1	10.1021/acs.jmedchem.8b01136
	1647	1313	None	34	Human	Functional	pEC50	=	6.7	6.7	-3	9	Agonist activity at human mu opioid receptor expressed in CHO-K1 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO-K1 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay	ChEMBL		None	None	None		None	10.1021/acs.jnatprod.0c01036
	5462471	1313	None	34	Human	Functional	pEC50	=	6.7	6.7	-3	9	Agonist activity at human mu opioid receptor expressed in CHO-K1 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO-K1 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay	ChEMBL		None	None	None		None	10.1021/acs.jnatprod.0c01036
	CHEMBL113995	1313	None	34	Human	Functional	pEC50	=	6.7	6.7	-3	9	Agonist activity at human mu opioid receptor expressed in CHO-K1 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO-K1 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay	ChEMBL		None	None	None		None	10.1021/acs.jnatprod.0c01036
	CHEMBL38874	1313	None	34	Human	Functional	pEC50	=	6.7	6.7	-3	9	Agonist activity at human mu opioid receptor expressed in CHO-K1 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human mu opioid receptor expressed in CHO-K1 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay	ChEMBL		None	None	None		None	10.1021/acs.jnatprod.0c01036
	68314236	93210	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	351	6	1	4	4.0	c1ccc([C@]2(CCNCc3cccnc3)CCOC3(CCCC3)C2)nc1	10.1021/jm4010829
	CHEMBL2443274	93210	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	351	6	1	4	4.0	c1ccc([C@]2(CCNCc3cccnc3)CCOC3(CCCC3)C2)nc1	10.1021/jm4010829
	155515973	170122	None	0	Human	Functional	pEC50	=	5.7	5.7	-10	3	Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 minsAgonist activity at mu-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins	ChEMBL	1165	30	12	11	2.7	N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O	10.1016/j.bmc.2019.01.003
	CHEMBL4442534	170122	None	0	Human	Functional	pEC50	=	5.7	5.7	-10	3	Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 minsAgonist activity at mu-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins	ChEMBL	1165	30	12	11	2.7	N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O	10.1016/j.bmc.2019.01.003
	CHEMBL336381	214042	None	0	Rat	Functional	pEC50	=	8.7	8.7	-2	4	Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm050921q
	1647	1313	None	34	Human	Functional	pEC50	=	8.7	8.7	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1016/j.ejmech.2022.114649
	5462471	1313	None	34	Human	Functional	pEC50	=	8.7	8.7	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1016/j.ejmech.2022.114649
	CHEMBL113995	1313	None	34	Human	Functional	pEC50	=	8.7	8.7	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1016/j.ejmech.2022.114649
	CHEMBL38874	1313	None	34	Human	Functional	pEC50	=	8.7	8.7	-3	9	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 assayAgonist 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	ChEMBL		None	None	None		None	10.1016/j.ejmech.2022.114649
	118562403	180257	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	378	5	0	3	3.5	CC1OC2(CCN(CCc3ccccc3)CC2)CN(Cc2ccccc2)C1=O	10.1021/acs.jmedchem.0c01127
	CHEMBL4748898	180257	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	ChEMBL	378	5	0	3	3.5	CC1OC2(CCN(CCc3ccccc3)CC2)CN(Cc2ccccc2)C1=O	10.1021/acs.jmedchem.0c01127
	45483978	201396	None	0	Human	Functional	pEC50	=	8.7	8.7	-4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	774	15	0	7	9.8	C=CCN1CC[C@]23c4c5ccc(OC(=O)CCCCCCCCC(=O)Oc6ccc7c(c6)[C@@]68CCCC[C@H]6C(C7)N(CC6CCC6)CC8)c4O[C@H]2CCC[C@H]3[C@H]1C5	10.1021/jm900379p
	CHEMBL584791	201396	None	0	Human	Functional	pEC50	=	8.7	8.7	-4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	774	15	0	7	9.8	C=CCN1CC[C@]23c4c5ccc(OC(=O)CCCCCCCCC(=O)Oc6ccc7c(c6)[C@@]68CCCC[C@H]6C(C7)N(CC6CCC6)CC8)c4O[C@H]2CCC[C@H]3[C@H]1C5	10.1021/jm900379p
	139568897	195642	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Agonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assayAgonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assay	ChEMBL	380	7	2	3	3.6	Cc1cc(O)cc(C)c1C[C@@H](CNC(=O)[C@@H]1C[C@@]1(C)c1ccccc1)N(C)C	10.1016/j.bmcl.2023.129405
	CHEMBL5407881	195642	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Agonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assayAgonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assay	ChEMBL	380	7	2	3	3.6	Cc1cc(O)cc(C)c1C[C@@H](CNC(=O)[C@@H]1C[C@@]1(C)c1ccccc1)N(C)C	10.1016/j.bmcl.2023.129405
	54582933	62098	None	0	Human	Functional	pEC50	=	8.7	8.7	2	2	Agonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	820	15	2	10	7.2	C=CCN1CC[C@]23c4c5ccc(OC(=O)CCCCCCCCC(=O)Oc6ccc7c(c6)[C@@]68CCCC[C@@]6(O)[C@@H](C7)N(CC6CCC6)CC8)c4O[C@H]2C(=O)CC[C@@]3(O)[C@H]1C5	10.1016/j.bmc.2011.03.052
	CHEMBL1774950	62098	None	0	Human	Functional	pEC50	=	8.7	8.7	2	2	Agonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	820	15	2	10	7.2	C=CCN1CC[C@]23c4c5ccc(OC(=O)CCCCCCCCC(=O)Oc6ccc7c(c6)[C@@]68CCCC[C@@]6(O)[C@@H](C7)N(CC6CCC6)CC8)c4O[C@H]2C(=O)CC[C@@]3(O)[C@H]1C5	10.1016/j.bmc.2011.03.052
	71452742	79144	None	0	Human	Functional	pEC50	=	8.7	8.7	-4	2	Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	804	15	1	9	8.1	C=CCN1CC[C@]23c4c5ccc(OC(=O)CCCCCCCCC(=O)Oc6ccc7c(c6)[C@@]68CCCCC6[C@@H](C7)N(CC6CCC6)CC8)c4O[C@H]2C(=O)CC[C@@]3(O)[C@H]1C5	10.1021/jm061327z
	CHEMBL2113275	79144	None	0	Human	Functional	pEC50	=	8.7	8.7	-4	2	Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	804	15	1	9	8.1	C=CCN1CC[C@]23c4c5ccc(OC(=O)CCCCCCCCC(=O)Oc6ccc7c(c6)[C@@]68CCCCC6[C@@H](C7)N(CC6CCC6)CC8)c4O[C@H]2C(=O)CC[C@@]3(O)[C@H]1C5	10.1021/jm061327z
	155545759	173596	None	0	Mouse	Functional	pEC50	=	8.7	8.7	147	2	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 analysisAgonist 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	ChEMBL	400	4	2	7	2.6	CC[C@@H]1CN2CC[C@]3(Nc4cccc(O)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.6b00748
	CHEMBL4530421	173596	None	0	Mouse	Functional	pEC50	=	8.7	8.7	147	2	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 analysisAgonist 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	ChEMBL	400	4	2	7	2.6	CC[C@@H]1CN2CC[C@]3(Nc4cccc(O)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.6b00748
	CHEMBL5077763	217002	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL		None	None	None		c1ccc([C@]2(CCNCc3scc4c3COC4)CCOC3(CCCC3)C2)nc1	10.1016/j.ejmech.2021.113986
	9909946	138370	None	0	Human	Functional	pEC50	=	8.7	8.7	18	3	Agonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay	ChEMBL	418	5	3	4	4.0	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CCCC[C@H]1c1nc(-c2ccccc2)c[nH]1	10.1016/j.bmcl.2012.05.042
	CHEMBL377069	138370	None	0	Human	Functional	pEC50	=	8.7	8.7	18	3	Agonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay	ChEMBL	418	5	3	4	4.0	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CCCC[C@H]1c1nc(-c2ccccc2)c[nH]1	10.1016/j.bmcl.2012.05.042
	25260181	189173	None	0	Rat	Functional	pEC50	=	8.7	8.7	-2	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	562	8	2	5	5.4	O=C(/C=C/c1ccccc1)N[C@@H]1CC[C@@]2(OCc3ccccc3)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/jm8015552
	CHEMBL509552	189173	None	0	Rat	Functional	pEC50	=	8.7	8.7	-2	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	562	8	2	5	5.4	O=C(/C=C/c1ccccc1)N[C@@H]1CC[C@@]2(OCc3ccccc3)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/jm8015552
	71625028	87910	None	0	Rat	Functional	pEC50	=	8.7	8.7	-8	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	507	7	2	5	5.3	CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)CCC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338716	87910	None	0	Rat	Functional	pEC50	=	8.7	8.7	-8	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	507	7	2	5	5.3	CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)CCC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL5090510	217756	None	0	Mouse	Functional	pEC50	=	8.7	8.7	-	1	Antagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method	ChEMBL		None	None	None		O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ncc[nH]1	10.1021/acs.jmedchem.1c02185
	CHEMBL5076290	218020	None	0	Mouse	Functional	pEC50	=	8.7	8.7	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc[nH]c1	10.1021/acs.jmedchem.2c00087
	CHEMBL5095592	218020	None	0	Mouse	Functional	pEC50	=	8.7	8.7	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc[nH]c1	10.1021/acs.jmedchem.2c00087
	CHEMBL1927270	211551	None	0	Human	Functional	pEC50	=	8.7	8.7	-3	6	Agonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assay	ChEMBL		None	None	None		NC(=O)[C@@H]1CC(=O)NCCCC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1	10.1021/acs.jmedchem.0c01915
	CHEMBL1927270	211551	None	0	Human	Functional	pEC50	=	8.7	8.7	-3	6	Agonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysisAgonist activity at human recombinant MOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis	ChEMBL		None	None	None		NC(=O)[C@@H]1CC(=O)NCCCC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1	10.1016/j.ejmech.2015.12.012
	164620873	188654	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2ccncc12	10.1016/j.bmcl.2021.127953
	CHEMBL4864454	188654	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2ccncc12	10.1016/j.bmcl.2021.127953
	CHEMBL5028618	188654	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2ccncc12	10.1016/j.bmcl.2021.127953
	164624221	188689	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2ccncc12	10.1016/j.bmcl.2021.127953
	CHEMBL4868660	188689	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2ccncc12	10.1016/j.bmcl.2021.127953
	CHEMBL5028813	188689	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Partial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	484	4	4	6	2.4	O=C(N[C@H]1C=C[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1c[nH]c2ccncc12	10.1016/j.bmcl.2021.127953
	CHEMBL5076048	216900	None	0	Mouse	Functional	pEC50	=	8.7	8.7	-	1	Antagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method	ChEMBL		None	None	None		O=C(Cc1ncc[nH]1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.1c02185
	156017329	177740	None	0	Human	Functional	pEC50	=	8.7	8.7	1	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	613	9	1	6	6.9	CN(C)c1ccc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)cc1	10.1021/acs.jmedchem.0c00503
	CHEMBL4641271	177740	None	0	Human	Functional	pEC50	=	8.7	8.7	1	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	613	9	1	6	6.9	CN(C)c1ccc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)cc1	10.1021/acs.jmedchem.0c00503
	127049273	141102	None	0	Rat	Functional	pEC50	=	8.7	8.7	2	2	Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay	ChEMBL	511	7	3	4	4.9	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CCC2)c2ccc(Cc3ccccc3)cc21	10.1021/acs.jmedchem.6b00308
	CHEMBL3823787	141102	None	0	Rat	Functional	pEC50	=	8.7	8.7	2	2	Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay	ChEMBL	511	7	3	4	4.9	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CCC2)c2ccc(Cc3ccccc3)cc21	10.1021/acs.jmedchem.6b00308
	44565363	189565	None	0	Rat	Functional	pEC50	=	8.7	8.7	-2	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	502	6	3	6	3.2	COc1ccccc1/C=C/C(=O)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/jm8015552
	CHEMBL513598	189565	None	0	Rat	Functional	pEC50	=	8.7	8.7	-2	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	502	6	3	6	3.2	COc1ccccc1/C=C/C(=O)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/jm8015552
	71624445	87939	None	0	Rat	Functional	pEC50	=	8.7	8.7	-25	3	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	453	5	2	5	4.0	CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338743	87939	None	0	Rat	Functional	pEC50	=	8.7	8.7	-25	3	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	453	5	2	5	4.0	CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	86582747	154081	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	354	3	2	3	3.4	NC(=O)c1ccc2c(c1O)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	nan
	CHEMBL3983967	154081	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	354	3	2	3	3.4	NC(=O)c1ccc2c(c1O)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3	nan
	11694	3673	None	0	Human	Functional	pEC50	=	8.7	8.7	-1	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting analysisAgonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting analysis	ChEMBL	564	6	1	5	6.7	CN1CC[C@]23[C@H]4Oc5c(O)ccc(C[C@@H]1[C@@]2(Cc1c4ncc(c1)c1ccc(Cl)cc1)OCCCc1ccccc1)c35	10.1021/jm300686p
	71460944	3673	None	0	Human	Functional	pEC50	=	8.7	8.7	-1	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting analysisAgonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting analysis	ChEMBL	564	6	1	5	6.7	CN1CC[C@]23[C@H]4Oc5c(O)ccc(C[C@@H]1[C@@]2(Cc1c4ncc(c1)c1ccc(Cl)cc1)OCCCc1ccccc1)c35	10.1021/jm300686p
	CHEMBL2179656	3673	None	0	Human	Functional	pEC50	=	8.7	8.7	-1	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting analysisAgonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting analysis	ChEMBL	564	6	1	5	6.7	CN1CC[C@]23[C@H]4Oc5c(O)ccc(C[C@@H]1[C@@]2(Cc1c4ncc(c1)c1ccc(Cl)cc1)OCCCc1ccccc1)c35	10.1021/jm300686p
	44427179	96631	None	0	Human	Functional	pEC50	=	8.7	8.7	-5	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	ChEMBL	430	5	1	3	5.4	O=C(NCc1ccccc1)Oc1ccc2c(c1)C13CCCCC1C(C2)N(CC1CC1)CC3	10.1016/j.bmcl.2007.01.013
	CHEMBL263096	96631	None	0	Human	Functional	pEC50	=	8.7	8.7	-5	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	ChEMBL	430	5	1	3	5.4	O=C(NCc1ccccc1)Oc1ccc2c(c1)C13CCCCC1C(C2)N(CC1CC1)CC3	10.1016/j.bmcl.2007.01.013
	CHEMBL2387328	212866	None	0	Rat	Functional	pEC50	=	8.7	8.7	-1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL		None	None	None		C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCC(=O)NCCCCCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)C(=O)N[C@@H](Cc1c(F)c(F)c(F)c(F)c1F)C(N)=O	10.1016/j.bmcl.2013.03.065
	155536455	176361	None	0	Rat	Functional	pEC50	=	8.7	8.7	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	480	6	4	5	4.7	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3cnc4ccccc4c3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4473177	176361	None	0	Rat	Functional	pEC50	=	8.7	8.7	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	480	6	4	5	4.7	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3cnc4ccccc4c3)cc21	10.1021/acs.jmedchem.9b00378
	CHEMBL4594933	176361	None	0	Rat	Functional	pEC50	=	8.7	8.7	-	1	Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr	ChEMBL	480	6	4	5	4.7	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3cnc4ccccc4c3)cc21	10.1021/acs.jmedchem.9b00378
	86582906	145153	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	302	4	1	3	2.0	COCCN1CC[C@@]2(C)c3cc(C(N)=O)ccc3C[C@@H]1[C@@H]2C	nan
	CHEMBL3911427	145153	None	0	Human	Functional	pEC50	=	8.7	8.7	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	302	4	1	3	2.0	COCCN1CC[C@@]2(C)c3cc(C(N)=O)ccc3C[C@@H]1[C@@H]2C	nan
	44240971	88196	None	0	Human	Functional	pEC50	=	8.7	8.7	-3	2	Partial 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 countingPartial 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	ChEMBL	479	7	1	3	5.7	C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccncc5)cc4)cc3[C@@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2013.01.117
	CHEMBL2347235	88196	None	0	Human	Functional	pEC50	=	8.7	8.7	-3	2	Partial 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 countingPartial 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	ChEMBL	479	7	1	3	5.7	C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccncc5)cc4)cc3[C@@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2013.01.117
	CHEMBL5088630	218047	None	0	Mouse	Functional	pEC50	=	8.7	8.7	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc[nH]c1	10.1021/acs.jmedchem.2c00087
	CHEMBL5095898	218047	None	0	Mouse	Functional	pEC50	=	8.7	8.7	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc[nH]c1	10.1021/acs.jmedchem.2c00087
	155526659	176602	None	0	Mouse	Functional	pEC50	=	8.7	8.7	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccoc2c1	10.1021/acs.jmedchem.9b01767
	CHEMBL4459104	176602	None	0	Mouse	Functional	pEC50	=	8.7	8.7	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccoc2c1	10.1021/acs.jmedchem.9b01767
	CHEMBL4596745	176602	None	0	Mouse	Functional	pEC50	=	8.7	8.7	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	486	4	3	6	3.5	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccoc2c1	10.1021/acs.jmedchem.9b01767
	168277640	190268	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity at MOP (unknown origin) stably expressed in HEK293 cells assessed as forskolin stimulated cAMP accumulation incubated for 30 mins by radioactivity based scintillation counter analysisAgonist activity at MOP (unknown origin) stably expressed in HEK293 cells assessed as forskolin stimulated cAMP accumulation incubated for 30 mins by radioactivity based scintillation counter analysis	ChEMBL	610	13	6	6	2.2	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](C)N(C)C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccccc1	10.1021/acs.jmedchem.0c01915
	CHEMBL5173837	190268	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity at MOP (unknown origin) stably expressed in HEK293 cells assessed as forskolin stimulated cAMP accumulation incubated for 30 mins by radioactivity based scintillation counter analysisAgonist activity at MOP (unknown origin) stably expressed in HEK293 cells assessed as forskolin stimulated cAMP accumulation incubated for 30 mins by radioactivity based scintillation counter analysis	ChEMBL	610	13	6	6	2.2	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](C)N(C)C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccccc1	10.1021/acs.jmedchem.0c01915
	25233078	193310	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	497	4	3	6	3.3	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cnc2ccccc2c1	10.1021/jm801272c
	CHEMBL523382	193310	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	497	4	3	6	3.3	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cnc2ccccc2c1	10.1021/jm801272c
	154594323	175237	None	0	Mouse	Functional	pEC50	=	8.6	8.6	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	475	5	3	6	2.7	CCc1cnccc1C(=O)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.8b01158
	CHEMBL4569785	175237	None	0	Mouse	Functional	pEC50	=	8.6	8.6	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	475	5	3	6	2.7	CCc1cnccc1C(=O)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.8b01158
	CHEMBL5081993	217269	None	0	Human	Functional	pEC50	=	8.6	8.6	-1	3	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human mu opioid receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay	ChEMBL		None	None	None		Cc1cc(O)cc(C)c1C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O	10.1021/acs.jmedchem.0c02062
	24822630	97916	None	0	Human	Functional	pEC50	=	8.6	8.6	-22	4	Activity at mu opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at mu opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	514	4	3	5	4.1	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)c(Cl)c1	10.1016/j.bmc.2009.07.069
	CHEMBL272215	97916	None	0	Human	Functional	pEC50	=	8.6	8.6	-22	4	Activity at mu opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at mu opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	514	4	3	5	4.1	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)c(Cl)c1	10.1016/j.bmc.2009.07.069
	CHEMBL593215	97916	None	0	Human	Functional	pEC50	=	8.6	8.6	-22	4	Activity at mu opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at mu opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	514	4	3	5	4.1	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)c(Cl)c1	10.1016/j.bmc.2009.07.069
	9848990	189274	None	0	Human	Functional	pEC50	=	8.6	8.6	-3	7	Activity was evaluated in human mu opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assayActivity was evaluated in human mu opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assay	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1016/s0960-894x(99)00085-2
	9848990.0	189274	None	0	Human	Functional	pEC50	=	8.6	8.6	-3	7	Activity was evaluated in human mu opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assayActivity was evaluated in human mu opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assay	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1016/s0960-894x(99)00085-2
	CHEMBL2368861	189274	None	0	Human	Functional	pEC50	=	8.6	8.6	-3	7	Activity was evaluated in human mu opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assayActivity was evaluated in human mu opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assay	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1016/s0960-894x(99)00085-2
	CHEMBL511142	189274	None	0	Human	Functional	pEC50	=	8.6	8.6	-3	7	Activity was evaluated in human mu opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assayActivity was evaluated in human mu opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assay	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1016/s0960-894x(99)00085-2
	CHEMBL5094951	218013	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity at human MOR expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 60 mins by cAMP HTRF assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 60 mins by cAMP HTRF assay	ChEMBL		None	None	None		CCC(=O)N(CC(C)N1CCC(Cc2ccccc2)CC1)c1ccccc1	10.1016/j.ejmech.2021.113879
	162667205	183842	None	0	Rat	Functional	pEC50	=	8.6	8.6	47	3	Agonist activity at rat mu opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat mu opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	369	4	3	4	2.7	CN(C)CC1CN(C(=O)Nc2ccccc2)CCC1(O)c1cccc(O)c1	10.1016/j.ejmech.2020.112070
	CHEMBL4786173	183842	None	0	Rat	Functional	pEC50	=	8.6	8.6	47	3	Agonist activity at rat mu opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat mu opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	369	4	3	4	2.7	CN(C)CC1CN(C(=O)Nc2ccccc2)CCC1(O)c1cccc(O)c1	10.1016/j.ejmech.2020.112070
	CHEMBL4803577	183842	None	0	Rat	Functional	pEC50	=	8.6	8.6	47	3	Agonist activity at rat mu opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat mu opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	369	4	3	4	2.7	CN(C)CC1CN(C(=O)Nc2ccccc2)CCC1(O)c1cccc(O)c1	10.1016/j.ejmech.2020.112070
	86582904	144233	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	312	3	1	2	3.1	C[C@H]1[C@H]2Cc3ccc(C(N)=O)cc3[C@]1(C)CCN2CC1CCC1	nan
	CHEMBL3903900	144233	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	312	3	1	2	3.1	C[C@H]1[C@H]2Cc3ccc(C(N)=O)cc3[C@]1(C)CCN2CC1CCC1	nan
	9848990	189274	None	0	Human	Functional	pEC50	=	8.6	8.6	-3	7	GTPgammaS binding in cloned human Opioid receptor mu 1 transfected into hamster ovary cellsGTPgammaS binding in cloned human Opioid receptor mu 1 transfected into hamster ovary cells	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm991165p
	9848990.0	189274	None	0	Human	Functional	pEC50	=	8.6	8.6	-3	7	GTPgammaS binding in cloned human Opioid receptor mu 1 transfected into hamster ovary cellsGTPgammaS binding in cloned human Opioid receptor mu 1 transfected into hamster ovary cells	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm991165p
	CHEMBL2368861	189274	None	0	Human	Functional	pEC50	=	8.6	8.6	-3	7	GTPgammaS binding in cloned human Opioid receptor mu 1 transfected into hamster ovary cellsGTPgammaS binding in cloned human Opioid receptor mu 1 transfected into hamster ovary cells	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm991165p
	CHEMBL511142	189274	None	0	Human	Functional	pEC50	=	8.6	8.6	-3	7	GTPgammaS binding in cloned human Opioid receptor mu 1 transfected into hamster ovary cellsGTPgammaS binding in cloned human Opioid receptor mu 1 transfected into hamster ovary cells	ChEMBL	467	4	2	5	4.4	CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm991165p
	58443192	84217	None	0	Human	Functional	pEC50	=	8.6	8.6	-1	3	Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	536	9	1	3	7.0	CC(C)Oc1ccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)cc1	10.1016/j.bmcl.2012.10.081
	CHEMBL2208361	84217	None	0	Human	Functional	pEC50	=	8.6	8.6	-1	3	Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	536	9	1	3	7.0	CC(C)Oc1ccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)cc1	10.1016/j.bmcl.2012.10.081
	12733	1535	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL	377	6	2	3	4.3	OC/C=C/[C@H]1[C@H]2N(CC[C@@]1(CCC2)C=3C=C(C=CC3)O)CCC4=CC=CC=C4	10.1039/d0md00104j
	155771774	1535	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL	377	6	2	3	4.3	OC/C=C/[C@H]1[C@H]2N(CC[C@@]1(CCC2)C=3C=C(C=CC3)O)CCC4=CC=CC=C4	10.1039/d0md00104j
	CHEMBL4752583	1535	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay	ChEMBL	377	6	2	3	4.3	OC/C=C/[C@H]1[C@H]2N(CC[C@@]1(CCC2)C=3C=C(C=CC3)O)CCC4=CC=CC=C4	10.1039/d0md00104j
	156020282	178188	None	0	Human	Functional	pEC50	=	8.6	8.6	1	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	584	8	1	5	7.1	Cc1ccc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)cc1	10.1021/acs.jmedchem.0c00503
	CHEMBL4647696	178188	None	0	Human	Functional	pEC50	=	8.6	8.6	1	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	584	8	1	5	7.1	Cc1ccc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)cc1	10.1021/acs.jmedchem.0c00503
	CHEMBL5091983	218039	None	0	Mouse	Functional	pEC50	=	8.6	8.6	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(CCc1ccoc1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	CHEMBL5095833	218039	None	0	Mouse	Functional	pEC50	=	8.6	8.6	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(CCc1ccoc1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	56658452	66635	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	481	4	3	6	2.8	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1Cl	10.1016/j.bmcl.2011.06.135
	CHEMBL1824514	66635	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	481	4	3	6	2.8	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1Cl	10.1016/j.bmcl.2011.06.135
	CHEMBL1852672	66635	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	481	4	3	6	2.8	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1Cl	10.1016/j.bmcl.2011.06.135
	56665407	66662	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	461	5	3	6	2.1	O=C(Cc1ccncc1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2011.06.135
	CHEMBL1824516	66662	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	461	5	3	6	2.1	O=C(Cc1ccncc1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2011.06.135
	CHEMBL1852814	66662	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	461	5	3	6	2.1	O=C(Cc1ccncc1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2011.06.135
	CHEMBL5075031	216843	None	0	Mouse	Functional	pEC50	=	8.6	8.6	-	1	Antagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method	ChEMBL		None	None	None		O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc[nH]n1	10.1021/acs.jmedchem.1c02185
	16733485	137300	None	0	Human	Functional	pEC50	=	8.6	8.6	-3	3	Agonist activity at human mu opioid receptor by [35S]GTP-gamma-S binding assayAgonist activity at human mu opioid receptor by [35S]GTP-gamma-S binding assay	ChEMBL	551	7	7	7	-0.5	N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1C/C=C\C[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O	10.1021/jm061048b
	CHEMBL375025	137300	None	0	Human	Functional	pEC50	=	8.6	8.6	-3	3	Agonist activity at human mu opioid receptor by [35S]GTP-gamma-S binding assayAgonist activity at human mu opioid receptor by [35S]GTP-gamma-S binding assay	ChEMBL	551	7	7	7	-0.5	N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1C/C=C\C[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O	10.1021/jm061048b
	66553195	93198	None	26	Mouse	Functional	pEC50	=	8.6	8.6	-2	5	Partial 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 assayPartial 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	ChEMBL	386	7	1	5	4.7	COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1	10.1021/acs.jmedchem.3c00417
	66553195.0	93198	None	26	Mouse	Functional	pEC50	=	8.6	8.6	-2	5	Partial 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 assayPartial 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	ChEMBL	386	7	1	5	4.7	COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1	10.1021/acs.jmedchem.3c00417
	CHEMBL2443262	93198	None	26	Mouse	Functional	pEC50	=	8.6	8.6	-2	5	Partial 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 assayPartial 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	ChEMBL	386	7	1	5	4.7	COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1	10.1021/acs.jmedchem.3c00417
	DB14881	93198	None	26	Mouse	Functional	pEC50	=	8.6	8.6	-2	5	Partial 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 assayPartial 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	ChEMBL	386	7	1	5	4.7	COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1	10.1021/acs.jmedchem.3c00417
	44427177	166599	None	0	Human	Functional	pEC50	=	8.6	8.6	-4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	ChEMBL	368	4	1	3	4.3	CCNC(=O)Oc1ccc2c(c1)C13CCCCC1C(C2)N(CC1CC1)CC3	10.1016/j.bmcl.2007.01.013
	CHEMBL427862	166599	None	0	Human	Functional	pEC50	=	8.6	8.6	-4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	ChEMBL	368	4	1	3	4.3	CCNC(=O)Oc1ccc2c(c1)C13CCCCC1C(C2)N(CC1CC1)CC3	10.1016/j.bmcl.2007.01.013
	66553195	93198	None	26	Mouse	Functional	pEC50	=	8.6	8.6	-2	5	Partial 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 assayPartial 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	ChEMBL	386	7	1	5	4.7	COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1	10.1021/acs.jmedchem.3c00417
	66553195.0	93198	None	26	Mouse	Functional	pEC50	=	8.6	8.6	-2	5	Partial 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 assayPartial 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	ChEMBL	386	7	1	5	4.7	COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1	10.1021/acs.jmedchem.3c00417
	CHEMBL2443262	93198	None	26	Mouse	Functional	pEC50	=	8.6	8.6	-2	5	Partial 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 assayPartial 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	ChEMBL	386	7	1	5	4.7	COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1	10.1021/acs.jmedchem.3c00417
	DB14881	93198	None	26	Mouse	Functional	pEC50	=	8.6	8.6	-2	5	Partial 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 assayPartial 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	ChEMBL	386	7	1	5	4.7	COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1	10.1021/acs.jmedchem.3c00417
	71459951	79173	None	0	Human	Functional	pEC50	=	8.6	8.6	-1	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	520	5	2	5	4.3	CO[C@@]12CC[C@@]3(C[C@@H]1CNC(=O)/C=C/c1ccc(Cl)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1021/jm070255o
	CHEMBL2113307	79173	None	0	Human	Functional	pEC50	=	8.6	8.6	-1	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	520	5	2	5	4.3	CO[C@@]12CC[C@@]3(C[C@@H]1CNC(=O)/C=C/c1ccc(Cl)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1021/jm070255o
	146408973	175156	None	0	Mouse	Functional	pEC50	=	8.6	8.6	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	529	5	3	6	4.2	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1C1CCCCC1	10.1021/acs.jmedchem.8b01158
	CHEMBL4567820	175156	None	0	Mouse	Functional	pEC50	=	8.6	8.6	-	1	Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins	ChEMBL	529	5	3	6	4.2	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1C1CCCCC1	10.1021/acs.jmedchem.8b01158
	155558237	176408	None	0	Mouse	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2sccc2c1	10.1021/acs.jmedchem.9b01767
	CHEMBL4560853	176408	None	0	Mouse	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2sccc2c1	10.1021/acs.jmedchem.9b01767
	CHEMBL4595221	176408	None	0	Mouse	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2sccc2c1	10.1021/acs.jmedchem.9b01767
	44406723	72793	None	0	Human	Functional	pEC50	=	8.6	8.6	-1	2	Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	762	13	1	8	8.0	CN1CC[C@]23c4c5ccc(OC(=O)CCCCCCCCC(=O)Oc6ccc7c(c6)[C@@]68CCCCC6[C@@H](C7)N(CC6CCC6)CC8)c4O[C@H]2[C@@H](O)C=C[C@H]3[C@H]1C5	10.1021/jm050577x
	CHEMBL199931	72793	None	0	Human	Functional	pEC50	=	8.6	8.6	-1	2	Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	762	13	1	8	8.0	CN1CC[C@]23c4c5ccc(OC(=O)CCCCCCCCC(=O)Oc6ccc7c(c6)[C@@]68CCCCC6[C@@H](C7)N(CC6CCC6)CC8)c4O[C@H]2[C@@H](O)C=C[C@H]3[C@H]1C5	10.1021/jm050577x
	121596705	3246	None	34	Human	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity at human MOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 5 mins with coelenterazine H followed by compound addition and measured after 15 mins by BRET assayAgonist activity at human MOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 5 mins with coelenterazine H followed by compound addition and measured after 15 mins by BRET assay	ChEMBL	361	8	3	4	2.9	C[C@@H](Cc1cscc1)NC(=O)NC[C@@H](N(C)C)Cc1ccc(cc1)O	10.1039/d0md00104j
	9286	3246	None	34	Human	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity at human MOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 5 mins with coelenterazine H followed by compound addition and measured after 15 mins by BRET assayAgonist activity at human MOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 5 mins with coelenterazine H followed by compound addition and measured after 15 mins by BRET assay	ChEMBL	361	8	3	4	2.9	C[C@@H](Cc1cscc1)NC(=O)NC[C@@H](N(C)C)Cc1ccc(cc1)O	10.1039/d0md00104j
	CHEMBL4467777	3246	None	34	Human	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity at human MOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 5 mins with coelenterazine H followed by compound addition and measured after 15 mins by BRET assayAgonist activity at human MOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 5 mins with coelenterazine H followed by compound addition and measured after 15 mins by BRET assay	ChEMBL	361	8	3	4	2.9	C[C@@H](Cc1cscc1)NC(=O)NC[C@@H](N(C)C)Cc1ccc(cc1)O	10.1039/d0md00104j
	DB14030	3246	None	34	Human	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity at human MOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 5 mins with coelenterazine H followed by compound addition and measured after 15 mins by BRET assayAgonist activity at human MOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 5 mins with coelenterazine H followed by compound addition and measured after 15 mins by BRET assay	ChEMBL	361	8	3	4	2.9	C[C@@H](Cc1cscc1)NC(=O)NC[C@@H](N(C)C)Cc1ccc(cc1)O	10.1039/d0md00104j
	16048864	169055	None	0	Human	Functional	pEC50	=	8.6	8.6	-1	3	Agonist activity at human mu opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assay	ChEMBL	512	7	1	2	6.9	C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccc(Cl)cc5)cc4)cc3[C@@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2007.09.082
	CHEMBL438871	169055	None	0	Human	Functional	pEC50	=	8.6	8.6	-1	3	Agonist activity at human mu opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assay	ChEMBL	512	7	1	2	6.9	C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccc(Cl)cc5)cc4)cc3[C@@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2007.09.082
	117706009	157789	None	0	Human	Functional	pEC50	=	8.6	8.6	-2	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assay	ChEMBL	492	4	1	5	3.3	O=S(=O)(c1ccccc1)N1C[C@H]2OC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21	10.1016/j.bmcl.2017.04.059
	CHEMBL4081856	157789	None	0	Human	Functional	pEC50	=	8.6	8.6	-2	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assay	ChEMBL	492	4	1	5	3.3	O=S(=O)(c1ccccc1)N1C[C@H]2OC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21	10.1016/j.bmcl.2017.04.059
	71624779	87930	None	0	Rat	Functional	pEC50	=	8.6	8.6	-5	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	521	7	2	5	5.7	CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)CCC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338734	87930	None	0	Rat	Functional	pEC50	=	8.6	8.6	-5	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	521	7	2	5	5.7	CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)CCC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL5081372	217232	None	0	Mouse	Functional	pEC50	=	8.6	8.6	-	1	Antagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method	ChEMBL		None	None	None		O=C(Cc1cc[nH]n1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.1c02185
	86582147	160855	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	338	3	1	2	3.6	NC(=O)c1ccc2c(c1)[C@@]13CCCCC1[C@@H](C2)N(CC1CCC1)CC3	nan
	CHEMBL4114055	160855	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	338	3	1	2	3.6	NC(=O)c1ccc2c(c1)[C@@]13CCCCC1[C@@H](C2)N(CC1CCC1)CC3	nan
	11849283	204309	None	0	Human	Functional	pEC50	=	8.6	8.6	30	3	Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR	ChEMBL	458	4	1	5	3.2	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccc(C)cc5)[C@@H](C2)N(C)CC[C@]314	10.1021/jm0604777
	CHEMBL607127	204309	None	0	Human	Functional	pEC50	=	8.6	8.6	30	3	Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR	ChEMBL	458	4	1	5	3.2	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccc(C)cc5)[C@@H](C2)N(C)CC[C@]314	10.1021/jm0604777
	44421400	84727	None	0	Human	Functional	pEC50	=	8.6	8.6	1	2	Activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	472	4	2	5	4.2	Oc1ccc2c3c1O[C@H]1c4c(c5c(n4CC4CC4)CCCC5)C[C@@]4(O)C(C2)N(CC2CC2)CC[C@]314	10.1021/jm040817t
	CHEMBL222597	84727	None	0	Human	Functional	pEC50	=	8.6	8.6	1	2	Activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	472	4	2	5	4.2	Oc1ccc2c3c1O[C@H]1c4c(c5c(n4CC4CC4)CCCC5)C[C@@]4(O)C(C2)N(CC2CC2)CC[C@]314	10.1021/jm040817t
	72712157	93208	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	384	6	1	3	5.3	Clc1cccc(CNCC[C@@]2(c3ccccn3)CCOC3(CCCC3)C2)c1	10.1021/jm4010829
	CHEMBL2443272	93208	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	ChEMBL	384	6	1	3	5.3	Clc1cccc(CNCC[C@@]2(c3ccccn3)CCOC3(CCCC3)C2)c1	10.1021/jm4010829
	CHEMBL3580745	214232	None	0	Human	Functional	pEC50	=	8.6	8.6	-4	5	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 assayAgonist 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	ChEMBL		None	None	None		Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(F)cc2)NC1=O	10.1021/acsmedchemlett.5b00056
	CHEMBL3582484	214255	None	0	Human	Functional	pEC50	=	8.6	8.6	-3	6	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 assayAgonist 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	ChEMBL		None	None	None		NC(=O)[C@@H]1CC(=O)NCCCC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1	10.1021/acsmedchemlett.5b00056
	71454517	79179	None	0	Human	Functional	pEC50	=	8.6	8.6	1	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	510	3	1	5	3.7	CO[C@@]12C=C[C@@]3([C@@H]4CN(C(=O)/C=C/c5ccccc5C)C[C@@H]41)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1021/jm070255o
	CHEMBL2113313	79179	None	0	Human	Functional	pEC50	=	8.6	8.6	1	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	ChEMBL	510	3	1	5	3.7	CO[C@@]12C=C[C@@]3([C@@H]4CN(C(=O)/C=C/c5ccccc5C)C[C@@H]41)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5	10.1021/jm070255o
	1393	1955	None	8	Human	Functional	pEC50	=	8.6	8.6	4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	285	0	1	4	1.6	O=C1CC[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmcl.2009.02.078
	5284570	1955	None	8	Human	Functional	pEC50	=	8.6	8.6	4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	285	0	1	4	1.6	O=C1CC[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmcl.2009.02.078
	5284570.0	1955	None	8	Human	Functional	pEC50	=	8.6	8.6	4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	285	0	1	4	1.6	O=C1CC[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmcl.2009.02.078
	7082	1955	None	8	Human	Functional	pEC50	=	8.6	8.6	4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	285	0	1	4	1.6	O=C1CC[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmcl.2009.02.078
	CHEMBL398707	1955	None	8	Human	Functional	pEC50	=	8.6	8.6	4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	285	0	1	4	1.6	O=C1CC[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmcl.2009.02.078
	DB00327	1955	None	8	Human	Functional	pEC50	=	8.6	8.6	4	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	285	0	1	4	1.6	O=C1CC[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O	10.1016/j.bmcl.2009.02.078
	16720650	138001	None	0	Human	Functional	pEC50	=	8.6	8.6	-3	3	Agonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	381	2	2	5	3.5	Nc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CCC1)C2	10.1021/jm0701674
	CHEMBL376355	138001	None	0	Human	Functional	pEC50	=	8.6	8.6	-3	3	Agonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS binding	ChEMBL	381	2	2	5	3.5	Nc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CCC1)C2	10.1021/jm0701674
	24798598	112648	None	12	Human	Functional	pEC50	=	8.6	8.6	23	2	Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	364	2	2	2	4.8	CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(F)ccc3[nH]c12	10.1021/ml500117c
	CHEMBL3301613	112648	None	12	Human	Functional	pEC50	=	8.6	8.6	23	2	Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	364	2	2	2	4.8	CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(F)ccc3[nH]c12	10.1021/ml500117c
	CHEMBL3325959	112648	None	12	Human	Functional	pEC50	=	8.6	8.6	23	2	Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay	ChEMBL	364	2	2	2	4.8	CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(F)ccc3[nH]c12	10.1021/ml500117c
	CHEMBL5093645	217926	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL		None	None	None		Clc1cccc(CNCC[C@@]2(c3ccccn3)CCOC3(CCOC3)C2)c1	10.1016/j.ejmech.2021.113986
	127049276	141116	None	0	Rat	Functional	pEC50	=	8.6	8.6	165	2	Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay	ChEMBL	533	7	3	4	5.4	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)c2ccccc2)c2ccc(Cc3ccccc3)cc21	10.1021/acs.jmedchem.6b00308
	CHEMBL3823958	141116	None	0	Rat	Functional	pEC50	=	8.6	8.6	165	2	Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay	ChEMBL	533	7	3	4	5.4	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)c2ccccc2)c2ccc(Cc3ccccc3)cc21	10.1021/acs.jmedchem.6b00308
	122195955	124276	None	0	Rat	Functional	pEC50	=	8.6	8.6	38	2	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	435	6	4	4	4.7	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(CC3CCCCC3)cc21	10.1021/acs.jmedchem.5b01270
	CHEMBL3634249	124276	None	0	Rat	Functional	pEC50	=	8.6	8.6	38	2	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	435	6	4	4	4.7	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(CC3CCCCC3)cc21	10.1021/acs.jmedchem.5b01270
	45271055	197709	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Inverse agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 3 hrs by [35S]GTPgammaS binding assayInverse agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 3 hrs by [35S]GTPgammaS binding assay	ChEMBL	421	4	2	7	1.3	CS(=O)(=O)O[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2012.06.056
	CHEMBL551074	197709	None	0	Human	Functional	pEC50	=	8.6	8.6	-	1	Inverse agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 3 hrs by [35S]GTPgammaS binding assayInverse agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 3 hrs by [35S]GTPgammaS binding assay	ChEMBL	421	4	2	7	1.3	CS(=O)(=O)O[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2012.06.056
	54756989	65724	None	0	Human	Functional	pEC50	=	8.6	8.6	19	2	Partial agonist activity at human MOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human MOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	481	5	2	5	4.8	CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm2003238
	CHEMBL1834410	65724	None	0	Human	Functional	pEC50	=	8.6	8.6	19	2	Partial agonist activity at human MOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human MOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	481	5	2	5	4.8	CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm2003238
	11849247	204961	None	0	Human	Functional	pEC50	=	8.6	8.6	-1	3	Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR	ChEMBL	498	6	1	5	4.0	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccccc5C)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/jm0604777
	CHEMBL611400	204961	None	0	Human	Functional	pEC50	=	8.6	8.6	-1	3	Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR	ChEMBL	498	6	1	5	4.0	COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccccc5C)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/jm0604777
	72164179	92100	None	0	Mouse	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	ChEMBL	531	4	3	6	4.0	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2c(Cl)n1	10.1016/j.bmcl.2013.07.043
	CHEMBL2419124	92100	None	0	Mouse	Functional	pEC50	=	8.6	8.6	-	1	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	ChEMBL	531	4	3	6	4.0	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2c(Cl)n1	10.1016/j.bmcl.2013.07.043
	72164179	92100	None	0	Mouse	Functional	pEC50	=	8.6	8.6	-	1	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	531	4	3	6	4.0	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2c(Cl)n1	10.1016/j.bmc.2015.02.055
	CHEMBL2419124	92100	None	0	Mouse	Functional	pEC50	=	8.6	8.6	-	1	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	ChEMBL	531	4	3	6	4.0	O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2c(Cl)n1	10.1016/j.bmc.2015.02.055
	16733487	85824	None	0	Human	Functional	pEC50	=	8.6	8.6	-3	3	Agonist activity at human mu opioid receptor by [35S]GTP-gamma-S binding assayAgonist activity at human mu opioid receptor by [35S]GTP-gamma-S binding assay	ChEMBL	551	7	7	7	-0.5	N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1C/C=C/C[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O	10.1021/jm061048b
	CHEMBL229440	85824	None	0	Human	Functional	pEC50	=	8.6	8.6	-3	3	Agonist activity at human mu opioid receptor by [35S]GTP-gamma-S binding assayAgonist activity at human mu opioid receptor by [35S]GTP-gamma-S binding assay	ChEMBL	551	7	7	7	-0.5	N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1C/C=C/C[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O	10.1021/jm061048b
	156011239	177405	None	0	Human	Functional	pEC50	=	8.6	8.6	-3	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	601	9	1	7	6.2	COc1cc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)ccn1	10.1021/acs.jmedchem.0c00503
	CHEMBL4636598	177405	None	0	Human	Functional	pEC50	=	8.6	8.6	-3	2	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	601	9	1	7	6.2	COc1cc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)ccn1	10.1021/acs.jmedchem.0c00503
	68196155	89232	None	0	Human	Functional	pEC50	=	8.6	8.6	-3	3	Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	301	2	1	3	3.1	C[C@H]1[C@H]2Cc3ccc(O)cc3[C@@]1(C)CCN2C[C@@H]1CCCO1	10.1016/j.bmcl.2008.10.134
	CHEMBL2367604	89232	None	0	Human	Functional	pEC50	=	8.6	8.6	-3	3	Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	301	2	1	3	3.1	C[C@H]1[C@H]2Cc3ccc(O)cc3[C@@]1(C)CCN2C[C@@H]1CCCO1	10.1016/j.bmcl.2008.10.134
	72713097	106464	None	0	Human	Functional	pEC50	=	8.6	8.6	3	3	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	432	8	1	3	5.5	C[C@@H]1CN(CCCc2ccccc2)[C@H]2C[C@H](N(C)CC3CC3)C[C@]1(c1cccc(O)c1)C2	10.1021/jm401250s
	CHEMBL3139482	106464	None	0	Human	Functional	pEC50	=	8.6	8.6	3	3	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	432	8	1	3	5.5	C[C@@H]1CN(CCCc2ccccc2)[C@H]2C[C@H](N(C)CC3CC3)C[C@]1(c1cccc(O)c1)C2	10.1021/jm401250s
	CHEMBL3217271	106464	None	0	Human	Functional	pEC50	=	8.6	8.6	3	3	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	432	8	1	3	5.5	C[C@@H]1CN(CCCc2ccccc2)[C@H]2C[C@H](N(C)CC3CC3)C[C@]1(c1cccc(O)c1)C2	10.1021/jm401250s
	10086063	201516	None	1	Human	Functional	pEC50	=	8.6	8.6	-1	2	Partial 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 countingPartial 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	ChEMBL	298	3	1	2	2.7	C[C@H]1C2Cc3ccc(C(N)=O)cc3[C@@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2013.01.117
	CHEMBL58646	201516	None	1	Human	Functional	pEC50	=	8.6	8.6	-1	2	Partial 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 countingPartial 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	ChEMBL	298	3	1	2	2.7	C[C@H]1C2Cc3ccc(C(N)=O)cc3[C@@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2013.01.117
	CHEMBL5083572	218022	None	0	Mouse	Functional	pEC50	=	8.6	8.6	2	3	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(Cc1ccco1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	CHEMBL5095617	218022	None	0	Mouse	Functional	pEC50	=	8.6	8.6	2	3	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(Cc1ccco1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	90656665	111019	None	0	Human	Functional	pEC50	=	8.6	8.6	-1	3	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysis	ChEMBL	471	5	2	5	4.1	CO[C@]12C=C[C@@]3(C[C@@H]1[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm401964y
	CHEMBL3262093	111019	None	0	Human	Functional	pEC50	=	8.6	8.6	-1	3	Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysis	ChEMBL	471	5	2	5	4.1	CO[C@]12C=C[C@@]3(C[C@@H]1[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm401964y
	CHEMBL3580748	214235	None	0	Human	Functional	pEC50	=	8.6	8.6	-5	6	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 assayAgonist 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	ChEMBL		None	None	None		Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.5b00056
	CHEMBL5082472	217294	None	0	Mouse	Functional	pEC50	=	8.6	8.6	-	1	Antagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity at mouse mu opioid receptor expressed in CHO cell membrane assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method	ChEMBL		None	None	None		O=C(CCc1cc[nH]n1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.1c02185
	CHEMBL5094496	218064	None	0	Mouse	Functional	pEC50	=	8.6	8.6	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(CCc1ccco1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	CHEMBL5096020	218064	None	0	Mouse	Functional	pEC50	=	8.6	8.6	-	1	Partial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting methodPartial agonist activity at mouse mu opioid receptor expressed in CHO cell membranes incubated for 1.5 hrs by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL		None	None	None		O=C(CCc1ccco1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1021/acs.jmedchem.2c00087
	172466389	196630	None	0	Human	Functional	pEC50	=	8.6	8.6	21	4	Agonist activity at MOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at MOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay	ChEMBL	1136	24	13	13	-0.8	CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C\C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1	10.1021/acs.jmedchem.3c02093
	CHEMBL5428360	196630	None	0	Human	Functional	pEC50	=	8.6	8.6	21	4	Agonist activity at MOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at MOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay	ChEMBL	1136	24	13	13	-0.8	CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C\C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1	10.1021/acs.jmedchem.3c02093
	CHEMBL2387213	212861	None	0	Rat	Functional	pEC50	=	8.6	8.6	-1	3	Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL		None	None	None		CC(C)C[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCNC(=O)NCCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)C(=O)O	10.1016/j.bmcl.2013.03.065
	71624661	87942	None	0	Rat	Functional	pEC50	=	8.6	8.6	-41	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	479	5	2	5	4.6	CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338746	87942	None	0	Rat	Functional	pEC50	=	8.6	8.6	-41	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	479	5	2	5	4.6	CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	44592053	189406	None	0	Human	Functional	pEC50	=	8.6	8.6	-2	2	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	386	3	4	5	1.4	NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@]1(O)CC[C@H](O)C3	nan
	CHEMBL512150	189406	None	0	Human	Functional	pEC50	=	8.6	8.6	-2	2	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	386	3	4	5	1.4	NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@]1(O)CC[C@H](O)C3	nan
	44279699	99345	None	0	Human	Functional	pEC50	=	8.6	8.6	-70	3	GTPgammaS binding in cloned human Opioid receptor mu 1 transfected into hamster ovary cellsGTPgammaS binding in cloned human Opioid receptor mu 1 transfected into hamster ovary cells	ChEMBL	435	3	2	5	3.3	CO[C@]12C=CC3(CC14CCC[C@H]4O)C1Cc4ccc(O)c5c4C3(CCN1CC1CC1)[C@@H]2O5	10.1021/jm991165p
	CHEMBL281986	99345	None	0	Human	Functional	pEC50	=	8.6	8.6	-70	3	GTPgammaS binding in cloned human Opioid receptor mu 1 transfected into hamster ovary cellsGTPgammaS binding in cloned human Opioid receptor mu 1 transfected into hamster ovary cells	ChEMBL	435	3	2	5	3.3	CO[C@]12C=CC3(CC14CCC[C@H]4O)C1Cc4ccc(O)c5c4C3(CCN1CC1CC1)[C@@H]2O5	10.1021/jm991165p
	168284684	191664	None	0	Human	Functional	pEC50	=	8.6	8.6	-1	3	Agonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assay	ChEMBL	713	7	8	8	1.0	Cc1ccc([C@@H]2NC(=O)[C@H](NC(=O)[C@@H](N)Cc3c(C)cc(O)cc3C)CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](c3ccccc3)NC2=O)cc1	10.1021/acs.jmedchem.0c01915
	CHEMBL5194625	191664	None	0	Human	Functional	pEC50	=	8.6	8.6	-1	3	Agonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assay	ChEMBL	713	7	8	8	1.0	Cc1ccc([C@@H]2NC(=O)[C@H](NC(=O)[C@@H](N)Cc3c(C)cc(O)cc3C)CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](c3ccccc3)NC2=O)cc1	10.1021/acs.jmedchem.0c01915
	145961634	162459	None	0	Mouse	Functional	pEC50	=	8.6	8.6	20	2	Agonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopyAgonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopy	ChEMBL	389	2	2	5	2.0	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](NC(=O)c2cccnc2)C=C[C@H]3[C@H]1C5	10.1039/C6MD00450D
	CHEMBL4165157	162459	None	0	Mouse	Functional	pEC50	=	8.6	8.6	20	2	Agonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopyAgonist activity at mouse MOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopy	ChEMBL	389	2	2	5	2.0	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](NC(=O)c2cccnc2)C=C[C@H]3[C@H]1C5	10.1039/C6MD00450D
	53388316	66574	None	0	Human	Functional	pEC50	=	8.6	8.6	6	3	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	504	6	4	7	1.3	O=C(CNC(=O)c1ccncc1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2011.06.135
	CHEMBL1824517	66574	None	0	Human	Functional	pEC50	=	8.6	8.6	6	3	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	504	6	4	7	1.3	O=C(CNC(=O)c1ccncc1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2011.06.135
	CHEMBL1852458	66574	None	0	Human	Functional	pEC50	=	8.6	8.6	6	3	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	ChEMBL	504	6	4	7	1.3	O=C(CNC(=O)c1ccncc1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5	10.1016/j.bmcl.2011.06.135
	CHEMBL5079432	217105	None	0	Human	Functional	pEC50	=	8.5	8.5	38	2	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis	ChEMBL		None	None	None		Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)c1ccccc1	10.1021/acs.jmedchem.0c02062
	44406732	73318	None	0	Human	Functional	pEC50	=	8.5	8.5	-6	2	Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	775	15	0	6	10.6	O=C(CCCCCCCCC(=O)Oc1ccc2c(c1)[C@@]13CCCCC1[C@@H](C2)N(CC1CC1)CC3)Oc1ccc2c(c1)[C@@]13CCCCC1[C@@H](C2)N(CC1CCC1)CC3	10.1021/jm050577x
	CHEMBL201271	73318	None	0	Human	Functional	pEC50	=	8.5	8.5	-6	2	Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	775	15	0	6	10.6	O=C(CCCCCCCCC(=O)Oc1ccc2c(c1)[C@@]13CCCCC1[C@@H](C2)N(CC1CC1)CC3)Oc1ccc2c(c1)[C@@]13CCCCC1[C@@H](C2)N(CC1CCC1)CC3	10.1021/jm050577x
	122195954	124275	None	0	Rat	Functional	pEC50	=	8.5	8.5	-	1	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	428	6	3	3	4.7	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCCc2ccc(Cc3ccccc3)cc21	10.1021/acs.jmedchem.5b01270
	CHEMBL3634248	124275	None	0	Rat	Functional	pEC50	=	8.5	8.5	-	1	Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis	ChEMBL	428	6	3	3	4.7	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCCc2ccc(Cc3ccccc3)cc21	10.1021/acs.jmedchem.5b01270
	71624553	87944	None	0	Rat	Functional	pEC50	=	8.5	8.5	-107	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	507	7	2	5	5.3	CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CCC1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	CHEMBL2338748	87944	None	0	Rat	Functional	pEC50	=	8.5	8.5	-107	2	Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr	ChEMBL	507	7	2	5	5.3	CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CCC1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	10.1021/jm301543e
	117862199	159984	None	0	Human	Functional	pEC50	=	8.5	8.5	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	551	7	3	6	4.2	O=C1CC[C@@]2(O)[C@H]3Cc4ccc(C(=O)NCCc5ccc(-c6cccnc6)cc5)c(O)c4[C@@]2(CCN3CC2CC2)C1	nan
	CHEMBL4106879	159984	None	0	Human	Functional	pEC50	=	8.5	8.5	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	551	7	3	6	4.2	O=C1CC[C@@]2(O)[C@H]3Cc4ccc(C(=O)NCCc5ccc(-c6cccnc6)cc5)c(O)c4[C@@]2(CCN3CC2CC2)C1	nan
	168282879	191330	None	0	Human	Functional	pEC50	=	8.5	8.5	-3	3	Agonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assay	ChEMBL	713	7	8	8	1.0	Cc1cccc([C@@H]2NC(=O)[C@H](NC(=O)[C@@H](N)Cc3c(C)cc(O)cc3C)CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](c3ccccc3)NC2=O)c1	10.1021/acs.jmedchem.0c01915
	CHEMBL5189745	191330	None	0	Human	Functional	pEC50	=	8.5	8.5	-3	3	Agonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant MOP expressed in CHO cells by calcium mobilization assay	ChEMBL	713	7	8	8	1.0	Cc1cccc([C@@H]2NC(=O)[C@H](NC(=O)[C@@H](N)Cc3c(C)cc(O)cc3C)CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](c3ccccc3)NC2=O)c1	10.1021/acs.jmedchem.0c01915
	137641618	158346	None	0	Human	Functional	pEC50	=	8.5	8.5	-	1	Agonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	315	1	1	4	2.6	CO[C@@]12CCC[C@]3(C)Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5	10.1021/acs.jmedchem.7b01363
	CHEMBL4088589	158346	None	0	Human	Functional	pEC50	=	8.5	8.5	-	1	Agonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	ChEMBL	315	1	1	4	2.6	CO[C@@]12CCC[C@]3(C)Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5	10.1021/acs.jmedchem.7b01363
	155531667	176601	None	0	Mouse	Functional	pEC50	=	8.5	8.5	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2ccsc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4466248	176601	None	0	Mouse	Functional	pEC50	=	8.5	8.5	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2ccsc12	10.1021/acs.jmedchem.9b01767
	CHEMBL4596736	176601	None	0	Mouse	Functional	pEC50	=	8.5	8.5	-	1	Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method	ChEMBL	502	4	3	6	4.0	O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2ccsc12	10.1021/acs.jmedchem.9b01767
	CHEMBL205306	211627	None	0	Rat	Functional	pEC50	=	7.7	7.7	-8	4	Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCC)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/jm050921q
	71819401	92084	None	0	Human	Functional	pEC50	=	7.7	7.7	-1	5	Agonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assayAgonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay	ChEMBL	301	0	2	4	1.7	C[C@@H]1C[C@H]2[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3C)[C@@H](O5)[C@H]1O	10.1016/j.bmcl.2013.06.084
	CHEMBL2418739	92084	None	0	Human	Functional	pEC50	=	7.7	7.7	-1	5	Agonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assayAgonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay	ChEMBL	301	0	2	4	1.7	C[C@@H]1C[C@H]2[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3C)[C@@H](O5)[C@H]1O	10.1016/j.bmcl.2013.06.084
	CHEMBL5080554	217180	None	0	Human	Functional	pEC50	=	7.7	7.7	-	1	Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometryAgonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry	ChEMBL		None	None	None		COc1ccsc1CNCC[C@@]1(c2ccccn2)CCO[C@]2(CCOC2)C1	10.1016/j.ejmech.2021.113986
	73212445	104519	None	0	Rat	Functional	pEC50	=	7.7	7.7	75	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cells assessed as stimulation of [35S]-GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat mu opioid receptor expressed in rat C6 cells assessed as stimulation of [35S]-GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	407	7	2	4	2.8	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CCN(C/C=C/Cc2ccccc2)CC1	10.1016/j.bmcl.2013.12.021
	CHEMBL3104101	104519	None	0	Rat	Functional	pEC50	=	7.7	7.7	75	2	Agonist activity at rat mu opioid receptor expressed in rat C6 cells assessed as stimulation of [35S]-GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat mu opioid receptor expressed in rat C6 cells assessed as stimulation of [35S]-GTPgammaS binding after 1 hr by liquid scintillation counting analysis	ChEMBL	407	7	2	4	2.8	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CCN(C/C=C/Cc2ccccc2)CC1	10.1016/j.bmcl.2013.12.021
	86580957	149653	None	0	Human	Functional	pEC50	=	7.7	7.7	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	346	8	1	3	3.8	CCCCCCN1CCC(C(=O)N(C)CC)(c2cccc(O)c2)CC1	nan
	CHEMBL3946804	149653	None	0	Human	Functional	pEC50	=	7.7	7.7	-	1	Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.	ChEMBL	346	8	1	3	3.8	CCCCCCN1CCC(C(=O)N(C)CC)(c2cccc(O)c2)CC1	nan
	162643991	181904	None	0	Human	Functional	pEC50	=	7.7	7.7	1	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1126	32	14	14	-3.6	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.6b01181
	CHEMBL4777999	181904	None	0	Human	Functional	pEC50	=	7.7	7.7	1	5	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay	ChEMBL	1126	32	14	14	-3.6	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.6b01181
	5748293	109753	None	13	Human	Functional	pEC50	=	7.7	7.7	5	3	Concentration necessary to produce 50% of the Emax value, i.e. to stimulate [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cellsConcentration necessary to produce 50% of the Emax value, i.e. to stimulate [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells	ChEMBL	355	4	0	4	3.1	COc1cccc2c1[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(OC)CCC(=O)C3	10.1021/jm031126k
	CHEMBL1628270	109753	None	13	Human	Functional	pEC50	=	7.7	7.7	5	3	Concentration necessary to produce 50% of the Emax value, i.e. to stimulate [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cellsConcentration necessary to produce 50% of the Emax value, i.e. to stimulate [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells	ChEMBL	355	4	0	4	3.1	COc1cccc2c1[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(OC)CCC(=O)C3	10.1021/jm031126k
	CHEMBL322796	109753	None	13	Human	Functional	pEC50	=	7.7	7.7	5	3	Concentration necessary to produce 50% of the Emax value, i.e. to stimulate [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cellsConcentration necessary to produce 50% of the Emax value, i.e. to stimulate [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells	ChEMBL	355	4	0	4	3.1	COc1cccc2c1[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(OC)CCC(=O)C3	10.1021/jm031126k
	127041366	138057	None	0	Human	Functional	pEC50	=	7.7	7.7	-	1	Agonist activity at human recombinant MOR expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant MOR expressed in CHO cells by calcium mobilization assay	ChEMBL	557	9	4	6	0.7	NC(=O)[C@H]1CC(F)(F)CN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1	10.1016/j.bmc.2016.02.034
	CHEMBL3764219	138057	None	0	Human	Functional	pEC50	=	7.7	7.7	-	1	Agonist activity at human recombinant MOR expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant MOR expressed in CHO cells by calcium mobilization assay	ChEMBL	557	9	4	6	0.7	NC(=O)[C@H]1CC(F)(F)CN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1	10.1016/j.bmc.2016.02.034
	156011089	177201	None	0	Human	Functional	pEC50	=	7.7	7.7	-	1	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	584	8	1	5	7.1	Cc1cccc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)c1	10.1021/acs.jmedchem.0c00503
	CHEMBL4633223	177201	None	0	Human	Functional	pEC50	=	7.7	7.7	-	1	Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	584	8	1	5	7.1	Cc1cccc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)c1	10.1021/acs.jmedchem.0c00503
	16082873	103648	None	0	Human	Functional	pEC50	=	7.7	7.7	-	1	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	364	5	2	3	4.1	C[C@H]1CN(CCCc2ccccc2)[C@@H]2C[C@@H](N)C[C@@]1(c1cccc(O)c1)C2	10.1021/jm401250s
	CHEMBL3086465	103648	None	0	Human	Functional	pEC50	=	7.7	7.7	-	1	Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	ChEMBL	364	5	2	3	4.1	C[C@H]1CN(CCCc2ccccc2)[C@@H]2C[C@@H](N)C[C@@]1(c1cccc(O)c1)C2	10.1021/jm401250s
	53521863	164246	None	5	Human	Functional	pEC50	=	6.7	6.7	-	1	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 methodAgonist 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	ChEMBL	341	3	1	3	3.8	O=c1[nH]c2ccccc2n1C1CCN(Cc2ccccc2Cl)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4210229	164246	None	5	Human	Functional	pEC50	=	6.7	6.7	-	1	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 methodAgonist 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	ChEMBL	341	3	1	3	3.8	O=c1[nH]c2ccccc2n1C1CCN(Cc2ccccc2Cl)CC1	10.1021/acs.jmedchem.8b01136
	172460140	196479	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	365	6	0	3	4.3	CC(C)C(=O)N(CC(C)N1CCC(c2ccccc2)CC1)c1ccccn1	10.1021/acs.jmedchem.3c01637
	CHEMBL5424782	196479	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assayAgonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	ChEMBL	365	6	0	3	4.3	CC(C)C(=O)N(CC(C)N1CCC(c2ccccc2)CC1)c1ccccn1	10.1021/acs.jmedchem.3c01637
	71819400	92083	None	0	Human	Functional	pEC50	=	5.7	5.7	-3	5	Agonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assayAgonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay	ChEMBL	315	1	1	4	2.0	COc1ccc2c3c1O[C@H]1[C@@H](O)[C@H](C)C[C@H]4[C@@H](C2)N(C)CC[C@]314	10.1016/j.bmcl.2013.06.084
	CHEMBL2418738	92083	None	0	Human	Functional	pEC50	=	5.7	5.7	-3	5	Agonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assayAgonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay	ChEMBL	315	1	1	4	2.0	COc1ccc2c3c1O[C@H]1[C@@H](O)[C@H](C)C[C@H]4[C@@H](C2)N(C)CC[C@]314	10.1016/j.bmcl.2013.06.084
	71819526	92089	None	0	Mouse	Functional	pEC50	=	5.7	5.7	2	4	Agonist activity at mouse MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assayAgonist activity at mouse MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay	ChEMBL	329	1	1	4	2.3	COc1cc(C)c2c3c1O[C@H]1[C@@H](O)[C@H](C)C[C@H]4[C@@H](C2)N(C)CC[C@]314	10.1016/j.bmcl.2013.06.084
	CHEMBL2418744	92089	None	0	Mouse	Functional	pEC50	=	5.7	5.7	2	4	Agonist activity at mouse MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assayAgonist activity at mouse MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay	ChEMBL	329	1	1	4	2.3	COc1cc(C)c2c3c1O[C@H]1[C@@H](O)[C@H](C)C[C@H]4[C@@H](C2)N(C)CC[C@]314	10.1016/j.bmcl.2013.06.084
	CHEMBL5078349	217039	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISAAgonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISA	ChEMBL		None	None	None		N=C(N)NCCC[C@@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.1c01631
	72735564	106380	None	0	Human	Functional	pEC50	=	6.7	6.7	-81	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay	ChEMBL	430	4	2	5	3.4	CCOCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13	10.1016/j.bmc.2013.10.032
	CHEMBL3139135	106380	None	0	Human	Functional	pEC50	=	6.7	6.7	-81	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay	ChEMBL	430	4	2	5	3.4	CCOCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13	10.1016/j.bmc.2013.10.032
	CHEMBL4296736	106380	None	0	Human	Functional	pEC50	=	6.7	6.7	-81	3	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay	ChEMBL	430	4	2	5	3.4	CCOCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13	10.1016/j.bmc.2013.10.032
	13149	2545	None	18	Mouse	Functional	pEC50	=	6.7	6.7	-8	4	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 analysisAgonist 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	ChEMBL	398	5	1	5	3.8	CC[C@@H]1CN2CCC3=C([C@@H]2C[C@@H]1/C(=C\OC)/C(=O)OC)NC4=C3C(=CC=C4)OC	10.1021/acs.jmedchem.6b00748
	3034396	2545	None	18	Mouse	Functional	pEC50	=	6.7	6.7	-8	4	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 analysisAgonist 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	ChEMBL	398	5	1	5	3.8	CC[C@@H]1CN2CCC3=C([C@@H]2C[C@@H]1/C(=C\OC)/C(=O)OC)NC4=C3C(=CC=C4)OC	10.1021/acs.jmedchem.6b00748
	CHEMBL299031	2545	None	18	Mouse	Functional	pEC50	=	6.7	6.7	-8	4	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 analysisAgonist 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	ChEMBL	398	5	1	5	3.8	CC[C@@H]1CN2CCC3=C([C@@H]2C[C@@H]1/C(=C\OC)/C(=O)OC)NC4=C3C(=CC=C4)OC	10.1021/acs.jmedchem.6b00748
	146025806	173607	None	0	Human

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Main reference

Ligand source activities (1 row/activity)