GPCRdb

Ligand source activities (1 row/activity)

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Ligands (move mouse cursor over ligand name to see structure)					Receptor			Assay information							Chemical information
Sel. page	Common name	GPCRdb ID	#Vendors	Reference ligand	Fold selectivity	# Tested GPCRs	Species	p-value (-log)	Activity Type	Activity Relation	Activity Value	AssayType	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
	3826	178792	94	None	13182	2	Human	8.9	pAC50	=	8.9	Functional	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	178792	94	None	13182	2	Human	8.9	pAC50	=	8.9	Functional	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	44	None	-794	18	Human	6.0	pAC50	=	6	Functional	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	44	None	-794	18	Human	6.0	pAC50	=	6	Functional	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	44	None	-794	18	Human	6.0	pAC50	=	6	Functional	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	44	None	-794	18	Human	6.0	pAC50	=	6	Functional	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	44	None	-794	18	Human	6.0	pAC50	=	6	Functional	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	44	None	-794	18	Human	6.0	pAC50	=	6	Functional	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	93	None	-660	39	Human	5.0	pAC50	=	5.0	Functional	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	93	None	-660	39	Human	5.0	pAC50	=	5.0	Functional	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	93	None	-660	39	Human	5.0	pAC50	=	5.0	Functional	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	93	None	-660	39	Human	5.0	pAC50	=	5.0	Functional	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	93	None	-660	39	Human	5.0	pAC50	=	5.0	Functional	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	102730	47	None	-562	17	Human	5.0	pAC50	=	5.0	Functional	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	102730	47	None	-562	17	Human	5.0	pAC50	=	5.0	Functional	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	154856	29	None	-19	15	Human	5.0	pAC50	=	5.0	Functional	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	154856	29	None	-19	15	Human	5.0	pAC50	=	5.0	Functional	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	203783	71	None	-7	8	Human	5.0	pAC50	=	5.0	Functional	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	203783	71	None	-7	8	Human	5.0	pAC50	=	5.0	Functional	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	203783	71	None	-7	8	Human	5.0	pAC50	=	5.0	Functional	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	24	None	1	3	Human	6.0	pAC50	=	6.0	Functional	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	24	None	1	3	Human	6.0	pAC50	=	6.0	Functional	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	24	None	1	3	Human	6.0	pAC50	=	6.0	Functional	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	24	None	1	3	Human	6.0	pAC50	=	6.0	Functional	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	24	None	1	3	Human	6.0	pAC50	=	6.0	Functional	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	207948	15	None	16	3	Human	5.9	pAC50	=	5.9	Functional	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	207948	15	None	16	3	Human	5.9	pAC50	=	5.9	Functional	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	98126	80	None	5	4	Human	5.9	pAC50	=	5.9	Functional	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	98126	80	None	5	4	Human	5.9	pAC50	=	5.9	Functional	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	19	None	1	4	Human	5.8	pAC50	=	5.8	Functional	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	19	None	1	4	Human	5.8	pAC50	=	5.8	Functional	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	19	None	1	4	Human	5.8	pAC50	=	5.8	Functional	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	19	None	1	4	Human	5.8	pAC50	=	5.8	Functional	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	19	None	1	4	Human	5.8	pAC50	=	5.8	Functional	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	19	None	1	4	Human	5.8	pAC50	=	5.8	Functional	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	133512	54	None	-208	15	Human	4.8	pAC50	=	4.8	Functional	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	133512	54	None	-208	15	Human	4.8	pAC50	=	4.8	Functional	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	133512	54	None	-208	15	Human	4.8	pAC50	=	4.8	Functional	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	205150	39	None	-2	4	Human	4.8	pAC50	=	4.8	Functional	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	205150	39	None	-2	4	Human	4.8	pAC50	=	4.8	Functional	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	15294	12	None	2	7	Human	6.8	pAC50	=	6.8	Functional	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	15294	12	None	2	7	Human	6.8	pAC50	=	6.8	Functional	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	4300	49	None	-7	22	Human	4.8	pAC50	=	4.8	Functional	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	4300	49	None	-7	22	Human	4.8	pAC50	=	4.8	Functional	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	4300	49	None	-7	22	Human	4.8	pAC50	=	4.8	Functional	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	203127	52	None	-10	11	Human	4.8	pAC50	=	4.8	Functional	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	203127	52	None	-10	11	Human	4.8	pAC50	=	4.8	Functional	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	29276	76	None	-173	19	Human	5.8	pAC50	=	5.8	Functional	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	29276	76	None	-173	19	Human	5.8	pAC50	=	5.8	Functional	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	29276	76	None	-173	19	Human	5.8	pAC50	=	5.8	Functional	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	77	None	-134	29	Human	5.7	pAC50	=	5.7	Functional	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	77	None	-134	29	Human	5.7	pAC50	=	5.7	Functional	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	77	None	-134	29	Human	5.7	pAC50	=	5.7	Functional	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	77	None	-134	29	Human	5.7	pAC50	=	5.7	Functional	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	77	None	-134	29	Human	5.7	pAC50	=	5.7	Functional	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	74	None	-34	15	Human	5.7	pAC50	=	5.7	Functional	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	74	None	-34	15	Human	5.7	pAC50	=	5.7	Functional	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	74	None	-34	15	Human	5.7	pAC50	=	5.7	Functional	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	74	None	-34	15	Human	5.7	pAC50	=	5.7	Functional	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	74	None	-34	15	Human	5.7	pAC50	=	5.7	Functional	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	67581	92	None	-1	6	Human	6.7	pAC50	=	6.7	Functional	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	67581	92	None	-1	6	Human	6.7	pAC50	=	6.7	Functional	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	67581	92	None	-1	6	Human	6.7	pAC50	=	6.7	Functional	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	97	None	-1230	24	Human	5.7	pAC50	=	5.7	Functional	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	97	None	-1230	24	Human	5.7	pAC50	=	5.7	Functional	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	97	None	-1230	24	Human	5.7	pAC50	=	5.7	Functional	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	97	None	-1230	24	Human	5.7	pAC50	=	5.7	Functional	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	97	None	-1230	24	Human	5.7	pAC50	=	5.7	Functional	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	99323	70	None	-91	15	Human	5.7	pAC50	=	5.7	Functional	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	99323	70	None	-91	15	Human	5.7	pAC50	=	5.7	Functional	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	203413	19	None	-19	6	Human	6.6	pAC50	=	6.6	Functional	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	203413	19	None	-19	6	Human	6.6	pAC50	=	6.6	Functional	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	83	None	-4786	22	Human	4.6	pAC50	=	4.6	Functional	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	83	None	-4786	22	Human	4.6	pAC50	=	4.6	Functional	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	83	None	-4786	22	Human	4.6	pAC50	=	4.6	Functional	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	83	None	-4786	22	Human	4.6	pAC50	=	4.6	Functional	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	83	None	-4786	22	Human	4.6	pAC50	=	4.6	Functional	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	83	None	-4786	22	Human	4.6	pAC50	=	4.6	Functional	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	34222	85	None	-89	18	Human	4.6	pAC50	=	4.6	Functional	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	34222	85	None	-89	18	Human	4.6	pAC50	=	4.6	Functional	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	19094	80	None	7	3	Human	5.6	pAC50	=	5.6	Functional	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	19094	80	None	7	3	Human	5.6	pAC50	=	5.6	Functional	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	51	None	-602	28	Human	5.6	pAC50	=	5.6	Functional	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	51	None	-602	28	Human	5.6	pAC50	=	5.6	Functional	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	51	None	-602	28	Human	5.6	pAC50	=	5.6	Functional	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	51	None	-602	28	Human	5.6	pAC50	=	5.6	Functional	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	51	None	-602	28	Human	5.6	pAC50	=	5.6	Functional	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	58	None	-1071	38	Human	5.6	pAC50	=	5.6	Functional	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	58	None	-1071	38	Human	5.6	pAC50	=	5.6	Functional	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	58	None	-1071	38	Human	5.6	pAC50	=	5.6	Functional	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	58	None	-1071	38	Human	5.6	pAC50	=	5.6	Functional	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	58	None	-1071	38	Human	5.6	pAC50	=	5.6	Functional	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	54	None	-19498	30	Human	4.6	pAC50	=	4.6	Functional	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	54	None	-19498	30	Human	4.6	pAC50	=	4.6	Functional	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	54	None	-19498	30	Human	4.6	pAC50	=	4.6	Functional	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	54	None	-19498	30	Human	4.6	pAC50	=	4.6	Functional	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	54	None	-19498	30	Human	4.6	pAC50	=	4.6	Functional	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	104342	111	None	-	1	Human	4.6	pAC50	=	4.6	Functional	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	104342	111	None	-	1	Human	4.6	pAC50	=	4.6	Functional	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	104342	111	None	-	1	Human	4.6	pAC50	=	4.6	Functional	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	33	None	-524	34	Human	5.5	pAC50	=	5.5	Functional	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	33	None	-524	34	Human	5.5	pAC50	=	5.5	Functional	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	33	None	-524	34	Human	5.5	pAC50	=	5.5	Functional	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	33	None	-524	34	Human	5.5	pAC50	=	5.5	Functional	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	33	None	-524	34	Human	5.5	pAC50	=	5.5	Functional	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	138429	33	None	-53	10	Human	5.5	pAC50	=	5.5	Functional	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	138429	33	None	-53	10	Human	5.5	pAC50	=	5.5	Functional	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	12	None	-6	5	Human	5.5	pAC50	=	5.5	Functional	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	12	None	-6	5	Human	5.5	pAC50	=	5.5	Functional	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	12	None	-6	5	Human	5.5	pAC50	=	5.5	Functional	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	12	None	-6	5	Human	5.5	pAC50	=	5.5	Functional	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	12	None	-6	5	Human	5.5	pAC50	=	5.5	Functional	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	65	None	-1096	23	Human	5.5	pAC50	=	5.5	Functional	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	65	None	-1096	23	Human	5.5	pAC50	=	5.5	Functional	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	65	None	-1096	23	Human	5.5	pAC50	=	5.5	Functional	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	65	None	-1096	23	Human	5.5	pAC50	=	5.5	Functional	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	65	None	-1096	23	Human	5.5	pAC50	=	5.5	Functional	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	65	None	-1096	23	Human	5.5	pAC50	=	5.5	Functional	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	100614	50	None	-6	16	Human	5.5	pAC50	=	5.5	Functional	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	100614	50	None	-6	16	Human	5.5	pAC50	=	5.5	Functional	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	13	None	3	3	Human	6.5	pAC50	=	6.5	Functional	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	13	None	3	3	Human	6.5	pAC50	=	6.5	Functional	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	13	None	3	3	Human	6.5	pAC50	=	6.5	Functional	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	13	None	3	3	Human	6.5	pAC50	=	6.5	Functional	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	13	None	3	3	Human	6.5	pAC50	=	6.5	Functional	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	5718	50	None	-1	11	Human	5.4	pAC50	=	5.4	Functional	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	5718	50	None	-1	11	Human	5.4	pAC50	=	5.4	Functional	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	118	None	-2630	16	Human	5.4	pAC50	=	5.4	Functional	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	118	None	-2630	16	Human	5.4	pAC50	=	5.4	Functional	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	118	None	-2630	16	Human	5.4	pAC50	=	5.4	Functional	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	118	None	-2630	16	Human	5.4	pAC50	=	5.4	Functional	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	118	None	-2630	16	Human	5.4	pAC50	=	5.4	Functional	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	178228	69	None	-5	11	Human	5.4	pAC50	=	5.4	Functional	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	178228	69	None	-5	11	Human	5.4	pAC50	=	5.4	Functional	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	78	None	-9772	14	Human	5.4	pAC50	=	5.4	Functional	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	78	None	-9772	14	Human	5.4	pAC50	=	5.4	Functional	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	78	None	-9772	14	Human	5.4	pAC50	=	5.4	Functional	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	78	None	-9772	14	Human	5.4	pAC50	=	5.4	Functional	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	78	None	-9772	14	Human	5.4	pAC50	=	5.4	Functional	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	207509	57	None	-1	5	Human	5.4	pAC50	=	5.4	Functional	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	207509	57	None	-1	5	Human	5.4	pAC50	=	5.4	Functional	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	116963	25	None	-3	6	Human	5.4	pAC50	=	5.4	Functional	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	116963	25	None	-3	6	Human	5.4	pAC50	=	5.4	Functional	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	43454	67	None	-1	7	Human	5.4	pAC50	=	5.4	Functional	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	43454	67	None	-1	7	Human	5.4	pAC50	=	5.4	Functional	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	183535	112	None	-72	14	Human	5.4	pAC50	=	5.4	Functional	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	183535	112	None	-72	14	Human	5.4	pAC50	=	5.4	Functional	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	57407	25	None	-6	7	Human	5.4	pAC50	=	5.4	Functional	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	57407	25	None	-6	7	Human	5.4	pAC50	=	5.4	Functional	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	68	None	-3890	42	Human	5.3	pAC50	=	5.3	Functional	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	68	None	-3890	42	Human	5.3	pAC50	=	5.3	Functional	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	68	None	-3890	42	Human	5.3	pAC50	=	5.3	Functional	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	68	None	-3890	42	Human	5.3	pAC50	=	5.3	Functional	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	68	None	-3890	42	Human	5.3	pAC50	=	5.3	Functional	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	103	None	-3801	33	Human	5.3	pAC50	=	5.3	Functional	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	103	None	-3801	33	Human	5.3	pAC50	=	5.3	Functional	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	103	None	-3801	33	Human	5.3	pAC50	=	5.3	Functional	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	103	None	-3801	33	Human	5.3	pAC50	=	5.3	Functional	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	103	None	-3801	33	Human	5.3	pAC50	=	5.3	Functional	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	81	None	-97	42	Human	6.3	pAC50	=	6.3	Functional	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	81	None	-97	42	Human	6.3	pAC50	=	6.3	Functional	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	81	None	-97	42	Human	6.3	pAC50	=	6.3	Functional	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	81	None	-97	42	Human	6.3	pAC50	=	6.3	Functional	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	81	None	-97	42	Human	6.3	pAC50	=	6.3	Functional	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	24	None	-2884	26	Human	5.3	pAC50	=	5.3	Functional	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	24	None	-2884	26	Human	5.3	pAC50	=	5.3	Functional	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	24	None	-2884	26	Human	5.3	pAC50	=	5.3	Functional	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	24	None	-2884	26	Human	5.3	pAC50	=	5.3	Functional	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	24	None	-2884	26	Human	5.3	pAC50	=	5.3	Functional	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	24	None	-2884	26	Human	5.3	pAC50	=	5.3	Functional	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	21	None	-1	3	Human	8.2	pAC50	=	8.2	Functional	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	21	None	-1	3	Human	8.2	pAC50	=	8.2	Functional	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	21	None	-1	3	Human	8.2	pAC50	=	8.2	Functional	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	21	None	-1	3	Human	8.2	pAC50	=	8.2	Functional	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	21	None	-1	3	Human	8.2	pAC50	=	8.2	Functional	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	205527	62	None	-28	30	Human	5.2	pAC50	=	5.2	Functional	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	205527	62	None	-28	30	Human	5.2	pAC50	=	5.2	Functional	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	205527	62	None	-28	30	Human	5.2	pAC50	=	5.2	Functional	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	98	None	-1174	36	Human	5.2	pAC50	=	5.2	Functional	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	98	None	-1174	36	Human	5.2	pAC50	=	5.2	Functional	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	98	None	-1174	36	Human	5.2	pAC50	=	5.2	Functional	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	98	None	-1174	36	Human	5.2	pAC50	=	5.2	Functional	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	98	None	-1174	36	Human	5.2	pAC50	=	5.2	Functional	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	49	None	-41	24	Human	5.1	pAC50	=	5.1	Functional	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	49	None	-41	24	Human	5.1	pAC50	=	5.1	Functional	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	49	None	-41	24	Human	5.1	pAC50	=	5.1	Functional	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	49	None	-41	24	Human	5.1	pAC50	=	5.1	Functional	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	49	None	-41	24	Human	5.1	pAC50	=	5.1	Functional	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	205784	10	None	-407	7	Human	5.1	pAC50	=	5.1	Functional	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	205784	10	None	-407	7	Human	5.1	pAC50	=	5.1	Functional	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	208402	79	None	-1	2	Human	5.1	pAC50	=	5.1	Functional	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	208402	79	None	-1	2	Human	5.1	pAC50	=	5.1	Functional	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	208402	79	None	-1	2	Human	5.1	pAC50	=	5.1	Functional	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	50	None	-15488	23	Human	6.0	pAC50	=	6.0	Functional	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	50	None	-15488	23	Human	6.0	pAC50	=	6.0	Functional	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	50	None	-15488	23	Human	6.0	pAC50	=	6.0	Functional	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	50	None	-15488	23	Human	6.0	pAC50	=	6.0	Functional	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	50	None	-15488	23	Human	6.0	pAC50	=	6.0	Functional	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	161359	0	None	11	3	Rat	10.9	pEC50	=	10.9	Functional	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	161359	0	None	11	3	Rat	10.9	pEC50	=	10.9	Functional	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	161365	0	None	38	3	Rat	10.9	pEC50	=	10.9	Functional	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	161365	0	None	38	3	Rat	10.9	pEC50	=	10.9	Functional	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	175972	0	None	-	1	Human	10.9	pEC50	=	10.9	Functional	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	175972	0	None	-	1	Human	10.9	pEC50	=	10.9	Functional	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	183451	0	None	8	3	Human	10.8	pEC50	=	10.8	Functional	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	183451	0	None	8	3	Human	10.8	pEC50	=	10.8	Functional	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	175527	0	None	-	1	Human	10.6	pEC50	=	10.6	Functional	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	175527	0	None	-	1	Human	10.6	pEC50	=	10.6	Functional	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	191026	0	None	-	1	Human	10.5	pEC50	=	10.5	Functional	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	191026	0	None	-	1	Human	10.5	pEC50	=	10.5	Functional	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	81712	0	None	478	2	Human	10.5	pEC50	=	10.5	Functional	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	81712	0	None	478	2	Human	10.5	pEC50	=	10.5	Functional	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	81713	0	None	301	2	Human	10.5	pEC50	=	10.5	Functional	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	81713	0	None	301	2	Human	10.5	pEC50	=	10.5	Functional	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	87497	0	None	57	2	Human	10.4	pEC50	=	10.4	Functional	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	87497	0	None	57	2	Human	10.4	pEC50	=	10.4	Functional	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	42	None	1	4	Human	10.4	pEC50	=	10.4	Functional	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	42	None	1	4	Human	10.4	pEC50	=	10.4	Functional	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	42	None	1	4	Human	10.4	pEC50	=	10.4	Functional	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	42	None	1	4	Human	10.4	pEC50	=	10.4	Functional	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	161611	0	None	36	3	Rat	10.4	pEC50	=	10.4	Functional	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	161611	0	None	36	3	Rat	10.4	pEC50	=	10.4	Functional	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	42	None	1	4	Human	10.4	pEC50	=	10.4	Functional	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	42	None	1	4	Human	10.4	pEC50	=	10.4	Functional	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	42	None	1	4	Human	10.4	pEC50	=	10.4	Functional	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	42	None	1	4	Human	10.4	pEC50	=	10.4	Functional	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	79457	0	None	2	3	Human	10.4	pEC50	=	10.4	Functional	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	79457	0	None	2	3	Human	10.4	pEC50	=	10.4	Functional	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	201850	0	None	5	3	Human	10.4	pEC50	=	10.4	Functional	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	201850	0	None	5	3	Human	10.4	pEC50	=	10.4	Functional	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	87495	0	None	85	2	Human	10.2	pEC50	=	10.2	Functional	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	87495	0	None	85	2	Human	10.2	pEC50	=	10.2	Functional	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	57223	0	None	2	3	Rat	10.2	pEC50	=	10.2	Functional	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	57223	0	None	2	3	Rat	10.2	pEC50	=	10.2	Functional	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	57223	0	None	2	3	Rat	10.2	pEC50	=	10.2	Functional	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	57223	0	None	2	3	Rat	10.2	pEC50	=	10.2	Functional	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	123982	0	None	-	1	Human	10.2	pEC50	=	10.2	Functional	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	123982	0	None	-	1	Human	10.2	pEC50	=	10.2	Functional	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	123890	0	None	-	1	Human	10.2	pEC50	=	10.2	Functional	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	123890	0	None	-	1	Human	10.2	pEC50	=	10.2	Functional	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	214328	0	None	-	1	Human	10.2	pEC50	=	10.2	Functional	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	209290	0	None	3	3	Human	10.1	pEC50	=	10.1	Functional	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	65657	0	None	2	3	Human	10.1	pEC50	=	10.1	Functional	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	65657	0	None	2	3	Human	10.1	pEC50	=	10.1	Functional	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	187621	0	None	-	1	Human	10.1	pEC50	=	10.1	Functional	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	187621	0	None	-	1	Human	10.1	pEC50	=	10.1	Functional	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	87496	0	None	52	2	Human	10.0	pEC50	=	10.0	Functional	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	87496	0	None	52	2	Human	10.0	pEC50	=	10.0	Functional	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	87887	0	None	-3	2	Rat	10.0	pEC50	=	10.0	Functional	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	87887	0	None	-3	2	Rat	10.0	pEC50	=	10.0	Functional	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	118176	0	None	-3	3	Human	10.0	pEC50	=	10	Functional	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	118176	0	None	-3	3	Human	10.0	pEC50	=	10	Functional	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	166820	0	None	-	1	Human	10.0	pEC50	=	10	Functional	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	166820	0	None	-	1	Human	10.0	pEC50	=	10	Functional	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	211362	3	None	1	2	Human	10.0	pEC50	=	10	Functional	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	213034	0	None	-	1	Human	10.0	pEC50	=	10	Functional	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	118176	0	None	-3	3	Human	10.0	pEC50	=	10	Functional	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	118176	0	None	-3	3	Human	10.0	pEC50	=	10	Functional	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	214821	0	None	-	1	Human	10.0	pEC50	=	10	Functional	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	161383	0	None	5	3	Rat	10.0	pEC50	=	10	Functional	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	161383	0	None	5	3	Rat	10.0	pEC50	=	10	Functional	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	189165	1	None	-3	7	Human	10.0	pEC50	=	10.0	Functional	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	189165	1	None	-3	7	Human	10.0	pEC50	=	10.0	Functional	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	189165	1	None	-3	7	Human	10.0	pEC50	=	10.0	Functional	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	57213	0	None	-1	3	Rat	10.0	pEC50	=	10.0	Functional	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	57213	0	None	-1	3	Rat	10.0	pEC50	=	10.0	Functional	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	57213	0	None	-1	3	Rat	10.0	pEC50	=	10.0	Functional	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	57213	0	None	-1	3	Rat	10.0	pEC50	=	10.0	Functional	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	176589	0	None	371	2	Rat	9.9	pEC50	=	9.9	Functional	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	176589	0	None	371	2	Rat	9.9	pEC50	=	9.9	Functional	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	176589	0	None	371	2	Rat	9.9	pEC50	=	9.9	Functional	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	161395	0	None	2	3	Rat	9.9	pEC50	=	9.9	Functional	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	161395	0	None	2	3	Rat	9.9	pEC50	=	9.9	Functional	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	161568	0	None	-1	3	Rat	9.9	pEC50	=	9.9	Functional	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	161568	0	None	-1	3	Rat	9.9	pEC50	=	9.9	Functional	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	87886	0	None	-	1	Rat	9.9	pEC50	=	9.9	Functional	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	87886	0	None	-	1	Rat	9.9	pEC50	=	9.9	Functional	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	159614	0	None	-	1	Human	9.9	pEC50	=	9.9	Functional	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	159614	0	None	-	1	Human	9.9	pEC50	=	9.9	Functional	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	57216	0	None	-1	3	Rat	9.9	pEC50	=	9.9	Functional	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	57216	0	None	-1	3	Rat	9.9	pEC50	=	9.9	Functional	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	57216	0	None	-1	3	Rat	9.9	pEC50	=	9.9	Functional	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	57216	0	None	-1	3	Rat	9.9	pEC50	=	9.9	Functional	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	84174	0	None	-3	3	Human	9.8	pEC50	=	9.8	Functional	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	84174	0	None	-3	3	Human	9.8	pEC50	=	9.8	Functional	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	45	None	-3	8	Mouse	9.8	pEC50	=	9.8	Functional	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	45	None	-3	8	Mouse	9.8	pEC50	=	9.8	Functional	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	45	None	-3	8	Mouse	9.8	pEC50	=	9.8	Functional	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	45	None	-3	8	Mouse	9.8	pEC50	=	9.8	Functional	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	45	None	-3	8	Mouse	9.8	pEC50	=	9.8	Functional	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	81718	0	None	47	2	Human	9.8	pEC50	=	9.8	Functional	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	81718	0	None	47	2	Human	9.8	pEC50	=	9.8	Functional	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	87882	0	None	-	1	Rat	9.8	pEC50	=	9.8	Functional	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	87882	0	None	-	1	Rat	9.8	pEC50	=	9.8	Functional	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	87884	0	None	-	1	Rat	9.8	pEC50	=	9.8	Functional	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	87884	0	None	-	1	Rat	9.8	pEC50	=	9.8	Functional	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	87885	0	None	-	1	Rat	9.8	pEC50	=	9.8	Functional	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	87885	0	None	-	1	Rat	9.8	pEC50	=	9.8	Functional	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	45	None	-3	8	Mouse	9.8	pEC50	=	9.8	Functional	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	45	None	-3	8	Mouse	9.8	pEC50	=	9.8	Functional	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	45	None	-3	8	Mouse	9.8	pEC50	=	9.8	Functional	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	45	None	-3	8	Mouse	9.8	pEC50	=	9.8	Functional	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	45	None	-3	8	Mouse	9.8	pEC50	=	9.8	Functional	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	173901	0	None	-1	2	Rat	9.7	pEC50	=	9.7	Functional	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	173901	0	None	-1	2	Rat	9.7	pEC50	=	9.7	Functional	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	168007	0	None	-	1	Rat	9.7	pEC50	=	9.7	Functional	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	168007	0	None	-	1	Rat	9.7	pEC50	=	9.7	Functional	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	166398	0	None	-	1	Human	9.7	pEC50	=	9.7	Functional	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	166398	0	None	-	1	Human	9.7	pEC50	=	9.7	Functional	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	87907	0	None	-2	2	Rat	9.7	pEC50	=	9.7	Functional	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	87907	0	None	-2	2	Rat	9.7	pEC50	=	9.7	Functional	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	176246	0	None	-	1	Mouse	9.7	pEC50	=	9.7	Functional	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	176246	0	None	-	1	Mouse	9.7	pEC50	=	9.7	Functional	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	176246	0	None	-	1	Mouse	9.7	pEC50	=	9.7	Functional	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	174226	1	None	-	1	Human	9.7	pEC50	=	9.7	Functional	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	174226	1	None	-	1	Human	9.7	pEC50	=	9.7	Functional	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	169593	0	None	-	1	Human	9.7	pEC50	=	9.7	Functional	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	169593	0	None	-	1	Human	9.7	pEC50	=	9.7	Functional	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	120565	0	None	6	2	Human	9.7	pEC50	=	9.7	Functional	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	120565	0	None	6	2	Human	9.7	pEC50	=	9.7	Functional	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	120565	0	None	6	2	Human	9.7	pEC50	=	9.7	Functional	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	214935	0	None	-	1	Human	9.7	pEC50	=	9.7	Functional	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	210404	0	None	1	3	Rat	9.7	pEC50	=	9.7	Functional	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	87888	0	None	-4	2	Rat	9.7	pEC50	=	9.7	Functional	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	87888	0	None	-4	2	Rat	9.7	pEC50	=	9.7	Functional	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
	155517331	176247	0	None	-	1	Mouse	9.7	pEC50	=	9.7	Functional	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	176247	0	None	-	1	Mouse	9.7	pEC50	=	9.7	Functional	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	176247	0	None	-	1	Mouse	9.7	pEC50	=	9.7	Functional	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	121397	0	None	33	2	Rat	9.7	pEC50	=	9.7	Functional	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	121397	0	None	33	2	Rat	9.7	pEC50	=	9.7	Functional	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	84180	0	None	-1	3	Human	9.7	pEC50	=	9.7	Functional	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	84180	0	None	-1	3	Human	9.7	pEC50	=	9.7	Functional	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	188513	0	None	-	1	Mouse	9.7	pEC50	=	9.7	Functional	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	188513	0	None	-	1	Mouse	9.7	pEC50	=	9.7	Functional	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	188513	0	None	-	1	Mouse	9.7	pEC50	=	9.7	Functional	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
	155542413	176295	0	None	524	2	Rat	9.6	pEC50	=	9.6	Functional	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	176295	0	None	524	2	Rat	9.6	pEC50	=	9.6	Functional	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	176295	0	None	524	2	Rat	9.6	pEC50	=	9.6	Functional	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	176559	0	None	-	1	Rat	9.6	pEC50	=	9.6	Functional	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	176559	0	None	-	1	Rat	9.6	pEC50	=	9.6	Functional	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	176559	0	None	-	1	Rat	9.6	pEC50	=	9.6	Functional	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	87889	0	None	-3	2	Rat	9.6	pEC50	=	9.6	Functional	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	87889	0	None	-3	2	Rat	9.6	pEC50	=	9.6	Functional	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	180053	0	None	21	3	Human	9.6	pEC50	=	9.6	Functional	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	180053	0	None	21	3	Human	9.6	pEC50	=	9.6	Functional	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	86846	0	None	281	2	Rat	9.6	pEC50	=	9.6	Functional	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	86846	0	None	281	2	Rat	9.6	pEC50	=	9.6	Functional	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	121396	0	None	-	1	Rat	9.6	pEC50	=	9.6	Functional	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	121396	0	None	-	1	Rat	9.6	pEC50	=	9.6	Functional	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	86846	0	None	281	2	Rat	9.6	pEC50	=	9.6	Functional	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	86846	0	None	281	2	Rat	9.6	pEC50	=	9.6	Functional	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	113487	0	None	-	1	Mouse	9.6	pEC50	=	9.6	Functional	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	113487	0	None	-	1	Mouse	9.6	pEC50	=	9.6	Functional	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	113487	0	None	-	1	Mouse	9.6	pEC50	=	9.6	Functional	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	79139	0	None	-	1	Human	9.6	pEC50	=	9.6	Functional	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	79139	0	None	-	1	Human	9.6	pEC50	=	9.6	Functional	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	176315	0	None	-	1	Rat	9.6	pEC50	=	9.6	Functional	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	176315	0	None	-	1	Rat	9.6	pEC50	=	9.6	Functional	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	176315	0	None	-	1	Rat	9.6	pEC50	=	9.6	Functional	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	45	None	-5	8	Rat	9.6	pEC50	=	9.6	Functional	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	45	None	-5	8	Rat	9.6	pEC50	=	9.6	Functional	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	45	None	-5	8	Rat	9.6	pEC50	=	9.6	Functional	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	45	None	-5	8	Rat	9.6	pEC50	=	9.6	Functional	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	87903	0	None	-4	2	Rat	9.6	pEC50	=	9.6	Functional	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	87903	0	None	-4	2	Rat	9.6	pEC50	=	9.6	Functional	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	192662	0	None	-	1	Human	9.6	pEC50	=	9.6	Functional	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	192662	0	None	-	1	Human	9.6	pEC50	=	9.6	Functional	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	189165	1	None	2	7	Rat	9.6	pEC50	=	9.6	Functional	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	189165	1	None	2	7	Rat	9.6	pEC50	=	9.6	Functional	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	189165	1	None	2	7	Rat	9.6	pEC50	=	9.6	Functional	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	167030	0	None	-	1	Human	9.6	pEC50	=	9.6	Functional	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	167030	0	None	-	1	Human	9.6	pEC50	=	9.6	Functional	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	173238	1	None	-	1	Human	9.6	pEC50	=	9.6	Functional	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	173238	1	None	-	1	Human	9.6	pEC50	=	9.6	Functional	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	57217	0	None	1	3	Rat	9.5	pEC50	=	9.5	Functional	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	57217	0	None	1	3	Rat	9.5	pEC50	=	9.5	Functional	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	87883	0	None	-14	2	Rat	9.5	pEC50	=	9.5	Functional	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	87883	0	None	-14	2	Rat	9.5	pEC50	=	9.5	Functional	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	57217	0	None	1	3	Rat	9.5	pEC50	=	9.5	Functional	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	57217	0	None	1	3	Rat	9.5	pEC50	=	9.5	Functional	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	45	None	-3	8	Human	9.5	pEC50	=	9.5	Functional	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	45	None	-3	8	Human	9.5	pEC50	=	9.5	Functional	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	45	None	-3	8	Human	9.5	pEC50	=	9.5	Functional	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	45	None	-3	8	Human	9.5	pEC50	=	9.5	Functional	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	79140	0	None	3	2	Human	9.5	pEC50	=	9.5	Functional	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	79140	0	None	3	2	Human	9.5	pEC50	=	9.5	Functional	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	187439	2	None	-	1	Human	9.5	pEC50	=	9.5	Functional	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	187439	2	None	-	1	Human	9.5	pEC50	=	9.5	Functional	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	145916	0	None	-	1	Human	9.5	pEC50	=	9.5	Functional	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	145916	0	None	-	1	Human	9.5	pEC50	=	9.5	Functional	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	57218	0	None	-1	3	Rat	9.5	pEC50	=	9.5	Functional	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	57218	0	None	-1	3	Rat	9.5	pEC50	=	9.5	Functional	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	87877	0	None	-4	2	Rat	9.5	pEC50	=	9.5	Functional	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	87877	0	None	-4	2	Rat	9.5	pEC50	=	9.5	Functional	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	201887	0	None	4	2	Human	9.5	pEC50	=	9.5	Functional	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	201887	0	None	4	2	Human	9.5	pEC50	=	9.5	Functional	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	176681	0	None	-	1	Mouse	9.5	pEC50	=	9.5	Functional	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	176681	0	None	-	1	Mouse	9.5	pEC50	=	9.5	Functional	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	176681	0	None	-	1	Mouse	9.5	pEC50	=	9.5	Functional	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	179260	0	None	-	1	Human	9.5	pEC50	=	9.5	Functional	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	179260	0	None	-	1	Human	9.5	pEC50	=	9.5	Functional	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
	155527203	176296	0	None	-	1	Rat	9.5	pEC50	=	9.5	Functional	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	176296	0	None	-	1	Rat	9.5	pEC50	=	9.5	Functional	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	176296	0	None	-	1	Rat	9.5	pEC50	=	9.5	Functional	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	176528	0	None	-	1	Rat	9.5	pEC50	=	9.5	Functional	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	176528	0	None	-	1	Rat	9.5	pEC50	=	9.5	Functional	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	176528	0	None	-	1	Rat	9.5	pEC50	=	9.5	Functional	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	57218	0	None	-1	3	Rat	9.5	pEC50	=	9.5	Functional	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	57218	0	None	-1	3	Rat	9.5	pEC50	=	9.5	Functional	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	214858	2	None	-	1	Human	9.5	pEC50	=	9.5	Functional	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	176466	0	None	-	1	Mouse	9.4	pEC50	=	9.4	Functional	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	176466	0	None	-	1	Mouse	9.4	pEC50	=	9.4	Functional	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	176466	0	None	-	1	Mouse	9.4	pEC50	=	9.4	Functional	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	141058	0	None	-	1	Rat	9.4	pEC50	=	9.4	Functional	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	141058	0	None	-	1	Rat	9.4	pEC50	=	9.4	Functional	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	113488	0	None	-	1	Mouse	9.4	pEC50	=	9.4	Functional	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	113488	0	None	-	1	Mouse	9.4	pEC50	=	9.4	Functional	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	113488	0	None	-	1	Mouse	9.4	pEC50	=	9.4	Functional	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	150458	0	None	-	1	Human	9.4	pEC50	=	9.4	Functional	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	150458	0	None	-	1	Human	9.4	pEC50	=	9.4	Functional	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	114781	0	None	-12	3	Human	9.4	pEC50	=	9.4	Functional	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	114781	0	None	-12	3	Human	9.4	pEC50	=	9.4	Functional	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	85376	0	None	-7	3	Human	9.4	pEC50	=	9.4	Functional	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	85376	0	None	-7	3	Human	9.4	pEC50	=	9.4	Functional	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	85376	0	None	-7	3	Human	9.4	pEC50	=	9.4	Functional	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	176630	0	None	223	2	Rat	9.4	pEC50	=	9.4	Functional	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	176630	0	None	223	2	Rat	9.4	pEC50	=	9.4	Functional	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	176630	0	None	223	2	Rat	9.4	pEC50	=	9.4	Functional	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	176330	0	None	-	1	Mouse	9.4	pEC50	=	9.4	Functional	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	176330	0	None	-	1	Mouse	9.4	pEC50	=	9.4	Functional	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	176330	0	None	-	1	Mouse	9.4	pEC50	=	9.4	Functional	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	176399	0	None	-	1	Rat	9.4	pEC50	=	9.4	Functional	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	176399	0	None	-	1	Rat	9.4	pEC50	=	9.4	Functional	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	176399	0	None	-	1	Rat	9.4	pEC50	=	9.4	Functional	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	191738	0	None	-	1	Human	9.4	pEC50	=	9.4	Functional	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	191738	0	None	-	1	Human	9.4	pEC50	=	9.4	Functional	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	87893	0	None	-2	2	Rat	9.4	pEC50	=	9.4	Functional	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	87893	0	None	-2	2	Rat	9.4	pEC50	=	9.4	Functional	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	87911	0	None	-13	2	Rat	9.4	pEC50	=	9.4	Functional	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	87911	0	None	-13	2	Rat	9.4	pEC50	=	9.4	Functional	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	152386	0	None	-4	2	Human	9.4	pEC50	=	9.4	Functional	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	152386	0	None	-4	2	Human	9.4	pEC50	=	9.4	Functional	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	215545	2	None	3	3	Mouse	9.4	pEC50	=	9.4	Functional	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	215545	2	None	3	3	Mouse	9.4	pEC50	=	9.4	Functional	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	209199	0	None	-1	5	Rat	9.3	pEC50	=	9.3	Functional	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	209199	0	None	-1	5	Rat	9.3	pEC50	=	9.3	Functional	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	180590	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	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	180590	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	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	214367	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	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	176479	0	None	-	1	Mouse	9.3	pEC50	=	9.3	Functional	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	176479	0	None	-	1	Mouse	9.3	pEC50	=	9.3	Functional	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	176479	0	None	-	1	Mouse	9.3	pEC50	=	9.3	Functional	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	124214	0	None	-	1	Rat	9.3	pEC50	=	9.3	Functional	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	124214	0	None	-	1	Rat	9.3	pEC50	=	9.3	Functional	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	87881	0	None	-37	2	Rat	9.3	pEC50	=	9.3	Functional	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	87881	0	None	-37	2	Rat	9.3	pEC50	=	9.3	Functional	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	36	None	8	4	Human	9.3	pEC50	=	9.3	Functional	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	36	None	8	4	Human	9.3	pEC50	=	9.3	Functional	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	36	None	8	4	Human	9.3	pEC50	=	9.3	Functional	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	45	None	-3	8	Human	9.3	pEC50	=	9.3	Functional	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	45	None	-3	8	Human	9.3	pEC50	=	9.3	Functional	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	45	None	-3	8	Human	9.3	pEC50	=	9.3	Functional	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	45	None	-3	8	Human	9.3	pEC50	=	9.3	Functional	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	188615	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	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	188615	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	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	188615	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	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	214807	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	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	84170	0	None	-5	3	Human	9.3	pEC50	=	9.3	Functional	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	84170	0	None	-5	3	Human	9.3	pEC50	=	9.3	Functional	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	201822	0	None	4	3	Human	9.3	pEC50	=	9.3	Functional	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	201822	0	None	4	3	Human	9.3	pEC50	=	9.3	Functional	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	201823	0	None	9	3	Human	9.3	pEC50	=	9.3	Functional	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	201823	0	None	9	3	Human	9.3	pEC50	=	9.3	Functional	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	26	None	-1	13	Human	9.3	pEC50	=	9.3	Functional	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	26	None	-1	13	Human	9.3	pEC50	=	9.3	Functional	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	26	None	-1	13	Human	9.3	pEC50	=	9.3	Functional	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	26	None	-1	13	Human	9.3	pEC50	=	9.3	Functional	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	26	None	-1	13	Human	9.3	pEC50	=	9.3	Functional	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	103582	0	None	1	2	Human	9.3	pEC50	=	9.3	Functional	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	103582	0	None	1	2	Human	9.3	pEC50	=	9.3	Functional	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	106407	0	None	-1	2	Human	9.3	pEC50	=	9.3	Functional	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	106407	0	None	-1	2	Human	9.3	pEC50	=	9.3	Functional	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	106407	0	None	-1	2	Human	9.3	pEC50	=	9.3	Functional	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	176461	0	None	-	1	Rat	9.3	pEC50	=	9.3	Functional	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	176461	0	None	-	1	Rat	9.3	pEC50	=	9.3	Functional	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	176461	0	None	-	1	Rat	9.3	pEC50	=	9.3	Functional	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	86845	0	None	-	1	Rat	9.3	pEC50	=	9.3	Functional	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	86845	0	None	-	1	Rat	9.3	pEC50	=	9.3	Functional	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	86845	0	None	-	1	Rat	9.3	pEC50	=	9.3	Functional	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	86845	0	None	-	1	Rat	9.3	pEC50	=	9.3	Functional	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	173496	0	None	-	1	Mouse	9.3	pEC50	=	9.3	Functional	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	173496	0	None	-	1	Mouse	9.3	pEC50	=	9.3	Functional	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	149838	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	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	149838	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	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	215528	2	None	13	3	Mouse	9.3	pEC50	=	9.3	Functional	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	215528	2	None	13	3	Mouse	9.3	pEC50	=	9.3	Functional	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	124216	0	None	1096	2	Rat	9.3	pEC50	=	9.3	Functional	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	124216	0	None	1096	2	Rat	9.3	pEC50	=	9.3	Functional	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	87904	0	None	-2	2	Rat	9.3	pEC50	=	9.3	Functional	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	87904	0	None	-2	2	Rat	9.3	pEC50	=	9.3	Functional	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	87909	0	None	-51	2	Rat	9.3	pEC50	=	9.3	Functional	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	87909	0	None	-51	2	Rat	9.3	pEC50	=	9.3	Functional	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	61260	0	None	-7	5	Rat	9.2	pEC50	=	9.2	Functional	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	61260	0	None	-7	5	Rat	9.2	pEC50	=	9.2	Functional	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	61260	0	None	-7	5	Rat	9.2	pEC50	=	9.2	Functional	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	61260	0	None	-7	5	Rat	9.2	pEC50	=	9.2	Functional	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	90564	0	None	10	3	Rat	9.2	pEC50	=	9.2	Functional	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	90564	0	None	10	3	Rat	9.2	pEC50	=	9.2	Functional	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	176467	0	None	-	1	Mouse	9.2	pEC50	=	9.2	Functional	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	176467	0	None	-	1	Mouse	9.2	pEC50	=	9.2	Functional	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	176467	0	None	-	1	Mouse	9.2	pEC50	=	9.2	Functional	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	176480	0	None	-	1	Mouse	9.2	pEC50	=	9.2	Functional	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	176480	0	None	-	1	Mouse	9.2	pEC50	=	9.2	Functional	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	176480	0	None	-	1	Mouse	9.2	pEC50	=	9.2	Functional	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	45	None	-4	8	Human	9.2	pEC50	=	9.2	Functional	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	45	None	-4	8	Human	9.2	pEC50	=	9.2	Functional	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	45	None	-4	8	Human	9.2	pEC50	=	9.2	Functional	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	45	None	-4	8	Human	9.2	pEC50	=	9.2	Functional	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	45	None	-4	8	Human	9.2	pEC50	=	9.2	Functional	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	45	None	-3	8	Human	9.2	pEC50	=	9.2	Functional	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	45	None	-3	8	Human	9.2	pEC50	=	9.2	Functional	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	45	None	-3	8	Human	9.2	pEC50	=	9.2	Functional	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	45	None	-3	8	Human	9.2	pEC50	=	9.2	Functional	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
	25256965	179194	0	None	-7	2	Rat	9.2	pEC50	=	9.2	Functional	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	179194	0	None	-7	2	Rat	9.2	pEC50	=	9.2	Functional	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	87902	0	None	-2	2	Rat	9.2	pEC50	=	9.2	Functional	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	87902	0	None	-2	2	Rat	9.2	pEC50	=	9.2	Functional	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	84175	0	None	-6	3	Human	9.2	pEC50	=	9.2	Functional	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	84175	0	None	-6	3	Human	9.2	pEC50	=	9.2	Functional	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	124210	0	None	389	2	Rat	9.2	pEC50	=	9.2	Functional	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	124210	0	None	389	2	Rat	9.2	pEC50	=	9.2	Functional	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	172834	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	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	172834	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	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	159869	0	None	1	2	Human	9.2	pEC50	=	9.2	Functional	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	159869	0	None	1	2	Human	9.2	pEC50	=	9.2	Functional	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	215559	0	None	-	1	Mouse	9.2	pEC50	=	9.2	Functional	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	215559	0	None	-	1	Mouse	9.2	pEC50	=	9.2	Functional	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	136945	0	None	1	5	Rat	9.2	pEC50	=	9.2	Functional	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	136945	0	None	1	5	Rat	9.2	pEC50	=	9.2	Functional	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	136945	0	None	1	5	Rat	9.2	pEC50	=	9.2	Functional	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	136945	0	None	1	5	Rat	9.2	pEC50	=	9.2	Functional	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	187622	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	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	187622	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	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	60114	0	None	-1	3	Human	9.2	pEC50	=	9.2	Functional	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	60114	0	None	-1	3	Human	9.2	pEC50	=	9.2	Functional	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	60114	0	None	-1	3	Human	9.2	pEC50	=	9.2	Functional	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	57221	0	None	-1	3	Rat	9.2	pEC50	=	9.2	Functional	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	57221	0	None	-1	3	Rat	9.2	pEC50	=	9.2	Functional	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	172460	0	None	2	2	Rat	9.2	pEC50	=	9.2	Functional	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	172460	0	None	2	2	Rat	9.2	pEC50	=	9.2	Functional	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	57221	0	None	-1	3	Rat	9.2	pEC50	=	9.2	Functional	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	57221	0	None	-1	3	Rat	9.2	pEC50	=	9.2	Functional	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	170493	0	None	102	3	Mouse	9.2	pEC50	=	9.2	Functional	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	170493	0	None	102	3	Mouse	9.2	pEC50	=	9.2	Functional	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	189165	1	None	2	7	Rat	9.2	pEC50	=	9.2	Functional	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	189165	1	None	2	7	Rat	9.2	pEC50	=	9.2	Functional	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	189165	1	None	2	7	Rat	9.2	pEC50	=	9.2	Functional	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	97748	0	None	18	3	Rat	9.2	pEC50	=	9.2	Functional	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	97748	0	None	18	3	Rat	9.2	pEC50	=	9.2	Functional	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	26	None	-6	5	Human	9.1	pEC50	=	9.1	Functional	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	26	None	-6	5	Human	9.1	pEC50	=	9.1	Functional	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	26	None	-6	5	Human	9.1	pEC50	=	9.1	Functional	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	26	None	-6	5	Human	9.1	pEC50	=	9.1	Functional	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	26	None	-6	5	Human	9.1	pEC50	=	9.1	Functional	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	81708	0	None	95	2	Human	9.1	pEC50	=	9.1	Functional	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	81708	0	None	95	2	Human	9.1	pEC50	=	9.1	Functional	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	57222	0	None	-25	3	Rat	9.1	pEC50	=	9.1	Functional	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	57222	0	None	-25	3	Rat	9.1	pEC50	=	9.1	Functional	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	61263	0	None	-1	5	Rat	9.1	pEC50	=	9.1	Functional	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	61263	0	None	-1	5	Rat	9.1	pEC50	=	9.1	Functional	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	87895	0	None	-2	2	Rat	9.1	pEC50	=	9.1	Functional	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	87895	0	None	-2	2	Rat	9.1	pEC50	=	9.1	Functional	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	57222	0	None	-25	3	Rat	9.1	pEC50	=	9.1	Functional	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	57222	0	None	-25	3	Rat	9.1	pEC50	=	9.1	Functional	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	215132	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	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	215132	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	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	188605	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	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	188605	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	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	188605	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	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	161038	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	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	161038	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	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	161038	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	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	176297	0	None	-	1	Mouse	9.1	pEC50	=	9.1	Functional	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	176297	0	None	-	1	Mouse	9.1	pEC50	=	9.1	Functional	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	176297	0	None	-	1	Mouse	9.1	pEC50	=	9.1	Functional	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	141018	0	None	323	2	Rat	9.1	pEC50	=	9.1	Functional	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	141018	0	None	323	2	Rat	9.1	pEC50	=	9.1	Functional	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	187255	9	None	-6	2	Human	9.1	pEC50	=	9.1	Functional	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	187255	9	None	-6	2	Human	9.1	pEC50	=	9.1	Functional	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	187255	9	None	-6	2	Human	9.1	pEC50	=	9.1	Functional	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	187255	9	None	-6	2	Human	9.1	pEC50	=	9.1	Functional	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	187255	9	None	-6	2	Human	9.1	pEC50	=	9.1	Functional	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	187255	9	None	-6	2	Human	9.1	pEC50	=	9.1	Functional	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	187255	9	None	-6	2	Human	9.1	pEC50	=	9.1	Functional	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	187255	9	None	-6	2	Human	9.1	pEC50	=	9.1	Functional	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	187255	9	None	-6	2	Human	9.1	pEC50	=	9.1	Functional	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	187255	9	None	-6	2	Human	9.1	pEC50	=	9.1	Functional	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	210443	0	None	1	3	Rat	9.1	pEC50	=	9.1	Functional	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	187255	9	None	-6	2	Human	9.1	pEC50	=	9.1	Functional	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	187255	9	None	-6	2	Human	9.1	pEC50	=	9.1	Functional	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	107114	0	None	1	3	Human	9.1	pEC50	=	9.1	Functional	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	107114	0	None	1	3	Human	9.1	pEC50	=	9.1	Functional	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	215552	0	None	-	1	Mouse	9.1	pEC50	=	9.1	Functional	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	215552	0	None	-	1	Mouse	9.1	pEC50	=	9.1	Functional	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	215550	0	None	-	1	Mouse	9.1	pEC50	=	9.1	Functional	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	215550	0	None	-	1	Mouse	9.1	pEC50	=	9.1	Functional	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	66637	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	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	66637	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	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	66637	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	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	61262	0	None	-1	5	Rat	9.1	pEC50	=	9.1	Functional	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	61262	0	None	-1	5	Rat	9.1	pEC50	=	9.1	Functional	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	61262	0	None	-1	5	Rat	9.1	pEC50	=	9.1	Functional	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	61262	0	None	-1	5	Rat	9.1	pEC50	=	9.1	Functional	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	81709	0	None	436	2	Human	9.1	pEC50	=	9.1	Functional	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	81709	0	None	436	2	Human	9.1	pEC50	=	9.1	Functional	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	86844	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	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	86844	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	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	86844	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	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	86844	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	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	87892	0	None	-4	2	Rat	9.1	pEC50	=	9.1	Functional	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	87892	0	None	-4	2	Rat	9.1	pEC50	=	9.1	Functional	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	88163	0	None	1	2	Human	9.1	pEC50	=	9.1	Functional	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	88163	0	None	1	2	Human	9.1	pEC50	=	9.1	Functional	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	189241	0	None	1	3	Human	9.1	pEC50	=	9.1	Functional	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	189241	0	None	1	3	Human	9.1	pEC50	=	9.1	Functional	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
	24768397	146418	0	None	-4	3	Rat	9.1	pEC50	=	9.1	Functional	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	146418	0	None	-4	3	Rat	9.1	pEC50	=	9.1	Functional	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	88508	0	None	-1	3	Rat	9.1	pEC50	=	9.1	Functional	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	88508	0	None	-1	3	Rat	9.1	pEC50	=	9.1	Functional	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	160054	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	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	160054	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	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	146418	0	None	-4	3	Rat	9.1	pEC50	=	9.1	Functional	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	146418	0	None	-4	3	Rat	9.1	pEC50	=	9.1	Functional	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	88508	0	None	-1	3	Rat	9.1	pEC50	=	9.1	Functional	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	88508	0	None	-1	3	Rat	9.1	pEC50	=	9.1	Functional	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	141027	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	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	141027	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	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	91628	0	None	3	3	Rat	9.1	pEC50	=	9.1	Functional	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	91628	0	None	3	3	Rat	9.1	pEC50	=	9.1	Functional	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	176493	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	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	176493	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	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	176493	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	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	201839	0	None	5	3	Human	9.1	pEC50	=	9.1	Functional	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	201839	0	None	5	3	Human	9.1	pEC50	=	9.1	Functional	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	215535	0	None	-	1	Mouse	9.0	pEC50	=	9.0	Functional	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	215535	0	None	-	1	Mouse	9.0	pEC50	=	9.0	Functional	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	91628	0	None	3	3	Rat	9.0	pEC50	=	9.0	Functional	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	91628	0	None	3	3	Rat	9.0	pEC50	=	9.0	Functional	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	124212	0	None	-	1	Rat	9.0	pEC50	=	9.0	Functional	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	124212	0	None	-	1	Rat	9.0	pEC50	=	9.0	Functional	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	57215	0	None	6	3	Rat	9.0	pEC50	=	9.0	Functional	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	57215	0	None	6	3	Rat	9.0	pEC50	=	9.0	Functional	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	190032	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	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	190032	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	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	57215	0	None	6	3	Rat	9.0	pEC50	=	9.0	Functional	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	57215	0	None	6	3	Rat	9.0	pEC50	=	9.0	Functional	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	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	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	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	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	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	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	176633	0	None	-	1	Mouse	9.0	pEC50	=	9.0	Functional	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	176633	0	None	-	1	Mouse	9.0	pEC50	=	9.0	Functional	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	176633	0	None	-	1	Mouse	9.0	pEC50	=	9.0	Functional	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	215570	0	None	1	3	Mouse	9.0	pEC50	=	9.0	Functional	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	215570	0	None	1	3	Mouse	9.0	pEC50	=	9.0	Functional	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	61263	0	None	-1	5	Rat	9.0	pEC50	=	9.0	Functional	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	61263	0	None	-1	5	Rat	9.0	pEC50	=	9.0	Functional	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	188466	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	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	188466	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	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	188466	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	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	176665	0	None	-	1	Mouse	9.0	pEC50	=	9.0	Functional	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	176665	0	None	-	1	Mouse	9.0	pEC50	=	9.0	Functional	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	176665	0	None	-	1	Mouse	9.0	pEC50	=	9.0	Functional	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	215575	0	None	13	3	Mouse	9.0	pEC50	=	9.0	Functional	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	215575	0	None	13	3	Mouse	9.0	pEC50	=	9.0	Functional	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	189241	0	None	1	3	Human	9.0	pEC50	=	9.0	Functional	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	189241	0	None	1	3	Human	9.0	pEC50	=	9.0	Functional	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	215540	0	None	6	3	Mouse	9.0	pEC50	=	9.0	Functional	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	215540	0	None	6	3	Mouse	9.0	pEC50	=	9.0	Functional	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	45	None	-3	8	Human	9.0	pEC50	=	9	Functional	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	45	None	-3	8	Human	9.0	pEC50	=	9	Functional	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	45	None	-3	8	Human	9.0	pEC50	=	9	Functional	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	45	None	-3	8	Human	9.0	pEC50	=	9	Functional	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	101421	0	None	1	2	Human	9.0	pEC50	=	9	Functional	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	101421	0	None	1	2	Human	9.0	pEC50	=	9	Functional	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	170713	0	None	-	1	Human	9.0	pEC50	=	9	Functional	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	170713	0	None	-	1	Human	9.0	pEC50	=	9	Functional	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	172894	0	None	-	1	Human	9.0	pEC50	=	9	Functional	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	172894	0	None	-	1	Human	9.0	pEC50	=	9	Functional	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	36	None	1584	2	Human	9.0	pEC50	=	9	Functional	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	36	None	1584	2	Human	9.0	pEC50	=	9	Functional	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	36	None	1584	2	Human	9.0	pEC50	=	9	Functional	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	36	None	1584	2	Human	9.0	pEC50	=	9	Functional	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	36	None	1584	2	Human	9.0	pEC50	=	9	Functional	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	36	None	1584	2	Human	9.0	pEC50	=	9	Functional	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	179216	0	None	2	2	Rat	9.0	pEC50	=	9	Functional	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	179216	0	None	2	2	Rat	9.0	pEC50	=	9	Functional	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	176561	0	None	-	1	Rat	9.0	pEC50	=	9	Functional	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	176561	0	None	-	1	Rat	9.0	pEC50	=	9	Functional	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	176561	0	None	-	1	Rat	9.0	pEC50	=	9	Functional	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	87874	0	None	-19	2	Rat	9.0	pEC50	=	9	Functional	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	87874	0	None	-19	2	Rat	9.0	pEC50	=	9	Functional	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	87894	0	None	-12	2	Rat	9.0	pEC50	=	9	Functional	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	87894	0	None	-12	2	Rat	9.0	pEC50	=	9	Functional	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	87899	0	None	-1	2	Rat	9.0	pEC50	=	9	Functional	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	87899	0	None	-1	2	Rat	9.0	pEC50	=	9	Functional	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	132758	0	None	-	1	Human	9.0	pEC50	=	9	Functional	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	132758	0	None	-	1	Human	9.0	pEC50	=	9	Functional	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	188532	0	None	-	1	Mouse	9.0	pEC50	=	9	Functional	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	188532	0	None	-	1	Mouse	9.0	pEC50	=	9	Functional	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	188532	0	None	-	1	Mouse	9.0	pEC50	=	9	Functional	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	189604	0	None	-	1	Human	9.0	pEC50	=	9	Functional	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	189604	0	None	-	1	Human	9.0	pEC50	=	9	Functional	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	191838	0	None	-	1	Human	9.0	pEC50	=	9	Functional	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	191838	0	None	-	1	Human	9.0	pEC50	=	9	Functional	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	176537	0	None	-	1	Mouse	9.0	pEC50	=	9.0	Functional	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	176537	0	None	-	1	Mouse	9.0	pEC50	=	9.0	Functional	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	176537	0	None	-	1	Mouse	9.0	pEC50	=	9.0	Functional	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	92011	0	None	-	1	Mouse	9.0	pEC50	=	9.0	Functional	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	92011	0	None	-	1	Mouse	9.0	pEC50	=	9.0	Functional	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	92011	0	None	-	1	Mouse	9.0	pEC50	=	9.0	Functional	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	92011	0	None	-	1	Mouse	9.0	pEC50	=	9.0	Functional	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	215571	2	None	15	3	Mouse	9.0	pEC50	=	9.0	Functional	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	215571	2	None	15	3	Mouse	9.0	pEC50	=	9.0	Functional	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	114782	0	None	-6	2	Human	9.0	pEC50	=	9.0	Functional	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	114782	0	None	-6	2	Human	9.0	pEC50	=	9.0	Functional	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	75844	0	None	-3	2	Human	9.0	pEC50	=	9.0	Functional	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	75844	0	None	-3	2	Human	9.0	pEC50	=	9.0	Functional	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	190280	0	None	-13	2	Human	9.0	pEC50	=	9.0	Functional	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	190280	0	None	-13	2	Human	9.0	pEC50	=	9.0	Functional	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	86843	0	None	-	1	Rat	9.0	pEC50	=	9.0	Functional	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	86843	0	None	-	1	Rat	9.0	pEC50	=	9.0	Functional	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	176544	0	None	-	1	Rat	9.0	pEC50	=	9.0	Functional	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	176544	0	None	-	1	Rat	9.0	pEC50	=	9.0	Functional	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	176544	0	None	-	1	Rat	9.0	pEC50	=	9.0	Functional	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	176562	0	None	-	1	Rat	9.0	pEC50	=	9.0	Functional	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	176562	0	None	-	1	Rat	9.0	pEC50	=	9.0	Functional	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	176562	0	None	-	1	Rat	9.0	pEC50	=	9.0	Functional	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	160116	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	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	160116	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	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	177538	0	None	1	2	Human	9.0	pEC50	=	9.0	Functional	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	177538	0	None	1	2	Human	9.0	pEC50	=	9.0	Functional	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	66586	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	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	66586	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	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	66586	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	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	192800	2	None	4	3	Human	8.9	pEC50	=	8.9	Functional	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	192800	2	None	4	3	Human	8.9	pEC50	=	8.9	Functional	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	92061	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	92061	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	92061	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	92061	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	212211	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	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	215033	2	None	10	3	Mouse	8.9	pEC50	=	8.9	Functional	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	169506	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	169506	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	169506	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	215565	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	215565	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	66527	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	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	66527	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	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	66527	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	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	106316	0	None	1	2	Human	8.9	pEC50	=	8.9	Functional	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	106316	0	None	1	2	Human	8.9	pEC50	=	8.9	Functional	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	106316	0	None	1	2	Human	8.9	pEC50	=	8.9	Functional	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	59068	0	None	1	3	Human	8.9	pEC50	=	8.9	Functional	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	59068	0	None	1	3	Human	8.9	pEC50	=	8.9	Functional	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
	156043182	183138	0	None	67	2	Human	8.9	pEC50	=	8.9	Functional	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	183138	0	None	67	2	Human	8.9	pEC50	=	8.9	Functional	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	182469	0	None	5	2	Human	8.9	pEC50	=	8.9	Functional	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	182469	0	None	5	2	Human	8.9	pEC50	=	8.9	Functional	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	62077	0	None	-1	2	Human	8.9	pEC50	=	8.9	Functional	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	62077	0	None	-1	2	Human	8.9	pEC50	=	8.9	Functional	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	52	None	10	2	Human	8.9	pEC50	=	8.9	Functional	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	52	None	10	2	Human	8.9	pEC50	=	8.9	Functional	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	52	None	10	2	Human	8.9	pEC50	=	8.9	Functional	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	52	None	10	2	Human	8.9	pEC50	=	8.9	Functional	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	52	None	10	2	Human	8.9	pEC50	=	8.9	Functional	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	120558	0	None	100	2	Human	8.9	pEC50	=	8.9	Functional	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	120558	0	None	100	2	Human	8.9	pEC50	=	8.9	Functional	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	120558	0	None	100	2	Human	8.9	pEC50	=	8.9	Functional	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	197855	0	None	10	2	Rat	8.9	pEC50	=	8.9	Functional	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	197855	0	None	10	2	Rat	8.9	pEC50	=	8.9	Functional	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	87906	0	None	-20	2	Rat	8.9	pEC50	=	8.9	Functional	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	87906	0	None	-20	2	Rat	8.9	pEC50	=	8.9	Functional	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	173838	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	173838	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	31436	26	None	3	3	Human	8.9	pEC50	=	8.9	Functional	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	31436	26	None	3	3	Human	8.9	pEC50	=	8.9	Functional	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	31436	26	None	3	3	Human	8.9	pEC50	=	8.9	Functional	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	210863	1	None	89	2	Human	8.9	pEC50	=	8.9	Functional	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	215524	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	215524	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	215538	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	215538	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	92064	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	92064	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	92064	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	92064	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	214982	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	215053	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	189743	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	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	189743	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	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	177094	0	None	-1	2	Human	8.9	pEC50	=	8.9	Functional	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	177094	0	None	-1	2	Human	8.9	pEC50	=	8.9	Functional	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	87918	0	None	-2	2	Rat	8.9	pEC50	=	8.9	Functional	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	87918	0	None	-2	2	Rat	8.9	pEC50	=	8.9	Functional	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	173894	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	173894	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	141791	0	None	2	4	Rat	8.9	pEC50	=	8.9	Functional	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	141791	0	None	2	4	Rat	8.9	pEC50	=	8.9	Functional	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	191878	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	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	191878	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	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	23	None	-6	3	Human	8.9	pEC50	=	8.9	Functional	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	23	None	-6	3	Human	8.9	pEC50	=	8.9	Functional	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	23	None	-6	3	Human	8.9	pEC50	=	8.9	Functional	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	23	None	-6	3	Human	8.9	pEC50	=	8.9	Functional	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	23	None	-6	3	Human	8.9	pEC50	=	8.9	Functional	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	92138	0	None	-2	2	Human	8.9	pEC50	=	8.9	Functional	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	92138	0	None	-2	2	Human	8.9	pEC50	=	8.9	Functional	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	79143	0	None	1	2	Human	8.9	pEC50	=	8.9	Functional	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	79143	0	None	1	2	Human	8.9	pEC50	=	8.9	Functional	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	39685	0	None	-5	2	Human	8.9	pEC50	=	8.9	Functional	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	39685	0	None	-5	2	Human	8.9	pEC50	=	8.9	Functional	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	42	None	-51	6	Human	8.9	pEC50	=	8.9	Functional	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	42	None	-51	6	Human	8.9	pEC50	=	8.9	Functional	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	42	None	-51	6	Human	8.9	pEC50	=	8.9	Functional	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	42	None	-51	6	Human	8.9	pEC50	=	8.9	Functional	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	42	None	-51	6	Human	8.9	pEC50	=	8.9	Functional	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	188629	0	None	-2	2	Rat	8.9	pEC50	=	8.9	Functional	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	188629	0	None	-2	2	Rat	8.9	pEC50	=	8.9	Functional	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	87914	0	None	-18	2	Rat	8.9	pEC50	=	8.9	Functional	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	87914	0	None	-18	2	Rat	8.9	pEC50	=	8.9	Functional	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	160785	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	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	160785	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	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	39685	0	None	-5	2	Human	8.9	pEC50	=	8.9	Functional	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	39685	0	None	-5	2	Human	8.9	pEC50	=	8.9	Functional	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	66595	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	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	66595	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	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	66595	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	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	215563	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	215563	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	156307	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	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	156307	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	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	92809	0	None	6	3	Mouse	8.9	pEC50	=	8.9	Functional	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	92809	0	None	6	3	Mouse	8.9	pEC50	=	8.9	Functional	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	92809	0	None	6	3	Mouse	8.9	pEC50	=	8.9	Functional	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	92809	0	None	6	3	Mouse	8.9	pEC50	=	8.9	Functional	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	171918	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	171918	0	None	-	1	Mouse	8.9	pEC50	=	8.9	Functional	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	212293	0	None	-8	5	Rat	8.9	pEC50	=	8.9	Functional	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	170822	0	None	138	3	Mouse	8.9	pEC50	=	8.9	Functional	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	170822	0	None	138	3	Mouse	8.9	pEC50	=	8.9	Functional	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	171132	0	None	-1	6	Mouse	8.9	pEC50	=	8.9	Functional	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	171132	0	None	-1	6	Mouse	8.9	pEC50	=	8.9	Functional	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	210405	0	None	5	3	Rat	8.9	pEC50	=	8.9	Functional	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	121395	0	None	10	2	Rat	8.9	pEC50	=	8.9	Functional	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	121395	0	None	10	2	Rat	8.9	pEC50	=	8.9	Functional	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	160961	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	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	160961	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	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	171132	0	None	-1	6	Human	8.9	pEC50	=	8.9	Functional	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	171132	0	None	-1	6	Human	8.9	pEC50	=	8.9	Functional	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	171132	0	None	-1	6	Human	8.9	pEC50	=	8.9	Functional	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	171132	0	None	-1	6	Human	8.9	pEC50	=	8.9	Functional	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	212293	0	None	-8	5	Rat	8.8	pEC50	=	8.8	Functional	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	192468	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	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	192468	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	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	201898	1	None	12	4	Human	8.8	pEC50	=	8.8	Functional	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	201898	1	None	12	4	Human	8.8	pEC50	=	8.8	Functional	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	66583	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	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	66583	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	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	66583	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	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	172503	0	None	-	1	Mouse	8.8	pEC50	=	8.8	Functional	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	172503	0	None	-	1	Mouse	8.8	pEC50	=	8.8	Functional	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	191667	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	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	191667	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	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	177149	0	None	2	2	Human	8.8	pEC50	=	8.8	Functional	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	177149	0	None	2	2	Human	8.8	pEC50	=	8.8	Functional	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	169940	0	None	25	3	Mouse	8.8	pEC50	=	8.8	Functional	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	169940	0	None	25	3	Mouse	8.8	pEC50	=	8.8	Functional	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	141054	0	None	251	2	Rat	8.8	pEC50	=	8.8	Functional	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	141054	0	None	251	2	Rat	8.8	pEC50	=	8.8	Functional	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	210403	0	None	-6	3	Rat	8.8	pEC50	=	8.8	Functional	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	87901	0	None	-36	2	Rat	8.8	pEC50	=	8.8	Functional	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	87901	0	None	-36	2	Rat	8.8	pEC50	=	8.8	Functional	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	160815	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	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	160815	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	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	84172	0	None	-114	3	Human	8.8	pEC50	=	8.8	Functional	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	84172	0	None	-114	3	Human	8.8	pEC50	=	8.8	Functional	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	66534	1	None	17	3	Human	8.8	pEC50	=	8.8	Functional	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	66534	1	None	17	3	Human	8.8	pEC50	=	8.8	Functional	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	66534	1	None	17	3	Human	8.8	pEC50	=	8.8	Functional	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	215502	0	None	-	1	Mouse	8.8	pEC50	=	8.8	Functional	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	215531	0	None	-	1	Mouse	8.8	pEC50	=	8.8	Functional	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	215531	0	None	-	1	Mouse	8.8	pEC50	=	8.8	Functional	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	110955	0	None	-4	3	Human	8.8	pEC50	=	8.8	Functional	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	110955	0	None	-4	3	Human	8.8	pEC50	=	8.8	Functional	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	42	None	1	4	Human	8.8	pEC50	=	8.8	Functional	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	42	None	1	4	Human	8.8	pEC50	=	8.8	Functional	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	42	None	1	4	Human	8.8	pEC50	=	8.8	Functional	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	42	None	1	4	Human	8.8	pEC50	=	8.8	Functional	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	176452	0	None	-	1	Mouse	8.8	pEC50	=	8.8	Functional	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	176452	0	None	-	1	Mouse	8.8	pEC50	=	8.8	Functional	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	176452	0	None	-	1	Mouse	8.8	pEC50	=	8.8	Functional	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	188577	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	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	188577	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	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	188577	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	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	101941	3	None	-4	2	Human	8.8	pEC50	=	8.8	Functional	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	101941	3	None	-4	2	Human	8.8	pEC50	=	8.8	Functional	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	101941	3	None	-4	2	Human	8.8	pEC50	=	8.8	Functional	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	101941	3	None	-4	2	Human	8.8	pEC50	=	8.8	Functional	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	101941	3	None	-4	2	Human	8.8	pEC50	=	8.8	Functional	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	101941	3	None	-4	2	Human	8.8	pEC50	=	8.8	Functional	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	101941	3	None	-4	2	Human	8.8	pEC50	=	8.8	Functional	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	101941	3	None	-4	2	Human	8.8	pEC50	=	8.8	Functional	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	101941	3	None	-4	2	Human	8.8	pEC50	=	8.8	Functional	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	101941	3	None	-4	2	Human	8.8	pEC50	=	8.8	Functional	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	179010	0	None	2	2	Human	8.8	pEC50	=	8.8	Functional	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	179010	0	None	2	2	Human	8.8	pEC50	=	8.8	Functional	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	101941	3	None	-4	2	Human	8.8	pEC50	=	8.8	Functional	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	101941	3	None	-4	2	Human	8.8	pEC50	=	8.8	Functional	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	86851	0	None	338	2	Rat	8.8	pEC50	=	8.8	Functional	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	86851	0	None	338	2	Rat	8.8	pEC50	=	8.8	Functional	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	86851	0	None	338	2	Rat	8.8	pEC50	=	8.8	Functional	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	86851	0	None	338	2	Rat	8.8	pEC50	=	8.8	Functional	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	86851	0	None	338	2	Rat	8.8	pEC50	=	8.8	Functional	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	86851	0	None	338	2	Rat	8.8	pEC50	=	8.8	Functional	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	123066	0	None	7	3	Rat	8.8	pEC50	=	8.8	Functional	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	123066	0	None	7	3	Rat	8.8	pEC50	=	8.8	Functional	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	86851	0	None	338	2	Rat	8.8	pEC50	=	8.8	Functional	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	86851	0	None	338	2	Rat	8.8	pEC50	=	8.8	Functional	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	86851	0	None	338	2	Rat	8.8	pEC50	=	8.8	Functional	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	101941	3	None	-4	2	Human	8.8	pEC50	=	8.8	Functional	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	101941	3	None	-4	2	Human	8.8	pEC50	=	8.8	Functional	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	84173	0	None	-2	3	Human	8.8	pEC50	=	8.8	Functional	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	84173	0	None	-2	3	Human	8.8	pEC50	=	8.8	Functional	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	215561	0	None	-	1	Mouse	8.8	pEC50	=	8.8	Functional	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	215561	0	None	-	1	Mouse	8.8	pEC50	=	8.8	Functional	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	177155	0	None	-1	2	Human	8.8	pEC50	=	8.8	Functional	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	177155	0	None	-1	2	Human	8.8	pEC50	=	8.8	Functional	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	211362	3	None	1	2	Human	8.8	pEC50	=	8.8	Functional	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	211776	0	None	-5	5	Human	8.8	pEC50	=	8.8	Functional	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	45	None	-3	8	Human	8.8	pEC50	=	8.8	Functional	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	45	None	-3	8	Human	8.8	pEC50	=	8.8	Functional	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	45	None	-3	8	Human	8.8	pEC50	=	8.8	Functional	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	45	None	-3	8	Human	8.8	pEC50	=	8.8	Functional	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	85324	0	None	-18	3	Human	8.8	pEC50	=	8.8	Functional	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	85324	0	None	-18	3	Human	8.8	pEC50	=	8.8	Functional	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	61784	0	None	1	2	Human	8.8	pEC50	=	8.8	Functional	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	61784	0	None	1	2	Human	8.8	pEC50	=	8.8	Functional	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	198825	3	None	-1	6	Mouse	8.8	pEC50	=	8.8	Functional	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	198825	3	None	-1	6	Mouse	8.8	pEC50	=	8.8	Functional	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	87912	0	None	-100	2	Rat	8.8	pEC50	=	8.8	Functional	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	87912	0	None	-100	2	Rat	8.8	pEC50	=	8.8	Functional	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	198825	3	None	-2	6	Human	8.8	pEC50	=	8.8	Functional	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	198825	3	None	-2	6	Human	8.8	pEC50	=	8.8	Functional	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	198825	3	None	-2	6	Human	8.8	pEC50	=	8.8	Functional	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	198825	3	None	-2	6	Human	8.8	pEC50	=	8.8	Functional	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	88164	0	None	-6	2	Human	8.8	pEC50	=	8.8	Functional	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	88164	0	None	-6	2	Human	8.8	pEC50	=	8.8	Functional	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	190008	0	None	-6	2	Human	8.8	pEC50	=	8.8	Functional	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	190008	0	None	-6	2	Human	8.8	pEC50	=	8.8	Functional	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	82708	0	None	1	3	Human	8.8	pEC50	=	8.8	Functional	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	82708	0	None	1	3	Human	8.8	pEC50	=	8.8	Functional	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	92063	0	None	13	4	Mouse	8.8	pEC50	=	8.8	Functional	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	92063	0	None	13	4	Mouse	8.8	pEC50	=	8.8	Functional	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	214298	0	None	-	1	Mouse	8.8	pEC50	=	8.8	Functional	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	92063	0	None	13	4	Mouse	8.8	pEC50	=	8.8	Functional	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	92063	0	None	13	4	Mouse	8.8	pEC50	=	8.8	Functional	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	215407	0	None	-	1	Mouse	8.8	pEC50	=	8.8	Functional	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	79148	0	None	1	2	Human	8.7	pEC50	=	8.7	Functional	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	79148	0	None	1	2	Human	8.7	pEC50	=	8.7	Functional	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	62075	0	None	-3	2	Human	8.7	pEC50	=	8.7	Functional	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	62075	0	None	-3	2	Human	8.7	pEC50	=	8.7	Functional	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	93145	34	None	-1	4	Human	8.7	pEC50	=	8.7	Functional	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	93145	34	None	-1	4	Human	8.7	pEC50	=	8.7	Functional	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	214593	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	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	140972	0	None	549	2	Rat	8.7	pEC50	=	8.7	Functional	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	140972	0	None	549	2	Rat	8.7	pEC50	=	8.7	Functional	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	179315	0	None	-15	4	Rat	8.7	pEC50	=	8.7	Functional	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	179315	0	None	-15	4	Rat	8.7	pEC50	=	8.7	Functional	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	215364	0	None	-	1	Mouse	8.7	pEC50	=	8.7	Functional	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	174526	0	None	-	1	Mouse	8.7	pEC50	=	8.7	Functional	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	174526	0	None	-	1	Mouse	8.7	pEC50	=	8.7	Functional	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	214221	0	None	-	1	Mouse	8.7	pEC50	=	8.7	Functional	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	176353	0	None	-	1	Mouse	8.7	pEC50	=	8.7	Functional	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	176353	0	None	-	1	Mouse	8.7	pEC50	=	8.7	Functional	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	176353	0	None	-	1	Mouse	8.7	pEC50	=	8.7	Functional	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	175631	0	None	-	1	Mouse	8.7	pEC50	=	8.7	Functional	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	175631	0	None	-	1	Mouse	8.7	pEC50	=	8.7	Functional	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	57214	0	None	1	3	Rat	8.7	pEC50	=	8.7	Functional	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	57214	0	None	1	3	Rat	8.7	pEC50	=	8.7	Functional	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	177934	0	None	-4	2	Human	8.7	pEC50	=	8.7	Functional	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	177934	0	None	-4	2	Human	8.7	pEC50	=	8.7	Functional	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	137444	0	None	3	3	Rat	8.7	pEC50	=	8.7	Functional	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	137444	0	None	3	3	Rat	8.7	pEC50	=	8.7	Functional	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	78375	0	None	10	3	Human	8.7	pEC50	=	8.7	Functional	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	78375	0	None	10	3	Human	8.7	pEC50	=	8.7	Functional	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	176231	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	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	176231	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	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	176231	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	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
	50994381	57214	0	None	1	3	Rat	8.7	pEC50	=	8.7	Functional	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	57214	0	None	1	3	Rat	8.7	pEC50	=	8.7	Functional	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	161066	0	None	-	1	Rat	8.7	pEC50	=	8.7	Functional	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	161066	0	None	-	1	Rat	8.7	pEC50	=	8.7	Functional	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	161066	0	None	-	1	Rat	8.7	pEC50	=	8.7	Functional	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	176237	0	None	-	1	Rat	8.7	pEC50	=	8.7	Functional	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	176237	0	None	-	1	Rat	8.7	pEC50	=	8.7	Functional	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	176237	0	None	-	1	Rat	8.7	pEC50	=	8.7	Functional	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	45	None	-3	8	Human	8.7	pEC50	=	8.7	Functional	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	45	None	-3	8	Human	8.7	pEC50	=	8.7	Functional	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	45	None	-3	8	Human	8.7	pEC50	=	8.7	Functional	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	45	None	-3	8	Human	8.7	pEC50	=	8.7	Functional	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	9227	0	None	10	2	Human	8.7	pEC50	=	8.7	Functional	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	9227	0	None	10	2	Human	8.7	pEC50	=	8.7	Functional	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	188612	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	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	188612	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	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	188612	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	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	8552	0	None	-15	2	Mouse	8.7	pEC50	=	8.7	Functional	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	8552	0	None	-15	2	Mouse	8.7	pEC50	=	8.7	Functional	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	211583	0	None	-2	4	Rat	8.7	pEC50	=	8.7	Functional	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	189165	1	None	-3	7	Human	8.7	pEC50	=	8.7	Functional	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	189165	1	None	-3	7	Human	8.7	pEC50	=	8.7	Functional	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	189165	1	None	-3	7	Human	8.7	pEC50	=	8.7	Functional	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	156728	0	None	1	3	Human	8.0	pEC50	=	8	Functional	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	156728	0	None	1	3	Human	8.0	pEC50	=	8	Functional	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	156834	0	None	2	2	Human	8.0	pEC50	=	8	Functional	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	156834	0	None	2	2	Human	8.0	pEC50	=	8	Functional	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	158603	22	None	19	2	Human	8.0	pEC50	=	8	Functional	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	158603	22	None	19	2	Human	8.0	pEC50	=	8	Functional	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	181700	0	None	-	1	Human	8.0	pEC50	=	8	Functional	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	181700	0	None	-	1	Human	8.0	pEC50	=	8	Functional	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	20	None	-1	8	Human	8.0	pEC50	=	8	Functional	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	20	None	-1	8	Human	8.0	pEC50	=	8	Functional	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	20	None	-1	8	Human	8.0	pEC50	=	8	Functional	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	20	None	-1	8	Human	8.0	pEC50	=	8	Functional	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	20	None	-1	8	Human	8.0	pEC50	=	8	Functional	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	178909	0	None	-1	3	Human	8.0	pEC50	=	8	Functional	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	178909	0	None	-1	3	Human	8.0	pEC50	=	8	Functional	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	93154	0	None	-	1	Human	8.0	pEC50	=	8	Functional	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	93154	0	None	-	1	Human	8.0	pEC50	=	8	Functional	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	62076	0	None	-1	2	Human	8.0	pEC50	=	8	Functional	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	62076	0	None	-1	2	Human	8.0	pEC50	=	8	Functional	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	156495	0	None	-2	3	Human	8.0	pEC50	=	8	Functional	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	156495	0	None	-2	3	Human	8.0	pEC50	=	8	Functional	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	92050	0	None	1	5	Mouse	8.0	pEC50	=	8	Functional	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	92050	0	None	1	5	Mouse	8.0	pEC50	=	8	Functional	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	214821	0	None	-	1	Human	8.0	pEC50	=	8	Functional	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	36	None	-	1	Human	8.0	pEC50	=	8	Functional	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	36	None	-	1	Human	8.0	pEC50	=	8	Functional	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	36	None	-	1	Human	8.0	pEC50	=	8	Functional	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	36	None	-	1	Human	8.0	pEC50	=	8	Functional	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	210445	0	None	2	3	Rat	8.0	pEC50	=	8	Functional	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	158237	0	None	-4	5	Rat	8.0	pEC50	=	8	Functional	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	158237	0	None	-4	5	Rat	8.0	pEC50	=	8	Functional	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	189165	1	None	-3	7	Human	8.0	pEC50	=	8.0	Functional	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	189165	1	None	-3	7	Human	8.0	pEC50	=	8.0	Functional	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	189165	1	None	-3	7	Human	8.0	pEC50	=	8.0	Functional	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	189165	1	None	-3	7	Human	8.0	pEC50	=	8.0	Functional	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	189165	1	None	-3	7	Human	8.0	pEC50	=	8.0	Functional	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	189165	1	None	-3	7	Human	8.0	pEC50	=	8.0	Functional	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	159282	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	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	159282	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	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	110953	0	None	-9	3	Human	8.0	pEC50	=	8.0	Functional	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	110953	0	None	-9	3	Human	8.0	pEC50	=	8.0	Functional	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	209574	4	None	7	4	Rat	8.0	pEC50	=	8.0	Functional	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	209574	4	None	7	4	Rat	8.0	pEC50	=	8.0	Functional	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	210834	30	None	-3	5	Human	8.0	pEC50	=	8.0	Functional	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	210834	30	None	-3	5	Human	8.0	pEC50	=	8.0	Functional	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	158237	0	None	-4	5	Rat	8.0	pEC50	=	8.0	Functional	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	158237	0	None	-4	5	Rat	8.0	pEC50	=	8.0	Functional	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	79131	0	None	1	2	Human	8.0	pEC50	=	8.0	Functional	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	79131	0	None	1	2	Human	8.0	pEC50	=	8.0	Functional	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	81711	0	None	39	2	Human	8.0	pEC50	=	8.0	Functional	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	81711	0	None	39	2	Human	8.0	pEC50	=	8.0	Functional	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	145684	0	None	-2	3	Human	8.0	pEC50	=	8.0	Functional	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	145684	0	None	-2	3	Human	8.0	pEC50	=	8.0	Functional	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	81710	0	None	27	2	Human	8.0	pEC50	=	8.0	Functional	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	81710	0	None	27	2	Human	8.0	pEC50	=	8.0	Functional	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	146448	0	None	10	3	Rat	8.0	pEC50	=	8.0	Functional	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	146448	0	None	10	3	Rat	8.0	pEC50	=	8.0	Functional	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	208811	0	None	-323	8	Human	8.0	pEC50	=	8.0	Functional	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	113926	0	None	1	2	Human	7.0	pEC50	=	7	Functional	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	113926	0	None	1	2	Human	7.0	pEC50	=	7	Functional	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	210440	0	None	-18	3	Rat	7.0	pEC50	=	7	Functional	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	211830	0	None	-2	3	Rat	7.0	pEC50	=	7	Functional	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	120560	0	None	10	2	Human	6.0	pEC50	=	6	Functional	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	120560	0	None	10	2	Human	6.0	pEC50	=	6	Functional	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	120560	0	None	10	2	Human	6.0	pEC50	=	6	Functional	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	120560	0	None	10	2	Human	6.0	pEC50	=	6	Functional	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	93150	0	None	-	1	Human	6.0	pEC50	=	6	Functional	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	93150	0	None	-	1	Human	6.0	pEC50	=	6	Functional	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	158635	0	None	-	1	Human	5.0	pEC50	=	5	Functional	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	158635	0	None	-	1	Human	5.0	pEC50	=	5	Functional	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	113876	1	None	-	1	Human	5.0	pEC50	=	5	Functional	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	113876	1	None	-	1	Human	5.0	pEC50	=	5	Functional	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	113879	0	None	-	1	Human	5.0	pEC50	=	5	Functional	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	113879	0	None	-	1	Human	5.0	pEC50	=	5	Functional	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	191298	0	None	-1737	3	Human	5.0	pEC50	=	5	Functional	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	191298	0	None	-1737	3	Human	5.0	pEC50	=	5	Functional	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	93164	0	None	-	1	Human	5.0	pEC50	=	5	Functional	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	93164	0	None	-	1	Human	5.0	pEC50	=	5	Functional	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	156162	11	None	-776	2	Human	5.0	pEC50	=	5	Functional	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	156162	11	None	-776	2	Human	5.0	pEC50	=	5	Functional	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	117168	0	None	-1445	3	Human	4.0	pEC50	=	4	Functional	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	117168	0	None	-1445	3	Human	4.0	pEC50	=	4	Functional	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	117173	0	None	-812	3	Human	4.0	pEC50	=	4	Functional	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	117173	0	None	-812	3	Human	4.0	pEC50	=	4	Functional	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	45884	7	None	-	1	Human	5.0	pEC50	=	5	Functional	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	45884	7	None	-	1	Human	5.0	pEC50	=	5	Functional	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	176576	0	None	1	2	Human	7.0	pEC50	=	7	Functional	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	176576	0	None	1	2	Human	7.0	pEC50	=	7	Functional	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	174768	0	None	-	1	Human	5.0	pEC50	=	5	Functional	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	174768	0	None	-	1	Human	5.0	pEC50	=	5	Functional	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	5412	0	None	-4	3	Human	6.0	pEC50	=	6.0	Functional	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	5412	0	None	-4	3	Human	6.0	pEC50	=	6.0	Functional	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	55653	5	None	5	2	Human	5.0	pEC50	=	5.0	Functional	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	55653	5	None	5	2	Human	5.0	pEC50	=	5.0	Functional	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	55653	5	None	5	2	Human	5.0	pEC50	=	5.0	Functional	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	163822	3	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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	163822	3	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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	160807	0	None	-7	3	Human	7.0	pEC50	=	7.0	Functional	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	160807	0	None	-7	3	Human	7.0	pEC50	=	7.0	Functional	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	176443	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	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	176443	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	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	176443	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	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	82549	0	None	-	1	Rat	6.0	pEC50	=	6.0	Functional	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	82549	0	None	-	1	Rat	6.0	pEC50	=	6.0	Functional	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	34289	14	None	-1	3	Human	5.0	pEC50	=	5.0	Functional	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	34289	14	None	-1	3	Human	5.0	pEC50	=	5.0	Functional	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	113881	0	None	-	1	Human	5.0	pEC50	=	5.0	Functional	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	113881	0	None	-	1	Human	5.0	pEC50	=	5.0	Functional	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	41	None	2	5	Rat	7.0	pEC50	=	7.0	Functional	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	41	None	2	5	Rat	7.0	pEC50	=	7.0	Functional	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	41	None	2	5	Rat	7.0	pEC50	=	7.0	Functional	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
	CHEMBL5075279	214365	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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
	CHEMBL5075279	214365	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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	214346	0	None	-	1	Human	5.0	pEC50	=	5.0	Functional	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	93259	1	None	-	1	Human	5.0	pEC50	=	5.0	Functional	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	93259	1	None	-	1	Human	5.0	pEC50	=	5.0	Functional	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	214346	0	None	-	1	Human	5.0	pEC50	=	5.0	Functional	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	215220	0	None	-63	2	Human	5.0	pEC50	=	5.0	Functional	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	174218	3	None	1	2	Human	7.0	pEC50	=	7.0	Functional	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	174218	3	None	1	2	Human	7.0	pEC50	=	7.0	Functional	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	79131	0	None	1	2	Human	7.0	pEC50	=	7.0	Functional	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	79131	0	None	1	2	Human	7.0	pEC50	=	7.0	Functional	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	170630	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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	170630	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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	106313	0	None	-97	2	Human	7.0	pEC50	=	7.0	Functional	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	106313	0	None	-97	2	Human	7.0	pEC50	=	7.0	Functional	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	106313	0	None	-97	2	Human	7.0	pEC50	=	7.0	Functional	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
	124037297	160079	0	None	4	2	Human	6.0	pEC50	=	6.0	Functional	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	160079	0	None	4	2	Human	6.0	pEC50	=	6.0	Functional	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	173437	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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	173437	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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	176486	0	None	-	1	Rat	7.0	pEC50	=	7.0	Functional	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	176486	0	None	-	1	Rat	7.0	pEC50	=	7.0	Functional	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	176486	0	None	-	1	Rat	7.0	pEC50	=	7.0	Functional	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	91400	0	None	-	1	Rat	6.0	pEC50	=	6.0	Functional	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	91400	0	None	-	1	Rat	6.0	pEC50	=	6.0	Functional	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	164587	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	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	164587	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	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	51946	4	None	-	1	Human	5.0	pEC50	=	5.0	Functional	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	51946	4	None	-	1	Human	5.0	pEC50	=	5.0	Functional	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	182638	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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	182638	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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	94039	0	None	-67	2	Human	6.0	pEC50	=	6.0	Functional	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	94039	0	None	-67	2	Human	6.0	pEC50	=	6.0	Functional	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	212705	0	None	-9	4	Rat	7.0	pEC50	=	7.0	Functional	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	59301	0	None	-	1	Human	5.0	pEC50	=	5.0	Functional	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	59301	0	None	-	1	Human	5.0	pEC50	=	5.0	Functional	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	214305	0	None	-41	2	Human	6.0	pEC50	=	6.0	Functional	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	214256	2	None	-	1	Human	5.0	pEC50	=	5.0	Functional	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	169742	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	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	169742	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	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	179861	0	None	13	2	Human	8.0	pEC50	=	8.0	Functional	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	179861	0	None	13	2	Human	8.0	pEC50	=	8.0	Functional	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	94230	0	None	-23	3	Human	8.0	pEC50	=	8.0	Functional	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	94230	0	None	-23	3	Human	8.0	pEC50	=	8.0	Functional	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	92136	0	None	-1	2	Human	8.0	pEC50	=	8.0	Functional	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	92136	0	None	-1	2	Human	8.0	pEC50	=	8.0	Functional	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	198939	0	None	-4	2	Human	8.0	pEC50	=	8.0	Functional	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	198939	0	None	-4	2	Human	8.0	pEC50	=	8.0	Functional	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	214593	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	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	146448	0	None	10	3	Rat	8.0	pEC50	=	8.0	Functional	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	146448	0	None	10	3	Rat	8.0	pEC50	=	8.0	Functional	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	214722	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	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	214722	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	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	79143	0	None	1	2	Human	8.0	pEC50	=	8.0	Functional	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	79143	0	None	1	2	Human	8.0	pEC50	=	8.0	Functional	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	160022	0	None	-7	3	Human	7.9	pEC50	=	7.9	Functional	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	160022	0	None	-7	3	Human	7.9	pEC50	=	7.9	Functional	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	117733	0	None	-	1	Mouse	7.9	pEC50	=	7.9	Functional	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	117733	0	None	-	1	Mouse	7.9	pEC50	=	7.9	Functional	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	212239	0	None	147	2	Human	7.9	pEC50	=	7.9	Functional	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	139193	0	None	-1	3	Human	7.9	pEC50	=	7.9	Functional	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	139193	0	None	-1	3	Human	7.9	pEC50	=	7.9	Functional	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	214647	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	79136	0	None	3	2	Human	7.9	pEC50	=	7.9	Functional	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	79136	0	None	3	2	Human	7.9	pEC50	=	7.9	Functional	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	210528	0	None	-7	5	Rat	7.9	pEC50	=	7.9	Functional	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	42	None	1	4	Human	7.9	pEC50	=	7.9	Functional	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	42	None	1	4	Human	7.9	pEC50	=	7.9	Functional	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	42	None	1	4	Human	7.9	pEC50	=	7.9	Functional	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	42	None	1	4	Human	7.9	pEC50	=	7.9	Functional	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	8550	0	None	-22	2	Mouse	7.9	pEC50	=	7.9	Functional	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	8550	0	None	-22	2	Mouse	7.9	pEC50	=	7.9	Functional	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	212705	0	None	-9	4	Rat	7.0	pEC50	=	7.0	Functional	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	45	None	-3	8	Human	7.0	pEC50	=	7.0	Functional	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	45	None	-3	8	Human	7.0	pEC50	=	7.0	Functional	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	45	None	-3	8	Human	7.0	pEC50	=	7.0	Functional	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	45	None	-3	8	Human	7.0	pEC50	=	7.0	Functional	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	158367	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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	158367	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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	164261	1	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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	164261	1	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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	45	None	-3	8	Human	7.0	pEC50	=	7.0	Functional	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	45	None	-3	8	Human	7.0	pEC50	=	7.0	Functional	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	45	None	-3	8	Human	7.0	pEC50	=	7.0	Functional	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	45	None	-3	8	Human	7.0	pEC50	=	7.0	Functional	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	45	None	-3	8	Human	7.0	pEC50	=	7.0	Functional	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	45	None	-3	8	Human	7.0	pEC50	=	7.0	Functional	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	45	None	-3	8	Human	7.0	pEC50	=	7.0	Functional	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	45	None	-3	8	Human	7.0	pEC50	=	7.0	Functional	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	45	None	-3	8	Human	7.0	pEC50	=	7.0	Functional	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	45	None	-3	8	Human	7.0	pEC50	=	7.0	Functional	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	45	None	-3	8	Human	7.0	pEC50	=	7.0	Functional	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	45	None	-3	8	Human	7.0	pEC50	=	7.0	Functional	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	179011	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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	179011	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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	137587	0	None	-158	3	Human	7.0	pEC50	=	7.0	Functional	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	137587	0	None	-158	3	Human	7.0	pEC50	=	7.0	Functional	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
	137631684	156365	0	None	-3890	2	Human	7.0	pEC50	=	7.0	Functional	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	156365	0	None	-3890	2	Human	7.0	pEC50	=	7.0	Functional	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	45	None	-3	8	Human	7.0	pEC50	=	7.0	Functional	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	45	None	-3	8	Human	7.0	pEC50	=	7.0	Functional	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	45	None	-3	8	Human	7.0	pEC50	=	7.0	Functional	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	45	None	-3	8	Human	7.0	pEC50	=	7.0	Functional	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	176846	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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	176846	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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	9981	0	None	-1	3	Human	7.0	pEC50	=	7.0	Functional	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	9981	0	None	-1	3	Human	7.0	pEC50	=	7.0	Functional	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
	11179386	159659	4	None	-43651	2	Human	6.0	pEC50	=	6.0	Functional	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	159659	4	None	-43651	2	Human	6.0	pEC50	=	6.0	Functional	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	198665	7	None	3	2	Human	6.0	pEC50	=	6.0	Functional	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	198665	7	None	3	2	Human	6.0	pEC50	=	6.0	Functional	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	214256	2	None	-	1	Human	5.0	pEC50	=	5.0	Functional	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	164322	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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	164322	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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	176523	0	None	-	1	Rat	7.0	pEC50	=	7.0	Functional	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	176523	0	None	-	1	Rat	7.0	pEC50	=	7.0	Functional	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	176523	0	None	-	1	Rat	7.0	pEC50	=	7.0	Functional	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
	CHEMBL5093143	215412	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	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	161414	0	None	-3	3	Human	7.0	pEC50	=	7.0	Functional	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	161414	0	None	-3	3	Human	7.0	pEC50	=	7.0	Functional	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
	145963594	161414	0	None	-3	3	Human	7.0	pEC50	=	7.0	Functional	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	161414	0	None	-3	3	Human	7.0	pEC50	=	7.0	Functional	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	159344	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	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	159344	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	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	159561	1	None	-	1	Human	6.0	pEC50	=	6.0	Functional	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	159561	1	None	-	1	Human	6.0	pEC50	=	6.0	Functional	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	113870	12	None	-	1	Human	6.0	pEC50	=	6.0	Functional	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	113870	12	None	-	1	Human	6.0	pEC50	=	6.0	Functional	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	215412	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	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	177199	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	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	177199	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	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	160495	0	None	-1	3	Human	7.0	pEC50	=	7.0	Functional	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	160495	0	None	-1	3	Human	7.0	pEC50	=	7.0	Functional	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	160948	0	None	1	2	Human	6.0	pEC50	=	6.0	Functional	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	160948	0	None	1	2	Human	6.0	pEC50	=	6.0	Functional	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
	72735386	106369	0	None	-81	2	Human	6.9	pEC50	=	6.9	Functional	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	106369	0	None	-81	2	Human	6.9	pEC50	=	6.9	Functional	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	106369	0	None	-81	2	Human	6.9	pEC50	=	6.9	Functional	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	96798	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	96798	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	163539	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	163539	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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
	CHEMBL5082661	214816	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	177876	0	None	-3	3	Human	6.9	pEC50	=	6.9	Functional	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	177876	0	None	-3	3	Human	6.9	pEC50	=	6.9	Functional	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	176346	0	None	-	1	Rat	6.9	pEC50	=	6.9	Functional	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	176346	0	None	-	1	Rat	6.9	pEC50	=	6.9	Functional	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	176346	0	None	-	1	Rat	6.9	pEC50	=	6.9	Functional	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	202582	0	None	-25	5	Rat	6.9	pEC50	=	6.9	Functional	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	202582	0	None	-25	5	Rat	6.9	pEC50	=	6.9	Functional	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	104469	0	None	-	1	Rat	6.9	pEC50	=	6.9	Functional	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	104469	0	None	-	1	Rat	6.9	pEC50	=	6.9	Functional	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	90464	0	None	-2	2	Human	6.9	pEC50	=	6.9	Functional	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	90464	0	None	-2	2	Human	6.9	pEC50	=	6.9	Functional	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	190589	0	None	-4	2	Rat	5.9	pEC50	=	5.9	Functional	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	190589	0	None	-4	2	Rat	5.9	pEC50	=	5.9	Functional	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	210528	0	None	-7	5	Rat	7.9	pEC50	=	7.9	Functional	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	132737	0	None	-7	2	Human	7.9	pEC50	=	7.9	Functional	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	132737	0	None	-7	2	Human	7.9	pEC50	=	7.9	Functional	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	42	None	1	4	Human	7.9	pEC50	=	7.9	Functional	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	42	None	1	4	Human	7.9	pEC50	=	7.9	Functional	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	42	None	1	4	Human	7.9	pEC50	=	7.9	Functional	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	42	None	1	4	Human	7.9	pEC50	=	7.9	Functional	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	215518	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	154645	0	None	3	2	Human	7.9	pEC50	=	7.9	Functional	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	154645	0	None	3	2	Human	7.9	pEC50	=	7.9	Functional	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	88538	0	None	4	3	Human	7.9	pEC50	=	7.9	Functional	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	88538	0	None	4	3	Human	7.9	pEC50	=	7.9	Functional	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	183328	0	None	-35	5	Human	7.9	pEC50	=	7.9	Functional	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	183328	0	None	-35	5	Human	7.9	pEC50	=	7.9	Functional	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	93145	34	None	-1	4	Human	7.9	pEC50	=	7.9	Functional	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	93145	34	None	-1	4	Human	7.9	pEC50	=	7.9	Functional	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	81707	0	None	3	2	Human	7.9	pEC50	=	7.9	Functional	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	81707	0	None	3	2	Human	7.9	pEC50	=	7.9	Functional	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	210408	0	None	-4	3	Rat	7.9	pEC50	=	7.9	Functional	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	72839	14	None	-6	4	Rat	7.9	pEC50	=	7.9	Functional	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	72839	14	None	-6	4	Rat	7.9	pEC50	=	7.9	Functional	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	189243	0	None	-30	2	Rat	7.9	pEC50	=	7.9	Functional	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	189243	0	None	-30	2	Rat	7.9	pEC50	=	7.9	Functional	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	176574	0	None	-	1	Rat	7.9	pEC50	=	7.9	Functional	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	176574	0	None	-	1	Rat	7.9	pEC50	=	7.9	Functional	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	176574	0	None	-	1	Rat	7.9	pEC50	=	7.9	Functional	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
	CHEMBL5085974	215004	0	None	11	2	Human	7.9	pEC50	=	7.9	Functional	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	215117	0	None	-	1	Mouse	7.9	pEC50	=	7.9	Functional	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	160144	0	None	-5	3	Human	7.9	pEC50	=	7.9	Functional	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	160144	0	None	-5	3	Human	7.9	pEC50	=	7.9	Functional	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	93152	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	93152	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	93162	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	93162	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	182720	0	None	-549	4	Human	7.9	pEC50	=	7.9	Functional	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	182720	0	None	-549	4	Human	7.9	pEC50	=	7.9	Functional	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	214906	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	159804	0	None	47	2	Human	6.9	pEC50	=	6.9	Functional	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	159804	0	None	47	2	Human	6.9	pEC50	=	6.9	Functional	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	31113	15	None	2	2	Human	6.9	pEC50	=	6.9	Functional	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	31113	15	None	2	2	Human	6.9	pEC50	=	6.9	Functional	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	31113	15	None	2	2	Human	6.9	pEC50	=	6.9	Functional	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	38	None	-19	3	Human	6.9	pEC50	=	6.9	Functional	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	38	None	-19	3	Human	6.9	pEC50	=	6.9	Functional	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	38	None	-19	3	Human	6.9	pEC50	=	6.9	Functional	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	19	None	-85	7	Human	6.9	pEC50	=	6.9	Functional	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	19	None	-85	7	Human	6.9	pEC50	=	6.9	Functional	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	19	None	-85	7	Human	6.9	pEC50	=	6.9	Functional	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	6578	0	None	-19	3	Human	6.9	pEC50	=	6.9	Functional	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	6578	0	None	-19	3	Human	6.9	pEC50	=	6.9	Functional	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	6578	0	None	-19	3	Human	6.9	pEC50	=	6.9	Functional	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	6579	0	None	-19	3	Human	6.9	pEC50	=	6.9	Functional	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	6579	0	None	-19	3	Human	6.9	pEC50	=	6.9	Functional	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	6652	0	None	-19	3	Human	6.9	pEC50	=	6.9	Functional	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	6652	0	None	-19	3	Human	6.9	pEC50	=	6.9	Functional	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	6652	0	None	-19	3	Human	6.9	pEC50	=	6.9	Functional	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	6653	0	None	-19	3	Human	6.9	pEC50	=	6.9	Functional	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	6653	0	None	-19	3	Human	6.9	pEC50	=	6.9	Functional	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	6956	0	None	-19	3	Human	6.9	pEC50	=	6.9	Functional	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	6956	0	None	-19	3	Human	6.9	pEC50	=	6.9	Functional	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	7079	0	None	-19	3	Human	6.9	pEC50	=	6.9	Functional	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	7079	0	None	-19	3	Human	6.9	pEC50	=	6.9	Functional	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	7080	0	None	-19	3	Human	6.9	pEC50	=	6.9	Functional	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	7080	0	None	-19	3	Human	6.9	pEC50	=	6.9	Functional	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	7081	0	None	-19	3	Human	6.9	pEC50	=	6.9	Functional	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	7081	0	None	-19	3	Human	6.9	pEC50	=	6.9	Functional	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	210441	0	None	-14	3	Rat	6.9	pEC50	=	6.9	Functional	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	202582	0	None	-25	5	Rat	6.9	pEC50	=	6.9	Functional	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	202582	0	None	-25	5	Rat	6.9	pEC50	=	6.9	Functional	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	20	None	-7	8	Mouse	6.9	pEC50	=	6.9	Functional	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	20	None	-7	8	Mouse	6.9	pEC50	=	6.9	Functional	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	20	None	-7	8	Mouse	6.9	pEC50	=	6.9	Functional	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	20	None	-7	8	Mouse	6.9	pEC50	=	6.9	Functional	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	20	None	-7	8	Mouse	6.9	pEC50	=	6.9	Functional	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	120552	0	None	3	2	Human	4.9	pEC50	=	4.9	Functional	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	120552	0	None	3	2	Human	4.9	pEC50	=	4.9	Functional	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	120552	0	None	3	2	Human	4.9	pEC50	=	4.9	Functional	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	109710	0	None	-13	3	Human	5.9	pEC50	=	5.9	Functional	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	109710	0	None	-13	3	Human	5.9	pEC50	=	5.9	Functional	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	59622	17	None	-	1	Human	4.9	pEC50	=	4.9	Functional	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	59622	17	None	-	1	Human	4.9	pEC50	=	4.9	Functional	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	190198	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	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	190198	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	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	156240	0	None	-467735	2	Human	4.9	pEC50	=	4.9	Functional	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	156240	0	None	-467735	2	Human	4.9	pEC50	=	4.9	Functional	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	57306	0	None	-138	2	Human	5.9	pEC50	=	5.9	Functional	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	57306	0	None	-138	2	Human	5.9	pEC50	=	5.9	Functional	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	20	None	1	8	Rat	6.9	pEC50	=	6.9	Functional	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	20	None	1	8	Rat	6.9	pEC50	=	6.9	Functional	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	20	None	1	8	Rat	6.9	pEC50	=	6.9	Functional	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	20	None	1	8	Rat	6.9	pEC50	=	6.9	Functional	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	20	None	1	8	Rat	6.9	pEC50	=	6.9	Functional	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	20	None	1	8	Rat	6.9	pEC50	=	6.9	Functional	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	20	None	1	8	Rat	6.9	pEC50	=	6.9	Functional	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	20	None	1	8	Rat	6.9	pEC50	=	6.9	Functional	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	20	None	1	8	Rat	6.9	pEC50	=	6.9	Functional	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	20	None	1	8	Rat	6.9	pEC50	=	6.9	Functional	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	20	None	1	8	Rat	6.9	pEC50	=	6.9	Functional	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	20	None	1	8	Rat	6.9	pEC50	=	6.9	Functional	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	20	None	1	8	Rat	6.9	pEC50	=	6.9	Functional	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	20	None	1	8	Rat	6.9	pEC50	=	6.9	Functional	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	20	None	1	8	Rat	6.9	pEC50	=	6.9	Functional	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	91404	0	None	-	1	Rat	5.9	pEC50	=	5.9	Functional	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	91404	0	None	-	1	Rat	5.9	pEC50	=	5.9	Functional	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	91412	0	None	-	1	Rat	5.9	pEC50	=	5.9	Functional	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	91412	0	None	-	1	Rat	5.9	pEC50	=	5.9	Functional	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	162105	1	None	-	1	Human	4.9	pEC50	=	4.9	Functional	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	162105	1	None	-	1	Human	4.9	pEC50	=	4.9	Functional	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	91404	0	None	-	1	Rat	5.9	pEC50	=	5.9	Functional	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	91404	0	None	-	1	Rat	5.9	pEC50	=	5.9	Functional	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	91412	0	None	-	1	Rat	5.9	pEC50	=	5.9	Functional	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	91412	0	None	-	1	Rat	5.9	pEC50	=	5.9	Functional	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	163777	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	163777	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	214783	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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
	5113115	20630	6	None	5	2	Human	4.9	pEC50	=	4.9	Functional	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	20630	6	None	5	2	Human	4.9	pEC50	=	4.9	Functional	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	171187	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	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	171187	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	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	88505	0	None	2	3	Rat	6.9	pEC50	=	6.9	Functional	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	88505	0	None	2	3	Rat	6.9	pEC50	=	6.9	Functional	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	181783	0	None	-3	5	Human	6.9	pEC50	=	6.9	Functional	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	181783	0	None	-3	5	Human	6.9	pEC50	=	6.9	Functional	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	88505	0	None	2	3	Rat	6.9	pEC50	=	6.9	Functional	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	88505	0	None	2	3	Rat	6.9	pEC50	=	6.9	Functional	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	160146	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	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	160146	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	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	93158	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	93158	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	181783	0	None	-3	5	Human	6.9	pEC50	=	6.9	Functional	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	181783	0	None	-3	5	Human	6.9	pEC50	=	6.9	Functional	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
	130431390	163684	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	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	163684	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	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	160545	0	None	-6	3	Human	6.9	pEC50	=	6.9	Functional	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	160545	0	None	-6	3	Human	6.9	pEC50	=	6.9	Functional	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	42	None	-51	6	Human	5.9	pEC50	=	5.9	Functional	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	42	None	-51	6	Human	5.9	pEC50	=	5.9	Functional	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	42	None	-51	6	Human	5.9	pEC50	=	5.9	Functional	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	42	None	-51	6	Human	5.9	pEC50	=	5.9	Functional	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	42	None	-51	6	Human	5.9	pEC50	=	5.9	Functional	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	177884	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	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	177884	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	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	159838	0	None	23	2	Human	6.9	pEC50	=	6.9	Functional	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	159838	0	None	23	2	Human	6.9	pEC50	=	6.9	Functional	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	42	None	-51	6	Human	5.9	pEC50	=	5.9	Functional	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	42	None	-51	6	Human	5.9	pEC50	=	5.9	Functional	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	42	None	-51	6	Human	5.9	pEC50	=	5.9	Functional	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	42	None	-51	6	Human	5.9	pEC50	=	5.9	Functional	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	42	None	-51	6	Human	5.9	pEC50	=	5.9	Functional	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	90463	0	None	-2	2	Human	6.9	pEC50	=	6.9	Functional	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	90463	0	None	-2	2	Human	6.9	pEC50	=	6.9	Functional	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	156917	0	None	-1698	2	Human	4.9	pEC50	=	4.9	Functional	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	156917	0	None	-1698	2	Human	4.9	pEC50	=	4.9	Functional	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	159837	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	159837	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	52178	6	None	3	2	Human	4.9	pEC50	=	4.9	Functional	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	52178	6	None	3	2	Human	4.9	pEC50	=	4.9	Functional	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	173640	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	173640	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	164184	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	164184	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	177137	0	None	-5	2	Human	7.9	pEC50	=	7.9	Functional	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	177137	0	None	-5	2	Human	7.9	pEC50	=	7.9	Functional	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	196810	0	None	-2	2	Human	7.9	pEC50	=	7.9	Functional	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	196810	0	None	-2	2	Human	7.9	pEC50	=	7.9	Functional	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
	127050833	140969	0	None	-	1	Rat	7.9	pEC50	=	7.9	Functional	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	140969	0	None	-	1	Rat	7.9	pEC50	=	7.9	Functional	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	209574	4	None	7	4	Rat	7.9	pEC50	=	7.9	Functional	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	176259	0	None	-	1	Rat	7.9	pEC50	=	7.9	Functional	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	176259	0	None	-	1	Rat	7.9	pEC50	=	7.9	Functional	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	176259	0	None	-	1	Rat	7.9	pEC50	=	7.9	Functional	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	209574	4	None	7	4	Rat	7.9	pEC50	=	7.9	Functional	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	160189	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	160189	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	42	None	1	4	Human	7.9	pEC50	=	7.9	Functional	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	42	None	1	4	Human	7.9	pEC50	=	7.9	Functional	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	42	None	1	4	Human	7.9	pEC50	=	7.9	Functional	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	42	None	1	4	Human	7.9	pEC50	=	7.9	Functional	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	181204	0	None	-5	4	Human	7.9	pEC50	=	7.9	Functional	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	181204	0	None	-5	4	Human	7.9	pEC50	=	7.9	Functional	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	175786	0	None	-	1	Mouse	7.9	pEC50	=	7.9	Functional	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	175786	0	None	-	1	Mouse	7.9	pEC50	=	7.9	Functional	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	188597	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	188597	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	188597	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	214451	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	45	None	-3	8	Human	7.9	pEC50	=	7.9	Functional	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	45	None	-3	8	Human	7.9	pEC50	=	7.9	Functional	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	45	None	-3	8	Human	7.9	pEC50	=	7.9	Functional	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	45	None	-3	8	Human	7.9	pEC50	=	7.9	Functional	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	42	None	1	4	Human	7.9	pEC50	=	7.9	Functional	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	42	None	1	4	Human	7.9	pEC50	=	7.9	Functional	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	42	None	1	4	Human	7.9	pEC50	=	7.9	Functional	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	42	None	1	4	Human	7.9	pEC50	=	7.9	Functional	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	84688	0	None	-10	3	Human	6.9	pEC50	=	6.9	Functional	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	84688	0	None	-10	3	Human	6.9	pEC50	=	6.9	Functional	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	177277	0	None	-39	2	Human	6.9	pEC50	=	6.9	Functional	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	177277	0	None	-39	2	Human	6.9	pEC50	=	6.9	Functional	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	61207	0	None	-4	2	Human	6.9	pEC50	=	6.9	Functional	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	61207	0	None	-4	2	Human	6.9	pEC50	=	6.9	Functional	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	106355	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	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	106355	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	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	106355	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	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	62079	0	None	-23	2	Human	6.9	pEC50	=	6.9	Functional	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	62079	0	None	-23	2	Human	6.9	pEC50	=	6.9	Functional	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	15331	0	None	-1000	5	Rat	6.9	pEC50	=	6.9	Functional	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	15331	0	None	-1000	5	Rat	6.9	pEC50	=	6.9	Functional	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	165873	0	None	-131	2	Rat	6.9	pEC50	=	6.9	Functional	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	165873	0	None	-131	2	Rat	6.9	pEC50	=	6.9	Functional	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
	5523	3851	25	None	-2	3	Human	5.9	pEC50	=	5.9	Functional	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	25	None	-2	3	Human	5.9	pEC50	=	5.9	Functional	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	25	None	-2	3	Human	5.9	pEC50	=	5.9	Functional	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	25	None	-2	3	Human	5.9	pEC50	=	5.9	Functional	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	180126	0	None	1	2	Human	6.9	pEC50	=	6.9	Functional	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	180126	0	None	1	2	Human	6.9	pEC50	=	6.9	Functional	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	215377	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	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	175929	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	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	175929	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	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
	49863732	15331	0	None	-1000	5	Rat	6.9	pEC50	=	6.9	Functional	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	15331	0	None	-1000	5	Rat	6.9	pEC50	=	6.9	Functional	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	15333	0	None	-79	5	Rat	6.9	pEC50	=	6.9	Functional	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	15333	0	None	-79	5	Rat	6.9	pEC50	=	6.9	Functional	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	164552	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	164552	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	160173	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	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	160173	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	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	160212	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	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	160212	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	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	177213	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	177213	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	121007	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	121007	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	113868	9	None	-	1	Human	4.9	pEC50	=	4.9	Functional	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	113868	9	None	-	1	Human	4.9	pEC50	=	4.9	Functional	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	113887	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	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	113887	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	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	160735	0	None	1	2	Human	5.9	pEC50	=	5.9	Functional	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	160735	0	None	1	2	Human	5.9	pEC50	=	5.9	Functional	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	96831	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	96831	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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
	126619400	172070	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	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	172070	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	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	91400	0	None	-	1	Rat	5.9	pEC50	=	5.9	Functional	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	91400	0	None	-	1	Rat	5.9	pEC50	=	5.9	Functional	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
	13787553	201809	0	None	-8	2	Rat	5.9	pEC50	=	5.9	Functional	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	201809	0	None	-8	2	Rat	5.9	pEC50	=	5.9	Functional	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	79144	0	None	-1	2	Human	6.9	pEC50	=	6.9	Functional	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	79144	0	None	-1	2	Human	6.9	pEC50	=	6.9	Functional	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	5449	0	None	-1	3	Human	6.9	pEC50	=	6.9	Functional	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	5449	0	None	-1	3	Human	6.9	pEC50	=	6.9	Functional	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	160573	0	None	-6	3	Human	6.9	pEC50	=	6.9	Functional	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	160573	0	None	-6	3	Human	6.9	pEC50	=	6.9	Functional	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	41	None	-2	5	Human	7.9	pEC50	=	7.9	Functional	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	41	None	-2	5	Human	7.9	pEC50	=	7.9	Functional	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	41	None	-2	5	Human	7.9	pEC50	=	7.9	Functional	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	173946	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	173946	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	173946	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	173946	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	92018	0	None	1	2	Human	7.9	pEC50	=	7.9	Functional	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	92018	0	None	1	2	Human	7.9	pEC50	=	7.9	Functional	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	19	None	-2	4	Human	7.9	pEC50	=	7.9	Functional	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	19	None	-2	4	Human	7.9	pEC50	=	7.9	Functional	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	19	None	-2	4	Human	7.9	pEC50	=	7.9	Functional	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	19	None	-2	4	Human	7.9	pEC50	=	7.9	Functional	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	19	None	-2	4	Human	7.9	pEC50	=	7.9	Functional	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	210442	0	None	-2	3	Rat	7.9	pEC50	=	7.9	Functional	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	124215	0	None	-	1	Rat	7.9	pEC50	=	7.9	Functional	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	124215	0	None	-	1	Rat	7.9	pEC50	=	7.9	Functional	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	92062	0	None	-	1	Mouse	7.9	pEC50	=	7.9	Functional	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	92062	0	None	-	1	Mouse	7.9	pEC50	=	7.9	Functional	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	214657	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	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	92062	0	None	-	1	Mouse	7.9	pEC50	=	7.9	Functional	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	92062	0	None	-	1	Mouse	7.9	pEC50	=	7.9	Functional	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	79135	0	None	5	2	Human	7.8	pEC50	=	7.8	Functional	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	79135	0	None	5	2	Human	7.8	pEC50	=	7.8	Functional	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	214949	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	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	79149	0	None	-1	2	Human	7.8	pEC50	=	7.8	Functional	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	79149	0	None	-1	2	Human	7.8	pEC50	=	7.8	Functional	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	41	None	-2	5	Human	7.8	pEC50	=	7.8	Functional	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	41	None	-2	5	Human	7.8	pEC50	=	7.8	Functional	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	41	None	-2	5	Human	7.8	pEC50	=	7.8	Functional	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	41	None	-2	5	Human	7.8	pEC50	=	7.8	Functional	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	41	None	-2	5	Human	7.8	pEC50	=	7.8	Functional	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	41	None	-2	5	Human	7.8	pEC50	=	7.8	Functional	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	161310	0	None	-6	5	Rat	7.8	pEC50	=	7.8	Functional	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	161310	0	None	-6	5	Rat	7.8	pEC50	=	7.8	Functional	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
	9848990	189165	1	None	-3	7	Human	7.8	pEC50	=	7.8	Functional	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	189165	1	None	-3	7	Human	7.8	pEC50	=	7.8	Functional	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	189165	1	None	-3	7	Human	7.8	pEC50	=	7.8	Functional	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	156770	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	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	156770	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	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	145645	0	None	-26	2	Human	6.9	pEC50	=	6.9	Functional	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	145645	0	None	-26	2	Human	6.9	pEC50	=	6.9	Functional	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	61221	0	None	-3	2	Human	6.9	pEC50	=	6.9	Functional	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	61221	0	None	-3	2	Human	6.9	pEC50	=	6.9	Functional	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	85361	0	None	-16	3	Human	6.9	pEC50	=	6.9	Functional	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	85361	0	None	-16	3	Human	6.9	pEC50	=	6.9	Functional	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	210518	0	None	-3	3	Rat	6.9	pEC50	=	6.9	Functional	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	15333	0	None	-79	5	Rat	6.9	pEC50	=	6.9	Functional	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	15333	0	None	-79	5	Rat	6.9	pEC50	=	6.9	Functional	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	97004	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	97004	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	170886	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	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	170886	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	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	164332	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	164332	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	160755	0	None	-2	2	Human	5.9	pEC50	=	5.9	Functional	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	160755	0	None	-2	2	Human	5.9	pEC50	=	5.9	Functional	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	178063	0	None	-57	2	Human	6.9	pEC50	=	6.9	Functional	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	178063	0	None	-57	2	Human	6.9	pEC50	=	6.9	Functional	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	214987	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	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	59564	5	None	18	2	Human	5.9	pEC50	=	5.9	Functional	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	59564	5	None	18	2	Human	5.9	pEC50	=	5.9	Functional	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	158742	0	None	-114815	2	Human	4.9	pEC50	=	4.9	Functional	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	158742	0	None	-114815	2	Human	4.9	pEC50	=	4.9	Functional	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	170229	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	170229	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	170343	0	None	-	1	Rat	5.9	pEC50	=	5.9	Functional	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	170343	0	None	-	1	Rat	5.9	pEC50	=	5.9	Functional	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	57314	0	None	-3	3	Human	6.8	pEC50	=	6.8	Functional	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	57314	0	None	-3	3	Human	6.8	pEC50	=	6.8	Functional	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	173304	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	173304	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	91401	0	None	-4	2	Rat	5.8	pEC50	=	5.8	Functional	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	91401	0	None	-4	2	Rat	5.8	pEC50	=	5.8	Functional	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	41376	7	None	-	1	Human	4.8	pEC50	=	4.8	Functional	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	41376	7	None	-	1	Human	4.8	pEC50	=	4.8	Functional	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	45	None	-5	8	Rat	6.8	pEC50	=	6.8	Functional	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	45	None	-5	8	Rat	6.8	pEC50	=	6.8	Functional	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	45	None	-5	8	Rat	6.8	pEC50	=	6.8	Functional	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	45	None	-5	8	Rat	6.8	pEC50	=	6.8	Functional	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	165408	0	None	-2	2	Rat	6.8	pEC50	=	6.8	Functional	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	165408	0	None	-2	2	Rat	6.8	pEC50	=	6.8	Functional	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	45	None	-5	8	Rat	6.8	pEC50	=	6.8	Functional	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	45	None	-5	8	Rat	6.8	pEC50	=	6.8	Functional	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	45	None	-5	8	Rat	6.8	pEC50	=	6.8	Functional	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	45	None	-5	8	Rat	6.8	pEC50	=	6.8	Functional	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	214360	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	20	None	-1	8	Human	6.8	pEC50	=	6.8	Functional	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	20	None	-1	8	Human	6.8	pEC50	=	6.8	Functional	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	20	None	-1	8	Human	6.8	pEC50	=	6.8	Functional	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	20	None	-1	8	Human	6.8	pEC50	=	6.8	Functional	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	20	None	-1	8	Human	6.8	pEC50	=	6.8	Functional	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	175405	0	None	-2	2	Rat	5.8	pEC50	=	5.8	Functional	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	175405	0	None	-2	2	Rat	5.8	pEC50	=	5.8	Functional	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	163607	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	163607	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	164721	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	164721	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	79145	0	None	1	2	Human	6.8	pEC50	=	6.8	Functional	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	79145	0	None	1	2	Human	6.8	pEC50	=	6.8	Functional	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	79179	0	None	-44	3	Human	6.8	pEC50	=	6.8	Functional	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	79179	0	None	-44	3	Human	6.8	pEC50	=	6.8	Functional	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
	118560889	180248	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	180248	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	45	None	-3	8	Human	7.8	pEC50	=	7.8	Functional	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	45	None	-3	8	Human	7.8	pEC50	=	7.8	Functional	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	45	None	-3	8	Human	7.8	pEC50	=	7.8	Functional	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	45	None	-3	8	Human	7.8	pEC50	=	7.8	Functional	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	176582	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	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	176582	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	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	176582	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	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	180774	0	None	4	3	Human	7.8	pEC50	=	7.8	Functional	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	180774	0	None	4	3	Human	7.8	pEC50	=	7.8	Functional	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	106430	0	None	-1	2	Human	7.8	pEC50	=	7.8	Functional	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	106430	0	None	-1	2	Human	7.8	pEC50	=	7.8	Functional	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	106430	0	None	-1	2	Human	7.8	pEC50	=	7.8	Functional	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	89931	0	None	1	3	Human	7.8	pEC50	=	7.8	Functional	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	89931	0	None	1	3	Human	7.8	pEC50	=	7.8	Functional	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	124218	0	None	22	2	Rat	7.8	pEC50	=	7.8	Functional	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	124218	0	None	22	2	Rat	7.8	pEC50	=	7.8	Functional	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	160834	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	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	160834	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	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	161310	0	None	-6	5	Rat	7.8	pEC50	=	7.8	Functional	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	161310	0	None	-6	5	Rat	7.8	pEC50	=	7.8	Functional	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	79130	0	None	2	2	Human	7.8	pEC50	=	7.8	Functional	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	79130	0	None	2	2	Human	7.8	pEC50	=	7.8	Functional	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	215505	0	None	1	2	Human	7.8	pEC50	=	7.8	Functional	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	9161	0	None	-4	3	Human	7.8	pEC50	=	7.8	Functional	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	9161	0	None	-4	3	Human	7.8	pEC50	=	7.8	Functional	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	106333	0	None	-11	3	Human	7.8	pEC50	=	7.8	Functional	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	106333	0	None	-11	3	Human	7.8	pEC50	=	7.8	Functional	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	106333	0	None	-11	3	Human	7.8	pEC50	=	7.8	Functional	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	215091	0	None	7	2	Human	7.8	pEC50	=	7.8	Functional	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	170744	34	None	-	1	Human	7.8	pEC50	=	7.8	Functional	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	170744	34	None	-	1	Human	7.8	pEC50	=	7.8	Functional	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	20	None	-1	8	Human	7.8	pEC50	=	7.8	Functional	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	20	None	-1	8	Human	7.8	pEC50	=	7.8	Functional	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	20	None	-1	8	Human	7.8	pEC50	=	7.8	Functional	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	20	None	-1	8	Human	7.8	pEC50	=	7.8	Functional	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	20	None	-1	8	Human	7.8	pEC50	=	7.8	Functional	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	20	None	-1	8	Human	7.8	pEC50	=	7.8	Functional	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	20	None	-1	8	Human	7.8	pEC50	=	7.8	Functional	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	20	None	-1	8	Human	7.8	pEC50	=	7.8	Functional	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	20	None	-1	8	Human	7.8	pEC50	=	7.8	Functional	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	20	None	-1	8	Human	7.8	pEC50	=	7.8	Functional	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	20	None	-1	8	Human	7.8	pEC50	=	7.8	Functional	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	20	None	-1	8	Human	7.8	pEC50	=	7.8	Functional	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	20	None	-1	8	Human	7.8	pEC50	=	7.8	Functional	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	20	None	-1	8	Human	7.8	pEC50	=	7.8	Functional	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	20	None	-1	8	Human	7.8	pEC50	=	7.8	Functional	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	42	None	1	4	Human	7.8	pEC50	=	7.8	Functional	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	42	None	1	4	Human	7.8	pEC50	=	7.8	Functional	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	42	None	1	4	Human	7.8	pEC50	=	7.8	Functional	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	42	None	1	4	Human	7.8	pEC50	=	7.8	Functional	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	214277	0	None	3	2	Human	7.8	pEC50	=	7.8	Functional	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	93140	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	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	93140	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	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	93161	1	None	12	3	Human	7.8	pEC50	=	7.8	Functional	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	93161	1	None	12	3	Human	7.8	pEC50	=	7.8	Functional	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
	71458063	79141	0	None	-1	2	Human	7.8	pEC50	=	7.8	Functional	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	79141	0	None	-1	2	Human	7.8	pEC50	=	7.8	Functional	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	113883	12	None	2	3	Human	6.8	pEC50	=	6.8	Functional	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	113883	12	None	2	3	Human	6.8	pEC50	=	6.8	Functional	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
	118725855	117180	0	None	-75	3	Human	6.8	pEC50	=	6.8	Functional	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	117180	0	None	-75	3	Human	6.8	pEC50	=	6.8	Functional	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	212411	0	None	-72	4	Rat	6.8	pEC50	=	6.8	Functional	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	104470	0	None	-	1	Rat	6.8	pEC50	=	6.8	Functional	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	104470	0	None	-	1	Rat	6.8	pEC50	=	6.8	Functional	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	77228	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	77228	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	77228	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	177755	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	177755	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	159977	0	None	-19	2	Human	4.8	pEC50	=	4.8	Functional	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	159977	0	None	-19	2	Human	4.8	pEC50	=	4.8	Functional	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	212411	0	None	-72	4	Rat	6.8	pEC50	=	6.8	Functional	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	160505	0	None	-29	2	Human	5.8	pEC50	=	5.8	Functional	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	160505	0	None	-29	2	Human	5.8	pEC50	=	5.8	Functional	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	91405	0	None	-	1	Rat	5.8	pEC50	=	5.8	Functional	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	91405	0	None	-	1	Rat	5.8	pEC50	=	5.8	Functional	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	164649	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	164649	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	164099	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	164099	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	158855	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	158855	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	209574	4	None	7	4	Rat	6.8	pEC50	=	6.8	Functional	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	214894	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	215495	0	None	-5	2	Human	6.8	pEC50	=	6.8	Functional	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	113888	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	113888	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	215336	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	179983	0	None	-61	5	Human	5.8	pEC50	=	5.8	Functional	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	179983	0	None	-61	5	Human	5.8	pEC50	=	5.8	Functional	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	91405	0	None	-	1	Rat	5.8	pEC50	=	5.8	Functional	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	91405	0	None	-	1	Rat	5.8	pEC50	=	5.8	Functional	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	30596	6	None	-	1	Human	4.8	pEC50	=	4.8	Functional	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	30596	6	None	-	1	Human	4.8	pEC50	=	4.8	Functional	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	164721	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	164721	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	159590	0	None	-676	3	Human	6.8	pEC50	=	6.8	Functional	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	159590	0	None	-676	3	Human	6.8	pEC50	=	6.8	Functional	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	179983	0	None	-61	5	Human	5.8	pEC50	=	5.8	Functional	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	179983	0	None	-61	5	Human	5.8	pEC50	=	5.8	Functional	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	176340	0	None	-	1	Rat	6.8	pEC50	=	6.8	Functional	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	176340	0	None	-	1	Rat	6.8	pEC50	=	6.8	Functional	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	176340	0	None	-	1	Rat	6.8	pEC50	=	6.8	Functional	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	215336	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	103347	0	None	-109	2	Human	5.8	pEC50	=	5.8	Functional	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	103347	0	None	-109	2	Human	5.8	pEC50	=	5.8	Functional	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	59600	6	None	-	1	Human	4.8	pEC50	=	4.8	Functional	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	59600	6	None	-	1	Human	4.8	pEC50	=	4.8	Functional	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	160099	0	None	14	2	Human	6.8	pEC50	=	6.8	Functional	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	160099	0	None	14	2	Human	6.8	pEC50	=	6.8	Functional	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	35723	6	None	-	1	Human	4.8	pEC50	=	4.8	Functional	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	35723	6	None	-	1	Human	4.8	pEC50	=	4.8	Functional	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	214518	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	106318	0	None	-69	2	Human	6.8	pEC50	=	6.8	Functional	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	106318	0	None	-69	2	Human	6.8	pEC50	=	6.8	Functional	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	106318	0	None	-69	2	Human	6.8	pEC50	=	6.8	Functional	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	176376	0	None	13	2	Rat	6.8	pEC50	=	6.8	Functional	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	176376	0	None	13	2	Rat	6.8	pEC50	=	6.8	Functional	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	176376	0	None	13	2	Rat	6.8	pEC50	=	6.8	Functional	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
	68314562	93136	4	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	93136	4	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	93156	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	93156	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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
	68314329	93166	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	93166	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	170509	0	None	-6	4	Human	5.8	pEC50	=	5.8	Functional	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	170509	0	None	-6	4	Human	5.8	pEC50	=	5.8	Functional	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
	66829005	160441	0	None	-1	2	Human	6.8	pEC50	=	6.8	Functional	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	160441	0	None	-1	2	Human	6.8	pEC50	=	6.8	Functional	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	91410	0	None	-1	2	Rat	5.8	pEC50	=	5.8	Functional	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	91410	0	None	-1	2	Rat	5.8	pEC50	=	5.8	Functional	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	164316	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	164316	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	165496	0	None	-1	2	Rat	5.8	pEC50	=	5.8	Functional	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	165496	0	None	-1	2	Rat	5.8	pEC50	=	5.8	Functional	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	14176	0	None	-3	4	Human	7.8	pEC50	=	7.8	Functional	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	14176	0	None	-3	4	Human	7.8	pEC50	=	7.8	Functional	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	14176	0	None	-3	4	Human	7.8	pEC50	=	7.8	Functional	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	170593	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	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	170593	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	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	180777	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	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	180777	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	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	94171	0	None	1	3	Human	7.8	pEC50	=	7.8	Functional	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	94171	0	None	1	3	Human	7.8	pEC50	=	7.8	Functional	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	164810	4	None	-	1	Human	7.8	pEC50	=	7.8	Functional	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	164810	4	None	-	1	Human	7.8	pEC50	=	7.8	Functional	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	45	None	-4	8	Human	7.8	pEC50	=	7.8	Functional	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	45	None	-4	8	Human	7.8	pEC50	=	7.8	Functional	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	45	None	-4	8	Human	7.8	pEC50	=	7.8	Functional	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	45	None	-4	8	Human	7.8	pEC50	=	7.8	Functional	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	45	None	-4	8	Human	7.8	pEC50	=	7.8	Functional	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	88506	0	None	1	3	Rat	7.8	pEC50	=	7.8	Functional	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	88506	0	None	1	3	Rat	7.8	pEC50	=	7.8	Functional	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	210662	0	None	-31	3	Rat	7.8	pEC50	=	7.8	Functional	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	88506	0	None	1	3	Rat	7.8	pEC50	=	7.8	Functional	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	88506	0	None	1	3	Rat	7.8	pEC50	=	7.8	Functional	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	168007	0	None	-	1	Rat	7.8	pEC50	=	7.8	Functional	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	168007	0	None	-	1	Rat	7.8	pEC50	=	7.8	Functional	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
	155569411	176661	0	None	-3	2	Human	7.8	pEC50	=	7.8	Functional	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	176661	0	None	-3	2	Human	7.8	pEC50	=	7.8	Functional	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	176661	0	None	-3	2	Human	7.8	pEC50	=	7.8	Functional	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	106338	0	None	-10	2	Human	7.8	pEC50	=	7.8	Functional	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	106338	0	None	-10	2	Human	7.8	pEC50	=	7.8	Functional	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	106338	0	None	-10	2	Human	7.8	pEC50	=	7.8	Functional	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	158735	0	None	1	2	Human	6.8	pEC50	=	6.8	Functional	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	158735	0	None	1	2	Human	6.8	pEC50	=	6.8	Functional	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	79129	0	None	1	2	Human	6.8	pEC50	=	6.8	Functional	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	79129	0	None	1	2	Human	6.8	pEC50	=	6.8	Functional	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	203413	19	None	-1	6	Mouse	6.8	pEC50	=	6.8	Functional	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	203413	19	None	-1	6	Mouse	6.8	pEC50	=	6.8	Functional	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	214700	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	92051	0	None	-3	4	Human	4.8	pEC50	=	4.8	Functional	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	92051	0	None	-3	4	Human	4.8	pEC50	=	4.8	Functional	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	92052	0	None	-2	3	Human	4.8	pEC50	=	4.8	Functional	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	92052	0	None	-2	3	Human	4.8	pEC50	=	4.8	Functional	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	173183	2	None	-16	2	Human	4.8	pEC50	=	4.8	Functional	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	173183	2	None	-16	2	Human	4.8	pEC50	=	4.8	Functional	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	177431	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	177431	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	166317	0	None	-7	3	Human	6.8	pEC50	=	6.8	Functional	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	166317	0	None	-7	3	Human	6.8	pEC50	=	6.8	Functional	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
	24735749	164234	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	164234	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	91410	0	None	-1	2	Rat	5.8	pEC50	=	5.8	Functional	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	91410	0	None	-1	2	Rat	5.8	pEC50	=	5.8	Functional	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	112859	0	None	-13	2	Human	6.8	pEC50	=	6.8	Functional	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	112859	0	None	-13	2	Human	6.8	pEC50	=	6.8	Functional	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	79136	0	None	3	2	Human	6.8	pEC50	=	6.8	Functional	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	79136	0	None	3	2	Human	6.8	pEC50	=	6.8	Functional	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	177077	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	177077	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	165538	0	None	1	2	Rat	6.8	pEC50	=	6.8	Functional	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	165538	0	None	1	2	Rat	6.8	pEC50	=	6.8	Functional	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	164322	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	164322	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	108574	0	None	-7	3	Human	5.8	pEC50	=	5.8	Functional	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	108574	0	None	-7	3	Human	5.8	pEC50	=	5.8	Functional	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
	CHEMBL5085013	214943	0	None	-2	4	Human	6.8	pEC50	=	6.8	Functional	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	214948	0	None	1	2	Human	6.8	pEC50	=	6.8	Functional	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	41	None	2	5	Rat	6.8	pEC50	=	6.8	Functional	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	41	None	2	5	Rat	6.8	pEC50	=	6.8	Functional	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	41	None	2	5	Rat	6.8	pEC50	=	6.8	Functional	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	214943	0	None	-2	4	Human	6.8	pEC50	=	6.8	Functional	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	96142	0	None	2	2	Human	5.8	pEC50	=	5.8	Functional	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	96142	0	None	2	2	Human	5.8	pEC50	=	5.8	Functional	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	164643	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	164643	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	215509	0	None	-1	5	Human	6.8	pEC50	=	6.8	Functional	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	176430	0	None	8	2	Human	6.8	pEC50	=	6.8	Functional	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	176430	0	None	8	2	Human	6.8	pEC50	=	6.8	Functional	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	176430	0	None	8	2	Human	6.8	pEC50	=	6.8	Functional	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	96085	0	None	-1	2	Human	5.8	pEC50	=	5.8	Functional	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	96085	0	None	-1	2	Human	5.8	pEC50	=	5.8	Functional	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	215509	0	None	-1	5	Human	6.8	pEC50	=	6.8	Functional	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	181210	0	None	1	5	Human	6.8	pEC50	=	6.8	Functional	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	181210	0	None	1	5	Human	6.8	pEC50	=	6.8	Functional	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	202583	0	None	-138	5	Rat	6.8	pEC50	=	6.8	Functional	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	202583	0	None	-138	5	Rat	6.8	pEC50	=	6.8	Functional	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	189323	0	None	-33	2	Human	5.8	pEC50	=	5.8	Functional	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	189323	0	None	-33	2	Human	5.8	pEC50	=	5.8	Functional	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	83224	0	None	-6	5	Rat	7.8	pEC50	=	7.8	Functional	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	83224	0	None	-6	5	Rat	7.8	pEC50	=	7.8	Functional	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	174830	33	None	17	2	Human	7.8	pEC50	=	7.8	Functional	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	174830	33	None	17	2	Human	7.8	pEC50	=	7.8	Functional	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	203413	19	None	-19	6	Human	7.8	pEC50	=	7.8	Functional	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	203413	19	None	-19	6	Human	7.8	pEC50	=	7.8	Functional	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	203413	19	None	-19	6	Human	7.8	pEC50	=	7.8	Functional	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	203413	19	None	-19	6	Human	7.8	pEC50	=	7.8	Functional	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	203413	19	None	-19	6	Human	7.8	pEC50	=	7.8	Functional	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	203413	19	None	-19	6	Human	7.8	pEC50	=	7.8	Functional	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	58965	0	None	-	1	Rat	7.8	pEC50	=	7.8	Functional	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	58965	0	None	-	1	Rat	7.8	pEC50	=	7.8	Functional	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	26	None	-1	13	Human	7.8	pEC50	=	7.8	Functional	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	26	None	-1	13	Human	7.8	pEC50	=	7.8	Functional	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	26	None	-1	13	Human	7.8	pEC50	=	7.8	Functional	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	26	None	-1	13	Human	7.8	pEC50	=	7.8	Functional	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	26	None	-1	13	Human	7.8	pEC50	=	7.8	Functional	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	26	None	-1	13	Human	7.8	pEC50	=	7.8	Functional	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	26	None	-1	13	Human	7.8	pEC50	=	7.8	Functional	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	26	None	-1	13	Human	7.8	pEC50	=	7.8	Functional	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	26	None	-1	13	Human	7.8	pEC50	=	7.8	Functional	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	26	None	-1	13	Human	7.8	pEC50	=	7.8	Functional	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	178019	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	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	178019	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	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	176367	0	None	-48	3	Human	7.8	pEC50	=	7.8	Functional	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	176367	0	None	-48	3	Human	7.8	pEC50	=	7.8	Functional	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	176367	0	None	-48	3	Human	7.8	pEC50	=	7.8	Functional	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	212302	0	None	-14	5	Rat	7.8	pEC50	=	7.8	Functional	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	194822	0	None	-97	5	Rat	7.8	pEC50	=	7.8	Functional	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	194822	0	None	-97	5	Rat	7.8	pEC50	=	7.8	Functional	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	141808	0	None	1	3	Human	7.8	pEC50	=	7.8	Functional	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	141808	0	None	1	3	Human	7.8	pEC50	=	7.8	Functional	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	77168	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	77168	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	77168	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	202583	0	None	-138	5	Rat	6.8	pEC50	=	6.8	Functional	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	202583	0	None	-138	5	Rat	6.8	pEC50	=	6.8	Functional	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	211833	0	None	-1	2	Rat	6.8	pEC50	=	6.8	Functional	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	59466	4	None	-	1	Human	4.8	pEC50	=	4.8	Functional	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	59466	4	None	-	1	Human	4.8	pEC50	=	4.8	Functional	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	181210	0	None	1	5	Human	6.8	pEC50	=	6.8	Functional	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	181210	0	None	1	5	Human	6.8	pEC50	=	6.8	Functional	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	160355	0	None	3	2	Human	6.8	pEC50	=	6.8	Functional	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	160355	0	None	3	2	Human	6.8	pEC50	=	6.8	Functional	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	34548	7	None	-	1	Human	4.8	pEC50	=	4.8	Functional	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	34548	7	None	-	1	Human	4.8	pEC50	=	4.8	Functional	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	160878	0	None	4	2	Human	6.8	pEC50	=	6.8	Functional	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	160878	0	None	4	2	Human	6.8	pEC50	=	6.8	Functional	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	214774	0	None	-2	2	Human	6.8	pEC50	=	6.8	Functional	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	195594	0	None	-64	4	Rat	6.8	pEC50	=	6.8	Functional	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	195594	0	None	-64	4	Rat	6.8	pEC50	=	6.8	Functional	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	195799	0	None	-2	3	Human	6.8	pEC50	=	6.8	Functional	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	195799	0	None	-2	3	Human	6.8	pEC50	=	6.8	Functional	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	192041	0	None	-16	2	Rat	5.8	pEC50	=	5.8	Functional	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	192041	0	None	-16	2	Rat	5.8	pEC50	=	5.8	Functional	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	214629	0	None	-	1	Human	4.8	pEC50	=	4.8	Functional	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	180679	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	180679	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	215340	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	84706	0	None	-16	3	Human	6.8	pEC50	=	6.8	Functional	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	84706	0	None	-16	3	Human	6.8	pEC50	=	6.8	Functional	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	84726	0	None	-14	3	Human	6.8	pEC50	=	6.8	Functional	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	84726	0	None	-14	3	Human	6.8	pEC50	=	6.8	Functional	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	117181	0	None	-173	3	Human	5.8	pEC50	=	5.8	Functional	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	117181	0	None	-173	3	Human	5.8	pEC50	=	5.8	Functional	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	214629	0	None	-	1	Human	4.8	pEC50	=	4.8	Functional	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	29614	7	None	-	1	Human	4.8	pEC50	=	4.8	Functional	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	29614	7	None	-	1	Human	4.8	pEC50	=	4.8	Functional	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	162702	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	162702	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	176634	0	None	-7	2	Human	5.8	pEC50	=	5.8	Functional	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	176634	0	None	-7	2	Human	5.8	pEC50	=	5.8	Functional	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	176634	0	None	-7	2	Human	5.8	pEC50	=	5.8	Functional	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	164530	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	164530	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	192150	0	None	-41	4	Human	4.8	pEC50	=	4.8	Functional	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	192150	0	None	-41	4	Human	4.8	pEC50	=	4.8	Functional	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	179448	0	None	-2	5	Human	6.8	pEC50	=	6.8	Functional	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	179448	0	None	-2	5	Human	6.8	pEC50	=	6.8	Functional	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	170509	0	None	-6	4	Human	5.8	pEC50	=	5.8	Functional	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	170509	0	None	-6	4	Human	5.8	pEC50	=	5.8	Functional	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	57312	0	None	-46	3	Human	5.8	pEC50	=	5.8	Functional	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	57312	0	None	-46	3	Human	5.8	pEC50	=	5.8	Functional	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	192150	0	None	-41	4	Human	4.8	pEC50	=	4.8	Functional	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	192150	0	None	-41	4	Human	4.8	pEC50	=	4.8	Functional	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	214478	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	179448	0	None	-2	5	Human	6.8	pEC50	=	6.8	Functional	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	179448	0	None	-2	5	Human	6.8	pEC50	=	6.8	Functional	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	181254	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	181254	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	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	125799	0	None	-9	2	Human	4.8	pEC50	=	4.8	Functional	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	125799	0	None	-9	2	Human	4.8	pEC50	=	4.8	Functional	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	172796	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	172796	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	155035	0	None	-	1	Mouse	4.8	pEC50	=	4.8	Functional	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	155035	0	None	-	1	Mouse	4.8	pEC50	=	4.8	Functional	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	160050	0	None	-	1	Human	4.8	pEC50	=	4.8	Functional	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	160050	0	None	-	1	Human	4.8	pEC50	=	4.8	Functional	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	21453	4	None	-	1	Human	4.8	pEC50	=	4.8	Functional	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	21453	4	None	-	1	Human	4.8	pEC50	=	4.8	Functional	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	212302	0	None	-14	5	Rat	7.8	pEC50	=	7.8	Functional	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	164253	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	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	164253	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	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	179356	0	None	-75	2	Human	7.8	pEC50	=	7.8	Functional	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	179356	0	None	-75	2	Human	7.8	pEC50	=	7.8	Functional	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	106354	0	None	16	2	Human	7.8	pEC50	=	7.8	Functional	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	106354	0	None	16	2	Human	7.8	pEC50	=	7.8	Functional	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	106354	0	None	16	2	Human	7.8	pEC50	=	7.8	Functional	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	182821	0	None	-22	5	Human	7.8	pEC50	=	7.8	Functional	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	182821	0	None	-22	5	Human	7.8	pEC50	=	7.8	Functional	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	65657	0	None	-213	3	Rat	7.8	pEC50	=	7.8	Functional	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	65657	0	None	-213	3	Rat	7.8	pEC50	=	7.8	Functional	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	194822	0	None	-97	5	Rat	7.8	pEC50	=	7.8	Functional	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	194822	0	None	-97	5	Rat	7.8	pEC50	=	7.8	Functional	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	195728	0	None	-8	4	Rat	7.8	pEC50	=	7.8	Functional	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	195728	0	None	-8	4	Rat	7.8	pEC50	=	7.8	Functional	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	190439	0	None	-	1	Rat	7.8	pEC50	=	7.8	Functional	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	190439	0	None	-	1	Rat	7.8	pEC50	=	7.8	Functional	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	195728	0	None	-8	4	Rat	7.7	pEC50	=	7.7	Functional	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	195728	0	None	-8	4	Rat	7.7	pEC50	=	7.7	Functional	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	209804	0	None	-	1	Rat	7.7	pEC50	=	7.7	Functional	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	160394	0	None	-4	3	Human	7.7	pEC50	=	7.7	Functional	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	160394	0	None	-4	3	Human	7.7	pEC50	=	7.7	Functional	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	110954	0	None	-2	3	Human	7.7	pEC50	=	7.7	Functional	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	110954	0	None	-2	3	Human	7.7	pEC50	=	7.7	Functional	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	160921	0	None	-2	3	Human	7.7	pEC50	=	7.7	Functional	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	160921	0	None	-2	3	Human	7.7	pEC50	=	7.7	Functional	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	170486	2	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	170486	2	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	215404	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	93637	0	None	-43	2	Human	6.8	pEC50	=	6.8	Functional	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	93637	0	None	-43	2	Human	6.8	pEC50	=	6.8	Functional	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
	44233410	195594	0	None	-64	4	Rat	6.8	pEC50	=	6.8	Functional	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	195594	0	None	-64	4	Rat	6.8	pEC50	=	6.8	Functional	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	170486	2	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	170486	2	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	117166	0	None	-251	3	Human	5.8	pEC50	=	5.8	Functional	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	117166	0	None	-251	3	Human	5.8	pEC50	=	5.8	Functional	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	170275	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	170275	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	45	None	-3	8	Human	6.7	pEC50	=	6.7	Functional	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	45	None	-3	8	Human	6.7	pEC50	=	6.7	Functional	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	45	None	-3	8	Human	6.7	pEC50	=	6.7	Functional	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	45	None	-3	8	Human	6.7	pEC50	=	6.7	Functional	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	214299	0	None	-107	2	Human	6.7	pEC50	=	6.7	Functional	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
	12956	730	3	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	3	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	3	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	45	None	-3	8	Human	6.7	pEC50	=	6.7	Functional	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	45	None	-3	8	Human	6.7	pEC50	=	6.7	Functional	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	45	None	-3	8	Human	6.7	pEC50	=	6.7	Functional	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	45	None	-3	8	Human	6.7	pEC50	=	6.7	Functional	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	215036	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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
	137659520	159266	0	None	-17378	2	Human	4.7	pEC50	=	4.7	Functional	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	159266	0	None	-17378	2	Human	4.7	pEC50	=	4.7	Functional	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	91399	0	None	-	1	Rat	5.7	pEC50	=	5.7	Functional	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	91399	0	None	-	1	Rat	5.7	pEC50	=	5.7	Functional	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	172442	0	None	-	1	Rat	5.7	pEC50	=	5.7	Functional	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	172442	0	None	-	1	Rat	5.7	pEC50	=	5.7	Functional	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	163791	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	163791	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	164810	4	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	164810	4	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	65632	0	None	-	1	Rat	6.7	pEC50	=	6.7	Functional	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	65632	0	None	-	1	Rat	6.7	pEC50	=	6.7	Functional	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	79181	0	None	-549	2	Human	6.7	pEC50	=	6.7	Functional	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	79181	0	None	-549	2	Human	6.7	pEC50	=	6.7	Functional	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	113874	2	None	-	1	Human	4.7	pEC50	=	4.7	Functional	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	113874	2	None	-	1	Human	4.7	pEC50	=	4.7	Functional	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	147541	0	None	-1	2	Human	6.7	pEC50	=	6.7	Functional	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	147541	0	None	-1	2	Human	6.7	pEC50	=	6.7	Functional	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	59409	4	None	1	2	Human	4.7	pEC50	=	4.7	Functional	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	59409	4	None	1	2	Human	4.7	pEC50	=	4.7	Functional	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	173707	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	173707	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	214609	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	214609	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	91399	0	None	-	1	Rat	5.7	pEC50	=	5.7	Functional	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	91399	0	None	-	1	Rat	5.7	pEC50	=	5.7	Functional	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	79002	0	None	10	2	Rat	6.7	pEC50	=	6.7	Functional	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	79002	0	None	10	2	Rat	6.7	pEC50	=	6.7	Functional	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	55524	7	None	-	1	Human	4.7	pEC50	=	4.7	Functional	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	55524	7	None	-	1	Human	4.7	pEC50	=	4.7	Functional	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	55524	7	None	-	1	Human	4.7	pEC50	=	4.7	Functional	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	36559	7	None	1	2	Human	4.7	pEC50	=	4.7	Functional	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	36559	7	None	1	2	Human	4.7	pEC50	=	4.7	Functional	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	164587	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	164587	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	90459	0	None	-2	2	Human	6.7	pEC50	=	6.7	Functional	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	90459	0	None	-2	2	Human	6.7	pEC50	=	6.7	Functional	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	214670	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	214779	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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
	44406695	140714	0	None	-1	2	Human	7.7	pEC50	=	7.7	Functional	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	140714	0	None	-1	2	Human	7.7	pEC50	=	7.7	Functional	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	45	None	-2	8	Mouse	7.7	pEC50	=	7.7	Functional	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	45	None	-2	8	Mouse	7.7	pEC50	=	7.7	Functional	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	45	None	-2	8	Mouse	7.7	pEC50	=	7.7	Functional	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	45	None	-2	8	Mouse	7.7	pEC50	=	7.7	Functional	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	45	None	-2	8	Mouse	7.7	pEC50	=	7.7	Functional	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	45	None	-2	8	Mouse	7.7	pEC50	=	7.7	Functional	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	45	None	-2	8	Mouse	7.7	pEC50	=	7.7	Functional	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	45	None	-2	8	Mouse	7.7	pEC50	=	7.7	Functional	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	45	None	-2	8	Mouse	7.7	pEC50	=	7.7	Functional	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	45	None	-2	8	Mouse	7.7	pEC50	=	7.7	Functional	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	45	None	-2	8	Mouse	7.7	pEC50	=	7.7	Functional	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	45	None	-2	8	Mouse	7.7	pEC50	=	7.7	Functional	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	57219	0	None	2	3	Rat	7.7	pEC50	=	7.7	Functional	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	57219	0	None	2	3	Rat	7.7	pEC50	=	7.7	Functional	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	161067	0	None	39	2	Rat	7.7	pEC50	=	7.7	Functional	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	161067	0	None	39	2	Rat	7.7	pEC50	=	7.7	Functional	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	161067	0	None	39	2	Rat	7.7	pEC50	=	7.7	Functional	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	88166	0	None	-2	2	Human	7.7	pEC50	=	7.7	Functional	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	88166	0	None	-2	2	Human	7.7	pEC50	=	7.7	Functional	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	57219	0	None	2	3	Rat	7.7	pEC50	=	7.7	Functional	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	57219	0	None	2	3	Rat	7.7	pEC50	=	7.7	Functional	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	139047	0	None	-10	3	Human	7.7	pEC50	=	7.7	Functional	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	139047	0	None	-10	3	Human	7.7	pEC50	=	7.7	Functional	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	9493	0	None	1	2	Human	7.7	pEC50	=	7.7	Functional	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	9493	0	None	1	2	Human	7.7	pEC50	=	7.7	Functional	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	92059	0	None	-	1	Mouse	7.7	pEC50	=	7.7	Functional	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	92059	0	None	-	1	Mouse	7.7	pEC50	=	7.7	Functional	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	92059	0	None	-	1	Mouse	7.7	pEC50	=	7.7	Functional	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	92059	0	None	-	1	Mouse	7.7	pEC50	=	7.7	Functional	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	210863	1	None	89	2	Human	7.7	pEC50	=	7.7	Functional	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	112662	0	None	-2	2	Human	7.7	pEC50	=	7.7	Functional	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	112662	0	None	-2	2	Human	7.7	pEC50	=	7.7	Functional	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	112662	0	None	-2	2	Human	7.7	pEC50	=	7.7	Functional	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	176235	0	None	2	3	Human	7.7	pEC50	=	7.7	Functional	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	176235	0	None	2	3	Human	7.7	pEC50	=	7.7	Functional	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	176235	0	None	2	3	Human	7.7	pEC50	=	7.7	Functional	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	45	None	-3	8	Human	7.7	pEC50	=	7.7	Functional	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	45	None	-3	8	Human	7.7	pEC50	=	7.7	Functional	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	45	None	-3	8	Human	7.7	pEC50	=	7.7	Functional	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	45	None	-3	8	Human	7.7	pEC50	=	7.7	Functional	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	169941	0	None	-	1	Mouse	7.7	pEC50	=	7.7	Functional	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	169941	0	None	-	1	Mouse	7.7	pEC50	=	7.7	Functional	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	214962	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	209168	0	None	-8	4	Rat	7.7	pEC50	=	7.7	Functional	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	214698	0	None	134	2	Human	7.7	pEC50	=	7.7	Functional	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	212227	0	None	64	2	Human	7.7	pEC50	=	7.7	Functional	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	181798	0	None	1	5	Human	7.7	pEC50	=	7.7	Functional	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	181798	0	None	1	5	Human	7.7	pEC50	=	7.7	Functional	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	152699	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	152699	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	161563	0	None	1	3	Human	6.7	pEC50	=	6.7	Functional	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	161563	0	None	1	3	Human	6.7	pEC50	=	6.7	Functional	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	170019	0	None	-10	3	Human	5.7	pEC50	=	5.7	Functional	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	170019	0	None	-10	3	Human	5.7	pEC50	=	5.7	Functional	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	113873	0	None	-	1	Human	4.7	pEC50	=	4.7	Functional	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	113873	0	None	-	1	Human	4.7	pEC50	=	4.7	Functional	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	40331	13	None	-	1	Human	4.7	pEC50	=	4.7	Functional	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	40331	13	None	-	1	Human	4.7	pEC50	=	4.7	Functional	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	215049	0	None	-	1	Human	4.7	pEC50	=	4.7	Functional	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	161563	0	None	1	3	Human	6.7	pEC50	=	6.7	Functional	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	161563	0	None	1	3	Human	6.7	pEC50	=	6.7	Functional	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
	156014932	177549	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	177549	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	192301	0	None	-3	2	Rat	6.7	pEC50	=	6.7	Functional	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	192301	0	None	-3	2	Rat	6.7	pEC50	=	6.7	Functional	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	215049	0	None	-	1	Human	4.7	pEC50	=	4.7	Functional	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	191861	0	None	-32	3	Human	6.7	pEC50	=	6.7	Functional	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	191861	0	None	-32	3	Human	6.7	pEC50	=	6.7	Functional	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	215268	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	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	103338	0	None	-102	2	Human	5.7	pEC50	=	5.7	Functional	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	103338	0	None	-102	2	Human	5.7	pEC50	=	5.7	Functional	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	20	None	1	8	Rat	6.7	pEC50	=	6.7	Functional	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	20	None	1	8	Rat	6.7	pEC50	=	6.7	Functional	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	20	None	1	8	Rat	6.7	pEC50	=	6.7	Functional	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	20	None	1	8	Rat	6.7	pEC50	=	6.7	Functional	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	20	None	1	8	Rat	6.7	pEC50	=	6.7	Functional	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	20	None	1	8	Rat	6.7	pEC50	=	6.7	Functional	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	20	None	1	8	Rat	6.7	pEC50	=	6.7	Functional	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	20	None	1	8	Rat	6.7	pEC50	=	6.7	Functional	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	20	None	1	8	Rat	6.7	pEC50	=	6.7	Functional	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	20	None	1	8	Rat	6.7	pEC50	=	6.7	Functional	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	215425	0	None	-10	2	Human	6.7	pEC50	=	6.7	Functional	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	180232	0	None	-1	5	Human	6.7	pEC50	=	6.7	Functional	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	180232	0	None	-1	5	Human	6.7	pEC50	=	6.7	Functional	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	180675	0	None	-1	4	Human	6.7	pEC50	=	6.7	Functional	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	180675	0	None	-1	4	Human	6.7	pEC50	=	6.7	Functional	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	91401	0	None	-4	2	Rat	5.7	pEC50	=	5.7	Functional	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	91401	0	None	-4	2	Rat	5.7	pEC50	=	5.7	Functional	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	171368	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	171368	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	171368	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	171368	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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
	162651091	180232	0	None	-1	5	Human	6.7	pEC50	=	6.7	Functional	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	180232	0	None	-1	5	Human	6.7	pEC50	=	6.7	Functional	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	180675	0	None	-1	4	Human	6.7	pEC50	=	6.7	Functional	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	180675	0	None	-1	4	Human	6.7	pEC50	=	6.7	Functional	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	159967	0	None	-1	2	Human	6.7	pEC50	=	6.7	Functional	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	159967	0	None	-1	2	Human	6.7	pEC50	=	6.7	Functional	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	163890	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	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	163890	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	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	111792	0	None	-77	3	Human	6.7	pEC50	=	6.7	Functional	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	111792	0	None	-77	3	Human	6.7	pEC50	=	6.7	Functional	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	148048	0	None	-	1	Human	4.7	pEC50	=	4.7	Functional	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	148048	0	None	-	1	Human	4.7	pEC50	=	4.7	Functional	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	108745	6	None	-11	2	Human	5.7	pEC50	=	5.7	Functional	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	108745	6	None	-11	2	Human	5.7	pEC50	=	5.7	Functional	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	175561	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	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	175561	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	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	172528	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	172528	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	38051	0	None	-5	4	Human	6.7	pEC50	=	6.7	Functional	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	38051	0	None	-5	4	Human	6.7	pEC50	=	6.7	Functional	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	45	None	-3	8	Human	6.7	pEC50	=	6.7	Functional	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	45	None	-3	8	Human	6.7	pEC50	=	6.7	Functional	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	45	None	-3	8	Human	6.7	pEC50	=	6.7	Functional	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	45	None	-3	8	Human	6.7	pEC50	=	6.7	Functional	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	93157	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	93157	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	170019	0	None	-10	3	Human	5.7	pEC50	=	5.7	Functional	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	170019	0	None	-10	3	Human	5.7	pEC50	=	5.7	Functional	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	211583	0	None	-2	4	Rat	8.7	pEC50	=	8.7	Functional	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	45	None	-3	8	Human	8.7	pEC50	=	8.7	Functional	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	45	None	-3	8	Human	8.7	pEC50	=	8.7	Functional	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	45	None	-3	8	Human	8.7	pEC50	=	8.7	Functional	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	45	None	-3	8	Human	8.7	pEC50	=	8.7	Functional	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	180151	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	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	180151	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	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	198940	0	None	-4	2	Human	8.7	pEC50	=	8.7	Functional	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	198940	0	None	-4	2	Human	8.7	pEC50	=	8.7	Functional	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
	54582933	62078	0	None	2	2	Human	8.7	pEC50	=	8.7	Functional	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	62078	0	None	2	2	Human	8.7	pEC50	=	8.7	Functional	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	79113	0	None	-4	2	Human	8.7	pEC50	=	8.7	Functional	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	79113	0	None	-4	2	Human	8.7	pEC50	=	8.7	Functional	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	173492	0	None	147	2	Mouse	8.7	pEC50	=	8.7	Functional	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	173492	0	None	147	2	Mouse	8.7	pEC50	=	8.7	Functional	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	214514	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	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	138283	0	None	18	3	Human	8.7	pEC50	=	8.7	Functional	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	138283	0	None	18	3	Human	8.7	pEC50	=	8.7	Functional	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	189064	0	None	-2	2	Rat	8.7	pEC50	=	8.7	Functional	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	189064	0	None	-2	2	Rat	8.7	pEC50	=	8.7	Functional	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	87876	0	None	-8	2	Rat	8.7	pEC50	=	8.7	Functional	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	87876	0	None	-8	2	Rat	8.7	pEC50	=	8.7	Functional	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	215266	0	None	-	1	Mouse	8.7	pEC50	=	8.7	Functional	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	215530	0	None	-	1	Mouse	8.7	pEC50	=	8.7	Functional	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	215530	0	None	-	1	Mouse	8.7	pEC50	=	8.7	Functional	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	209092	0	None	-3	5	Human	8.7	pEC50	=	8.7	Functional	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	209092	0	None	-3	5	Human	8.7	pEC50	=	8.7	Functional	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	188547	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	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	188547	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	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	188547	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	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	188582	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	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	188582	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	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	188582	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	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	214412	0	None	-	1	Mouse	8.7	pEC50	=	8.7	Functional	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	177635	0	None	1	2	Human	8.7	pEC50	=	8.7	Functional	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	177635	0	None	1	2	Human	8.7	pEC50	=	8.7	Functional	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	141015	0	None	-	1	Rat	8.7	pEC50	=	8.7	Functional	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	141015	0	None	-	1	Rat	8.7	pEC50	=	8.7	Functional	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	189456	0	None	-2	2	Rat	8.7	pEC50	=	8.7	Functional	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	189456	0	None	-2	2	Rat	8.7	pEC50	=	8.7	Functional	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	87905	0	None	-25	3	Rat	8.7	pEC50	=	8.7	Functional	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	87905	0	None	-25	3	Rat	8.7	pEC50	=	8.7	Functional	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	153992	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	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	153992	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	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	0	None	-1	2	Human	8.7	pEC50	=	8.7	Functional	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	0	None	-1	2	Human	8.7	pEC50	=	8.7	Functional	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	0	None	-1	2	Human	8.7	pEC50	=	8.7	Functional	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	96578	0	None	-5	2	Human	8.7	pEC50	=	8.7	Functional	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	96578	0	None	-5	2	Human	8.7	pEC50	=	8.7	Functional	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	210407	0	None	-1	3	Rat	8.7	pEC50	=	8.7	Functional	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	176256	0	None	-	1	Rat	8.7	pEC50	=	8.7	Functional	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	176256	0	None	-	1	Rat	8.7	pEC50	=	8.7	Functional	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	176256	0	None	-	1	Rat	8.7	pEC50	=	8.7	Functional	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	145065	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	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	145065	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	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	88162	0	None	-3	2	Human	8.7	pEC50	=	8.7	Functional	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	88162	0	None	-3	2	Human	8.7	pEC50	=	8.7	Functional	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	215557	0	None	-	1	Mouse	8.7	pEC50	=	8.7	Functional	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	215557	0	None	-	1	Mouse	8.7	pEC50	=	8.7	Functional	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	176497	0	None	-	1	Mouse	8.7	pEC50	=	8.7	Functional	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	176497	0	None	-	1	Mouse	8.7	pEC50	=	8.7	Functional	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	176497	0	None	-	1	Mouse	8.7	pEC50	=	8.7	Functional	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	190159	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	190159	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	193201	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	193201	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	175133	0	None	-	1	Mouse	8.6	pEC50	=	8.6	Functional	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	175133	0	None	-	1	Mouse	8.6	pEC50	=	8.6	Functional	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	214781	0	None	-1	3	Human	8.6	pEC50	=	8.6	Functional	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	97863	0	None	-22	4	Human	8.6	pEC50	=	8.6	Functional	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	97863	0	None	-22	4	Human	8.6	pEC50	=	8.6	Functional	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	97863	0	None	-22	4	Human	8.6	pEC50	=	8.6	Functional	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	189165	1	None	-3	7	Human	8.6	pEC50	=	8.6	Functional	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	189165	1	None	-3	7	Human	8.6	pEC50	=	8.6	Functional	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	189165	1	None	-3	7	Human	8.6	pEC50	=	8.6	Functional	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	215523	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	183736	0	None	47	2	Rat	8.6	pEC50	=	8.6	Functional	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	183736	0	None	47	2	Rat	8.6	pEC50	=	8.6	Functional	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	183736	0	None	47	2	Rat	8.6	pEC50	=	8.6	Functional	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	144145	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	144145	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	189165	1	None	-3	7	Human	8.6	pEC50	=	8.6	Functional	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	189165	1	None	-3	7	Human	8.6	pEC50	=	8.6	Functional	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	189165	1	None	-3	7	Human	8.6	pEC50	=	8.6	Functional	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	84183	0	None	-1	3	Human	8.6	pEC50	=	8.6	Functional	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	84183	0	None	-1	3	Human	8.6	pEC50	=	8.6	Functional	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	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	178083	0	None	1	2	Human	8.6	pEC50	=	8.6	Functional	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	178083	0	None	1	2	Human	8.6	pEC50	=	8.6	Functional	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	215549	0	None	-	1	Mouse	8.6	pEC50	=	8.6	Functional	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	215549	0	None	-	1	Mouse	8.6	pEC50	=	8.6	Functional	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	66614	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	66614	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	66614	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	66641	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	66641	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	66641	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	214355	0	None	-	1	Mouse	8.6	pEC50	=	8.6	Functional	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	137213	0	None	-3	3	Human	8.6	pEC50	=	8.6	Functional	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	137213	0	None	-3	3	Human	8.6	pEC50	=	8.6	Functional	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
	44427177	166504	0	None	-4	2	Human	8.6	pEC50	=	8.6	Functional	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	166504	0	None	-4	2	Human	8.6	pEC50	=	8.6	Functional	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
	71459951	79142	0	None	-1	2	Human	8.6	pEC50	=	8.6	Functional	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	79142	0	None	-1	2	Human	8.6	pEC50	=	8.6	Functional	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	175052	0	None	-	1	Mouse	8.6	pEC50	=	8.6	Functional	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	175052	0	None	-	1	Mouse	8.6	pEC50	=	8.6	Functional	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	176303	0	None	-	1	Mouse	8.6	pEC50	=	8.6	Functional	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	176303	0	None	-	1	Mouse	8.6	pEC50	=	8.6	Functional	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	176303	0	None	-	1	Mouse	8.6	pEC50	=	8.6	Functional	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	72768	0	None	-1	2	Human	8.6	pEC50	=	8.6	Functional	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	72768	0	None	-1	2	Human	8.6	pEC50	=	8.6	Functional	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	36	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	36	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	36	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	36	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	168952	0	None	-1	3	Human	8.6	pEC50	=	8.6	Functional	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	168952	0	None	-1	3	Human	8.6	pEC50	=	8.6	Functional	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	157697	0	None	-2	2	Human	8.6	pEC50	=	8.6	Functional	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	157697	0	None	-2	2	Human	8.6	pEC50	=	8.6	Functional	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	87896	0	None	-5	2	Rat	8.6	pEC50	=	8.6	Functional	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	87896	0	None	-5	2	Rat	8.6	pEC50	=	8.6	Functional	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	214744	0	None	-	1	Mouse	8.6	pEC50	=	8.6	Functional	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	160761	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	160761	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	201852	0	None	30	3	Human	8.6	pEC50	=	8.6	Functional	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	201852	0	None	30	3	Human	8.6	pEC50	=	8.6	Functional	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	84693	0	None	1	2	Human	8.6	pEC50	=	8.6	Functional	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	84693	0	None	1	2	Human	8.6	pEC50	=	8.6	Functional	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	93155	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	93155	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	211772	0	None	-4	4	Human	8.6	pEC50	=	8.6	Functional	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	211795	0	None	-3	5	Human	8.6	pEC50	=	8.6	Functional	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	79148	0	None	1	2	Human	8.6	pEC50	=	8.6	Functional	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	79148	0	None	1	2	Human	8.6	pEC50	=	8.6	Functional	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	17	None	4	2	Human	8.6	pEC50	=	8.6	Functional	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	17	None	4	2	Human	8.6	pEC50	=	8.6	Functional	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	17	None	4	2	Human	8.6	pEC50	=	8.6	Functional	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	17	None	4	2	Human	8.6	pEC50	=	8.6	Functional	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	17	None	4	2	Human	8.6	pEC50	=	8.6	Functional	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	137914	0	None	-3	3	Human	8.6	pEC50	=	8.6	Functional	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	137914	0	None	-3	3	Human	8.6	pEC50	=	8.6	Functional	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	112585	11	None	23	2	Human	8.6	pEC50	=	8.6	Functional	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	112585	11	None	23	2	Human	8.6	pEC50	=	8.6	Functional	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	112585	11	None	23	2	Human	8.6	pEC50	=	8.6	Functional	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	215436	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	141029	0	None	165	2	Rat	8.6	pEC50	=	8.6	Functional	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	141029	0	None	165	2	Rat	8.6	pEC50	=	8.6	Functional	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	124209	0	None	38	2	Rat	8.6	pEC50	=	8.6	Functional	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	124209	0	None	38	2	Rat	8.6	pEC50	=	8.6	Functional	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	195253	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	195253	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	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	65703	0	None	19	2	Human	8.6	pEC50	=	8.6	Functional	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	65703	0	None	19	2	Human	8.6	pEC50	=	8.6	Functional	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	202504	0	None	-1	3	Human	8.6	pEC50	=	8.6	Functional	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	202504	0	None	-1	3	Human	8.6	pEC50	=	8.6	Functional	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	92066	0	None	-	1	Mouse	8.6	pEC50	=	8.6	Functional	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	92066	0	None	-	1	Mouse	8.6	pEC50	=	8.6	Functional	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	92066	0	None	-	1	Mouse	8.6	pEC50	=	8.6	Functional	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	92066	0	None	-	1	Mouse	8.6	pEC50	=	8.6	Functional	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	85790	0	None	-3	3	Human	8.6	pEC50	=	8.6	Functional	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	85790	0	None	-3	3	Human	8.6	pEC50	=	8.6	Functional	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	177300	0	None	-3	2	Human	8.6	pEC50	=	8.6	Functional	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	177300	0	None	-3	2	Human	8.6	pEC50	=	8.6	Functional	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	89198	0	None	-3	3	Human	8.6	pEC50	=	8.6	Functional	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	89198	0	None	-3	3	Human	8.6	pEC50	=	8.6	Functional	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	106408	0	None	3	3	Human	8.6	pEC50	=	8.6	Functional	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	106408	0	None	3	3	Human	8.6	pEC50	=	8.6	Functional	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	106408	0	None	3	3	Human	8.6	pEC50	=	8.6	Functional	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	199060	1	None	-1	2	Human	8.6	pEC50	=	8.6	Functional	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	199060	1	None	-1	2	Human	8.6	pEC50	=	8.6	Functional	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	215532	0	None	2	3	Mouse	8.6	pEC50	=	8.6	Functional	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	215532	0	None	2	3	Mouse	8.6	pEC50	=	8.6	Functional	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	110956	0	None	-1	3	Human	8.6	pEC50	=	8.6	Functional	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	110956	0	None	-1	3	Human	8.6	pEC50	=	8.6	Functional	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	211775	0	None	-5	5	Human	8.6	pEC50	=	8.6	Functional	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	214805	0	None	-	1	Mouse	8.6	pEC50	=	8.6	Functional	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	215574	0	None	-	1	Mouse	8.6	pEC50	=	8.6	Functional	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	215574	0	None	-	1	Mouse	8.6	pEC50	=	8.6	Functional	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
	CHEMBL2387213	210402	0	None	-1	3	Rat	8.6	pEC50	=	8.6	Functional	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	87908	0	None	-41	2	Rat	8.6	pEC50	=	8.6	Functional	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	87908	0	None	-41	2	Rat	8.6	pEC50	=	8.6	Functional	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	189297	0	None	-2	2	Human	8.6	pEC50	=	8.6	Functional	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	189297	0	None	-2	2	Human	8.6	pEC50	=	8.6	Functional	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	99291	0	None	-70	3	Human	8.6	pEC50	=	8.6	Functional	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	99291	0	None	-70	3	Human	8.6	pEC50	=	8.6	Functional	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	191555	0	None	-1	2	Human	8.6	pEC50	=	8.6	Functional	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	191555	0	None	-1	2	Human	8.6	pEC50	=	8.6	Functional	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	162365	0	None	20	2	Mouse	8.6	pEC50	=	8.6	Functional	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	162365	0	None	20	2	Mouse	8.6	pEC50	=	8.6	Functional	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	66553	0	None	6	3	Human	8.6	pEC50	=	8.6	Functional	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	66553	0	None	6	3	Human	8.6	pEC50	=	8.6	Functional	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	66553	0	None	6	3	Human	8.6	pEC50	=	8.6	Functional	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	214617	0	None	38	2	Human	8.5	pEC50	=	8.5	Functional	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	73293	0	None	-6	2	Human	8.5	pEC50	=	8.5	Functional	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	73293	0	None	-6	2	Human	8.5	pEC50	=	8.5	Functional	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	124208	0	None	-	1	Rat	8.5	pEC50	=	8.5	Functional	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	124208	0	None	-	1	Rat	8.5	pEC50	=	8.5	Functional	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	87910	0	None	-107	2	Rat	8.5	pEC50	=	8.5	Functional	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	87910	0	None	-107	2	Rat	8.5	pEC50	=	8.5	Functional	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	159890	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	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	159890	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	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	191221	0	None	-3	2	Human	8.5	pEC50	=	8.5	Functional	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	191221	0	None	-3	2	Human	8.5	pEC50	=	8.5	Functional	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	158254	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	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	158254	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	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	176496	0	None	-	1	Mouse	8.5	pEC50	=	8.5	Functional	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	176496	0	None	-	1	Mouse	8.5	pEC50	=	8.5	Functional	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	176496	0	None	-	1	Mouse	8.5	pEC50	=	8.5	Functional	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	209168	0	None	-8	4	Rat	7.7	pEC50	=	7.7	Functional	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	92050	0	None	-1	5	Human	7.7	pEC50	=	7.7	Functional	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	92050	0	None	-1	5	Human	7.7	pEC50	=	7.7	Functional	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	214692	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	104463	0	None	75	2	Rat	7.7	pEC50	=	7.7	Functional	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	104463	0	None	75	2	Rat	7.7	pEC50	=	7.7	Functional	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	149565	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	149565	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	181798	0	None	1	5	Human	7.7	pEC50	=	7.7	Functional	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	181798	0	None	1	5	Human	7.7	pEC50	=	7.7	Functional	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	109697	16	None	5	3	Human	7.7	pEC50	=	7.7	Functional	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	109697	16	None	5	3	Human	7.7	pEC50	=	7.7	Functional	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	109697	16	None	5	3	Human	7.7	pEC50	=	7.7	Functional	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	137970	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	137970	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	177096	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	177096	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	103593	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	103593	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	164151	6	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	164151	6	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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
	71819400	92049	0	None	-3	5	Human	5.7	pEC50	=	5.7	Functional	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	92049	0	None	-3	5	Human	5.7	pEC50	=	5.7	Functional	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	92055	0	None	2	4	Mouse	5.7	pEC50	=	5.7	Functional	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	92055	0	None	2	4	Mouse	5.7	pEC50	=	5.7	Functional	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	214551	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	106324	0	None	-81	3	Human	6.7	pEC50	=	6.7	Functional	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	106324	0	None	-81	3	Human	6.7	pEC50	=	6.7	Functional	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	106324	0	None	-81	3	Human	6.7	pEC50	=	6.7	Functional	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	36	None	-8	4	Mouse	6.7	pEC50	=	6.7	Functional	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	36	None	-8	4	Mouse	6.7	pEC50	=	6.7	Functional	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	36	None	-8	4	Mouse	6.7	pEC50	=	6.7	Functional	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	173503	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Inhibition of mu opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 60 minsInhibition of mu opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 60 mins	ChEMBL	381	8	2	3	3.9	CN(C)[C@H](CNC(=O)NCCc1ccsc1)Cc1cccc2ccccc12	10.1016/j.ejmech.2019.111701
	CHEMBL4530626	173503	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Inhibition of mu opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 60 minsInhibition of mu opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 60 mins	ChEMBL	381	8	2	3	3.9	CN(C)[C@H](CNC(=O)NCCc1ccsc1)Cc1cccc2ccccc12	10.1016/j.ejmech.2019.111701
	44408590	161726	0	None	-5	5	Rat	6.7	pEC50	=	6.7	Functional	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	1134	30	12	15	2.6	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)OC(C)(C)C)c2ccccc12)C(=O)O	10.1021/jm050851n
	CHEMBL413644	161726	0	None	-5	5	Rat	6.7	pEC50	=	6.7	Functional	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	1134	30	12	15	2.6	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)OC(C)(C)C)c2ccccc12)C(=O)O	10.1021/jm050851n
	137630132	161050	0	None	-	1	Rat	5.7	pEC50	=	5.7	Functional	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	273	3	2	3	2.4	C=CCN1CC[C@@]2(c3cccc(O)c3)CCC[C@@H]1[C@H]2O	10.1016/j.bmc.2017.02.064
	CHEMBL4073254	161050	0	None	-	1	Rat	5.7	pEC50	=	5.7	Functional	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	273	3	2	3	2.4	C=CCN1CC[C@@]2(c3cccc(O)c3)CCC[C@@H]1[C@H]2O	10.1016/j.bmc.2017.02.064
	CHEMBL4116539	161050	0	None	-	1	Rat	5.7	pEC50	=	5.7	Functional	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	273	3	2	3	2.4	C=CCN1CC[C@@]2(c3cccc(O)c3)CCC[C@@H]1[C@H]2O	10.1016/j.bmc.2017.02.064
	71761638	91401	0	None	-4	2	Rat	5.7	pEC50	=	5.7	Functional	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	91401	0	None	-4	2	Rat	5.7	pEC50	=	5.7	Functional	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
	CHEMBL5075990	214407	0	None	2	2	Human	6.7	pEC50	=	6.7	Functional	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		CCc1cc(Cl)c(OC)c(C(=O)NCC2CCCN2CCCCNCCC(C(=O)N(C)C)(c2ccccc2)c2ccccc2)c1O	10.1021/acs.jmedchem.1c00611
	24906155	188813	0	None	-	1	Rat	5.7	pEC50	=	5.7	Functional	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	585	13	6	6	1.5	NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC[C@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm800223t
	CHEMBL506168	188813	0	None	-	1	Rat	5.7	pEC50	=	5.7	Functional	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	585	13	6	6	1.5	NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC[C@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm800223t
	3244713	67603	1	None	-	1	Human	4.7	pEC50	=	4.7	Functional	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	489	7	1	6	5.1	COc1ccc(-c2nc(CN3CCC(C(=O)NC4CCCc5ccccc54)CC3)c(C)o2)cc1OC	nan
	CHEMBL1902708	67603	1	None	-	1	Human	4.7	pEC50	=	4.7	Functional	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	489	7	1	6	5.1	COc1ccc(-c2nc(CN3CCC(C(=O)NC4CCCc5ccccc54)CC3)c(C)o2)cc1OC	nan
	137646492	157777	0	None	-9332	2	Human	6.7	pEC50	=	6.7	Functional	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	502	5	3	6	3.0	CN(C(=O)/C=C/c1ccccc1)[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
	CHEMBL4082823	157777	0	None	-9332	2	Human	6.7	pEC50	=	6.7	Functional	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	502	5	3	6	3.0	CN(C(=O)/C=C/c1ccccc1)[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
	3054741	78279	18	None	-15	2	Human	7.7	pEC50	=	7.7	Functional	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	285	2	1	3	3.0	C[C@H]1[C@H]2C(=O)c3ccc(O)cc3[C@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2008.10.134
	CHEMBL2107292	78279	18	None	-15	2	Human	7.7	pEC50	=	7.7	Functional	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	285	2	1	3	3.0	C[C@H]1[C@H]2C(=O)c3ccc(O)cc3[C@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2008.10.134
	156011205	178314	0	None	1	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay	ChEMBL	1341	18	13	19	-0.4	CN(C)c1cccc2c(S(=O)(=O)NCCN3C(=O)C4=C(SC[C@@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)C(=O)NCC(=O)N[C@@H](Cc5ccccc5)C(=O)NNC(=O)[C@H](Cc5ccccc5)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)CS4)C3=O)cccc12	10.1021/acsmedchemlett.9b00569
	CHEMBL4638703	178314	0	None	1	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay	ChEMBL	1341	18	13	19	-0.4	CN(C)c1cccc2c(S(=O)(=O)NCCN3C(=O)C4=C(SC[C@@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)C(=O)NCC(=O)N[C@@H](Cc5ccccc5)C(=O)NNC(=O)[C@H](Cc5ccccc5)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)CS4)C3=O)cccc12	10.1021/acsmedchemlett.9b00569
	CHEMBL4651062	178314	0	None	1	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay	ChEMBL	1341	18	13	19	-0.4	CN(C)c1cccc2c(S(=O)(=O)NCCN3C(=O)C4=C(SC[C@@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)C(=O)NCC(=O)N[C@@H](Cc5ccccc5)C(=O)NNC(=O)[C@H](Cc5ccccc5)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)CS4)C3=O)cccc12	10.1021/acsmedchemlett.9b00569
	118561045	181022	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	2.7	CC1OC2(CCN(CCc3ccccc3)CC2)CN(C(C)C)C1=O	10.1021/acs.jmedchem.0c01127
	CHEMBL4759184	181022	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	2.7	CC1OC2(CCN(CCc3ccccc3)CC2)CN(C(C)C)C1=O	10.1021/acs.jmedchem.0c01127
	117706085	159206	0	None	-12	3	Human	7.7	pEC50	=	7.7	Functional	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	446	4	1	3	5.4	Oc1ccc2c(c1)C13CCN(CC4CC4)C(C2)C12CCC1C3[C@@H](CN1CC1CCCCC1)C2	10.1016/j.bmcl.2017.05.072
	CHEMBL4098662	159206	0	None	-12	3	Human	7.7	pEC50	=	7.7	Functional	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	446	4	1	3	5.4	Oc1ccc2c(c1)C13CCN(CC4CC4)C(C2)C12CCC1C3[C@@H](CN1CC1CCCCC1)C2	10.1016/j.bmcl.2017.05.072
	25129135	172597	0	None	-5	5	Rat	7.7	pEC50	=	7.7	Functional	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assayAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assay	ChEMBL	1073	27	10	11	2.9	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)NCc1ccccc1	10.1021/jm800389v
	CHEMBL448998	172597	0	None	-5	5	Rat	7.7	pEC50	=	7.7	Functional	Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assayAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assay	ChEMBL	1073	27	10	11	2.9	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)NCc1ccccc1	10.1021/jm800389v
	71625395	87890	0	None	-28	2	Rat	7.7	pEC50	=	7.7	Functional	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	7	2	5	4.6	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
	CHEMBL2338729	87890	0	None	-28	2	Rat	7.7	pEC50	=	7.7	Functional	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	7	2	5	4.6	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
	5360630	102393	4	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	357	2	3	5	1.7	Oc1ccc2c3c1OC1[C@@H](O)CC[C@@]4(O)[C@@H](C2)N(CC2CCC2)CC[C@]314	nan
	CHEMBL3039334	102393	4	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	357	2	3	5	1.7	Oc1ccc2c3c1OC1[C@@H](O)CC[C@@]4(O)[C@@H](C2)N(CC2CCC2)CC[C@]314	nan
	1623	1560	41	None	-2	5	Human	7.7	pEC50	=	7.7	Functional	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
	5311080	1560	41	None	-2	5	Human	7.7	pEC50	=	7.7	Functional	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
	CHEMBL316446	1560	41	None	-2	5	Human	7.7	pEC50	=	7.7	Functional	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
	1627	2594	20	None	1	8	Rat	7.7	pEC50	=	7.7	Functional	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	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/s0960-894x(98)00472-7
	1845	2594	20	None	1	8	Rat	7.7	pEC50	=	7.7	Functional	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	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/s0960-894x(98)00472-7
	5288826	2594	20	None	1	8	Rat	7.7	pEC50	=	7.7	Functional	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	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/s0960-894x(98)00472-7
	CHEMBL70	2594	20	None	1	8	Rat	7.7	pEC50	=	7.7	Functional	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	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/s0960-894x(98)00472-7
	DB00295	2594	20	None	1	8	Rat	7.7	pEC50	=	7.7	Functional	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	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/s0960-894x(98)00472-7
	121596705	3246	36	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	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	36	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	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	36	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	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	36	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	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
	71461668	79178	0	None	-2	3	Human	7.7	pEC50	=	7.7	Functional	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	476	4	2	3	6.1	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(CCCc2ccccc2)C1C5	10.1021/jm021073r
	CHEMBL2113380	79178	0	None	-2	3	Human	7.7	pEC50	=	7.7	Functional	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	476	4	2	3	6.1	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(CCCc2ccccc2)C1C5	10.1021/jm021073r
	46227363	199665	0	None	-169	5	Rat	7.7	pEC50	=	7.7	Functional	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	16	10	12	4.7	CCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@H](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	10.1016/j.bmc.2009.08.035
	CHEMBL592969	199665	0	None	-169	5	Rat	7.7	pEC50	=	7.7	Functional	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	16	10	12	4.7	CCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@H](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	10.1016/j.bmc.2009.08.035
	44418923	161785	0	None	-5	5	Rat	6.7	pEC50	=	6.7	Functional	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
	CHEMBL414087	161785	0	None	-5	5	Rat	6.7	pEC50	=	6.7	Functional	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
	CHEMBL5090993	215289	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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		CCOCCN1CCN(C2(CN(C(=O)CC)c3cccc(C(F)(F)F)n3)CCOCC2)CC1	10.1021/acs.jmedchem.1c00417
	57412593	75860	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	404	4	2	5	3.1	COc1ccccc1CNc1ccc2c3c1O[C@H]1[C@@H](O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314	10.1021/jm3001086
	CHEMBL2048782	75860	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	404	4	2	5	3.1	COc1ccccc1CNc1ccc2c3c1O[C@H]1[C@@H](O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314	10.1021/jm3001086
	44408590	161726	0	None	-5	5	Rat	6.7	pEC50	=	6.7	Functional	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	1134	30	12	15	2.6	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)OC(C)(C)C)c2ccccc12)C(=O)O	10.1021/jm050851n
	CHEMBL413644	161726	0	None	-5	5	Rat	6.7	pEC50	=	6.7	Functional	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	1134	30	12	15	2.6	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)OC(C)(C)C)c2ccccc12)C(=O)O	10.1021/jm050851n
	44398175	67856	0	None	2	2	Human	5.7	pEC50	=	5.7	Functional	Stimulation of [35S]GTP-gamma-S, binding to Opioid receptor mu1 expressed in CHO cells; ND = Not determinedStimulation of [35S]GTP-gamma-S, binding to Opioid receptor mu1 expressed in CHO cells; ND = Not determined	ChEMBL	495	4	0	9	3.7	COC(=O)[C@@H]1C[C@H](OC(=O)c2cccnc2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@]21C	10.1021/jm048963m
	CHEMBL191014	67856	0	None	2	2	Human	5.7	pEC50	=	5.7	Functional	Stimulation of [35S]GTP-gamma-S, binding to Opioid receptor mu1 expressed in CHO cells; ND = Not determinedStimulation of [35S]GTP-gamma-S, binding to Opioid receptor mu1 expressed in CHO cells; ND = Not determined	ChEMBL	495	4	0	9	3.7	COC(=O)[C@@H]1C[C@H](OC(=O)c2cccnc2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@]21C	10.1021/jm048963m
	90655979	111012	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human mu opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis	ChEMBL	360	5	0	2	4.7	CCC1C(=O)N(C2CCN(C/C=C/c3ccccc3)CC2)c2ccccc21	10.1016/j.bmc.2014.02.047
	CHEMBL3262552	111012	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human mu opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis	ChEMBL	360	5	0	2	4.7	CCC1C(=O)N(C2CCN(C/C=C/c3ccccc3)CC2)c2ccccc21	10.1016/j.bmc.2014.02.047
	3668	1561	42	None	-1	4	Rat	6.7	pEC50	=	6.7	Functional	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
	5311081	1561	42	None	-1	4	Rat	6.7	pEC50	=	6.7	Functional	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
	CHEMBL333357	1561	42	None	-1	4	Rat	6.7	pEC50	=	6.7	Functional	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
	CHEMBL589982	1561	42	None	-1	4	Rat	6.7	pEC50	=	6.7	Functional	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
	145964503	164085	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	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	371	4	1	4	3.8	COc1ccc2c(c1)[nH]c(=O)n2C1CCN(Cc2ccccc2Cl)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4209504	164085	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	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	371	4	1	4	3.8	COc1ccc2c(c1)[nH]c(=O)n2C1CCN(Cc2ccccc2Cl)CC1	10.1021/acs.jmedchem.8b01136
	1619	1517	38	None	-147	7	Human	6.7	pEC50	=	6.7	Functional	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
	25075996	1517	38	None	-147	7	Human	6.7	pEC50	=	6.7	Functional	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
	25077992	1517	38	None	-147	7	Human	6.7	pEC50	=	6.7	Functional	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
	CHEMBL265813	1517	38	None	-147	7	Human	6.7	pEC50	=	6.7	Functional	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
	CHEMBL405618	1517	38	None	-147	7	Human	6.7	pEC50	=	6.7	Functional	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
	1619	1517	38	None	-147	7	Human	6.7	pEC50	=	6.7	Functional	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		None	None	None		None	10.1016/j.bmc.2016.02.034
	25075996	1517	38	None	-147	7	Human	6.7	pEC50	=	6.7	Functional	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		None	None	None		None	10.1016/j.bmc.2016.02.034
	25077992	1517	38	None	-147	7	Human	6.7	pEC50	=	6.7	Functional	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		None	None	None		None	10.1016/j.bmc.2016.02.034
	CHEMBL265813	1517	38	None	-147	7	Human	6.7	pEC50	=	6.7	Functional	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		None	None	None		None	10.1016/j.bmc.2016.02.034
	CHEMBL405618	1517	38	None	-147	7	Human	6.7	pEC50	=	6.7	Functional	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		None	None	None		None	10.1016/j.bmc.2016.02.034
	101600082	1516	28	None	-933	6	Human	6.7	pEC50	=	6.7	Functional	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
	16133805	1516	28	None	-933	6	Human	6.7	pEC50	=	6.7	Functional	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
	1620	1516	28	None	-933	6	Human	6.7	pEC50	=	6.7	Functional	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
	44298303	1516	28	None	-933	6	Human	6.7	pEC50	=	6.7	Functional	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
	91928823	1516	28	None	-933	6	Human	6.7	pEC50	=	6.7	Functional	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
	CHEMBL411557	1516	28	None	-933	6	Human	6.7	pEC50	=	6.7	Functional	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
	DB16146	1516	28	None	-933	6	Human	6.7	pEC50	=	6.7	Functional	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
	CHEMBL5075990	214407	0	None	2	2	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human mu opioid receptor expressed in HEK293T cells assessed as Nb33 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 Nb33 recruitment preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay	ChEMBL		None	None	None		CCc1cc(Cl)c(OC)c(C(=O)NCC2CCCN2CCCCNCCC(C(=O)N(C)C)(c2ccccc2)c2ccccc2)c1O	10.1021/acs.jmedchem.1c00611
	49863733	15332	0	None	-20	5	Rat	5.7	pEC50	=	5.7	Functional	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
	CHEMBL1214026	15332	0	None	-20	5	Rat	5.7	pEC50	=	5.7	Functional	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
	71461664	79134	0	None	1	2	Human	6.7	pEC50	=	6.7	Functional	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	545	7	1	7	3.9	COc1ccc2c3c1O[C@H]1[C@]4(OC)CC[C@@]5(C[C@@H]4CNC(=O)/C=C/c4ccc([N+](=O)[O-])cc4)[C@@H](C2)N(C)CC[C@]315	10.1021/jm070255o
	CHEMBL2113299	79134	0	None	1	2	Human	6.7	pEC50	=	6.7	Functional	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	545	7	1	7	3.9	COc1ccc2c3c1O[C@H]1[C@]4(OC)CC[C@@]5(C[C@@H]4CNC(=O)/C=C/c4ccc([N+](=O)[O-])cc4)[C@@H](C2)N(C)CC[C@]315	10.1021/jm070255o
	1647	1313	45	None	-5	8	Rat	6.7	pEC50	=	6.7	Functional	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
	5462471	1313	45	None	-5	8	Rat	6.7	pEC50	=	6.7	Functional	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
	CHEMBL113995	1313	45	None	-5	8	Rat	6.7	pEC50	=	6.7	Functional	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
	CHEMBL38874	1313	45	None	-5	8	Rat	6.7	pEC50	=	6.7	Functional	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
	44574705	178787	0	None	-15	2	Human	5.7	pEC50	=	5.7	Functional	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	451	5	1	2	6.6	OCC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl	10.1016/j.bmcl.2009.03.031
	CHEMBL468952	178787	0	None	-15	2	Human	5.7	pEC50	=	5.7	Functional	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	451	5	1	2	6.6	OCC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl	10.1016/j.bmcl.2009.03.031
	86711658	160245	0	None	-7	2	Human	6.7	pEC50	=	6.7	Functional	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	496	7	0	5	5.0	CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(C#N)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	nan
	CHEMBL4109954	160245	0	None	-7	2	Human	6.7	pEC50	=	6.7	Functional	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	496	7	0	5	5.0	CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(C#N)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5	nan
	89978654	160798	0	None	-2	2	Human	5.7	pEC50	=	5.7	Functional	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	540	9	0	6	5.3	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)[C@@H]2CC#N	nan
	CHEMBL4114384	160798	0	None	-2	2	Human	5.7	pEC50	=	5.7	Functional	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	540	9	0	6	5.3	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)[C@@H]2CC#N	nan
	71450926	79135	0	None	5	2	Human	6.7	pEC50	=	6.7	Functional	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	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	79135	0	None	5	2	Human	6.7	pEC50	=	6.7	Functional	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	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
	68091106	160464	0	None	4	2	Human	6.7	pEC50	=	6.7	Functional	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	2	6	2.6	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CNCC(=O)O)C2	nan
	CHEMBL4111763	160464	0	None	4	2	Human	6.7	pEC50	=	6.7	Functional	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	2	6	2.6	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CNCC(=O)O)C2	nan
	162670510	182978	0	None	-12	5	Human	6.7	pEC50	=	6.7	Functional	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
	CHEMBL4793250	182978	0	None	-12	5	Human	6.7	pEC50	=	6.7	Functional	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
	416359	101860	21	None	-28	3	Human	5.7	pEC50	=	5.7	Functional	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	307	3	1	4	3.6	Oc1nc2ccccc2n1C1CCN(Cc2ccccc2)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL300616	101860	21	None	-28	3	Human	5.7	pEC50	=	5.7	Functional	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	307	3	1	4	3.6	Oc1nc2ccccc2n1C1CCN(Cc2ccccc2)CC1	10.1021/acs.jmedchem.8b01136
	118567743	173826	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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(c2cccc(C(F)(F)F)n2)C1=O	10.1021/acs.jmedchem.9b01256
	CHEMBL4538620	173826	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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(c2cccc(C(F)(F)F)n2)C1=O	10.1021/acs.jmedchem.9b01256
	44181744	103373	9	None	-77	2	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human mu opioid receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP	ChEMBL	422	4	0	2	6.9	Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccccn1)C2	10.1021/jm9008218
	CHEMBL3084634	103373	9	None	-77	2	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human mu opioid receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP	ChEMBL	422	4	0	2	6.9	Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccccn1)C2	10.1021/jm9008218
	CHEMBL218763	209399	0	None	-7	5	Rat	7.7	pEC50	=	7.7	Functional	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](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm050921q
	118562325	183269	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	6	0	3	3.6	CC1OC2(CCN(CCc3ccccc3)CC2)CN(CCc2ccccc2)C1=O	10.1021/acs.jmedchem.0c01127
	CHEMBL4796605	183269	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	6	0	3	3.6	CC1OC2(CCN(CCc3ccccc3)CC2)CN(CCc2ccccc2)C1=O	10.1021/acs.jmedchem.0c01127
	132079911	179555	0	None	4	2	Human	7.7	pEC50	=	7.7	Functional	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	506	4	0	8	4.7	COC(=O)[C@@H]1C=C(OC(=O)c2ccc(C)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
	CHEMBL4741711	179555	0	None	4	2	Human	7.7	pEC50	=	7.7	Functional	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	506	4	0	8	4.7	COC(=O)[C@@H]1C=C(OC(=O)c2ccc(C)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
	145966212	164284	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	373	3	1	3	4.5	CC(c1ccc(Cl)cc1F)N1CCC(n2c(=O)[nH]c3ccccc32)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4211924	164284	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	373	3	1	3	4.5	CC(c1ccc(Cl)cc1F)N1CCC(n2c(=O)[nH]c3ccccc32)CC1	10.1021/acs.jmedchem.8b01136
	117860306	157263	0	None	-15	2	Human	7.7	pEC50	=	7.7	Functional	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	474	5	1	5	3.4	COCCCN1CCC23c4cc(O)ccc4CC1C21CCC2C3[C@@H](CN2C(=O)c2ccccc2)O1	10.1016/j.bmcl.2017.04.059
	CHEMBL4076673	157263	0	None	-15	2	Human	7.7	pEC50	=	7.7	Functional	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	474	5	1	5	3.4	COCCCN1CCC23c4cc(O)ccc4CC1C21CCC2C3[C@@H](CN2C(=O)c2ccccc2)O1	10.1016/j.bmcl.2017.04.059
	54585845	62080	0	None	-12	2	Human	7.7	pEC50	=	7.7	Functional	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	845	17	2	8	12.5	c1c2c(cc3sc(NCCCCCCCCCCNc4nc5cc6c(cc5s4)C[C@@H]4[C@@H]5CCCC[C@]65CCN4CC4CC4)nc13)C[C@@H]1[C@@H]3CCCC[C@]23CCN1CC1CC1	10.1016/j.bmc.2011.03.052
	CHEMBL1774952	62080	0	None	-12	2	Human	7.7	pEC50	=	7.7	Functional	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	845	17	2	8	12.5	c1c2c(cc3sc(NCCCCCCCCCCNc4nc5cc6c(cc5s4)C[C@@H]4[C@@H]5CCCC[C@]65CCN4CC4CC4)nc13)C[C@@H]1[C@@H]3CCCC[C@]23CCN1CC1CC1	10.1016/j.bmc.2011.03.052
	46227363	199665	0	None	-169	5	Rat	7.7	pEC50	=	7.7	Functional	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	16	10	12	4.7	CCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@H](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	10.1016/j.bmc.2009.08.035
	CHEMBL592969	199665	0	None	-169	5	Rat	7.7	pEC50	=	7.7	Functional	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	16	10	12	4.7	CCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@H](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	10.1016/j.bmc.2009.08.035
	16756840	142360	0	None	15	2	Rat	7.7	pEC50	=	7.7	Functional	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	337	4	2	3	3.5	Oc1cccc([C@]23CCC[C@H]([C@H]2O)N(CCc2ccccc2)CC3)c1	10.1016/j.bmc.2017.02.064
	CHEMBL388873	142360	0	None	15	2	Rat	7.7	pEC50	=	7.7	Functional	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	337	4	2	3	3.5	Oc1cccc([C@]23CCC[C@H]([C@H]2O)N(CCc2ccccc2)CC3)c1	10.1016/j.bmc.2017.02.064
	117862197	153294	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	495	7	2	4	5.4	C[C@H]1[C@H]2Cc3ccc(C(=O)NCCc4ccc(-c5ccc(O)nc5)cc4)cc3[C@@]1(C)CCN2CC1CC1	nan
	CHEMBL3977887	153294	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	495	7	2	4	5.4	C[C@H]1[C@H]2Cc3ccc(C(=O)NCCc4ccc(-c5ccc(O)nc5)cc4)cc3[C@@]1(C)CCN2CC1CC1	nan
	53317567	58958	0	None	-	1	Rat	7.7	pEC50	=	7.7	Functional	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	680	13	7	6	3.5	Cc1cc(CC(N)C(=O)N[C@@H]2CCCC[C@@H]2C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)[C@@H](C)c2ccccc2)cc(C)c1O	10.1021/jm101515v
	CHEMBL1689541	58958	0	None	-	1	Rat	7.7	pEC50	=	7.7	Functional	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	680	13	7	6	3.5	Cc1cc(CC(N)C(=O)N[C@@H]2CCCC[C@@H]2C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)[C@@H](C)c2ccccc2)cc(C)c1O	10.1021/jm101515v
	86711653	160588	0	None	-2	3	Human	7.7	pEC50	=	7.7	Functional	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	542	8	0	5	5.0	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CN(Cc1ccccc1)C(C)=O)C2	nan
	CHEMBL4112771	160588	0	None	-2	3	Human	7.7	pEC50	=	7.7	Functional	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	542	8	0	5	5.0	COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CN(Cc1ccccc1)C(C)=O)C2	nan
	22558157	111007	0	None	1	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human mu opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis	ChEMBL	374	3	0	2	4.5	CCC1C(=O)N(C2CCN(C3CCc4ccccc4C3)CC2)c2ccccc21	10.1016/j.bmc.2014.02.047
	CHEMBL3262547	111007	0	None	1	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human mu opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis	ChEMBL	374	3	0	2	4.5	CCC1C(=O)N(C2CCN(C3CCc4ccccc4C3)CC2)c2ccccc21	10.1016/j.bmc.2014.02.047
	CHEMBL5083135	214845	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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		Clc1ccc(CNCC[C@@]2(c3ccccn3)CCOC3(CCOC3)C2)s1	10.1016/j.ejmech.2021.113986
	CHEMBL218763	209399	0	None	-7	5	Rat	7.7	pEC50	=	7.7	Functional	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](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm050921q
	1647	1313	45	None	-3	8	Human	6.7	pEC50	=	6.7	Functional	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		None	None	None		None	10.1021/acs.jmedchem.8b01136
	5462471	1313	45	None	-3	8	Human	6.7	pEC50	=	6.7	Functional	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		None	None	None		None	10.1021/acs.jmedchem.8b01136
	CHEMBL113995	1313	45	None	-3	8	Human	6.7	pEC50	=	6.7	Functional	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		None	None	None		None	10.1021/acs.jmedchem.8b01136
	CHEMBL38874	1313	45	None	-3	8	Human	6.7	pEC50	=	6.7	Functional	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		None	None	None		None	10.1021/acs.jmedchem.8b01136
	CHEMBL2387212	210401	0	None	-2	3	Rat	6.7	pEC50	=	6.7	Functional	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@H](NC(=O)[C@H](CCC(=O)NCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)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(N)=O)C(C)C	10.1016/j.bmcl.2013.03.065
	16037891	77223	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	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	487	9	2	6	6.0	CCOc1ccc(Cc2nc3cc(NC(=N)c4cccs4)ccc3n2CCC2CCCN2C)cc1	10.1021/ml200268w
	CHEMBL2079477	77223	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	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	487	9	2	6	6.0	CCOc1ccc(Cc2nc3cc(NC(=N)c4cccs4)ccc3n2CCC2CCCN2C)cc1	10.1021/ml200268w
	CHEMBL3216780	77223	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	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	487	9	2	6	6.0	CCOc1ccc(Cc2nc3cc(NC(=N)c4cccs4)ccc3n2CCC2CCCN2C)cc1	10.1021/ml200268w
	124037300	152117	0	None	-	1	Human	4.7	pEC50	=	4.7	Functional	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	489	14	0	8	2.2	COCCOCCOCCOCCO[C@H]1C=CC2C3Cc4ccc(OC)c5c4[C@@]2(CCN3C)C1O5	nan
	CHEMBL3967811	152117	0	None	-	1	Human	4.7	pEC50	=	4.7	Functional	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	489	14	0	8	2.2	COCCOCCOCCOCCO[C@H]1C=CC2C3Cc4ccc(OC)c5c4[C@@]2(CCN3C)C1O5	nan
	162670510	182978	0	None	-12	5	Human	6.7	pEC50	=	6.7	Functional	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
	CHEMBL4793250	182978	0	None	-12	5	Human	6.7	pEC50	=	6.7	Functional	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
	156017302	177745	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	671	17	10	8	0.7	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1	10.1016/j.bmc.2020.115438
	CHEMBL4642564	177745	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	671	17	10	8	0.7	C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1	10.1016/j.bmc.2020.115438
	44421407	136896	0	None	-26	3	Human	6.7	pEC50	=	6.7	Functional	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	392	0	2	5	2.5	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2c(c4c(n2C)CCCC4)C[C@@]3(O)C1C5	10.1021/jm040817t
	CHEMBL374228	136896	0	None	-26	3	Human	6.7	pEC50	=	6.7	Functional	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	392	0	2	5	2.5	CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2c(c4c(n2C)CCCC4)C[C@@]3(O)C1C5	10.1021/jm040817t
	71765058	91408	0	None	-5	2	Rat	5.7	pEC50	=	5.7	Functional	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	612	7	8	10	-2.1	CS/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
	CHEMBL2402937	91408	0	None	-5	2	Rat	5.7	pEC50	=	5.7	Functional	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	612	7	8	10	-2.1	CS/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
	168287282	191787	0	None	-34	4	Human	5.7	pEC50	=	5.7	Functional	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	16	6	6	2.0	CCNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1	10.1039/D1MD00025J
	CHEMBL5198168	191787	0	None	-34	4	Human	5.7	pEC50	=	5.7	Functional	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	16	6	6	2.0	CCNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1	10.1039/D1MD00025J
	71765058	91408	0	None	-5	2	Rat	5.7	pEC50	=	5.7	Functional	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	612	7	8	10	-2.1	CS/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
	CHEMBL2402937	91408	0	None	-5	2	Rat	5.7	pEC50	=	5.7	Functional	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	612	7	8	10	-2.1	CS/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
	130431408	164603	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	Cc1ccc2c(c1)[nH]c(=O)n2C1CCN(Cc2ccccc2Cl)CC1	10.1021/acs.jmedchem.8b01136
	CHEMBL4215851	164603	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	Cc1ccc2c(c1)[nH]c(=O)n2C1CCN(Cc2ccccc2Cl)CC1	10.1021/acs.jmedchem.8b01136
	9927776	164853	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	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	337	4	1	4	3.2	COc1ccc(CN2CCC(n3c(=O)[nH]c4ccccc43)CC2)cc1	10.1021/acs.jmedchem.8b01136
	CHEMBL4219000	164853	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	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	337	4	1	4	3.2	COc1ccc(CN2CCC(n3c(=O)[nH]c4ccccc43)CC2)cc1	10.1021/acs.jmedchem.8b01136
	168287282	191787	0	None	-34	4	Human	5.6	pEC50	=	5.6	Functional	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	16	6	6	2.0	CCNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1	10.1039/D1MD00025J
	CHEMBL5198168	191787	0	None	-34	4	Human	5.6	pEC50	=	5.6	Functional	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	16	6	6	2.0	CCNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1	10.1039/D1MD00025J
	71765059	91409	0	None	1	2	Rat	5.6	pEC50	=	5.6	Functional	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	581	7	9	10	-3.5	NC(=O)[C@@H]1C/N=C(/N)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
	CHEMBL2402938	91409	0	None	1	2	Rat	5.6	pEC50	=	5.6	Functional	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	581	7	9	10	-3.5	NC(=O)[C@@H]1C/N=C(/N)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
	607612	113867	13	None	-	1	Human	5.6	pEC50	=	5.6	Functional	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(-c2ccccc2Cl)c2c1C(=O)CC(C)(C)C2	10.1016/j.bmc.2014.07.012
	CHEMBL3325696	113867	13	None	-	1	Human	5.6	pEC50	=	5.6	Functional	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(-c2ccccc2Cl)c2c1C(=O)CC(C)(C)C2	10.1016/j.bmc.2014.07.012
	71761637	91400	0	None	-	1	Rat	5.6	pEC50	=	5.6	Functional	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	91400	0	None	-	1	Rat	5.6	pEC50	=	5.6	Functional	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
	25163156	39591	4	None	-	1	Human	4.6	pEC50	=	4.6	Functional	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	480	9	0	7	3.7	COCCN(C(=O)C1CC(=O)N(Cc2ccccc2)C1)c1nc(-c2ccc([N+](=O)[O-])cc2)cs1	nan
	CHEMBL1473706	39591	4	None	-	1	Human	4.6	pEC50	=	4.6	Functional	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	480	9	0	7	3.7	COCCN(C(=O)C1CC(=O)N(Cc2ccccc2)C1)c1nc(-c2ccc([N+](=O)[O-])cc2)cs1	nan
	118562598	172202	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	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(CCc3ccccn3)CC2)CN(c2ccccc2)C1=O	10.1021/acs.jmedchem.9b01256
	CHEMBL4473746	172202	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	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(CCc3ccccn3)CC2)CN(c2ccccc2)C1=O	10.1021/acs.jmedchem.9b01256
	71765059	91409	0	None	1	2	Rat	5.6	pEC50	=	5.6	Functional	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	581	7	9	10	-3.5	NC(=O)[C@@H]1C/N=C(/N)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
	CHEMBL2402938	91409	0	None	1	2	Rat	5.6	pEC50	=	5.6	Functional	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	581	7	9	10	-3.5	NC(=O)[C@@H]1C/N=C(/N)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
	1647	1313	45	None	-3	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00569
	5462471	1313	45	None	-3	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00569
	CHEMBL113995	1313	45	None	-3	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00569
	CHEMBL38874	1313	45	None	-3	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00569
	25208097	183922	3	None	-2	4	Human	7.6	pEC50	=	7.6	Functional	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	408	3	1	4	5.6	CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1	10.1021/jm7012979
	CHEMBL481366	183922	3	None	-2	4	Human	7.6	pEC50	=	7.6	Functional	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	408	3	1	4	5.6	CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1	10.1021/jm7012979
	CHEMBL3609617	211831	0	None	12	3	Rat	7.6	pEC50	=	7.6	Functional	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](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1	10.1016/j.bmcl.2015.06.030
	90655975	111008	0	None	3	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human mu opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis	ChEMBL	373	4	1	2	4.7	CCC1C(=O)N(C2CCN(Cc3cccc4[nH]ccc34)CC2)c2ccccc21	10.1016/j.bmc.2014.02.047
	CHEMBL3262548	111008	0	None	3	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human mu opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis	ChEMBL	373	4	1	2	4.7	CCC1C(=O)N(C2CCN(Cc3cccc4[nH]ccc34)CC2)c2ccccc21	10.1016/j.bmc.2014.02.047
	23635166	168970	0	None	1	3	Rat	7.6	pEC50	=	7.6	Functional	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	784	17	7	9	1.0	CCC(=O)N(c1ccccc1)C1CCN(C(=O)CCC(=O)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC1	10.1021/jm061465o
	CHEMBL439026	168970	0	None	1	3	Rat	7.6	pEC50	=	7.6	Functional	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	784	17	7	9	1.0	CCC(=O)N(c1ccccc1)C1CCN(C(=O)CCC(=O)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC1	10.1021/jm061465o
	156013730	177262	0	None	-11	3	Human	7.6	pEC50	=	7.6	Functional	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	COc1ccc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)cc1	10.1021/acs.jmedchem.0c00503
	CHEMBL4636159	177262	0	None	-11	3	Human	7.6	pEC50	=	7.6	Functional	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	COc1ccc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)cc1	10.1021/acs.jmedchem.0c00503
	66826434	160263	0	None	-1	2	Human	7.6	pEC50	=	7.6	Functional	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	547	8	0	4	6.7	COc1ccc2c3c1O[C@H]1[C@@]4(c5ccccc5)CC[C@@]5(C[C@@H]4COCc4ccccc4)[C@@H](C2)N(CC2CC2)CC[C@]315	nan
	CHEMBL4110146	160263	0	None	-1	2	Human	7.6	pEC50	=	7.6	Functional	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	547	8	0	4	6.7	COc1ccc2c3c1O[C@H]1[C@@]4(c5ccccc5)CC[C@@]5(C[C@@H]4COCc4ccccc4)[C@@H](C2)N(CC2CC2)CC[C@]315	nan
	156019389	178008	0	None	1	3	Human	7.6	pEC50	=	7.6	Functional	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	5	7.5	Oc1ccc2c3c1O[C@H]1c4ncc(-c5ccccc5)cc4C[C@@]4(OCCCC5CCCCC5)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/acs.jmedchem.0c00503
	CHEMBL4646507	178008	0	None	1	3	Human	7.6	pEC50	=	7.6	Functional	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	5	7.5	Oc1ccc2c3c1O[C@H]1c4ncc(-c5ccccc5)cc4C[C@@]4(OCCCC5CCCCC5)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/acs.jmedchem.0c00503
	25232727	189608	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	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)c1ccccn1	10.1021/jm801272c
	CHEMBL514781	189608	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	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)c1ccccn1	10.1021/jm801272c
	137541794	158406	0	None	-2	3	Human	6.6	pEC50	=	6.6	Functional	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	3	2	2	3.0	O=C(NCC1NCCc2ccccc21)c1ccc(Cl)cc1	10.1016/j.ejmech.2016.09.003
	CHEMBL4090148	158406	0	None	-2	3	Human	6.6	pEC50	=	6.6	Functional	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	3	2	2	3.0	O=C(NCC1NCCc2ccccc21)c1ccc(Cl)cc1	10.1016/j.ejmech.2016.09.003
	118567547	171941	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	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(c2cncc(F)c2)C1=O	10.1021/acs.jmedchem.9b01256
	CHEMBL4470425	171941	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	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(c2cncc(F)c2)C1=O	10.1021/acs.jmedchem.9b01256
	118713811	114417	0	None	-1	3	Rat	6.6	pEC50	=	6.6	Functional	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	1026	12	12	14	0.3	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)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/ml500241n
	CHEMBL3331511	114417	0	None	-1	3	Rat	6.6	pEC50	=	6.6	Functional	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	1026	12	12	14	0.3	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)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/ml500241n
	164851900	192441	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Partial 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 assayPartial agonist activity at human MOR expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 45 mins by cAMP HTRF assay	ChEMBL	368	7	0	2	4.3	CCC(=O)N(Cc1ccc(F)cc1)C1CCN(CCc2ccccc2)CC1	10.1016/j.ejmech.2022.114649
	CHEMBL5208375	192441	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Partial 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 assayPartial agonist activity at human MOR expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 45 mins by cAMP HTRF assay	ChEMBL	368	7	0	2	4.3	CCC(=O)N(Cc1ccc(F)cc1)C1CCN(CCc2ccccc2)CC1	10.1016/j.ejmech.2022.114649
	129188443	169537	3	None	-1	2	Human	6.6	pEC50	=	6.6	Functional	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	324	3	0	2	5.5	CC(C)[C@H]1CC[C@@H](N2CCC(n3ccc4ccccc43)CC2)CC1	10.1021/acs.jmedchem.9b02134
	CHEMBL4435280	169537	3	None	-1	2	Human	6.6	pEC50	=	6.6	Functional	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	324	3	0	2	5.5	CC(C)[C@H]1CC[C@@H](N2CCC(n3ccc4ccccc43)CC2)CC1	10.1021/acs.jmedchem.9b02134
	52942137	18251	7	None	-446	3	Human	6.6	pEC50	=	6.6	Functional	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	372	0	2	4	3.0	CN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13	10.1016/j.bmc.2013.10.032
	CHEMBL1270282	18251	7	None	-446	3	Human	6.6	pEC50	=	6.6	Functional	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	372	0	2	4	3.0	CN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13	10.1016/j.bmc.2013.10.032
	CHEMBL4296720	18251	7	None	-446	3	Human	6.6	pEC50	=	6.6	Functional	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	372	0	2	4	3.0	CN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13	10.1016/j.bmc.2013.10.032
	124037301	147849	0	None	-	1	Human	4.6	pEC50	=	4.6	Functional	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	533	17	0	9	2.2	COCCOCCOCCOCCOCCO[C@H]1C=CC2C3Cc4ccc(OC)c5c4[C@@]2(CCN3C)C1O5	nan
	CHEMBL3933053	147849	0	None	-	1	Human	4.6	pEC50	=	4.6	Functional	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	533	17	0	9	2.2	COCCOCCOCCOCCOCCO[C@H]1C=CC2C3Cc4ccc(OC)c5c4[C@@]2(CCN3C)C1O5	nan
	156022148	178197	0	None	-19	2	Human	6.6	pEC50	=	6.6	Functional	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)c1ccccc1-c1cnc2c(c1)C[C@@]1(OCCCc3ccccc3)[C@H]3Cc4ccc(O)c5c4[C@@]1(CCN3CC1CC1)[C@H]2O5	10.1021/acs.jmedchem.0c00503
	CHEMBL4649485	178197	0	None	-19	2	Human	6.6	pEC50	=	6.6	Functional	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)c1ccccc1-c1cnc2c(c1)C[C@@]1(OCCCc3ccccc3)[C@H]3Cc4ccc(O)c5c4[C@@]1(CCN3CC1CC1)[C@H]2O5	10.1021/acs.jmedchem.0c00503
	CHEMBL5082892	214830	0	None	-2	5	Human	6.6	pEC50	=	6.6	Functional	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)CNC(=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
	90656667	110962	0	None	-1	3	Human	6.6	pEC50	=	6.6	Functional	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	479	5	2	5	4.6	CC[C@](O)([C@H]1C[C@@]23C=C[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5)C(C)(C)C	10.1021/jm401964y
	CHEMBL3262362	110962	0	None	-1	3	Human	6.6	pEC50	=	6.6	Functional	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	479	5	2	5	4.6	CC[C@](O)([C@H]1C[C@@]23C=C[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5)C(C)(C)C	10.1021/jm401964y
	CHEMBL5082892	214830	0	None	-2	5	Human	6.6	pEC50	=	6.6	Functional	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)CNC(=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
	44301524	202693	23	None	1	5	Human	6.6	pEC50	=	6.6	Functional	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	414	5	1	7	2.8	CC[C@@H]1CN2CC[C@@]3(O)C(=Nc4cccc(OC)c43)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.1c01273
	CHEMBL61630	202693	23	None	1	5	Human	6.6	pEC50	=	6.6	Functional	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	414	5	1	7	2.8	CC[C@@H]1CN2CC[C@@]3(O)C(=Nc4cccc(OC)c43)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC	10.1021/acs.jmedchem.1c01273
	44408483	168929	0	None	-14	5	Rat	6.6	pEC50	=	6.6	Functional	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	3.7	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)OC2C3CC4CC(C3)CC2C4)c2ccccc12)C(=O)O	10.1021/jm050851n
	CHEMBL438739	168929	0	None	-14	5	Rat	6.6	pEC50	=	6.6	Functional	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	3.7	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)OC2C3CC4CC(C3)CC2C4)c2ccccc12)C(=O)O	10.1021/jm050851n
	44570066	189272	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	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	258	1	1	2	1.9	CC1C2Cc3ccc(C(N)=O)cc3C1(C)CCN2C	10.1016/j.bmcl.2008.10.134
	CHEMBL511884	189272	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	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	258	1	1	2	1.9	CC1C2Cc3ccc(C(N)=O)cc3C1(C)CCN2C	10.1016/j.bmcl.2008.10.134
	CHEMBL5083736	214880	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	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)c1ncccc1F	10.1021/acs.jmedchem.1c00417
	118560963	181712	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	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(CCc3ccccc3F)CC2)O[C@H](C)C1=O	10.1021/acs.jmedchem.0c01127
	CHEMBL4776924	181712	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	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(CCc3ccccc3F)CC2)O[C@H](C)C1=O	10.1021/acs.jmedchem.0c01127
	16048940	167776	0	None	-13	2	Human	7.6	pEC50	=	7.6	Functional	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	466	7	1	2	6.1	C[C@H]1C2Cc3ccc(C(=O)NCCCc4ccc5ccccc5c4)cc3[C@@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2007.09.082
	CHEMBL430397	167776	0	None	-13	2	Human	7.6	pEC50	=	7.6	Functional	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	466	7	1	2	6.1	C[C@H]1C2Cc3ccc(C(=O)NCCCc4ccc5ccccc5c4)cc3[C@@]1(C)CCN2CC1CC1	10.1016/j.bmcl.2007.09.082
	23635166	168970	0	None	1	3	Rat	7.6	pEC50	=	7.6	Functional	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	784	17	7	9	1.0	CCC(=O)N(c1ccccc1)C1CCN(C(=O)CCC(=O)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC1	10.1021/jm061465o
	CHEMBL439026	168970	0	None	1	3	Rat	7.6	pEC50	=	7.6	Functional	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	784	17	7	9	1.0	CCC(=O)N(c1ccccc1)C1CCN(C(=O)CCC(=O)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC1	10.1021/jm061465o
	156014399	177180	0	None	2	2	Human	7.6	pEC50	=	7.6	Functional	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	9	1	5	7.2	Oc1ccc2c3c1O[C@H]1c4ncc(-c5ccccc5)cc4C[C@@]4(OCCCCc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/acs.jmedchem.0c00503
	CHEMBL4634862	177180	0	None	2	2	Human	7.6	pEC50	=	7.6	Functional	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	9	1	5	7.2	Oc1ccc2c3c1O[C@H]1c4ncc(-c5ccccc5)cc4C[C@@]4(OCCCCc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314	10.1021/acs.jmedchem.0c00503
	51353744	61229	0	None	-2	2	Human	6.6	pEC50	=	6.6	Functional	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	387	5	1	4	5.1	CCNc1nc2cc3c(cc2s1)C[C@@H]1[C@@H]2CCCC[C@]32CCN1CCCF	10.1021/jm101542c
	CHEMBL1766043	61229	0	None	-2	2	Human	6.6	pEC50	=	6.6	Functional	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	387	5	1	4	5.1	CCNc1nc2cc3c(cc2s1)C[C@@H]1[C@@H]2CCCC[C@]32CCN1CCCF	10.1021/jm101542c
	44408483	168929	0	None	-14	5	Rat	6.6	pEC50	=	6.6	Functional	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	3.7	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)OC2C3CC4CC(C3)CC2C4)c2ccccc12)C(=O)O	10.1021/jm050851n
	CHEMBL438739	168929	0	None	-14	5	Rat	6.6	pEC50	=	6.6	Functional	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	3.7	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)OC2C3CC4CC(C3)CC2C4)c2ccccc12)C(=O)O	10.1021/jm050851n
	118725741	117151	0	None	-72	3	Human	5.6	pEC50	=	5.6	Functional	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	352	5	1	4	3.5	O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1ccc(F)cc1	10.1016/j.bmcl.2014.12.064
	CHEMBL3393881	117151	0	None	-72	3	Human	5.6	pEC50	=	5.6	Functional	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	352	5	1	4	3.5	O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1ccc(F)cc1	10.1016/j.bmcl.2014.12.064
	46632087	164745	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	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	321	3	1	3	3.5	Cc1ccc(CN2CCC(n3c(=O)[nH]c4ccccc43)CC2)cc1	10.1021/acs.jmedchem.8b01136
	CHEMBL4217675	164745	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	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	321	3	1	3	3.5	Cc1ccc(CN2CCC(n3c(=O)[nH]c4ccccc43)CC2)cc1	10.1021/acs.jmedchem.8b01136
	13149	2545	36	None	8	4	Human	6.6	pEC50	=	6.6	Functional	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	36	None	8	4	Human	6.6	pEC50	=	6.6	Functional	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	36	None	8	4	Human	6.6	pEC50	=	6.6	Functional	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
	16192289	38447	1	None	15	2	Human	5.6	pEC50	=	5.6	Functional	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	389	6	1	5	4.6	Cc1ccc(-n2cc(CNC(C)c3cnn(C)c3)c(-c3ccc(F)cc3)n2)cc1	nan
	CHEMBL1463894	38447	1	None	15	2	Human	5.6	pEC50	=	5.6	Functional	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	389	6	1	5	4.6	Cc1ccc(-n2cc(CNC(C)c3cnn(C)c3)c(-c3ccc(F)cc3)n2)cc1	nan
	23723457	54826	40	None	1	2	Human	4.6	pEC50	=	4.6	Functional	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	408	8	1	4	4.4	CCOC(=O)C1(CCc2ccccc2)CCN(Cc2ccc(NC(C)=O)cc2)CC1	nan
	CHEMBL1612697	54826	40	None	1	2	Human	4.6	pEC50	=	4.6	Functional	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	408	8	1	4	4.4	CCOC(=O)C1(CCc2ccccc2)CCN(Cc2ccc(NC(C)=O)cc2)CC1	nan
	9838803	31113	15	None	-2	2	Rat	6.6	pEC50	=	6.6	Functional	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	249	3	2	3	2.3	CN(C)C[C@H]1CCCC[C@]1(O)c1cccc(O)c1	10.1016/j.ejmech.2020.112070
	CHEMBL1400	31113	15	None	-2	2	Rat	6.6	pEC50	=	6.6	Functional	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	249	3	2	3	2.3	CN(C)C[C@H]1CCCC[C@]1(O)c1cccc(O)c1	10.1016/j.ejmech.2020.112070
	CHEMBL201556	31113	15	None	-2	2	Rat	6.6	pEC50	=	6.6	Functional	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	249	3	2	3	2.3	CN(C)C[C@H]1CCCC[C@]1(O)c1cccc(O)c1	10.1016/j.ejmech.2020.112070
	9932852	123171	0	None	-128	3	Human	5.6	pEC50	=	5.6	Functional	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	438	5	3	4	4.0	N[C@@H](Cc1ccc(O)cc1)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1	10.1016/j.bmcl.2012.05.042
	CHEMBL361274	123171	0	None	-128	3	Human	5.6	pEC50	=	5.6	Functional	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	438	5	3	4	4.0	N[C@@H](Cc1ccc(O)cc1)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1	10.1016/j.bmcl.2012.05.042
	162669476	182742	0	None	3	3	Human	6.6	pEC50	=	6.6	Functional	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	1055	29	14	13	-3.2	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C)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
	CHEMBL4790011	182742	0	None	3	3	Human	6.6	pEC50	=	6.6	Functional	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	1055	29	14	13	-3.2	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C)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
	71761637	91400	0	None	-	1	Rat	5.6	pEC50	=	5.6	Functional	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	91400	0	None	-	1	Rat	5.6	pEC50	=	5.6	Functional	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
	4897494	51339	10	None	-	1	Human	4.6	pEC50	=	4.6	Functional	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	418	4	1	6	5.0	Cn1c(-c2c(N)n(CCc3ccccc3)c3nc4ccccc4nc23)nc2ccccc21	nan
	CHEMBL1581275	51339	10	None	-	1	Human	4.6	pEC50	=	4.6	Functional	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	418	4	1	6	5.0	Cn1c(-c2c(N)n(CCc3ccccc3)c3nc4ccccc4nc23)nc2ccccc21	nan
	CHEMBL267211	210714	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	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		NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1	10.1021/jm060998u
	162669476	182742	0	None	3	3	Human	6.6	pEC50	=	6.6	Functional	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	1055	29	14	13	-3.2	C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C)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

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Ligand source activities (1 row/activity)