Protein Information

General Information of the Protein

Protein ID	PT01200
Protein Name	Delta-type opioid receptor
Gene Name	OPRD1
Secondarily Gene Name	OPRD
Sequence	MEPAPSAGAELQPPLFANASDAYPSACPSAGANASGPPGARSASSLALAIAITALYSAVCAVGLLGNVLVMFGIVRYTKMKTATNIYIFNLALADALATSTLPFQSAKYLMETWPFGELLCKAVLSIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPAKAKLINICIWVLASGVGVPIMVMAVTRPRDGAVVCMLQFPSPSWYWDTVTKICVFLFAFVVPILIITVCYGLMLLRLRSVRLLSGSKEKDRSLRRITRMVLVVVGAFVVCWAPIHIFVIVWTLVDIDRRDPLVVAALHLCIALGYANSSLNPVLYAFLDENFKRCFRQLCRKPCGRPDPSSFSRAREATARERVTACTPSDGPGGGAAA Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Membrane receptor > Family A G protein-coupled receptor > Peptide receptor (family A GPCR) > Short peptide receptor (family A GPCR) > Opioid receptor
Function	G-protein coupled receptor that functions as a receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Plays a role in the perception of pain and in opiate-mediated analgesia. Plays a role in developing analgesic tolerance to morphine. Show/Hide
Uniprot ID	Primary ID: P41143 Secondarily ID: B5B0B8 Show/Hide
Ensembl ID	ENSG00000116329
HGNC ID	HGNC:8153
Subcellular Location	Cell membrane

Map of Molecular Bioactivity Related to the Protein

Map of Molecular Bioactivity Related to the Protein Protein Cell Line Compound Bioactivity Value: <= 0.1 μM > 0.1 μM and <= 10 μM > 10 μM Imprecise Activity

Table of Molecular Bioactivities Related to the Protein

Cell Line ID: CL000047 , 108CC15

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0423575 Compound Info	(1S,2S,10R,18R)-6-(4-chlorophenyl)-19-methyl-2-(3-phenylpropoxy)-11-oxa-8,19-diazahexacyclo[10.9.1.01,10.02,18.04,9.016,22]docosa-4(9),5,7,12,14,16(22)-hexaen-13-ol Show/Hide	C35H33ClN2O3	1
1	EC50 = 0.27 nM Bioactivity Info	TI LI LO TS
CP0435974 Compound Info	(1S,2S,10R,18R)-6-(4-chlorophenyl)-19-methyl-2-[(E)-3-phenylprop-2-enoxy]-11-oxa-8,19-diazahexacyclo[10.9.1.01,10.02,18.04,9.016,22]docosa-4(9),5,7,12,14,16(22)-hexaen-13-ol Show/Hide	C35H31ClN2O3	1
1	EC50 = 0.59 nM Bioactivity Info	TI LI LO TS
CP0397495 Compound Info	[(1S,2S,10R,18R)-6-(4-chlorophenyl)-13-hydroxy-19-methyl-11-oxa-8,19-diazahexacyclo[10.9.1.01,10.02,18.04,9.016,22]docosa-4(9),5,7,12,14,16(22)-hexaen-2-yl] 3-phenylpropanoate Show/Hide	C35H31ClN2O4	1
1	EC50 = 5.52 nM Bioactivity Info	TI LI LO TS
CP0423581 Compound Info	(1S,2S,10R,18R)-6-(4-chlorophenyl)-19-methyl-2-phenylmethoxy-11-oxa-8,19-diazahexacyclo[10.9.1.01,10.02,18.04,9.016,22]docosa-4(9),5,7,12,14,16(22)-hexaen-13-ol Show/Hide	C33H29ClN2O3	1
1	EC50 = 11 nM Bioactivity Info	TI LI LO TS
CP0446113 Compound Info	[(1S,2S,10R,18R)-6-(4-chlorophenyl)-13-hydroxy-19-methyl-11-oxa-8,19-diazahexacyclo[10.9.1.01,10.02,18.04,9.016,22]docosa-4(9),5,7,12,14,16(22)-hexaen-2-yl] 2-phenylacetate Show/Hide	C34H29ClN2O4	1
1	EC50 = 19 nM Bioactivity Info	TI LI LO TS
CP0489358 Compound Info	4-[(R)-((2S,5R)-4-Allyl-2,5-dimethyl-piperazin-1-yl)-(3-methoxy-phenyl)-methyl]-N-ethyl-benzamide Show/Hide	C26H35N3O2	1
1	ED50 = 55 nM Bioactivity Info	TI LI LO TS
CP0380730 Compound Info	(4aS,9aR)-2-[2-(4-fluorophenyl)ethyl]-4a-(2-phenylethyl)-1,3,4,9a-tetrahydro-[1]benzofuro[2,3-c]pyridin-6-ol Show/Hide	C27H28FNO2	1
1	ED50 = 350 nM Bioactivity Info	TI LI LO TS
CP0375137 Compound Info	(4aS,9aR)-2,4a-bis(2-phenylethyl)-1,3,4,9a-tetrahydro-[1]benzofuro[2,3-c]pyridin-6-ol Show/Hide	C27H29NO2	1
1	ED50 = 395 nM Bioactivity Info	TI LI LO TS
CP0432350 Compound Info	(4aS,9aR)-4a-(2-phenylethyl)-2-[2-[4-(trifluoromethyl)phenyl]ethyl]-1,3,4,9a-tetrahydro-[1]benzofuro[2,3-c]pyridin-6-ol Show/Hide	C28H28F3NO2	1
1	ED50 = 1250 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000901 , 661W

Cell Line Info

Cell Line ID: CL000049 , C6

Cell Line Info

Cell Line ID: CL000064 , Chem-1

Cell Line Info

Cell Line ID: CL000011 , CHO

Cell Line Info

Cell Line ID: CL001010 , CHO-hgamma

Cell Line Info

Cell Line ID: CL000026 , CHO-K1

Cell Line Info

Cell Line ID: CL000109 , COS-1

Cell Line Info

Cell Line ID: CL000053 , COS-7

Cell Line Info

Cell Line ID: CL000386 , Flp-In-CHO

Cell Line Info

Cell Line ID: CL000025 , HEK-293T

Cell Line Info

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000107 , HEK293S

Cell Line Info

Cell Line ID: CL000661 , HN9.10e

Cell Line Info

Cell Line ID: CL000004 , SH-SY5Y

Cell Line Info

Cell Line ID: CL000043 , U2OS

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0040319 Compound Info	4-((R)-((2S,5R)-4-allyl-2,5-dimethylpiperazin-1-yl)(3-hydroxyphenyl)methyl)-N,N-diethylbenzamide Show/Hide	C27H37N3O2	2
1	EC50 = 0.12 nM
2	IC50 = 0.23 nM
CP0045380 Compound Info	(2S)-2-amino-N-[(1R)-1-[({[(1S)-1-{N'-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-phenylpropanoyl]hydrazinecarbonyl}-2-phenylethyl]carbamoyl}methyl)carbamoyl]ethyl]-3-(4-hydroxyphenyl)propanamide Show/Hide	C46H56N10O10	4
1	EC50 = 1 nM
2	IC50 = 2.6 nM
3	Ki = 2.6 nM
4	Ki = 4.6 nM
CP0041255 Compound Info	(+)-4-((alpha R)-((2S,5R)-4-allyl-2,5-dimethylpiperazin-1-yl)(3-methoxyphenyl)methyl)-N,N-diethylbenzamide Show/Hide	C28H39N3O2	7
1	EC50 = 3.67 nM
2	IC50 = 1.3 nM
3	IC50 = 1.31 nM
4	IC50 = 2.85 nM
5	IC50 = 49.1 nM
6	Ki = 1.29 nM
7	Ki = 1.7 nM
CP0042565 Compound Info	(S)-3-((S)-2-{(R)-2-[(S)-2-Amino-3-(4-hydroxy-phenyl)-propionylamino]-propionylamino}-3-phenyl-propionylamino)-N-{(S)-1-[(S)-1-(carbamoylmethyl-carbamoyl)-2-methyl-propylcarbamoyl]-2-methyl-propyl}-succinamic acid Show/Hide	C37H52N8O10	2
1	EC50 = 4.71 nM
2	IC50 = 1.3 nM
CP0185172 Compound Info	4-[(4-Allyl-piperazin-1-yl)-phenyl-methyl]-N,N-diethyl-benzamide Show/Hide	C25H33N3O	2
1	EC50 = 33 nM
2	IC50 = 15.9 nM
CP0106490 Compound Info	N,N-diethyl-4-[phenyl(piperazin-1-yl)methyl]benzamide Show/Hide	C22H29N3O	2
1	EC50 = 36.5 nM
2	IC50 = 11.3 nM
CP0082474 Compound Info	N,N-diethyl-4-[phenyl(piperidin-4-yl)methyl]benzamide Show/Hide	C23H30N2O	2
1	EC50 = 121 nM
2	IC50 = 8.76 nM
CP0100342 Compound Info	(S)-2-amino-3-(4-hydroxy-phenyl)-N-((R)-1-{[((S)-1-{2-[(1-phenethyl-piperidin-4-yl)-phenyl-carbamoyl]-ethylcarbamoyl}-2-phenyl-ethylcarbamoyl)-methyl]-carbamoyl}-ethyl)-propionamide Show/Hide	C45H55N7O6	1
1	IC50 = 0.99 nM
CP0233356 Compound Info	(S)-1-((2S,5S,11R,14S)-14-amino-5-benzyl-15-(4-hydroxyphenyl)-11-methyl-2-(2-(methylthio)ethyl)-4,7,10,13-tetraoxo-3,6,9,12-tetraazapentadecane)-N-((S)-1-((S)-1-(3,5-bis(trifluoromethyl)benzylamino)-3-(1H-indol-3-yl)-1-oxopropan-2-ylamino)-4-methyl-1-oxopentan-2-yl)pyrrolidine-2-carboxamide Show/Hide	C59H70F6N10O9S	2
1	IC50 = 1.445 nM
2	Ki = 0.66 nM
CP0038418 Compound Info	13-[2-Amino-3-(4-hydroxy-phenyl)-propionylamino]-7-benzyl-3,3,14,14-tetramethyl-6,9,12-trioxo-1,2-dithia-5,8,11-triaza-cyclotetradecane-4-carboxylic acid Show/Hide	C30H39N5O7S2	6
1	IC50 = 1.8 nM
2	IC50 = 3.5 nM
3	IC50 = 10 nM
4	Ki = 0.5 nM
5	Ki = 2.2 nM
6	Ki = 2.9 nM
CP0088491 Compound Info	(2S)-1-[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]propanoyl]amino]acetyl]amino]-3-phenylpropanoyl]-N-[(2S)-1-[[(2S)-1-[[3,5-bis(trifluoromethyl)phenyl]methylamino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide Show/Hide	C56H65F6N9O8	2
1	IC50 = 2.188 nM
2	Ki = 1 nM
CP0072632 Compound Info	CAS_5985-38-6 Show/Hide	C17H23NO	1
1	IC50 = 2.9 nM
CP0048724 Compound Info	(4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-bis(oxidanyl)-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7-one;hydrochloride Show/Hide	C20H23NO4	4
1	IC50 = 10 nM
2	Ki = 10.8 nM
3	Ki = 11 nM
4	Ki = 95.46 nM
CP0076733 Compound Info	(2S)-1-[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]propanoyl]amino]acetyl]-methylamino]-3-phenylpropanoyl]-N-[(2S)-1-[[(2S)-1-[[3,5-bis(trifluoromethyl)phenyl]methylamino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide Show/Hide	C57H67F6N9O8	2
1	IC50 = 12.02 nM
2	Ki = 5 nM
CP0290016 Compound Info	(4R,4aS,7S,7aR,12bS)-3-(cyclopropylmethyl)-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinoline-4a,7,9-triol Show/Hide	C20H25NO4	1
1	IC50 = 32 nM
CP0206724 Compound Info	(2S)-1-[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]propanoyl]amino]acetyl]amino]-3-(4-fluorophenyl)propanoyl]-N-[(2S)-1-[[(2S)-1-[[3,5-bis(trifluoromethyl)phenyl]methylamino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide Show/Hide	C56H64F7N9O8	2
1	IC50 = 66.07 nM
2	Ki = 1 nM
CP0038839 Compound Info	(4R,4aS,7aR,12bS)-3-allyl-4a,9-dihydroxy-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7-one;hydrochloride Show/Hide	C19H21NO4	4
1	IC50 = 151 nM
2	Ki = 15.85 nM
3	Ki = 33 nM
4	Ki = 42.6 nM
CP0043850 Compound Info	(2S)-2-{[(2S)-1-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-phenylpropanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-({[3,5-bis(trifluoromethyl)phenyl]methyl}carbamoyl)-2-(1H-indol-3-yl)ethyl]-4-methylpentanamide Show/Hide	C54H61F6N9O8	2
1	IC50 = 158.49 nM
2	Ki = 72 nM
CP0146697 Compound Info	(S)-1-[(S)-2-[2-((S)-2-{(R)-2-[(S)-2-Amino-3-(4-hydroxy-phenyl)-propionylamino]-propionylamino}-3-phenyl-propionylamino)-acetylamino]-3-(4-hydroxy-phenyl)-propionyl]-pyrrolidine-2-carboxylic acid ((S)-1-carbamoyl-2-hydroxy-ethyl)-amide Show/Hide	C40H50N8O10	2
1	IC50 = 295 nM
2	Ki = 929 nM
CP0069870 Compound Info	17-cyclobutylmethyl-4,5alpha-epoxymorphinan-3,6alpha,14-triol Show/Hide	C21H27NO4	2
1	IC50 = 353 nM
2	Ki = 318.85 nM
CP0120551 Compound Info	(2S)-N-[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]-1-[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]-3-phenylpropanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carboxamide Show/Hide	C40H50N8O10	2
1	IC50 = 1247 nM
2	Ki > 40000 nM
CP0387607 Compound Info	(3S,6S,9S,12R)-3,9-dibenzyl-6-(1H-indol-3-ylmethyl)-1,4,7,10-tetrazabicyclo[10.3.0]pentadecane-2,5,8,11-tetrone Show/Hide	C34H35N5O4	1
1	IC50 = 2600 nM
CP0035617 Compound Info	N-methyl-2-phenyl-N-[(5R,7S,8S)-7-(pyrrolidin-1-yl)-1-oxaspiro[4.5]decan-8-yl]acetamide Show/Hide	C22H32N2O2	4
1	IC50 = 4970 nM
2	IC50 = 5844 nM
3	Ki > 1000 nM
4	Ki > 10000 nM
CP0042160 Compound Info	2-acetylamino-N-{2-[(1-phenethyl-piperidin-4-yl)-phenyl-carbamoyl]-ethyl}-3-phenyl-propionamide Show/Hide	C33H40N4O3	1
1	IC50 = 7600 nM
CP0435259 Compound Info	3-{phenyl[1-(2-phenylethyl)piperidin-4-yl]carbamoyl}propanoic acid Show/Hide	C23H28N2O3	1
1	IC50 = 9400 nM
CP0164874 Compound Info	3-Phenyl-1-(1-phenyl-2-pyrrolidin-1-yl-ethyl)-1H-pyridin-2-one Show/Hide	C23H24N2O	1
1	IC50 > 10000 nM
CP0164875 Compound Info	1-(1-Phenyl-2-pyrrolidin-1-yl-ethyl)-3-(4-trifluoromethyl-phenyl)-1H-pyridin-2-one Show/Hide	C24H23F3N2O	1
1	IC50 > 10000 nM
CP0095588 Compound Info	4-[(8-Benzo[1,3]dioxol-5-ylmethyl-8-aza-bicyclo[3.2.1]oct-3-ylidene)-phenyl-methyl]-N,N-diethyl-benzamide Show/Hide	C33H36N2O3	1
1	Ki = 0.01 nM
CP0120549 Compound Info	(3R)-2-[(2S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]-N-(1H-benzimidazol-2-ylmethyl)-3,4-dihydro-1H-isoquinoline-3-carboxamide Show/Hide	C29H31N5O3	1
1	Ki = 0.021 nM
CP0301886 Compound Info	4-[(R)-(S)-8-Aza-bicyclo[3.2.1]oct-(3Z)-ylidene-phenyl-methyl]-N,N-diethyl-benzamide Show/Hide	C25H30N2O	1
1	Ki = 0.023 nM
CP0078171 Compound Info	4-{[(1S,5R)-8-Allyl-8-aza-bicyclo[3.2.1]oct-(3Z)-ylidene]-phenyl-methyl}-N,N-diethyl-benzamide Show/Hide	C28H34N2O	1
1	Ki = 0.025 nM
CP0050068 Compound Info	(1S,2S,13R,21R)-22-(cyclopropylmethyl)-14-oxa-11,22-diazaheptacyclo[13.9.1.01,13.02,21.04,12.05,10.019,25]pentacosa-4(12),5,7,9,15,17,19(25)-heptaene-2,16-diol Show/Hide	C26H26N2O3	8
1	Ki = 0.062 nM
2	Ki = 0.07 nM
3	Ki = 0.15 nM
4	Ki = 0.16 nM
5	Ki = 0.22 nM
6	Ki = 0.24 nM
7	Ki = 0.9 nM
8	Ki = 2.53 nM
CP0220585 Compound Info	(E)-N-[(4R,4aS,7aR,12bR)-3-methyl-7-oxo-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-4a-yl]-3-(2-chlorophenyl)prop-2-enamide Show/Hide	C26H25ClN2O3	1
1	Ki = 0.08 nM
CP0235768 Compound Info	(3R)-2-[(2S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]-N-[2-(benzylamino)-2-oxoethyl]-3,4-dihydro-1H-isoquinoline-3-carboxamide Show/Hide	C30H34N4O4	1
1	Ki = 0.16 nM
CP0166197 Compound Info	N,N-diethyl-4-[phenyl-[(1S,5R)-8-(2-phenylethyl)-8-azabicyclo[3.2.1]octan-3-ylidene]methyl]benzamide Show/Hide	C33H38N2O	1
1	Ki = 0.24 nM
CP0101868 Compound Info	4-((R)-(S)-8-Aza-bicyclo[3.2.1]oct-3-yl-phenyl-amino)-N,N-diethyl-benzamide Show/Hide	C24H31N3O	1
1	Ki = 0.3 nM
CP0286968 Compound Info	4-{[(1R,5S)-8-Allyl-8-aza-bicyclo[3.2.1]oct-(3E)-ylidene]-phenyl-methyl}-N,N-diethyl-benzamide Show/Hide	C28H34N2O	1
1	Ki = 0.32 nM
CP0141598 Compound Info	4-[(S)-(R)-8-Aza-bicyclo[3.2.1]oct-(3E)-ylidene-phenyl-methyl]-N,N-diethyl-benzamide Show/Hide	C25H30N2O	1
1	Ki = 0.36 nM
CP0192615 Compound Info	N,N-diethyl-4-[[8-(2-phenoxyethyl)-8-azabicyclo[3.2.1]octan-3-ylidene]-phenylmethyl]benzamide Show/Hide	C33H38N2O2	1
1	Ki = 0.38 nM
CP0275440 Compound Info	N,N-diethyl-4-[phenyl-(8-propyl-8-azabicyclo[3.2.1]octan-3-ylidene)methyl]benzamide Show/Hide	C28H36N2O	1
1	Ki = 0.39 nM
CP0161130 Compound Info	4-[((1S,5R)-8-Allyl-8-aza-bicyclo[3.2.1]oct-3-yl)-phenyl-amino]-N,N-diethyl-benzamide Show/Hide	C27H35N3O	1
1	Ki = 0.5 nM
CP0347116 Compound Info	3-Cyclopropylmethyl-6,11-dimethyl-1,2,3,4,5,6-hexahydro-2,6-methano-benzo[d]azocine-8-carboxylic acid amide Show/Hide	C19H26N2O	1
1	Ki = 0.53 nM
CP0213756 Compound Info	N,N-diethyl-4-[phenyl-[8-(3-phenylpropyl)-8-azabicyclo[3.2.1]octan-3-ylidene]methyl]benzamide Show/Hide	C34H40N2O	1
1	Ki = 0.56 nM
CP0252887 Compound Info	4-[(8-Aza-bicyclo[3.2.1]oct-3-ylidene)-(4-hydroxy-phenyl)-methyl]-N,N-diethyl-benzamide Show/Hide	C25H30N2O2	1
1	Ki = 0.58 nM
CP0179632 Compound Info	N,N-diethyl-4-[(3-hydroxyphenyl)-(8-methyl-8-azabicyclo[3.2.1]octan-3-ylidene)methyl]benzamide Show/Hide	C26H32N2O2	1
1	Ki = 0.6 nM
CP0233352 Compound Info	(2S)-2-[[(2S)-2-[[2-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-4-methylsulfanylbutanamide Show/Hide	C28H38N6O6S	1
1	Ki = 0.66 nM
CP0041235 Compound Info	22-methyl-(2S,13R)-14-oxa-11,22-diazaheptacyclo[13.9.1.01,13.02,21.04,12.05,10.019,25]pentacosa-4(12),5(10),6,8,15(25),16,18-heptaene-2,16-diol(HCl0.5H2O) (Oxymorphindole, OMI) Show/Hide	C23H22N2O3	1
1	Ki = 0.9 nM
CP0112062 Compound Info	(2R,6R,11R)-3-Cyclopropylmethyl-6,11-dimethyl-1,2,3,4,5,6-hexahydro-2,6-methano-benzo[d]azocin-8-ol Show/Hide	C18H25NO	1
1	Ki = 1.1 nM
CP0233344 Compound Info	(-)-3-Hydroxy-N-cyclobutylmethylmorphinan S(+)-Mandelate Show/Hide	C21H29NO	1
1	Ki = 1.3 nM
CP0042484 Compound Info	N,N-diethyl-4-[(3-methoxyphenyl)-[8-(2-phenylethyl)-8-azabicyclo[3.2.1]octan-3-ylidene]methyl]benzamide Show/Hide	C34H40N2O2	1
1	Ki = 1.36 nM
CP0286049 Compound Info	4-{[8-(2-Cyclohexyl-ethyl)-8-aza-bicyclo[3.2.1]oct-3-ylidene]-phenyl-methyl}-N,N-diethyl-benzamide Show/Hide	C33H44N2O	1
1	Ki = 1.36 nM
CP0265889 Compound Info	N,N-diethyl-4-[(4-hydroxyphenyl)-(8-methyl-8-azabicyclo[3.2.1]octan-3-ylidene)methyl]benzamide Show/Hide	C26H32N2O2	1
1	Ki = 1.89 nM
CP0134169 Compound Info	(3S)-3-[(2S)-2-[(2R)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-(1H-indol-3-yl)-N-methylpropanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid Show/Hide	C45H57N9O10	1
1	Ki = 1.9 nM
CP0060012 Compound Info	(S)-2-[(S)-2-(2-{2-[(S)-2-Amino-3-(4-hydroxy-phenyl)-propionylamino]-acetylamino}-acetylamino)-3-phenyl-propionylamino]-4-methylsulfanyl-butyric acid Show/Hide	C27H35N5O7S	1
1	Ki = 2 nM
CP0255370 Compound Info	N,N-diethyl-4-[[8-[2-(4-fluorophenyl)ethyl]-8-azabicyclo[3.2.1]octan-3-ylidene]-phenylmethyl]benzamide Show/Hide	C33H37FN2O	1
1	Ki = 2.62 nM
CP0253252 Compound Info	N-ethyl-N-(2-methylprop-2-enyl)-4-[phenyl-[(1R,5S)-8-(2-phenylethyl)-8-azabicyclo[3.2.1]octan-3-ylidene]methyl]benzamide Show/Hide	C35H40N2O	1
1	Ki = 2.94 nM
CP0216238 Compound Info	(4S,7S,13S)-13-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]-7-benzyl-3,3,14,14-tetramethyl-6,9,12-trioxo-1,2-dithia-5,8,11-triazacyclotetradecane-4-carboxylic acid Show/Hide	C30H39N5O7S2	1
1	Ki = 3.2 nM
CP0095589 Compound Info	N-ethyl-N-(2-hydroxyethyl)-4-[phenyl-[8-(2-phenylethyl)-8-azabicyclo[3.2.1]octan-3-ylidene]methyl]benzamide Show/Hide	C33H38N2O2	1
1	Ki = 3.2 nM
CP0050359 Compound Info	4-(1-benzyl-1H-imidazol-2-yl)-N,4-diphenylpiperidine-1-sulfonamide Show/Hide	C27H28N4O2S	1
1	Ki = 3.2 nM
CP0186242 Compound Info	N,N-diethyl-4-[[8-[2-(1H-indol-3-yl)ethyl]-8-azabicyclo[3.2.1]octan-3-ylidene]-phenylmethyl]benzamide Show/Hide	C35H39N3O	1
1	Ki = 3.48 nM
CP0190938 Compound Info	N,N-diethyl-4-[(4-methoxyphenyl)-(8-methyl-8-azabicyclo[3.2.1]octan-3-ylidene)methyl]benzamide Show/Hide	C27H34N2O2	1
1	Ki = 3.5 nM
CP0100815 Compound Info	N,N-diethyl-4-[[(1S,5R)-8-methyl-8-azabicyclo[3.2.1]octan-3-ylidene]-phenylmethyl]benzamide Show/Hide	C26H32N2O	1
1	Ki = 4.5 nM
CP0072627 Compound Info	BUPRENORPHINE Show/Hide	C29H41NO4	1
1	Ki = 4.5 nM
CP0041449 Compound Info	C18130 Show/Hide	C40H43N3O6	2
1	Ki = 5.7 nM
2	Ki = 43 nM
CP0161795 Compound Info	N,N-diethyl-4-[[(1S,5R)-8-methyl-8-azabicyclo[3.2.1]octan-3-ylidene]-phenylmethyl]benzamide Show/Hide	C26H32N2O	1
1	Ki = 5.7 nM
CP0286113 Compound Info	N,N-diethyl-4-[(3-methoxyphenyl)-(8-methyl-8-azabicyclo[3.2.1]octan-3-ylidene)methyl]benzamide Show/Hide	C27H34N2O2	1
1	Ki = 5.9 nM
CP0106086 Compound Info	N,N-diethyl-4-[(8-phenacyl-8-azabicyclo[3.2.1]octan-3-ylidene)-phenylmethyl]benzamide Show/Hide	C33H36N2O2	1
1	Ki = 6.31 nM
CP0088373 Compound Info	(S)-2-[(S)-2-(2-{2-[(S)-2-Amino-3-(4-hydroxy-phenyl)-propionylamino]-acetylamino}-acetylamino)-3-phenyl-propionylamino]-4-methyl-pentanoic acid Show/Hide	C28H37N5O7	2
1	Ki = 6.9 nM
2	Ki = 31 nM
CP0184830 Compound Info	4-[(8-Phenethyl-8-aza-bicyclo[3.2.1]oct-3-ylidene)-phenyl-methyl]-N,N-dipropyl-benzamide Show/Hide	C35H42N2O	1
1	Ki = 7.39 nM
CP0076649 Compound Info	(6S,11R)-3-Cyclopropylmethyl-6,11-dimethyl-1,2,3,4,5,6-hexahydro-2,6-methano-benzo[d]azocine-8-carboxylic acid amide Show/Hide	C19H26N2O	1
1	Ki = 8.3 nM
CP0254970 Compound Info	4-(1-benzyl-1H-imidazol-2-yl)-N-methyl-N,4-diphenylpiperidine-1-carboxamide Show/Hide	C29H30N4O	1
1	Ki = 9 nM
CP0150135 Compound Info	(6S,11R)-3-Cyclopropylmethyl-6-ethyl-11-methyl-1-oxo-1,2,3,4,5,6-hexahydro-2,6-methano-benzo[d]azocine-8-carboxylic acid amide Show/Hide	C20H26N2O2	1
1	Ki = 9.8 nM
CP0167293 Compound Info	7-Benzylidenenaltrexone Show/Hide	C27H27NO4	1
1	Ki = 10 nM
CP0139581 Compound Info	(2,6-dimethylpiperidin-1-yl)-[4-[phenyl-[(1S,5R)-8-(2-phenylethyl)-8-azabicyclo[3.2.1]octan-3-ylidene]methyl]phenyl]methanone Show/Hide	C36H42N2O	1
1	Ki = 10.97 nM
CP0013111 Compound Info	ADL 8-2698 Show/Hide	C25H32N2O4	1
1	Ki = 12 nM
CP0273257 Compound Info	N,N-diethyl-4-[phenyl-[8-(2-thiophen-2-ylethyl)-8-azabicyclo[3.2.1]octan-3-ylidene]methyl]benzamide Show/Hide	C31H36N2OS	1
1	Ki = 13.12 nM
CP0126886 Compound Info	(4R,4aS,7aR,12bR)-9-hydroxy-4a-methoxy-3,7a-dimethyl-1,2,4,5,6,13-hexahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-one Show/Hide	C19H23NO4	1
1	Ki = 13.3 nM
CP0088316 Compound Info	N,N-bis(2-methoxyethyl)-4-[phenyl-[8-(2-phenylethyl)-8-azabicyclo[3.2.1]octan-3-ylidene]methyl]benzamide Show/Hide	C35H42N2O3	1
1	Ki = 16.61 nM
CP0253934 Compound Info	2-(4-(1-benzyl-1H-imidazol-2-yl)-4-phenylpiperidin-1-yl)pyrimidine Show/Hide	C25H25N5	1
1	Ki = 18 nM
CP0049540 Compound Info	(S)-2-(3,4-Dichloro-phenyl)-N-methyl-N-(1-phenyl-2-pyrrolidin-1-yl-ethyl)-acetamide(ICI 199441) Show/Hide	C21H24Cl2N2O	1
1	Ki = 24 nM
CP0139907 Compound Info	4-[(1-Allyl-piperidin-4-yl)-phenyl-amino]-N,N-diethyl-benzamide Show/Hide	C25H33N3O	1
1	Ki = 24 nM
CP0077971 Compound Info	[4-[phenyl-[8-(2-phenylethyl)-8-azabicyclo[3.2.1]octan-3-ylidene]methyl]phenyl]-pyrrolidin-1-ylmethanone Show/Hide	C33H36N2O	1
1	Ki = 24.1 nM
CP0212090 Compound Info	((7R,8R,9alphaR)-8-(3-hydroxyphenyl)-7,8-dimethyl-hexahydro-1H-pyrido[1,2-R]pyrazin-2(6H)-yl)(phenyl)methanone Show/Hide	C23H28N2O2	1
1	Ki = 25 nM
CP0386984 Compound Info	3-[(1R,9R,13R)-4-hydroxy-1,13-dimethyl-10-azatricyclo[7.3.1.02,7]trideca-2(7),3,5-trien-10-yl]-N-phenylpropanamide Show/Hide	C23H28N2O2	1
1	Ki = 29 nM
CP0055374 Compound Info	(3R)-7-Hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide Show/Hide	C28H39N3O3	1
1	Ki = 29.6 nM
CP0148658 Compound Info	3-((2R,3R,7S,9-alpha-S)-2,3-dimethyl-7-phenyl-octahydro-1H-quinolizin-2-yl)phenol Show/Hide	C23H29NO	1
1	Ki = 30 nM
CP0264750 Compound Info	4-(1-benzyl-1H-imidazol-2-yl)-N-(2-methoxyphenyl)-4-phenylpiperidine-1-carboxamide Show/Hide	C29H30N4O2	1
1	Ki = 31 nM
CP0155719 Compound Info	(+)-N-phenethyl trans-3(R),4(R)-dimethyl-4-(3-hydroxyphenyl)piperidine Show/Hide	C21H27NO	1
1	Ki = 33 nM
CP0280402 Compound Info	N,N-diethyl-4-(N-piperidin-4-ylanilino)benzamide Show/Hide	C22H29N3O	1
1	Ki = 35 nM
CP0336036 Compound Info	morpholin-4-yl-[4-[phenyl-[8-(2-phenylethyl)-8-azabicyclo[3.2.1]octan-3-ylidene]methyl]phenyl]methanone Show/Hide	C33H36N2O2	1
1	Ki = 35.2 nM
CP0204147 Compound Info	3-((3S,7R,8R,9alphaR)-3-benzyl-7,8-dimethyl-octahydro-1H-pyrido[1,2-R]pyrazin-8-yl)phenol Show/Hide	C23H30N2O	1
1	Ki = 36 nM
CP0264747 Compound Info	4-(1-benzyl-1H-imidazol-2-yl)-N-ethyl-4-phenylpiperidine-1-carboxamide Show/Hide	C24H28N4O	1
1	Ki = 39 nM
CP0208449 Compound Info	N,N-diethyl-4-[phenyl-[(1S,5R)-8-(2-phenylethyl)-8-azabicyclo[3.2.1]octan-3-ylidene]methyl]benzamide Show/Hide	C33H38N2O	1
1	Ki = 42.1 nM
CP0153609 Compound Info	(2S)-2-[[(Z,2R)-5-[[2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]-2-benzyl-4-fluoropent-3-enoyl]amino]-4-methylpentanoic acid Show/Hide	C29H37FN4O6	1
1	Ki = 43 nM
CP0172248 Compound Info	4-(1-benzyl-1H-imidazol-2-yl)-N-(3-methoxyphenyl)-4-phenylpiperidine-1-carboxamide Show/Hide	C29H30N4O2	1
1	Ki = 46 nM
CP0217280 Compound Info	4-[phenyl-[8-(2-phenylethyl)-8-azabicyclo[3.2.1]octan-3-ylidene]methyl]-N,N-di(propan-2-yl)benzamide Show/Hide	C35H42N2O	1
1	Ki = 49.01 nM
CP0000305 Compound Info	(-)-(etorphine) Show/Hide	C17H19NO3	8
1	Ki = 51 nM
2	Ki = 113.3 nM
3	Ki = 132 nM
4	Ki = 140 nM
5	Ki = 150 nM
6	Ki = 280 nM
7	Ki = 299 nM
8	Ki = 456 nM
CP0254507 Compound Info	2-(4-(1-benzyl-1H-imidazol-2-yl)-4-phenylpiperidin-1-yl)benzo[d]thiazole Show/Hide	C28H26N4S	1
1	Ki = 73 nM
CP0146308 Compound Info	4-(1-benzyl-1H-imidazol-2-yl)-4-phenyl-1-(thiazol-2-yl)piperidine Show/Hide	C24H24N4S	1
1	Ki = 79 nM
CP0172246 Compound Info	4-phenyl-4-[1H-imidazol-2-yl]-piperidine Show/Hide	C28H28N4O	1
1	Ki = 81 nM
CP0107932 Compound Info	3-((3S,7R,8R,9alphaR)-7,8-dimethyl-3-phenyl-octahydro-1H-pyrido[1,2-R]pyrazin-8-yl)phenol Show/Hide	C22H28N2O	1
1	Ki = 88 nM
CP0063166 Compound Info	3-desoxy-3-carboxamidonaltrexone Show/Hide	C21H24N2O4	1
1	Ki = 110 nM
CP0285959 Compound Info	(3R)-7-hydroxy-N-[(2S)-1-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]-3-methylbutan-2-yl]-2-methyl-3,4-dihydro-1H-isoquinoline-3-carboxamide Show/Hide	C29H41N3O3	1
1	Ki = 118 nM
CP0157306 Compound Info	4-[4-[[(2S)-2-(3,5-dimethylphenyl)pyrrolidin-1-yl]methyl]phenoxy]-3-fluorobenzamide Show/Hide	C26H27FN2O2	1
1	Ki = 122 nM
CP0122914 Compound Info	3-((7R,8R,9alphaR)-2-benzyl-7,8-dimethyl-octahydro-1H-pyrido-[1,2-R]pyrazin-8-yl)phenol Show/Hide	C23H30N2O	1
1	Ki = 139 nM
CP0102441 Compound Info	(3S,4aR,4bS,6S,8R,8aR,10aR)-3-Furan-3-yl-4a,8a-dimethyl-1,5-dioxo-6-phenylcarbamoyloxy-dodecahydro-2-oxa-phenanthrene-8-carboxylic acid methyl ester Show/Hide	C28H31NO8	1
1	Ki = 230 nM
CP0099525 Compound Info	3-((7R,8R,9alphaR)-7,8-dimethyl-2-phenethyl-octahydro-1H-pyrido[1,2-R]pyrazin-8-yl)phenol Show/Hide	C24H32N2O	1
1	Ki = 242 nM
CP0274703 Compound Info	8-Acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one Show/Hide	C25H25N3O	1
1	Ki = 251.19 nM
CP0043301 Compound Info	(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]-N-methylacetamido}-N-(2-hydroxyethyl)-3-phenylpropanamide Show/Hide	C26H35N5O6	4
1	Ki = 290 nM
2	Ki = 567 nM
3	Ki > 2000 nM
4	Ki > 10000 nM
CP0222936 Compound Info	(2S)-2-[[(E,2R)-5-[[2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]-2-benzylpent-3-enoyl]amino]-4-methylpentanoic acid Show/Hide	C29H38N4O6	1
1	Ki = 587 nM
CP0056488 Compound Info	3-((3S,7R,8R,9alphaR)-2,7,8-trimethyl-3-phenyl-octahydro-1Hpyrido[1,2-R]pyrazin-8-yl)phenol Show/Hide	C23H30N2O	1
1	Ki = 716 nM
CP0036846 Compound Info	(3S,4aR,4bS,6S,8R,8aR,10aR)-6-Benzoyloxy-3-furan-3-yl-4a,8a-dimethyl-1,5-dioxo-dodecahydro-2-oxa-phenanthrene-8-carboxylic acid methyl ester Show/Hide	C28H30O8	1
1	Ki = 1170 nM
CP0070299 Compound Info	methyl (2S,4aR,6aR,7R,9S,10aS,10bR)-2-(furan-3-yl)-6a,10b-dimethyl-4,10-dioxo-9-(thiophene-2-carbonyloxy)-2,4a,5,6,7,8,9,10a-octahydro-1H-benzo[f]isochromene-7-carboxylate Show/Hide	C26H28O8S	1
1	Ki = 1380 nM
CP0295999 Compound Info	(2S,4aR,6aR,7R,9S,10aS,10bR)-9-(4-Bromobenzoyloxy)-2-(3-furanyl)-dodecahydro-6a,10b-dimethyl-4,10-dioxo-2H-naphtho-[2,1-c]pyran-7-carboxylic Acid Methyl Ester Show/Hide	C28H29BrO8	1
1	Ki = 1410 nM
CP0099651 Compound Info	(3S)-3-[(2S)-2-[(2S)-2-(2-{2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]acetamido}acetamido)-3-(1H-indol-3-yl)-N-methylpropanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid Show/Hide	C44H55N9O10	1
1	Ki = 2000 nM
CP0032210 Compound Info	4-(4-piperidin-4-ylphenyl)-7-[4-(trifluoromethyl)phenyl]naphthalene-2-carboxylic acid Show/Hide	C29H24F3NO2	1
1	Ki = 2750 nM
CP0424009 Compound Info	3-[5-(3-aminopropylcarbamoyl)thiophen-2-yl]-5-[4-[4-(trifluoromethyl)phenyl]triazol-1-yl]benzoic acid Show/Hide	C24H20F3N5O3S	1
1	Ki = 3260 nM
CP0261931 Compound Info	(4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-3-methyl-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-3-ium-7-one Show/Hide	C21H26NO4+	1
1	Ki = 3454 nM
CP0036843 Compound Info	(2S,4aR,6aR,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(furan-3-yl)dodecahydro-6a,10b-dimethyl-4,10-dioxo-2H-naphtho-[2,1-c]pyran-7-carboxylic acid methyl ester Show/Hide	C23H28O8	2
1	Ki = 5790 nM
2	Ki > 10000 nM
CP0123984 Compound Info	(S)-1-[(S)-2-Amino-3-(4-hydroxy-phenyl)-propionyl]-pyrrolidine-2-carboxylic acid [(S)-1-((S)-1-carbamoyl-2-phenyl-ethylcarbamoyl)-2-phenyl-ethyl]-amide Show/Hide	C32H37N5O5	1
1	Ki = 6085 nM
CP0178560 Compound Info	(3S,4aR,4bS,6S,8R,8aR,10aR)-3-Furan-3-yl-4a,8a-dimethyl-6-(2-methyl-acryloyloxy)-1,5-dioxo-dodecahydro-2-oxa-phenanthrene-8-carboxylic acid methyl ester Show/Hide	C25H30O8	1
1	Ki = 8880 nM
CP0040101 Compound Info	2-(3,4-dichlorophenyl)-N-methyl-N-[(1R,2R)-2-pyrrolidin-1-ylcyclohexyl]acetamide Show/Hide	C19H26Cl2N2O	2
1	Ki = 21000 nM
2	Ki > 10000 nM
CP0038350 Compound Info	(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-6-amino-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-6-amino-2-[(2S)-2-[(2S)-2-{2-[(2S,3R)-2-[(2S)-2-(2-{2-[(2S)-2-amino-3-phenylpropanamido]acetamido}acetamido)-3-phenylpropanamido]-3-hydroxybutanamido]acetamido}propanamido]-5-carbamimidamidopentanamido]hexanamido]-3-hydroxypropanamido]propanamido]-5-carbamimidamidopentanamido]hexanamido]-4-methylpentanamido]propanamido]butanediamido]-4-carbamoylbutanoic acid Show/Hide	C79H129N27O22	1
1	Ki > 2000 nM
CP0070302 Compound Info	(2S,4aR,6aR,7R,9S,10aS,10bR)-methyl 9-(2-bromobenzoyloxy)-2-(furan-3-yl)-6a,10b-dimethyl-4,10-dioxo-dodecahydro-1H-benzo[f]isochromene-7-carboxylate Show/Hide	C28H29BrO8	1
1	Ki > 10000 nM
CP0233847 Compound Info	(2S,4aR,6aR,7R,9S,10aS,10bR)-methyl 9-(3-bromobenzoyloxy)-2-(furan-3-yl)-6a,10b-dimethyl-4,10-dioxo-dodecahydro-1H-benzo[f]isochromene-7-carboxylate Show/Hide	C28H29BrO8	1
1	Ki > 10000 nM
CP0130404 Compound Info	methyl (2S,4aR,6aR,7R,9S,10aS,10bR)-2-(furan-3-yl)-9-hydroxy-6a,10b-dimethyl-4,10-dioxo-2,4a,5,6,7,8,9,10a-octahydro-1H-benzo[f]isochromene-7-carboxylate Show/Hide	C21H26O7	1
1	Ki > 10000 nM

Clinical Information about the Protein

Target 1 ( Opioid receptor delta (OPRD1) )

Target Type	Successful Target
Disease	7 Target-related Diseases				7
1	Pain [ICD-11: MG30-MG3Z]
2	Diarrhea-predominant irritable bowel syndrome [ICD-11: DD91.01]
3	Diarrhea [ICD-11: ME05.1]
4	Opioid dependence [ICD-11: 6C43.2Z]
5	Cerebral vasospasm [ICD-11: BA85.Z]
6	Obesity [ICD-11: 5B81]
7	Alcohol dependence [ICD-11: 6C40.2]
Approved Drug(s)	6 Approved Drugs				6
1	Butorphanol	Drug Info	Approved	Pain
2	Codeine	Drug Info	Approved	Pain
3	Eluxadoline	Drug Info	Approved	Diarrhea-predominant irritable bowel syndrome
4	Hydromorphone	Drug Info	Approved	Pain
5	Loperamide	Drug Info	Approved	Diarrhea
6	Oxycodone	Drug Info	Approved	Pain
Clinical Trial Drug(s)	3 Clinical Trial Drugs				3
1	Met-enkephalin	Drug Info	Phase 2	Pain
2	AIKO-150	Drug Info	Phase 1	Opioid dependence
3	SALVINORIN A	Drug Info	Phase 1	Cerebral vasospasm
Discontinued Drug(s)	1 Discontinued Drug				1
1	DPI-3290	Drug Info	Discontinued in Phase 2	Pain
Preclinical Drug(s)	2 Preclinical Drugs				2
1	LY-25582	Drug Info	Preclinical	Obesity
2	SoRI-9409	Drug Info	Preclinical	Alcohol dependence

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han