Target Validation Information
TTD ID T60693
Target Name Opioid receptor kappa (OPRK1)
Type of Target
Successful
Drug Potency against Target Drug Info IC50 = 38 nM [36]
1-(1,2-diphenylethyl)-4-phenylpiperidin-4-ol Drug Info Ki = 288 nM [17]
1-(2-ethoxy-1-phenylethyl)-4-phenylpiperidin-4-ol Drug Info Ki = 1028 nM [17]
1-(dio-tolylmethyl)-4-phenylpiperidin-4-ol Drug Info Ki = 1712 nM [17]
1-benzhydryl-4-(2-fluorophenyl)piperidin-4-ol Drug Info Ki = 1738 nM [16]
1-benzhydryl-4-(2-methoxyphenyl)piperidin-4-ol Drug Info Ki = 4160 nM [16]
1-benzhydryl-4-(3-fluorophenyl)piperidin-4-ol Drug Info Ki = 1994 nM [16]
1-benzhydryl-4-(3-methoxyphenyl)piperidin-4-ol Drug Info Ki = 3668 nM [16]
1-benzhydryl-4-(3-phenylpropyl)piperidin-4-ol Drug Info Ki = 1801 nM [16]
1-benzhydryl-4-(4-bromophenyl)piperidin-4-ol Drug Info Ki = 2612 nM [16]
1-benzhydryl-4-(4-chlorophenyl)piperidin-4-ol Drug Info Ki = 1702 nM [16]
1-benzhydryl-4-(4-ethylphenyl)piperidin-4-ol Drug Info Ki = 11355 nM [16]
1-benzhydryl-4-(4-fluorophenyl)piperidin-4-ol Drug Info Ki = 759 nM [16]
1-benzhydryl-4-(4-methoxyphenyl)piperidin-4-ol Drug Info Ki = 10298 nM [16]
1-benzhydryl-4-(4-propylphenyl)piperidin-4-ol Drug Info Ki = 19695 nM [16]
1-benzhydryl-4-(benzyloxy)-4-phenylpiperidine Drug Info Ki = 13390 nM [17]
1-benzhydryl-4-(furan-2-yl)piperidin-4-ol Drug Info Ki = 9644 nM [16]
1-benzhydryl-4-(pyridin-2-yl)piperidin-4-ol Drug Info Ki = 13180 nM [16]
1-benzhydryl-4-(thiophen-2-yl)piperidin-4-ol Drug Info Ki = 3412 nM [16]
1-benzhydryl-4-benzylpiperidin-4-ol Drug Info Ki = 1438 nM [16]
1-benzhydryl-4-butylpiperidin-4-ol Drug Info Ki = 4563 nM [16]
1-benzhydryl-4-cyclohexylpiperidin-4-ol Drug Info Ki = 387 nM [16]
1-benzhydryl-4-ethoxy-4-phenylpiperidine Drug Info Ki = 488 nM [17]
1-benzhydryl-4-hexylpiperidin-4-ol Drug Info Ki = 9221 nM [16]
1-benzhydryl-4-isopropylpiperidin-4-ol Drug Info Ki = 7390 nM [16]
1-benzhydryl-4-m-tolylpiperidin-4-ol Drug Info Ki = 1151 nM [16]
1-benzhydryl-4-methoxy-4-phenylpiperidine Drug Info Ki = 343 nM [17]
1-benzhydryl-4-o-tolylpiperidin-4-ol Drug Info Ki = 818 nM [16]
1-benzhydryl-4-p-tolylpiperidin-4-ol Drug Info Ki = 4054 nM [16]
1-benzhydryl-4-phenyl-4-propoxypiperidine Drug Info Ki = 1484 nM [17]
1-benzhydryl-4-phenylpiperidin-4-ol Drug Info Ki = 364 nM [37]
1-benzhydryl-4-tert-butylpiperidin-4-ol Drug Info Ki = 1073 nM [16]
12-EPI-SALVINORIN A Drug Info Ki = 41 nM [34]
14-O-phenylpropylnaltrexone Drug Info Ki = 0.41 nM [35]
17-(Cyclobutylmethyl)-N-phenylmorphinan-3-amine Drug Info Ki = 1.5 nM [47]
17-methyl-4'-methyldihydromorphinone Drug Info Ki = 1.5 nM [9]
17-Methylmorphinan-3-yl 4-Iodophenyl Carbamate Drug Info Ki = 5.2 nM [47]
2-(2-methylquinolin-4-ylamino)-N-phenylacetamide Drug Info IC50 = 1.03 nM [43]
2-Benzylaminomethyl-3-hydroxymorphinan Drug Info Ki = 380 nM [47]
2-EPI-2-THIOSALVINORIN A Drug Info Ki = 151 nM [13]
2-EPI-2-THIOSALVINORIN B Drug Info Ki = 546 nM [13]
2-Hydroxymethyl-3-hydroxymorphinan Drug Info Ki = 40 nM [47]
2-THIOSALVINORIN B Drug Info Ki = 54.5 nM [13]
3-(1-benzylpiperidin-4-yl)-5-chloro-1H-indole Drug Info Ki = 330 nM [7]
3-(1-benzylpiperidin-4-yloxy)benzamide Drug Info IC50 = 585 nM [55]
3-desoxy-3-carboxamidonaltrexone Drug Info Ki = 11 nM [36]
4-(4-((phenethylamino)methyl)phenoxy)benzamide Drug Info Ki = 15.04 nM [23]
4-(Spiro[chromene-2,4'-piperidine]-4-yl)benzamide Drug Info Ki = 560 nM [44]
4-phenyl-1-(1-phenylbutyl)piperidin-4-ol Drug Info Ki = 245 nM [17]
4-phenyl-1-(1-phenylethyl)piperidin-4-ol Drug Info Ki = 4149 nM [17]
4-phenyl-1-(1-phenylheptyl)piperidin-4-ol Drug Info Ki = 335 nM [17]
4-phenyl-1-(1-phenylhexyl)piperidin-4-ol Drug Info Ki = 220 nM [17]
4-phenyl-1-(1-phenylpentyl)piperidin-4-ol Drug Info Ki = 36 nM [17]
4-phenyl-1-(1-phenylpropyl)piperidin-4-ol Drug Info Ki = 1427 nM [17]
4-phenyl-1-(phenyl(m-tolyl)methyl)piperidin-4-ol Drug Info Ki = 1095 nM [17]
4-phenyl-1-(phenyl(p-tolyl)methyl)piperidin-4-ol Drug Info Ki = 2687 nM [17]
4-phenyl-4-[1H-imidazol-2-yl]-piperidine Drug Info Ki = 126 nM [4]
4-Phenylspiro[chromene-2,4'-piperidine] Drug Info Ki = 3400 nM [32]
5-(4-((phenethylamino)methyl)phenoxy)picolinamide Drug Info Ki = 69.27 nM [23]
6-(4-((benzylamino)methyl)phenoxy)nicotinamide Drug Info Ki = 2.47 nM [23]
6-(4-((phenethylamino)methyl)phenoxy)nicotinamide Drug Info Ki = 8.38 nM [24]
6-(4-(2-(benzylamino)ethyl)phenoxy)nicotinamide Drug Info Ki = 136.26 nM [24]
6-(4-(3-(benzylamino)propyl)phenoxy)nicotinamide Drug Info Ki = 45.83 nM [23]
6-(Allyl-methyl-amino)-4,4-diphenyl-heptan-3-ol Drug Info Ki = 150 nM [60]
6-desoxonaltrexone Drug Info IC50 = 13 nM [36]
6beta-naltrexol HCl Drug Info Ki = 7.42 nM [39]
8-azabicyclo[3.2.1]octan-3-yloxy-benzamide Drug Info IC50 = 20 nM [54]
AIKO-150 Drug Info Ki = 0.48 nM [33]
ANISOCOUMARIN H Drug Info Ki = 2600 nM [26]
Benzyl derivative of M6G Drug Info Ki = 15.8 nM [3]
Bis-((-)-N-propargylmorphinan-3-yl) sebacoylate Drug Info Ki = 10 nM [5]
CHLOROXINE Drug Info IC50 = 4560 nM [57]
Cis-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH Drug Info Ki = 576 nM [20]
CLIOQUINOL Drug Info IC50 = 5790 nM [57]
Clocinnamox Drug Info Ki = 1.4 nM [35]
C[L-Ala-D-pro-L-Phe-D-trp] Drug Info IC50 = 5 nM [40]
C[L-mTyr-D-pro-L-Phe-D-trp] Drug Info Ki = 78 nM [40]
C[L-Phe-D-pro-L-mTyr-D-trp] Drug Info Ki = 20 nM [40]
C[L-Phe-D-pro-L-Phe-D-trp] Drug Info IC50 = 140 nM [40]
C[L-Phe-D-pro-L-Phe-L-trp] Drug Info IC50 = 47 nM [40]
C[L-Phe-D-pro-L-Tyr(OMe)-D-trp] Drug Info Ki = 14 nM [40]
C[L-Phe-D-pro-L-Tyr-D-trp] Drug Info Ki = 140 nM [40]
C[L-Tyr(OMe)-D-pro-L-Phe-D-trp] Drug Info Ki = 66 nM [40]
C[L-Tyr-D-pro-L-Phe-D-trp] Drug Info Ki = 220 nM [40]
DAMGO Drug Info Ki = 1841 nM [65]
Dcp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 Drug Info Ki = 980 nM [10]
DEOXY SALVINORIN A Drug Info Ki = 7.9 nM [8]
Deprotected cogener of M6G Drug Info Ki = 574.9 nM [3]
Dhp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 Drug Info Ki = 299 nM [10]
Dimepheptanol Drug Info Ki = 230 nM [60]
DM6S Drug Info Ki = 3129 nM [65]
Dmt-Pro-3,5Dmp-Phe-NH2 Drug Info Ki = 830 nM [19]
Dmt-Pro-Dmp-Phe-NH2 Drug Info Ki = 94.2 nM [19]
Dmt-Pro-Dmt-Phe-NH2 Drug Info Ki = 998 nM [19]
Dmt-Pro-Emp-Phe-NH2 Drug Info Ki = 278 nM [19]
Dmt-Pro-Imp-Phe-NH2 Drug Info Ki = 205 nM [19]
Dmt-Pro-Mmp-Phe-NH2 Drug Info Ki = 176 nM [19]
Dmt-Pro-Phe-Phe-NH2 Drug Info Ki = 489 nM [19]
Dmt-Pro-Tmp-Phe-NH2 Drug Info Ki = 172 nM [19]
DPDPE Drug Info IC50 = 2.8 nM [1]
Dynorphin a Drug Info Ki = 0.21 nM [30]
Dynorphin(1-8) Drug Info Ki = 40 nM [59]
ELAEOCARPENINE Drug Info Ki = 12000 nM [49]
ENDOMORPHIN 2 Drug Info Ki = 10.6 nM [2]
ENDOMORPHIN-1 Drug Info Ki = 52.7 nM [2]
ETONITAZENE Drug Info Ki = 0.6 nM [58]
FALCARINDIOL Drug Info Ki = 2515 nM [26]
H-Cdp-ala-Gly-Phe-leu-OH Drug Info Ki = 2400 nM [15]
H-Cdp-Gly-Gly-Phe-Leu-OH Drug Info Ki = 1300 nM [15]
H-Cpa-Gly-Gly-Phe-Met-NH2 Drug Info Ki = 460 nM [15]
H-Cpa-Gly-Gly-Phe-Met-OH Drug Info Ki = 1030 nM [15]
H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]-OH Drug Info Ki = 3960 nM [20]
H-Tyr-c[D-Cys-Gly-Phe-D-Cys]NH2 Drug Info Ki = 44.9 nM [14]
H-Tyr-c[D-Cys-Gly-Phe-L-Cys]NH2 Drug Info Ki = 40.1 nM [14]
H-Tyr-Gly-Gly-Phe-Met-NH2 Drug Info Ki = 210 nM [15]
HERKINORIN Drug Info Ki = 90 nM [28]
HTyr-Gly-Gly-Phe-Leu-Arg-Arg-lle-Arg-Pro-LysNH2 Drug Info Ki = 0.57 nM [45]
ICI-199441 Drug Info IC50 = 2.5 nM [62]
KETOCYCLAZOCINE Drug Info Ki = 1 nM [33]
KNT-62 Drug Info Ki = 0.152 nM [48]
KNT-63 Drug Info Ki = 0.111 nM [48]
LOFENTANIL Drug Info IC50 = 0.25 nM [61]
LY-25582 Drug Info Ki = 28 nM [64]
M3A6S Drug Info Ki = 1165 nM [65]
M3IBu6S Drug Info Ki = 4558 nM [65]
M3P6S Drug Info Ki = 1940 nM [65]
M3Pr6S Drug Info Ki = 252 nM [65]
M6S Drug Info Ki = 1192 nM [65]
MC-CAM Drug Info Ki = 16.4 nM [46]
MCL-149 Drug Info Ki = 0.18 nM [18]
MCL-153 Drug Info Ki = 18 nM [50]
MCL-154 Drug Info Ki = 120 nM [50]
MCL-182 Drug Info Ki = 1.8 nM [18]
MCL-183 Drug Info Ki = 0.79 nM [18]
MCL-431 Drug Info Ki = 36 nM [12]
MCL-432 Drug Info Ki = 4.3 nM [12]
MCL-433 Drug Info Ki = 3.3 nM [12]
MCL-434 Drug Info Ki = 3.4 nM [12]
MCL-435 Drug Info Ki = 0.81 nM [12]
MCL-443 Drug Info Ki = 0.3 nM [12]
MCL-444 Drug Info Ki = 0.14 nM [12]
MCL-445 Drug Info Ki = 20 nM [18]
MCL-446 Drug Info Ki = 2.3 nM [18]
MCL-447 Drug Info Ki = 8.9 nM [18]
MCL-448 Drug Info Ki = 0.61 nM [18]
MCL-449 Drug Info Ki = 0.14 nM [12]
MCL-450 Drug Info Ki = 0.28 nM [11]
MCL-457 Drug Info Ki = 47 nM [18]
MCL-458 Drug Info Ki = 1.9 nM [18]
METAZOCINE Drug Info Ki = 9.9 nM [33]
MK-1925 Drug Info IC50 = 9800 nM [41]
MR-1029 Drug Info IC50 = 5.7 nM [6]
MR-1526 Drug Info IC50 = 70 nM [6]
MR-2266 Drug Info IC50 = 1.6 nM [6]
N,N-diallyl[D-Pro-10]Dyn A-(1-11) Drug Info IC50 = 64.6 nM [63]
N,N-dibenzyl[D-Pro-10]Dyn A-(1-11) Drug Info IC50 = 391 nM [63]
N,N-diCPM[D-Pro-10]Dyn A-(1-11) Drug Info IC50 = 29.1 nM [63]
N-(17-Methylmorphinan-3-yl)-N'-phenylurea Drug Info Ki = 340 nM [47]
N-(4-Iodophenyl)-N'-(17-methylmorphinan-3-yl)urea Drug Info Ki = 280 nM [47]
N-allyl[D-Pro-10]Dyn A-(1-11) Drug Info IC50 = 229 nM [63]
N-Benzyl-17-(cyclobutylmethyl)morphinan-3-amine Drug Info Ki = 2.8 nM [47]
N-Benzyl-17-(cyclopropylmethyl)morphinan-3-amine Drug Info Ki = 0.34 nM [47]
N-benzyl[D-Pro-10]Dyn A-(1-11) Drug Info IC50 = 93.7 nM [63]
N-CPM[D-Pro-10]Dyn A-(1-11) Drug Info IC50 = 27.1 nM [63]
N-isobutylnoroxymorphone Drug Info Ki = 6.12 nM [31]
NalBzOH Drug Info Ki = 0.4 nM [65]
Nalfurafine hcl Drug Info Ki = 0.225 nM [48]
Naltrexone-6-alpha-ol Drug Info Ki = 0.56 nM [33]
NORBINALTORPHIMINE Drug Info Ki = 0.861 nM [53]
O-DESMETHYL TRAMADOL Drug Info Ki = 450 nM [33]
OXYMORPHINDOLE Drug Info Ki = 2170 nM [29]
Oxymorphone semicarbazone hydrochloride Drug Info Ki = 179 nM [59]
PHENAZOCINE Drug Info Ki = 2 nM [33]
RTI-5989-23 Drug Info Ki = 35.8 nM [64]
RTI-5989-25 Drug Info Ki = 38.9 nM [64]
RTI-5989-31 Drug Info Ki = 14.5 nM [22]
Salvinicin A Drug Info Ki = 390 nM [21]
SALVINICIN B Drug Info Ki = 7020 nM [21]
SALVINORIN A Drug Info Ki = 17.5 nM [27]
Salvinorin A (ester) Drug Info Ki = 140 nM [8]
SALVINORIN B Drug Info Ki = 280 nM [28]
Salvinorin B 1-ethoxyethyl ether Drug Info Ki = 6.6 nM [25]
Salvinorin B 2,2,2-trifluoroethoxymethyl ether Drug Info Ki = 31 nM [25]
Salvinorin B 2-fluoroethoxymethyl ether Drug Info Ki = 1.9 nM [25]
Salvinorin B 2-methoxy-2-propyl ether Drug Info Ki = 72 nM [25]
Salvinorin B 2-methoxyethoxymethyl ether Drug Info Ki = 141 nM [25]
Salvinorin B benzyloxymethyl ether Drug Info Ki = 147 nM [25]
Salvinorin B butoxymethyl ether Drug Info Ki = 5.3 nM [25]
Salvinorin B ethoxymethyl ether Drug Info Ki = 0.32 nM [25]
Salvinorin B fluoromethyl ether Drug Info Ki = 50 nM [25]
Salvinorin B isopropoxymethyl ether Drug Info Ki = 1.6 nM [25]
Salvinorin B methoxymethyl ether Drug Info Ki = 0.6 nM [25]
Salvinorin B methylthiomethyl ether Drug Info Ki = 13 nM [25]
Salvinorin B propoxymethyl ether Drug Info Ki = 2.2 nM [25]
Salvinorin B tert-butoxymethyl ether Drug Info Ki = 35 nM [25]
Salvinorin B tetrahydropyran-2-yl ether Drug Info Ki = 4 nM [25]
SB-213698 Drug Info Ki = 732.45 nM [38]
SN-11 Drug Info Ki = 0.36 nM [38]
SN-23 Drug Info Ki = 4.41 nM [38]
SN-28 Drug Info Ki = 49.4 nM [56]
SPIROINDANYLOXYMORPHONE Drug Info Ki = 588 nM [42]
Trans-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH Drug Info Ki = 74.8 nM [20]
ZYKLOPHIN Drug Info Ki = 30.3 nM [45]
[3H]U69593 Drug Info Ki = 0.97 nM [52]
[Dcp1]Dyn A(1-11)-NH2 Drug Info Ki = 32 nM [10]
[Leu5]enkephalin Drug Info Ki = 4570 nM [51]
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