Target Validation Information
TTD ID T52921
Target Name Nociceptin receptor (OPRL1)
Type of Target
Clinical trial
Drug Potency against Target 1-(1,2-diphenylethyl)-4-phenylpiperidin-4-ol Drug Info Ki = 16 nM [8]
1-(2-ethoxy-1-phenylethyl)-4-phenylpiperidin-4-ol Drug Info Ki = 134 nM [8]
1-(3,3-diphenylpropyl)-4-phenylpiperidin-4-ol Drug Info Ki = 613 nM [8]
1-(dio-tolylmethyl)-4-phenylpiperidin-4-ol Drug Info Ki = 4 nM [8]
1-benzhydryl-4-(2-fluorophenyl)piperidin-4-ol Drug Info Ki = 34 nM [7]
1-benzhydryl-4-(2-methoxyphenyl)piperidin-4-ol Drug Info Ki = 85 nM [7]
1-benzhydryl-4-(3-fluorophenyl)piperidin-4-ol Drug Info Ki = 23 nM [7]
1-benzhydryl-4-(3-methoxyphenyl)piperidin-4-ol Drug Info Ki = 180 nM [7]
1-benzhydryl-4-(3-phenylpropyl)piperidin-4-ol Drug Info Ki = 1667 nM [7]
1-benzhydryl-4-(4-bromophenyl)piperidin-4-ol Drug Info Ki = 51 nM [7]
1-benzhydryl-4-(4-butylphenyl)piperidin-4-ol Drug Info Ki = 9155 nM [7]
1-benzhydryl-4-(4-chlorophenyl)piperidin-4-ol Drug Info Ki = 24 nM [7]
1-benzhydryl-4-(4-ethylphenyl)piperidin-4-ol Drug Info Ki = 1281 nM [7]
1-benzhydryl-4-(4-fluorophenyl)piperidin-4-ol Drug Info Ki = 14 nM [7]
1-benzhydryl-4-(4-methoxyphenyl)piperidin-4-ol Drug Info Ki = 588 nM [7]
1-benzhydryl-4-(4-propylphenyl)piperidin-4-ol Drug Info Ki = 1745 nM [7]
1-benzhydryl-4-(benzyloxy)-4-phenylpiperidine Drug Info Ki = 162 nM [8]
1-benzhydryl-4-(furan-2-yl)piperidin-4-ol Drug Info Ki = 136 nM [7]
1-benzhydryl-4-(pyridin-2-yl)piperidin-4-ol Drug Info Ki = 313 nM [7]
1-benzhydryl-4-(thiophen-2-yl)piperidin-4-ol Drug Info Ki = 48 nM [7]
1-benzhydryl-4-benzylpiperidin-4-ol Drug Info Ki = 2176 nM [7]
1-benzhydryl-4-butylpiperidin-4-ol Drug Info Ki = 23 nM [7]
1-benzhydryl-4-cyclohexylpiperidin-4-ol Drug Info Ki = 17 nM [7]
1-benzhydryl-4-cyclopropylpiperidin-4-ol Drug Info Ki = 376 nM [7]
1-benzhydryl-4-ethoxy-4-phenylpiperidine Drug Info Ki = 59 nM [8]
1-benzhydryl-4-hexylpiperidin-4-ol Drug Info Ki = 1147 nM [7]
1-benzhydryl-4-isopropylpiperidin-4-ol Drug Info Ki = 433 nM [7]
1-benzhydryl-4-m-tolylpiperidin-4-ol Drug Info Ki = 27 nM [7]
1-benzhydryl-4-methoxy-4-phenylpiperidine Drug Info Ki = 54 nM [8]
1-benzhydryl-4-o-tolylpiperidin-4-ol Drug Info Ki = 11 nM [7]
1-benzhydryl-4-p-tolylpiperidin-4-ol Drug Info Ki = 55 nM [7]
1-benzhydryl-4-phenyl-4-propoxypiperidine Drug Info Ki = 72 nM [8]
1-benzhydryl-4-phenylpiperidin-4-ol Drug Info Ki = 13 nM [12]
1-benzhydryl-4-tert-butylpiperidin-4-ol Drug Info Ki = 62 nM [7]
1-benzyl-4-phenylpiperidin-4-ol Drug Info Ki = 1983 nM [8]
2,2-diMeBut-RYYRIK-NH2 Drug Info IC50 = 45.5 nM [9]
2-MePen-RYYRIK-NH2 Drug Info IC50 = 47.3 nM [9]
3-(1-benzylpiperidin-4-yl)-5-chloro-1H-indole Drug Info Ki = 1140 nM [4]
4-(2-(aminomethyl)phenyl)-1-benzylpiperidin-4-ol Drug Info Ki = 455 nM [7]
4-phenyl-1-(1-phenylbutyl)piperidin-4-ol Drug Info Ki = 19 nM [8]
4-phenyl-1-(1-phenylethyl)piperidin-4-ol Drug Info Ki = 323 nM [8]
4-phenyl-1-(1-phenylheptyl)piperidin-4-ol Drug Info Ki = 18 nM [8]
4-phenyl-1-(1-phenylhexyl)piperidin-4-ol Drug Info Ki = 14 nM [8]
4-phenyl-1-(1-phenylpentyl)piperidin-4-ol Drug Info Ki = 5 nM [8]
4-phenyl-1-(1-phenylpropyl)piperidin-4-ol Drug Info Ki = 135 nM [8]
4-phenyl-1-(phenyl(m-tolyl)methyl)piperidin-4-ol Drug Info Ki = 3 nM [8]
4-phenyl-1-(phenyl(p-tolyl)methyl)piperidin-4-ol Drug Info Ki = 53 nM [8]
Ac-RYYRIK-K-(NH2)-YAFGYPS Drug Info IC50 = 11.6 nM [5]
Ac-RYYRIK-K-(NH2)-YRFB Drug Info IC50 = 0.789 nM [5]
Ada-RYYRIK-NH2 Drug Info IC50 = 3.42 nM [9]
Bu-RYYRIK-NH2 Drug Info IC50 = 1.86 nM [9]
Bz--RYYRIK-NH2 Drug Info IC50 = 14.7 nM [9]
Cyclo-[Asp6,Lys10]N/OFQ(1-13)NH2 Drug Info Ki = 0.34 nM [10]
Cyclo[Cys6,Cys10]N/OFQ(1-13)NH2 Drug Info Ki = 0.83 nM [10]
Cyclo[Cys7,Cys10]N/OFQ(1-13)NH2 Drug Info Ki = 0.1 nM [10]
Cyclo[DAsp7,Lys10]N/OFQ(1-13)NH2 Drug Info Ki = 0.27 nM [10]
EtBut-RYYRIK-NH2 Drug Info IC50 = 92.6 nM [9]
F-G-G-F-T-G-A-R-K-S-A-R-K-L-Aib-N-Q-COOH Drug Info Ki = 0.15 nM [2]
F-G-G-F-T-G-A-R-K-S-A-R-K-L-MeA-N-Q-COOH Drug Info Ki = 1.1 nM [2]
F-G-G-F-T-G-A-R-K-S-Aib-R-K-L-A-N-Q-COOH Drug Info Ki = 0.48 nM [2]
F-G-G-F-T-G-A-R-K-S-MeA-R-K-L-A-N-Q-CONH2 Drug Info Ki = 6.7 nM [2]
F-G-G-F-T-G-A-R-K-S-MeA-R-K-L-A-N-Q-COOH Drug Info Ki = 20 nM [2]
F-G-G-F-T-G-Aib-R-K-S-A-R-K-L-A-N-Q-COOH Drug Info Ki = 0.1 nM [2]
F-G-G-F-T-G-MeA-R-K-S-A-R-K-L-A-N-Q-CONH2 Drug Info Ki = 2.2 nM [2]
F-G-G-F-T-G-MeA-R-K-S-A-R-K-L-A-N-Q-COOH Drug Info Ki = 15 nM [2]
FGGFTCARKCARK Drug Info IC50 = 3.03 nM [1]
FGGFTGARKCARKC Drug Info IC50 = 0.471 nM [1]
FGGFTGARKRKRKLANQ Drug Info IC50 = 0.94 nM [11]
FGGFTGARKSARKAANQ Drug Info IC50 = 1.5 nM [11]
FGGFTGARKSARKFANQ Drug Info IC50 = 1.1 nM [11]
FGGFTGARKSARKKANQ Drug Info IC50 = 0.41 nM [11]
FGGFTGARKSARKKKNQ Drug Info IC50 = 0.16 nM [11]
FGGFTGARKSARKKRNQ Drug Info IC50 = 0.21 nM [11]
FGGFTGARKSARKKWNQ Drug Info IC50 = 0.31 nM [13]
FGGFTGARKSARKL Drug Info IC50 = 0.52 nM [1]
FGGFTGARKSARKLADE Drug Info IC50 = 0.286 nM [1]
FGGFTGARKSARKLARK Drug Info IC50 = 0.54 nM [11]
FGGFTGARKSARKLFNQ Drug Info IC50 = 1 nM [11]
FGGFTGARKSARKLKNQ Drug Info IC50 = 0.41 nM [11]
FGGFTGARKSARKLLNQ Drug Info IC50 = 0.48 nM [11]
FGGFTGARKSARKLRNQ Drug Info IC50 = 0.31 nM [11]
FGGFTGARKSARKLVNQ Drug Info IC50 = 2.2 nM [11]
FGGFTGARKSARKLWNQ Drug Info IC50 = 2.1 nM [13]
FGGFTGARKSARKLYNQ Drug Info IC50 = 1 nM [11]
FGGFTGARKSARKRANQ Drug Info IC50 = 0.33 nM [11]
FGGFTGARKSARKRKNQ Drug Info IC50 = 0.21 nM [13]
FGGFTGARKSARKRKRK Drug Info IC50 = 0.42 nM [11]
FGGFTGARKSARKRRNQ Drug Info IC50 = 0.27 nM [11]
FGGFTGARKSARKRWNQ Drug Info IC50 = 0.3 nM [13]
FGGFTGARKSARKVANQ Drug Info IC50 = 1.1 nM [11]
FGGFTGARKSARKWANQ Drug Info IC50 = 0.41 nM [13]
FGGFTGARKSARKWKNQ Drug Info IC50 = 0.25 nM [13]
FGGFTGARKSARKWRNQ Drug Info IC50 = 0.23 nM [13]
FGGFTGARKSARKYANQ Drug Info IC50 = 1.1 nM [11]
FGGFTGCRKSCRK Drug Info IC50 = 3.04 nM [1]
FGGFTRKRKSARKLANQ Drug Info IC50 = 13 nM [11]
FLUPERAMIDE Drug Info Ki = 2151 nM [3]
For-RYYRIK-NH2 Drug Info IC50 = 0.66 nM [9]
H-RYYRIK-NH2 Drug Info IC50 = 218 nM [9]
Hex-RYYRIK-NH2 Drug Info IC50 = 21.7 nM [9]
IsoBu-RYYRIK-NH2 Drug Info IC50 = 2.81 nM [9]
IsoVa-RYYRIK-NH2 Drug Info IC50 = 7.42 nM [9]
MeBut-RYYRIK-NH2 Drug Info IC50 = 21.3 nM [9]
N/OFQ-(1-13)-NH2 Drug Info IC50 = 0.353 nM [1]
NOCICEPTIN Drug Info IC50 = 0.73 nM [11]
Piv-RYYRIK-NH2 Drug Info IC50 = 14.9 nM [9]
PMX-53 Drug Info IC50 = 2200 nM [6]
Pr-RYYRIK-NH2 Drug Info IC50 = 1.7 nM [9]
T-BuAc-RYYRIK-NH2 Drug Info IC50 = 16.9 nM [9]
Va-RYYRIK-NH2 Drug Info IC50 = 5.67 nM [9]
[Asp6,Lys10]N/OFQ(1-13)NH2 Drug Info Ki = 0.54 nM [10]
[D-Asp7,Lys10]N/OFQ(1-13)NH2 Drug Info Ki = 1.79 nM [10]
References
REF 1 Structure-activity studies on nociceptin analogues: ORL1 receptor binding and biological activity of cyclic disulfide-containing analogues of nocic... J Med Chem. 2001 Nov 8;44(23):4015-8.
REF 2 Novel, potent ORL-1 receptor agonist peptides containing alpha-Helix-promoting conformational constraints. J Med Chem. 2002 Nov 21;45(24):5280-6.
REF 3 Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor. Bioorg Med Chem Lett. 2004 Nov 1;14(21):5275-9.
REF 4 3-(4-Piperidinyl)indoles and 3-(4-piperidinyl)pyrrolo-[2,3-b]pyridines as ligands for the ORL-1 receptor. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3524-8.
REF 5 Synthesis and receptor binding properties of chimeric peptides containing a mu-opioid receptor ligand and nociceptin/orphanin FQ receptor ligand Ac... Bioorg Med Chem Lett. 2006 Sep 15;16(18):4839-41.
REF 6 Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5088-92.
REF 7 Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
REF 8 Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
REF 9 Designed modification of partial agonist of ORL1 nociceptin receptor for conversion into highly potent antagonist. Bioorg Med Chem. 2008 Mar 1;16(5):2635-44.
REF 10 High affinity conformationally constrained nociceptin/orphanin FQ(1-13) amide analogues. J Med Chem. 2008 Aug 14;51(15):4385-7.
REF 11 Synergistic effect of basic residues at positions 14-15 of nociceptin on binding affinity and receptor activation. Bioorg Med Chem. 2008 Oct 15;16(20):9261-7.
REF 12 The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety. Bioorg Med Chem Lett. 2009 May 1;19(9):2519-23.
REF 13 Discriminatory synergistic effect of Trp-substitutions in superagonist [(Arg/Lys)(14), (Arg/Lys)(15)]nociceptin on ORL1 receptor binding and activa... Bioorg Med Chem. 2009 Aug 1;17(15):5683-7.

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