Protein Information

General Information of the Protein

Protein ID	PT01199
Protein Name	Neuromedin-K receptor
Secondarily Protein Name	NK-3 receptor Neurokinin B receptor Tachykinin receptor 3
Gene Name	TACR3
Secondarily Gene Name	NK3R TAC3R
Sequence	MATLPAAETWIDGGGGVGADAVNLTASLAAGAATGAVETGWLQLLDQAGNLSSSPSALGLPVASPAPSQPWANLTNQFVQPSWRIALWSLAYGVVVAVAVLGNLIVIWIILAHKRMRTVTNYFLVNLAFSDASMAAFNTLVNFIYALHSEWYFGANYCRFQNFFPITAVFASIYSMTAIAVDRYMAIIDPLKPRLSATATKIVIGSIWILAFLLAFPQCLYSKTKVMPGRTLCFVQWPEGPKQHFTYHIIVIILVYCFPLLIMGITYTIVGITLWGGEIPGDTCDKYHEQLKAKRKVVKMMIIVVMTFAICWLPYHIYFILTAIYQQLNRWKYIQQVYLASFWLAMSSTMYNPIIYCCLNKRFRAGFKRAFRWCPFIKVSSYDELELKTTRFHPNRQSSMYTVTRMESMTVVFDPNDADTTRSSRKKRATPRDPSFNGCSRRNSKSASATSSFISSPYTSVDEYS 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) > Neurokinin receptor
Function	This is a receptor for the tachykinin neuropeptide neuromedin-K (neurokinin B). It is associated with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of affinity of this receptor to tachykinins is: neuromedin-K > substance K > substance P. Show/Hide
Uniprot ID	Primary ID: P29371 Secondarily ID: Q0P510 Show/Hide
Ensembl ID	ENSG00000169836
HGNC ID	HGNC:11528
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: CL000051 , BHK-21

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0426334 Compound Info	methyl N-[1-[[(1R,2S)-2-[benzyl(methyl)carbamoyl]-2-(3,4-dichlorophenyl)cyclopropyl]methyl]-4-phenylpiperidin-4-yl]carbamate Show/Hide	C32H35Cl2N3O3	1
1	Ki = 1.5 nM Bioactivity Info	TI LI LO TS
CP0512756 Compound Info	(1S,2R)-1-(3,4-dichlorophenyl)-N-(4-fluorobenzyl)-N-methyl-2-((4-(2-oxo-2-(pyrrolidin-1-yl)ethyl)piperazin-1-yl)methyl)cyclopropanecarboxamide Show/Hide	C29H35Cl2FN4O2	1
1	Ki = 1.8 nM Bioactivity Info	TI LI LO TS
CP0489233 Compound Info	(1S,2R)-1-(3,4-dichlorophenyl)-2-((3-(4-(N,N-dimethylsulfamoyl)piperazin-1-yl)azetidin-1-yl)methyl)-N-(4-fluorobenzyl)-N-methylcyclopropanecarboxamide Show/Hide	C28H36Cl2FN5O3S	1
1	Ki = 1.9 nM Bioactivity Info	TI LI LO TS
CP0426335 Compound Info	(1S,2R)-N-benzyl-1-(3,4-dichlorophenyl)-2-((4-(3,3-dimethylureido)-4-phenylpiperidin-1-yl)methyl)-N-methylcyclopropanecarboxamide Show/Hide	C33H38Cl2N4O2	1
1	Ki = 2.8 nM Bioactivity Info	TI LI LO TS
CP0516565 Compound Info	(1S,2R)-1-(3,4-dichlorophenyl)-N-(4-fluorobenzyl)-N-methyl-2-((4-(2-morpholinoacetyl)piperazin-1-yl)methyl)cyclopropanecarboxamide Show/Hide	C29H35Cl2FN4O3	1
1	Ki = 3.3 nM Bioactivity Info	TI LI LO TS
CP0513054 Compound Info	N'-[1-[[(1R,2S)-2-[benzyl(methyl)carbamoyl]-2-(3,4-dichlorophenyl)cyclopropyl]methyl]-4-phenylpiperidin-4-yl]-N'-methyloxamide Show/Hide	C33H36Cl2N4O3	1
1	Ki = 3.6 nM Bioactivity Info	TI LI LO TS
CP0426336 Compound Info	(1S,2R)-1-(3,4-dichlorophenyl)-N-(4-fluorobenzyl)-N-methyl-2-((4-(2-morpholinoethyl)piperazin-1-yl)methyl)cyclopropanecarboxamide Show/Hide	C29H37Cl2FN4O2	1
1	Ki = 3.7 nM Bioactivity Info	TI LI LO TS
CP0498917 Compound Info	(1S,2R)-N-benzyl-1-(3,4-dichlorophenyl)-N-methyl-2-((4-(N-methylacetamido)-4-phenylpiperidin-1-yl)methyl)cyclopropanecarboxamide Show/Hide	C33H37Cl2N3O2	1
1	Ki = 4.2 nM Bioactivity Info	TI LI LO TS
CP0489226 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-1-(3,4-dichlorophenyl)-N-methyl-N-[[4-(trifluoromethyl)phenyl]methyl]cyclopropane-1-carboxamide Show/Hide	C33H34Cl2F3N3O2	1
1	Ki = 4.6 nM Bioactivity Info	TI LI LO TS
CP0489224 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-1-(3,4-dichlorophenyl)-N-methyl-N-[(2-methylphenyl)methyl]cyclopropane-1-carboxamide Show/Hide	C33H37Cl2N3O2	1
1	Ki = 5.3 nM Bioactivity Info	TI LI LO TS
CP0399281 Compound Info	(1S,2R)-N-benzyl-1-(3,4-dichlorophenyl)-N-methyl-2-((4-(3-methylureido)-4-phenylpiperidin-1-yl)methyl)cyclopropanecarboxamide Show/Hide	C32H36Cl2N4O2	1
1	Ki = 5.6 nM Bioactivity Info	TI LI LO TS
CP0378685 Compound Info	(1S,2R)-1-(3,4-dichlorophenyl)-N-(4-fluorobenzyl)-N-methyl-2-((4-(pyrrolidin-1-ylsulfonyl)piperazin-1-yl)methyl)cyclopropanecarboxamide Show/Hide	C27H33Cl2FN4O3S	1
1	Ki = 5.8 nM Bioactivity Info	TI LI LO TS
CP0513051 Compound Info	(1S,2R)-2-((4-acetamido-4-phenylpiperidin-1-yl)methyl)-1-(3,4-dichlorophenyl)-N-(4-fluorobenzyl)-N-methylcyclopropanecarboxamide Show/Hide	C32H34Cl2FN3O2	1
1	Ki = 5.8 nM Bioactivity Info	TI LI LO TS
CP0057704 Compound Info	(1S,2R)-2-((4-acetamido-4-phenylpiperidin-1-yl)methyl)-N-benzyl-1-(3,4-dichlorophenyl)-N-methylcyclopropanecarboxamide Show/Hide	C32H35Cl2N3O2	1
1	Ki = 5.9 nM Bioactivity Info	TI LI LO TS
CP0498914 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-1-(3,4-dichlorophenyl)-N-[(2,4-dimethoxyphenyl)methyl]-N-methylcyclopropane-1-carboxamide Show/Hide	C34H39Cl2N3O4	1
1	Ki = 5.9 nM Bioactivity Info	TI LI LO TS
CP0409511 Compound Info	(1S,2R)-N-benzyl-1-(3,4-dichlorophenyl)-N-methyl-2-((4-phenyl-4-(piperidine-1-carbonyl)piperidin-1-yl)methyl)cyclopropanecarboxamide Show/Hide	C36H41Cl2N3O2	1
1	Ki = 6.1 nM Bioactivity Info	TI LI LO TS
CP0409512 Compound Info	(1S,2R)-1-(3,4-dichlorophenyl)-N-(4-fluorobenzyl)-N-methyl-2-((4-(2-(piperidin-1-yl)acetyl)piperazin-1-yl)methyl)cyclopropanecarboxamide Show/Hide	C30H37Cl2FN4O2	1
1	Ki = 7.3 nM Bioactivity Info	TI LI LO TS
CP0498916 Compound Info	(1S,2R)-2-((4-acetamido-4-phenylpiperidin-1-yl)methyl)-1-(3,4-dimethylphenyl)-N-(4-fluorobenzyl)-N-methylcyclopropanecarboxamide Show/Hide	C34H40FN3O2	1
1	Ki = 7.3 nM Bioactivity Info	TI LI LO TS
CP0513052 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-1-(3,4-dichlorophenyl)-N-methyl-N-[(4-methylphenyl)methyl]cyclopropane-1-carboxamide Show/Hide	C33H37Cl2N3O2	1
1	Ki = 7.5 nM Bioactivity Info	TI LI LO TS
CP0051744 Compound Info	(1S,2R)-1-(3,4-dichlorophenyl)-2-((4-(N,N-dimethylsulfamoyl)piperazin-1-yl)methyl)-N-(4-fluorobenzyl)-N-methylcyclopropanecarboxamide Show/Hide	C25H31Cl2FN4O3S	1
1	Ki = 7.6 nM Bioactivity Info	TI LI LO TS
CP0489232 Compound Info	(1S,2R)-N-benzyl-1-(3,4-dichlorophenyl)-N-methyl-2-((4-(methylsulfonamido)-4-phenylpiperidin-1-yl)methyl)cyclopropanecarboxamide Show/Hide	C31H35Cl2N3O3S	1
1	Ki = 7.8 nM Bioactivity Info	TI LI LO TS
CP0381520 Compound Info	(1S,2R)-2-((4-(2-(azepan-1-yl)acetyl)piperazin-1-yl)methyl)-1-(3,4-dichlorophenyl)-N-(4-fluorobenzyl)-N-methylcyclopropanecarboxamide Show/Hide	C31H39Cl2FN4O2	1
1	Ki = 8.7 nM Bioactivity Info	TI LI LO TS
CP0543425 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-N-[(4-chlorophenyl)methyl]-1-(3,4-dichlorophenyl)-N-methylcyclopropane-1-carboxamide Show/Hide	C32H34Cl3N3O2	1
1	Ki = 11 nM Bioactivity Info	TI LI LO TS
CP0381516 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-1-(3,4-dichlorophenyl)-N-[(3-fluorophenyl)methyl]-N-methylcyclopropane-1-carboxamide Show/Hide	C32H34Cl2FN3O2	1
1	Ki = 12 nM Bioactivity Info	TI LI LO TS
CP0477713 Compound Info	(1S,2R)-1-(3,4-dichlorophenyl)-N-(4-fluorobenzyl)-N-methyl-2-((4-(2-(pyrrolidin-1-yl)acetyl)piperazin-1-yl)methyl)cyclopropanecarboxamide Show/Hide	C29H35Cl2FN4O2	1
1	Ki = 12 nM Bioactivity Info	TI LI LO TS
CP0512755 Compound Info	(1S,2R)-N-benzyl-1-(3,4-dichlorophenyl)-N-methyl-2-((4-phenyl-4-ureidopiperidin-1-yl)methyl)cyclopropanecarboxamide Show/Hide	C31H34Cl2N4O2	1
1	Ki = 12 nM Bioactivity Info	TI LI LO TS
CP0498913 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-1-(3,4-dichlorophenyl)-N-[(3,4-dichlorophenyl)methyl]-N-methylcyclopropane-1-carboxamide Show/Hide	C32H33Cl4N3O2	1
1	Ki = 13 nM Bioactivity Info	TI LI LO TS
CP0543424 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-1-(3,4-dichlorophenyl)-N-[(2-methoxyphenyl)methyl]-N-methylcyclopropane-1-carboxamide Show/Hide	C33H37Cl2N3O3	1
1	Ki = 14 nM Bioactivity Info	TI LI LO TS
CP0543427 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-1-(3,4-dichlorophenyl)-N-methyl-N-(thiophen-3-ylmethyl)cyclopropane-1-carboxamide Show/Hide	C30H33Cl2N3O2S	1
1	Ki = 14 nM Bioactivity Info	TI LI LO TS
CP0487295 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-1-(3,4-dichlorophenyl)-N-[(4-methoxyphenyl)methyl]-N-methylcyclopropane-1-carboxamide Show/Hide	C33H37Cl2N3O3	1
1	Ki = 15 nM Bioactivity Info	TI LI LO TS
CP0512722 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-1-(3,4-dichlorophenyl)-N-[(2,4-dichlorophenyl)methyl]-N-methylcyclopropane-1-carboxamide Show/Hide	C32H33Cl4N3O2	1
1	Ki = 16 nM Bioactivity Info	TI LI LO TS
CP0469075 Compound Info	(1S,2R)-1-(3,4-dichlorophenyl)-2-((4-(3-(dimethylamino)-3-oxopropyl)piperazin-1-yl)methyl)-N-(4-fluorobenzyl)-N-methylcyclopropanecarboxamide Show/Hide	C28H35Cl2FN4O2	1
1	Ki = 17 nM Bioactivity Info	TI LI LO TS
CP0465489 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-1-(3,4-dichlorophenyl)-N-[(2-fluorophenyl)methyl]-N-methylcyclopropane-1-carboxamide Show/Hide	C32H34Cl2FN3O2	1
1	Ki = 18 nM Bioactivity Info	TI LI LO TS
CP0487294 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-N-[(2-chlorophenyl)methyl]-1-(3,4-dichlorophenyl)-N-methylcyclopropane-1-carboxamide Show/Hide	C32H34Cl3N3O2	1
1	Ki = 20 nM Bioactivity Info	TI LI LO TS
CP0438299 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-1-(3,4-dichlorophenyl)-N-[(3,5-dichlorophenyl)methyl]-N-methylcyclopropane-1-carboxamide Show/Hide	C32H33Cl4N3O2	1
1	Ki = 23 nM Bioactivity Info	TI LI LO TS
CP0426333 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-N-[(3-chlorophenyl)methyl]-1-(3,4-dichlorophenyl)-N-methylcyclopropane-1-carboxamide Show/Hide	C32H34Cl3N3O2	1
1	Ki = 24 nM Bioactivity Info	TI LI LO TS
CP0489227 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-1-(3,4-dichlorophenyl)-N-[(2,3-dichlorophenyl)methyl]-N-methylcyclopropane-1-carboxamide Show/Hide	C32H33Cl4N3O2	1
1	Ki = 24 nM Bioactivity Info	TI LI LO TS
CP0487296 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-1-(3,4-dichlorophenyl)-N-methyl-N-[(4-methylsulfanylphenyl)methyl]cyclopropane-1-carboxamide Show/Hide	C33H37Cl2N3O2S	1
1	Ki = 28 nM Bioactivity Info	TI LI LO TS
CP0378058 Compound Info	(1S,2R)-2-((4-acetamido-4-phenylpiperidin-1-yl)methyl)-1-(3-chlorophenyl)-N-(4-fluorobenzyl)-N-methylcyclopropanecarboxamide Show/Hide	C32H35ClFN3O2	1
1	Ki = 32 nM Bioactivity Info	TI LI LO TS
CP0543426 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-1-(3,4-dichlorophenyl)-N-[(3,5-dimethoxyphenyl)methyl]-N-methylcyclopropane-1-carboxamide Show/Hide	C34H39Cl2N3O4	1
1	Ki = 32 nM Bioactivity Info	TI LI LO TS
CP0505785 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-1-(3,4-dichlorophenyl)-N-[(3-methoxyphenyl)methyl]-N-methylcyclopropane-1-carboxamide Show/Hide	C33H37Cl2N3O3	1
1	Ki = 33 nM Bioactivity Info	TI LI LO TS
CP0377247 Compound Info	(1S,2R)-2-((4-acetamido-4-phenylpiperidin-1-yl)methyl)-1-(4-chlorophenyl)-N-(4-fluorobenzyl)-N-methylcyclopropanecarboxamide Show/Hide	C32H35ClFN3O2	1
1	Ki = 36 nM Bioactivity Info	TI LI LO TS
CP0509374 Compound Info	(1S,2R)-2-((4-acetamido-4-phenylpiperidin-1-yl)methyl)-N-(4-fluorobenzyl)-N-methyl-1-p-tolylcyclopropanecarboxamide Show/Hide	C33H38FN3O2	1
1	Ki = 37 nM Bioactivity Info	TI LI LO TS
CP0381518 Compound Info	(1S,2R)-2-((4-acetamido-4-phenylpiperidin-1-yl)methyl)-N-(4-fluorobenzyl)-N-methyl-1-m-tolylcyclopropanecarboxamide Show/Hide	C33H38FN3O2	1
1	Ki = 40 nM Bioactivity Info	TI LI LO TS
CP0489229 Compound Info	(1S,2R)-2-((4-acetamido-4-phenylpiperidin-1-yl)methyl)-1-(3,4-difluorophenyl)-N-(4-fluorobenzyl)-N-methylcyclopropanecarboxamide Show/Hide	C32H34F3N3O2	1
1	Ki = 47 nM Bioactivity Info	TI LI LO TS
CP0489225 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-1-(3,4-dichlorophenyl)-N-methyl-N-[[3-(trifluoromethyl)phenyl]methyl]cyclopropane-1-carboxamide Show/Hide	C33H34Cl2F3N3O2	1
1	Ki = 50 nM Bioactivity Info	TI LI LO TS
CP0404959 Compound Info	(1S,2R)-2-((4-acetamido-4-phenylpiperidin-1-yl)methyl)-N-(4-fluorobenzyl)-1-(3-methoxyphenyl)-N-methylcyclopropanecarboxamide Show/Hide	C33H38FN3O3	1
1	Ki = 56 nM Bioactivity Info	TI LI LO TS
CP0487297 Compound Info	(1S,2R)-2-((4-acetamido-4-phenylpiperidin-1-yl)methyl)-N-(4-fluorobenzyl)-1-(4-fluorophenyl)-N-methylcyclopropanecarboxamide Show/Hide	C32H35F2N3O2	1
1	Ki = 67 nM Bioactivity Info	TI LI LO TS
CP0512723 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-1-(3,4-dichlorophenyl)-N-[(3,4-dimethoxyphenyl)methyl]-N-methylcyclopropane-1-carboxamide Show/Hide	C34H39Cl2N3O4	1
1	Ki = 67 nM Bioactivity Info	TI LI LO TS
CP0498915 Compound Info	2-[(4-acetamido-4-phenylpiperidin-1-yl)methyl]-1-(3,4-dichlorophenyl)-N-methyl-N-(thiophen-2-ylmethyl)cyclopropane-1-carboxamide Show/Hide	C30H33Cl2N3O2S	1
1	Ki = 70 nM Bioactivity Info	TI LI LO TS
CP0505784 Compound Info	(1R,2S)-2-((4-acetamido-4-phenylpiperidin-1-yl)methyl)-N-benzyl-1-(3,4-dichlorophenyl)-N-methylcyclopropanecarboxamide Show/Hide	C32H35Cl2N3O2	1
1	Ki = 83 nM Bioactivity Info	TI LI LO TS
CP0489231 Compound Info	(1S,2R)-2-((4-acetamido-4-phenylpiperidin-1-yl)methyl)-1-(3,5-dichlorophenyl)-N-(4-fluorobenzyl)-N-methylcyclopropanecarboxamide Show/Hide	C32H34Cl2FN3O2	1
1	Ki = 90 nM Bioactivity Info	TI LI LO TS
CP0409510 Compound Info	(1S,2R)-2-((4-acetamido-4-phenylpiperidin-1-yl)methyl)-N-(4-fluorobenzyl)-N-methyl-1-(thiophen-2-yl)cyclopropanecarboxamide Show/Hide	C30H34FN3O2S	1
1	Ki = 93 nM Bioactivity Info	TI LI LO TS
CP0477712 Compound Info	(1S,2R)-2-((4-acetamido-4-phenylpiperidin-1-yl)methyl)-N-(4-fluorobenzyl)-N-methyl-1-(thiophen-3-yl)cyclopropanecarboxamide Show/Hide	C30H34FN3O2S	1
1	Ki = 110 nM Bioactivity Info	TI LI LO TS
CP0377248 Compound Info	(1S,2R)-2-((4-acetamido-4-phenylpiperidin-1-yl)methyl)-N-(4-fluorobenzyl)-1-(3-fluorophenyl)-N-methylcyclopropanecarboxamide Show/Hide	C32H35F2N3O2	1
1	Ki = 140 nM Bioactivity Info	TI LI LO TS
CP0438302 Compound Info	(1S,2R)-2-((4-acetamido-4-phenylpiperidin-1-yl)methyl)-1-(benzo[d][1,3]dioxol-5-yl)-N-(4-fluorobenzyl)-N-methylcyclopropanecarboxamide Show/Hide	C33H36FN3O4	1
1	Ki = 140 nM Bioactivity Info	TI LI LO TS
CP0509349 Compound Info	(1S,2R)-1-(3,4-dichlorophenyl)-N-(4-fluorobenzyl)-2-((isopropylamino)methyl)-N-methylcyclopropanecarboxamide Show/Hide	C22H25Cl2FN2O	1
1	Ki = 140 nM Bioactivity Info	TI LI LO TS
CP0498919 Compound Info	(1S,2R)-1-(3,4-dichlorophenyl)-N-(4-fluorobenzyl)-N-methyl-2-((propylamino)methyl)cyclopropanecarboxamide Show/Hide	C22H25Cl2FN2O	1
1	Ki = 150 nM Bioactivity Info	TI LI LO TS
CP0469074 Compound Info	(1S,2R)-2-((4-acetamido-4-phenylpiperidin-1-yl)methyl)-N-(4-fluorobenzyl)-N-methyl-1-(3-(trifluoromethyl)phenyl)cyclopropanecarboxamide Show/Hide	C33H35F4N3O2	1
1	Ki = 210 nM Bioactivity Info	TI LI LO TS
CP0489228 Compound Info	(1S,2R)-2-((4-acetamido-4-phenylpiperidin-1-yl)methyl)-1-(4-cyanophenyl)-N-(4-fluorobenzyl)-N-methylcyclopropanecarboxamide Show/Hide	C33H35FN4O2	1
1	Ki = 270 nM Bioactivity Info	TI LI LO TS
CP0438301 Compound Info	(1S,2R)-2-((4-acetamido-4-phenylpiperidin-1-yl)methyl)-N-(4-fluorobenzyl)-1-(4-methoxyphenyl)-N-methylcyclopropanecarboxamide Show/Hide	C33H38FN3O3	1
1	Ki = 350 nM Bioactivity Info	TI LI LO TS
CP0513053 Compound Info	(1S,2R)-2-((4-acetamido-4-phenylpiperidin-1-yl)methyl)-N-(4-fluorobenzyl)-N-methyl-1-(4-(trifluoromethyl)phenyl)cyclopropanecarboxamide Show/Hide	C33H35F4N3O2	1
1	Ki = 1000 nM Bioactivity Info	TI LI LO TS
CP0409508 Compound Info	(1S,2R)-2-((4-acetamido-4-phenylpiperidin-1-yl)methyl)-1-(3-cyanophenyl)-N-(4-fluorobenzyl)-N-methylcyclopropanecarboxamide Show/Hide	C33H35FN4O2	1
1	Ki = 1900 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000011 , CHO

Cell Line Info

Cell Line ID: CL000026 , CHO-K1

Cell Line Info

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000065 , HEK293-EBNA

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0058365 Compound Info	methyl N-[(3-methoxy-2-phenylquinoline-4-carbonyl)amino]-N-phenylcarbamate Show/Hide	C25H21N3O4	1
1	IC50 = 4.5 nM
CP0044631 Compound Info	(S)-3-methyl-2-phenyl-N-(1-phenylpropyl)quinoline-4-carboxamide Show/Hide	C26H24N2O	6
1	IC50 = 7.1 nM
2	IC50 = 8.8 nM
3	IC50 = 15 nM
4	Ki = 3.8 nM
5	Ki = 7.943 nM
6	Ki = 8.3 nM
CP0290288 Compound Info	tert-butyl N-[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate Show/Hide	C23H29N3O4	1
1	IC50 = 1600 nM
CP0117145 Compound Info	tert-butyl N-[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]carbamate Show/Hide	C25H30N4O4	1
1	IC50 = 3000 nM
CP0074738 Compound Info	(S)-(+)-N-((3-[1-Benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl]prop-1-yl)-4-phenylpiperidin-4-yl)-N-methylacetamine Show/Hide	C35H41Cl2N3O2	2
1	Ki = 0.1995 nM
2	Ki = 1.9 nM
CP0204318 Compound Info	(5S,8S,14S,17S,20S,23S,26S,29S,32S)-26-((1H-imidazol-5-yl)methyl)-32-amino-14,17,20-tribenzyl-5-carbamoyl-23-(carboxymethyl)-8-isobutyl-15-methyl-29-(2-(methylthio)ethyl)-7,10,13,16,19,22,25,28,31-nonaoxo-2-thia-6,9,12,15,18,21,24,27,30-nonaazatetratriacontan-34-oic acid Show/Hide	C60H81N13O14S2	1
1	Ki = 0.3 nM
CP0074740 Compound Info	[(8R)-3-[2-(2,4-difluorophenyl)-1,3-thiazol-4-yl]-8-methyl-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanone Show/Hide	C26H19F2N5OS2	1
1	Ki = 1.995 nM
CP0282991 Compound Info	2-[3,5-bis(trifluoromethyl)phenyl]-N-[4-(4-fluoro-2-methylphenyl)-6-[(2R,3S)-3-hydroxy-2-(hydroxymethyl)pyrrolidin-1-yl]pyridin-3-yl]-N,2-dimethylpropanamide Show/Hide	C30H30F7N3O3	1
1	Ki = 2.9 nM
CP0114969 Compound Info	[(8R)-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanone Show/Hide	C20H18N6OS2	1
1	Ki = 3.162 nM
CP0114970 Compound Info	(S)-(-)-N-(R-ethylbenzyl)-3-hydroxy-2-phenylquinoline-4-carboxamide Show/Hide	C25H22N2O2	1
1	Ki = 7.4 nM
CP0126344 Compound Info	(4-fluorophenyl)-[(8R)-8-methyl-3-[3-(trifluoromethyl)-1,2,4-thiadiazol-5-yl]-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanone Show/Hide	C16H12F4N6OS	1
1	Ki = 7.943 nM
CP0088854 Compound Info	[(8R)-8-methyl-3-(2-methyl-1,3-thiazol-4-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanone Show/Hide	C21H19N5OS2	1
1	Ki = 12.59 nM
CP0212153 Compound Info	(4-chlorophenyl)-[(8R)-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanone Show/Hide	C16H15ClN6OS	1
1	Ki = 19.95 nM
CP0112422 Compound Info	(4-fluorophenyl)-[(8R)-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanone Show/Hide	C16H15FN6OS	1
1	Ki = 25.12 nM
CP0126339 Compound Info	(4-fluorophenyl)-[(8R)-8-methyl-3-(3-propan-2-yl-1,2,4-oxadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanone Show/Hide	C18H19FN6O2	1
1	Ki = 25.12 nM
CP0126108 Compound Info	(4-fluorophenyl)-[(8R)-8-(2-hydroxyethyl)-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanone Show/Hide	C17H17FN6O2S	1
1	Ki = 31.62 nM
CP0147959 Compound Info	[(8R)-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-phenylmethanone Show/Hide	C16H16N6OS	1
1	Ki = 50.12 nM
CP0215350 Compound Info	(4-fluorophenyl)-[3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanone Show/Hide	C15H13FN6OS	1
1	Ki = 100 nM
CP0120396 Compound Info	(4-fluorophenyl)-[(8R)-8-methyl-3-(3-methyl-1,2,4-oxadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanone Show/Hide	C16H15FN6O2	1
1	Ki = 125.89 nM
CP0220343 Compound Info	[8,8-dimethyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-fluorophenyl)methanone Show/Hide	C17H17FN6OS	1
1	Ki = 199.53 nM
CP0142900 Compound Info	(5-(4-chlorophenyl)-1-methyl-1H-pyrazol-3-yl)(4-(2-methoxyphenyl)piperazin-1-yl)methanone Show/Hide	C22H23ClN4O2	1
1	Ki = 370 nM
CP0142901 Compound Info	(3-(4-chlorophenyl)-1-methyl-1H-pyrazol-5-yl)(4-(2-methoxyphenyl)piperazin-1-yl)methanone Show/Hide	C22H23ClN4O2	1
1	Ki = 540 nM
CP0064950 Compound Info	(4-fluorophenyl)-[(8R)-8-methyl-3-(1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanone Show/Hide	C15H13FN6OS	1
1	Ki = 1258.93 nM
CP0326360 Compound Info	(2S)-N-[(4-chlorophenyl)methyl]-2-(3,4-dichlorophenyl)-4-(6-fluoro-1-methyl-2-oxospiro[3,1-benzoxazine-4,4'-piperidine]-1'-yl)-N-methylbutanamide Show/Hide	C31H31Cl3FN3O3	1
1	Ki = 3981.07 nM
CP0247643 Compound Info	4-[4-[acetyl(propyl)amino]piperidin-1-yl]-2-(3,4-dichlorophenyl)-N-[(1R)-1-(4-fluorophenyl)-2-hydroxyethyl]-2-methylbutanamide Show/Hide	C29H38Cl2FN3O3	1
1	Ki = 5011.87 nM
CP0120399 Compound Info	(4-fluorophenyl)-[(8R)-8-methyl-3-(5-methyl-1,3,4-thiadiazol-2-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanone Show/Hide	C16H15FN6OS	1
1	Ki = 10000 nM

Clinical Information about the Protein

Target 1 ( Neuromedin-K receptor (TACR3) )

Target Type	Successful Target
Disease	6 Target-related Diseases				6
1	Hot flushes [ICD-11: GA30]
2	Ischemic stroke [ICD-11: 8B11.5Z]
3	Schizoaffective disorder [ICD-11: 6A21]
4	Multiple sclerosis [ICD-11: 8A40]
5	Schizophrenia [ICD-11: 6A20]
6	Asthma [ICD-11: CA23]
Approved Drug(s)	1 Approved Drug				1
1	Fezolinetant	Drug Info	Approved	Hot flushes
Clinical Trial Drug(s)	3 Clinical Trial Drugs				3
1	Senktide	Drug Info	Phase 2	Ischemic stroke
2	AZD2624	Drug Info	Phase 2	Multiple sclerosis
3	Talnetant	Drug Info	Phase 2	Schizophrenia
Discontinued Drug(s)	1 Discontinued Drug				1
1	Osanetant	Drug Info	Discontinued in Phase 2b	Schizoaffective disorder
Investigative Drug(s)	1 Investigative Drug				1
1	GSK-172981	Drug Info	Investigative	Asthma
Preclinical Drug(s)	1 Preclinical Drug				1
1	SB222200	Drug Info	Preclinical	Schizoaffective disorder

Similar Protein(s) and Bioactivity Statistics

50% Identity

Protein ID	Protein Name	Protein Organism
PT04126	Neuromedin-K receptor	Rattus norvegicus, Rat	Protein Info

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han