Protein Information

General Information of the Protein

Protein ID	PT04369
Protein Name	Mas-related G-protein coupled receptor member X1
Secondarily Protein Name	Sensory neuron-specific G-protein coupled receptor 3/4
Gene Name	MRGPRX1
Secondarily Gene Name	MRGX1 SNSR3 SNSR4
Sequence	MDPTISTLDTELTPINGTEETLCYKQTLSLTVLTCIVSLVGLTGNAVVLWLLGCRMRRNAFSIYILNLAAADFLFLSGRLIYSLLSFISIPHTISKILYPVMMFSYFAGLSFLSAVSTERCLSVLWPIWYRCHRPTHLSAVVCVLLWALSLLRSILEWMLCGFLFSGADSAWCQTSDFITVAWLIFLCVVLCGSSLVLLIRILCGSRKIPLTRLYVTILLTVLVFLLCGLPFGIQFFLFLWIHVDREVLFCHVHLVSIFLSALNSSANPIIYFFVGSFRQRQNRQNLKLVLQRALQDASEVDEGGGQLPEEILELSGSRLEQ Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Membrane receptor > Family A G protein-coupled receptor
Function	Orphan receptor. Probably involved in the function of nociceptive neurons. May regulate nociceptor function and/or development, including the sensation or modulation of pain. Potently activated by enkephalins including BAM22 (bovine adrenal medulla peptide 22) and BAM (8-22)(PubMed:26582731). BAM22 is the most potent compound and evoked a large and dose-dependent release of intracellular calcium in stably transfected cells. G(alpha)q proteins are involved in the calcium-signaling pathway. Activated by the antimalarial drug, chloroquine. May mediate chloroquine-induced itch, in a histamine-independent manner. Show/Hide
Uniprot ID	Primary ID: Q96LB2 Secondarily ID: Q4V9L2 Q8TDD8 Q8TDD9 Show/Hide
HGNC ID	HGNC:17962
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: CL000006 , HEK293

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0071244 Compound Info	4-(6-methoxypyridin-3-yl)-N-[2-methyl-3-[(6-oxo-4-piperazin-1-ylpyridazin-1-yl)methyl]phenyl]benzamide Show/Hide	C29H30N6O3	2
1	EC50 = 6.31 nM Bioactivity Info	TI LI LO TS
2	EC50 = 25.12 nM Bioactivity Info	TI LI LO TS
CP0568391 Compound Info	2-(cyclopropylsulfonylamino)-N-(2-ethoxy-5-fluorophenyl)-5-fluorobenzamide Show/Hide	C18H18F2N2O4S	1
1	EC50 = 13 nM Bioactivity Info	TI LI LO TS
CP0568389 Compound Info	2-(cyclopropylsulfonylamino)-N-(2-ethoxy-5-fluorophenyl)benzamide Show/Hide	C18H19FN2O4S	1
1	EC50 = 14 nM Bioactivity Info	TI LI LO TS
CP0428411 Compound Info	N-[2-methyl-3-[(6-oxo-4-piperazin-1-ylpyridazin-1-yl)methyl]phenyl]-4-phenylbenzamide Show/Hide	C29H29N5O2	1
1	EC50 = 19.95 nM Bioactivity Info	TI LI LO TS
CP0388361 Compound Info	N-[3-[(5-chloro-6-oxo-4-piperazin-1-ylpyridazin-1-yl)methyl]-2-methylphenyl]-4-(6-methoxypyridin-3-yl)benzamide Show/Hide	C29H29ClN6O3	1
1	EC50 = 23.99 nM Bioactivity Info	TI LI LO TS
CP0577373 Compound Info	N-(2-ethoxy-5-fluorophenyl)-2-(ethylsulfonylamino)-5-fluorobenzamide Show/Hide	C17H18F2N2O4S	1
1	EC50 = 31 nM Bioactivity Info	TI LI LO TS
CP0458062 Compound Info	N-[2-(1-aminoisoquinolin-6-yl)oxy-4-methylphenyl]-2-methoxybenzenesulfonamide Show/Hide	C23H21N3O4S	1
1	EC50 = 50 nM Bioactivity Info	TI LI LO TS
CP0719182 Compound Info	(5S,8S,11S,14S,17S,20S,23S,26S,29S,32S)-26,29-bis((1H-indol-3-yl)methyl)-32-((S)-1-((S)-2-(2-((S)-2-amino-3-methylbutanamido)acetamido)-5-guanidinopentanoyl)pyrrolidine-2-carboxamido)-14-(3-amino-3-oxopropyl)-11-(4-aminobutyl)-20-(carboxymethyl)-8-(3-guanidinopropyl)-5,17-bis(4-hydroxybenzyl)-23-(2-(methylthio)ethyl)-4,7,10,13,16,19,22,25,28,31-decaoxo-3,6,9,12,15,18,21,24,27,30-decaazapentatriacontane-1,35-dioic acid Show/Hide	C91H127N25O23S	1
1	EC50 = 50.12 nM Bioactivity Info	TI LI LO TS
CP0399908 Compound Info	3-[4-[[3-[(5-chloro-6-oxo-4-piperazin-1-ylpyridazin-1-yl)methyl]-2-methylphenyl]carbamoyl]phenyl]benzamide Show/Hide	C30H29ClN6O3	1
1	EC50 = 52.48 nM Bioactivity Info	TI LI LO TS
CP0574519 Compound Info	5-chloro-2-(cyclopropylsulfonylamino)-N-(2-ethoxyphenyl)benzamide Show/Hide	C18H19ClN2O4S	1
1	EC50 = 54 nM Bioactivity Info	TI LI LO TS
CP0572993 Compound Info	5-chloro-2-(cyclopropylsulfonylamino)-N-(2-ethoxy-5-fluorophenyl)benzamide Show/Hide	C18H18ClFN2O4S	1
1	EC50 = 55 nM Bioactivity Info	TI LI LO TS
CP0570230 Compound Info	2-(cyclopropylsulfonylamino)-N-(2-ethoxy-5-fluorophenyl)-5-methylbenzamide Show/Hide	C19H21FN2O4S	1
1	EC50 = 69 nM Bioactivity Info	TI LI LO TS
CP0576374 Compound Info	N-(2-ethoxy-5-fluorophenyl)-2-(ethylsulfonylamino)-5-methylbenzamide Show/Hide	C18H21FN2O4S	1
1	EC50 = 80 nM Bioactivity Info	TI LI LO TS
CP0504261 Compound Info	N-[3-[[5-chloro-4-(1,4-diazepan-1-yl)-6-oxopyridazin-1-yl]methyl]-2-methylphenyl]-4-(6-methoxypyridin-3-yl)benzamide Show/Hide	C30H31ClN6O3	1
1	EC50 = 81.28 nM Bioactivity Info	TI LI LO TS
CP0570354 Compound Info	N-(2-ethoxyphenyl)-2-(ethylsulfonylamino)-5-fluorobenzamide Show/Hide	C17H19FN2O4S	1
1	EC50 = 98 nM Bioactivity Info	TI LI LO TS
CP0561756 Compound Info	4-[2-[(2-methoxyphenyl)sulfonylamino]-5-methylphenoxy]benzenecarboximidamide Show/Hide	C21H21N3O4S	1
1	EC50 = 100 nM Bioactivity Info	TI LI LO TS
CP0488262 Compound Info	6-tert-butyl-5-(3,4-dichlorophenyl)-4-[2-(trifluoromethoxy)phenoxy]thieno[2,3-d]pyrimidine Show/Hide	C23H17Cl2F3N2O2S	1
1	EC50 = 100 nM Bioactivity Info	TI LI LO TS
CP0543887 Compound Info	2-(cyclopropylsulfonylamino)-N-(2-ethoxyphenyl)-5-methylbenzamide Show/Hide	C19H22N2O4S	1
1	EC50 = 103 nM Bioactivity Info	TI LI LO TS
CP0507940 Compound Info	N-[3-[[5-chloro-4-[(1S,4R)-5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl]-6-oxopyridazin-1-yl]methyl]-2-methylphenyl]-4-(6-methoxypyridin-3-yl)benzamide Show/Hide	C31H31ClN6O3	1
1	EC50 = 107.15 nM Bioactivity Info	TI LI LO TS
CP0475898 Compound Info	N-[3-[[5-chloro-4-(4-methylpiperazin-1-yl)-6-oxopyridazin-1-yl]methyl]-2-methylphenyl]-4-(6-methoxypyridin-3-yl)benzamide Show/Hide	C30H31ClN6O3	1
1	EC50 = 123.03 nM Bioactivity Info	TI LI LO TS
CP0543882 Compound Info	2-(cyclopropylsulfonylamino)-N-(2-ethoxyphenyl)benzamide Show/Hide	C18H20N2O4S	1
1	EC50 = 124 nM Bioactivity Info	TI LI LO TS
CP0388360 Compound Info	N-[3-[(5-chloro-6-oxo-4-piperazin-1-ylpyridazin-1-yl)methyl]-2-methylphenyl]-4-phenylbenzamide Show/Hide	C29H28ClN5O2	1
1	EC50 = 125.89 nM Bioactivity Info	TI LI LO TS
CP0444837 Compound Info	N-[3-[(5-chloro-6-oxo-4-piperazin-1-ylpyridazin-1-yl)methyl]-2-methylphenyl]-4-quinolin-6-ylbenzamide Show/Hide	C32H29ClN6O2	1
1	EC50 = 131.83 nM Bioactivity Info	TI LI LO TS
CP0504262 Compound Info	N-[3-[(5-chloro-6-oxo-4-piperazin-1-ylpyridazin-1-yl)methyl]-2-methylphenyl]-4-thiophen-3-ylbenzamide Show/Hide	C27H26ClN5O2S	1
1	EC50 = 144.54 nM Bioactivity Info	TI LI LO TS
CP0537760 Compound Info	4-[5-methyl-2-[[2-(trifluoromethoxy)phenyl]sulfonylamino]phenoxy]benzenecarboximidamide Show/Hide	C21H18F3N3O4S	1
1	EC50 = 150 nM Bioactivity Info	TI LI LO TS
CP0455793 Compound Info	4-[5-methyl-2-[(4-methylphenyl)sulfonylamino]phenoxy]benzenecarboximidamide Show/Hide	C21H21N3O3S	1
1	EC50 = 160 nM Bioactivity Info	TI LI LO TS
CP0543775 Compound Info	2-(cyclopropylsulfonylamino)-N-(2-ethoxyphenyl)-5-fluorobenzamide Show/Hide	C18H19FN2O4S	1
1	EC50 = 173 nM Bioactivity Info	TI LI LO TS
CP0543883 Compound Info	5-chloro-N-(2-ethoxy-5-fluorophenyl)-2-(ethylsulfonylamino)benzamide Show/Hide	C17H18ClFN2O4S	1
1	EC50 = 206 nM Bioactivity Info	TI LI LO TS
CP0568390 Compound Info	N-(2-ethoxyphenyl)-2-(ethylsulfonylamino)-5-methylbenzamide Show/Hide	C18H22N2O4S	1
1	EC50 = 217 nM Bioactivity Info	TI LI LO TS
CP0532501 Compound Info	4-(2-fluorophenoxy)-5,6-dimethylthieno[2,3-d]pyrimidine Show/Hide	C14H11FN2OS	1
1	EC50 = 220 nM Bioactivity Info	TI LI LO TS
CP0546293 Compound Info	6-tert-butyl-5-(4-fluorophenyl)-4-[2-(trifluoromethoxy)phenoxy]thieno[2,3-d]pyrimidine Show/Hide	C23H18F4N2O2S	1
1	EC50 = 230 nM Bioactivity Info	TI LI LO TS
CP0576375 Compound Info	N-(2-ethoxy-5-fluorophenyl)-2-(ethylsulfonylamino)benzamide Show/Hide	C17H19FN2O4S	1
1	EC50 = 285 nM Bioactivity Info	TI LI LO TS
CP0434313 Compound Info	N-[3-[(5-chloro-6-oxo-4-piperazin-1-ylpyridazin-1-yl)methyl]-2-methylphenyl]-4-quinolin-8-ylbenzamide Show/Hide	C32H29ClN6O2	1
1	EC50 = 288.4 nM Bioactivity Info	TI LI LO TS
CP0551521 Compound Info	4-[[3-methoxy-4-(thiophen-3-ylmethoxy)phenyl]methylamino]benzenecarboximidamide Show/Hide	C20H21N3O2S	1
1	EC50 = 290 nM Bioactivity Info	TI LI LO TS
CP0475009 Compound Info	N-[3-[[5-chloro-4-[2-(methylamino)ethylamino]-6-oxopyridazin-1-yl]methyl]-2-methylphenyl]-4-(6-methoxypyridin-3-yl)benzamide Show/Hide	C28H29ClN6O3	1
1	EC50 = 295.12 nM Bioactivity Info	TI LI LO TS
CP0423671 Compound Info	4-[2-(butylsulfonylamino)phenoxy]benzenecarboximidamide Show/Hide	C17H21N3O3S	1
1	EC50 = 300 nM Bioactivity Info	TI LI LO TS
CP0488264 Compound Info	6-tert-butyl-4-(2-fluorophenoxy)-5-(4-fluorophenyl)thieno[2,3-d]pyrimidine Show/Hide	C22H18F2N2OS	1
1	EC50 = 300 nM Bioactivity Info	TI LI LO TS
CP0567734 Compound Info	6-tert-butyl-4-(2-fluorophenoxy)thieno[2,3-d]pyrimidine Show/Hide	C16H15FN2OS	1
1	EC50 = 320 nM Bioactivity Info	TI LI LO TS
CP0573247 Compound Info	6-tert-butyl-4-(2-fluorophenoxy)-5-phenylthieno[2,3-d]pyrimidine Show/Hide	C22H19FN2OS	1
1	EC50 = 340 nM Bioactivity Info	TI LI LO TS
CP0576373 Compound Info	5-chloro-2-(ethylsulfonylamino)-N-[2-(2,2,2-trifluoroethoxy)phenyl]benzamide Show/Hide	C17H16ClF3N2O4S	1
1	EC50 = 366 nM Bioactivity Info	TI LI LO TS
CP0576376 Compound Info	2-(cyclopropylsulfonylamino)-5-methyl-N-[2-(2,2,2-trifluoroethoxy)phenyl]benzamide Show/Hide	C19H19F3N2O4S	1
1	EC50 = 369 nM Bioactivity Info	TI LI LO TS
CP0428412 Compound Info	N-[3-[(5-chloro-6-oxo-4-piperazin-1-ylpyridazin-1-yl)methyl]-2-methylphenyl]-4-[3-(dimethylamino)phenyl]benzamide Show/Hide	C31H33ClN6O2	1
1	EC50 = 398.11 nM Bioactivity Info	TI LI LO TS
CP0576378 Compound Info	5-chloro-N-(2-ethoxyphenyl)-2-(ethylsulfonylamino)benzamide Show/Hide	C17H19ClN2O4S	1
1	EC50 = 407 nM Bioactivity Info	TI LI LO TS
CP0576764 Compound Info	2-(ethylsulfonylamino)-5-fluoro-N-[2-(2,2,2-trifluoroethoxy)phenyl]benzamide Show/Hide	C17H16F4N2O4S	1
1	EC50 = 435 nM Bioactivity Info	TI LI LO TS
CP0488722 Compound Info	5,6-dimethyl-4-(2-methylphenoxy)thieno[2,3-d]pyrimidine Show/Hide	C15H14N2OS	1
1	EC50 = 480 nM Bioactivity Info	TI LI LO TS
CP0580002 Compound Info	2-(cyclopropylsulfonylamino)-N-[2-(2,2,2-trifluoroethoxy)phenyl]benzamide Show/Hide	C18H17F3N2O4S	1
1	EC50 = 502 nM Bioactivity Info	TI LI LO TS
CP0543773 Compound Info	2-(cyclopropylsulfonylamino)-N-(2-propoxyphenyl)benzamide Show/Hide	C19H22N2O4S	1
1	EC50 = 506 nM Bioactivity Info	TI LI LO TS
CP0078232 Compound Info	4-({[4-(benzyloxy)-3-methoxyphenyl]methyl}amino)benzene-1-carboximidamide Show/Hide	C22H23N3O2	1
1	EC50 = 510 nM Bioactivity Info	TI LI LO TS
CP0542656 Compound Info	5,6-dimethyl-4-[2-(trifluoromethyl)phenoxy]thieno[2,3-d]pyrimidine Show/Hide	C15H11F3N2OS	1
1	EC50 = 520 nM Bioactivity Info	TI LI LO TS
CP0399907 Compound Info	N-[3-[(5-chloro-6-oxo-4-piperazin-1-ylpyridazin-1-yl)methyl]-2-methylphenyl]-4-thiophen-2-ylbenzamide Show/Hide	C27H26ClN5O2S	1
1	EC50 = 588.84 nM Bioactivity Info	TI LI LO TS
CP0476909 Compound Info	4-[[3-methoxy-4-[(4-pyrrol-1-ylphenyl)methoxy]phenyl]methylamino]benzenecarboximidamide Show/Hide	C26H26N4O2	1
1	EC50 = 680 nM Bioactivity Info	TI LI LO TS
CP0521474 Compound Info	BAM-3200 Show/Hide	C147H207N41O34S2	1
1	EC50 = 794.33 nM Bioactivity Info	TI LI LO TS
CP0569421 Compound Info	2-(cyclopropylsulfonylamino)-N-(2-ethoxyphenyl)-4-fluorobenzamide Show/Hide	C18H19FN2O4S	1
1	EC50 = 860 nM Bioactivity Info	TI LI LO TS
CP0576377 Compound Info	5-chloro-2-(cyclopropylsulfonylamino)-N-[2-(2,2,2-trifluoroethoxy)phenyl]benzamide Show/Hide	C18H16ClF3N2O4S	1
1	EC50 = 915 nM Bioactivity Info	TI LI LO TS
CP0482743 Compound Info	4-[2-(butylsulfonylamino)-4-methylphenoxy]benzenecarboximidamide Show/Hide	C18H23N3O3S	1
1	EC50 = 920 nM Bioactivity Info	TI LI LO TS
CP0579869 Compound Info	2-(cyclopropylsulfonylamino)-N-(2-methyl-1-benzofuran-7-yl)benzamide Show/Hide	C19H18N2O4S	1
1	EC50 = 1040 nM Bioactivity Info	TI LI LO TS
CP0543774 Compound Info	2-(cyclopropylsulfonylamino)-N-(2,4-diethoxyphenyl)benzamide Show/Hide	C20H24N2O5S	1
1	EC50 = 1090 nM Bioactivity Info	TI LI LO TS
CP0542628 Compound Info	4-(4-fluorophenoxy)-5,6-dimethylthieno[2,3-d]pyrimidine Show/Hide	C14H11FN2OS	1
1	EC50 = 1100 nM Bioactivity Info	TI LI LO TS
CP0577389 Compound Info	N-[2-(cyclopropylmethoxy)phenyl]-2-(cyclopropylsulfonylamino)benzamide Show/Hide	C20H22N2O4S	1
1	EC50 = 1360 nM Bioactivity Info	TI LI LO TS
CP0579572 Compound Info	2-(ethylsulfonylamino)-N-[4-fluoro-2-(2,2,2-trifluoroethoxy)phenyl]benzamide Show/Hide	C17H16F4N2O4S	1
1	EC50 = 1400 nM Bioactivity Info	TI LI LO TS
CP0527825 Compound Info	4-(2-fluorophenoxy)-6-methylthieno[2,3-d]pyrimidine Show/Hide	C13H9FN2OS	1
1	EC50 = 1500 nM Bioactivity Info	TI LI LO TS
CP0534019 Compound Info	5,6-dimethyl-4-phenoxythieno[2,3-d]pyrimidine Show/Hide	C14H12N2OS	1
1	EC50 = 1600 nM Bioactivity Info	TI LI LO TS
CP0569903 Compound Info	4-(2-fluorophenoxy)-5-methylthieno[2,3-d]pyrimidine Show/Hide	C13H9FN2OS	1
1	EC50 = 1700 nM Bioactivity Info	TI LI LO TS
CP0531956 Compound Info	4-[[3-methoxy-4-(3-methylbutoxy)phenyl]methylamino]benzenecarboximidamide Show/Hide	C20H27N3O2	1
1	EC50 = 1900 nM Bioactivity Info	TI LI LO TS
CP0427785 Compound Info	4-[2-[(4-fluorophenyl)sulfonylamino]-5-methylphenoxy]benzenecarboximidamide Show/Hide	C20H18FN3O3S	1
1	EC50 = 2100 nM Bioactivity Info	TI LI LO TS
CP0542629 Compound Info	4-(2-fluorophenoxy)-5-(trifluoromethyl)thieno[2,3-d]pyrimidine Show/Hide	C13H6F4N2OS	1
1	EC50 = 2100 nM Bioactivity Info	TI LI LO TS
CP0475010 Compound Info	N-[3-[[5-chloro-4-[3-(methylamino)pyrrolidin-1-yl]-6-oxopyridazin-1-yl]methyl]-2-methylphenyl]-4-(6-methoxypyridin-3-yl)benzamide Show/Hide	C30H31ClN6O3	1
1	EC50 = 2137.96 nM Bioactivity Info	TI LI LO TS
CP0438694 Compound Info	4-[2-(butylsulfonylamino)-5-methylphenoxy]benzenecarboximidamide Show/Hide	C18H23N3O3S	1
1	EC50 = 2200 nM Bioactivity Info	TI LI LO TS
CP0428413 Compound Info	N-[3-[(5-chloro-6-oxo-4-piperazin-1-ylpyridazin-1-yl)methyl]-2-methylphenyl]-1-(4-cyanophenyl)piperidine-4-carboxamide Show/Hide	C29H32ClN7O2	1
1	EC50 = 2691.53 nM Bioactivity Info	TI LI LO TS
CP0558302 Compound Info	5,6-dimethyl-4-(4-methylphenoxy)thieno[2,3-d]pyrimidine Show/Hide	C15H14N2OS	1
1	EC50 = 2700 nM Bioactivity Info	TI LI LO TS
CP0569419 Compound Info	2-(cyclopropylsulfonylamino)-N-(2-propan-2-yloxyphenyl)benzamide Show/Hide	C19H22N2O4S	1
1	EC50 = 2830 nM Bioactivity Info	TI LI LO TS
CP0570352 Compound Info	N-(2-cyclopentyloxyphenyl)-2-(cyclopropylsulfonylamino)benzamide Show/Hide	C21H24N2O4S	1
1	EC50 = 3140 nM Bioactivity Info	TI LI LO TS
CP0531955 Compound Info	3-[(3-methoxy-4-phenylmethoxyphenyl)methylamino]benzenecarboximidamide Show/Hide	C22H23N3O2	1
1	EC50 = 3300 nM Bioactivity Info	TI LI LO TS
CP0531957 Compound Info	3-[2-[(2-methoxyphenyl)sulfonylamino]-5-methylphenoxy]benzenecarboximidamide Show/Hide	C21H21N3O4S	1
1	EC50 = 3600 nM Bioactivity Info	TI LI LO TS
CP0432763 Compound Info	6-N-[(3-methoxy-4-phenylmethoxyphenyl)methyl]isoquinoline-1,6-diamine Show/Hide	C24H23N3O2	1
1	EC50 = 3700 nM Bioactivity Info	TI LI LO TS
CP0399906 Compound Info	N-[5-[(5-chloro-6-oxo-4-piperazin-1-ylpyridazin-1-yl)methyl]-2-methylphenyl]-4-phenylbenzamide Show/Hide	C29H28ClN5O2	1
1	EC50 = 4073.8 nM Bioactivity Info	TI LI LO TS
CP0490687 Compound Info	N-[3-[(5-chloro-6-oxo-4-piperazin-1-ylpyridazin-1-yl)methyl]-2-methylphenyl]-3-thiophen-3-ylbenzamide Show/Hide	C27H26ClN5O2S	1
1	EC50 = 4168.69 nM Bioactivity Info	TI LI LO TS
CP0546292 Compound Info	4-(2-fluorophenoxy)thieno[2,3-d]pyrimidine Show/Hide	C12H7FN2OS	1
1	EC50 = 4200 nM Bioactivity Info	TI LI LO TS
CP0455792 Compound Info	4-[[3-methoxy-4-(pyridin-3-ylmethoxy)phenyl]methylamino]benzenecarboximidamide Show/Hide	C21H22N4O2	1
1	EC50 = 5200 nM Bioactivity Info	TI LI LO TS
CP0458061 Compound Info	4-[(4-phenylmethoxyphenyl)methylamino]benzenecarboximidamide Show/Hide	C21H21N3O	1
1	EC50 = 5200 nM Bioactivity Info	TI LI LO TS
CP0521473 Compound Info	N-[3-[[5-chloro-4-(3,5-dimethylpiperazin-1-yl)-6-oxopyridazin-1-yl]methyl]-2-methylphenyl]-4-(6-methoxypyridin-3-yl)benzamide Show/Hide	C31H33ClN6O3	1
1	EC50 = 5754.4 nM Bioactivity Info	TI LI LO TS
CP0444836 Compound Info	4-[5-chloro-1-[[3-[[4-(6-methoxypyridin-3-yl)benzoyl]amino]-2-methylphenyl]methyl]-6-oxopyridazin-4-yl]piperazine-2-carboxamide Show/Hide	C30H30ClN7O4	1
1	EC50 = 7079.46 nM Bioactivity Info	TI LI LO TS
CP0475897 Compound Info	N-[3-[(5-chloro-6-oxo-4-piperazin-1-ylpyridazin-1-yl)methyl]-2-methylphenyl]-3-thiophen-2-ylbenzamide Show/Hide	C27H26ClN5O2S	1
1	EC50 = 8128.31 nM Bioactivity Info	TI LI LO TS
CP0388359 Compound Info	N-[3-[(5-chloro-6-oxo-4-piperazin-1-ylpyridazin-1-yl)methyl]phenyl]-4-phenylbenzamide Show/Hide	C28H26ClN5O2	1
1	EC50 = 8317.64 nM Bioactivity Info	TI LI LO TS
CP0552121 Compound Info	2-(cyclopropylsulfonylamino)-N-(2,3-dihydro-1,4-benzodioxin-5-yl)benzamide Show/Hide	C18H18N2O5S	1
1	EC50 = 9010 nM Bioactivity Info	TI LI LO TS
CP0518435 Compound Info	N-[3-[(5-chloro-6-oxo-4-piperazin-1-ylpyridazin-1-yl)methyl]-2-methylphenyl]-2,2-diphenylacetamide Show/Hide	C30H30ClN5O2	1
1	EC50 = 10964.78 nM Bioactivity Info	TI LI LO TS
CP0543886 Compound Info	N-(1-benzofuran-4-yl)-2-(cyclopropylsulfonylamino)benzamide Show/Hide	C18H16N2O4S	1
1	EC50 = 14200 nM Bioactivity Info	TI LI LO TS
CP0332608 Compound Info	4-(2-methylphenoxy)thieno[2,3-d]pyrimidine Show/Hide	C13H10N2OS	1
1	EC50 = 14500 nM Bioactivity Info	TI LI LO TS
CP0475011 Compound Info	N-[3-[(5-chloro-6-oxo-4-piperazin-1-ylpyridazin-1-yl)methyl]-2-methylphenyl]pyridine-3-carboxamide Show/Hide	C22H23ClN6O2	1
1	EC50 = 19952.62 nM Bioactivity Info	TI LI LO TS
CP0490688 Compound Info	N-[3-[(5-chloro-6-oxo-4-piperazin-1-ylpyridazin-1-yl)methyl]-2-methylphenyl]-2-fluorobenzamide Show/Hide	C23H23ClFN5O2	1
1	EC50 = 20892.96 nM Bioactivity Info	TI LI LO TS
CP0455794 Compound Info	2-[2-[(2-methoxyphenyl)sulfonylamino]-5-methylphenoxy]benzenecarboximidamide Show/Hide	C21H21N3O4S	1
1	EC50 = 23000 nM Bioactivity Info	TI LI LO TS
CP0578058 Compound Info	5,6-dimethyl-4-(3-methylphenoxy)thieno[2,3-d]pyrimidine Show/Hide	C15H14N2OS	1
1	EC50 = 25000 nM Bioactivity Info	TI LI LO TS
CP0437939 Compound Info	N-[3-[(5-chloro-6-oxo-4-piperazin-1-ylpyridazin-1-yl)methyl]-2-methylphenyl]cyclohexanecarboxamide Show/Hide	C23H30ClN5O2	1
1	EC50 = 26302.68 nM Bioactivity Info	TI LI LO TS
CP0568443 Compound Info	4-(3-fluorophenoxy)-5,6-dimethylthieno[2,3-d]pyrimidine Show/Hide	C14H11FN2OS	1
1	EC50 = 30000 nM Bioactivity Info	TI LI LO TS
CP0388363 Compound Info	N-[3-[[4-(4-acetylpiperazin-1-yl)-5-chloro-6-oxopyridazin-1-yl]methyl]-2-methylphenyl]-4-(6-methoxypyridin-3-yl)benzamide Show/Hide	C31H31ClN6O4	1
1	EC50 = 32359.37 nM Bioactivity Info	TI LI LO TS
CP0179651 Compound Info	Adamantane-1-carboxylic acid [(S)-1-((S)-1-carbamoyl-2-phenyl-ethylcarbamoyl)-4-guanidino-butyl]-amide Show/Hide	C26H38N6O3	1
1	EC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0379134 Compound Info	(2S)-2-[[2-amino-2-[3-(diaminomethylideneamino)phenyl]acetyl]amino]-3-phenylpropanamide Show/Hide	C18H22N6O2	1
1	EC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0379135 Compound Info	(2S)-2-amino-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-3-[4-(diaminomethylideneamino)phenyl]propanamide Show/Hide	C19H24N6O2	1
1	EC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0379754 Compound Info	(2S,4S)-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-4-[(diaminomethylideneamino)methyl]pyrrolidine-2-carboxamide Show/Hide	C16H24N6O2	1
1	EC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0455916 Compound Info	(2S)-2-amino-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-5-(diaminomethylideneamino)pentanamide Show/Hide	C15H24N6O2	1
1	EC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0520596 Compound Info	(2S,4S)-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-4-(diaminomethylideneamino)pyrrolidine-2-carboxamide Show/Hide	C15H22N6O2	1
1	EC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0536802 Compound Info	(2R)-2-amino-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-3-[4-(diaminomethylideneamino)phenyl]propanamide Show/Hide	C19H24N6O2	1
1	EC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0551488 Compound Info	(2S)-2-[[2-amino-2-(1-carbamimidoylpiperidin-4-yl)acetyl]amino]-3-phenylpropanamide Show/Hide	C17H26N6O2	1
1	EC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0455791 Compound Info	2-[(3-methoxy-4-phenylmethoxyphenyl)methylamino]benzenecarboximidamide Show/Hide	C22H23N3O2	1
1	EC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0482744 Compound Info	N-[2-[(2-amino-1,3-benzothiazol-5-yl)oxy]-4-methylphenyl]-2-methoxybenzenesulfonamide Show/Hide	C21H19N3O4S2	1
1	EC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0528061 Compound Info	5,6-dimethyl-4-[4-(trifluoromethyl)phenoxy]thieno[2,3-d]pyrimidine Show/Hide	C15H11F3N2OS	1
1	EC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0568444 Compound Info	5,6-dimethyl-4-[3-(trifluoromethyl)phenoxy]thieno[2,3-d]pyrimidine Show/Hide	C15H11F3N2OS	1
1	EC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0466178 Compound Info	2-(4-(2-(4-chlorophenethylamino)pyrimidin-4-yl)piperazin-1-yl)-N-((3,5-dichloropyridin-4-yl)methyl)-N-(3-morpholinopropyl)acetamide Show/Hide	C31H39Cl3N8O2	2
1	IC50 = 14 nM Bioactivity Info	TI LI LO TS
2	IC50 = 50 nM Bioactivity Info	TI LI LO TS
CP0476751 Compound Info	2-(4-(2-(4-chlorophenethylamino)pyrimidin-4-yl)piperazin-1-yl)-N-(furan-2-ylmethyl)-N-(pyridin-4-ylmethyl)acetamide Show/Hide	C29H32ClN7O2	1
1	IC50 = 20 nM Bioactivity Info	TI LI LO TS
CP0473995 Compound Info	N-benzyl-2-[4-[2-[2-(4-chlorophenyl)ethylamino]pyrimidin-4-yl]piperazin-1-yl]-N-(pyridin-4-ylmethyl)acetamide Show/Hide	C31H34ClN7O	1
1	IC50 = 22 nM Bioactivity Info	TI LI LO TS
CP0466175 Compound Info	2-(4-(2-(4-chlorophenethylamino)pyrimidin-4-yl)piperazin-1-yl)-N-((3,5-dichloropyridin-4-yl)methyl)-N-(pyridin-4-ylmethyl)acetamide Show/Hide	C30H31Cl3N8O	1
1	IC50 = 24 nM Bioactivity Info	TI LI LO TS
CP0476752 Compound Info	2-(4-(2-(4-chlorophenethylamino)pyrimidin-4-yl)piperazin-1-yl)-N-(pyridin-4-ylmethyl)-N-((tetrahydrofuran-2-yl)methyl)acetamide Show/Hide	C29H36ClN7O2	1
1	IC50 = 40 nM Bioactivity Info	TI LI LO TS
CP0464757 Compound Info	2-(4-(2-(4-chlorophenethylamino)pyrimidin-4-yl)piperazin-1-yl)-N-((3,5-dichloropyridin-4-yl)methyl)-N-ethylacetamide Show/Hide	C26H30Cl3N7O	1
1	IC50 = 77 nM Bioactivity Info	TI LI LO TS
CP0512550 Compound Info	2-(4-(2-(4-chlorophenethylamino)pyrimidin-4-yl)piperazin-1-yl)-N-(3-methoxypropyl)-N-(pyridin-4-ylmethyl)acetamide Show/Hide	C28H36ClN7O2	1
1	IC50 = 88 nM Bioactivity Info	TI LI LO TS
CP0565788 Compound Info	N-[(3-bromopyridin-4-yl)methyl]-2-[4-[2-[2-(4-chlorophenyl)ethylamino]pyrimidin-4-yl]piperazin-1-yl]-N-ethylacetamide Show/Hide	C26H31BrClN7O	1
1	IC50 = 108 nM Bioactivity Info	TI LI LO TS
CP0501259 Compound Info	2-(4-(2-(4-chlorophenethylamino)pyrimidin-4-yl)piperazin-1-yl)-N-ethyl-N-(pyridin-4-ylmethyl)acetamide Show/Hide	C26H32ClN7O	1
1	IC50 = 244 nM Bioactivity Info	TI LI LO TS
CP0466176 Compound Info	2-(4-(2-(4-chlorophenethylamino)pyrimidin-4-yl)piperazin-1-yl)-N-(cyclopropylmethyl)-N-(pyridin-4-ylmethyl)acetamide Show/Hide	C28H34ClN7O	1
1	IC50 = 295 nM Bioactivity Info	TI LI LO TS
CP0477967 Compound Info	4-(2-(2-(4-chlorophenethylamino)pyrimidin-4-ylamino)ethyl)benzenesulfonamide Show/Hide	C20H22ClN5O2S	1
1	IC50 = 301 nM Bioactivity Info	TI LI LO TS
CP0466177 Compound Info	N-benzyl-2-[4-[2-[2-(4-chlorophenyl)ethylamino]pyrimidin-4-yl]piperazin-1-yl]-N-ethylacetamide Show/Hide	C27H33ClN6O	1
1	IC50 = 330 nM Bioactivity Info	TI LI LO TS
CP0512000 Compound Info	1-(2-(4-chlorophenethylamino)-4-(pyrrolidin-1-yl)quinazolin-6-ylsulfonyl)-N-(1-(dimethylamino)propan-2-yl)piperidine-4-carboxamide Show/Hide	C31H42ClN7O3S	1
1	IC50 = 530 nM Bioactivity Info	TI LI LO TS
CP0473994 Compound Info	4-(2-(2-(4-chlorophenethylamino)quinazolin-4-ylamino)ethyl)benzenesulfonamide Show/Hide	C24H24ClN5O2S	1
1	IC50 = 640 nM Bioactivity Info	TI LI LO TS
CP0530640 Compound Info	2-(4-(2-(4-chlorophenethylamino)pyrimidin-4-yl)piperazin-1-yl)-1-(piperidin-1-yl)ethanone Show/Hide	C23H31ClN6O	1
1	IC50 = 758 nM Bioactivity Info	TI LI LO TS
CP0364413 Compound Info	(2E)-2-(2-benzhydryl-1-azabicyclo[2.2.2]octan-3-ylidene)-1-(2-methoxyphenyl)ethanone Show/Hide	C29H29NO2	1
1	IC50 = 800 nM Bioactivity Info	TI LI LO TS
CP0494698 Compound Info	N-[2-(4-chlorophenyl)ethyl]-4-pyrrolidin-1-ylquinazolin-2-amine Show/Hide	C20H21ClN4	1
1	IC50 = 8060 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000035 , NIH 3T3

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0719182 Compound Info	(5S,8S,11S,14S,17S,20S,23S,26S,29S,32S)-26,29-bis((1H-indol-3-yl)methyl)-32-((S)-1-((S)-2-(2-((S)-2-amino-3-methylbutanamido)acetamido)-5-guanidinopentanoyl)pyrrolidine-2-carboxamido)-14-(3-amino-3-oxopropyl)-11-(4-aminobutyl)-20-(carboxymethyl)-8-(3-guanidinopropyl)-5,17-bis(4-hydroxybenzyl)-23-(2-(methylthio)ethyl)-4,7,10,13,16,19,22,25,28,31-decaoxo-3,6,9,12,15,18,21,24,27,30-decaazapentatriacontane-1,35-dioic acid Show/Hide	C91H127N25O23S	1
1	EC50 = 50 nM
CP0364413 Compound Info	(2E)-2-(2-benzhydryl-1-azabicyclo[2.2.2]octan-3-ylidene)-1-(2-methoxyphenyl)ethanone Show/Hide	C29H29NO2	1
1	IC50 = 320 nM

Clinical Information about the Protein

Target 1 ( Mas-related G protein-coupled receptor X1 (MRGX1) )

Target Type	Literature-reported Target

Similar Protein(s) and Bioactivity Statistics

50% Identity

Protein ID	Protein Name	Protein Organism
PT01155	Growth hormone secretagogue receptor type 1	Homo sapiens, Human	Protein Info

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han