Protein Information

General Information of the Protein

Protein ID	PT01307
Protein Name	5-hydroxytryptamine receptor 4
Secondarily Protein Name	Serotonin receptor 4
Gene Name	HTR4
Sequence	MDKLDANVSSEEGFGSVEKVVLLTFLSTVILMAILGNLLVMVAVCWDRQLRKIKTNYFIVSLAFADLLVSVLVMPFGAIELVQDIWIYGEVFCLVRTSLDVLLTTASIFHLCCISLDRYYAICCQPLVYRNKMTPLRIALMLGGCWVIPTFISFLPIMQGWNNIGIIDLIEKRKFNQNSNSTYCVFMVNKPYAITCSVVAFYIPFLLMVLAYYRIYVTAKEHAHQIQMLQRAGASSESRPQSADQHSTHRMRTETKAAKTLCIIMGCFCLCWAPFFVTNIVDPFIDYTVPGQVWTAFLWLGYINSGLNPFLYAFLNKSFRRAFLIILCCDDERYRRPSILGQTVPCSTTTINGSTHVLRDAVECGGQWESQCHPPATSPLVAAQPSDT Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Membrane receptor > Family A G protein-coupled receptor > Small molecule receptor (family A GPCR) > Monoamine receptor > Serotonin receptor
Function	This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase. Show/Hide
Uniprot ID	Primary ID: Q13639 Secondarily ID: C4WYH4 Q546Q1 Q684M0 Q712M9 Q96KH9 Q96KI0 Q9H199 Q9NY73 Q9UBM6 Q9UBT4 Q9UE22 Q9UE23 Q9UQR6 Show/Hide
Ensembl ID	ENSG00000164270
HGNC ID	HGNC:5299
Subcellular Location	Cell membrane Endosome

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: CL000049 , C6

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0908258 Compound Info	2-[4-({6-[6-Amino-1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl]hexanoyl}amino)piperidino]ethyl 4-Amino-5-chloro-2-methoxybenzoate Show/Hide	C32H36ClN5O6	2
1	EC50 = 4 nM Bioactivity Info	TI LI LO TS
2	Ki = 111 nM Bioactivity Info	TI LI LO TS
CP0481292 Compound Info	ML10302 scaffold, 14 Show/Hide	C50H72Cl2N8O8	2
1	EC50 = 9 nM Bioactivity Info	TI LI LO TS
2	Ki = 14 nM Bioactivity Info	TI LI LO TS
CP0001238 Compound Info	14C-5-hydroxy tryptamine creatinine disulfate Show/Hide	C10H12N2O	2
1	EC50 = 12 nM Bioactivity Info	TI LI LO TS
2	Ki = 1049 nM Bioactivity Info	TI LI LO TS
CP0481291 Compound Info	ML10302 scaffold, 9{a;q} Show/Hide	C23H27Cl2N3O4	2
1	EC50 = 18 nM Bioactivity Info	TI LI LO TS
2	Ki = 5 nM Bioactivity Info	TI LI LO TS
CP0290551 Compound Info	2-Piperidinoethyl 4-amino-5-chloro-2-methoxybenzoate Show/Hide	C15H21ClN2O3	4
1	EC50 = 51 nM Bioactivity Info	TI LI LO TS
2	Ki = 1 nM Bioactivity Info	TI LI LO TS
3	Ki = 5 nM Bioactivity Info	TI LI LO TS
4	Ki = 5.6 nM Bioactivity Info	TI LI LO TS
CP0435095 Compound Info	ML10302 scaffold, 9{b;w} Show/Hide	C27H37ClN4O6S	2
1	EC50 = 68 nM Bioactivity Info	TI LI LO TS
2	Ki = 2 nM Bioactivity Info	TI LI LO TS
CP0123097 Compound Info	3H-GR113808 Show/Hide	C19H27N3O4S	2
1	Ki = 0.1 nM Bioactivity Info	TI LI LO TS
2	Ki = 0.5 nM Bioactivity Info	TI LI LO TS
CP0373139 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-(4-pyrimidin-2-yl-piperazin-1-yl)-ethyl ester Show/Hide	C18H22ClN5O3	1
1	Ki = 1 nM Bioactivity Info	TI LI LO TS
CP0404014 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-(4-pyridazin-3-yl-piperazin-1-yl)-ethyl ester Show/Hide	C18H22ClN5O3	1
1	Ki = 1.4 nM Bioactivity Info	TI LI LO TS
CP0482880 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-(2,3,5,6-tetrahydro-[1,2']bipyrazinyl-4-yl)-ethyl ester Show/Hide	C18H22ClN5O3	1
1	Ki = 1.4 nM Bioactivity Info	TI LI LO TS
CP0397652 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-(4-pyridin-2-yl-piperazin-1-yl)-ethyl ester Show/Hide	C19H23ClN4O3	1
1	Ki = 1.5 nM Bioactivity Info	TI LI LO TS
CP0449044 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(6-chloro-pyridazin-3-yl)-piperazin-1-yl]-ethyl ester Show/Hide	C18H21Cl2N5O3	1
1	Ki = 2 nM Bioactivity Info	TI LI LO TS
CP0265345 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(3-methoxy-phenyl)-piperazin-1-yl]-ethyl ester Show/Hide	C21H26ClN3O4	1
1	Ki = 3 nM Bioactivity Info	TI LI LO TS
CP0457326 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-(4-pyridin-4-yl-piperazin-1-yl)-ethyl ester Show/Hide	C19H23ClN4O3	1
1	Ki = 3.5 nM Bioactivity Info	TI LI LO TS
CP0448448 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-{4-[(5-dimethylamino-naphthalene-1-sulfonylamino)-methyl]-piperidin-1-yl}-ethyl ester Show/Hide	C28H35ClN4O5S	1
1	Ki = 7 nM Bioactivity Info	TI LI LO TS
CP0463026 Compound Info	2-[4-({5-[(1-{2-[(4-amino-5-chloro-2-methoxyphenyl)carbonyloxy]ethyl}piperidin-4-yl)carbamoyl]pentyl}carbamoyl)piperidin-1-yl]ethyl 4-amino-5-chloro-2-methoxybenzoate Show/Hide	C37H52Cl2N6O8	1
1	Ki = 7 nM Bioactivity Info	TI LI LO TS
CP0374637 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-{4-[(7-nitro-benzo[1,2,5]oxadiazol-4-ylamino)-methyl]-piperidin-1-yl}-ethyl ester Show/Hide	C22H25ClN6O6	1
1	Ki = 7.5 nM Bioactivity Info	TI LI LO TS
CP0876620 Compound Info	2-(4-{4-[N-(3-{3-[3-(N-{3-[(1-{2-[(4-amino-2-methoxyphenyl)carbonyloxy]ethyl}piperidin-4-yl)carbamoyl]propyl}-2,2-dimethylpropanamido)prop-1-yn-1-yl]phenyl}prop-2-yn-1-yl)-2,2-dimethylpropanamido]butanamido}piperidin-1-yl)ethyl 4-amino-5-chloro-2-methoxybenzoate Show/Hide	C60H80Cl2N8O12	1
1	Ki = 8 nM Bioactivity Info	TI LI LO TS
CP0184481 Compound Info	1-[2-(4-amino-5-chloro-2-methoxyphenylcarbonyloxy)ethyl]-4-{2-[10-(2-{1-[2-(4-amino-5-chloro-2-methoxyphenylcarbonyloxy)ethyl]hexahydro-4-pyridinyl}ethylcarbamoyl)decylcarboxamido]ethyl}hexahydropyridine Show/Hide	C46H70Cl2N6O8	1
1	Ki = 9 nM Bioactivity Info	TI LI LO TS
CP0432877 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-(4-pyrimidin-5-yl-piperazin-1-yl)-ethyl ester Show/Hide	C18H22ClN5O3	1
1	Ki = 9.2 nM Bioactivity Info	TI LI LO TS
CP0461031 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(2-chloro-pyrimidin-5-yl)-piperazin-1-yl]-ethyl ester Show/Hide	C18H21Cl2N5O3	1
1	Ki = 9.8 nM Bioactivity Info	TI LI LO TS
CP0860113 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 3-(4-cyclohexa-2,4-dienyl-piperazin-1-yl)-propyl ester Show/Hide	C21H26ClN3O3	1
1	Ki = 11.5 nM Bioactivity Info	TI LI LO TS
CP0913714 Compound Info	2-(4-{4-[N-(3-{4-[3-(N-{3-[(1-{2-[(4-amino-5-chloro-2-methoxyphenyl)carbonyloxy]ethyl}piperidin-4-yl)carbamoyl]propyl}-2,2-dimethylpropanamido)propyl]phenyl}propyl)-2,2-dimethylpropanamido]butanamido}piperidin-1-yl)ethyl 4-amino-5-chloro-2-methoxybenzoate Show/Hide	C60H88Cl2N8O12	1
1	Ki = 12 nM Bioactivity Info	TI LI LO TS
CP0527048 Compound Info	ML10302 scaffold, 19 Show/Hide	C28H39ClN4O4	1
1	Ki = 12 nM Bioactivity Info	TI LI LO TS
CP0448968 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-(4-phenyl-piperazin-1-yl)-ethyl ester Show/Hide	C20H24ClN3O3	1
1	Ki = 14.3 nM Bioactivity Info	TI LI LO TS
CP0460082 Compound Info	2-[4-[[4-[3-[4-[3-[[4-[[1-[2-(4-amino-5-chloro-2-methoxybenzoyl)oxyethyl]piperidin-4-yl]methylamino]-4-oxobutyl]-(2,2-dimethylpropanoyl)amino]propyl]phenyl]propyl-(2,2-dimethylpropanoyl)amino]butanoylamino]methyl]piperidin-1-yl]ethyl 4-amino-5-chloro-2-methoxybenzoate Show/Hide	C62H92Cl2N8O10	1
1	Ki = 15 nM Bioactivity Info	TI LI LO TS
CP0464531 Compound Info	2-(4-{4-[N-(3-{3-[3-(N-{3-[(1-{2-[(4-amino-5-chloro-2-methoxyphenyl)carbonyloxy]ethyl}piperidin-4-yl)carbamoyl]propyl}-2,2-dimethylpropanamido)propyl]phenyl}propyl)-2,2-dimethylpropanamido]butanamido}piperidin-1-yl)ethyl 4-amino-5-chloro-2-methoxybenzoate Show/Hide	C60H88Cl2N8O10	1
1	Ki = 15 nM Bioactivity Info	TI LI LO TS
CP0116432 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(2-fluoro-phenyl)-piperazin-1-yl]-ethyl ester Show/Hide	C20H23ClFN3O3	1
1	Ki = 16.8 nM Bioactivity Info	TI LI LO TS
CP0158852 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(4-methoxy-phenyl)-piperazin-1-yl]-ethyl ester Show/Hide	C21H26ClN3O4	1
1	Ki = 17.7 nM Bioactivity Info	TI LI LO TS
CP0878443 Compound Info	2-(4-{4-[N-(3-{4-[3-(N-{3-[(1-{2-[(4-amino-5-chloro-2-methoxyphenyl)carbonyloxy]ethyl}piperidin-4-yl)carbamoyl]propyl}-2,2-dimethylpropanamido)prop-1-yn-1-yl]phenyl}prop-2-yn-1-yl)-2,2-dimethylpropanamido]butanamido}piperidin-1-yl)ethyl 4-amino-5-chloro-2-methoxybenzoate Show/Hide	C60H80Cl2N8O12	1
1	Ki = 18 nM Bioactivity Info	TI LI LO TS
CP0878598 Compound Info	2-{4-[(2-{N-[3-(4-{3-[N-({[(1-{2-[(4-amino-5-chloro-2-methoxyphenyl)carbonyloxy]ethyl}piperidin-4-yl)methyl]carbamoyl}methyl)-2,2-dimethylpropanamido]propyl}phenyl)propyl]-2,2-dimethylpropanamido}acetamido)methyl]piperidin-1-yl}ethyl 4-amino-5-chloro-2-methoxybenzoate Show/Hide	C58H84Cl2N8O12	1
1	Ki = 19 nM Bioactivity Info	TI LI LO TS
CP0269667 Compound Info	2-[4-({10-[(1-{2-[(4-amino-5-chloro-2-methoxyphenyl)carbonyloxy]ethyl}piperidin-4-yl)carbamoyl]decyl}carbamoyl)piperidin-1-yl]ethyl 4-amino-5-chloro-2-methoxybenzoate Show/Hide	C42H62Cl2N6O8	1
1	Ki = 20 nM Bioactivity Info	TI LI LO TS
CP0449155 Compound Info	4-[2-(4-Amino-5-chloro-2-methoxy-benzoyloxy)-ethyl]-piperazine-1-carboxylic acid ethyl ester Show/Hide	C17H24ClN3O5	1
1	Ki = 23 nM Bioactivity Info	TI LI LO TS
CP0911403 Compound Info	2-{4-[(4-{N-[3-(3-{3-[N-(3-{[(1-{2-[(4-amino-5-chloro-2-methoxyphenyl)carbonyloxy]ethyl}piperidin-4-yl)methyl]carbamoyl}propyl)-2,2-dimethylpropanamido]propyl}phenyl)propyl]-2,2-dimethylpropanamido}butanamido)methyl]piperidin-1-yl}ethyl 4-amino-5-chloro-2-methoxybenzoate Show/Hide	C62H92Cl2N8O12	1
1	Ki = 23 nM Bioactivity Info	TI LI LO TS
CP0504843 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(4-fluoro-phenyl)-piperazin-1-yl]-ethyl ester Show/Hide	C20H23ClFN3O3	1
1	Ki = 23.1 nM Bioactivity Info	TI LI LO TS
CP0374634 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-{4-[4-(5-dimethylamino-naphthalene-1-sulfonylamino)-butyl]-piperidin-1-yl}-ethyl ester Show/Hide	C31H41ClN4O5S	1
1	Ki = 24 nM Bioactivity Info	TI LI LO TS
CP0881790 Compound Info	2-{4-[(4-{N-[3-(4-{3-[N-(3-{[(1-{2-[(4-amino-5-chloro-2-methoxyphenyl)carbonyloxy]ethyl}piperidin-4-yl)methyl]carbamoyl}propyl)-2,2-dimethylpropanamido]prop-1-yn-1-yl}phenyl)prop-2-yn-1-yl]-2,2-dimethylpropanamido}butanamido)methyl]piperidin-1-yl}ethyl 4-amino-5-chloro-2-methoxybenzoate Show/Hide	C62H84Cl2N8O12	1
1	Ki = 25 nM Bioactivity Info	TI LI LO TS
CP0406296 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-{4-[8-(5-dimethylamino-naphthalene-1-sulfonylamino)-octanoyl]-piperazin-1-yl}-ethyl ester Show/Hide	C34H46ClN5O6S	1
1	Ki = 31 nM Bioactivity Info	TI LI LO TS
CP0453192 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-{4-[3-(5-dimethylamino-naphthalene-1-sulfonylamino)-propyl]-piperidin-1-yl}-ethyl ester Show/Hide	C30H39ClN4O5S	1
1	Ki = 32 nM Bioactivity Info	TI LI LO TS
CP0897739 Compound Info	2-(4-(4-(tert-butoxycarbonyl(3-(4-(3-(tert-butoxycarbonyl(4-(cyclohexylamino)-4-oxobutyl)amino)propyl)phenyl)propyl)-amino)butanamido)piperidin-1-yl)ethyl 4-Amino-5-chloro-2-methoxybenzoate Show/Hide	C51H79ClN6O9	1
1	Ki = 34 nM Bioactivity Info	TI LI LO TS
CP0899660 Compound Info	2-{4-[(4-{N-[3-(3-{3-[N-(3-{[(1-{2-[(4-amino-2-methoxyphenyl)carbonyloxy]ethyl}piperidin-4-yl)methyl]carbamoyl}propyl)-2,2-dimethylpropanamido]prop-1-yn-1-yl}phenyl)prop-2-yn-1-yl]-2,2-dimethylpropanamido}butanamido)methyl]piperidin-1-yl}ethyl 4-amino-5-chloro-2-methoxybenzoate Show/Hide	C62H84Cl2N8O12	1
1	Ki = 40 nM Bioactivity Info	TI LI LO TS
CP0877556 Compound Info	2-{4-[(2-{N-[3-(4-{3-[N-({[(1-{2-[(4-amino-5-chloro-2-methoxyphenyl)carbonyloxy]ethyl}piperidin-4-yl)methyl]carbamoyl}methyl)-2,2-dimethylpropanamido]prop-1-yn-1-yl}phenyl)prop-2-yn-1-yl]-2,2-dimethylpropanamido}acetamido)methyl]piperidin-1-yl}ethyl 4-amino-5-chloro-2-methoxybenzoate Show/Hide	C58H76Cl2N8O12	1
1	Ki = 44 nM Bioactivity Info	TI LI LO TS
CP0273452 Compound Info	1-[2-(4-amino-5-chloro-2-methoxyphenylcarbonyloxy)ethyl]-4-{10-[10-{1-[2-(4-amino-5-chloro-2-methoxyphenylcarbonyloxy)ethyl]hexahydro-4-pyridinylcarbamoyl}decyl(hexahydro-4-pyridinylmethylcarbamoylmethyl)amino]decylcarboxamido}hexahydropyridine Show/Hide	C60H97Cl2N9O9	1
1	Ki = 50 nM Bioactivity Info	TI LI LO TS
CP0502414 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-{4-[4-(6-dimethylamino-1,3-dioxo-1H,3H-benzo[de]isoquinolin-2-yl)-butyl]-piperidin-1-yl}-ethyl ester Show/Hide	C33H39ClN4O5	1
1	Ki = 59 nM Bioactivity Info	TI LI LO TS
CP0225714 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(2-methoxy-phenyl)-piperazin-1-yl]-ethyl ester Show/Hide	C21H26ClN3O4	1
1	Ki = 64 nM Bioactivity Info	TI LI LO TS
CP0391272 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(6-amino-1,3-dioxo-1H,3H-benzo[de]isoquinolin-2-ylmethyl)-piperidin-1-yl]-ethyl ester Show/Hide	C28H29ClN4O5	1
1	Ki = 64 nM Bioactivity Info	TI LI LO TS
CP0502406 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-{4-[2-(5-dimethylamino-naphthalene-1-sulfonylamino)-ethyl]-piperidin-1-yl}-ethyl ester Show/Hide	C29H37ClN4O5S	1
1	Ki = 77 nM Bioactivity Info	TI LI LO TS
CP0408850 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-{4-[11-(5-dimethylamino-naphthalene-1-sulfonylamino)-undecanoyl]-piperazin-1-yl}-ethyl ester Show/Hide	C37H52ClN5O6S	1
1	Ki = 96 nM Bioactivity Info	TI LI LO TS
CP0776488 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(3-{4-[2-(1-benzoyl-piperidin-4-ylcarbamoyl)-ethylamino]-6-benzylamino-[1,3,5]triazin-2-ylamino}-propionylamino)-piperidin-1-yl]-ethyl ester Show/Hide	C62H92Cl2N12O8	1
1	Ki = 113 nM Bioactivity Info	TI LI LO TS
CP0399971 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-{4-[3-(5-dimethylamino-naphthalene-1-sulfonylamino)-propionyl]-piperazin-1-yl}-ethyl ester Show/Hide	C29H36ClN5O6S	1
1	Ki = 116 nM Bioactivity Info	TI LI LO TS
CP0246165 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(3-chloro-phenyl)-piperazin-1-yl]-ethyl ester Show/Hide	C20H23Cl2N3O3	1
1	Ki = 162 nM Bioactivity Info	TI LI LO TS
CP0448456 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-{4-[6-(5-dimethylamino-naphthalene-1-sulfonylamino)-hexanoyl]-piperazin-1-yl}-ethyl ester Show/Hide	C32H42ClN5O6S	1
1	Ki = 180 nM Bioactivity Info	TI LI LO TS
CP0449396 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(6-dimethylamino-1,3-dioxo-1H,3H-benzo[de]isoquinolin-2-ylmethyl)-piperidin-1-yl]-ethyl ester Show/Hide	C30H33ClN4O5	1
1	Ki = 181 nM Bioactivity Info	TI LI LO TS
CP0453489 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-{4-[4-(5-dimethylamino-naphthalene-1-sulfonylamino)-butyryl]-piperazin-1-yl}-ethyl ester Show/Hide	C30H38ClN5O6S	1
1	Ki = 183 nM Bioactivity Info	TI LI LO TS
CP0535310 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(3-trifluoromethyl-phenyl)-piperazin-1-yl]-ethyl ester Show/Hide	C21H23ClF3N3O3	1
1	Ki = 199.2 nM Bioactivity Info	TI LI LO TS
CP0529762 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-(4-benzyl-piperazin-1-yl)-ethyl ester Show/Hide	C21H26ClN3O3	1
1	Ki = 240 nM Bioactivity Info	TI LI LO TS
CP0448513 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(5-dimethylamino-naphthalene-1-sulfonylamino)-piperidin-1-yl]-ethyl ester Show/Hide	C27H33ClN4O5S	1
1	Ki = 264 nM Bioactivity Info	TI LI LO TS
CP0225715 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(2-chloro-phenyl)-piperazin-1-yl]-ethyl ester Show/Hide	C20H23Cl2N3O3	1
1	Ki = 296 nM Bioactivity Info	TI LI LO TS
CP0265346 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(4-chloro-phenyl)-piperazin-1-yl]-ethyl ester Show/Hide	C20H23Cl2N3O3	1
1	Ki = 715 nM Bioactivity Info	TI LI LO TS
CP0441827 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-{4-[2-(5-dimethylamino-naphthalene-1-sulfonylamino)-acetyl]-piperazin-1-yl}-ethyl ester Show/Hide	C28H34ClN5O6S	1
1	Ki = 1720 nM Bioactivity Info	TI LI LO TS
CP0439606 Compound Info	4-[2-(4-Amino-5-chloro-2-methoxy-benzoyloxy)-ethyl]-piperazine-1-carboxylic acid tert-butyl ester Show/Hide	C19H28ClN3O5	1
1	Ki > 1000 nM Bioactivity Info	TI LI LO TS
CP0496435 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-piperazin-1-yl-ethyl ester Show/Hide	C14H20ClN3O3	1
1	Ki > 1000 nM Bioactivity Info	TI LI LO TS
CP0511290 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-(4-naphthalen-1-yl-piperazin-1-yl)-ethyl ester Show/Hide	C24H26ClN3O3	1
1	Ki > 1000 nM Bioactivity Info	TI LI LO TS
CP0529761 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-(4-methyl-piperazin-1-yl)-ethyl ester Show/Hide	C15H22ClN3O3	1
1	Ki > 1000 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000011 , CHO

Cell Line Info

Cell Line ID: CL000053 , COS-7

Cell Line Info

Cell Line ID: CL000025 , HEK-293T

Cell Line Info

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000017 , HeLa

Cell Line Info

Cell Line ID: CL000004 , SH-SY5Y

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0148502 Compound Info	4-[[4-[[4-[(3R)-oxolan-3-yl]oxy-1,2-benzoxazol-3-yl]oxymethyl]piperidin-1-yl]methyl]oxan-4-ol Show/Hide	C23H32N2O6	1
1	EC50 = 0.26 nM
CP0204174 Compound Info	N-[[1-[(4-hydroxyoxan-4-yl)methyl]piperidin-4-yl]methyl]-2-oxo-3-propan-2-ylbenzimidazole-1-carboxamide Show/Hide	C23H34N4O4	1
1	EC50 = 1.3 nM
CP0169714 Compound Info	CHEMBL538635 Show/Hide	C28H41N5O5S	1
1	EC50 = 3.981 nM
CP0156475 Compound Info	CHEMBL2059590 Show/Hide	C26H38N6O2	1
1	EC50 = 6.31 nM
CP0043343 Compound Info	(Z)-2-butenedioic acid;1-[[(Z)-(5-methoxy-3-indolylidene)methyl]amino]-2-pentylguanidine Show/Hide	C16H23N5O	2
1	EC50 = 15.85 nM
2	Ki = 3.981 nM
CP0240582 Compound Info	Prx-03140 Show/Hide	C19H27N3O3S	1
1	EC50 = 17 nM
CP0120561 Compound Info	CHEMBL3740472 Show/Hide	C21H30N4O2	2
1	EC50 = 20 nM
2	EC50 = 22 nM
CP0106868 Compound Info	4-Amino-5-chloro-2,3-dihydro-benzofuran-7-carboxylic acid [1-(3-methoxy-propyl)-piperidin-4-yl]-amide Show/Hide	C18H26ClN3O3	2
1	EC50 = 26 nM
2	Ki = 2.512 nM
CP0120660 Compound Info	N-(1-Butylpiperidine-4-ylmethyl)-1,2-(trimethyleneoxy)-1H-indole-3-carboxamide Show/Hide	C22H31N3O2	4
1	IC50 = 0.631 nM
2	Ki = 0.2512 nM
3	Ki = 0.5012 nM
4	Ki = 1.585 nM
CP0265345 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(3-methoxy-phenyl)-piperazin-1-yl]-ethyl ester Show/Hide	C21H26ClN3O4	1
1	IC50 = 3 nM
CP0116432 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(2-fluoro-phenyl)-piperazin-1-yl]-ethyl ester Show/Hide	C20H23ClFN3O3	1
1	IC50 = 17 nM
CP0158852 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(4-methoxy-phenyl)-piperazin-1-yl]-ethyl ester Show/Hide	C21H26ClN3O4	1
1	IC50 = 18 nM
CP0225714 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(2-methoxy-phenyl)-piperazin-1-yl]-ethyl ester Show/Hide	C21H26ClN3O4	1
1	IC50 = 64 nM
CP0246165 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(3-chloro-phenyl)-piperazin-1-yl]-ethyl ester Show/Hide	C20H23Cl2N3O3	1
1	IC50 = 162 nM
CP0225715 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(2-chloro-phenyl)-piperazin-1-yl]-ethyl ester Show/Hide	C20H23Cl2N3O3	1
1	IC50 = 296 nM
CP0265346 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(4-chloro-phenyl)-piperazin-1-yl]-ethyl ester Show/Hide	C20H23Cl2N3O3	1
1	IC50 = 715 nM
CP0123097 Compound Info	3H-GR113808 Show/Hide	C19H27N3O4S	1
1	Ki = 0.1585 nM
CP0043344 Compound Info	methyl 4-[[4-[[(2-propan-2-yl-1H-benzimidazole-4-carbonyl)amino]methyl]piperidin-1-yl]methyl]piperidine-1-carboxylate Show/Hide	C25H37N5O3	1
1	Ki = 0.3981 nM
CP0071842 Compound Info	4-fluoro-6-[(1-propylpiperidin-4-yl)methoxy]phenanthridine Show/Hide	C22H25FN2O	1
1	Ki = 3.1 nM
CP0290551 Compound Info	2-Piperidinoethyl 4-amino-5-chloro-2-methoxybenzoate Show/Hide	C15H21ClN2O3	1
1	Ki = 5 nM
CP0072246 Compound Info	1-(4-amino-5-chloro-2-methoxyphenyl)-3-[1-(cyclohexylmethyl)piperidin-4-yl]propan-1-one Show/Hide	C22H33ClN2O2	1
1	Ki = 10.4 nM
CP0184481 Compound Info	1-[2-(4-amino-5-chloro-2-methoxyphenylcarbonyloxy)ethyl]-4-{2-[10-(2-{1-[2-(4-amino-5-chloro-2-methoxyphenylcarbonyloxy)ethyl]hexahydro-4-pyridinyl}ethylcarbamoyl)decylcarboxamido]ethyl}hexahydropyridine Show/Hide	C46H70Cl2N6O8	1
1	Ki = 18 nM
CP0269667 Compound Info	2-[4-({10-[(1-{2-[(4-amino-5-chloro-2-methoxyphenyl)carbonyloxy]ethyl}piperidin-4-yl)carbamoyl]decyl}carbamoyl)piperidin-1-yl]ethyl 4-amino-5-chloro-2-methoxybenzoate Show/Hide	C42H62Cl2N6O8	1
1	Ki = 20 nM
CP0030226 Compound Info	4-Amino-5-chloro-N-{1-[3-(4-fluoro-phenoxy)-propyl]-3-methoxy-piperidin-4-yl}-2-methoxy-benzamide Show/Hide	C23H29ClFN3O4	3
1	Ki = 29 nM
2	Ki = 100 nM
3	Ki = 125.89 nM
CP0273452 Compound Info	1-[2-(4-amino-5-chloro-2-methoxyphenylcarbonyloxy)ethyl]-4-{10-[10-{1-[2-(4-amino-5-chloro-2-methoxyphenylcarbonyloxy)ethyl]hexahydro-4-pyridinylcarbamoyl}decyl(hexahydro-4-pyridinylmethylcarbamoylmethyl)amino]decylcarboxamido}hexahydropyridine Show/Hide	C60H97Cl2N9O9	1
1	Ki = 50 nM
CP0776488 Compound Info	4-Amino-5-chloro-2-methoxy-benzoic acid 2-[4-(3-{4-[2-(1-benzoyl-piperidin-4-ylcarbamoyl)-ethylamino]-6-benzylamino-[1,3,5]triazin-2-ylamino}-propionylamino)-piperidin-1-yl]-ethyl ester Show/Hide	C62H92Cl2N12O8	1
1	Ki = 113 nM
CP0113176 Compound Info	5-Chloro-3-methyl-benzo[b]thiophene-2-sulfonic acid [4-methoxy-3-(4-methyl-piperazin-1-yl)-phenyl]-amide Show/Hide	C21H24ClN3O3S2	1
1	Ki = 3162.28 nM

Clinical Information about the Protein

Target 1 ( 5-HT 4 receptor (HTR4) )

Target Type	Successful Target
Disease	8 Target-related Diseases				8
1	Gastroesophageal reflux disease [ICD-11: DA22.Z]
2	Constipation [ICD-11: DD91.1]
3	Irritable bowel syndrome [ICD-11: DD91.0]
4	Atrial fibrillation [ICD-11: BC81.3]
5	Gastrointestinal disease [ICD-11: DE2Z]
6	Alzheimer disease [ICD-11: 8A20]
7	Parkinson disease [ICD-11: 8A00.0]
8	Gastric motility disorder [ICD-11: DA21]
Approved Drug(s)	4 Approved Drugs				4
1	Cisapride	Drug Info	Approved	Gastroesophageal reflux disease
2	HTF 919	Drug Info	Approved	Constipation
3	R0-93877	Drug Info	Approved	Irritable bowel syndrome
4	Tegaserod	Drug Info	Approved	Irritable bowel syndrome
Clinical Trial Drug(s)	5 Clinical Trial Drugs				5
1	Piboserod	Drug Info	Phase 2	Atrial fibrillation
2	TD-8954	Drug Info	Phase 2	Gastrointestinal disease
3	DA-6886	Drug Info	Phase 1	Irritable bowel syndrome
4	PF-04995274	Drug Info	Phase 1	Alzheimer disease
5	SUVN-D4010	Drug Info	Phase 1	Alzheimer disease
Discontinued Drug(s)	3 Discontinued Drugs				3
1	Norcisapride	Drug Info	Discontinued in Phase 2	Gastroesophageal reflux disease
2	SL65.0155	Drug Info	Discontinued in Phase 2	Parkinson disease
3	SC-53116	Drug Info	Terminated	Gastric motility disorder

Similar Protein(s) and Bioactivity Statistics

50% Identity

Protein ID	Protein Name	Protein Organism
PT01897	5-hydroxytryptamine receptor 4	Rattus norvegicus, Rat	Protein Info

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han