Protein Information

General Information of the Protein

Protein ID	PT01372
Protein Name	Endothelin-1 receptor
Secondarily Protein Name	Endothelin receptor type A
Gene Name	EDNRA
Secondarily Gene Name	ETA ETRA
Sequence	METLCLRASFWLALVGCVISDNPERYSTNLSNHVDDFTTFRGTELSFLVTTHQPTNLVLPSNGSMHNYCPQQTKITSAFKYINTVISCTIFIVGMVGNATLLRIIYQNKCMRNGPNALIASLALGDLIYVVIDLPINVFKLLAGRWPFDHNDFGVFLCKLFPFLQKSSVGITVLNLCALSVDRYRAVASWSRVQGIGIPLVTAIEIVSIWILSFILAIPEAIGFVMVPFEYRGEQHKTCMLNATSKFMEFYQDVKDWWLFGFYFCMPLVCTAIFYTLMTCEMLNRRNGSLRIALSEHLKQRREVAKTVFCLVVIFALCWFPLHLSRILKKTVYNEMDKNRCELLSFLLLMDYIGINLATMNSCINPIALYFVSKKFKNCFQSCLCCCCYQSKSLMTSVPMNGTSIQWKNHDQNNHNTDRSSHKDSMN 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) > Endothelin receptor
Function	Receptor for endothelin-1. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of binding affinities for ET-A is: ET1 > ET2 >> ET3. Show/Hide
Uniprot ID	Primary ID: P25101 Secondarily ID: B2R723 B4E2V6 B7Z9G6 D3DP03 E7ER36 O43441 Q16432 Q16433 Q8TBH2 Show/Hide
Ensembl ID	ENSG00000151617
HGNC ID	HGNC:3179
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: CL000139 , A-10

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0041337 Compound Info	5-Dimethylamino-naphthalene-1-sulfonic acid (3,4-dimethyl-2,3-dihydro-oxazol-5-yl)-amide Show/Hide	C17H19N3O3S	3
1	IC50 = 150 nM Bioactivity Info	TI LI LO TS
2	IC50 = 570 nM Bioactivity Info	TI LI LO TS
3	Ki = 55 nM Bioactivity Info	TI LI LO TS
CP0040571 Compound Info	4-Amino-N-(3,4-dimethyl-isoxazol-5-yl)-benzenesulfonamide Show/Hide	C11H13N3O3S	1
1	IC50 = 780 nM Bioactivity Info	TI LI LO TS
CP0522222 Compound Info	N-[5-[(3,4-dimethyl-1,2-oxazol-5-yl)sulfamoyl]naphthalen-1-yl]acetamide Show/Hide	C17H17N3O4S	1
1	IC50 = 880 nM Bioactivity Info	TI LI LO TS
CP0476037 Compound Info	5-Dimethylaminomethyl-naphthalene-1-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide Show/Hide	C18H21N3O3S	1
1	IC50 = 2800 nM Bioactivity Info	TI LI LO TS
CP0375462 Compound Info	5-Amino-naphthalene-1-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide Show/Hide	C15H15N3O3S	1
1	IC50 = 4000 nM Bioactivity Info	TI LI LO TS
CP0415327 Compound Info	5-Isopropenyl-naphthalene-1-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide Show/Hide	C18H18N2O3S	1
1	IC50 = 5700 nM Bioactivity Info	TI LI LO TS
CP0427317 Compound Info	5-Methoxy-naphthalene-1-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide Show/Hide	C16H16N2O4S	1
1	IC50 = 6500 nM Bioactivity Info	TI LI LO TS
CP0441723 Compound Info	N-(3,4-dimethyl-1,2-oxazol-5-yl)-4-hydroxybenzenesulfonamide Show/Hide	C11H12N2O4S	1
1	IC50 = 9200 nM Bioactivity Info	TI LI LO TS
CP0448219 Compound Info	4-Benzylamino-N-(3,4-dimethyl-isoxazol-5-yl)-benzenesulfonamide Show/Hide	C18H19N3O3S	1
1	IC50 = 9800 nM Bioactivity Info	TI LI LO TS
CP0380128 Compound Info	5-(3,4-Dimethyl-isoxazol-5-ylsulfamoyl)-naphthalene-1-carboxylic acid Show/Hide	C16H14N2O5S	1
1	IC50 = 13000 nM Bioactivity Info	TI LI LO TS
CP0429826 Compound Info	N-(3,4-dimethyl-1,2-oxazol-5-yl)naphthalene-1-sulfonamide Show/Hide	C15H14N2O3S	1
1	IC50 = 20000 nM Bioactivity Info	TI LI LO TS
CP0486361 Compound Info	N-(3,4-dimethyl-1,2-oxazol-5-yl)-4-(propylamino)benzenesulfonamide Show/Hide	C14H19N3O3S	1
1	IC50 = 27000 nM Bioactivity Info	TI LI LO TS
CP0391264 Compound Info	4-Amino-N-(3-methyl-isoxazol-5-yl)-benzenesulfonamide Show/Hide	C10H11N3O3S	1
1	IC50 = 28000 nM Bioactivity Info	TI LI LO TS
CP0506908 Compound Info	4-Cyano-N-(3,4-dimethyl-isoxazol-5-yl)-benzenesulfonamide Show/Hide	C12H11N3O3S	1
1	IC50 > 32000 nM Bioactivity Info	TI LI LO TS
CP0508901 Compound Info	4-Dimethylamino-N-(3,4-dimethyl-isoxazol-5-yl)-benzenesulfonamide Show/Hide	C13H17N3O3S	1
1	IC50 = 84000 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: CL000025 , HEK-293T

Cell Line Info

Cell Line ID: CL000041 , LTK-

Cell Line Info

Cell Line ID: CL000304 , MMQ

Cell Line Info

Cell Line ID: CL000013 , Sf9

Cell Line Info

Cell Line ID: CL000074 , SK-N-MC

Cell Line Info

Cell Line ID: CL000005 , TE 671

Cell Line Info

Cell Line ID: CL000057 , Vero

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0037579 Compound Info	(2R,3R,4S)-4-Benzo[1,3]dioxol-5-yl-1-dibutylcarbamoylmethyl-2-(4-methoxy-phenyl)-pyrrolidine-3-carboxylic acid Show/Hide	C29H38N2O6	3
1	IC50 = 0.034 nM
2	IC50 = 0.08 nM
3	IC50 = 0.31 nM
CP0104972 Compound Info	(3S)-3-[[(2S)-2-[[(2S)-2-[[(1S,4S,7S,10R,13S,16R,19S,22R,25R,28R,31S,36R,39S,42R,45S)-31-amino-7-(4-aminobutyl)-39-benzyl-4-(2-carboxyethyl)-10-(carboxymethyl)-19,22,28-tris(hydroxymethyl)-42-[(4-hydroxyphenyl)methyl]-16-(2-methylpropyl)-13-(2-methylsulfanylethyl)-3,6,9,12,15,18,21,24,27,30,38,41,44,47-tetradecaoxo-45-propan-2-yl-33,34,49,50-tetrathia-2,5,8,11,14,17,20,23,26,29,37,40,43,46-tetradecazabicyclo[23.22.4]henpentacontane-36-carbonyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-[[(2S,3S)-1-[[(2S,3S)-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-oxobutanoic acid Show/Hide	C109H159N25O32S5	6
1	IC50 = 0.05 nM
2	IC50 = 0.11 nM
3	IC50 = 0.16 nM
4	IC50 = 0.38 nM
5	Ki = 0.025 nM
6	Ki = 0.14 nM
CP0084273 Compound Info	(2R,3R,4S)-4-Benzo[1,3]dioxol-5-yl-2-(3-fluoro-4-methoxy-phenyl)-1-{2-[(pentane-1-sulfonyl)-propyl-amino]-ethyl}-pyrrolidine-3-carboxylic acid Show/Hide	C29H39FN2O7S	1
1	IC50 = 0.08 nM
CP0184415 Compound Info	4-[1-Benzo[1,3]dioxol-5-yl-2-(4-isopropyl-benzenesulfonylamino)-2-oxo-ethoxy]-3-propyl-benzoic acid Show/Hide	C28H29NO8S	1
1	IC50 = 0.26 nM
CP0278704 Compound Info	3-(benzo[d][1,3]dioxol-5-yl)-5-hydroxy-5-(4-methoxyphenyl)-4-(3,4,5-trimethoxybenzyl)furan-2(5H)-one Show/Hide	C28H26O9	1
1	IC50 = 0.3 nM
CP0430251 Compound Info	N-[6-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-5-(4-methylphenyl)pyrimidin-4-yl]-4-(1-hydroxy-2-methylpropan-2-yl)benzenesulfonamide Show/Hide	C27H28BrN5O5S	1
1	IC50 = 0.4 nM
CP0023329 Compound Info	(2S,3R,4S)-1-Dibutylcarbamoylmethyl-2-(2,2-dimethyl-pentyl)-4-(7-methoxy-benzo[1,3]dioxol-5-yl)-pyrrolidine-3-carboxylic acid Show/Hide	C30H48N2O6	3
1	IC50 = 0.49 nM
2	IC50 ~ 0.49 nM
3	Ki ~ 0.46 nM
CP0298518 Compound Info	3-[1-Benzo[1,3]dioxol-5-yl-2-(2-ethoxy-4-methyl-benzenesulfonylamino)-2-oxo-ethyl]-1-methyl-1H-indole-6-carboxylic acid amide Show/Hide	C28H27N3O7S	1
1	IC50 = 0.55 nM
CP0249832 Compound Info	N-(benzylsulfamoyl)-6-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-5-(4-methylphenyl)pyrimidin-4-amine Show/Hide	C24H23BrN6O4S	1
1	IC50 = 0.7 nM
CP0041197 Compound Info	(S)-2-(4,6-Dimethoxy-pyrimidin-2-yloxy)-3-methoxy-3,3-diphenyl-propionic acid Show/Hide	C22H22N2O6	1
1	IC50 = 0.8 nM
CP0146575 Compound Info	3-[1-Benzo[1,3]dioxol-5-yl-2-(2-methoxy-4-methyl-benzenesulfonylamino)-2-oxo-ethyl]-1-methyl-1H-indole-6-carboxylic acid amide Show/Hide	C27H25N3O7S	1
1	IC50 = 1.1 nM
CP0368400 Compound Info	N-(benzylsulfamoyl)-6-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-5-(2-methoxyphenoxy)-2-pyrimidin-2-ylpyrimidin-4-amine Show/Hide	C28H25BrN8O6S	1
1	IC50 = 1.9 nM
CP0249256 Compound Info	N-[6-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-5-(2-methoxyphenoxy)-2-pyrimidin-2-ylpyrimidin-4-yl]-2-phenylethanesulfonamide Show/Hide	C29H26BrN7O6S	1
1	IC50 = 2.2 nM
CP0270554 Compound Info	3-[1-Benzo[1,3]dioxol-5-yl-2-(4-isopropyl-benzenesulfonylamino)-2-oxo-ethyl]-1-methyl-1H-indole-6-carboxylic acid Show/Hide	C28H27N3O6S	1
1	IC50 = 2.3 nM
CP0552680 Compound Info	Avosentan Show/Hide	C23H21N5O5S	1
1	IC50 = 3.1 nM
CP0249829 Compound Info	N-[6-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-5-(2-methoxyphenoxy)-2-pyrimidin-2-ylpyrimidin-4-yl]butane-1-sulfonamide Show/Hide	C25H26BrN7O6S	1
1	IC50 = 4.3 nM
CP0065655 Compound Info	4-(1,1-Dimethylethyl)-N-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-(2,2'-bipyrimidin)-4-yl) benzenesulfornamide Show/Hide	C27H29N5O6S	4
1	IC50 = 4.7 nM
2	IC50 = 45 nM
3	IC50 = 1584.89 nM
4	Ki = 6.5 nM
CP0149984 Compound Info	N-(benzylsulfamoyl)-6-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-5-(2-methoxyphenoxy)pyrimidin-4-amine Show/Hide	C24H23BrN6O6S	1
1	IC50 = 6.9 nM
CP0362696 Compound Info	N-[5-(2-methoxyphenoxy)-2-pyrimidin-2-yl-6-(2-pyrimidin-2-yloxyethoxy)pyrimidin-4-yl]-2-phenylethanesulfonamide Show/Hide	C29H27N7O6S	1
1	IC50 = 8 nM
CP0225450 Compound Info	Biphenyl-2-sulfonic acid (4-bromo-3-methyl-isoxazol-5-yl)-amide Show/Hide	C16H13BrN2O3S	1
1	IC50 = 16.2 nM
CP0156307 Compound Info	CHEBI:2965 Show/Hide	C31H42N6O7	3
1	IC50 = 22 nM
2	IC50 = 37 nM
3	Ki = 18 nM
CP0330253 Compound Info	5-Isopropyl-pyridine-2-sulfonic acid {6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-[2-(1H-tetrazol-5-yl)-pyridin-4-yl]-pyrimidin-4-yl}-amide Show/Hide	C27H27N9O6S	1
1	IC50 = 23 nM
CP0087311 Compound Info	2-(1,3-benzodioxol-5-yl)-2-[4-[(2-ethyl-5,7-dimethylimidazo[4,5-b]pyridin-3-yl)methyl]-2-propylphenoxy]-N-(4-propan-2-ylphenyl)sulfonylacetamide Show/Hide	C38H42N4O6S	1
1	IC50 = 24 nM
CP0271450 Compound Info	N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-pyrimidin-2-ylpyrimidin-4-yl]-2-phenylethanesulfonamide Show/Hide	C25H25N5O6S	1
1	IC50 = 25 nM
CP0134357 Compound Info	3-[1-Benzo[1,3]dioxol-5-yl-2-(4-isopropyl-benzenesulfonylamino)-2-oxo-ethyl]-1-ethyl-1H-indole-6-carboxylic acid Show/Hide	C29H28N2O7S	1
1	IC50 = 32 nM
CP0041337 Compound Info	5-Dimethylamino-naphthalene-1-sulfonic acid (3,4-dimethyl-2,3-dihydro-oxazol-5-yl)-amide Show/Hide	C17H19N3O3S	2
1	IC50 = 50.12 nM
2	IC50 = 150 nM
CP0305262 Compound Info	3-Benzo[1,3]dioxol-5-yl-1-benzo[1,3]dioxol-5-ylmethyl-5,6-dimethoxy-1H-indole-2-carboxylic acid Show/Hide	C26H21NO8	1
1	IC50 = 150 nM
CP0040571 Compound Info	4-Amino-N-(3,4-dimethyl-isoxazol-5-yl)-benzenesulfonamide Show/Hide	C11H13N3O3S	1
1	IC50 = 780 nM
CP0096733 Compound Info	N-(4-bromo-3-methyl-1,2-oxazol-5-yl)benzenesulfonamide Show/Hide	C10H9BrN2O3S	1
1	IC50 = 2510 nM
CP0082372 Compound Info	5-Benzyloxy-3-isopropoxy-benzo[b]thiophene-2-carboxylic acid Show/Hide	C19H18O4S	2
1	IC50 = 6000 nM
2	IC50 = 8800 nM
CP0077943 Compound Info	(2,5-Dibromo-3,4-dimethoxy-phenyl)-[4-(2-ethyl-5,7-dimethyl-imidazo[4,5-b]pyridin-3-ylmethyl)-2,6-dipropyl-phenoxy]-acetic acid Show/Hide	C33H39Br2N3O5	1
1	IC50 = 11000 nM
CP0050692 Compound Info	(1S,2R,3S)-1-Benzo[1,3]dioxol-5-yl-3-(2-carboxymethoxy-4-methoxy-phenyl)-5-propoxy-indan-2-carboxylic acid Show/Hide	C29H28O9	2
1	Ki = 0.2 nM
2	Ki = 0.43 nM
CP0186021 Compound Info	(1S,2R,3S)-1-Benzo[1,3]dioxol-5-yl-3-[2-(2-hydroxy-ethoxy)-4-methoxy-phenyl]-5-propoxy-indan-2-carboxylic acid Show/Hide	C29H30O8	1
1	Ki = 1.1 nM
CP0088035 Compound Info	4''-Oxazol-2-yl-biphenyl-2-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide Show/Hide	C20H17N3O4S	1
1	Ki = 1.4 nM
CP0113958 Compound Info	4''-(2-Butyl-4-oxo-1,3-diaza-spiro[4.4]non-1-en-3-ylmethyl)-2''-(3,3-dimethyl-2-oxo-pyrrolidin-1-ylmethyl)-biphenyl-2-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide Show/Hide	C36H45N5O5S	1
1	Ki = 1.9 nM
CP0016436 Compound Info	(S)-2-{(R)-3-Biphenyl-4-yl-2-[(3,5-dimethyl-benzoyl)-methyl-amino]-propionylamino}-3-(1H-indol-3-yl)-propionic acid Show/Hide	C36H35N3O4	1
1	Ki = 440 nM

Clinical Information about the Protein

Target 1 ( Endothelin A receptor (EDNRA) )

Target Type	Successful Target
Disease	10 Target-related Diseases				10
1	Pulmonary arterial hypertension [ICD-11: BB01.0]
2	Cardiovascular disease [ICD-11: BA00-BE2Z]
3	Hypotension [ICD-11: BA20-BA21]
4	Hypertension [ICD-11: BA00-BA04]
5	IgA nephropathy [ICD-11: MF8Y]
6	Diabetic nephropathy [ICD-11: GB61.Z]
7	Cerebral vasospasm [ICD-11: BA85.Z]
8	Prostate cancer [ICD-11: 2C82.0]
9	Arrhythmia [ICD-11: BC9Z]
10	Nerve injury [ICD-11: ND56.4]
Approved Drug(s)	4 Approved Drugs				4
1	Ambrisentan	Drug Info	Approved	Pulmonary arterial hypertension
2	Bosentan	Drug Info	Approved	Pulmonary arterial hypertension
3	Macitentan	Drug Info	Approved	Cardiovascular disease
4	Sparsentan	Drug Info	Approved	IgA nephropathy
Clinical Trial Drug(s)	7 Clinical Trial Drugs				7
1	Darusentan	Drug Info	Phase 3	Hypotension
2	BQ-123	Drug Info	Phase 2	Pulmonary arterial hypertension
3	PD-145065	Drug Info	Phase 2	Hypertension
4	TBC-3711	Drug Info	Phase 2	Hypotension
5	Atrasentan	Drug Info	Phase 3	Diabetic nephropathy
6	Clazosentan	Drug Info	Phase 3	Cerebral vasospasm
7	FR139317	Drug Info	Phase 2	Hypertension
Discontinued Drug(s)	11 Discontinued Drugs				11
1	Sitaxsentan	Drug Info	Withdrawn from market	Pulmonary arterial hypertension
2	Zibotentan	Drug Info	Discontinued in Phase 3	Prostate cancer
3	Avosentan	Drug Info	Discontinued in Phase 2	Diabetic nephropathy
4	BMS-193884	Drug Info	Discontinued in Phase 2	Pulmonary arterial hypertension
5	ENRASENTAN	Drug Info	Discontinued in Phase 2	Pulmonary arterial hypertension
6	J-104132	Drug Info	Discontinued in Phase 2	Pulmonary arterial hypertension
7	SB-209670	Drug Info	Discontinued in Phase 2	Arrhythmia
8	SB-234551	Drug Info	Discontinued in Phase 1	Nerve injury
9	BMS-182874	Drug Info	Terminated	Hypertension
10	BQ-518	Drug Info	Terminated	Hypertension
11	PD-155080	Drug Info	Terminated	Hypertension

Similar Protein(s) and Bioactivity Statistics

90% Identity

Protein ID	Protein Name	Protein Organism
PT01785	Endothelin-1 receptor	Rattus norvegicus, Rat	Protein Info
PT06168	Endothelin-1 receptor	Mus musculus, Mouse	Protein Info

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han