Protein Information

General Information of the Protein

Protein ID	PT01493
Protein Name	Beta-3 adrenergic receptor
Secondarily Protein Name	Beta-3 adrenoreceptor
Gene Name	ADRB3
Secondarily Gene Name	ADRB3R B3AR
Sequence	MAPWPHENSSLAPWPDLPTLAPNTANTSGLPGVPWEAALAGALLALAVLATVGGNLLVIVAIAWTPRLQTMTNVFVTSLAAADLVMGLLVVPPAATLALTGHWPLGATGCELWTSVDVLCVTASIETLCALAVDRYLAVTNPLRYGALVTKRCARTAVVLVWVVSAAVSFAPIMSQWWRVGADAEAQRCHSNPRCCAFASNMPYVLLSSSVSFYLPLLVMLFVYARVFVVATRQLRLLRGELGRFPPEESPPAPSRSLAPAPVGTCAPPEGVPACGRRPARLLPLREHRALCTLGLIMGTFTLCWLPFFLANVLRALGGPSLVPGPAFLALNWLGYANSAFNPLIYCRSPDFRSAFRRLLCRCGRRLPPEPCAAARPALFPSGVPAARSSPAQPRLCQRLDGASWGVS Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Membrane receptor > Family A G protein-coupled receptor > Small molecule receptor (family A GPCR) > Monoamine receptor > Adrenergic receptor
Function	Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. Beta-3 is involved in the regulation of lipolysis and thermogenesis. Show/Hide
Uniprot ID	Primary ID: P13945 Secondarily ID: Q4JFT4 Show/Hide
Ensembl ID	ENSG00000188778
HGNC ID	HGNC:288
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: CL000901 , 661W

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0411059 Compound Info	(3S,4S)-4-ethyl-3-methyl-1-phenyl-2,4-dihydroquinolin-3-amine Show/Hide	C18H22N2	1
1	Ki = 1000 nM Bioactivity Info	TI LI LO TS
CP0387083 Compound Info	(3aS,9bS)-3a-methyl-5-phenyl-2,3,4,9b-tetrahydro-1H-pyrrolo[2,3-c]quinoline Show/Hide	C18H20N2	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0391120 Compound Info	(1S,2R)-1-ethyl-7-methoxy-2-methyl-3,4-dihydro-1H-naphthalen-2-amine Show/Hide	C14H21NO	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0391121 Compound Info	(3S,4S)-4-ethyl-3,6-dimethyl-2,4-dihydrochromen-3-amine Show/Hide	C13H19NO	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0391154 Compound Info	(3aS,9bS)-7,9-dimethoxy-3a-methyl-2,3,4,9b-tetrahydro-1H-chromeno[3,4-b]pyrrole Show/Hide	C14H19NO3	1
1	Ki > 10000 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: CL000088 , Flp-In-293

Cell Line Info

Cell Line ID: CL000006 , HEK293

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0071872 Compound Info	(3-{2-[(R)-2-(3-Chloro-phenyl)-2-hydroxy-ethylamino]-propyl}-1H-indol-7-yloxy)-acetic acid Show/Hide	C21H23ClN2O4	1
1	EC50 = 0.062 nM
CP0217241 Compound Info	4'-(2-((1R,2S)-1-hydroxy-1-(4-hydroxyphenyl)propan-2-ylamino)ethyl)-3-isopropoxy-N-(methylsulfonyl)biphenyl-4-carboxamide Show/Hide	C28H34N2O6S	1
1	EC50 = 0.16 nM
CP0039168 Compound Info	[3-[(2R)-2-[[(2R)-2-hydroxy-2-[3-(thiophen-2-ylsulfonylamino)phenyl]ethyl]amino]propyl]-1H-indol-7-yl] methanesulfonate Show/Hide	C24H27N3O6S3	2
1	EC50 = 0.21 nM
2	Ki = 4 nM
CP0103438 Compound Info	[3-[(2R)-2-[[(2R)-2-hydroxy-2-[3-(thiophen-2-ylsulfonylamino)phenyl]ethyl]amino]propyl]-1H-indol-7-yl] pyridine-3-sulfonate Show/Hide	C28H28N4O6S3	1
1	EC50 = 0.26 nM
CP0039163 Compound Info	[3-[(2R)-2-[[(2R)-2-hydroxy-2-[3-(thiophen-2-ylsulfonylamino)phenyl]ethyl]amino]propyl]-1H-indol-7-yl] octane-1-sulfonate Show/Hide	C31H41N3O6S3	1
1	EC50 = 0.28 nM
CP0058502 Compound Info	(R)-1-(3-Chloro-phenyl)-2-[2-(7-methoxy-1H-indol-3-yl)-1-methyl-ethylamino]-ethanol Show/Hide	C20H23ClN2O2	1
1	EC50 = 0.36 nM
CP0047480 Compound Info	(S)-4-(3-hexylureido)-N-(4-(2-(1-hydroxy-2-(4-hydroxyphenoxy)ethylamino)ethyl)phenyl)benzenesulfonamide Show/Hide	C30H40N4O6S	1
1	EC50 = 0.43 nM
CP0118799 Compound Info	[3-[(2R)-2-[[(2R)-2-hydroxy-2-[3-(thiophen-2-ylsulfonylamino)phenyl]ethyl]amino]propyl]-1H-indol-7-yl] propane-2-sulfonate Show/Hide	C26H31N3O6S3	1
1	EC50 = 0.51 nM
CP0071878 Compound Info	N-[3-[(1R)-1-hydroxy-2-[[(2R)-1-(7-methoxy-1H-indol-3-yl)propan-2-yl]amino]ethyl]phenyl]thiophene-2-sulfonamide Show/Hide	C24H27N3O4S2	2
1	EC50 = 0.55 nM
2	Ki = 14 nM
CP0279836 Compound Info	Butane-1-sulfonic acid 3-(2-{(R)-(R)-2-hydroxy-2-[3-(thiophene-2-sulfonylamino)-phenyl]-ethylamino}-propyl)-1H-indol-7-yl ester Show/Hide	C27H33N3O6S3	1
1	EC50 = 0.59 nM
CP0118781 Compound Info	[3-[(2R)-2-[[(2R)-2-hydroxy-2-[3-(thiophen-2-ylsulfonylamino)phenyl]ethyl]amino]propyl]-1H-indol-7-yl] thiophene-2-sulfonate Show/Hide	C27H27N3O6S4	1
1	EC50 = 0.64 nM
CP0071879 Compound Info	N-[3-[(1R)-1-hydroxy-2-[[(2R)-1-(7-phenylmethoxy-1H-indol-3-yl)propan-2-yl]amino]ethyl]phenyl]thiophene-2-sulfonamide Show/Hide	C30H31N3O4S2	1
1	EC50 = 0.76 nM
CP0103437 Compound Info	Benzenesulfonic acid 3-(2-{(R)-(R)-2-hydroxy-2-[3-(thiophene-2-sulfonylamino)-phenyl]-ethylamino}-propyl)-1H-indol-7-yl ester Show/Hide	C29H29N3O6S3	1
1	EC50 = 0.87 nM
CP0071873 Compound Info	N-[3-[(1R)-1-hydroxy-2-[[(2R)-1-(1H-indol-3-yl)propan-2-yl]amino]ethyl]phenyl]thiophene-2-sulfonamide Show/Hide	C23H25N3O3S2	2
1	EC50 = 0.88 nM
2	Ki = 30 nM
CP0039162 Compound Info	[3-[(2R)-2-[[(2R)-2-[3-[[(E)-but-2-enyl]amino]phenyl]-2-hydroxyethyl]amino]propyl]-1H-indol-7-yl] methanesulfonate Show/Hide	C24H31N3O4S	1
1	EC50 = 1.2 nM
CP0075978 Compound Info	2-[[3-[(2R)-2-[[(2R)-2-hydroxy-2-[3-(thiophen-2-ylsulfonylamino)phenyl]ethyl]amino]propyl]-1H-indol-7-yl]oxy]acetic acid Show/Hide	C25H27N3O6S2	2
1	EC50 = 1.7 nM
2	Ki = 17 nM
CP0198056 Compound Info	[3-[(2R)-2-[[(2R)-2-hydroxy-2-[3-(naphthalen-2-ylmethylamino)phenyl]ethyl]amino]propyl]-1H-indol-7-yl] methanesulfonate Show/Hide	C31H33N3O4S	1
1	EC50 = 2.9 nM
CP0198066 Compound Info	(R)-1-((R)-3-Chloro-phenyl)-2-[2-(1H-indol-3-yl)-1-methyl-ethylamino]-ethanol Show/Hide	C19H21ClN2O	1
1	EC50 = 5.4 nM
CP0279585 Compound Info	4-(3-Hexyl-ureido)-N-{4-[2-((R)-2-hydroxy-2-pyridin-3-yl-ethylamino)-ethyl]-phenyl}-benzenesulfonamide Show/Hide	C28H37N5O4S	1
1	EC50 = 6.3 nM
CP0279642 Compound Info	(S)-N-(4-(2-(2-hydroxy-3-(4-hydroxyphenoxy)propylamino)ethyl)phenyl)benzenesulfonamide Show/Hide	C23H26N2O5S	1
1	EC50 = 6.3 nM
CP0058497 Compound Info	[3-[(2R)-2-[[(2R)-2-hydroxy-2-[3-(prop-2-ynylamino)phenyl]ethyl]amino]propyl]-1H-indol-7-yl] methanesulfonate Show/Hide	C23H27N3O4S	1
1	EC50 = 10 nM
CP0277683 Compound Info	4-(3-Hexyl-2-oxo-2,3-dihydro-imidazol-1-yl)-N-{4-[2-((R)-2-hydroxy-2-pyridin-3-yl-ethylamino)-ethyl]-phenyl}-benzenesulfonamide Show/Hide	C30H37N5O4S	1
1	EC50 = 14 nM
CP0071877 Compound Info	(+/-)-2-(4-((R)-2-((R)-2-(3-chlorophenyl)-2-hydroxyethylamino)propyl)phenoxy)acetic acid Show/Hide	C19H22ClNO4	1
1	EC50 = 21 nM
CP0039161 Compound Info	[3-[(2R)-2-[[(2R)-2-hydroxy-2-[3-(3-methylbut-2-enylamino)phenyl]ethyl]amino]propyl]-1H-indol-7-yl] methanesulfonate Show/Hide	C25H33N3O4S	1
1	EC50 = 36 nM
CP0144828 Compound Info	(4-{(R)-2-[(R)-2-(3-Chloro-phenyl)-2-hydroxy-ethylamino]-propyl}-phenoxy)-methanesulfonic acid Show/Hide	C18H22ClNO5S	1
1	EC50 = 60 nM
CP0288880 Compound Info	ethyl 2-[[(6S)-6-[[(2R)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]-6,7,8,9-tetrahydro-5H-benzo[7]annulen-3-yl]oxy]acetate Show/Hide	C23H28ClNO4	1
1	EC50 < 100 nM
CP0039165 Compound Info	(S)-1-((R)-3-Chloro-phenyl)-2-[2-(1H-indol-3-yl)-1-methyl-ethylamino]-ethanol Show/Hide	C19H21ClN2O	1
1	EC50 = 220 nM
CP0718208 Compound Info	SID50106054 Show/Hide	C20H18ClNNa2O7	1
1	EC50 = 220 nM
CP0144775 Compound Info	(4-{(R)-2-[(S)-2-Hydroxy-3-(4-hydroxy-3-methanesulfonylamino-phenoxy)-propylamino]-propyl}-phenoxymethyl)-phenyl-phosphinic acid Show/Hide	C26H33N2O8PS	1
1	EC50 < 300 nM
CP0067545 Compound Info	1-(1-Benzyl-1,2,3,4-tetrahydroquinolin-6-yloxy)-3-isopropylaminopropan-2-ol Show/Hide	C22H30N2O2	1
1	IC50 = 590 nM
CP0247615 Compound Info	1-(1-Benzyl-1,2,3,4-tetrahydroquinolin-6-yloxy)-3-[2-(4-methoxyphenyl)ethylamino]propan-2-ol Show/Hide	C28H34N2O3	1
1	IC50 = 1180 nM
CP0133061 Compound Info	3-Amino-N-(3-{(R)-1-hydroxy-2-[(R)-2-(7-methanesulfonyl-1H-indol-3-yl)-1-methyl-ethylamino]-ethyl}-phenyl)-benzenesulfonamide Show/Hide	C26H30N4O5S2	1
1	Ki = 1.1 nM
CP0133084 Compound Info	3-Amino-N-(3-{(R)-1-hydroxy-2-[2-(7-methanesulfonyl-1H-indol-3-yl)-ethylamino]-ethyl}-phenyl)-benzenesulfonamide Show/Hide	C25H28N4O5S2	1
1	Ki = 2.6 nM
CP0307131 Compound Info	[3-[2-[[(2R)-2-hydroxy-2-[3-(thiophen-2-ylsulfonylamino)phenyl]ethyl]amino]ethyl]-1H-indol-7-yl] methanesulfonate Show/Hide	C23H25N3O6S3	1
1	Ki = 33 nM

Clinical Information about the Protein

Target 1 ( Adrenergic receptor beta-3 (ADRB3) )

Target Type	Successful Target
Disease	9 Target-related Diseases				9
1	Hypertension [ICD-11: BA00-BA04]
2	Angina pectoris [ICD-11: BA40]
3	Overactive bladder [ICD-11: GC50.0]
4	Dystonia [ICD-11: 8A02]
5	Heart failure with reduced ejection fraction [ICD-11: BD11.2]
6	Obesity [ICD-11: 5B81]
7	Urinary incontinence [ICD-11: MF50.2]
8	Diabetic complication [ICD-11: 5A2Y]
9	Type-2 diabetes [ICD-11: 5A11]
Approved Drug(s)	6 Approved Drugs				6
1	Amosulalol	Drug Info	Approved	Hypertension
2	Bopindolol	Drug Info	Approved	Hypertension
3	Mepindolol	Drug Info	Approved	Angina pectoris
4	Mirabegron	Drug Info	Approved	Overactive bladder
5	Trihexyphenidyl	Drug Info	Approved	Dystonia
6	Vibegron	Drug Info	Approved	Overactive bladder
Clinical Trial Drug(s)	5 Clinical Trial Drugs				5
1	APD418	Drug Info	Phase 2	Heart failure with reduced ejection fraction
2	CL-316,243	Drug Info	Phase 2	Obesity
3	GW-427353	Drug Info	Phase 2	Urinary incontinence
4	LY-377604	Drug Info	Phase 2	Obesity
5	BMS-196085	Drug Info	Phase 1	Diabetic complication
Discontinued Drug(s)	5 Discontinued Drugs				5
1	Epanolol	Drug Info	Discontinued in Preregistration	Angina pectoris
2	Rafabegron	Drug Info	Discontinued in Phase 2	Type-2 diabetes
3	Tienoxolol	Drug Info	Discontinued in Phase 2	Hypertension
4	PAFENOLOL	Drug Info	Discontinued in Phase 1	Hypertension
5	BMS-210285	Drug Info	Terminated	Type-2 diabetes
Preclinical Drug(s)	2 Preclinical Drugs				2
1	L-742791	Drug Info	Preclinical	Obesity
2	L-751250	Drug Info	Preclinical	Obesity

Similar Protein(s) and Bioactivity Statistics

50% Identity

Protein ID	Protein Name	Protein Organism
PT04360	Beta-3 adrenergic receptor	Rattus norvegicus, Rat	Protein Info
PT06057	Beta-3 adrenergic receptor	Canis lupus familiaris, Dog, Canis familiaris	Protein Info
PT06423	Beta-3 adrenergic receptor	Macaca mulatta, Rhesus macaque	Protein Info

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han