Protein Information

General Information of the Protein

Protein ID	PT01089
Protein Name	Alpha-1A adrenergic receptor
Secondarily Protein Name	Alpha-1A adrenoreceptor Alpha-1C adrenergic receptor Alpha-adrenergic receptor 1c
Gene Name	ADRA1A
Secondarily Gene Name	ADRA1C
Sequence	MVFLSGNASDSSNCTQPPAPVNISKAILLGVILGGLILFGVLGNILVILSVACHRHLHSVTHYYIVNLAVADLLLTSTVLPFSAIFEVLGYWAFGRVFCNIWAAVDVLCCTASIMGLCIISIDRYIGVSYPLRYPTIVTQRRGLMALLCVWALSLVISIGPLFGWRQPAPEDETICQINEEPGYVLFSALGSFYLPLAIILVMYCRVYVVAKRESRGLKSGLKTDKSDSEQVTLRIHRKNAPAGGSGMASAKTKTHFSVRLLKFSREKKAAKTLGIVVGCFVLCWLPFFLVMPIGSFFPDFKPSETVFKIVFWLGYLNSCINPIIYPCSSQEFKKAFQNVLRIQCLCRKQSSKHALGYTLHPPSQAVEGQHKDMVRIPVGSRETFYRISKTDGVCEWKFFSSMPRGSARITVSKDQSSCTTARVRSKSFLQVCCCVGPSTPSLDKNHQVPTIKVHTISLSENGEEV 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	This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes. Show/Hide
Uniprot ID	Primary ID: P35348 Secondarily ID: A8K0I3 B0ZBD1 B0ZBD2 B0ZBD4 B0ZBD5 B0ZBD6 B0ZBD8 B0ZBD9 O60451 Q13675 Q13729 Q4VBM7 Q6RUJ4 Q6RUJ5 Q6RUJ7 Q6RUJ8 Q6RUJ9 Q96RE8 Q9UD63 Q9UD67 Show/Hide
Ensembl ID	ENSG00000120907
HGNC ID	HGNC:277
Subcellular Location	Nucleus membrane Cell membrane Cytoplasm Membrane Caveola

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 = 1584.89 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: CL000880 , COS

Cell Line Info

Cell Line ID: CL000109 , COS-1

Cell Line Info

Cell Line ID: CL000053 , COS-7

Cell Line Info

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000065 , HEK293-EBNA

Cell Line Info

Cell Line ID: CL000101 , L-M(TK-)

Cell Line Info

Cell Line ID: CL000440 , LM

Cell Line Info

Cell Line ID: CL000019 , Rat1

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0049024 Compound Info	1-(4-Amino-6,7-dimethoxy-2-quinazolinyl)-4-((tetrahydro-2-furanyl)carbonyl)piperazine Show/Hide	C19H25N5O4	8
1	EC50 = 51 nM
2	Ki = 2 nM
3	Ki = 4 nM
4	Ki = 4.2 nM
5	Ki = 6.9 nM
6	Ki = 6.918 nM
7	Ki = 7.3 nM
8	Ki = 39.81 nM
CP0039841 Compound Info	ABT-866 Show/Hide	C12H15N3O2S	1
1	EC50 = 600 nM
CP0043740 Compound Info	1-[4-(2-methoxyphenyl)-1-piperazinyl]-3-(1-naphthalenyloxy)-2-propanol;hydrochloride Show/Hide	C24H28N2O3	1
1	IC50 = 555 nM
CP0035002 Compound Info	(R)-5-(2-((2-(2-ethoxyphenoxy)ethyl)amino)propyl)-2-methoxybenzenesulfonamide Show/Hide	C20H28N2O5S	3
1	Ki = 0.029 nM
2	Ki = 0.13 nM
3	Ki = 0.19 nM
CP0013593 Compound Info	1-(3-Hydroxy-propyl)-5-((R)-2-{2-[2-(2,2,2-trifluoro-ethoxy)-phenoxy]-ethylamino}-propyl)-2,3-dihydro-1H-indole-7-carboxylic acid amide Show/Hide	C25H32F3N3O4	1
1	Ki = 0.03981 nM
CP0082953 Compound Info	2,3-dihydro-1,4-benzodioxin-3-ylmethyl-[2-(2,6-dimethoxyphenoxy)ethyl]amine;hydrochloride Show/Hide	C19H23NO5	3
1	Ki = 0.1585 nM
2	Ki = 0.37 nM
3	Ki = 0.4266 nM
CP0087323 Compound Info	Niguldipine Show/Hide	C36H39N3O6	1
1	Ki = 0.16 nM
CP0040814 Compound Info	[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-(furan-2-yl)methanone Show/Hide	C19H21N5O4	6
1	Ki = 0.1995 nM
2	Ki = 0.27 nM
3	Ki = 0.39 nM
4	Ki = 0.51 nM
5	Ki = 0.58 nM
6	Ki = 0.61 nM
CP0645895 Compound Info	SID50112869 Show/Hide	C36H40N4O5	3
1	Ki = 0.2 nM
2	Ki = 0.3467 nM
3	Ki = 0.35 nM
CP0055045 Compound Info	2-{2-[4-(2-Methoxy-phenyl)-piperazin-1-yl]-ethyl}-4,9-dihydro-2,4,9-triaza-fluorene-1,3-dione Show/Hide	C23H25N5O3	1
1	Ki = 0.2692 nM
CP0192450 Compound Info	3-(3-{3-[4-Fluoro-2-(2,2,2-trifluoro-ethoxy)-phenyl]-piperazin-1-yl}-propyl)-5-methyl-1H-pyrimidine-2,4-dione Show/Hide	C20H24F4N4O3	1
1	Ki = 1 nM
CP0345915 Compound Info	3-Methyl-4-oxo-2-phenyl-4H-chromene-8-carboxylic acid {3-[4-(2-methoxy-phenyl)-piperazin-1-yl]-propyl}-amide Show/Hide	C31H33N3O4	1
1	Ki = 1 nM
CP0654918 Compound Info	rac-N3-(3-(4,4-diphenylpiperidin-1-yl)propyl)-2,6-dimethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxamide Show/Hide	C35H39N5O4	1
1	Ki = 1.87 nM
CP0048996 Compound Info	CAS_74191-85-8 Show/Hide	C23H25N5O5	2
1	Ki = 2.6 nM
2	Ki = 3.162 nM
CP0040436 Compound Info	5-N-[3-(4,4-diphenylpiperidin-1-yl)propyl]-3-N,2,6-trimethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxamide Show/Hide	C36H41N5O4	2
1	Ki = 3.162 nM
2	Ki = 4.467 nM
CP0327530 Compound Info	[(4aR,8aS)-4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-2,3,4a,5,6,7,8,8a-octahydroquinoxalin-1-yl]-(2,3-dihydro-1,4-benzodioxin-3-yl)methanone Show/Hide	C27H31N5O5	1
1	Ki = 3.388 nM
CP0095298 Compound Info	(R)-3-fluoro-1-((5-fluoro-1-(1H-imidazol-2-yl)-2,3-dihydro-1H-inden-4-yl)methyl)-1H-pyrazole Show/Hide	C16H14F2N4	1
1	Ki = 5 nM
CP0239195 Compound Info	6-(3,5-dimethyl-4-isoxazolylsulfonamido)-1'-[2-(1-naphthyl)ethyl]-4-oxospiro[3,4-dihydro-2H-chromene-2,4'-(hexahydropyridine)] Show/Hide	C30H31N3O5S	1
1	Ki = 10 nM
CP0037866 Compound Info	CAS_146714-97-8 Show/Hide	C25H34N4O2	1
1	Ki = 20 nM
CP0048998 Compound Info	5-Chloro-8-methyl-1-vinyl-6,7,8,9-tetrahydro-2-thia-8-aza-benzo[cd]azulene Show/Hide	C14H14ClNS	2
1	Ki = 25.12 nM
2	Ki = 36 nM
CP0097484 Compound Info	CYCLAZOSIN Show/Hide	C23H27N5O4	1
1	Ki = 25.12 nM
CP0714031 Compound Info	SID50105948 Show/Hide	C22H33Cl2N3O3	2
1	Ki = 42.66 nM
2	Ki = 251.19 nM
CP0148986 Compound Info	(R)-2-(5-chloro-4-(methoxymethyl)-2,3-dihydro-1H-inden-1-yl)-1H-imidazole Show/Hide	C14H15ClN2O	1
1	Ki = 83 nM
CP0126495 Compound Info	N-[(9-amino-6,7-dimethoxy-1,2,3,4-tetrahydroacridin-3-yl)methyl]-4-(trifluoromethyl)benzamide Show/Hide	C24H24F3N3O3	1
1	Ki = 85.11 nM
CP0121063 Compound Info	1-(1,4-dioxaspiro[4.5]decan-3-ylmethyl)-4-(2-methoxyphenyl)piperazine Show/Hide	C20H30N2O3	1
1	Ki = 91.2 nM
CP0061623 Compound Info	8-(2-(4-(2-methoxyphenyl)piperazin-1-yl)ethyl)-8-azaspiro[4.5]decane-7,9-dione Show/Hide	C22H31N3O3	5
1	Ki = 130 nM
2	Ki = 251 nM
3	Ki = 290 nM
4	Ki = 294 nM
5	Ki = 380.19 nM
CP0037227 Compound Info	7-(dipropylamino)-5,6,7,8-tetrahydronaphthalen-1-ol Show/Hide	C16H25NO	3
1	Ki = 1757 nM
2	Ki = 1757.2 nM
3	Ki < 1000 nM
CP0002071 Compound Info	N-[2-(5-methoxy-1H-indol-3-yl)ethyl]-N-prop-2-enylprop-2-en-1-amine Show/Hide	C17H22N2O	1
1	Ki < 10000 nM

Clinical Information about the Protein

Target 1 ( Adrenergic receptor alpha-1A (ADRA1A) )

Target Type	Successful Target
Disease	6 Target-related Diseases				6
1	Hypertension [ICD-11: BA00-BA04]
2	Benign prostatic hyperplasia [ICD-11: GA90]
3	Cognitive impairment [ICD-11: 6D71]
4	Pain [ICD-11: MG30-MG3Z]
5	Prostate disease [ICD-11: GA91]
6	Stress urinary incontinence [ICD-11: MF50.20]
Approved Drug(s)	4 Approved Drugs				4
1	NAFTOPIDIL	Drug Info	Approved	Hypertension
2	SILODOSIN	Drug Info	Approved	Benign prostatic hyperplasia
3	Tamsulosin	Drug Info	Approved	Benign prostatic hyperplasia
4	Xatral	Drug Info	Approved	Benign prostatic hyperplasia
Clinical Trial Drug(s)	2 Clinical Trial Drugs				2
1	Besipirdine	Drug Info	Phase 3	Cognitive impairment
2	MEDETOMIDINE	Drug Info	Phase 2	Pain
Discontinued Drug(s)	4 Discontinued Drugs				4
1	L-771688	Drug Info	Discontinued in Phase 2	Prostate disease
2	REC-15-2739	Drug Info	Discontinued in Phase 2	Prostate disease
3	RS-100975	Drug Info	Discontinued in Phase 1	Prostate disease
4	A-204176	Drug Info	Terminated	Stress urinary incontinence

Similar Protein(s) and Bioactivity Statistics

90% Identity

Protein ID	Protein Name	Protein Organism
PT01339	Alpha-1A adrenergic receptor	Rattus norvegicus, Rat	Protein Info
PT02060	Alpha-1A adrenergic receptor	Bos taurus, Bovine	Protein Info

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han