General Information of the Protein
Protein ID
PT01197
Protein Name
Type-1 angiotensin II receptor
Secondarily
Protein Name
AT1AR
AT1BR
Angiotensin II type-1 receptor
Gene Name
AGTR1
Secondarily
Gene Name
AGTR1A
AGTR1B
AT2R1
AT2R1B
Sequence
MILNSSTEDGIKRIQDDCPKAGRHNYIFVMIPTLYSIIFVVGIFGNSLVVIVIYFYMKLKTVASVFLLNLALADLCFLLTLPLWAVYTAMEYRWPFGNYLCKIASASVSFNLYASVFLLTCLSIDRYLAIVHPMKSRLRRTMLVAKVTCIIIWLLAGLASLPAIIHRNVFFIENTNITVCAFHYESQNSTLPIGLGLTKNILGFLFPFLIILTSYTLIWKALKKAYEIQKNKPRNDDIFKIIMAIVLFFFFSWIPHQIFTFLDVLIQLGIIRDCRIADIVDTAMPITICIAYFNNCLNPLFYGFLGKKFKRYFLQLLKYIPPKAKSHSNLSTKMSTLSYRPSDNVSSSTKKPAPCFEVE
    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)
>
Angiotensin receptor
Function
Receptor for angiotensin II, a vasoconstricting peptide, which acts as a key regulator of blood pressure and sodium retention by the kidney (PubMed:1567413, PubMed:8987975, PubMed:15611106, PubMed:25913193, PubMed:26420482, PubMed:30639100, PubMed:32079768). The activated receptor in turn couples to G-alpha proteins G(q) (GNAQ, GNA11, GNA14 or GNA15) and thus activates phospholipase C and increases the cytosolic Ca(2+) concentrations, which in turn triggers cellular responses such as stimulation of protein kinase C (PubMed:15611106).
    Show/Hide
Uniprot ID
Primary ID:
P30556

Secondarily ID:
Q13725
Q8TBK4
    Show/Hide
Ensembl ID
ENSG00000144891
HGNC ID
HGNC:336
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: CL000880 , COS
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0449141
 Compound Info 
3-(5,7-Dimethyl-2-propyl-imidazo[4,5-b]pyridin-3-ylmethyl)-11-(1H-tetrazol-5-yl)-dibenzo[a,d]cyclohepten-5-one
   Show/Hide
C28H25N7O
  1
1
Ki = 0.29 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0532731
 Compound Info 
3-(2-Cyclopropyl-5,7-dimethyl-imidazo[4,5-b]pyridin-3-ylmethyl)-11-(1H-tetrazol-5-yl)-dibenzo[a,d]cyclohepten-5-one
   Show/Hide
C28H23N7O
  1
1
Ki = 0.45 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0476963
 Compound Info 
3-(2-Ethyl-6-methoxy-[1,5]naphthyridin-4-yloxymethyl)-11-(1H-tetrazol-5-yl)-dibenzo[a,d]cyclohepten-5-one
   Show/Hide
C28H22N6O3
  1
1
Ki = 0.48 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0507237
 Compound Info 
5,7-Dimethyl-2-propyl-3-[11-(1H-tetrazol-5-yl)-5H-dibenzo[a,d]cyclohepten-3-ylmethyl]-3H-imidazo[4,5-b]pyridine
   Show/Hide
C28H27N7
  1
1
Ki = 0.49 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0384158
 Compound Info 
3-(2-Ethyl-quinolin-4-yloxymethyl)-11-(1H-tetrazol-5-yl)-dibenzo[a,d]cyclohepten-5-one
   Show/Hide
C28H21N5O2
  1
1
Ki = 0.65 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0466031
 Compound Info 
3-(2-Ethyl-5,7-dimethyl-imidazo[4,5-b]pyridin-3-ylmethyl)-11-(1H-tetrazol-5-yl)-dibenzo[a,d]cyclohepten-5-one
   Show/Hide
C27H23N7O
  1
1
Ki = 0.66 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0395442
 Compound Info 
5,7-Dimethyl-2-propyl-3-[11-(1H-tetrazol-5-yl)-dibenzo[b,f]oxepin-3-ylmethyl]-3H-imidazo[4,5-b]pyridine
   Show/Hide
C27H25N7O
  1
1
Ki = 0.7 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0488957
 Compound Info 
3-[(5-Ethyl-pyrazolo[1,5-a]pyrimidin-7-ylamino)-methyl]-11-(1H-tetrazol-5-yl)-dibenzo[a,d]cyclohepten-5-one
   Show/Hide
C25H20N8O
  1
1
Ki = 1.1 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0498353
 Compound Info 
3-(2-Ethyl-5,6,7,8-tetrahydro-quinolin-4-yloxymethyl)-11-(1H-tetrazol-5-yl)-dibenzo[a,d]cyclohepten-5-one
   Show/Hide
C28H25N5O2
  1
1
Ki = 1.3 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0453436
 Compound Info 
2-Butyl-5-chloro-3-[5-oxo-11-(1H-tetrazol-5-yl)-5H-dibenzo[a,d]cyclohepten-3-ylmethyl]-3H-imidazole-4-carboxylic acid
   Show/Hide
C25H21ClN6O3
  1
1
Ki = 2.1 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0463883
 Compound Info 
2-Ethyl-4-[5-oxo-11-(1H-tetrazol-5-yl)-5H-dibenzo[a,d]cyclohepten-3-ylmethoxy]-quinoline-6-carboxylic acid
   Show/Hide
C29H21N5O4
  1
1
Ki = 2.7 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0540251
 Compound Info 
2-Ethoxy-3-[5-oxo-11-(1H-tetrazol-5-yl)-5H-dibenzo[a,d]cyclohepten-3-ylmethyl]-3H-benzoimidazole-4-carboxylic acid
   Show/Hide
C27H20N6O4
  1
1
Ki = 2.7 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0544900
 Compound Info 
2,6-Dimethyl-4-{[5-oxo-11-(1H-tetrazol-5-yl)-5H-dibenzo[a,d]cyclohepten-3-ylmethyl]-amino}-nicotinic acid ethyl ester
   Show/Hide
C27H24N6O3
  1
1
Ki = 2.9 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0448269
 Compound Info 
2-Ethoxy-3-[11-(1H-tetrazol-5-yl)-dibenzo[b,f]oxepin-3-ylmethyl]-3H-benzoimidazole-4-carboxylic acid
   Show/Hide
C26H20N6O4
  1
1
Ki = 3.9 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0479908
 Compound Info 
2,6-Dimethyl-4-[5-oxo-11-(1H-tetrazol-5-yl)-5H-dibenzo[a,d]cyclohepten-3-ylmethoxy]-nicotinic acid ethyl ester
   Show/Hide
C27H23N5O4
  1
1
Ki = 4.3 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0544903
 Compound Info 
3-(2-Methyl-5,6,7,8-tetrahydro-quinolin-4-yloxymethyl)-11-(1H-tetrazol-5-yl)-dibenzo[a,d]cyclohepten-5-one
   Show/Hide
C27H23N5O2
  1
1
Ki = 4.3 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0461038
 Compound Info 
(S)-3-Methyl-2-{[5-oxo-11-(1H-tetrazol-5-yl)-5H-dibenzo[a,d]cyclohepten-3-ylmethyl]-pentanoyl-amino}-butyric acid
   Show/Hide
C27H29N5O4
  1
1
Ki = 8.7 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0448379
 Compound Info 
(S)-3-Methyl-2-{pentanoyl-[11-(1H-tetrazol-5-yl)-dibenzo[b,f]oxepin-3-ylmethyl]-amino}-butyric acid
   Show/Hide
C26H29N5O4
  1
1
Ki = 9.6 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0468051
 Compound Info 
2-Butyl-5-chloro-3-[5-oxo-11-(1H-tetrazol-5-yl)-5H-dibenzo[a,d]cyclohepten-3-ylmethyl]-3H-imidazole-4-carbaldehyde
   Show/Hide
C25H21ClN6O2
  1
1
Ki = 12 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: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000050 , HEK293-A
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0169597
 Compound Info 
(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-(methylamino)acetyl]amino]pentanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]propanoic acid
   Show/Hide
C43H68N14O10
  1
1 EC50 = 44 nM
CP0043276
 Compound Info 
CAS_114798-26-4
   Show/Hide
C22H23ClN6O
  5
1 IC50 = 0.33 nM
2 IC50 = 8 nM
3 IC50 = 16.2 nM
4 IC50 = 28 nM
5 IC50 = 350 nM
CP0035923
 Compound Info 
(S)-2-((S)-1-((S)-2-((S)-2-((S)-2-((S)-2-((S)-5-(diaminomethyleneamino)-2-(2-(methylamino)acetamido)pentanamido)-3-methylbutanamido)-3-(4-hydroxyphenyl)propanamido)-3-methylbutanamido)-3-(1H-imidazol-5-yl)propanoyl)pyrrolidine-5-carboxamido)propanoic acid
   Show/Hide
C42H65N13O10
  8
1 IC50 = 0.35 nM
2 IC50 = 0.57 nM
3 IC50 = 0.6 nM
4 IC50 = 0.67 nM
5 IC50 = 1 nM
6 Ki = 0.17 nM
7 Ki = 0.22 nM
8 Ki = 0.33 nM
CP0083167
 Compound Info 
4'-((1,4'-dimethyl-2'-propyl(2,6'-bi-1H-benzimidazol)-1'-yl)methyl)-(1,1'-biphenyl)-2-carboxylic acid
   Show/Hide
C33H30N4O2
  5
1 IC50 = 0.49 nM
2 IC50 = 1 nM
3 IC50 = 2 nM
4 IC50 = 3 nM
5 IC50 = 150 nM
CP0158590
 Compound Info 
7-methyl-N-(2-phenylpropyl)-2-propyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]benzimidazole-5-carboxamide
   Show/Hide
C35H35N7O
  1
1 IC50 = 0.9 nM
CP0129932
 Compound Info 
3-[(2'-(butylsulfonylcarbamate)-3'-propyl-1,1'-biphenyl-4-yl)methyl]-2-ethyl-5,7-dimethyl-3H-imidazo[4,5-b]pyridine
   Show/Hide
C31H38N4O4S
  1
1 IC50 = 1.5 nM
CP0041674
 Compound Info 
(S)-3-Methyl-2-{pentanoyl-[2'-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-amino}-butyric acid
   Show/Hide
C24H29N5O3
  2
1 IC50 = 2.7 nM
2 Ki = 4700 nM
CP0066395
 Compound Info 
2-[4-[[4-methyl-6-(2-phenylethylcarbamoyl)-2-propylbenzimidazol-1-yl]methyl]phenyl]benzoic acid
   Show/Hide
C34H33N3O3
  1
1 IC50 = 3 nM
CP0041261
 Compound Info 
2-butyl-3-{[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl}-1,3-diazaspiro[4.4]non-1-en-4-one
   Show/Hide
C25H28N6O
  3
1 IC50 = 20.8 nM
2 Ki = 0.8 nM
3 Ki = 1.1 nM
CP0114119
 Compound Info 
2-Ethoxy-3-[2'-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3H-benzoimidazole-4-carboxylic acid(CV-11974)
   Show/Hide
C24H20N6O3
  1
1 IC50 = 110 nM
CP0036566
 Compound Info 
5-L-isoleucineangiotensin II
   Show/Hide
C50H71N13O12
  1
1 Kd = 2 nM
CP0451213
 Compound Info 
(2S,3S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-(methylamino)acetyl]amino]pentanoyl]amino]-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]-3-methylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoic acid
   Show/Hide
C42H73N13O9
  1
1 Kd = 300 nM
CP0047101
 Compound Info 
(1-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-2-butyl-4-chloro-1H-imidazol-5-yl)methanol
   Show/Hide
C23H29N3O4S2
  2
1 Ki = 10000 nM
2 Ki > 10000 nM
CP0083007
 Compound Info 
butyl N-[3-[3-(imidazol-1-ylmethyl)phenyl]-5-(2-methylpropyl)thiophen-2-yl]sulfonylcarbamate
   Show/Hide
C23H29N3O4S2
  1
1 Ki > 10000 nM
Clinical Information about the Protein
Target 1 ( Angiotensin II receptor type-1 (AGTR1) )
Target Type Successful Target
Disease 6 Target-related Diseases  6
1 Increase blood pressure [ICD-11: BA04]
2 Hypertension [ICD-11: BA00-BA04]
3 High blood pressure [ICD-11: BA00]
4 IgA nephropathy [ICD-11: MF8Y]
5 Heart failure [ICD-11: BD10-BD13]
6 Hypotension [ICD-11: BA20-BA21]
Approved Drug(s) 14 Approved Drugs  14
1 ANGIOTENSIN II
 Drug Info 
Approved
Increase blood pressure
2 Azilsartan
 Drug Info 
Approved
Hypertension
3 Candesartan
 Drug Info 
Approved
Hypertension
4 Eprosartan
 Drug Info 
Approved
Hypertension
5 Forasartan
 Drug Info 
Approved
Hypertension
6 Irbesartan
 Drug Info 
Approved
Hypertension
7 Losartan
 Drug Info 
Approved
Hypertension
8 Olmesartan medoxomil
 Drug Info 
Approved
High blood pressure
9 Saprisartan
 Drug Info 
Approved
Hypertension
10 SARALASIN
 Drug Info 
Approved
Hypertension
11 Tasosartan
 Drug Info 
Approved
Hypertension
12 Telmisartan
 Drug Info 
Approved
Hypertension
13 Valsartan
 Drug Info 
Approved
Hypertension
14 Sparsentan
 Drug Info 
Approved
IgA nephropathy
Clinical Trial Drug(s) 4 Clinical Trial Drugs  4
1 Pratosartan
 Drug Info 
Phase 3
Hypertension
2 CL-329167
 Drug Info 
Phase 2
Hypertension
3 TRV027
 Drug Info 
Phase 2
Heart failure
4 YM-358
 Drug Info 
Phase 2
Hypertension
Discontinued Drug(s) 7 Discontinued Drugs  7
1 MILFASARTAN
 Drug Info 
Discontinued in Phase 2
Hypertension
2 RIPISARTAN
 Drug Info 
Discontinued in Phase 2
Hypertension
3 Zolasartan
 Drug Info 
Discontinued in Phase 2
Hypotension
4 A-81988
 Drug Info 
Terminated
Hypertension
5 L-158809
 Drug Info 
Terminated
Hypertension
6 L-159689
 Drug Info 
Terminated
Hypertension
7 XR-510
 Drug Info 
Terminated
Hypertension
Target 2 ( HUMAN type-1 angiotensin II receptor (AGTR1) )
Target Type Unknown Type Target
Disease 1 Target-related Disease  1
1 Hypertension [ICD-11: BA00-BA04]
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 Losartan
 Drug Info 
Approved
Hypertension
2 Telmisartan
 Drug Info 
Approved
Hypertension
Investigative Drug(s) 1 Investigative Drug  1
1 Irbesartan
 Drug Info 
Approved
Hypertension
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT04214 Type-1 angiotensin II receptor A Rattus norvegicus, Rat
 Protein Info 
PT06588 Type-1 angiotensin II receptor A Mus musculus, Mouse
 Protein Info