AGTR1
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Also known as AT1AT2R1AGTR1AAT2R1AHAT1RAG2SAT2R1BAT1BATR1
Summary
AGTR1 (angiotensin II receptor type 1, HGNC:336) is a protein-coding gene on chromosome 3q24, encoding Type-1 angiotensin II receptor (P30556). Receptor for angiotensin II, a vasoconstricting peptide, which acts as a key regulator of blood pressure and sodium retention by the kidney.
Angiotensin II is a potent vasopressor hormone and a primary regulator of aldosterone secretion. It is an important effector controlling blood pressure and volume in the cardiovascular system. It acts through at least two types of receptors. This gene encodes the type 1 receptor which is thought to mediate the major cardiovascular effects of angiotensin II. This gene may play a role in the generation of reperfusion arrhythmias following restoration of blood flow to ischemic or infarcted myocardium. It was previously thought that a related gene, denoted as AGTR1B, existed; however, it is now believed that there is only one type 1 receptor gene in humans. Alternative splicing of this gene results in multiple transcript variants.
Source: NCBI Gene 185 — RefSeq curated summary.
At a glance
- Gene–disease (curated): renal tubular dysgenesis of genetic origin (Strong, GenCC) — +1 more curated relationship
- GWAS associations: 6
- Clinical variants (ClinVar): 184 total — 5 pathogenic, 9 likely-pathogenic
- Phenotypes (HPO): 15
- Druggable target: yes — 88 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_000685
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:336 |
| Approved symbol | AGTR1 |
| Name | angiotensin II receptor type 1 |
| Location | 3q24 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | AT1, AT2R1, AGTR1A, AT2R1A, HAT1R, AG2S, AT2R1B, AT1B, ATR1 |
| Ensembl gene | ENSG00000144891 |
| Ensembl biotype | protein_coding |
| OMIM | 106165 |
| Entrez | 185 |
Gene structure
Transcript identifiers
Ensembl transcripts: 28 — 27 protein_coding, 1 protein_coding_CDS_not_defined
ENST00000349243, ENST00000402260, ENST00000404754, ENST00000418473, ENST00000461609, ENST00000474935, ENST00000475166, ENST00000475347, ENST00000497524, ENST00000892854, ENST00000892855, ENST00000892856, ENST00000892857, ENST00000892858, ENST00000892859, ENST00000892860, ENST00000892861, ENST00000892862, ENST00000892863, ENST00000892864, ENST00000892865, ENST00000892866, ENST00000892867, ENST00000892868, ENST00000892869, ENST00000944541, ENST00000944542, ENST00000944543
RefSeq mRNA: 7 — MANE Select: NM_000685
NM_000685, NM_001382736, NM_001382737, NM_004835, NM_009585, NM_031850, NM_032049
CCDS: CCDS3137
Canonical transcript exons
ENST00000349243 — 3 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001249603 | 148707944 | 148708027 |
| ENSE00001249611 | 148697903 | 148698127 |
| ENSE00001837679 | 148740989 | 148743003 |
Expression profiles
Bgee: expression breadth ubiquitous, 224 present calls, max score 96.35.
Top tissues by expression
284 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| skin of hip | UBERON:0001554 | 96.35 | gold quality |
| placenta | UBERON:0001987 | 95.02 | gold quality |
| subcutaneous adipose tissue | UBERON:0002190 | 94.83 | gold quality |
| liver | UBERON:0002107 | 94.31 | gold quality |
| right lobe of liver | UBERON:0001114 | 94.29 | gold quality |
| adipose tissue | UBERON:0001013 | 93.48 | gold quality |
| right adrenal gland | UBERON:0001233 | 92.77 | gold quality |
| left adrenal gland | UBERON:0001234 | 92.64 | gold quality |
| adrenal cortex | UBERON:0001235 | 92.31 | gold quality |
| left adrenal gland cortex | UBERON:0035825 | 92.25 | gold quality |
| right adrenal gland cortex | UBERON:0035827 | 92.21 | gold quality |
| connective tissue | UBERON:0002384 | 92.06 | gold quality |
| adipose tissue of abdominal region | UBERON:0007808 | 91.89 | gold quality |
| adrenal gland | UBERON:0002369 | 91.72 | gold quality |
| omental fat pad | UBERON:0010414 | 91.71 | gold quality |
| peritoneum | UBERON:0002358 | 91.63 | gold quality |
| parietal pleura | UBERON:0002400 | 91.02 | gold quality |
| lower lobe of lung | UBERON:0008949 | 89.40 | gold quality |
| mucosa of stomach | UBERON:0001199 | 88.82 | gold quality |
| diaphragm | UBERON:0001103 | 88.16 | silver quality |
| thoracic mammary gland | UBERON:0005200 | 87.87 | gold quality |
| mammary gland | UBERON:0001911 | 87.60 | gold quality |
| synovial joint | UBERON:0002217 | 87.51 | gold quality |
| right lung | UBERON:0002167 | 87.46 | gold quality |
| adrenal tissue | UBERON:0018303 | 87.37 | gold quality |
| muscle layer of sigmoid colon | UBERON:0035805 | 87.08 | gold quality |
| pleura | UBERON:0000977 | 87.07 | gold quality |
| pericardium | UBERON:0002407 | 86.09 | gold quality |
| upper leg skin | UBERON:0004262 | 85.61 | gold quality |
| tibialis anterior | UBERON:0001385 | 85.49 | gold quality |
Single-cell (SCXA)
Detected in 3 experiment(s), a significant marker in 3.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-HCAD-24 | yes | 1250.28 |
| E-MTAB-6701 | yes | 1027.49 |
| E-ANND-3 | yes | 34.02 |
Regulation
Is transcription factor: yes
Downstream targets (CollecTRI)
1 targets.
| Target | Regulation |
|---|---|
| PAX2 | Activation |
Upstream regulators (CollecTRI, top): AP1, AR, CREB1, CREM, CUX1, ELK1, ETV4, GATA4, HIF1A, KLF4, MEF2A, MYC, NFKB, NR1H3, PPARA, PPARG, SMAD2, SMAD3, SMAD4, SND1, SP1, SP3, VDR
miRNA regulators (miRDB)
84 targeting AGTR1, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-LET-7A-3P | 100.00 | 74.03 | 3932 |
| HSA-LET-7B-3P | 100.00 | 74.08 | 3913 |
| HSA-LET-7F-1-3P | 100.00 | 74.02 | 3928 |
| HSA-MIR-98-3P | 100.00 | 74.08 | 3907 |
| HSA-MIR-3163 | 100.00 | 77.23 | 8605 |
| HSA-MIR-5011-5P | 100.00 | 83.46 | 5820 |
| HSA-MIR-1277-5P | 100.00 | 73.95 | 5056 |
| HSA-MIR-4282 | 99.99 | 75.36 | 6408 |
| HSA-MIR-511-3P | 99.99 | 68.85 | 1467 |
| HSA-MIR-34A-5P | 99.99 | 71.21 | 1784 |
| HSA-MIR-449A | 99.99 | 71.05 | 1776 |
| HSA-MIR-548AW | 99.99 | 72.57 | 3559 |
| HSA-MIR-6888-3P | 99.97 | 65.95 | 1170 |
| HSA-MIR-34C-5P | 99.97 | 70.45 | 1577 |
| HSA-MIR-449B-5P | 99.97 | 70.26 | 1580 |
| HSA-MIR-551B-5P | 99.96 | 71.28 | 3493 |
| HSA-MIR-1468-3P | 99.96 | 72.74 | 3797 |
| HSA-MIR-559 | 99.95 | 72.28 | 3609 |
| HSA-MIR-548AB | 99.95 | 71.31 | 3488 |
| HSA-LET-7C-3P | 99.95 | 73.42 | 2862 |
| HSA-MIR-548A-5P | 99.94 | 71.27 | 3482 |
| HSA-MIR-548AD-5P | 99.94 | 71.23 | 3502 |
| HSA-MIR-548AE-5P | 99.94 | 71.23 | 3502 |
| HSA-MIR-548AK | 99.94 | 71.24 | 3488 |
| HSA-MIR-548AM-5P | 99.94 | 71.24 | 3488 |
| HSA-MIR-548AP-5P | 99.94 | 71.14 | 3489 |
| HSA-MIR-548AQ-5P | 99.94 | 71.34 | 3426 |
| HSA-MIR-548AR-5P | 99.94 | 71.28 | 3515 |
| HSA-MIR-548AS-5P | 99.94 | 71.22 | 3482 |
| HSA-MIR-548AU-5P | 99.94 | 71.24 | 3488 |
Literature-anchored findings (GeneRIF, showing 40)
- Generated a new transgenic rat model that exhibits an upregulated myocardial AT1 receptor density and demonstrates augmented cardiac hypertrophy and contractile response to angiotensin II after volume and pressure overload. (PMID:11692158)
- Stimulation of cardiac apoptosis in essential hypertension: potential role of angiotensin II. (PMID:11799082)
- Lys(199) mutation of the human angiotensin type 1 receptor differentially affects the binding of surmountable and insurmountable non-peptide antagonists. (PMID:11881039)
- role in familial hyperaldosteronism (PMID:11903322)
- Polymorphisms of genes encoding the AT1 receptor as risk factors for orthostatic hypotension. (PMID:11910300)
- angiotensinogen T174M and M235T and the AT1-receptor A1166C polymorphisms were related to the change in LVH during antihypertensive treatment with an AT1-receptor antagonist (PMID:11910301)
- Adenine/cytosine1166 polymorphism is not associated with mitral valve prolapse syndrome in Taiwan Chinese. (PMID:11999641)
- angiotensin IV is a potent agonist for constitutive active human AT1 receptor (PMID:12006574)
- Stimulation of the Ang II type 1 receptor by Ang II reduced adipose conversion, whereas blockade of this receptor markedly enhanced adipogenesis. (PMID:12031955)
- Pivotal role of the renin/prorenin receptor in angiotensin II production and cellular responses to renin (PMID:12045255)
- AT1R gene contributes to the development of essential hypertension. (PMID:12048678)
- AT1 receptor antagonism improves endothelial function during hypercholesterolemia. (PMID:12117739)
- Type I Ang II receptor subtype (AT1) mediates Ang II-dependent [Ca2+]i increase in cancerous breast cells in culture (PMID:12127057)
- explore the relation among myocardial AT(1)-/AT(2)- receptor expression, myocardial remodeling and cardiac function in patients with congestive heart failure (PMID:12133421)
- that the presence of C allele of the AT1R locus polymorphism might be associated with faster deterioration of renal function in renal failure (PMID:12187084)
- A1166C polymorphism of the angiotensin II type 1 receptor gene and essential hypertension in Han, Tibetan and Yi populations. (PMID:12358135)
- AT1R gene contributed to T2DM complicated by hypertension, but is only associated with cases of elevated systolic blood pressure. (PMID:12390711)
- results suggest that the caveolin-binding-like motif of the angiotensin II type 1 receptor may act as a docking site for regulatory proteins modulating the routing and the functionality of the receptor (PMID:12446598)
- The angiotensin II (Ang II) molecule must adopt an extended structure when ligand incorporation occurs on the C-terminal Ang II fragment at residues Phe-293 and Asn-294 of the seventh transmembrane domain of the AT1 receptor. (PMID:12450401)
- in this large cohort of older adults, the A1166C polymorphism was not associated with BP control or incident cardiovascular events (PMID:12460700)
- The results for the AT1R gene polymorphism revealed significant differences in allele and genotype frequencies. (PMID:12476891)
- Analysis of A1166C polymorphism in Serbian hypertensives showed significant association between hypertension and CC genotype in the males only. (PMID:12482634)
- Tyr-319 of the AT1 receptor is phosphorylated in response to Ang II and plays a key role in mediating Ang II-induced transactivation of EGFR and cell proliferation, possibly through its interaction with SHP-2 and EGFR (PMID:12522132)
- angiotensin II AT(1) receptor autoantibodies (anti-AT(1)-AABs) in preeclamptic women (PMID:12534336)
- Association of ACE I/D and AT(1)R-A C polymorphisms with BP in a healthy normotensive primary care population. Although synergistic effect of both polymorphisms on BP does not seem to be present, an additive effect on DBP is likely. (PMID:12544439)
- Importance of alternative splicing as an additional post-transcriptional mechanism regulating human AT(1) receptor number and function. (review) (PMID:12591176)
- Our findings suggest that maternal autoantibody with the ability to activate AT1 receptors may account for two features of preeclampsia, increased PAI-1 production and shallow trophoblast invasion (PMID:12593997)
- Polymorphism in essential arterial hypertension in childhood. (PMID:12597535)
- the A1166C polymorphism of AT1 receptor is unlikely to influence blood pressure status in the Japanese population. (PMID:12627871)
- that AT1 A/C1166 polymorphism was not associated with any clinical parameters associated with hypertension or atherosclerosis in the Japanese population. (PMID:12627873)
- In young healthy subjects, there is an important interaction between gender, the AGT1R A1166–>C gene polymorphism, and blood pressure. (PMID:12631360)
- mRNA levels as well as the protein production of angiotensin II receptors of type 1 was monitored during differentiation of primary human preadipocytes in culture and in mature adipocytes. (PMID:12660887)
- Polymorphism is associated with diabetic retinopathy in NIDDM in Chinese patients. (PMID:12716844)
- Susceptibility to faster progression to ESRD is associated with the AT1R A1166C polymorphism. (PMID:12832734)
- activation of the angiotensin II type 1 receptor alters the spatial proximity of transmembrane 7 to the ligand-binding pocket (PMID:12842881)
- Placental AT1R expression and its normal vascular and endocrine activity plays a very important role in oxygenation and nutrition of the fetus and this ensures proper fetal development and growth. (PMID:12860335)
- results confirmed that angiotensin II receptor type 1 immunoreactivity is elevated in vascular endothelial cells of human placenta from pregnancies complicated by preeclampsia (PMID:12897464)
- Polymorphisms of the angiotensin II receptor, type 1 gene is associated with increased risk of coronary heart disease in hypertension. (PMID:12925562)
- findings suggest that the angiotensinogen and angiotensin II type 1 receptor gene polymorphisms would not have an effect on hypertension or the end stage renal disease in autosomal dominant polycystic kidney disease (PMID:12950120)
- the N111G-AT1 receptor maintains a high affinity conformation despite being uncoupled from the G protein Gq/11. (PMID:12960024)
Cross-species orthologs
6 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | agtr1a | ENSDARG00000018616 |
| danio_rerio | agtr1b | ENSDARG00000045443 |
| mus_musculus | Agtr1a | ENSMUSG00000049115 |
| mus_musculus | Agtr1b | ENSMUSG00000054988 |
| rattus_norvegicus | Agtr1b | ENSRNOG00000010640 |
| rattus_norvegicus | Agtr1a | ENSRNOG00000018346 |
Paralogs (7): BDKRB1 (ENSG00000100739), APLNR (ENSG00000134817), GPR15 (ENSG00000154165), BDKRB2 (ENSG00000168398), GPR25 (ENSG00000170128), RXFP4 (ENSG00000173080), AGTR2 (ENSG00000180772)
Protein
Protein identifiers
Type-1 angiotensin II receptor — P30556 (reviewed: P30556)
Alternative names: AT1AR, AT1BR, Angiotensin II type-1 receptor
All UniProt accessions (4): P30556, A0A0A0MSE3, D3DNG8, Q53YY0
UniProt curated annotations — full annotation on UniProt →
Function. Receptor for angiotensin II, a vasoconstricting peptide, which acts as a key regulator of blood pressure and sodium retention by the kidney. 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. (Microbial infection) During SARS coronavirus-2/SARS-CoV-2 infection, it is able to recognize and internalize the complex formed by secreted ACE2 and SARS-CoV-2 spike protein through DNM2/dynamin 2-dependent endocytosis.
Subunit / interactions. Interacts with MAS1. Interacts with ARRB1. Interacts with FLNA (via filamin repeat 21); increases PKA-mediated phosphorylation of FLNA.
Subcellular location. Cell membrane.
Tissue specificity. Liver, lung, adrenal and adrenocortical adenomas.
Post-translational modifications. C-terminal Ser or Thr residues may be phosphorylated.
Disease relevance. Renal tubular dysgenesis (RTD) [MIM:267430] Autosomal recessive severe disorder of renal tubular development characterized by persistent fetal anuria and perinatal death, probably due to pulmonary hypoplasia from early-onset oligohydramnios (the Potter phenotype). The disease is caused by variants affecting the gene represented in this entry.
Activity regulation. Strongly inhibited by anti-hypertensive drugs losartan, candesartan, valsartan, irbesartan, telmisartan, eprosartan, olmesartan and azilsartan, most of which share a common biphenyl-tetrazole scaffold.
Similarity. Belongs to the G-protein coupled receptor 1 family.
RefSeq proteins (7): NP_000676, NP_001369665, NP_001369666, NP_004826, NP_033611, NP_114038, NP_114438 (=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000190 | ATII_AT1_rcpt | Family |
| IPR000248 | ATII_rcpt | Family |
| IPR000276 | GPCR_Rhodpsn | Family |
| IPR017452 | GPCR_Rhodpsn_7TM | Domain |
| IPR050119 | CCR1-9-like | Family |
Pfam: PF00001
UniProt features (81 total): mutagenesis site 14, helix 13, topological domain 8, transmembrane region 7, binding site 7, sequence variant 7, sequence conflict 6, strand 5, turn 5, glycosylation site 3, disulfide bond 2, chain 1, region of interest 1, compositionally biased region 1, lipid moiety-binding region 1
Structure
Experimental structures (PDB)
11 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 6OS2 | X-RAY DIFFRACTION | 2.7 |
| 6OS1 | X-RAY DIFFRACTION | 2.79 |
| 4ZUD | X-RAY DIFFRACTION | 2.8 |
| 4YAY | X-RAY DIFFRACTION | 2.9 |
| 6OS0 | X-RAY DIFFRACTION | 2.9 |
| 6DO1 | X-RAY DIFFRACTION | 2.9 |
| 8TH3 | ELECTRON MICROSCOPY | 3 |
| 9EAH | ELECTRON MICROSCOPY | 3.1 |
| 9EAI | ELECTRON MICROSCOPY | 3.1 |
| 9EAJ | ELECTRON MICROSCOPY | 3.2 |
| 8TH4 | ELECTRON MICROSCOPY | 3.3 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P30556-F1 | 82.55 | 0.58 |
Antibody-complex structures (SAbDab): 5 — 6DO1, 6OS0, 6OS1, 6OS2, 8TH4
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Ligand- & substrate-binding residues (7): 15; 17; 167; 182; 183; 184; 199
Post-translational modifications (1): 355
Disulfide bonds (2): 18–274, 101–180
Glycosylation sites (3): 4, 176, 188
Mutagenesis-validated functional residues (14):
| Position | Phenotype |
|---|---|
| 35 | abolished binding to angiotensin ii; abolished binding to olmesartan inhibitor. |
| 84 | abolished binding to angiotensin ii; abolished binding to olmesartan inhibitor. |
| 92 | decreased binding to telmisartan inhibitor. |
| 111 | reduced affinity for angiotensin ii. |
| 111 | induces a conformational change in the angiotensin ii-binding pocket, leading to constitutive activation of the receptor |
| 112 | increased affinity for angiotensin ii. |
| 135 | abolished binding to angiotensin ii. |
| 167 | abolished binding to angiotensin ii; abolished binding to olmesartan inhibitor. |
| 182 | reduced binding to angiotensin ii without affecting binding to candesartan inhibitor. |
| 199 | abolished binding to angiotensin ii. |
| 284 | slightly affects binding to eprosartan inhibitor. |
| 285 | decreased binding to eprosartan inhibitor. |
| 288 | decreased binding to eprosartan inhibitor. |
| 292 | mimics the disordered side chain induced by angiotensin ii-binding; increased affinity for g-protein subunit alpha prote |
Function
Pathways and Gene Ontology
Reactome pathways
11 pathways
| ID | Pathway |
|---|---|
| R-HSA-375276 | Peptide ligand-binding receptors |
| R-HSA-416476 | G alpha (q) signalling events |
| R-HSA-8856825 | Cargo recognition for clathrin-mediated endocytosis |
| R-HSA-8856828 | Clathrin-mediated endocytosis |
| R-HSA-162582 | Signal Transduction |
| R-HSA-199991 | Membrane Trafficking |
| R-HSA-372790 | Signaling by GPCR |
| R-HSA-373076 | Class A/1 (Rhodopsin-like receptors) |
| R-HSA-388396 | GPCR downstream signalling |
| R-HSA-500792 | GPCR ligand binding |
| R-HSA-5653656 | Vesicle-mediated transport |
MSigDB gene sets: 338 (showing top):
GSE45365_CD8A_DC_VS_CD11B_DC_IFNAR_KO_MCMV_INFECTION_DN, GSE45365_CTRL_VS_MCMV_INFECTION_NK_CELL_UP, GOBP_EXCRETION, MODULE_416, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, chr3q24, GOBP_REGULATION_OF_BLOOD_PRESSURE, GOBP_CIRCULATORY_SYSTEM_PROCESS, GOBP_CELL_CHEMOTAXIS, GOBP_INFLAMMATORY_RESPONSE, MODULE_64, KAAB_HEART_ATRIUM_VS_VENTRICLE_UP, GOBP_RESPONSE_TO_ANGIOTENSIN, GOBP_GROWTH, GOBP_REGULATION_OF_SYSTEMIC_ARTERIAL_BLOOD_PRESSURE
GO Biological Process (27): regulation of cell growth (GO:0001558), kidney development (GO:0001822), renin-angiotensin regulation of aldosterone production (GO:0002018), maintenance of blood vessel diameter homeostasis by renin-angiotensin (GO:0002034), regulation of systemic arterial blood pressure by renin-angiotensin (GO:0003081), inflammatory response (GO:0006954), G protein-coupled receptor signaling pathway (GO:0007186), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), positive regulation of cytosolic calcium ion concentration (GO:0007204), Rho protein signal transduction (GO:0007266), positive regulation of macrophage derived foam cell differentiation (GO:0010744), regulation of vasoconstriction (GO:0019229), calcium-mediated signaling (GO:0019722), low-density lipoprotein particle remodeling (GO:0034374), regulation of renal sodium excretion (GO:0035813), angiotensin-activated signaling pathway (GO:0038166), regulation of cell population proliferation (GO:0042127), symbiont entry into host cell (GO:0046718), regulation of inflammatory response (GO:0050727), positive regulation of inflammatory response (GO:0050729), cell chemotaxis (GO:0060326), phospholipase C-activating angiotensin-activated signaling pathway (GO:0086097), positive regulation of cholesterol metabolic process (GO:0090205), blood vessel diameter maintenance (GO:0097746), positive regulation of blood vessel endothelial cell proliferation involved in sprouting angiogenesis (GO:1903589), positive regulation of reactive oxygen species metabolic process (GO:2000379), signal transduction (GO:0007165)
GO Molecular Function (6): angiotensin type I receptor activity (GO:0001596), angiotensin type II receptor activity (GO:0004945), bradykinin receptor binding (GO:0031711), protein heterodimerization activity (GO:0046982), G protein-coupled receptor activity (GO:0004930), protein binding (GO:0005515)
GO Cellular Component (2): plasma membrane (GO:0005886), membrane (GO:0016020)
Reactome top-level categories
Rollup of top-8 pathways:
| Category | Pathways |
|---|---|
| Signaling by GPCR | 2 |
| Class A/1 (Rhodopsin-like receptors) | 1 |
| GPCR downstream signalling | 1 |
| Clathrin-mediated endocytosis | 1 |
| Membrane Trafficking | 1 |
| Vesicle-mediated transport | 1 |
| Signal Transduction | 1 |
| GPCR ligand binding | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| G protein-coupled receptor signaling pathway | 3 |
| blood vessel diameter maintenance | 2 |
| inflammatory response | 2 |
| angiotensin receptor activity | 2 |
| cell growth | 1 |
| regulation of growth | 1 |
| regulation of cellular component organization | 1 |
| animal organ development | 1 |
| renal system development | 1 |
| regulation of blood volume by renin-angiotensin | 1 |
| renal system process involved in regulation of systemic arterial blood pressure | 1 |
| aldosterone secretion | 1 |
| regulation of aldosterone secretion | 1 |
| regulation of systemic arterial blood pressure by renin-angiotensin | 1 |
| regulation of systemic arterial blood pressure by hormone | 1 |
| defense response | 1 |
| G protein-coupled receptor activity | 1 |
| signal transduction | 1 |
| phospholipase C activator activity | 1 |
| regulation of biological quality | 1 |
| small GTPase-mediated signal transduction | 1 |
| macrophage derived foam cell differentiation | 1 |
| regulation of macrophage derived foam cell differentiation | 1 |
| positive regulation of cell differentiation | 1 |
| vasoconstriction | 1 |
| regulation of blood circulation | 1 |
| intracellular signaling cassette | 1 |
| plasma lipoprotein particle remodeling | 1 |
| renal sodium excretion | 1 |
| regulation of excretion | 1 |
| regulation of renal system process | 1 |
| cellular response to angiotensin | 1 |
| cell population proliferation | 1 |
| regulation of cellular process | 1 |
| viral life cycle | 1 |
| symbiont entry into host | 1 |
| regulation of defense response | 1 |
| regulation of response to external stimulus | 1 |
| positive regulation of defense response | 1 |
| positive regulation of response to external stimulus | 1 |
Protein interactions and networks
STRING
2434 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| AGTR1 | AGT | P01019 | 999 |
| AGTR1 | ACE2 | Q9BYF1 | 996 |
| AGTR1 | ACE | P12821 | 975 |
| AGTR1 | AGTRAP | Q6RW13 | 974 |
| AGTR1 | GNAQ | P50148 | 971 |
| AGTR1 | REN | P00797 | 969 |
| AGTR1 | BDKRB2 | P30411 | 945 |
| AGTR1 | KNG1 | P01042 | 938 |
| AGTR1 | ARRB2 | P32121 | 872 |
| AGTR1 | CYP11B2 | P19099 | 871 |
| AGTR1 | AGTR2 | P50052 | 835 |
| AGTR1 | ADRB2 | P07550 | 791 |
| AGTR1 | MAS1L | P35410 | 790 |
| AGTR1 | ARRB1 | P49407 | 790 |
| AGTR1 | EDN1 | P05305 | 785 |
IntAct
91 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| AGTR1 | APLNR | psi-mi:“MI:0915”(physical association) | 0.710 |
| AGTR1 | APLNR | psi-mi:“MI:2364”(proximity) | 0.710 |
| APLNR | AGTR1 | psi-mi:“MI:0915”(physical association) | 0.710 |
| AGTR1 | ATP1B1 | psi-mi:“MI:0915”(physical association) | 0.510 |
| AGTR1 | CERS6 | psi-mi:“MI:0915”(physical association) | 0.510 |
| AGTR1 | DNAJC8 | psi-mi:“MI:0915”(physical association) | 0.510 |
| AGTR1 | OAZ1 | psi-mi:“MI:0915”(physical association) | 0.510 |
| ATP1B1 | AGTR1 | psi-mi:“MI:0915”(physical association) | 0.510 |
| DNAJC8 | AGTR1 | psi-mi:“MI:0915”(physical association) | 0.510 |
| CERS6 | AGTR1 | psi-mi:“MI:0915”(physical association) | 0.510 |
| OAZ1 | AGTR1 | psi-mi:“MI:0915”(physical association) | 0.510 |
| AGTR1 | VAC14 | psi-mi:“MI:0915”(physical association) | 0.400 |
| AGTR1 | AGT | psi-mi:“MI:0915”(physical association) | 0.400 |
| RAMP2 | AGTR1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| AGTR1 | RAMP3 | psi-mi:“MI:0915”(physical association) | 0.400 |
| RAMP3 | AGTR1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| AGTR1 | RAMP2 | psi-mi:“MI:0915”(physical association) | 0.400 |
BioGRID (126): PDE6H (Two-hybrid), VKORC1L1 (Affinity Capture-MS), ATP12A (Affinity Capture-MS), ATP2B4 (Affinity Capture-MS), ATP2B3 (Affinity Capture-MS), PIGU (Affinity Capture-MS), CLCC1 (Affinity Capture-MS), THOC7 (Affinity Capture-MS), SETD7 (Affinity Capture-MS), SLC6A8 (Affinity Capture-MS), ALG10 (Affinity Capture-MS), CAV1 (Affinity Capture-MS), SLC19A2 (Affinity Capture-MS), C1orf112 (Affinity Capture-MS), TMEM11 (Affinity Capture-MS)
ESM2 similar proteins: O00574, O18793, O18983, O19024, O35210, O55193, O77590, O97881, O97882, P25095, P25104, P29089, P29754, P29755, P30555, P30556, P32303, P33396, P34976, P35351, P35373, P35374, P43240, P50052, P51678, P51681, P51683, P56440, P56493, P60574, P61756, P79785, Q28929, Q2HJ17, Q5ECR9, Q64H34, Q6WN98, Q8HZT9, Q95NC2, Q95NC3
Diamond homologs: A0T2N3, F1MV99, O00155, O00590, O08707, O08858, O09027, O35210, O77590, O88410, O89039, O97666, P0C5I1, P0C7U4, P11613, P21109, P25024, P25025, P25095, P25104, P25106, P29089, P29754, P29755, P30555, P30556, P30680, P30874, P30875, P30935, P30936, P30937, P30938, P31391, P32303, P32745, P33396, P33535, P34976, P34993
SIGNOR signaling
25 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| AGTR1 | up-regulates | GNAQ | binding |
| AGT | up-regulates | AGTR1 | binding |
| AGTR1 | up-regulates | GNA13 | binding |
| AGTR1 | up-regulates | GNG12 | binding |
| AGTR1 | “up-regulates activity” | GNAI1 | binding |
| AGTR1 | “up-regulates activity” | GNAI3 | binding |
| AGTR1 | “up-regulates activity” | GNAQ | binding |
| AGTR1 | “up-regulates activity” | GNA14 | binding |
| AGTR1 | “up-regulates activity” | GNA15 | binding |
| “Ile(5)-angiotensin II” | “up-regulates activity” | AGTR1 | “chemical activation” |
| eprosartan | “down-regulates activity” | AGTR1 | “chemical inhibition” |
| valsartan | “down-regulates activity” | AGTR1 | “chemical inhibition” |
| telmisartan | “down-regulates activity” | AGTR1 | “chemical inhibition” |
| AGTR1 | up-regulates | Inflammation | |
| AGTR1 | up-regulates | Fibrosis | |
| Angiotensin-2 | “up-regulates activity” | AGTR1 | binding |
| MAS1 | “down-regulates activity” | AGTR1 | binding |
| hsa-miR-155-5p | “down-regulates quantity by repression” | AGTR1 | “post transcriptional regulation” |
| hsa-miR-410-3p | “down-regulates quantity by repression” | AGTR1 | “post transcriptional regulation” |
| AGTR1 | “up-regulates activity” | GNA11 | binding |
| AGTR1 | up-regulates | Membrane_blebbing | |
| hsa-miR-410-3p | “down-regulates quantity by destabilization” | AGTR1 | “post transcriptional regulation” |
| AGTR1 | “up-regulates quantity by expression” | PAX2 | “transcriptional regulation” |
| AGT | “up-regulates activity” | AGTR1 | binding |
| AGTR1 | “down-regulates activity” | NPHS1 |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 69 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| protein transport | 9 | 6.2× | 8e-03 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
184 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 5 |
| Likely pathogenic | 9 |
| Uncertain significance | 113 |
| Likely benign | 29 |
| Benign | 18 |
Top pathogenic / likely-pathogenic (14)
| Variant ID | HGVS | Classification |
|---|---|---|
| 1685512 | NM_000685.5(AGTR1):c.233del (p.Leu78fs) | Pathogenic |
| 18067 | NM_000685.5(AGTR1):c.845C>T (p.Thr282Met) | Pathogenic |
| 3246874 | NC_000003.11:g.(?148447967)(149678891_?)del | Pathogenic |
| 4700197 | NM_000685.5(AGTR1):c.-47-10764C>T | Pathogenic |
| 50206 | NM_000685.5(AGTR1):c.251G>A (p.Trp84Ter) | Pathogenic |
| 1179033 | NM_000685.5(AGTR1):c.599dup (p.Asn200fs) | Likely pathogenic |
| 1184963 | NM_000685.5(AGTR1):c.696_700del (p.Pro233fs) | Likely pathogenic |
| 1328400 | NM_000685.5(AGTR1):c.879del (p.Phe293fs) | Likely pathogenic |
| 18066 | NM_000685.5(AGTR1):c.110dup (p.Ile38fs) | Likely pathogenic |
| 3588650 | NM_000685.5(AGTR1):c.166del (p.Tyr56fs) | Likely pathogenic |
| 3588655 | NM_000685.5(AGTR1):c.337dup (p.Tyr113fs) | Likely pathogenic |
| 3588656 | NM_000685.5(AGTR1):c.340del (p.Ala114fs) | Likely pathogenic |
| 50207 | NM_000685.5(AGTR1):c.376C>T (p.Arg126Ter) | Likely pathogenic |
| 814486 | GRCh37/hg19 3q24-25.1(chr3:144053029-150272658)x1 | Likely pathogenic |
SpliceAI
798 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 3:148740984:CCCA:C | acceptor_loss | 1.0000 |
| 3:148740985:CCA:C | acceptor_loss | 1.0000 |
| 3:148740986:CA:C | acceptor_loss | 1.0000 |
| 3:148740988:G:GT | acceptor_loss | 1.0000 |
| 3:148740988:GGT:G | acceptor_gain | 1.0000 |
| 3:148709244:G:GG | donor_gain | 0.9900 |
| 3:148724681:GTCC:G | donor_gain | 0.9900 |
| 3:148740987:A:AG | acceptor_gain | 0.9900 |
| 3:148740988:G:GG | acceptor_gain | 0.9900 |
| 3:148740988:GGTGT:G | acceptor_gain | 0.9900 |
| 3:148698125:CGGG:C | donor_loss | 0.9800 |
| 3:148698126:GGGT:G | donor_loss | 0.9800 |
| 3:148698129:TGAG:T | donor_loss | 0.9800 |
| 3:148709240:GACA:G | donor_gain | 0.9800 |
| 3:148698124:GCGG:G | donor_gain | 0.9700 |
| 3:148698126:GG:G | donor_gain | 0.9700 |
| 3:148698127:GG:G | donor_gain | 0.9700 |
| 3:148698130:G:GC | donor_loss | 0.9700 |
| 3:148709396:G:T | donor_gain | 0.9700 |
| 3:148731319:C:A | donor_gain | 0.9700 |
| 3:148739856:AG:A | donor_gain | 0.9700 |
| 3:148740022:G:T | donor_gain | 0.9700 |
| 3:148698128:G:GG | donor_gain | 0.9600 |
| 3:148698131:A:AC | donor_loss | 0.9600 |
| 3:148698132:G:C | donor_loss | 0.9600 |
| 3:148724685:G:GG | donor_gain | 0.9600 |
| 3:148740978:A:AG | acceptor_gain | 0.9600 |
| 3:148709396:G:GT | donor_gain | 0.9500 |
| 3:148738860:GGCT:G | donor_gain | 0.9500 |
| 3:148738861:GCTG:G | donor_gain | 0.9500 |
AlphaMissense
0 scored. Top likely-pathogenic:
dbSNP variants (sampled 300 via entrez): RS1000007579 (3:148708365 C>A), RS1000031525 (3:148722290 A>G), RS1000167694 (3:148702682 G>A,T), RS1000222985 (3:148696146 G>A,T), RS1000376053 (3:148729237 G>C), RS1000426050 (3:148735011 C>G,T), RS1000541694 (3:148729502 G>T), RS1000624822 (3:148703030 G>T), RS1000677989 (3:148709358 A>G), RS1000731274 (3:148709624 T>A), RS1000765650 (3:148736635 GA>G,GAA), RS1000982836 (3:148730726 C>T), RS1000997254 (3:148729849 C>T), RS1001083675 (3:148724218 G>A), RS1001183821 (3:148708009 C>T)
Disease associations
OMIM: gene MIM:106165 | disease phenotypes: MIM:145500, MIM:267430, MIM:601331, MIM:613801, MIM:604290
GenCC curated gene-disease
| Disease | Classification | Inheritance |
|---|---|---|
| renal tubular dysgenesis of genetic origin | Strong | Autosomal recessive |
| essential hypertension, genetic | No Known Disease Relationship | Unknown |
Mondo (7): essential hypertension (MONDO:0001134), renal tubular dysgenesis (MONDO:0017609), essential hypertension, genetic (MONDO:0007781), renal tubular dysgenesis of genetic origin (MONDO:0009970), renal dysplasia, cystic, susceptibility to (MONDO:0011037), retinitis pigmentosa 40 (MONDO:0013429), aceruloplasminemia (MONDO:0011426)
Orphanet (5): Renal tubular dysgenesis (Orphanet:3033), Renal tubular dysgenesis of genetic origin (Orphanet:97369), Retinitis pigmentosa (Orphanet:791), Aceruloplasminemia (Orphanet:48818), NON RARE IN EUROPE: Essential hypertension (Orphanet:243761)
HPO phenotypes
15 total (15 of 15 shown, HPO-id order):
| HPO | Term |
|---|---|
| HP:0000007 | Autosomal recessive inheritance |
| HP:0000079 | Abnormality of the urinary system |
| HP:0000252 | Microcephaly |
| HP:0001426 | Non-Mendelian inheritance |
| HP:0001562 | Oligohydramnios |
| HP:0002009 | Potter facies |
| HP:0002089 | Pulmonary hypoplasia |
| HP:0002093 | Respiratory insufficiency |
| HP:0002615 | Hypotension |
| HP:0004421 | Elevated systolic blood pressure |
| HP:0004492 | Widely patent fontanelles and sutures |
| HP:0004972 | Elevated mean arterial pressure |
| HP:0005117 | Elevated diastolic blood pressure |
| HP:0008660 | Renotubular dysgenesis |
| HP:0100519 | Anuria |
GWAS associations
6 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST002831_6 | Lead levels in blood | 2.000000e-06 |
| GCST003989_43 | Chin dimples | 4.000000e-09 |
| GCST003996_20 | Monobrow | 2.000000e-09 |
| GCST008114_14 | Type 2 diabetes | 8.000000e-07 |
| GCST008362_211 | Birth weight | 2.000000e-13 |
| GCST008839_425 | Height | 1.000000e-07 |
EFO canonical traits (2, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0007906 | synophrys measurement |
| EFO:0004344 | birth weight |
MeSH disease descriptors (2)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D000075222 | Essential Hypertension | C14.907.489.165 |
| C537755 | Renal dysplasia diffuse cystic (supp.) |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL2094256 (PROTEIN FAMILY), CHEMBL227 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
88 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 554,388 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL1513 | IRBESARTAN | 4 | 31,667 |
| CHEMBL191 | LOSARTAN | 4 | 88,932 |
| CHEMBL938 | SARALASIN | 4 | 7,408 |
| CHEMBL995 | LOSARTAN POTASSIUM | 4 | 11,860 |
| CHEMBL1014 | CANDESARTAN CILEXETIL | 4 | 11,194 |
| CHEMBL1017 | TELMISARTAN | 4 | 27,457 |
| CHEMBL104 | CLOTRIMAZOLE | 4 | 56,325 |
| CHEMBL1064 | SIMVASTATIN | 4 | 123,163 |
| CHEMBL1069 | VALSARTAN | 4 | 38,585 |
| CHEMBL111 | RIMONABANT | 4 | 15,726 |
| CHEMBL1112 | ARIPIPRAZOLE | 4 | 24,205 |
| CHEMBL1171837 | PONATINIB | 4 | 8,955 |
| CHEMBL1200585 | OXYMETHOLONE | 4 | 5,113 |
| CHEMBL1200692 | OLMESARTAN MEDOXOMIL | 4 | 17,268 |
| CHEMBL1200934 | NORGESTIMATE | 4 | 7,839 |
| CHEMBL1201244 | ROCURONIUM | 4 | 2,682 |
| CHEMBL1201303 | PYRVINIUM | 4 | 1,797 |
| CHEMBL1201304 | INDOCYANINE GREEN ACID FORM | 4 | 7,044 |
| CHEMBL1201346 | BALSALAZIDE | 4 | 8,319 |
| CHEMBL121 | ROSIGLITAZONE | 4 | 58,849 |
| CHEMBL1221 | SULCONAZOLE | 4 | |
| CHEMBL125 | MILTEFOSINE | 4 | |
| CHEMBL1295 | BUTOCONAZOLE | 4 | |
| CHEMBL1336 | SORAFENIB | 4 | |
| CHEMBL1401 | NITAZOXANIDE | 4 | |
| CHEMBL1423 | PIMOZIDE | 4 | |
| CHEMBL1480 | FELODIPINE | 4 | |
| CHEMBL1533 | DESOGESTREL | 4 | |
| CHEMBL1601669 | ALFACALCIDOL | 4 | |
| CHEMBL163 | RITONAVIR | 4 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
PharmGKB clinical annotations
15 annotations.
| Variant | Type | Level | Drugs | Phenotypes |
|---|---|---|---|---|
| rs12721226 | Efficacy | 3 | losartan | |
| rs275651 | Efficacy | 3 | perindopril | Coronary Artery Disease |
| rs5182 | Toxicity | 3 | Ace Inhibitors;Plain | Hypertension |
| rs5182 | Efficacy | 3 | perindopril | Coronary Artery Disease |
| rs5186 | Efficacy,Toxicity | 3 | Ace Inhibitors;Plain | Coronary Artery Disease |
| rs5186 | Metabolism/PK | 3 | atorvastatin | |
| rs5186 | Efficacy | 3 | irbesartan | Hypertension;Hypertrophy;Left Ventricular |
| rs5186 | Efficacy | 3 | candesartan | Heart Failure |
| rs5186 | Efficacy | 3 | captopril | Diabetes Mellitus;Type 2 |
| rs5186 | Efficacy | 3 | nitrendipine | Hypertension |
| rs5186 | Efficacy | 3 | losartan | |
| rs5186 | Efficacy | 3 | angiotensin II | |
| rs5186 | Efficacy | 3 | perindopril | Hypertension |
| rs5186 | Efficacy | 3 | losartan | Liver Cirrhosis |
| rs5186 | Toxicity | 3 | Thiazides;plain |
PharmGKB variants
5 variants.
| Variant | Genes | Level | Score | #Clin annots | Drugs |
|---|---|---|---|---|---|
| rs5182 | AGTR1 | 3 | 3.00 | 2 | perindopril;Ace Inhibitors;Plain |
| rs5186 | AGTR1 | 3 | 3.75 | 11 | Ace Inhibitors;Plain;captopril;candesartan;atorvastatin;irbesartan;losartan;perindopril;nitrendipine;Thiazides |
| rs275651 | AGTR1 | 3 | 5.50 | 1 | perindopril |
| rs2640543 | AGTR1 | 0.00 | 0 | ||
| rs12721226 | AGTR1 | 3 | 0.00 | 1 | losartan |
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: gpcr — Angiotensin receptors
Most potent curated ligand interactions (45 total), top 25:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| [3H]candesartan | Antagonist | 10.29 | pKd |
| candesartan | Antagonist | 9.72 | pIC50 |
| EXP3174 | Antagonist | 9.49 | pIC50 |
| [125I][Sar1]Ang-II | Full agonist | 9.48 | pKd |
| [Sar1,Ile8]Ang-II | Antagonist | 9.43 | pKd |
| [125I][Sar1,Ile8]Ang-II | Partial agonist | 9.43 | pKd |
| [Sar1,Cha8]Ang-II | Partial agonist | 9.33 | pKd |
| angiotensin II | Full agonist | 9.3 | pIC50 |
| [3H]A81988 | Antagonist | 9.24 | pKd |
| [3H]L158809 | Antagonist | 9.18 | pKd |
| [3H]eprosartan | Antagonist | 9.1 | pKd |
| saprisartan | Antagonist | 9.1 | pKi |
| [Sar1,Ala8]Ang-II | Antagonist | 9.05 | pKd |
| [3H]valsartan | Antagonist | 9.0 | pIC50 |
| tasosartan | Antagonist | 8.92 | pIC50 |
| [125I]EXP985 | Antagonist | 8.83 | pKd |
| eprosartan | Antagonist | 8.8 | pIC50 |
| irbesartan | Antagonist | 8.8 | pIC50 |
| 5-oxo-1-2-4-oxadiazol biphenyl | Antagonist | 8.8 | pIC50 |
| [3H]irbesartan | Antagonist | 8.71 | pKd |
| losartan | Antagonist | 8.7 | pIC50 |
| valsartan | Antagonist | 8.61 | pIC50 |
| forasartan | Antagonist | 8.6 | pIC50 |
| angiotensin III | Full agonist | 8.5 | pIC50 |
| sparsentan | Antagonist | 8.44 | pKi |
Binding affinities (BindingDB)
283 measured of 402 human assays (418 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| US8501750, 56 | IC50 | 0.34 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 83 | IC50 | 0.77 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 60 | IC50 | 1 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 76 | IC50 | 1 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 105 | IC50 | 1 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 63 | IC50 | 1.1 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 107 | IC50 | 1.1 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 59 | IC50 | 1.2 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 99 | IC50 | 1.2 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 131 | IC50 | 1.2 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 181 | IC50 | 1.2 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 186 | IC50 | 1.2 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 153 | IC50 | 1.3 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 215 | IC50 | 1.3 nM | US-8501750: Heterocyclic compound and use thereof |
| 3-[2-[4-[[6-ethyl-3-[2-(2-methoxyphenyl)-2-oxoethyl]-2,4-dioxothieno[2,3-d]pyrimidin-1-yl]methyl]phenyl]phenyl]-1,2,4-oxadiazol-5-olate | IC50 | 1.4 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 127 | IC50 | 1.4 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 143 | IC50 | 1.4 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 157 | IC50 | 1.4 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 197 | IC50 | 1.4 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 209 | IC50 | 1.4 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 221 | IC50 | 1.4 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 73 | IC50 | 1.5 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 135 | IC50 | 1.5 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 136 | IC50 | 1.5 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 142 | IC50 | 1.5 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 148 | IC50 | 1.5 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 150 | IC50 | 1.5 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 152 | IC50 | 1.5 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 198 | IC50 | 1.5 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 205 | IC50 | 1.5 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 58 | IC50 | 1.6 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 129 | IC50 | 1.6 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 130 | IC50 | 1.6 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 180 | IC50 | 1.6 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 210 | IC50 | 1.6 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 225 | IC50 | 1.6 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 121 | IC50 | 1.7 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 132 | IC50 | 1.7 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 140 | IC50 | 1.7 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 144 | IC50 | 1.7 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 145 | IC50 | 1.7 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 158 | IC50 | 1.7 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 194 | IC50 | 1.7 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 116 | IC50 | 1.8 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 117 | IC50 | 1.8 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 149 | IC50 | 1.8 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 203 | IC50 | 1.8 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 214 | IC50 | 1.8 nM | US-8501750: Heterocyclic compound and use thereof |
| 2-[4-[(6-ethyl-2,4-dioxothieno[2,3-d]pyrimidin-1-yl)methyl]-3-methoxyphenyl]benzonitrile | IC50 | 1.9 nM | US-8501750: Heterocyclic compound and use thereof |
| US8501750, 222 | IC50 | 1.9 nM | US-8501750: Heterocyclic compound and use thereof |
ChEMBL bioactivities
1724 potent at pChembl≥5 of 1954 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 10.90 | Kd | 0.01259 | nM | CHEMBL47177 |
| 10.90 | Kd | 0.01259 | nM | CL-329167 |
| 10.70 | Kd | 0.01995 | nM | CHEMBL416477 |
| 10.33 | Kd | 0.04677 | nM | CHEMBL125218 |
| 10.30 | IC50 | 0.05 | nM | CHEMBL346728 |
| 10.30 | Kd | 0.05012 | nM | CHEMBL293511 |
| 10.30 | Kd | 0.05012 | nM | CHEMBL418226 |
| 10.25 | Kd | 0.05623 | nM | CHEMBL92542 |
| 10.18 | IC50 | 0.066 | nM | SARALASIN |
| 10.10 | Kd | 0.07943 | nM | CHEMBL416477 |
| 10.10 | IC50 | 0.08 | nM | CHEMBL295854 |
| 10.09 | Kd | 0.08128 | nM | CARBOXYLIC ACID METABOLITE |
| 10.04 | Kd | 0.0912 | nM | PRATOSARTAN |
| 10.01 | Kd | 0.09772 | nM | PRATOSARTAN |
| 10.00 | IC50 | 0.1 | nM | CHEMBL2435828 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL24322 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL307318 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL70935 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL305238 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL305017 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL70789 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL70843 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL69721 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL70370 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL70161 |
| 10.00 | IC50 | 0.1 | nM | L-158809 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL42775 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL298417 |
| 9.85 | IC50 | 0.14 | nM | CHEMBL435811 |
| 9.80 | Kd | 0.1585 | nM | CHEMBL313371 |
| 9.80 | Ki | 0.16 | nM | ANGIOTENSIN II |
| 9.80 | Kd | 0.1585 | nM | CHEMBL44295 |
| 9.80 | Kd | 0.1585 | nM | CHEMBL289391 |
| 9.77 | Ki | 0.17 | nM | SARALASIN |
| 9.77 | IC50 | 0.17 | nM | ENOLTASOSARTAN |
| 9.71 | Kd | 0.195 | nM | CARBOXYLIC ACID METABOLITE |
| 9.70 | IC50 | 0.2 | nM | CHEMBL338027 |
| 9.70 | Kd | 0.1995 | nM | CHEMBL88411 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL293511 |
| 9.70 | Kd | 0.1995 | nM | CHEMBL387040 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL2369937 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL311625 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL70868 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL303427 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL430792 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL302964 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL308323 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL311253 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL73283 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL71639 |
PubChem BioAssay actives
922 with measured affinity, of 3197 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| 6-[(2S,3aR)-2-methyl-3a,4,5,6-tetrahydro-3H-pyrrolo[1,2-b][1,2]oxazol-2-yl]-2-butyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]quinazolin-4-one | 167381: Inhibition of angiotensin II-induced contractions in rabbit aorta in vitro. | kd | <0.0001 | uM |
| 2-[propyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]pyridine-3-carboxylic acid | 167381: Inhibition of angiotensin II-induced contractions in rabbit aorta in vitro. | kd | <0.0001 | uM |
| 2-[butyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]pyridine-3-carboxylic acid | 37542: Potency to antagonize the ability of angiotensin II to contract rabbit aorta | kd | <0.0001 | uM |
| 2-butyl-6-(2-methoxypropan-2-yl)-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]quinazolin-4-one | 568789: Antagonist activity at angiotensin AT1 receptor | kd | <0.0001 | uM |
| N,N-dimethyl-2-[4-oxo-2-propyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazo[4,5-c]pyridin-5-yl]acetamide | 39047: Inhibition of Angiotensin II induced contractions in rabbit aortic rings | ic50 | 0.0001 | uM |
| N-tert-butyl-2-[2-butyl-4-oxo-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazo[4,5-c]pyridin-5-yl]acetamide | 39047: Inhibition of Angiotensin II induced contractions in rabbit aortic rings | ic50 | 0.0001 | uM |
| tert-butyl N-[2-[4-[[3-butyl-1-[2-chloro-5-(3-methoxypropanoylamino)phenyl]-5-oxo-1,2,4-triazol-4-yl]methyl]-3-fluorophenyl]phenyl]sulfonylcarbamate | 39659: In vitro inhibitory activity against angiotensin II receptor type 1, in human adrenal membrane preparations. | ic50 | 0.0001 | uM |
| 2-butyl-5-chloro-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylic acid | 167381: Inhibition of angiotensin II-induced contractions in rabbit aorta in vitro. | kd | 0.0001 | uM |
| N-[2-[4-[(2-ethyl-5,7-dimethylimidazo[4,5-b]pyridin-3-yl)methyl]phenyl]phenyl]sulfonylbenzamide | 167381: Inhibition of angiotensin II-induced contractions in rabbit aorta in vitro. | kd | 0.0001 | uM |
| 3-[butyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]pyridazine-4-carboxylic acid | 37542: Potency to antagonize the ability of angiotensin II to contract rabbit aorta | kd | 0.0001 | uM |
| 2-ethyl-5,7-dimethyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazo[4,5-b]pyridine | 39047: Inhibition of Angiotensin II induced contractions in rabbit aortic rings | ic50 | 0.0001 | uM |
| 2-[2-butyl-4-oxo-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazo[4,5-c]pyridin-5-yl]-N,N-diethylacetamide | 39047: Inhibition of Angiotensin II induced contractions in rabbit aortic rings | ic50 | 0.0001 | uM |
| (2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-(methylamino)acetyl]amino]pentanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]propanoic acid | 31303: Inhibitory activity as antagonist of AII on guinea pig ileum | ic50 | 0.0001 | uM |
| 2-[4-[[4-methyl-6-(3-phenylpropanoylamino)-2-propylbenzimidazol-1-yl]methyl]phenyl]benzoic acid | 774875: Displacement of [125I]-Sar1Ile8-angiotensin 2 from angiotensin 2 AT1 receptor (unknown origin) after 180 mins by gamma counting analysis | ic50 | 0.0001 | uM |
| 2-propyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-5,6,7,8-tetrahydrocyclohepta[d]imidazol-4-one | 167381: Inhibition of angiotensin II-induced contractions in rabbit aorta in vitro. | kd | 0.0001 | uM |
| 3-[2-butyl-4-oxo-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]quinazolin-6-yl]-1-methyl-1-propan-2-ylurea | 254757: Inhibitory concentration against angiotensin II receptor, type 1 | ic50 | 0.0001 | uM |
| 2-ethyl-4-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methoxy]-5,6,7,8-tetrahydroquinoline | 167381: Inhibition of angiotensin II-induced contractions in rabbit aorta in vitro. | kd | 0.0001 | uM |
| N-[2-[4-[(2-ethyl-5,7-dimethylimidazo[4,5-b]pyridin-3-yl)methyl]phenyl]phenyl]sulfonyl-2,2-diphenylacetamide | 38124: Inhibition of Angiotensin II receptor, type 1 | ic50 | 0.0001 | uM |
| (2S,3S)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-(methylamino)acetyl]amino]pentanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoic acid | 31303: Inhibitory activity as antagonist of AII on guinea pig ileum | ic50 | 0.0002 | uM |
| 5-butyl-2-(2-phenylethyl)-4-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-1,2,4-triazol-3-one | 166678: Antagonism of angiotensin-II mediated contraction of rabbit aortic rings expressed as pA2 (in vitro) | kd | 0.0002 | uM |
| methyl 2-[2-butyl-4-oxo-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazo[4,5-c]pyridin-5-yl]acetate | 39047: Inhibition of Angiotensin II induced contractions in rabbit aortic rings | ic50 | 0.0002 | uM |
| 2-butyl-5-(2-oxo-2-pyrrolidin-1-ylethyl)-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazo[4,5-c]pyridin-4-one | 39047: Inhibition of Angiotensin II induced contractions in rabbit aortic rings | ic50 | 0.0002 | uM |
| 4-[propyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]pyrimidine-5-carboxylic acid | 37542: Potency to antagonize the ability of angiotensin II to contract rabbit aorta | kd | 0.0002 | uM |
| 3-[propyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]pyridazine-4-carboxylic acid | 37542: Potency to antagonize the ability of angiotensin II to contract rabbit aorta | kd | 0.0002 | uM |
| 3-[butyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]pyrazine-2-carboxylic acid | 37542: Potency to antagonize the ability of angiotensin II to contract rabbit aorta | kd | 0.0002 | uM |
| 6-fluoro-2-[propyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]pyridine-3-carboxylic acid | 37542: Potency to antagonize the ability of angiotensin II to contract rabbit aorta | kd | 0.0002 | uM |
| 4-methyl-2-[propyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]pyridine-3-carboxylic acid | 37542: Potency to antagonize the ability of angiotensin II to contract rabbit aorta | kd | 0.0002 | uM |
| Angiotensin Ii | 1289936: Displacement of [3H]-Asp-{Nomega-[N-(4-propanoylaminobutyl)aminocarbonyl]}Arg-ValTyr-Ile-His-Pro-Phe-OH Tris(hydrotrifluoroacetate) from human AT1 receptor transfected in CHO cells co-expressing Galpha16-mtAEQ after 2 hrs by liquid scintillation counting | ki | 0.0002 | uM |
| 2-ethyl-5-(2-oxo-2-piperidin-1-ylethyl)-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazo[4,5-c]pyridin-4-one | 39047: Inhibition of Angiotensin II induced contractions in rabbit aortic rings | ic50 | 0.0002 | uM |
| (2R)-2-[[(2R)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-5-(diaminomethylideneamino)-2-[[2-(methylamino)acetyl]amino]pentanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]-2-methyl-3-phenylpropanoic acid | 167386: pA2 value was determined in the range of competitive inhibition in the in vitro rabbit aorta strip assay. | kd | 0.0002 | uM |
| 5-hydroxy-2,4-dimethyl-8-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]pyrido[2,3-d]pyrimidin-7-one | 39655: Compound was tested for inhibition against Angiotensin II receptor, type 1 | ic50 | 0.0002 | uM |
| (3S)-4-[[(2S)-5-(diaminomethylideneamino)-1-[[(2S)-1-[[(2S)-3-(4-hydroxyphenyl)-1-[[(2S,3S)-1-[[(2S)-3-(1H-imidazol-5-yl)-1-[[(2S)-3-(1H-imidazol-5-yl)-1-[[(2S,3S)-3-methyl-1-oxo-1-[[(2S)-3-oxo-1-phenylbutan-2-yl]amino]pentan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopentan-2-yl]amino]-3-(methylamino)-4-oxobutanoic acid | 39195: Binding affinity towards Angiotensin receptor from rabbit aorta | ic50 | 0.0002 | uM |
| tert-butyl N-[2-[4-[[1-[2-bromo-5-(pentanoylamino)phenyl]-3-ethyl-5-oxo-1,2,4-triazol-4-yl]methyl]-3-fluorophenyl]phenyl]sulfonylcarbamate | 38124: Inhibition of Angiotensin II receptor, type 1 | ic50 | 0.0002 | uM |
| 2-[2-butyl-4-oxo-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazo[4,5-c]pyridin-5-yl]-N,N-dimethylacetamide | 39047: Inhibition of Angiotensin II induced contractions in rabbit aortic rings | ic50 | 0.0002 | uM |
| N-[2-[4-[[3-butyl-1-[2-chloro-5-(propanoylamino)phenyl]-5-oxo-1,2,4-triazol-4-yl]methyl]-3-fluorophenyl]phenyl]sulfonyl-2-chlorobenzamide | 39659: In vitro inhibitory activity against angiotensin II receptor type 1, in human adrenal membrane preparations. | ic50 | 0.0003 | uM |
| 2-[2-ethyl-4-oxo-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazo[4,5-c]pyridin-5-yl]-N,N-dimethylacetamide | 39047: Inhibition of Angiotensin II induced contractions in rabbit aortic rings | ic50 | 0.0003 | uM |
| tert-butyl N-[2-[4-[[3-butyl-1-[2-chloro-5-(propanoylamino)phenyl]-5-oxo-1,2,4-triazol-4-yl]methyl]phenyl]phenyl]sulfonylcarbamate | 39659: In vitro inhibitory activity against angiotensin II receptor type 1, in human adrenal membrane preparations. | ic50 | 0.0003 | uM |
| tert-butyl N-[2-[4-[[1-[2-bromo-5-(propanoylamino)phenyl]-5-oxo-3-propyl-1,2,4-triazol-4-yl]methyl]-3-fluorophenyl]phenyl]sulfonylcarbamate | 39659: In vitro inhibitory activity against angiotensin II receptor type 1, in human adrenal membrane preparations. | ic50 | 0.0003 | uM |
| ethyl N-[2-[4-[[3-butyl-5-oxo-1-[5-(propanoylamino)-2-(trifluoromethyl)phenyl]-1,2,4-triazol-4-yl]methyl]-3-fluorophenyl]phenyl]sulfonylcarbamate | 39659: In vitro inhibitory activity against angiotensin II receptor type 1, in human adrenal membrane preparations. | ic50 | 0.0003 | uM |
| 5-[(5,7-dimethyl-2-propylimidazo[4,5-b]pyridin-3-yl)methyl]-9-(2H-tetrazol-5-yl)tricyclo[9.4.0.03,8]pentadeca-1(15),3(8),4,6,9,11,13-heptaen-2-one | 39665: Ability to displace [125I]AII binding to COS cells transfected with a cDNA encoding human Angiotensin II receptor, type 1 | ki | 0.0003 | uM |
| N-[2-[4-[[3-butyl-5-oxo-1-[5-(propanoylamino)-2-(trifluoromethyl)phenyl]-1,2,4-triazol-4-yl]methyl]-3-fluorophenyl]phenyl]sulfonyl-2-chlorobenzamide | 39660: In vitro inhibitory activity against Angiotensin II receptor, type 1 in human adrenal membrane preparations. For this assay, only 0.02%BSA was present in the assay mixture. | ic50 | 0.0003 | uM |
| 2-methyl-4-[propyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]pyrimidine-5-carboxylic acid | 37542: Potency to antagonize the ability of angiotensin II to contract rabbit aorta | kd | 0.0003 | uM |
| N,N-diethyl-2-[2-ethyl-4-oxo-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazo[4,5-c]pyridin-5-yl]acetamide | 39047: Inhibition of Angiotensin II induced contractions in rabbit aortic rings | ic50 | 0.0003 | uM |
| 2-[2-butyl-4-oxo-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazo[4,5-c]pyridin-5-yl]-N-methyl-N-phenylacetamide | 39047: Inhibition of Angiotensin II induced contractions in rabbit aortic rings | ic50 | 0.0003 | uM |
| N-[2-[4-[[3-butyl-5-oxo-1-[5-(propanoylamino)-2-(trifluoromethyl)phenyl]-1,2,4-triazol-4-yl]methyl]-3-fluorophenyl]phenyl]sulfonylbenzamide | 39659: In vitro inhibitory activity against angiotensin II receptor type 1, in human adrenal membrane preparations. | ic50 | 0.0003 | uM |
| 5,7-dimethyl-2-propyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazo[4,5-b]pyridine | 39195: Binding affinity towards Angiotensin receptor from rabbit aorta | ic50 | 0.0003 | uM |
| Losartan | 673042: Inhibition of angiotensin AT1 receptor | ic50 | 0.0003 | uM |
| (2S)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-(methylamino)acetyl]amino]pentanoyl]amino]-3-[4-[3-(trifluoromethyl)diazirin-3-yl]phenyl]propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoic acid | 466198: Displacement of [125I][Sar1,Ile8]Ang2 from human AT1 receptor N111G constitutively active mutant expressed in CHO cells by gamma counting | ki | 0.0003 | uM |
| 4-[butyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]pyrimidine-5-carboxylic acid;hydrochloride | 37542: Potency to antagonize the ability of angiotensin II to contract rabbit aorta | kd | 0.0003 | uM |
| 5-[2-[4-[[4-butyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazol-1-ium-1-yl]methyl]phenyl]phenyl]-2H-tetrazole bromide | 736072: Displacement of [125I-Sar1-Ile8]-ANG2 from human Angiotensin 2 type-1 receptor expressed in HEK293 cells after 1 hr by gamma counting analysis | ic50 | 0.0003 | uM |
CTD chemical–gene interactions
76 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Estradiol | decreases reaction, increases expression, decreases expression | 4 |
| Cyclosporine | affects cotreatment, affects expression, decreases expression, decreases methylation | 4 |
| bisphenol A | decreases methylation, increases expression, affects cotreatment, increases methylation | 3 |
| Glucose | decreases reaction, increases expression | 3 |
| Tetrachlorodibenzodioxin | affects expression, decreases expression | 3 |
| Valproic Acid | affects expression, increases expression | 3 |
| Aflatoxin B1 | decreases methylation, affects expression, decreases expression | 3 |
| Losartan | affects binding, decreases activity, decreases abundance, increases expression | 3 |
| sodium arsenite | affects reaction, increases expression, affects binding, increases reaction | 2 |
| potassium chromate(VI) | affects cotreatment, decreases expression, increases expression | 2 |
| epigallocatechin gallate | decreases reaction, increases expression, increases reaction, affects cotreatment, decreases expression | 2 |
| Irbesartan | affects response to substance, affects binding, decreases activity | 2 |
| Acetaminophen | decreases expression | 2 |
| Benzo(a)pyrene | affects methylation, decreases expression, increases methylation | 2 |
| Tretinoin | decreases expression, increases expression | 2 |
| Simvastatin | decreases expression | 2 |
| diminazene aceturate | affects reaction, decreases reaction, increases expression | 1 |
| propionaldehyde | decreases expression | 1 |
| steviol | increases expression | 1 |
| stevioside | increases expression | 1 |
| arsenite | increases methylation | 1 |
| butyraldehyde | decreases expression | 1 |
| 3,4,5,3’,4’-pentachlorobiphenyl | increases expression | 1 |
| rebaudioside A | increases expression | 1 |
| mercuric bromide | increases expression | 1 |
| benazepril | affects cotreatment, affects response to substance | 1 |
| pentanal | decreases expression | 1 |
| chromium hexavalent ion | affects expression | 1 |
| perfluorooctane sulfonic acid | decreases expression | 1 |
| candesartan | affects binding, decreases activity | 1 |
ChEMBL screening assays
421 unique, capped per target: 315 binding, 105 functional, 1 admet
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL4327279 | Binding | Antagonist activity at angiotensin-2 receptor (unknown origin) | Naphthalene, a versatile platform in medicinal chemistry: Sky-high perspective. — Eur J Med Chem |
| CHEMBL642870 | Functional | The compound was tested for its inhibitory activity as antagonist of AII on guinea pig ileum | Synthesis and biological activity of angiotensin II analogues containing a Val-His replacement, Val psi[CH(CONH2)NH]His. — J Med Chem |
| CHEMBL4810226 | ADMET | Inhibition of human angiotensin 2, AT1 at 0.1 to 1 uM | Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor. — J Med Chem |
Cellosaurus cell lines
9 cell lines: 5 cancer cell line, 3 transformed cell line, 1 spontaneously immortalized cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B7VU | Abcam Raji AGTR1 KO | Cancer cell line | Male |
| CVCL_B9WC | Abcam THP-1 AGTR1 KO | Cancer cell line | Male |
| CVCL_C6YD | Abcam PC-3 AGTR1 KO | Cancer cell line | Male |
| CVCL_D7JU | Ubigene A-549 AGTR1 KO | Cancer cell line | Male |
| CVCL_E7HM | LhAT1-D6 | Transformed cell line | Male |
| CVCL_H376 | 293T/AT1 | Transformed cell line | Female |
| CVCL_H514 | HEK293/AT1 | Transformed cell line | Female |
| CVCL_KW31 | PathHunter CHO-K1 AGTR1 beta-arrestin | Spontaneously immortalized cell line | Female |
| CVCL_ZJ96 | Tango AGTR1-bla U2OS | Cancer cell line | Female |
Clinical trials (associated diseases)
300 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT00157963 | PHASE4 | COMPLETED | Hydrochlorothiazide (+) Losartan Potassium vs. Amlodipine Comparative Study (0954A-314) |
| NCT00295555 | PHASE4 | COMPLETED | Doxazosin Effects on ABPM in Hypertensive Patients With Diabetic Nephropathy |
| NCT00311155 | PHASE4 | COMPLETED | Olmesartan and an add-on Treatment in Patients With Mild to Moderate Hypertension |
| NCT00328965 | PHASE4 | COMPLETED | Lacidipine In Mild To Moderate Essential Hypertension Patients With Type 2 Diabetes In Korea |
| NCT00366119 | PHASE4 | UNKNOWN | Safety and Efficacy of Ramipril in the Treatment of Essential Hypertension |
| NCT00408512 | PHASE4 | COMPLETED | Pharmacosurveillance and Pharmacogenetics of First-line Diuretics in Hypertension: The StayOnDiur Study |
| NCT00438945 | PHASE4 | COMPLETED | The Effect of Eprosartan on Hormones and Kidney Function in Patients With Essential Hypertension |
| NCT00457483 | PHASE4 | COMPLETED | Nijmegen Antihypertensive Management Improvement Study |
| NCT00509470 | PHASE4 | COMPLETED | Evaluation of Effect of Combination With Telmisartan and Hydrochlorothiazide in Hypertensives Uncontrolled on Amlodipine |
| NCT00654875 | PHASE4 | COMPLETED | Efficacy and Safety of Once Daily Dosing of Aliskiren (300 mg (qd) Once a Day) to Twice Daily Dosing of Aliskiren (150 mg (Bid) Twice a Day) in Treating Moderate Hypertension. |
| NCT00716950 | PHASE4 | UNKNOWN | Valsartan and Amlodipine Compared to Losartan and Amlodipine in Hypertensive Patients |
| NCT00741585 | PHASE4 | COMPLETED | Prognostic Value of the Circadian Pattern of Ambulatory Blood Pressure for Multiple Risk Assessment |
| NCT00765947 | PHASE4 | COMPLETED | Efficacy and Tolerability of an Aliskiren-based Treatment Algorithm in Patients With Mild to Moderate Hypertension |
| NCT00794885 | PHASE4 | COMPLETED | China Stroke Primary Prevention Trial |
| NCT00819104 | PHASE4 | COMPLETED | A Study to Compare the Efficacy, Safety and Tolerability of Selomax With Its Individual Components |
| NCT00841308 | PHASE4 | UNKNOWN | Home Blood Pressure in Hypertension Management |
| NCT00890591 | PHASE4 | COMPLETED | Efficacy and Safety of Olmesartan Medoxomil in Stage 1 and 2 Essential Hypertension |
| NCT00994617 | PHASE4 | UNKNOWN | Monotherapy Versus Dual Therapy for Initial Treatment for Hypertension |
| NCT01011660 | PHASE4 | UNKNOWN | Effects of Angiotensin II Receptor Blocker Compared With Diuretics in High-risk Hypertensive Patients |
| NCT01042392 | PHASE4 | COMPLETED | Efficacy of Aliskiren Compared to Ramipril in the Treatment of Moderate Systolic Hypertensive Patients |
| NCT01120990 | PHASE4 | COMPLETED | Hybrid Blood Pressure Monitor Validation |
| NCT01131546 | PHASE4 | COMPLETED | Efficacy and Safety of Levamlodipine Besylate Compared to Amlodipine Maleate in Patients With Essential Hypertension |
| NCT01132768 | PHASE4 | TERMINATED | The Confirmatory Olmesartan Plaque Regression Study |
| NCT01180413 | PHASE4 | COMPLETED | Intensive Vasodilator Therapy in Patients With Essential Hypertension |
| NCT01241487 | PHASE4 | COMPLETED | A National Multicentre Study to Assess the Efficacy of the Fixed Combination of Valsartan and Amlodipine in Hypertensive Patients Not Controlled by Monotherapy |
| NCT01629225 | PHASE4 | UNKNOWN | GRK4 Polymorphisms Blood Pressure Response to Candesartan |
| NCT01825759 | PHASE4 | UNKNOWN | Danshen Dropping Pill for Coronary Heart Disease Heart and Artery Structure and Function |
| NCT02031861 | PHASE4 | COMPLETED | Efficacy Study of Nifedipine Controlled-Release Tablets (Xin Ran) to Treat Mild to Moderate Essential Hypertension |
| NCT02058446 | PHASE4 | COMPLETED | PMS Study of Amlodipine/Valsartan for the Treatment of Hypertension |
| NCT02062645 | PHASE4 | COMPLETED | Study of Efficacy and Safety of CVAA489 in Hypertensive Patients |
| NCT02184858 | PHASE4 | COMPLETED | Dose Titration of Lisinopril in Children Aged 1 to 18 Years With Primary or Secondary Hypertension |
| NCT02214498 | PHASE4 | UNKNOWN | Treatment of HYpertension: Morning Versus Evening |
| NCT02357615 | PHASE4 | UNKNOWN | Efficacy Study of Nifedipine Controlled-Release Tablets (Xin Ran) to Treat Early Morning Blood Pressure and Central Arterial Pressure |
| NCT02517866 | PHASE4 | COMPLETED | Azilsartan Medoxomil in the Treatment of Essential Hypertension and Type 2 Diabetes in Asia |
| NCT02612298 | PHASE4 | COMPLETED | Efficacy and Safety of Arotinolol Hydrochloride on Morning Blood Pressure and Heart Rate |
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Related Atlas pages
- Associated diseases: renal tubular dysgenesis of genetic origin, essential hypertension, genetic
- Targeted by drugs: Angiotensin Ii, Azilsartan, Candesartan, Eprosartan, Irbesartan, Losartan, Olmesartan, Olmesartan Medoxomil, Sparsentan, Telmisartan, Valsartan
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): aceruloplasminemia, essential hypertension, essential hypertension, genetic, renal dysplasia, cystic, susceptibility to, renal tubular dysgenesis, renal tubular dysgenesis of genetic origin, retinitis pigmentosa 40