ADRB1

Summary

ADRB1 (adrenoceptor beta 1, HGNC:285) is a protein-coding gene on chromosome 10q25.3, encoding Beta-1 adrenergic receptor (P08588). G protein-coupled receptor for catecholamines that couples to G(s) proteins to activate adenylate cyclase and cAMP-dependent pathway.

The adrenergic receptors (subtypes alpha 1, alpha 2, beta 1, and beta 2) are a prototypic family of guanine nucleotide binding regulatory protein-coupled receptors that mediate the physiological effects of the hormone epinephrine and the neurotransmitter norepinephrine. Beta-1 adrenoceptors are predominately located in the heart. Specific polymorphisms in this gene have been shown to affect the resting heart rate and can be involved in heart failure.

Source: NCBI Gene 153 — RefSeq curated summary.

At a glance

• Gene–disease (curated): short sleep, familial natural, 2 (Limited, GenCC)
• GWAS associations: 57 (top 1% of genes corpus-wide)
• Clinical variants (ClinVar): 81 total — 1 pathogenic
• GTEx eGene: eQTL in 20 tissues, sQTL in 0 (q < 0.05)
• Phenotypes (HPO): 2
• Drug target: yes — 28 curated mechanism-of-action drugs, 12 via a complex or family; 154 molecules with ChEMBL bioactivity (top 1% of genes corpus-wide)
• Approved drugs (ChEMBL mechanism of action): 25 — Acebutolol Hydrochloride, Atenolol, Betaxolol Hydrochloride, +22 more
• Approved drugs acting on a complex or family including it: 12 — Carteolol Hydrochloride, Carvedilol, Dilevalol Hydrochloride, +9 more (Adrenergic receptor beta; Adrenergic receptor)
• Pharmacogenomics (PharmGKB): 1 CPIC/DPWG dosing guideline (e.g. acebutolol;atenolol;betaxolol;bisoprolol;carvedilol;esmolol;labetalol;metoprolol;nadolol;nebivolol;pindolol;propranolol;sotalol)
• Constraint (gnomAD): pLI 0.11 (intermediate), LOEUF 1.94 (unconstrained)
• MANE Select transcript: NM_000684

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:285
Approved symbol	ADRB1
Name	adrenoceptor beta 1
Location	10q25.3
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000043591
Ensembl biotype	protein_coding
OMIM	109630
Entrez	153

Gene structure

Transcript identifiers

Ensembl transcripts: 1 — 1 protein_coding

MANE Select: ENST00000369295

ENST00000369295

RefSeq mRNA: 1 — MANE Select: NM_000684 NM_000684

CCDS: CCDS7586

Canonical transcript exons

ENST00000369295 — 1 exons

Exon	Start	End
ENSE00001449426	114043866	114046904

Expression profiles

Bgee: expression breadth ubiquitous, 205 present calls, max score 97.28.

FANTOM5 (CAGE): breadth broad, TPM avg 5.8674 / max 852.7263, expressed in 588 samples.

Highest expression (Bgee): heart right ventricle, parotid gland, bronchial epithelial cell, lower lobe of lung, endothelial cell.

Genetic regulation across tissues (GTEx eQTL / sQTL)

ADRB1 is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 20 tissues and its splicing (sQTL) in 0 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

20 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Testis	eqtl	2.0e-13	+0.45	10:114032303:G:A
Cells EBV-transformed lymphocytes	eqtl	1.6e-11	+0.81	10:114026474:G:A
Whole Blood	eqtl	3.6e-11	+0.36	10:114070959:C:G
Muscle Skeletal	eqtl	2.4e-09	-0.33	10:114004273:C:T
Spleen	eqtl	2.4e-08	+0.78	10:114026474:G:A
Pancreas	eqtl	3.3e-08	-0.44	10:114013537:G:A
Adipose Subcutaneous	eqtl	5.9e-04	+0.22	10:114029514:AG:A
Esophagus Muscularis	eqtl	1.0e-03	+0.21	10:113804141:A:ACT
Brain Cortex	eqtl	1.1e-03	+0.23	10:114054165:C:T
Brain Cerebellar Hemisphere	eqtl	5.2e-03	+0.74	10:113371869:G:T
Skin Sun Exposed Lower leg	eqtl	5.4e-03	+0.76	10:113118515:TGG:T
Heart Atrial Appendage	eqtl	5.9e-03	-0.27	10:114047123:C:T
Stomach	eqtl	8.0e-03	+0.84	10:113725065:T:C
Esophagus Gastroesophageal Junction	eqtl	2.5e-02	-0.70	10:114604383:G:A
Brain Frontal Cortex BA9	eqtl	2.8e-02	+0.19	10:114054633:C:T
Colon Sigmoid	eqtl	2.9e-02	-0.23	10:114051382:A:G
Thyroid	eqtl	3.0e-02	+0.34	10:114003155:A:T
Brain Amygdala	eqtl	3.9e-02	+2.15	10:114304525:T:C
Artery Coronary	eqtl	4.1e-02	+0.25	10:113971957:G:A
Brain Spinal cord cervical c-1	eqtl	5.0e-02	+0.32	10:114039718:T:C

FANTOM5 promoters

4 alternative TSS:

Promoter ID	TPM avg	Samples expressed
107148	3.9371	495
107147	0.9851	319
107150	0.6932	183
107149	0.2521	118

Top tissues by expression

showing 100 of 279 tissues by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
heart right ventricle	UBERON:0002080	97.28	gold quality
parotid gland	UBERON:0001831	96.39	gold quality
bronchial epithelial cell	CL:0002328	93.58	gold quality
lower lobe of lung	UBERON:0008949	92.36	gold quality
endothelial cell	CL:0000115	91.25	gold quality
placenta	UBERON:0001987	90.98	gold quality
Brodmann (1909) area 23	UBERON:0013554	89.82	gold quality
apex of heart	UBERON:0002098	89.28	gold quality
adult organism	UBERON:0007023	87.75	gold quality
postcentral gyrus	UBERON:0002581	87.28	gold quality
buccal mucosa cell	CL:0002336	86.76	silver quality
parietal lobe	UBERON:0001872	86.62	gold quality
cardiac ventricle	UBERON:0002082	86.61	gold quality
colonic epithelium	UBERON:0000397	86.53	gold quality
entorhinal cortex	UBERON:0002728	86.39	gold quality
heart left ventricle	UBERON:0002084	86.27	gold quality
superior frontal gyrus	UBERON:0002661	85.33	gold quality
primary visual cortex	UBERON:0002436	85.11	gold quality
middle temporal gyrus	UBERON:0002771	84.68	gold quality
epithelium of bronchus	UBERON:0002031	84.45	gold quality
myocardium	UBERON:0002349	83.78	gold quality
occipital lobe	UBERON:0002021	83.72	gold quality
right atrium auricular region	UBERON:0006631	83.71	gold quality
cardiac atrium	UBERON:0002081	83.55	gold quality
bronchus	UBERON:0002185	83.50	gold quality
mucosa of paranasal sinus	UBERON:0005030	82.27	gold quality
heart	UBERON:0000948	81.98	gold quality
left ventricle myocardium	UBERON:0006566	79.80	gold quality
upper lobe of lung	UBERON:0008948	79.51	gold quality
right lung	UBERON:0002167	79.13	gold quality
upper lobe of left lung	UBERON:0008952	79.03	gold quality
nucleus accumbens	UBERON:0001882	78.92	gold quality
cardiac muscle of right atrium	UBERON:0003379	78.15	gold quality
lateral globus pallidus	UBERON:0002476	77.18	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	76.48	gold quality
medial globus pallidus	UBERON:0002477	76.24	gold quality
temporal lobe	UBERON:0001871	76.15	gold quality
bone marrow cell	CL:0002092	75.88	gold quality
frontal cortex	UBERON:0001870	75.78	gold quality
putamen	UBERON:0001874	75.64	gold quality
globus pallidus	UBERON:0001875	74.91	gold quality
right frontal lobe	UBERON:0002810	74.90	gold quality
neocortex	UBERON:0001950	74.82	gold quality
lung	UBERON:0002048	74.79	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	74.73	gold quality
telencephalon	UBERON:0001893	74.59	gold quality
prefrontal cortex	UBERON:0000451	74.48	gold quality
caudate nucleus	UBERON:0001873	74.48	gold quality
cerebral cortex	UBERON:0000956	74.30	gold quality
Brodmann (1909) area 9	UBERON:0013540	74.05	gold quality
nasal cavity mucosa	UBERON:0001826	74.04	gold quality
adipose tissue	UBERON:0001013	72.00	gold quality
cingulate cortex	UBERON:0003027	71.78	gold quality
anterior cingulate cortex	UBERON:0009835	71.49	gold quality
forebrain	UBERON:0001890	70.87	gold quality
connective tissue	UBERON:0002384	70.55	gold quality
adipose tissue of abdominal region	UBERON:0007808	69.87	gold quality
amygdala	UBERON:0001876	69.85	gold quality
vena cava	UBERON:0004087	69.76	gold quality
Ammon’s horn	UBERON:0001954	69.30	gold quality
prostate gland	UBERON:0002367	69.17	gold quality
substantia nigra pars reticulata	UBERON:0001966	68.92	gold quality
nasal cavity epithelium	UBERON:0005384	68.76	gold quality
visceral pleura	UBERON:0002401	68.74	gold quality
omental fat pad	UBERON:0010414	68.56	gold quality
peritoneum	UBERON:0002358	68.49	gold quality
upper leg skin	UBERON:0004262	68.30	gold quality
brain	UBERON:0000955	67.90	gold quality
lower esophagus muscularis layer	UBERON:0035833	67.66	gold quality
lower esophagus	UBERON:0013473	67.63	gold quality
central nervous system	UBERON:0001017	67.39	gold quality
urethra	UBERON:0000057	67.26	gold quality
jejunal mucosa	UBERON:0000399	66.81	gold quality
pleura	UBERON:0000977	66.40	gold quality
parietal pleura	UBERON:0002400	66.39	gold quality
amniotic fluid	UBERON:0000173	66.36	gold quality
substantia nigra pars compacta	UBERON:0001965	65.41	silver quality
substantia nigra	UBERON:0002038	65.22	gold quality
midbrain	UBERON:0001891	64.60	gold quality
muscle layer of sigmoid colon	UBERON:0035805	64.39	gold quality
subcutaneous adipose tissue	UBERON:0002190	63.80	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	63.72	gold quality
thoracic mammary gland	UBERON:0005200	63.71	gold quality
mammary gland	UBERON:0001911	63.63	gold quality
sigmoid colon	UBERON:0001159	63.09	gold quality
monocyte	CL:0000576	62.84	gold quality
mononuclear cell	CL:0000842	62.72	gold quality
leukocyte	CL:0000738	62.46	gold quality
skin of hip	UBERON:0001554	62.28	gold quality
right coronary artery	UBERON:0001625	61.70	gold quality
small intestine	UBERON:0002108	61.65	gold quality
small intestine Peyer’s patch	UBERON:0003454	61.07	gold quality
trachea	UBERON:0003126	60.66	gold quality
colon	UBERON:0001155	60.51	gold quality
duodenum	UBERON:0002114	60.50	gold quality
large intestine	UBERON:0000059	60.26	gold quality
intestine	UBERON:0000160	60.25	gold quality
hypothalamus	UBERON:0001898	60.07	gold quality
corpus epididymis	UBERON:0004359	60.07	gold quality
cortical plate	UBERON:0005343	59.80	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	10.23
E-GEOD-124858	no	1.28

HPA expression

RNA tissue specificity: Tissue enhanced

showing 60 of 73 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM	Protein (IHC)
Placenta	tissue	27.4	low
Nucleus accumbens	tissue	26.3
Postcentral gyrus	tissue	20.3
Heart muscle	tissue	14.6	medium
Frontal cortex	tissue	12.9
Hippocampus	tissue	12.0	low
Locus coeruleus	tissue	7.7
Hippocampal formation	tissue	7.2
Entorhinal cortex	tissue	7.2
Cerebral cortex	tissue	6.7	low
Temporal cortex	tissue	6.7
Insular cortex	tissue	6.4
Prefrontal cortex	tissue	6.3
Caudate putamen	tissue	6.2
Basal ganglia	tissue	6.0	low
Motor cortex	tissue	5.8
Somatosensory cortex	tissue	5.7
Occipital cortex	tissue	5.4
Retrosplenial and cingulate cortex	tissue	5.2
Retrosplenial cortex	tissue	5.2
Salivary gland	tissue	5.0	not detected
Lung	tissue	4.7	not detected
Putamen	tissue	4.1
Prostate	tissue	4.1	not detected
Choroid plexus	tissue	3.8
Amygdala	tissue	3.5
Ventral forebrain	tissue	3.4
Adipose tissue	tissue	2.9	not detected
Superior colliculi	tissue	2.8
Skeletal muscle	tissue	2.2	not detected
Pons	tissue	2.1
Substantia nigra	tissue	2.0
Septum	tissue	2.0
Retina	tissue	1.9
Midbrain	tissue	1.9
Thalamus	tissue	1.6
Pancreas	tissue	1.3	not detected
Hypothalamus	tissue	1.3
Liver	tissue	1.3	not detected
Small intestine	tissue	1.2	not detected
Cerebellum	tissue	1.1	not detected
Medulla oblongata	tissue	1.0
Esophagus	tissue	0.8	not detected
Parathyroid gland	tissue	0.8	not detected
Colon	tissue	0.8	not detected
Duodenum	tissue	0.8	not detected
Periaqueductal gray	tissue	0.8
Pituitary gland	tissue	0.7
Spleen	tissue	0.7	not detected
Kidney	tissue	0.7	medium
Spinal cord	tissue	0.7
Corpus callosum	tissue	0.7
Rectum	tissue	0.6	not detected
Stomach 1	tissue	0.5	not detected
Bone marrow	tissue	0.5	not detected
Olfactory bulb	tissue	0.4
Urinary bladder	tissue	0.3	not detected
Tonsil	tissue	0.3	not detected
Appendix	tissue	0.3	not detected
Skin 1	tissue	0.2	not detected

Brain sub-regions (HPA Brain Atlas): detected in 189; highest nTPM — Temporo-occipital transitional zone (30.0), Transversal temporal gyrus, anterior (25.8), Inferior parietal lobule (25.3), Area parastriata, superior (24.8), Supramarginal gyrus (24.7).

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): BMAL1, CREM, EGR1, MYC, NCOA1, NR3C1, RARA, RXRA, SP1, ZHX2

miRNA regulators (miRDB)

Targeting ADRB1 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).

showing 30 of 117 miRNAs:

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-8485	100.00	77.57	4731
HSA-MIR-6833-3P	100.00	70.63	3197
HSA-MIR-7110-3P	100.00	73.18	2486
HSA-MIR-6873-3P	100.00	71.42	2626
HSA-MIR-30A-5P	100.00	76.31	3233
HSA-MIR-30B-5P	100.00	76.29	3248
HSA-MIR-30C-5P	100.00	76.29	3248
HSA-MIR-30D-5P	100.00	76.32	3233
HSA-MIR-30E-5P	100.00	76.32	3242
HSA-MIR-4768-5P	100.00	69.49	2861
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-5692B	100.00	71.32	2622
HSA-MIR-5692C	100.00	71.32	2622
HSA-MIR-3185	99.99	68.12	1959
HSA-MIR-4500	99.99	72.72	2367
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-548AW	99.99	72.57	3559
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-19A-3P	99.98	75.33	2762
HSA-MIR-19B-3P	99.98	75.44	2754
HSA-MIR-32-5P	99.98	75.21	1964
HSA-MIR-92A-3P	99.98	75.21	1960
HSA-MIR-92B-3P	99.98	75.25	1955
HSA-MIR-25-3P	99.98	74.60	1817
HSA-MIR-363-3P	99.98	74.72	1821
HSA-MIR-367-3P	99.98	74.83	1819
HSA-LET-7A-5P	99.98	72.29	1790
HSA-LET-7B-5P	99.98	72.31	1790
HSA-LET-7C-5P	99.98	72.29	1790
HSA-LET-7E-5P	99.98	72.29	1790

Functional genomics

gnomAD constraint: pLI 0.111, LOEUF 1.94, missense Z -0.848 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD

Regional missense constraint (gnomAD)

ENST00000369295 splits into 4 regions with different missense tolerance; 0 are missense-constrained. Missense variants in a constrained region (low observed/expected) are more likely to be pathogenic. gnomAD

Region (GRCh38)	Missense obs / exp	o/e	Constrained
10:114,044,133–114,044,904	289 / 371.6	0.78	no
10:114,044,905–114,045,084	104 / 96.7	1.08	no
10:114,045,085–114,045,153	12 / 30.3	0.40	no
10:114,045,154–114,045,563	230 / 210.5	1.09	no

Literature-anchored findings (GeneRIF, showing 40)

• A polymorphism in the beta1 adrenergic receptor is associated with resting heart rate (PMID:11854867)
• Gly389Arg ADRB1 variant is associated with greater body weight and BMI in Caucasian women due to a greater fat mass (PMID:12032746)
• The agonist-specific component of beta1AR downregulation requires internalization correlating more closely with receptor degradation, while the cAMP-specific component does not require internalization and is associated with downregulation of beta1AR mRNA. (PMID:12069593)
• beta1-adrenoceptor and beta2-adrenoceptor couple to Gs-proteins to activate adenylyl cyclase (PMID:12106601)
• role of heterodimerization with beta 2-adrenergic receptor regulates beta 2-adrenergic receptor internalization and ERK signaling efficacy (PMID:12140284)
• Suppressive effect of the Gly389 allele of the beta1-adrenergic receptor gene on the occurrence of ventricular tachycardia in dilated cardiomyopathy. (PMID:12197595)
• Results indicate that the proportion of homo- and heterodimers between the closely related beta(1)- and beta(2)-adrenergic receptors is determined by their relative levels of expression. (PMID:12244098)
• Glycosylation regulates receptor surface expression and dimerization (PMID:12270132)
• These results suggest a model whereby the physical interaction between the beta1-AR and CNrasGEF facilitates the transduction of Gsalpha-induced cAMP signal into the activation of Ras. (PMID:12391161)
• An interaction between beta(1)AR and alpha(2A)AR is regulated by glycosylation and may play a key role in cross-talk and mutual regulation between these receptors. (PMID:12529373)
• An association was not found between B1AR polymorphism and major depression, but there was a tendency for a relation between CC homozygosity and a better and even faster response to antidepressant treatment in patients with major depression. (PMID:12815745)
• The partial agonist activity of bucindolol is dependent on the activation state of the human beta-1 adrenergic receptor (PMID:12847069)
• Data show that the beta(1)-adrenergic receptor Arg389 variant predisposes to heart failure through hyperactive signaling programs, depressed receptor coupling and ventricular dysfunction, and influences the therapeutic response to beta-receptor blockade. (PMID:14502278)
• internalization of beta(1)AR is both arrestin- and dynamin-dependent and follows the same clathrin-mediated endocytic pathway as beta(2)AR (PMID:14734649)
• PKA-mediated phosphorylation of G protein-coupled receptors might result in motif-dependent desensitization or resensitization. (PMID:14990580)
• The ADRB1/R389G polymorphism tended to be associated with hypertensive status in male subjects (p=0.0117, p(c)=0.0702). (PMID:15055253)
• Single-nucleotide polymorphisms (SNPs) in the beta1-adrenergic receptor (ADRB1) allelic frequencies were analyzed in Alzheimer’s disease. The combination of G protein beta3 subunit and ADRB1 polymorphisms produces AD susceptibility. (PMID:15212839)
• The Ser49Gly functional polymorphism in the beta(1) adrenergic receptor might explain some of the population variance in extraversion and related personality traits. (PMID:15312808)
• the lack of agonist-mediated ubiquitination of beta1AR may prevent its extensive trafficking to lysosomes (PMID:15331590)
• Substitution of the C-terminal cytoplasmic tail of the beta2-adrenergic receptor on the beta1-adrenergic receptor enabled the chimeric G protein-coupled receptor to be functionally and spatially regulated by insulin. (PMID:15388645)
• evidence for an interaction between the beta1- and beta2-adrenergic receptors was observed in men for longitudinal change in body mass index and women showed suggestive evidence for an interaction between the beta1- and beta3-adrenergic receptors (PMID:15833937)
• beta1AR or the beta2AR polymorphisms do not affect patient response to beta-blockade treatment for stable congestive heart failure (PMID:15861037)
• the Arg389Arg and Ser49Gly polymorphisms may have roles in left ventricular remodeling changes in response to beta-blocker therapy (PMID:15864115)
• Beta(1)-adrenergic receptor mRNA expressions in myocardium were significantly lower in patients with heart failure than those in control subjects. (PMID:15932670)
• In this small pilot series, a single nucleotide polymorphism at codon 389 in the beta1-AR seems to correlate with a response to betaxolol therapy in normal, nonglaucomatous volunteers. (PMID:16325708)
• the amphipathic character of helix 8 and side chain projections of Asp382 and Arg384 within the hydrophilic interface might serve as a tethering site for the G protein (PMID:16500896)
• Val-120, Ile-185, Asp-212, and Lys-253 are critically involved in conformational changes occurring during receptor activation (PMID:16648137)
• Homozygousbeta1AR Arg389Gly predicts cardiac troponin release in subarachnoid hemorrhage. Combining homozygous B1AR Arg389Gly & homozygous deletion of B2AR increases the odds of reduced left ventricular ejection fraction. (PMID:16728691)
• These findings indicate that Lys324 lies in a groove between helices 3 and 6, and its mutagenesis generates a mutant receptor with very low binding affinity for the GDP-bound isoform of G(s). (PMID:16760361)
• beta1-adrenergic receptors are upregulated and troponin I is dephosphorylated in end-stage heart failure patients supported by ventricular assist devices (PMID:16765375)
• Certain polymorphisms of the ADRB1 and ADRB2 genes influence the pathophysiology of open-angle glaucoma in Japanese patients. (PMID:16785856)
• beta(1)AR-389 variation alters signaling in multiple models and affects the beta-blocker therapeutic response in heart failure (PMID:16844790)
• These results suggest that the dynamic association of 14-3-3 proteins to both beta(1)AR and Kv11.1 channels is involved in the adrenergic modulation of this critical regulator of cardiac repolarization and refractoriness. (PMID:16914520)
• AKAP79 provides cyclic AMP-dependent protein kinase to phosphorylate the beta1-adrenergic receptor and thereby dictate the recycling and resensitization itineraries of the beta1-adrenergic receptor (PMID:16940053)
• Our results suggest that CRM 1-dependent NES-mediated mechanisms influence the degradation and agonist-mediated down-regulation of the beta1-AR mRNAs. (PMID:16997396)
• In this relatively small study, double homozygosity for Arg389 and Ser49 of the human beta1-adrenergic receptor associated with the risk of symptoms in LQT1. (PMID:17023080)
• Golgin-160 interacts with beta1AR (PMID:17118120)
• Genetic polymorphisms in the B1AR gene have the potential to explain some of the observed ethnic variability in drug response and to improve clinical practice (Review) (PMID:17329986)
• results suggest that the Arg389Gly polymorphism does not have any clinically important impact on the pathogenesis of obesity in Danish white subjects; this variant is most likely not to be a major contributor to the development of hypertension (PMID:17335470)
• Pulse wave velocity and nitroglycerin-induced hyperemia were both closely associated with the Ser49Gly polymorphism. (PMID:17345787)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	adrb1	ENSDARG00000007490
mus_musculus	Adrb1	ENSMUSG00000035283
rattus_norvegicus	Adrb1	ENSRNOG00000017002
caenorhabditis_elegans	ser-5	WBGENE00008890

Paralogs (18): ADRA1A (ENSG00000120907), DRD2 (ENSG00000149295), ADRA2A (ENSG00000150594), GPR101 (ENSG00000165370), ADRB2 (ENSG00000169252), ADRA1B (ENSG00000170214), ADRA1D (ENSG00000171873), OR5T3 (ENSG00000172489), OR56A1 (ENSG00000180934), OR5T1 (ENSG00000181698), OR5T2 (ENSG00000181718), OR56A4 (ENSG00000183389), ADRA2C (ENSG00000184160), OR56A3 (ENSG00000184478), OR13F1 (ENSG00000186881), OR56A5 (ENSG00000188691), ADRB3 (ENSG00000188778), ADRA2B (ENSG00000274286)

Mouse-model phenotypes

Observed phenotypes of the mouse ortholog (MGI:87937) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 3 distinct phenotype terms.

Mouse phenotype (MP)	Records
abnormal cardiovascular system physiology	1
abnormal physiological response to xenobiotic	1
prenatal lethality, incomplete penetrance	1

Additional cross-species homologs

Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.

Organism	UniProt	Identity	Method
Capra hircus	Q9XT57	98.8%	Diamond
Ovis aries	Q9XT58	98.8%	Diamond
Meriones unguiculatus	O70430	98.6%	Diamond
Macaca mulatta	P47899	98.6%	Diamond
Felis catus	Q9TST6	98.6%	Diamond
Bos taurus	P46626	97.8%	Diamond
Canis lupus familiaris	P79148	97.3%	Diamond
Mesocricetus auratus	P04274	95.7%	Diamond
Tscherskia triton	Q4KWL2	95.7%	Diamond
Xenopus laevis	P34973	92.9%	Diamond
Cavia porcellus	Q8K4Z4	90.8%	Diamond
Sus scrofa	Q95252	90.6%	Diamond
Takifugu rubripes	P53452	80.8%	Diamond
Aplysia californica	Q16950	77.5%	Diamond
Meleagris gallopavo	P07700	68.0%	Diamond
Oncorhynchus mykiss	Q8UUY8	64.5%	Diamond
Oryzias latipes	Q91178	43.4%	Diamond

Genomic neighbors (locus context)

Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).

Symbol	Type	Entrez
NHLRC2	protein-coding	374354
MIR2110	ncRNA	100302224
CCDC186	protein-coding	55088

Protein

Protein identifiers

Beta-1 adrenergic receptor — P08588 (reviewed: P08588)

Alternative names: Beta-1 adrenoreceptor

All UniProt accessions (1): P08588

UniProt curated annotations — full annotation on UniProt →

Function. G protein-coupled receptor for catecholamines that couples to G(s) proteins to activate adenylate cyclase and cAMP-dependent pathway. Binds epinephrine and norepinephrine with approximately equal affinity. Mediates the activation of Ras via binding with cAMP-dependent RAPGEF2. As part of the sympathetic nervous system, plays a role in the physiologic regulation of cardiac functions such as stimulation of cardiomyocyte contraction. Also delivers proapoptotic signals in cardiomyocytes. Involved in the regulation of sleep/wake behaviors.

Subunit / interactions. Interacts (via PDZ-binding motif) with RAPGEF2 (via PDZ domain); the interaction is direct and is required for Ras activation upon ligand stimulation. Interacts (via PDZ-binding motif) with GOPC, MAGI3 and DLG4; interaction mediates ADRB1 trafficking and signaling in a cell-specific manner.

Subcellular location. Cell membrane.

Post-translational modifications. Homologous desensitization of the receptor is mediated by its phosphorylation by beta-adrenergic receptor kinase.

Domain organisation. The PDZ domain-binding motif mediates competitive interactions with GOPC, MAGI3 and DLG4 and plays a role in subcellular location of the receptor.

Polymorphism. Genetic variations in ADRB1 are associated with inter-individual variability in the resting heart rate. This quantitative trait has been significantly correlated with cardiovascular morbidity and mortality [MIM:607276]. Genetic variations in ADRB1 are associated with the familial natural short sleep 2 (FNSS2) phenotype, an autosomal dominant trait [MIM:618591]. Individuals with this trait require less sleep in any 24-hour period than is typical for their age group.

Similarity. Belongs to the G protein-coupled receptor 1 family. Adrenergic receptor subfamily. ADRB1 sub-subfamily.

RefSeq proteins (1): NP_000675* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000507	ADRB1_rcpt	Family
IPR002233	ADR_fam	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (71 total): helix 16, mutagenesis site 11, topological domain 8, sequence variant 8, transmembrane region 7, binding site 6, modified residue 3, region of interest 2, compositionally biased region 2, disulfide bond 2, turn 2, chain 1, short sequence motif 1, lipid moiety-binding region 1, glycosylation site 1

Structure

Experimental structures (PDB)

7 structures by resolution:

PDB	Title	Method	Resolution (Å)
7BVQ	Structure of human beta1 adrenergic receptor bound to carazolol	X-RAY DIFFRACTION	2.5
7BU7	Structure of human beta1 adrenergic receptor bound to BI-167107 and nanobody 6B9	X-RAY DIFFRACTION	2.6
7BU6	Structure of human beta1 adrenergic receptor bound to norepinephrine and nanobody 6B9	X-RAY DIFFRACTION	2.7
7BTS	Structure of human beta1 adrenergic receptor bound to epinephrine and nanobody 6B9	X-RAY DIFFRACTION	3.13
9L84	Structure of beta1-AR-Gs complex bound to epinephrine and an allosteric modulator	ELECTRON MICROSCOPY	3.22
8S2T	Cryo-EM structure of cell-free synthesized Human beta-1 adrenergic receptor …	ELECTRON MICROSCOPY	3.3
2LSQ	Analog of the fragment 197-221 of beta-1 adrenoreceptor	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P08588-F1	77.01	0.52

Antibody-complex structures (SAbDab)

4 antibodies co-crystallized with this protein: 7BTS, 7BU6, 7BU7, 8S2T

Human Protein Atlas

Protein class: Transporters, G-protein coupled receptors, GPCRs excl olfactory receptors, Predicted membrane proteins, GPCRHMM predicted membrane proteins, FDA approved drug targets, Small molecule drugs

Protein evidence: Evidence at protein level

Antibody reliability (HPA): IH enhanced

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 (6)

Position	Role
138	(R)-adrenaline
138	(R)-noradrenaline
344	(R)-adrenaline
344	(R)-noradrenaline
363	(R)-adrenaline
363	(R)-noradrenaline

Post-translational modifications (4)

Type	Positions
Phosphoserine	312, 412, 428
S-palmitoyl cysteine	392

Disulfide bonds (2)

Type	Positions
Disulfide bond	131–216, 209–215

Glycosylation sites (1)

Type	Positions
N-linked (glcnac…) asparagine	15

Mutagenesis-validated functional residues (11)

Position	Phenotype
199	decreased noradrenaline affinity.
347	decreased noradrenaline affinity.
359	decreased noradrenaline affinity.
474	loss of interaction with gopc.
474	loss of interaction with gopc; when associated with a-477.
475	loss of interaction with gopc. loss of interaction with rapgef2. abolishes agonist-induced ras activation.
475	loss of interaction with rapgef2.
475	partial loss of interaction with gopc.
476	partial loss of interaction with gopc.
477	loss of interaction with gopc.
477	loss of interaction with rapgef2. abolishes agonist-induced ras activation.

Function

Pathways and Gene Ontology

Reactome pathways

2 curated (TAS) of 8; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

8 pathways:

ID	Pathway	Evidence
R-HSA-390696	Adrenoceptors	curated
R-HSA-418555	G alpha (s) signalling events	curated
R-HSA-375280	Amine ligand-binding receptors	—
R-HSA-373076	Class A/1 (Rhodopsin-like receptors)	—
R-HSA-388396	GPCR downstream signalling	—
R-HSA-500792	GPCR ligand binding	—
R-HSA-162582	Signal Transduction	—
R-HSA-372790	Signaling by GPCR	—

MSigDB gene sets: 238 (showing top): GOBP_CIRCADIAN_RHYTHM, BENPORATH_ES_WITH_H3K27ME3, GOBP_BEHAVIOR, GOBP_REGULATION_OF_BLOOD_PRESSURE, GOBP_RESPONSE_TO_COLD, GOBP_CIRCULATORY_SYSTEM_PROCESS, XU_GH1_AUTOCRINE_TARGETS_UP, GOCC_SECRETORY_GRANULE, GOBP_REGULATION_OF_DEVELOPMENTAL_GROWTH, GOBP_RESPONSE_TO_DIETARY_EXCESS, GCANCTGNY_MYOD_Q6, GOBP_GROWTH, GOBP_REGULATION_OF_SYSTEMIC_ARTERIAL_BLOOD_PRESSURE, GOBP_POSITIVE_REGULATION_OF_MAPK_CASCADE, SP1_Q2_01

GO Biological Process (11): positive regulation of heart rate by epinephrine-norepinephrine (GO:0001996), norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure (GO:0002025), adenylate cyclase-activating G protein-coupled receptor signaling pathway (GO:0007189), positive regulation of cardiac muscle cell apoptotic process (GO:0010666), positive regulation of MAPK cascade (GO:0043410), regulation of circadian sleep/wake cycle, sleep (GO:0045187), adenylate cyclase-activating adrenergic receptor signaling pathway (GO:0071880), positive regulation of cold-induced thermogenesis (GO:0120162), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186), positive regulation of heart contraction (GO:0045823)

GO Molecular Function (9): beta-adrenergic receptor activity (GO:0004939), beta1-adrenergic receptor activity (GO:0004940), PDZ domain binding (GO:0030165), alpha-2A adrenergic receptor binding (GO:0031694), protein heterodimerization activity (GO:0046982), G protein-coupled receptor activity (GO:0004930), adrenergic receptor activity (GO:0004935), protein binding (GO:0005515), G protein-coupled neurotransmitter receptor activity (GO:0099528)

GO Cellular Component (5): early endosome (GO:0005769), plasma membrane (GO:0005886), Schaffer collateral - CA1 synapse (GO:0098685), neuronal dense core vesicle (GO:0098992), membrane (GO:0016020)

Reactome top-level categories

6 top-level categories:

Category	Pathways
Signaling by GPCR	2
Amine ligand-binding receptors	1
GPCR downstream signalling	1
Signal Transduction	1
GPCR ligand binding	1
Class A/1 (Rhodopsin-like receptors)	1

GO top-level categories

46 GO namespaces:

Category	Terms
adrenergic receptor signaling pathway	2
G protein-coupled receptor activity	2
positive regulation of blood pressure by epinephrine-norepinephrine	1
positive regulation of heart rate	1
regulation of systemic arterial blood pressure by norepinephrine-epinephrine	1
negative regulation of systemic arterial blood pressure	1
vasodilation	1
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	1
adenylate cyclase activator activity	1
cardiac muscle cell apoptotic process	1
positive regulation of striated muscle cell apoptotic process	1
regulation of cardiac muscle cell apoptotic process	1
MAPK cascade	1
regulation of MAPK cascade	1
positive regulation of intracellular signal transduction	1
regulation of circadian sleep/wake cycle	1
circadian sleep/wake cycle, sleep	1
adenylate cyclase-activating G protein-coupled receptor signaling pathway	1
positive regulation of multicellular organismal process	1
cold-induced thermogenesis	1
regulation of cold-induced thermogenesis	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
signal transduction	1
regulation of heart contraction	1
heart contraction	1
positive regulation of blood circulation	1
adrenergic receptor activity	1
beta-adrenergic receptor activity	1
protein domain specific binding	1
adrenergic receptor binding	1
protein dimerization activity	1
transmembrane signaling receptor activity	1
G protein-coupled receptor signaling pathway	1
G protein-coupled amine receptor activity	1
binding	1
neurotransmitter receptor activity	1
endosome	1
membrane	1
cell periphery	1
synapse	1
dense core granule	1
cellular anatomical structure	1

Experimentally-supported GO annotations

GO terms backed by direct experimental evidence (ECO experimental codes) — 9 of 26 annotations. The rest are phylogenetic / computational / electronic (IEA).

9 experimentally-supported GO terms:

GO term	NS	Evidence
adenylate cyclase-activating adrenergic receptor signaling pathway	BP	direct assay
positive regulation of heart rate by epinephrine-norepinephrine	BP	direct assay
regulation of circadian sleep/wake cycle, sleep	BP	mutant phenotype
early endosome	CC	direct assay
plasma membrane	CC	direct assay
PDZ domain binding	MF	physical interaction
alpha-2A adrenergic receptor binding	MF	physical interaction
beta1-adrenergic receptor activity	MF	direct assay
protein heterodimerization activity	MF	physical interaction

Protein interactions and networks

STRING

showing 15 of 1,270 interactions by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
ADRB1	CAMK2D	Q13557	770
ADRB1	ARRB1	P49407	759
ADRB1	GRK5	P34947	722
ADRB1	PRKACG	P22612	692
ADRB1	ARRB2	P32121	646
ADRB1	RHO	P08100	623
ADRB1	DBH	P09172	605
ADRB1	UCP1	P25874	600
ADRB1	VGF	O15240	593
ADRB1	TPM3	P06753	593
ADRB1	GRK2	P25098	586
ADRB1	KCNN3	Q9UGI6	584
ADRB1	ACE	P12821	571
ADRB1	REN	P00797	570
ADRB1	ADGRD1	Q6QNK2	563

IntAct

Human interaction partners of ADRB1 in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).

showing 30 of 85 partners by confidence:

Partner	Interaction type	MIscore	Records
MAGI2	direct interaction	0.830	13
MAGI3	direct interaction	0.740	6
MAGI1	direct interaction	0.620	2
ADORA1	physical association	0.610	4
GPER1	physical association	0.570	6
DRD4	physical association	0.470	2
PATJ	direct interaction	0.440	7
GRIP1	direct interaction	0.440	5
GRIP2	direct interaction	0.440	5
DLG4	direct interaction	0.440	3
IL16	direct interaction	0.440	3
MPDZ	direct interaction	0.440	3
NHERF4	direct interaction	0.440	3
PDZK1	direct interaction	0.440	3
WHRN	direct interaction	0.440	3
APBA2	direct interaction	0.440	2
DLG1	direct interaction	0.440	2
FRMPD2	direct interaction	0.440	2
GRID2IP	direct interaction	0.440	2
LNX1	direct interaction	0.440	2
LNX2	direct interaction	0.440	2
SCRIB	direct interaction	0.440	2
TJP1	direct interaction	0.440	2
AHNAK	direct interaction	0.440	1
APBA1	direct interaction	0.440	1
APBA3	direct interaction	0.440	1
ARHGAP21	direct interaction	0.440	1
ARHGEF11	direct interaction	0.440	1
CARD11	direct interaction	0.440	1
CASK	direct interaction	0.440	1

BioGRID (16 interactions; top human partners by supporting records): DLG4 (Affinity Capture-Western; 4 records), ARRB1 (Reconstituted Complex; 2 records), GIPC1 (Two-hybrid; 2 records), MAGI2 (Affinity Capture-Western; 2 records), ADRB2 (Two-hybrid), ARRB2 (Affinity Capture-Western), GPRASP1 (Reconstituted Complex), GPRASP2 (Reconstituted Complex), SNTA1 (Protein-peptide), USP20 (Affinity Capture-Western)

SIGNOR signaling

showing 26 of 28 signaling interactions:

A	Effect	B	Mechanism
GOPC	down-regulates	ADRB1	relocalization
ADRB1	“up-regulates activity”	GNAS	binding
ADRB1	“up-regulates activity”	GNAL	binding
ADRB1	“up-regulates activity”	GNA14	binding
L-isoprenaline	“up-regulates activity”	ADRB1	“chemical activation”
ADRB1	“up-regulates activity”	GNAZ	binding
ADRB1	“up-regulates activity”	GNAQ	binding
ADRB1	“up-regulates activity”	GNA12	binding
ADRB1	“up-regulates activity”	GNA13	binding
ADRB1	“up-regulates activity”	GNAO1	binding
ADRB1	“up-regulates activity”	GNA15	binding
ARRB2	“down-regulates activity”	ADRB1	binding
N-[2-hydroxy-5-(1-hydroxy-2-{[1-(4-methoxyphenyl)propan-2-yl]amino}ethyl)phenyl]formamide	“up-regulates activity”	ADRB1	“chemical activation”
“Cy3-bifunctional dye zwitterion”	“up-regulates activity”	ADRB1	“chemical activation”
denopamine	“up-regulates activity”	ADRB1	“chemical activation”
clenbuterol	“up-regulates activity”	ADRB1	“chemical activation”
procaterol	“up-regulates activity”	ADRB1	“chemical activation”
(R)-salbutamol	“up-regulates activity”	ADRB1	“chemical activation”
fenoterol	“up-regulates activity”	ADRB1	“chemical activation”
terbutaline	“up-regulates activity”	ADRB1	“chemical activation”
metaproterenol	“up-regulates activity”	ADRB1	“chemical activation”
adrenaline	“up-regulates activity”	ADRB1	“chemical activation”
arformoterol	“up-regulates activity”	ADRB1	“chemical activation”
practolol	“down-regulates activity”	ADRB1	“chemical inhibition”
metoprolol	“down-regulates activity”	ADRB1	“chemical inhibition”
isoprenaline	“up-regulates activity”	ADRB1	“chemical activation”

Protein complexes (CORUM) (16)

Experimentally-characterized complexes this protein is a subunit of (★ = the complex contains a known drug target).

16 complexes by size:

Complex	Subunits	Members
★ beta(1)-AR receptosome (ADRB1-SAP97-AKAP79-PRKAR2A)	4	ADRB1, AKAP5, DLG1, PRKAR2A
★ PKA (RII-alpha and RII-beta)-AKAP5-ADRB1 complex	4	ADRB1, AKAP5, PRKAR2A, PRKAR2B
★ ADRB1-DRD4 complex	2	ADRB1, DRD4
★ ADRA2A-ADRB1 complex	2	ADRA2A, ADRB1
★ ADRB1-GRK2 complex	2	ADRB1, GRK2
★ ADRB1-GOPC complex	2	ADRB1, GOPC
★ ADRB1-ADRB2 complex	2	ADRB1, ADRB2
★ ADRB1-MAGI2 complex	2	ADRB1, MAGI2
★ ADRB1-GIPC1 complex	2	ADRB1, GIPC1
★ ADRB1-GOLGA3 complex	2	ADRB1, GOLGA3
★ ADRB1-YWHAE complex	2	ADRB1, YWHAE
★ ADRB1-SSTR5 complex	2	ADRB1, SSTR5
★ ADRB1-GPER1 complex	2	ADRB1, GPER1
★ ADRB1-GPRASP1 complex	2	ADRB1, GPRASP1
★ ADRB1-GPRASP2 complex	2	ADRB1, GPRASP2
★ Beta-1 adrenergic receptor	1	ADRB1

Ligand–receptor pairs (CellPhoneDB) (6)

Curated ligand–receptor partners (cell-cell communication), distinct from the protein–protein interactions above.

6 ligand–receptor pairs:

Partner	This gene’s role	Signaling class
PNMT;SLC18A1	receptor	Signaling by Adrenaline
PNMT	receptor	Signaling by Epinephrine
DBH;SLC18A1	receptor	Signaling by Noradrenaline
PNMT;SLC18A2	receptor	Signaling by Adrenaline
DBH;SLC18A2	receptor	Signaling by Noradrenaline
DBH;SLC6A2	receptor	Signaling by Noradrenaline

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 85 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.

Reactome pathways:

Pathway	Partners	Fold	FDR
Dopamine Neurotransmitter Release Cycle	5	44.3×	4e-06
Protein-protein interactions at synapses	7	33.2×	1e-07
Assembly and cell surface presentation of NMDA receptors	7	31.7×	1e-07
Neurexins and neuroligins	9	31.6×	2e-09
Neuronal System	7	5.5×	5e-03

GO biological processes:

GO term	Partners	Fold	FDR
establishment or maintenance of epithelial cell apical/basal polarity	8	56.0×	6e-10
regulation of postsynaptic membrane neurotransmitter receptor levels	5	29.9×	8e-05
bicellular tight junction assembly	5	19.9×	3e-04
protein-containing complex assembly	9	12.3×	9e-06
protein localization to plasma membrane	8	10.5×	9e-05
cell-cell adhesion	7	8.6×	7e-04
protein transport	12	6.3×	6e-05

Disease & clinical

Genetic variants

Variant evidence for ADRB1: 81 ClinVar records (1 pathogenic / likely pathogenic); 1 PharmGKB dosing guideline; 57 GWAS associations. Per-variant detail is on Sugi Variant.

ClinVar

81 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	0
Uncertain significance	57
Likely benign	13
Benign	8

Top pathogenic / likely-pathogenic (1)

Showing all 1 pathogenic / likely-pathogenic ClinVar records, ranked by ClinVar review status (expert panel → multiple submitters → single submitter), then by number of submitting labs.

Variant ID	HGVS	Classification	Review	Submitters
691285	NM_000684.3(ADRB1):c.560C>T (p.Ala187Val)	Pathogenic	no assertion criteria provided	1

Per-variant reference — Sugi Variant

Explore ADRB1’s pathogenic and likely-pathogenic variants individually — each with its ClinVar classification and conditions, applied ACMG criteria (ClinGen expert panel, where curated), the calibrated in-silico predictors (AlphaMissense, REVEL, SaProt, conservation), gnomAD frequency, and the predictor-disagreement QC signal — on Sugi Variant.

SpliceAI

Top 3 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 3 predictions of 3):

Position(s)	Effect	Δscore	Sites
10:114043976	donor_gain	0.4900
10:114045723	donor_gain	0.4600
10:114046751	acceptor_gain	0.3600

AlphaMissense

1,202 missense substitutions predicted likely pathogenic (of 3,017 scored), across 268 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:

Residue	Likely-pathogenic substitutions	Mean am_pathogenicity	Max am_pathogenicity
M240	9	0.966	0.999
D104	8	0.999	1.000
D138	8	0.998	0.999
N76	8	0.996	0.999
F333	8	0.996	1.000
F233	8	0.995	1.000
F341	8	0.994	1.000
D155	8	0.993	0.998
F218	8	0.991	1.000
S145	8	0.988	0.999
N373	8	0.988	0.999
F340	8	0.987	1.000
F383	8	0.981	0.999
N369	8	0.980	1.000
F387	8	0.975	0.999
F96	8	0.974	0.997
M107	8	0.950	0.993
F191	8	0.948	0.993
F359	8	0.942	0.994
F164	8	0.936	0.991

HPA cancer prognostics

RNA cancer specificity: Group enriched (Kidney Chromophobe, Prostate Adenocarcinoma)

Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.

1 prognostic cancer types:

Cancer	Prognostic	p-value
Colon Adenocarcinoma (validation)	unfavorable	0.000397

Disease associations

OMIM: gene MIM:109630 | disease phenotypes:

GenCC curated gene-disease

1 curated gene-disease records:

Disease	Classification	Inheritance	Records
short sleep, familial natural, 2	Limited	Autosomal dominant

Mondo (1): (MONDO:0020786)

HPO phenotypes

2 phenotypes (HPO-id order):

HPO	Term
HP:0000006	Autosomal dominant inheritance
HP:0033063	Shortened sleep phase

GWAS associations

showing 30 of 57 associations:

Study	Trait	p-value
GCST008362_73	Birth weight	2e-28
GCST010242_527	HDL cholesterol levels	5e-25
GCST006166_34	Diastolic blood pressure x alcohol consumption interaction (2df test)	8e-23
GCST006188_7	Systolic blood pressure (cigarette smoking interaction)	1e-22
GCST006187_28	Diastolic blood pressure (cigarette smoking interaction)	3e-22
GCST006187_27	Diastolic blood pressure (cigarette smoking interaction)	1e-21
GCST006434_107	Systolic blood pressure x alcohol consumption interaction (2df test)	2e-20
GCST005146_35	Birth weight	5e-18
GCST010244_151	Triglyceride levels	2e-16
GCST009151_14	High density lipoprotein cholesterol levels	9e-16
GCST010241_395	Apolipoprotein A1 levels	8e-15
GCST006258_14	Diastolic blood pressure	9e-15
GCST006188_6	Systolic blood pressure (cigarette smoking interaction)	2e-14
GCST90002401_370	Platelet distribution width	1e-13
GCST007930_143	Medication use (agents acting on the renin-angiotensin system)	2e-13
GCST010243_93	Apolipoprotein B levels	2e-13
GCST007267_325	Systolic blood pressure	4e-13
GCST006259_39	Systolic blood pressure	5e-13
GCST007094_68	Diastolic blood pressure	4e-12
GCST006190_47	Diastolic blood pressure x smoking status (ever vs never) interaction (2df test)	5e-12
GCST006193_78	Diastolic blood pressure x smoking status (current vs non-current) interaction (2df test)	5e-12
GCST010245_21	LDL cholesterol levels	6e-12
GCST006192_55	Systolic blood pressure x smoking status (ever vs never) interaction (2df test)	5e-11
GCST006195_32	Systolic blood pressure x smoking status (current vs non-current) interaction (2df test)	8e-11
GCST006021_43	Systolic blood pressure	1e-10
GCST006172_41	Mean arterial pressure x alcohol consumption (light vs heavy) interaction (2df test)	1e-10
GCST006167_76	Mean arterial pressure x alcohol consumption interaction (2df test)	2e-10
GCST007099_34	Systolic blood pressure	2e-10
GCST010321_127	PR interval	2e-10
GCST008363_93	Offspring birth weight	5e-10

EFO canonical traits (from GWAS)

19 canonical traits:

EFO ID	Trait name
EFO:0006340	mean arterial pressure
EFO:0004344	birth weight
EFO:0006336	diastolic blood pressure
EFO:0006335	systolic blood pressure
EFO:0004329	alcohol drinking
EFO:0006527	smoking status measurement
EFO:0004530	triglyceride measurement
EFO:0004574	total cholesterol measurement
EFO:0004611	low density lipoprotein cholesterol measurement
EFO:0004612	high density lipoprotein cholesterol measurement
EFO:0009928	Diuretic use measurement
EFO:0009931	Agents acting on the renin-angiotensin system use measurement
EFO:0005939	parental genotype effect measurement
EFO:0004614	apolipoprotein A 1 measurement
EFO:0004615	apolipoprotein B measurement
EFO:0004462	PR interval
EFO:0004327	electrocardiography
EFO:0007984	platelet component distribution width
EFO:0004736	aspartate aminotransferase measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (5): CHEMBL2094118 (PROTEIN FAMILY), CHEMBL2096974 (SELECTIVITY GROUP), CHEMBL2097169 (SELECTIVITY GROUP), CHEMBL213 (SINGLE PROTEIN), CHEMBL2331074 (PROTEIN FAMILY)

Drugs by curated mechanism of action (ChEMBL)

Drugs whose curated ChEMBL mechanism of action targets the ADRB1 protein itself — single-protein targets only (drugs acting on a protein family or complex that merely includes it are excluded). Includes antibodies and oligonucleotides that bioactivity screening does not capture.

28 curated-mechanism drugs:

Drug	Modality	Max phase
ACEBUTOLOL HYDROCHLORIDE	Small molecule	4
ATENOLOL	Small molecule	4
BETAXOLOL HYDROCHLORIDE	Small molecule	4
BISOPROLOL FUMARATE	Small molecule	4
CELIPROLOL	Small molecule	4
DOBUTAMINE HYDROCHLORIDE	Small molecule	4
DOPAMINE HYDROCHLORIDE	Small molecule	4
ESMOLOL HYDROCHLORIDE	Small molecule	4
FOSLEVODOPA	Small molecule	4
LANDIOLOL	Small molecule	4
LEVOBETAXOLOL HYDROCHLORIDE	Small molecule	4
LEVOBUNOLOL HYDROCHLORIDE	Small molecule	4
METIPRANOLOL HYDROCHLORIDE	Small molecule	4
METOPROLOL FUMARATE	Small molecule	4
NADOLOL	Small molecule	4
NEBIVOLOL HYDROCHLORIDE	Small molecule	4
OXPRENOLOL HYDROCHLORIDE	Small molecule	4
PENBUTOLOL SULFATE	Small molecule	4
PINDOLOL	Small molecule	4
PRACTOLOL	Small molecule	4
PRONETALOL	Small molecule	4
PROPAFENONE HYDROCHLORIDE	Small molecule	4
PROPRANOLOL HYDROCHLORIDE	Small molecule	4
SOTALOL HYDROCHLORIDE	Small molecule	4
TIMOLOL	Small molecule	4
BUCINDOLOL	Small molecule	2
LY377604	Small molecule	2
XAMOTEROL	Small molecule	2

Drugs acting on a complex or family that includes this protein

Curated ChEMBL mechanism-of-action drugs whose target is a protein complex or family of ≤10 members that includes ADRB1 — the drug acts on the assembly or class, not necessarily on this subunit alone.

12 drugs via a complex or family:

Drug	Target (ChEMBL)	Members	Max phase
CARTEOLOL HYDROCHLORIDE	Adrenergic receptor beta	3	4
CARVEDILOL	Adrenergic receptor beta	3	4
DILEVALOL HYDROCHLORIDE	Adrenergic receptor beta	3	4
DIPIVEFRIN HYDROCHLORIDE	Adrenergic receptor	9	4
DROXIDOPA	Adrenergic receptor	9	4
EPHEDRINE SULFATE	Adrenergic receptor	9	4
EPINEPHRINE	Adrenergic receptor	9	4
HYDROXYAMPHETAMINE HYDROBROMIDE	Adrenergic receptor	9	4
ISOPROTERENOL SULFATE	Adrenergic receptor beta	3	4
LABETALOL HYDROCHLORIDE	Adrenergic receptor	9	4
MEPHENTERMINE SULFATE	Adrenergic receptor	9	4
NOREPINEPHRINE BITARTRATE	Adrenergic receptor	9	4

Molecules with ChEMBL bioactivity

Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 423,338 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

showing 60 of 154 molecules by phase:

Molecule	Name	Phase	Patents
CHEMBL642	ACEBUTOLOL	4	21,014
CHEMBL24	ATENOLOL	4	49,046
CHEMBL423	BETAXOLOL	4	23,977
CHEMBL1691	BETAXOLOL HYDROCHLORIDE	4	6,498
CHEMBL645	BISOPROLOL	4	20,610
CHEMBL27810	CELIPROLOL	4	9,214
CHEMBL926	DOBUTAMINE	4	17,217
CHEMBL768	ESMOLOL	4	15,192
CHEMBL1201237	LEVOBUNOLOL	4	10,688
CHEMBL13	METOPROLOL	4	44,694
CHEMBL521606	NADOLOL	4	74
CHEMBL434394	NEBIVOLOL	4	9,764
CHEMBL546	OXPRENOLOL	4	14,901
CHEMBL500	PINDOLOL	4	28,862
CHEMBL6995	PRACTOLOL	4	4,278
CHEMBL631	PROPAFENONE	4	12,817
CHEMBL27	PROPRANOLOL	4	86,565
CHEMBL1671	PROPRANOLOL HYDROCHLORIDE	4	22,003
CHEMBL471	SOTALOL	4	21,915
CHEMBL1700	SOTALOL HYDROCHLORIDE	4	4,009
CHEMBL499	TIMOLOL	4
CHEMBL714	ALBUTEROL	4
CHEMBL633	AMIODARONE	4
CHEMBL629	AMITRIPTYLINE	4
CHEMBL1363	ARFORMOTEROL	4
CHEMBL1112	ARIPIPRAZOLE	4
CHEMBL296419	ASTEMIZOLE	4
CHEMBL639	AZELASTINE	4
CHEMBL400599	BENFLUOREX	4
CHEMBL297302	BENPERIDOL	4
CHEMBL388590	BENZBROMARONE	4
CHEMBL1008	BEPRIDIL	4
CHEMBL2105760	BREXPIPRAZOLE	4
CHEMBL493	BROMOCRIPTINE	4
CHEMBL1014	CANDESARTAN CILEXETIL	4
CHEMBL2024517	CARIPRAZINE HYDROCHLORIDE	4
CHEMBL839	CARTEOLOL	4
CHEMBL723	CARVEDILOL	4
CHEMBL790	CHLORHEXIDINE	4
CHEMBL908	CHLORPROTHIXENE	4
CHEMBL1201284	CINACALCET	4
CHEMBL1626	CLEMASTINE	4
CHEMBL415	CLOMIPRAMINE	4
CHEMBL104	CLOTRIMAZOLE	4
CHEMBL485	CODEINE	4
CHEMBL1346	DARIFENACIN	4
CHEMBL178	DAUNORUBICIN	4
CHEMBL1201129	DECITABINE	4
CHEMBL411	DIETHYLSTILBESTROL	4
CHEMBL219916	DOMPERIDONE	4
CHEMBL1175	DULOXETINE	4
CHEMBL305660	EBASTINE	4
CHEMBL808	ECONAZOLE	4
CHEMBL223228	EFAVIRENZ	4
CHEMBL56337	EPALRESTAT	4
CHEMBL679	EPINEPHRINE	4
CHEMBL442	ERGOTAMINE	4
CHEMBL32800	FENOTEROL	4
CHEMBL46516	FLUSPIRILENE	4
CHEMBL1256786	FORMOTEROL	4

PharmGKB: 1 entry (CPIC guideline: yes)

PharmGKB clinical annotations

14 annotations by evidence level (1 strongest → 4):

Variant	Association	Level	Drugs	Phenotypes
rs1801252	Efficacy	3	timolol
rs1801252	Toxicity	3	Beta Blocking Agents	Major Adverse Cardiac Events (MACE)
rs1801252	Efficacy	3	metoprolol	Hypertension
rs1801252	Efficacy	3	carvedilol
rs1801253	Toxicity	3	muraglitazar	Diabetes Mellitus;Edema;Hyperlipidemias
rs1801253	Efficacy	3	dobutamine
rs1801253	Dosage	3	catecholamines	Coronary Artery Disease
rs1801253	Efficacy	3	metoprolol
rs1801253	Dosage	3	carvedilol	Heart Failure
rs1801253	Efficacy	3	bucindolol	Heart Failure
rs1801253	Efficacy	3	Ace Inhibitors;Plain;Angiotensin II Antagonists;Beta Blocking Agents;digoxin;diuretics;spironolactone	Heart Failure
rs1801253	Efficacy	4	Beta Blocking Agents	Cardiomyopathy;Dilated;Heart Failure
rs1801253	Efficacy	4	atenolol	Atrial Fibrillation;Essential hypertension;Tachycardia
rs1801253	Efficacy	4	carvedilol	Heart Failure

PharmGKB variants

2 variants:

Variant	Genes	Level	Score	#Clin annots	Drugs
rs1801252	ADRB1	3	3.50	4	carvedilol;timolol;Beta Blocking Agents;metoprolol
rs1801253	ADRB1	3	7.00	10	muraglitazar;carvedilol;bucindolol;dobutamine;catecholamines;Ace Inhibitors;Plain;Angiotensin II Antagonists;Beta Blocking Agents;digoxin;diuretics;spironolactone;Beta Blocking Agents;metoprolol;atenolol

PharmGKB variant annotations

Per-publication pharmacogenomic findings for this gene (significant associations).

showing 34 of 35 published findings:

Variant	Drug(s)	Category	Finding	PMID
rs1801252	Beta Blocking Agents, metoprolol	Efficacy	Genotypes AG + GG are associated with increased improvement in left ventricular(LV) remodeling when treated with Beta Blocking Agents and metoprolol in people with Heart Failure as compared to genotype AA.	PMID:15864115
rs1801253	catecholamines	Dosage	Genotype CC is associated with decreased dose of catecholamines in people with Coronary Artery Disease as compared to genotypes CG + GG.	PMID:17541557
rs1801253	metoprolol	Efficacy	Genotype CC is associated with increased response to metoprolol in healthy individuals as compared to genotypes CG + GG.	PMID:21311897
rs1801252	timolol	Other	Genotype AA is associated with increased systolic (SAP) and diastolic (DAP) arterial pressure responses to timolol when exposed to timolol in healthy individuals as compared to genotypes AG + GG.	PMID:16315032
rs1801253	dobutamine	Efficacy	Genotype CC is associated with increased response to dobutamine in healthy individuals as compared to genotype GG.	PMID:26313487
rs1801253	Beta Blocking Agents, flecainide	Efficacy	Allele G is associated with decreased response to Beta Blocking Agents and flecainide in people with Tachycardia as compared to allele C.	PMID:27500822
rs1801252	Beta Blocking Agents	Efficacy	Genotypes AG + GG are associated with increased risk of major adverse cardiac events (mace) when treated with Beta Blocking Agents as compared to genotype AA.	PMID:28351962
rs1801253	atenolol	Efficacy	Allele C is associated with increased response to atenolol in healthy individuals as compared to allele G.	PMID:18794726
rs1801252	carvedilol	Efficacy	Allele G is associated with increased response to carvedilol in healthy individuals as compared to allele A.	PMID:21599570
rs1801253	carvedilol	Efficacy	Allele C is associated with increased response to carvedilol in healthy individuals as compared to allele G.	PMID:21599570
rs1801253	Beta Blocking Agents	Efficacy	Allele C is associated with increased response to Beta Blocking Agents in children with Cardiomyopathy, Dilated as compared to allele G.	PMID:25406899
rs1801253	Beta Blocking Agents	Other	Genotype CC is associated with decreased risk of Death in people not taking Beta Blocking Agents in people with Heart Failure as compared to genotypes CG + GG.	PMID:19628119
rs1801253	Antihypertensives, Beta Blocking Agents, diuretics	Efficacy	Genotype CC is associated with increased likelihood of Stroke when treated with Antihypertensives, Beta Blocking Agents or diuretics in people with Hypertension as compared to genotypes CG + GG.	PMID:38298191
rs1801252	Antihypertensives	Efficacy	Genotype GG is associated with increased likelihood of resistant hypertension when treated with Antihypertensives in people with Hypertension as compared to genotypes AA + AG.	PMID:39063918
rs1801253	sufentanil	Efficacy	Genotype GG is associated with decreased severity of Pain, Postoperative when treated with sufentanil in children with Surgical procedure as compared to genotype CC.	PMID:40331998
rs1801253	apraclonidine, atenolol, propranolol	Efficacy	Genotype CC is associated with increased clinical benefit to apraclonidine, atenolol or propranolol in people with Hypertension.	PMID:41968188
rs1801252	verapamil	Efficacy	Genotypes AA + AG are associated with increased risk of Death when treated with verapamil in people with Coronary Artery Disease as compared to genotype GG.	PMID:18615004
rs1801253	metoprolol	Efficacy	Allele C is associated with increased response to metoprolol in people with Hypertension as compared to allele G.	PMID:12844134
rs1801253	atenolol	Efficacy	Genotype CC is associated with increased reduction in blood pressure when treated with atenolol in healthy individuals as compared to genotype GG.	PMID:12709726
rs1801253	atenolol, carvedilol, diltiazem, metoprolol, verapamil	Efficacy	Genotypes CG + GG are associated with increased response to atenolol, carvedilol, diltiazem, metoprolol or verapamil in people with Atrial Fibrillation as compared to genotype CC.	PMID:22192668
rs1801253	bucindolol	Efficacy	Genotype CC is associated with increased response when treated with bucindolol in people with Heart Failure as compared to genotype GG.	PMID:16844790
rs1801253	metoprolol	Efficacy	Genotype CC is associated with increased improvement in left ventricular(LV) remodeling and greater increase in LVEF (left ventricular ejection fraction) when treated with metoprolol in people with Heart Failure as compared to genotypes CG + GG.	PMID:15864115
rs1801253	carvedilol	Efficacy	Genotype CC is associated with significantly greater improvement in left ventricular ejection fraction (LVEF) when treated with carvedilol in people with Heart Failure as compared to genotypes CG + GG.	PMID:18075464
rs1801253	carvedilol	Efficacy	Genotype CC is associated with increased improvement in left ventricular function (LVEF) when treated with carvedilol in people with Heart Failure as compared to genotype GG.	PMID:14502278
rs1801253	carvedilol	Efficacy	Genotype CC is associated with decreased response (heart-rate lowering) when treated with carvedilol in people with Heart Failure as compared to genotypes CG + GG.	PMID:22617224
rs1801252	metoprolol	Efficacy	Genotype AA is associated with increased response to metoprolol in people with Hypertension as compared to genotype AG.	PMID:12844134
rs1801252	metoprolol	Efficacy	Genotype AA is associated with increased response to metoprolol in people with Essential hypertension as compared to genotype AG.	PMID:16815314
rs1801253	metoprolol	Efficacy	Genotype CC is associated with increased response to metoprolol in people with Essential hypertension as compared to genotypes CG + GG.	PMID:16815314
rs1801253	metoprolol	Efficacy	Genotype CC is associated with increased response to metoprolol in people with Heart Failure as compared to genotypes CG + GG.	PMID:17496726
rs1801253	verapamil	Efficacy	Genotypes CC + CG are associated with increased risk of Death when treated with verapamil in people with Coronary Artery Disease as compared to genotype GG.	PMID:18615004
rs1801253	dobutamine	Efficacy	Genotype CC is associated with increased response to dobutamine in healthy individuals as compared to genotypes CG + GG.	PMID:15564877
rs1801253	carvedilol	Dosage	Genotype GG is associated with increased dose of carvedilol in people with Heart Failure as compared to genotype CC.	PMID:20643254
rs1801253	bucindolol	Efficacy	Genotype CC is associated with increased response to bucindolol in people with Heart Failure as compared to genotypes CG + GG.	PMID:23071495
rs1801253	“““Ace Inhibitors, Plain””, ““Angiotensin II Antagonists””, ““Beta Blocking Agents””, ““digoxin””, ““diuretics””, ““spironolactone”””	Other	Genotype GG is associated with decreased risk of Emergencies when treated with Ace Inhibitors, Plain, Angiotensin II Antagonists, Beta Blocking Agents, digoxin, diuretics or spironolactone in people with Heart Failure as compared to genotypes CC + CG.	PMID:22543981

PharmGKB dosing guidelines

CPIC / DPWG genotype-guided dosing for this gene (drug × pharmacogene).

1 dosing guidelines:

Guideline	Source	Drug	Dosing?	Recommendation?
Annotation of CPIC Guideline for acebutolol, atenolol, betaxolol, biso	CPIC	acebutolol;atenolol;betaxolol;bisoprolol;carvedilol;esmolol;labetalol;metoprolol;nadolol;nebivolol;pindolol;propranolol;sotalol

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: gpcr — Adrenoceptors

Most potent curated ligand interactions (66 total), top 25:

Ligand	Action	Affinity	Parameter
[125I]ICYP	Partial agonist	10.8	pKd
7-methylcyanopindolol	Antagonist	10.4	pKd
cyanopindolol	Partial agonist	10.3	pEC50
carazolol	Partial agonist	10.0	pEC50
CGP20712A	Antagonist	9.6	pA2
bucindolol	Partial agonist	9.5	pEC50
3HCGP12177	Partial agonist	9.5	pKd
[3H]CGP12177	Partial agonist	9.5	pKd
bupranolol	Antagonist	9.4	pKi
nebivolol	Antagonist	9.4	pKi
pindolol	Partial agonist	9.3	pKi
carvedilol	Partial agonist	9.2	pEC50
CGP12177	Partial agonist	9.1	pEC50
BI-167107	Partial agonist	9.0	pEC50
NDD-825	Antagonist	9.0	pKi
timolol	Antagonist	9.0	pA2
ICI89406	Partial agonist	8.9	pKi
betaxolol	Antagonist	8.9	pA2
bisoprolol	Antagonist	8.8	pA2
carteolol	Partial agonist	8.7	pKi
xamoterol	Partial agonist	8.6	pEC50
(-)-propranolol	Antagonist	8.6	pA2
NDD-713	Antagonist	8.5	pKi
LK 204-545	Partial agonist	8.5	pKi
NIP	Antagonist	8.4	pKi

Binding affinities (BindingDB)

1463 measured of 1738 human assays (1811 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
[O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin-1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione	EC50	0.01 nM
2-(8-Bromo-2,3,6,7-tetrahydro-benzo[1,2-b;4,5-b’]difuran-4-yl)-ethylamine	EC50	0.029 nM
2-((1-(3-(9H-carbazol-4-yloxy)-2-hydroxypropyl)piperidin-4-yl)methyl)-5-methoxy-1H-benzo[de]isoquinoline-1,3(2H)-dione	KI	0.1 nM
(R)-1-((R)-3-Chloro-phenyl)-2-[2-(7-methoxy-1H-indol-3-yl)-1-methyl-ethylamino]-ethanol	EC50	0.13 nM
(R)-1-(3-Chloro-phenyl)-2-[2-(7-methoxy-1H-indol-3-yl)-1-methyl-ethylamino]-ethanol	EC50	0.13 nM
3,3-diethyl-1-[(4R,7R)-6-methyl-6,11-diazatetracyclo[7.6.1.0^{2,7}.0^{12,16}]hexadeca-1(15),2,9,12(16),13-pentaen-4-yl]urea	KI	0.15 nM
CAS_163091	KI	0.21 nM
4-(3-tert-Butylamino-2-hydroxy-propoxy)-1,3-dihydro-benzoimidazol-2-one	KI	0.25 nM
SB-649915	KI	0.316 nM
1-(2-{4-[5-chloro-1-(4-fluorophenyl)-1H-indol-3-yl]piperidin-1-yl}ethyl)imidazolidin-2-one	KI	0.38 nM
(S)-1-(isopropylamino)-3-(m-tolyloxy)propan-2-ol ((2S)-toliprolol)	KD	0.38 nM
CHEMBL238520	KI	0.398 nM
ss-2c	KI	0.4 nM
3-[[5-[4-(tert-butylsulfamoyl)naphthalen-1-yl]-4-(cyclohexylmethyl)-1,3-thiazole-2-carbonyl]amino]cyclobutane-1-carboxylic acid	IC50	0.43 nM	US-10301272: Carboxamide or sulfonamide substituted thiazoles and related derivatives as modulators for the orphan nuclear receptor ROR[γ]
(2,4-Dimethyl-azetidin-1-yl)-(7-methyl-4,6,6a,7,8,9-hexahydro-indolo[4,3-fg]quinolin-9-yl)-methanone	KI	0.45 nM
2-(4-Ethylsulfanyl-2,5-dimethoxy-phenyl)-1-methyl-ethylamine	EC50	0.489 nM
3-(2-hydroxy-3-(1-(5-phenylthieno[2,3-d]pyrimidin-4-yl)piperidin-4-ylamino)propoxy)phenol	EC50	0.57 nM
5-hydroxy-8-(1-hydroxy-2-(2-methyl-1-o-tolylpropan-2-ylamino)ethyl)-2H-benzo[b][1,4]oxazin-3(4H)-one	EC50	0.6 nM
CHEMBL4868585	EC50	0.603 nM
4-[3-(tert-butylamino)-2-hydroxypropoxy]-2,3-dihydro-1H-1,3-benzodiazol-2-one hydrochloride	KD	0.62 nM
roxindole	IC50	0.8 nM
CHEMBL3323658	KI	0.8 nM
5-hydroxy-8-(1-hydroxy-2-(2-methyl-1-phenylpropan-2-ylamino)ethyl)-2H-benzo[b][1,4]oxazin-3(4H)-one	EC50	0.8 nM
ICI 89,406	EC50	0.813 nM
CHEMBL4862449	EC50	0.851 nM
CHEMBL369346	EC50	0.9 nM
5-hydroxy-8-(1-hydroxy-2-(1-(4-hydroxyphenyl)-2-methylpropan-2-ylamino)ethyl)-2H-benzo[b][1,4]oxazin-3(4H)-one	EC50	0.9 nM
7-((R)-2-((1R,2R)-2-(benzyloxy)cyclopentylamino)-1-hydroxyethyl)-4-hydroxybenzo[d]thiazol-2(3H)-one	KI	0.9 nM
CHEMBL4092412	KD	0.977 nM
1-(9H-carbazol-4-yloxy)-3-(4-(pyridin-3-ylmethyl)piperidin-1-yl)propan-2-ol	KI	1 nM
1-(3-Thiophen-2-yl-phenyl)-ethanone, O-(phenylaminocarbonyl)oxime	IC50	1 nM
(4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[7.6.1.0^{2,7}.0^{12,16}]hexadeca-1(16),2,9,12,14-pentaene-4-carboxamide	KI	1.09 nM
(2,4-Dimethyl-azetidin-1-yl)-(7-methyl-4,6,6a,7,8,9-hexahydro-indolo[4,3-fg]quinolin-9-yl)-methanone	KI	1.1 nM
Thiophene-2-sulfonic acid 3-(2-{(R)-(R)-2-hydroxy-2-[3-(thiophene-2-sulfonylamino)-phenyl]-ethylamino}-propyl)-1H-indol-7-yl ester	EC50	1.2 nM
4-Amino-N-(1-aza-tricyclo[3.3.1.0*3,7*]non-4-yl)-5-chloro-2-methoxy-benzamide; hydrochloride	KI	1.2 nM
CHEMBL4645927	EC50	1.2 nM
CHEMBL183283	EC50	1.3 nM
Pyridine-3-sulfonic acid 3-(2-{(R)-(R)-2-hydroxy-2-[3-(thiophene-2-sulfonylamino)-phenyl]-ethylamino}-propyl)-1H-indol-7-yl ester	EC50	1.3 nM
(S)-1-(1H-indol-4-yloxy)-3-(cyclohexylamino)propan-2-ol	KI	1.3 nM
4-Chloro-benzene-1,3-disulfonic acid 3-amide 1-({2-[2-hydroxy-3-(2-oxo-1,2,3,4-tetrahydro-quinolin-5-yloxy)-propylamino]-ethyl}-amide)	KI	1.4 nM
4-hydroxy-7-((R)-1-hydroxy-2-((R)-1-(naphthalen-2-yl)ethylamino)ethyl)benzo[d]thiazol-2(3H)-one	KI	1.4 nM
CHEMBL272234	EC50	1.4 nM
CHEMBL4635163	EC50	1.4 nM
4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol	EC50	1.5 nM
7-((R)-2-((R)-1-cyclohexylethylamino)-1-hydroxyethyl)-4-hydroxybenzo[d]thiazol-2(3H)-one	KI	1.5 nM
CHEMBL4854569	EC50	1.5 nM
CHEMBL3298987	EC50	1.6 nM
5-[2-(4-Benzo[d]isothiazol-3-yl-piperazin-1-yl)-ethyl]-6-chloro-1,3-dihydro-indol-2-one	KI	1.6 nM
CHEMBL393539	KI	1.6 nM
(R)-7-(2-(2-(4-chlorophenylthio)ethylamino)-1-hydroxyethyl)-4-hydroxybenzo[d]thiazol-2(3H)-one	KI	1.7 nM

ChEMBL bioactivities

2185 potent at pChembl≥5 of 2377 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.64	Ki	0.023	nM	CHEMBL2012522
10.40	IC50	0.04	nM	CHEMBL2011218
10.30	IC50	0.05	nM	CHEMBL2011226
10.30	IC50	0.05	nM	CHEMBL2011227
10.12	Kd	0.075	nM	CHEMBL4860528
10.12	Kd	0.075	nM	CHEMBL5207281
10.12	Kd	0.075	nM	CHEMBL5206565
10.12	Kd	0.075	nM	CHEMBL5201074
10.10	IC50	0.08	nM	CHEMBL2011216
10.08	EC50	0.084	nM	ISOPROTERENOL
10.00	IC50	0.1	nM	CHEMBL2011215
10.00	IC50	0.1	nM	CHEMBL2011224
10.00	Ki	0.1	nM	CHEMBL1084707
9.99	Ki	0.103	nM	CARVEDILOL
9.98	EC50	0.1047	nM	CHEMBL5574456
9.96	IC50	0.11	nM	CHEMBL2011213
9.92	EC50	0.1202	nM	CHEMBL5572781
9.89	EC50	0.13	nM	CHEMBL416012
9.89	EC50	0.1288	nM	CHEMBL5575873
9.89	EC50	0.13	nM	CHEMBL26183
9.86	EC50	0.138	nM	CHEMBL5567636
9.85	IC50	0.14	nM	CHEMBL2011235
9.82	EC50	0.1514	nM	CHEMBL5563982
9.77	EC50	0.1698	nM	CHEMBL5550060
9.75	EC50	0.1778	nM	CHEMBL5565088
9.75	IC50	0.178	nM	CARVEDILOL
9.74	Ki	0.182	nM	AROTINOLOL
9.70	IC50	0.2	nM	CHEMBL2011214
9.63	EC50	0.2344	nM	CHEMBL5573953
9.61	EC50	0.2455	nM	CHEMBL5569415
9.61	EC50	0.2455	nM	CHEMBL5595588
9.60	IC50	0.25	nM	CHEMBL2011217
9.60	Ki	0.25	nM	CHEMBL36060
9.59	EC50	0.257	nM	CHEMBL5562809
9.52	IC50	0.3	nM	CHEMBL2011225
9.51	EC50	0.309	nM	CHEMBL5574770
9.49	EC50	0.3236	nM	CHEMBL5570271
9.48	Kd	0.3311	nM	CHEMBL3392321
9.48	Kd	0.3311	nM	CGP-20712A
9.46	IC50	0.35	nM	CHEMBL2011228
9.42	Kd	0.38	nM	(S)-TOLIPROLOL
9.40	EC50	0.3981	nM	CHEMBL5564275
9.36	Ki	0.434	nM	CHEMBL117405
9.29	EC50	0.5129	nM	CHEMBL5592612
9.29	EC50	0.5129	nM	CHEMBL5568704
9.28	Ki	0.52	nM	PINDOLOL
9.27	Ki	0.532	nM	PINDOLOL
9.24	EC50	0.57	nM	CHEMBL1257913
9.22	EC50	0.6026	nM	CHEMBL4868585
9.22	EC50	0.6	nM	CHEMBL579394

PubChem BioAssay actives

2074 with measured affinity, of 5884 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
butanedioic acid;6-[4-[2-[[(2S)-3-(9H-carbazol-4-yloxy)-2-hydroxypropyl]amino]-2-methylpropyl]phenoxy]pyridine-3-carboxamide	652453: Displacement of [125I]Iodocyanopindolol from human adrenergic beta1 receptor expressed in insect sf9 cells by scintillation counting	ki	<0.0001	uM
1-[2-[[(2S)-3-(2-cyanophenoxy)-2-hydroxypropyl]amino]ethyl]-3-[3-(2-fluoroethoxy)phenyl]urea	652407: Displacement of 3H-CGP-12177 from adrenergic beta1 receptor by cell based assay	ic50	<0.0001	uM
(1R)-1-(3-chlorophenyl)-2-[[(2R)-1-(7-methoxy-1H-indol-3-yl)propan-2-yl]amino]ethanol	40110: Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR	ec50	0.0001	uM
1-[2-[[(2S)-3-(2-cyanophenoxy)-2-hydroxypropyl]amino]ethyl]-3-(4-methoxyphenyl)urea	652407: Displacement of 3H-CGP-12177 from adrenergic beta1 receptor by cell based assay	ic50	0.0001	uM
1-[2-[[(2S)-3-(2-cyanophenoxy)-2-hydroxypropyl]amino]ethyl]-3-[4-(2-fluoroethoxy)phenyl]urea	652407: Displacement of 3H-CGP-12177 from adrenergic beta1 receptor by cell based assay	ic50	0.0001	uM
1-[N’-[3-(2-amino-4-methyl-1,3-thiazol-5-yl)propyl]carbamimidoyl]-3-pentylurea	1895233: Displacement of [3H]CGP12177 from human beta-1 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis	kd	0.0001	uM
1-[(1R)-1-phenylethyl]-3-[N’-[3-(1H-1,2,4-triazol-5-yl)propyl]carbamimidoyl]urea;dihydrochloride	1895233: Displacement of [3H]CGP12177 from human beta-1 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis	kd	0.0001	uM
1-[N’-[3-(5-amino-1,3,4-thiadiazol-2-yl)propyl]carbamimidoyl]-3-pentylurea;bis(2,2,2-trifluoroacetic acid)	1895233: Displacement of [3H]CGP12177 from human beta-1 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis	kd	0.0001	uM
1-[N’-[3-(5-amino-1,3,4-thiadiazol-2-yl)propyl]carbamimidoyl]-3-benzylurea;bis(2,2,2-trifluoroacetic acid)	1895233: Displacement of [3H]CGP12177 from human beta-1 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis	kd	0.0001	uM
methyl (2R)-2-amino-3-[4-[(2S)-3-(2,3-dihydro-1,4-benzodioxin-3-ylmethylamino)-2-hydroxypropoxy]phenyl]propanoate	2002280: Antagonist activity at human beta1-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as inhibition of fenoterol-induced CRE-SPAP production by measuring rightward shift of the fenoterol concentration response curve measured after 5 hrs incubation	kd	0.0001	uM
5-hydroxy-8-[1-hydroxy-2-[3-(3-hydroxyphenyl)propylamino]ethyl]-4H-1,4-benzoxazin-3-one;hydrochloride	2089646: Agonist activity at human beta1 adrenoceptor expressed in HEK293 cells assessed as induction of accumulation of cAMP by HTRF assay	ec50	0.0001	uM
5-hydroxy-8-[1-hydroxy-2-[3-(4-hydroxyphenyl)propylamino]ethyl]-4H-1,4-benzoxazin-3-one;hydrochloride	2089646: Agonist activity at human beta1 adrenoceptor expressed in HEK293 cells assessed as induction of accumulation of cAMP by HTRF assay	ec50	0.0001	uM
8-[2-[3-(3,5-difluorophenyl)propylamino]-1-hydroxyethyl]-5-hydroxy-4H-1,4-benzoxazin-3-one;hydrochloride	2089646: Agonist activity at human beta1 adrenoceptor expressed in HEK293 cells assessed as induction of accumulation of cAMP by HTRF assay	ec50	0.0001	uM
5-hydroxy-8-[1-hydroxy-2-[3-(2-hydroxyphenyl)propylamino]ethyl]-4H-1,4-benzoxazin-3-one;hydrochloride	2089646: Agonist activity at human beta1 adrenoceptor expressed in HEK293 cells assessed as induction of accumulation of cAMP by HTRF assay	ec50	0.0001	uM
Isoproterenol	246460: Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor	ec50	0.0001	uM
2-[[1-[3-(9H-carbazol-4-yloxy)-2-hydroxypropyl]piperidin-4-yl]methyl]-5-methoxybenzo[de]isoquinoline-1,3-dione	484592: Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cells	ki	0.0001	uM
N-[2-[[(2S)-3-(2-cyanophenoxy)-2-hydroxypropyl]amino]ethyl]-2-(4-fluorophenyl)acetamide	652407: Displacement of 3H-CGP-12177 from adrenergic beta1 receptor by cell based assay	ic50	0.0001	uM
1-[2-[[(2S)-3-(2-cyanophenoxy)-2-hydroxypropyl]amino]ethyl]-3-[6-(2-fluoroethoxy)-3-pyridinyl]urea	652407: Displacement of 3H-CGP-12177 from adrenergic beta1 receptor by cell based assay	ic50	0.0001	uM
1-[2-[[(2S)-3-(2-cyanophenoxy)-2-hydroxypropyl]amino]ethyl]-3-(6-iodo-3-pyridinyl)urea	652407: Displacement of 3H-CGP-12177 from adrenergic beta1 receptor by cell based assay	ic50	0.0001	uM
1-[2-[[(2S)-3-(2-cyanophenoxy)-2-hydroxypropyl]amino]ethyl]-3-(4-fluorophenyl)urea	652407: Displacement of 3H-CGP-12177 from adrenergic beta1 receptor by cell based assay	ic50	0.0001	uM
1-(6-bromo-3-pyridinyl)-3-[2-[[(2S)-3-(2-cyanophenoxy)-2-hydroxypropyl]amino]ethyl]urea	652407: Displacement of 3H-CGP-12177 from adrenergic beta1 receptor by cell based assay	ic50	0.0001	uM
(1R)-1-(3-chlorophenyl)-2-[1-(7-methoxy-1H-indol-3-yl)propan-2-ylamino]ethanol	1095332: Agonist activity at Homo sapiens (human) beta1 adrenoreceptor	ec50	0.0001	uM
5-hydroxy-8-[1-hydroxy-2-[3-(3-methylphenyl)propylamino]ethyl]-4H-1,4-benzoxazin-3-one;hydrochloride	2089646: Agonist activity at human beta1 adrenoceptor expressed in HEK293 cells assessed as induction of accumulation of cAMP by HTRF assay	ec50	0.0002	uM
8-[2-[3-(3-fluorophenyl)propylamino]-1-hydroxyethyl]-5-hydroxy-4H-1,4-benzoxazin-3-one;hydrochloride	2089646: Agonist activity at human beta1 adrenoceptor expressed in HEK293 cells assessed as induction of accumulation of cAMP by HTRF assay	ec50	0.0002	uM
8-[2-[3-(4-chlorophenyl)propylamino]-1-hydroxyethyl]-5-hydroxy-4H-1,4-benzoxazin-3-one;hydrochloride	2089646: Agonist activity at human beta1 adrenoceptor expressed in HEK293 cells assessed as induction of accumulation of cAMP by HTRF assay	ec50	0.0002	uM
8-[2-[3-(4-fluorophenyl)propylamino]-1-hydroxyethyl]-5-hydroxy-4H-1,4-benzoxazin-3-one;hydrochloride	2089646: Agonist activity at human beta1 adrenoceptor expressed in HEK293 cells assessed as induction of accumulation of cAMP by HTRF assay	ec50	0.0002	uM
5-hydroxy-8-[1-hydroxy-2-[3-(2-methoxyphenyl)propylamino]ethyl]-4H-1,4-benzoxazin-3-one;hydrochloride	2089646: Agonist activity at human beta1 adrenoceptor expressed in HEK293 cells assessed as induction of accumulation of cAMP by HTRF assay	ec50	0.0002	uM
8-[2-[3-(2-fluorophenyl)propylamino]-1-hydroxyethyl]-5-hydroxy-4H-1,4-benzoxazin-3-one;hydrochloride	2089646: Agonist activity at human beta1 adrenoceptor expressed in HEK293 cells assessed as induction of accumulation of cAMP by HTRF assay	ec50	0.0002	uM
5-[2-[3-(tert-butylamino)-2-hydroxypropyl]sulfanyl-1,3-thiazol-4-yl]thiophene-2-carboxamide	2033266: Inhibition of beta-1 adrenoceptor (unknown origin)	ki	0.0002	uM
1-[2-[[(2S)-3-(2-cyanophenoxy)-2-hydroxypropyl]amino]ethyl]-3-(2-fluorophenyl)urea	652407: Displacement of 3H-CGP-12177 from adrenergic beta1 receptor by cell based assay	ic50	0.0002	uM
1-[2-[[3-(2-cyanophenoxy)-2-hydroxypropyl]amino]ethyl]-3-phenylurea;hydrate	739711: Antagonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs	kd	0.0003	uM
5-hydroxy-8-[1-hydroxy-2-(3-phenylpropylamino)ethyl]-4H-1,4-benzoxazin-3-one;hydrochloride	2089646: Agonist activity at human beta1 adrenoceptor expressed in HEK293 cells assessed as induction of accumulation of cAMP by HTRF assay	ec50	0.0003	uM
5-hydroxy-8-[1-hydroxy-2-(4-phenylbutylamino)ethyl]-4H-1,4-benzoxazin-3-one;hydrochloride	2089646: Agonist activity at human beta1 adrenoceptor expressed in HEK293 cells assessed as induction of accumulation of cAMP by HTRF assay	ec50	0.0003	uM
5-hydroxy-8-[1-hydroxy-2-[3-(2-methylphenyl)propylamino]ethyl]-4H-1,4-benzoxazin-3-one;hydrochloride	2089646: Agonist activity at human beta1 adrenoceptor expressed in HEK293 cells assessed as induction of accumulation of cAMP by HTRF assay	ec50	0.0003	uM
2-hydroxy-5-[2-[[2-hydroxy-3-[4-[1-methyl-4-(trifluoromethyl)imidazol-2-yl]phenoxy]propyl]amino]ethoxy]benzamide	739711: Antagonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs	kd	0.0003	uM
4-[(2S)-3-(tert-butylamino)-2-hydroxypropoxy]-1,3-dihydrobenzimidazol-2-one	220776: Inhibition of I-iodocyanopindolol binding to human beta 1 adrenergic receptors	ki	0.0003	uM
1-[2-[[(2S)-3-(2-cyanophenoxy)-2-hydroxypropyl]amino]ethyl]-3-(6-fluoro-3-pyridinyl)urea	652407: Displacement of 3H-CGP-12177 from adrenergic beta1 receptor by cell based assay	ic50	0.0003	uM
1-[2-[[(2S)-3-(2-cyanophenoxy)-2-hydroxypropyl]amino]ethyl]-3-[4-(3-fluoropropoxy)phenyl]urea	652407: Displacement of 3H-CGP-12177 from adrenergic beta1 receptor by cell based assay	ic50	0.0003	uM
1-(5-bromopyrazin-2-yl)-3-[2-[[(2S)-3-(2-cyanophenoxy)-2-hydroxypropyl]amino]ethyl]urea	652407: Displacement of 3H-CGP-12177 from adrenergic beta1 receptor by cell based assay	ic50	0.0003	uM
(2S)-1-(3-methylphenoxy)-3-(propan-2-ylamino)propan-2-ol	366093: Binding affinity to beta-1 adrenergic receptor	kd	0.0004	uM
5-hydroxy-8-[1-hydroxy-2-[3-(3-methoxyphenyl)propylamino]ethyl]-4H-1,4-benzoxazin-3-one;hydrochloride	2089646: Agonist activity at human beta1 adrenoceptor expressed in HEK293 cells assessed as induction of accumulation of cAMP by HTRF assay	ec50	0.0004	uM
5-hydroxy-8-[1-hydroxy-2-[3-[3-(trifluoromethyl)phenyl]propylamino]ethyl]-4H-1,4-benzoxazin-3-one;hydrochloride	2089646: Agonist activity at human beta1 adrenoceptor expressed in HEK293 cells assessed as induction of accumulation of cAMP by HTRF assay	ec50	0.0005	uM
5-hydroxy-8-[1-hydroxy-2-[3-(4-methoxyphenyl)propylamino]ethyl]-4H-1,4-benzoxazin-3-one;hydrochloride	2089646: Agonist activity at human beta1 adrenoceptor expressed in HEK293 cells assessed as induction of accumulation of cAMP by HTRF assay	ec50	0.0005	uM
Pindolol	301362: Binding affinity at human adrenergic beta-1 receptor	ki	0.0005	uM
5-[(1R)-2-[[4-(3-chlorophenyl)-2-methylbutan-2-yl]amino]-1-hydroxyethyl]-8-hydroxy-1H-quinolin-2-one;hydrochloride	1783429: Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation	ec50	0.0006	uM
3-[2-hydroxy-3-[[1-(5-phenylthieno[2,3-d]pyrimidin-4-yl)piperidin-4-yl]amino]propoxy]phenol	517619: Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay	ec50	0.0006	uM
4-[3-(tert-butylamino)-2-hydroxypropoxy]-1,3-dihydrobenzimidazol-2-one	1798580: 3H-CGP 12177 Whole Cell Binding Assay from Article 10.1038/sj.bjp.0706048: “The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.”	kd	0.0006	uM
5-hydroxy-8-[1-hydroxy-2-[[2-methyl-1-(2-methylphenyl)propan-2-yl]amino]ethyl]-4H-1,4-benzoxazin-3-one	438906: Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation	ec50	0.0006	uM
5-hydroxy-8-[1-hydroxy-2-[3-(4-methylphenyl)propylamino]ethyl]-4H-1,4-benzoxazin-3-one;hydrochloride	2089646: Agonist activity at human beta1 adrenoceptor expressed in HEK293 cells assessed as induction of accumulation of cAMP by HTRF assay	ec50	0.0007	uM
4-hydroxy-7-[(1R)-1-hydroxy-2-[[(1R,2R)-2-(2-phenylethyl)cyclopentyl]amino]ethyl]-3H-1,3-benzothiazol-2-one	1185818: Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay	ki	0.0008	uM

CTD chemical–gene interactions

100 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Carvedilol	increases uptake, affects binding, decreases abundance, decreases activity, decreases reaction (+7 more)	18
Metoprolol	increases abundance, affects response to substance, affects cotreatment, affects binding, decreases activity (+2 more)	13
Atenolol	affects binding, decreases reaction, decreases abundance, affects response to substance, decreases activity (+6 more)	11
Propranolol	affects binding, decreases activity, decreases abundance, affects cotreatment, increases abundance (+6 more)	11
Cyclic AMP	decreases reaction, increases activity, decreases abundance, decreases activity, increases abundance (+5 more)	8
Dobutamine	increases phosphorylation, increases activity, affects response to substance, decreases reaction, increases reaction (+3 more)	8
Isoproterenol	increases activity, affects binding, increases uptake, increases phosphorylation, affects response to substance (+3 more)	7
Bisoprolol	decreases reaction, increases abundance, affects binding, decreases activity, decreases abundance	7
CGP 12177	increases abundance, increases activity, decreases activity, decreases abundance, affects cotreatment (+2 more)	5
CGP 20712A	decreases reaction, increases abundance, affects reaction, increases activity, decreases abundance (+3 more)	5
Valproic Acid	affects expression, increases expression, increases methylation	5
Alprenolol	increases reaction, affects binding, decreases abundance, increases abundance, increases activity (+6 more)	4
Norepinephrine	affects binding, increases activity, increases abundance, decreases reaction, increases reaction	4
Pindolol	decreases abundance, decreases reaction, increases abundance, increases expression, affects reaction (+3 more)	4
Bupranolol	decreases reaction, decreases activity, affects cotreatment, increases abundance, affects binding	3
Epinephrine	decreases reaction, increases activity, affects reaction, affects binding, increases abundance	3
Estradiol	decreases reaction, increases expression	3
Terbutaline	increases activity, decreases reaction, affects binding, decreases activity	3
broxaterol	increases activity, decreases reaction, affects binding, decreases activity	2
cyanopindolol	affects binding, decreases reaction	2
Nebivolol	increases activity, affects binding, decreases reaction	2
Albuterol	affects binding, decreases reaction	2
Colforsin	affects binding, affects cotreatment, increases abundance, increases reaction, increases activity (+3 more)	2
Labetalol	decreases activity, affects cotreatment, decreases reaction, increases abundance, increases activity	2
Nickel	decreases expression	2
Nicotine	decreases activity, decreases reaction, increases expression, increases phosphorylation, decreases response to substance (+1 more)	2
Timolol	affects binding, decreases activity, decreases reaction, increases abundance	2
Betaxolol	affects binding, decreases activity	2
Iodocyanopindolol	affects binding, decreases reaction	2
aristolochic acid I	decreases expression	1

ChEMBL screening assays

809 unique, capped per target: 509 binding, 290 functional, 10 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL3254788	Binding	Inhibition of beta-adrenergic receptor (unknown origin)	Linked Aryl Aryloxypropanolamines as a new class of lipid catabolis agents. — *J Med Chem*
CHEMBL646912	Functional	In vitro agonistic activity against cAMP accumulation level in CHO cells expressing human beta-AR receptor	4-Aminopiperidine ureas as potent selective agonists of the human beta(3)-adrenergic receptor. — *Bioorg Med Chem Lett*
CHEMBL4051048	ADMET	Agonist activity at recombinant human beta1 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins	Discovery of Novel Indazole Derivatives as Orally Available β3-Adrenergic Receptor Agonists Lacking Off-Target-Based Cardiovascular Side Effects. — *J Med Chem*

Cellosaurus cell lines

7 cell lines: 4 spontaneously immortalized cell line, 2 transformed cell line, 1 cancer cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_B1J6	Abcam HeLa ADRB1 KO	Cancer cell line	Female
CVCL_C0S4	ACTOne ADRB1	Transformed cell line	Female
CVCL_H393	CHO-K1/ADRB1/Galpha15	Spontaneously immortalized cell line	Female
CVCL_KU78	cAMP Hunter CHO-K1 ADRB1 Gs	Spontaneously immortalized cell line	Female
CVCL_KW29	PathHunter CHO-K1 ADRB1 beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_W457	HEK-293B1	Transformed cell line	Female
CVCL_ZK41	GeneBLAzer ADRB1-CRE-bla CHO-K1	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

Via MONDO — disease-level, not drug-specific.

Predicted chemistry — Sugi Predict

The predicted patent-compound landscape for ADRB1 across ~30M SureChEMBL compounds — explore on Sugi Predict.