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PsychedeliaDokholyan Laboratory
TargetAdrenergic receptors

Beta-3 adrenergic receptor

α and β adrenoceptors.

Measurements
16
Compounds
9
Binding constants
8
Median pX
—

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

ADRB3_HUMANADRB3Homo sapiens

Beta-3 adrenergic receptor

G protein-coupled receptor for catecholamines that couples to both G(s) and G(i) proteins, leading to either activation or inhibition of adenylate cyclase and cAMP-dependent pathway, respectively10188996,2570461,8641219. The rank order of potency for physiological agonists is norepinephrine > epinephrine10188996,2570461,8641219. Involved in the regulation of thermogenesis and lipolysis in brown and white adipose tissue, after coupling to G(s) proteins and stimulation of the cAMP-PKA axis (By similarity). Also activates lipolytic process by coupling to G(i) proteins and consequent initiation of the ERK1/2 MAP kinase cascade10207024. Participates in relaxation of the blood vessels and the urinary bladder10188996. Also mediates negative inotropic effects in cardiomyocytes through activation of an NO synthase pathway and subsequent increase in cGMP levels, possibly involving G(i/o) protein-mediated coupling9769330

Quoted from UniProt’s FUNCTION annotation for P13945 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

PartnerCombinedExperimentDatabaseText mining
UCP10.9430.0000.0000.937
GNAS0.9410.2880.9000.249
ADRB20.9400.0000.9000.426
GNAI10.9150.1300.9000.107
GNAI30.9140.1300.9000.095
GNAI20.9120.1300.9000.076
ADRB10.9070.0000.9000.106
SRC0.8940.2920.5000.720
LIPE0.8330.0000.0000.826
FGF210.7690.0000.0000.761

Where it sits in the cell

  • Vesicles
  • Basal body

Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.

UniProt, curated Cell membrane

Expression by tissue

The tissues this gene is enriched in, by consensus RNA. A tissue absent from this list is one the Atlas does not call specific for this gene, which is not the same as absent from it.

  • ovary12.8 nTPM
  • fallopian tube5.3 nTPM
  • urinary bladder5.2 nTPM

II · Anatomy

Where the gene is transcribed

The same two atlases the compound plates use, asked about this gene alone. Brain on the left, peripheral and autonomic tissues on the right.

Brain

cerebral cortex — 0.2 nTPM, from ADRB3cerebellum — no resolved target expressed herehippocampal formation — no resolved target expressed hereamygdala — 0.1 nTPM, from ADRB3hypothalamus — no resolved target expressed herethalamus — no resolved target expressed herebasal ganglia — no resolved target expressed heremedulla oblongata — no resolved target expressed here

basal ganglia: drawn as the caudate nucleus, putamen and globus pallidus.

Body

heart — no resolved target expressed heresmooth muscle — 0.9 nTPM, from ADRB3lung — 0.1 nTPM, from ADRB3liver — no resolved target expressed herekidney — no resolved target expressed herestomach — 2.3 nTPM, from ADRB3duodenum — 0.2 nTPM, from ADRB3small intestine — 0.7 nTPM, from ADRB3colon — 2.3 nTPM, from ADRB3adrenal gland — no resolved target expressed herethyroid gland — no resolved target expressed herepancreas — no resolved target expressed hereurinary bladder — 5.2 nTPM, from ADRB3skeletal muscle — no resolved target expressed herespleen — no resolved target expressed heresalivary gland — no resolved target expressed here
05 nTPM

Square-root ramp · shared scale across both plates

Shading is transcript level — not affinity, and not affinity combined with expression. Outlined but unshaded organs hold none of ADRB3 transcript above the atlas’s detection threshold. Anatomy from EMBL-EBI Anatomogram (Apache License 2.0); regions identified by Uberon (uberon.org), CC BY 3.0.

Brain · 2

  • cerebral cortex0.2 nTPM
  • amygdala0.1 nTPM

Peripheral and autonomic · 7

  • urinary bladder5.2 nTPM
  • stomach 12.3 nTPM
  • colon2.3 nTPM
  • smooth muscle0.9 nTPM
  • small intestine0.7 nTPM
  • duodenum0.2 nTPM
  • lung0.1 nTPM

Transcript is not protein. These are RNA levels for ADRB3, shaded on √nTPM so that a three-order range stays legible — on a linear ramp every region but the strongest would read as blank, which looks like absence rather than less. A region carrying no shading is one the atlas reports no consensus value for, not one where the gene is silent. And a gene being transcribed somewhere is not evidence that any compound reaches it. Human Protein Atlas, RNA expression, nTPM (normalized transcripts per million), consensus tissue dataset.

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Equilibrium binding constants 8

Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.

TargetClassTypeValue (nM)pXOrganismAssay
Beta-3 adrenergic receptorAdrenergic receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL2395833
Beta-3 adrenergic receptorAdrenergic receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909093
Beta-3 adrenergic receptorAdrenergic receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909093
Beta-3 adrenergic receptorAdrenergic receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909093
Beta-3 adrenergic receptorAdrenergic receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909093
Beta-3 adrenergic receptorAdrenergic receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909093
Beta-3 adrenergic receptorAdrenergic receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909093
Beta-3 adrenergic receptorAdrenergic receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909093

Functional readouts 7

IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.

TargetClassTypeValue (nM)pXOrganismAssay
Beta-3 adrenergic receptorAdrenergic receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909093
Beta-3 adrenergic receptorAdrenergic receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909093
Beta-3 adrenergic receptorAdrenergic receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909093
Beta-3 adrenergic receptorAdrenergic receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909093
Beta-3 adrenergic receptorAdrenergic receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909093
Beta-3 adrenergic receptorAdrenergic receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909093
Beta-3 adrenergic receptorAdrenergic receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909093

Other measurements 1

Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.

TargetClassTypeValue (nM)pXOrganismAssay
Beta-3 adrenergic receptorAdrenergic receptorsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL4687659
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