TargetIon channels

Transient receptor potential cation channel subfamily V member 4

Voltage- and ligand-gated channels, including the TRP family and hERG (KCNH2).

Measurements: 19
Compounds: 6
Binding constants: 0
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

TRPV4_HUMANTRPV4Homo sapiens

Transient receptor potential cation channel subfamily V member 4

Non-selective calcium permeant cation channel involved in osmotic sensitivity and mechanosensitivity16293632,18695040,18826956,22526352,23136043,29899501. Activation by exposure to hypotonicity within the physiological range exhibits an outward rectification18695040,18826956,29899501. Also activated by heat, low pH, citrate and phorbol esters16293632,18695040,18826956,20037586,21964574,25256292. Increase of intracellular Ca(2+) potentiates currents. Channel activity seems to be regulated by a calmodulin-dependent mechanism with a negative feedback mechanism12724311,18826956. Promotes cell-cell junction formation in skin keratinocytes and plays an important role in the formation and/or maintenance of functional intercellular barriers (By similarity). Acts as a regulator of intracellular Ca(2+) in synoviocytes19759329. Plays an obligatory role as a molecular component in the nonselective cation channel activation induced by 4-alpha-phorbol 12,13-didecanoate and hypotonic stimulation in synoviocytes and also regulates production of IL-819759329. Together with PKD2, forms mechano- and thermosensitive channels in cilium18695040. Negatively regulates expression of PPARGC1A, UCP1, oxidative metabolism and respiration in adipocytes (By similarity). Regulates expression of chemokines and cytokines related to pro-inflammatory pathway in adipocytes (By similarity). Together with AQP5, controls regulatory volume decrease in salivary epithelial cells (By similarity). Required for normal development and maintenance of bone and cartilage26249260. In its inactive state, may sequester DDX3X at the plasma membrane. When activated, the interaction between both proteins is affected and DDX3X relocalizes to the nucleus29899501. In neurons of the central nervous system, could play a role in triggering voluntary water intake in response to increased sodium concentration in body fluid (By similarity)

Non-selective calcium permeant cation channel involved in osmotic sensitivity and mechanosensitivity. Activation by exposure to hypotonicity within the physiological range exhibits an outward rectification. Also activated by phorbol esters. Has the same channel activity as isoform 1, and is activated by the same stimuli

Lacks channel activity, due to impaired oligomerization and intracellular retention

(Microbial infection) Facilitates hepatitis C virus (HCV) replication, possibly through its action on DDX3X

(Microbial infection) Facilitates Dengue virus (DENV) replication, possibly through its action on DDX3X

(Microbial infection) Facilitates Zika virus (ZIKV) replication, possibly through its action on DDX3X

Quoted from UniProt’s FUNCTION annotation for Q9HBA0 (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.

Partner	Combined	Database	Text mining
TRPC1	0.995	0.000	0.995
PKD2	0.974	0.000	0.974
CAV1	0.947	0.000	0.945
TRPC6	0.940	0.000	0.940
PRKCA	0.923	0.900	0.265
PRKCG	0.911	0.900	0.146
PRKCE	0.911	0.900	0.142
PRKCD	0.905	0.900	0.079
PRKCB	0.905	0.900	0.095
PRKCH	0.902	0.900	0.050

Where it sits in the cell

UniProt, curated Cell membrane · Apical cell membrane · Cell junction, adherens junction · Cell projection, cilium · Endoplasmic reticulum

Expression by cell type

Single cell type RNA, the 9 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

Choroid plexus epithelial cells679.7 nCPM
Esophageal apical cells207.7 nCPM
Proximal tubule cells156.7 nCPM
Renal connecting tubule cells134 nCPM
Respiratory ciliated cells128 nCPM
Kupffer cells111.7 nCPM
Renal collecting duct principal cells107.8 nCPM
Retinal pigment epithelial cells106.6 nCPM
Respiratory basal cells86.6 nCPM

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.

choroid plexus69.8 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.

018 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 TRPV4 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 · 9

pituitary gland1.8 nTPM
hippocampal formation0.2 nTPM
midbrain0.2 nTPM
spinal cord0.2 nTPM
cerebral cortex0.1 nTPM
cerebellum0.1 nTPM
amygdala0.1 nTPM
hypothalamus0.1 nTPM
basal ganglia0.1 nTPM

Peripheral and autonomic · 15

salivary gland18.1 nTPM
kidney13.0 nTPM
liver7.7 nTPM
pancreas3.9 nTPM
spleen2.5 nTPM
lung1.9 nTPM
urinary bladder1.6 nTPM
thyroid gland0.8 nTPM
heart muscle0.7 nTPM
smooth muscle0.7 nTPM
adrenal gland0.7 nTPM
stomach 10.6 nTPM
duodenum0.6 nTPM
colon0.4 nTPM
small intestine0.3 nTPM

Transcript is not protein. These are RNA levels for TRPV4, 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.

Functional readouts 13

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

Target	Class	Type	Value (nM)	pX	Organism	Assay
Transient receptor potential cation channel subfamily V member 4	Ion channels	EC50	600	6.22	Homo sapiens	CHEMBL5096632
Transient receptor potential cation channel subfamily V member 4	Ion channels	EC50	900	6.05	Homo sapiens	CHEMBL5096632
Transient receptor potential cation channel subfamily V member 4	Ion channels	IC50	1,300	5.89	Homo sapiens	CHEMBL5096634
Transient receptor potential cation channel subfamily V member 4	Ion channels	IC50	2,900	5.54	Homo sapiens	CHEMBL5096634
Transient receptor potential cation channel subfamily V member 4	Ion channels	IC50	3,200	5.49	Homo sapiens	CHEMBL5096634
Transient receptor potential cation channel subfamily V member 4	Ion channels	EC50	5,100	5.29	Homo sapiens	CHEMBL5096632
Transient receptor potential cation channel subfamily V member 4	Ion channels	IC50	5,400	5.27	Homo sapiens	CHEMBL5096634
Transient receptor potential cation channel subfamily V member 4	Ion channels	EC50	6,400	5.19	Homo sapiens	CHEMBL5096632
Transient receptor potential cation channel subfamily V member 4	Ion channels	IC50	9,900	5.00	Homo sapiens	CHEMBL5096634
Transient receptor potential cation channel subfamily V member 4	Ion channels	EC50	16,100	4.79	Homo sapiens	CHEMBL5096632
Transient receptor potential cation channel subfamily V member 4	Ion channels	EC50	— no normalized value	— value does not convert to pX	Rattus norvegicus	CHEMBL4143895
Transient receptor potential cation channel subfamily V member 4	Ion channels	IC50	— no normalized value	— value does not convert to pX	Rattus norvegicus	CHEMBL4675870
Transient receptor potential cation channel subfamily V member 4	Ion channels	EC50	— no normalized value	— value does not convert to pX	Rattus norvegicus	CHEMBL4675871

Other measurements 6

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.

Target	Class	Type	Value (nM)	pX	Organism	Assay
Transient receptor potential cation channel subfamily V member 4	Ion channels	Efficacy	— no normalized value	— value does not convert to pX	Homo sapiens	CHEMBL5096633
Transient receptor potential cation channel subfamily V member 4	Ion channels	Efficacy	— no normalized value	— value does not convert to pX	Homo sapiens	CHEMBL5096633
Transient receptor potential cation channel subfamily V member 4	Ion channels	Efficacy	— no normalized value	— value does not convert to pX	Homo sapiens	CHEMBL5096633
Transient receptor potential cation channel subfamily V member 4	Ion channels	Efficacy	— no normalized value	— value does not convert to pX	Homo sapiens	CHEMBL5096633
Transient receptor potential cation channel subfamily V member 4	Ion channels	Efficacy	— no normalized value	— value does not convert to pX	Homo sapiens	CHEMBL5096633
Transient receptor potential cation channel subfamily V member 4	Ion channels	Efficacy	— no normalized value	— value does not convert to pX	Rattus norvegicus	CHEMBL4675872

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