Gamma-aminobutyric acid receptor subunit rho-1
GABA-A and GABA-B receptors.
- Measurements
- 8
- Compounds
- 1
- Binding constants
- 1
- 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.
Gamma-aminobutyric acid receptor subunit rho-1
Rho subunit of the pentameric ligand-gated chloride channels responsible for mediating the effects of gamma-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the brain37659407. Rho-containing GABA-gated chloride channels are a subclass of GABA(A) receptors (GABAARs) entirely composed of rho subunits, where GABA molecules bind at the rho intersubunit interfaces37659407. When activated by GABA, rho-GABAARs selectively allow the flow of chloride anions across the cell membrane down their electrochemical gradient37659407. Rho-1 subunits are primarily expressed in retina where rho-1-containing GABAARs may play a role in retinal neurotransmission1849271. Rho-1 GABAARs are also involved in neuronal tonic (extrasynaptic) and phasic (synaptic) transmission in the Purkinje neurons of the cerebellum (By similarity). Rho-1 GABAARs may also contribute to the regulation of glial development in the cerebellum by controlling extrasynaptic transmission (By similarity)
Quoted from UniProt’s FUNCTION annotation for P24046 (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 | Experiment | Database | Text mining |
|---|---|---|---|---|
| GABRR2 | 0.928 | 0.000 | 0.900 | 0.283 |
| GABRR3 | 0.913 | 0.000 | 0.900 | 0.095 |
| GABBR2 | 0.738 | 0.000 | 0.540 | 0.446 |
| GABRG2 | 0.711 | 0.189 | 0.540 | 0.210 |
| GABRA2 | 0.708 | 0.189 | 0.540 | 0.202 |
| GABRA5 | 0.707 | 0.189 | 0.540 | 0.198 |
| GABRE | 0.701 | 0.178 | 0.540 | 0.204 |
| GABRA1 | 0.701 | 0.189 | 0.540 | 0.201 |
| GABRA6 | 0.699 | 0.189 | 0.540 | 0.190 |
| GABRA4 | 0.699 | 0.189 | 0.540 | 0.207 |
Where it sits in the cell
UniProt, curated Postsynaptic cell membrane · Cell membrane
Expression by cell type
Single cell type RNA, the 1 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.
- Retinal bipolar cells188.9 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.
- retina22.8 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.
Brain
basal ganglia: drawn as the caudate nucleus, putamen and globus pallidus.
Measured but not drawn — this anatomogram has no outline for them: retina 22.8.
Body
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 GABRR1 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 · 1
- retina22.8 nTPM
Peripheral and autonomic · 3
- kidney0.1 nTPM
- urinary bladder0.1 nTPM
- skeletal muscle0.1 nTPM
Transcript is not protein. These are RNA levels for GABRR1, 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 1
Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Gamma-aminobutyric acid receptor subunit rho-1 | GABA receptors | Kd | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL679669 |
Functional readouts 6
IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Gamma-aminobutyric acid receptor subunit rho-1 | GABA receptors | EC50 | 692 | 6.16 | Homo sapiens | CHEMBL3370253 |
| Gamma-aminobutyric acid receptor subunit rho-1 | GABA receptors | EC50 | 700 | 6.15 | Homo sapiens | CHEMBL3370253 |
| Gamma-aminobutyric acid receptor subunit rho-1 | GABA receptors | EC50 | 2,300 | 5.64 | Homo sapiens | CHEMBL2340049 |
| Gamma-aminobutyric acid receptor subunit rho-1 | GABA receptors | EC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL2317988 |
| Gamma-aminobutyric acid receptor subunit rho-1 | GABA receptors | EC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL2317988 |
| Gamma-aminobutyric acid receptor subunit rho-1 | GABA receptors | EC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL964513 |
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.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Gamma-aminobutyric acid receptor subunit rho-1 | GABA receptors | Rmax | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3370498 |