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Target Snapshot

CHEMBL2109244 Target Snapshot

GABA-A receptor; agonist GABA site · PROTEIN COMPLEX GROUP · Homo sapiens

97Compounds
34Assays
3Approved Drugs
83.0Activities
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Broader Open DB context

Frame the target before identity details

Structured disease, protein, and project context should read before the lower-level identity rail.

As of 2026-09-14

GABA-A receptor; agonist GABA site shows late clinical disease relevance led by anxiety. 5 more disease programs remain visible in the same review block. 1 linked drug keeps the current disease frame grounded. Protein identity stays anchored to UniProt P14867. Start with anxiety, then reuse UniProt P14867 as the stable protein anchor across project notes and exports.

Review focus
Review-ready target frame

Start with anxiety, then reuse UniProt P14867 as the stable protein anchor across project notes and exports.

ChEMBL component mapping + Open Targets-ready proxy + ChEMBL 36 via Core Engine 2026-09-14 1 linked drug
Open source guide
Disease program
anxiety

GABA-A receptor; agonist GABA site shows late clinical disease relevance led by anxiety. 5 more disease programs remain visible in the same review block. 1 linked drug remains visible in the same block.

Start review with anxiety because it currently carries late clinical support. Linked drugs include ZOPICLONE. This disease block keeps the Open Targets-ready contract explicit while current evidence comes from ChEMBL mechanism and indication mappings.

Disease source · ChEMBL drug mechanism + indication proxy
Late clinical Open Targets-ready proxy 1 linked drug
Open disease block
Protein anchor
Gamma-aminobutyric acid receptor subunit alpha-1

Gamma-aminobutyric acid receptor subunit alpha-1

Review this target as GABA-A receptor; agonist GABA site, mapped to UniProt P14867. ChEMBL maps the protein component as Gamma-aminobutyric acid receptor subunit alpha-1. Sequence length is 456 aa.

Protein source · UniProt accession via ChEMBL component mapping
UniProt P14867 Protein 456 aa
Open protein block
Identity Layer

Cross-source identity

Keep the review anchor, source IDs, and context contract aligned before reusing this target elsewhere.

This review treats GABA-A receptor; agonist GABA site as ChEMBL target CHEMBL2109244, mapped to UniProt P14867. Disease framing currently uses the Open Targets-ready proxy contract.

Review anchor
GABA-A receptor; agonist GABA site
PROTEIN COMPLEX GROUP · Homo sapiens
As of 2026-09-14
ChEMBL target ID
CHEMBL2109244
Primary anchor for compounds, assays, approvals, and exports
ChEMBL 36 via Core Engine As of 2026-09-14
www.ebi.ac.uk
UniProt accession
P14867
Gamma-aminobutyric acid receptor subunit alpha-1
UniProt accession via ChEMBL component mapping As of 2026-09-14
www.uniprot.org
Disease evidence contract
Open Targets-ready proxy
ChEMBL drug mechanism + indication proxy
ChEMBL drug mechanism + indication proxy As of 2026-09-14
www.ebi.ac.uk

Reuse the same identifiers in notes, watch rules, exports, and review packs so provenance stays stable across surfaces.

Source Guidance

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UniProt Target Context
UniProt accession via ChEMBL component mapping

Start here when your first question is whether GABA-A receptor; agonist GABA site is the right protein anchor across sources, using UniProt P14867 as the stable mapping.

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Disease Relevance & Evidence Level
ChEMBL drug mechanism + indication proxy

Use this block first when you need to confirm why anxiety is currently framed as late clinical support. It currently carries 1 linked drug in the same disease frame.

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Evidence Card
Review-ready rationale with source-aware context

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Overview

Basic Information

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UniProt Context

UniProt Target Context

Reviewable protein naming and mapping context for this target snapshot.

Protein LabelGamma-aminobutyric acid receptor subunit alpha-1
UniProt AccessionP14867
Component TypeProtein
Sequence Length456 aa

Gamma-aminobutyric acid receptor subunit alpha-1

Source · UniProt accession via ChEMBL component mapping
Review Cue

How to read this target

Review this target as GABA-A receptor; agonist GABA site, mapped to UniProt P14867. ChEMBL maps the protein component as Gamma-aminobutyric acid receptor subunit alpha-1. Sequence length is 456 aa.

Mapped IDP14867
Review nameGABA-A receptor; agonist GABA site
OrganismHomo sapiens
Disease Relevance

Disease Relevance & Evidence Level

Open Targets-ready disease context using the current target-indication evidence contract.

Late clinical Open Targets-ready proxy

GABA-A receptor; agonist GABA site shows late clinical disease relevance led by anxiety. 5 more disease programs remain visible in the same review block.

Late clinical Phase III
anxiety
1 linked drug · 1 direct · 1 efficacy
Linked drugZOPICLONE
Late clinical Phase III
Dementia
1 linked drug · 1 direct · 1 efficacy
Linked drugZOPICLONE
Late clinical Phase III
depressive disorder
1 linked drug · 1 direct · 1 efficacy
Linked drugZOPICLONE
Late clinical Phase III
insomnia
1 linked drug · 1 direct · 1 efficacy
Linked drugZOPICLONE
Late clinical Phase III
obstructive sleep apnea
1 linked drug · 1 direct · 1 efficacy
Linked drugZOPICLONE
Late clinical Phase III
schizophrenia
1 linked drug · 1 direct · 1 efficacy
Linked drugZOPICLONE
Source · ChEMBL drug mechanism + indication proxy
Review Cue

How to read disease relevance

Start review with anxiety because it currently carries late clinical support. Linked drugs include ZOPICLONE. This disease block keeps the Open Targets-ready contract explicit while current evidence comes from ChEMBL mechanism and indication mappings.

Lead diseaseanxiety
Strongest levelLate clinical
Block modeOpen Targets-ready proxy
Clinical Profile

Clinical Phase Distribution

3
Approved
2
Phase I
Assay Mix

Activity Type Distribution

IC505.0
KI4.0
EC5074.0
Lead Set

Top Inhibitors (by pChEMBL)

ChEMBL IDpChEMBLTypeValue (nM)Phase
CHEMBL207538 7.12 EC50 75.5 Approved
CHEMBL2440295 7.0 IC50 100.0 Preclinical
CHEMBL3354673 7.0 IC50 100.0 Preclinical
CHEMBL1568698 6.99 EC50 103.0 Approved
CHEMBL3427528 6.92 EC50 119.0 Preclinical
CHEMBL3427532 6.9 EC50 125.0 Preclinical
CHEMBL3427537 6.75 EC50 178.0 Preclinical
CHEMBL3427543 6.75 EC50 178.0 Preclinical
CHEMBL3427526 6.54 EC50 292.0 Preclinical
CHEMBL3427535 6.46 EC50 345.0 Preclinical
Distribution

pChEMBL Value Distribution

2
5.0
21
5.5
15
6.0
9
6.5
3
7.0
0
7.5
0
8.0
0
8.5
0
9.0
0
9.5
pChEMBL
Approved Drugs

Approved Drugs

GANAXOLONE
CHEMBL1568698
Approved 2022
BREXANOLONE
CHEMBL207538
Approved 2019
Assay Landscape

Assay Landscape

34
Total Assays
32
Tested Compounds
2
Assay Types
Binding — 19 assays, 32 compounds
BAO Format Assays Compounds Avg pChEMBL
protein complex format 15 5 5.8
cell-based format 4 27 6.1
Functional — 15 assays, 5 compounds
BAO Format Assays Compounds Avg pChEMBL
cell-based format 10 4 5.2
assay format 5 1 6.2

Confidence Score Distribution

Source · ChEMBL 36 via Core Engine