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Evidence Snapshot

GABA-A receptor; agonist GABA site

CHEMBL2109244 PROTEIN COMPLEX GROUP Homo sapiens
Source Header

ChEMBL 36 via Core Engine

Target Snapshot 2026-09-13T18:31:32Z
Source · ChEMBL 36 via Core Engine
ChEMBL ChEMBL 36 CHEMBL2109244
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 2026-09-13
ChEMBL target ID
CHEMBL2109244
Primary anchor for compounds, assays, approvals, and exports
ChEMBL 36 via Core Engine As of 2026-09-13
www.ebi.ac.uk
UniProt accession
P14867
Gamma-aminobutyric acid receptor subunit alpha-1
UniProt accession via ChEMBL component mapping As of 2026-09-13
www.uniprot.org
Disease evidence contract
Open Targets-ready proxy
ChEMBL drug mechanism + indication proxy
ChEMBL drug mechanism + indication proxy As of 2026-09-13
www.ebi.ac.uk

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

Review-ready Target Rationale

Why GABA-A receptor; agonist GABA site matters

As of 2026-09-13

GABA-A receptor; agonist GABA site is reviewed as Gamma-aminobutyric acid receptor subunit alpha-1 (UniProt P14867); 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 keep this evidence frame grounded.; the current evidence base includes 3 approved drugs, 97 compounds, and 34 assays, with lead potency reaching pChEMBL 7.1.

Protein context
Gamma-aminobutyric acid receptor subunit alpha-1

Gamma-aminobutyric acid receptor subunit alpha-1 Sequence length is 456 aa.

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
Disease context
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 keep the rationale reviewable. 5 additional disease programs remain visible in the same card. Linked drugs include ZOPICLONE.

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.

ChEMBL target record
Late clinical 1 linked drug
Activity base
Portfolio and assay base

ChEMBL currently tracks 3 approved drugs, 97 compounds, and 34 assays for this target. The dominant activity type is EC50. CHEMBL207538 is the current potency anchor at pChEMBL 7.1.

Use CHEMBL207538 as the tractability anchor when discussing potency (pChEMBL 7.1).

Activity source · ChEMBL 36 via Core Engine
3 approved pChEMBL 7.1
Source Guidance

Start with the right source

Pick the first block or linked source that matches the review question in front of you.

Need the shortest review narrative first?
Review-ready Target Rationale
One-page rationale with as-of-date and attribution

Start with the review rationale when you need to explain why GABA-A receptor; agonist GABA site matters before drilling into raw source blocks.

Jump to Review Rationale
Need stable protein naming or accession mapping?
UniProt Target Context
UniProt accession via ChEMBL component mapping

Go back to the target snapshot when you need the naming and mapping contract behind UniProt P14867, not just the summarized rationale.

Open Protein Context
Need disease fit or evidence level for program framing?
Disease Relevance & Evidence Level
ChEMBL drug mechanism + indication proxy

Use the target snapshot disease block when you need to see why anxiety is currently treated as late clinical support.

Open Disease Context

Snapshot State

No project snapshot selected. Export uses the live evidence card state.

97
Total Compounds
34
Total Assays
3
Approved Drugs
IC50: 5.0, KI: 4.0, EC50: 74.0
Activity Types

pChEMBL Activity Distribution

Top 5 Inhibitors (by pChEMBL)

Structure Compound pChEMBL Type Phase
No preferred name
CHEMBL207538
7.1 EC50 Approved
No preferred name
CHEMBL3354673
7.0 IC50
No preferred name
CHEMBL2440295
7.0 IC50
No preferred name
CHEMBL1568698
7.0 EC50 Approved
No preferred name
CHEMBL3427528
6.9 EC50

Approved Drugs

Structure Compound First Approval
GANAXOLONE
CHEMBL1568698
2022
BREXANOLONE
CHEMBL207538
2019
← Target Page
Source Header

ChEMBL 36 via Core Engine

Target Snapshot 2026-09-13T18:31:32Z
Source · ChEMBL 36 via Core Engine
ChEMBL ChEMBL 36 CHEMBL2109244