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Target Snapshot

CHEMBL2095172 Target Snapshot

GABA-A receptor; alpha-1/beta-2/gamma-2 · PROTEIN COMPLEX · Homo sapiens

712Compounds
217Assays
14Approved Drugs
505.0Activities
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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 2026-09-13

Protein identity stays anchored to UniProt P14867. Use UniProt P14867 as the stable identity anchor, then attach disease evidence before program review.

Review focus
Protein anchor ready

Use UniProt P14867 as the stable identity anchor, then attach disease evidence before program review.

ChEMBL component mapping + Open Targets-ready proxy + ChEMBL 36 via Core Engine 2026-09-13
Open source guide
Protein anchor
Gamma-aminobutyric acid receptor subunit alpha-1

Gamma-aminobutyric acid receptor subunit alpha-1

Review this target as GABA-A receptor; alpha-1/beta-2/gamma-2, 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; alpha-1/beta-2/gamma-2 as ChEMBL target CHEMBL2095172, mapped to UniProt P14867. Disease framing currently uses the Open Targets-ready proxy contract.

Review anchor
GABA-A receptor; alpha-1/beta-2/gamma-2
PROTEIN COMPLEX · Homo sapiens
As of 2026-09-13
ChEMBL target ID
CHEMBL2095172
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.

Source Guidance

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UniProt Target Context
UniProt accession via ChEMBL component mapping

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Disease Relevance & Evidence Level
ChEMBL drug mechanism + indication proxy

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Evidence Card
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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; alpha-1/beta-2/gamma-2, 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; alpha-1/beta-2/gamma-2
OrganismHomo sapiens
Clinical Profile

Clinical Phase Distribution

14
Approved
1
Phase III
4
Phase II
2
Phase I
Assay Mix

Activity Type Distribution

IC50111.0
KI84.0
EC50310.0
Lead Set

Top Inhibitors (by pChEMBL)

ChEMBL IDpChEMBLTypeValue (nM)Phase
CHEMBL1709464 10.3 Ki 0.05 Preclinical
CHEMBL469477 9.92 Ki 0.12 Preclinical
CHEMBL487686 9.92 Ki 0.12 Preclinical
CHEMBL488283 9.92 Ki 0.12 Preclinical
CHEMBL487687 9.85 Ki 0.14 Preclinical
CHEMBL50763 9.77 Ki 0.17 Preclinical
CHEMBL48403 9.66 Ki 0.22 Preclinical
CHEMBL3274851 9.59 Ki 0.26 Preclinical
CHEMBL381059 9.57 Ki 0.27 Preclinical
CHEMBL49888 9.52 Ki 0.3 Preclinical
Distribution

pChEMBL Value Distribution

31
5.0
55
5.5
54
6.0
52
6.5
18
7.0
24
7.5
21
8.0
9
8.5
9
9.0
10
9.5
pChEMBL
Approved Drugs

Approved Drugs

ZURANOLONE
CHEMBL4105630
Approved 2023
GANAXOLONE
CHEMBL1568698
Approved 2022
BREXANOLONE
CHEMBL207538
Approved 2019
ZALEPLON
CHEMBL1521
Approved 1999
ZOLPIDEM
CHEMBL911
Approved 1992
ALPRAZOLAM
CHEMBL661
Approved 1981
DIAZEPAM
CHEMBL12
Approved 1963
Assay Landscape

Assay Landscape

217
Total Assays
264
Tested Compounds
2
Assay Types
Binding — 173 assays, 264 compounds
BAO Format Assays Compounds Avg pChEMBL
cell-based format 137 183 6.2
protein complex format 27 43 5.8
assay format 7 13 6.4
cell membrane format 2 25 7.3
Functional — 44 assays, 39 compounds
BAO Format Assays Compounds Avg pChEMBL
cell-based format 27 33 6.4
assay format 17 6 5.0

Confidence Score Distribution

Source · ChEMBL 36 via Core Engine