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Evidence Snapshot

5-hydroxytryptamine receptor 2A

CHEMBL224 SINGLE PROTEIN Homo sapiens
Source Header

ChEMBL 36 via Core Engine

Target Snapshot 2026-09-13T22:30:16Z
Source · ChEMBL 36 via Core Engine
ChEMBL ChEMBL 36 CHEMBL224
Identity Layer

Cross-source identity

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

This review treats 5-hydroxytryptamine receptor 2A as ChEMBL target CHEMBL224, mapped to UniProt P28223. Disease framing currently uses the Open Targets-ready proxy contract.

Review anchor
5-hydroxytryptamine receptor 2A
SINGLE PROTEIN · Homo sapiens
As of 2026-09-13
ChEMBL target ID
CHEMBL224
Primary anchor for compounds, assays, approvals, and exports
ChEMBL 36 via Core Engine As of 2026-09-13
www.ebi.ac.uk
UniProt accession
P28223
5-hydroxytryptamine receptor 2A
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 5-hydroxytryptamine receptor 2A matters

As of 2026-09-13

5-hydroxytryptamine receptor 2A is reviewed as 5-hydroxytryptamine receptor 2A (UniProt P28223); 5-hydroxytryptamine receptor 2A shows approved-linked disease relevance led by schizophrenia. 5 more disease programs remain visible in the same review block.; 32 linked drugs keep this evidence frame grounded.; the current evidence base includes 205 approved drugs, 10019 compounds, and 1406 assays, with lead potency reaching pChEMBL 11.0.

Disease context
schizophrenia

5-hydroxytryptamine receptor 2A shows approved-linked disease relevance led by schizophrenia. 5 more disease programs remain visible in the same review block. 32 linked drugs keep the rationale reviewable. 5 additional disease programs remain visible in the same card. Linked drugs include ARIPIPRAZOLE, ARIPIPRAZOLE LAUROXIL, ASENAPINE MALEATE.

Start review with schizophrenia because it currently carries approved-linked support. Linked drugs include ARIPIPRAZOLE, ARIPIPRAZOLE LAUROXIL, ASENAPINE MALEATE, BLONANSERIN. This disease block keeps the Open Targets-ready contract explicit while current evidence comes from ChEMBL mechanism and indication mappings.

ChEMBL target record
Approved-linked 32 linked drugs
Activity base
Portfolio and assay base

ChEMBL currently tracks 205 approved drugs, 10019 compounds, and 1406 assays for this target. The dominant activity type is KI. CHEMBL252818 is the current potency anchor at pChEMBL 11.0.

Use CHEMBL252818 as the tractability anchor when discussing potency (pChEMBL 11.0).

Activity source · ChEMBL 36 via Core Engine
205 approved pChEMBL 11.0
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 5-hydroxytryptamine receptor 2A 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 P28223, 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 schizophrenia is currently treated as approved-linked support.

Open Disease Context

Snapshot State

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

10019
Total Compounds
1406
Total Assays
205
Approved Drugs
IC50: 2346.0, KI: 7803.0, EC50: 1386.0, KD: 6.0
Activity Types

pChEMBL Activity Distribution

Top 5 Inhibitors (by pChEMBL)

Structure Compound pChEMBL Type Phase
No preferred name
CHEMBL252818
 11.0 Ki —
No preferred name
CHEMBL253022
 11.0 Ki —
No preferred name
CHEMBL6023465
 10.8 Ki —
No preferred name
CHEMBL157138
 10.7 EC50 Clinical
No preferred name
CHEMBL3652592
 10.6 IC50 —

Approved Drugs

Structure Compound First Approval
LUMATEPERONE
CHEMBL3306803
 2019
LUMATEPERONE TOSYLATE
CHEMBL3233142
 2019
PIMAVANSERIN
CHEMBL2111101
 2016
BREXPIPRAZOLE
CHEMBL2105760
 2015
CARIPRAZINE
CHEMBL2028019
 2015
CARIPRAZINE HYDROCHLORIDE
CHEMBL2024517
 2015
LORCASERIN
CHEMBL360328
 2012
LURASIDONE
CHEMBL1237021
 2010
ASENAPINE
CHEMBL3187365
 2009
BLONANSERIN
CHEMBL178803
 2008
PALIPERIDONE
CHEMBL1621
 2006
TETRACAINE
CHEMBL698
 2005
CINACALCET HYDROCHLORIDE
CHEMBL1200776
 2004
TEGASEROD MALEATE
CHEMBL1516474
 2002
ARIPIPRAZOLE
CHEMBL1112
 2002
IMATINIB
CHEMBL941
 2001
ZIPRASIDONE
CHEMBL708
 2001
APOMORPHINE
CHEMBL53
 2001
DESLORATADINE
CHEMBL1172
 2001
KETOTIFEN FUMARATE
CHEMBL1633
 1999
KETOTIFEN
CHEMBL534
 1999
ROPINIROLE
CHEMBL589
 1997
QUETIAPINE
CHEMBL716
 1997
RALOXIFENE
CHEMBL81
 1997
SERTINDOLE
CHEMBL12713
 1996
OLANZAPINE
CHEMBL715
 1996
MIRTAZAPINE
CHEMBL654
 1996
AZELASTINE HYDROCHLORIDE
CHEMBL1200809
 1996
CARVEDILOL
CHEMBL723
 1995
NEFAZODONE
CHEMBL623
 1994
NEFAZODONE HYDROCHLORIDE
CHEMBL1200492
 1994
CISAPRIDE
CHEMBL1729
 1993
FENOFIBRATE
CHEMBL672
 1993
RISPERIDONE
CHEMBL85
 1993
SUMATRIPTAN
CHEMBL128
 1992
SERTRALINE
CHEMBL809
 1991
EBASTINE
CHEMBL305660
 1990
DAPIPRAZOLE
CHEMBL1201216
 1990
PROPAFENONE
CHEMBL631
 1989
CLOZAPINE
CHEMBL42
 1989
CLOMIPRAMINE
CHEMBL415
 1989
ASTEMIZOLE
CHEMBL296419
 1988
PERGOLIDE
CHEMBL531
 1988
FLUOXETINE
CHEMBL41
 1987
BUSPIRONE
CHEMBL49
 1986
AMISULPRIDE
CHEMBL243712
 1986
GUANFACINE
CHEMBL862
 1986
OXYMETAZOLINE
CHEMBL762
 1986
TERFENADINE
CHEMBL17157
 1985
PENTAMIDINE
CHEMBL55
 1984
← Target Page
Source Header

ChEMBL 36 via Core Engine

Target Snapshot 2026-09-13T22:30:16Z
Source · ChEMBL 36 via Core Engine
ChEMBL ChEMBL 36 CHEMBL224