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Target Snapshot

CHEMBL224 Target Snapshot

5-hydroxytryptamine receptor 2A · SINGLE PROTEIN · Homo sapiens

10,019Compounds
1,406Assays
205Approved Drugs
11,541.0Activities
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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 2026-09-12

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 current disease frame grounded. Protein identity stays anchored to UniProt P28223. Start with schizophrenia, then reuse UniProt P28223 as the stable protein anchor across project notes and exports.

Review focus
Review-ready target frame

Start with schizophrenia, then reuse UniProt P28223 as the stable protein anchor across project notes and exports.

ChEMBL component mapping + Open Targets-ready proxy + ChEMBL 36 via Core Engine 2026-09-12 32 linked drugs
Open source guide
Disease program
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 remain visible in the same block.

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.

Disease source · ChEMBL drug mechanism + indication proxy
Approved-linked Open Targets-ready proxy 32 linked drugs
Open disease block
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 2026-09-12
ChEMBL target ID
CHEMBL224
Primary anchor for compounds, assays, approvals, and exports
ChEMBL 36 via Core Engine As of 2026-09-12
www.ebi.ac.uk
UniProt accession
P28223
5-hydroxytryptamine receptor 2A
UniProt accession via ChEMBL component mapping As of 2026-09-12
www.uniprot.org
Disease evidence contract
Open Targets-ready proxy
ChEMBL drug mechanism + indication proxy
ChEMBL drug mechanism + indication proxy As of 2026-09-12
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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Need stable target naming and protein identity?
UniProt Target Context
UniProt accession via ChEMBL component mapping

Start here when your first question is whether 5-hydroxytryptamine receptor 2A is the right protein anchor across sources, using UniProt P28223 as the stable mapping.

Jump to Protein Context
Need disease fit before discussing compounds?
Disease Relevance & Evidence Level
ChEMBL drug mechanism + indication proxy

Use this block first when you need to confirm why schizophrenia is currently framed as approved-linked support. It currently carries 32 linked drugs 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 Label5-hydroxytryptamine receptor 2A
UniProt AccessionP28223
Component TypeProtein
Sequence Length471 aa

5-hydroxytryptamine receptor 2A

Source · UniProt accession via ChEMBL component mapping
Review Cue

How to read this target

Review this target as 5-hydroxytryptamine receptor 2A, mapped to UniProt P28223. Sequence length is 471 aa.

Mapped IDP28223
Review name5-hydroxytryptamine receptor 2A
OrganismHomo sapiens
Disease Relevance

Disease Relevance & Evidence Level

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

Approved-linked Open Targets-ready proxy

5-hydroxytryptamine receptor 2A shows approved-linked disease relevance led by schizophrenia. 5 more disease programs remain visible in the same review block.

Approved-linked Approved
schizophrenia
32 linked drugs · 32 direct · 32 efficacy
Linked drugARIPIPRAZOLE
Linked drugARIPIPRAZOLE LAUROXIL
Linked drugASENAPINE MALEATE
Linked drugBLONANSERIN
Approved-linked Approved
psychosis
19 linked drugs · 19 direct · 19 efficacy
Linked drugARIPIPRAZOLE
Linked drugASENAPINE MALEATE
Linked drugBREXPIPRAZOLE
Linked drugCHLORPROMAZINE
Approved-linked Approved
bipolar disorder
15 linked drugs · 15 direct · 15 efficacy
Linked drugARIPIPRAZOLE
Linked drugASENAPINE MALEATE
Linked drugBREXPIPRAZOLE
Linked drugCLOZAPINE
Approved-linked Approved
depressive disorder
15 linked drugs · 15 direct · 15 efficacy
Linked drugARIPIPRAZOLE
Linked drugBREXPIPRAZOLE
Linked drugCHLORPROTHIXENE
Linked drugCLOZAPINE
Approved-linked Approved
schizoaffective disorder
12 linked drugs · 12 direct · 12 efficacy
Linked drugARIPIPRAZOLE
Linked drugARIPIPRAZOLE LAUROXIL
Linked drugASENAPINE MALEATE
Linked drugBREXPIPRAZOLE
Approved-linked Approved
major depressive disorder
11 linked drugs · 11 direct · 11 efficacy
Linked drugARIPIPRAZOLE
Linked drugBREXPIPRAZOLE
Linked drugLUMATEPERONE
Linked drugMIRTAZAPINE
Source · ChEMBL drug mechanism + indication proxy
Review Cue

How to read disease relevance

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.

Lead diseaseschizophrenia
Strongest levelApproved-linked
Block modeOpen Targets-ready proxy
Clinical Profile

Clinical Phase Distribution

205
Approved
30
Phase III
65
Phase II
3
Phase I
Assay Mix

Activity Type Distribution

IC502,346.0
KI7,803.0
EC501,386.0
KD6.0
Lead Set

Top Inhibitors (by pChEMBL)

ChEMBL IDpChEMBLTypeValue (nM)Phase
CHEMBL252818 11.0 Ki 0.01 Preclinical
CHEMBL253022 11.0 Ki 0.01 Preclinical
CHEMBL6023465 10.8 Ki 0.016 Preclinical
CHEMBL157138 10.65 EC50 0.02239 Clinical
CHEMBL3652592 10.6 IC50 0.025 Preclinical
CHEMBL5414080 10.5 Ki 0.03162 Preclinical
CHEMBL5838844 10.49 Ki 0.032 Preclinical
CHEMBL149024 10.4 Ki 0.04 Preclinical
CHEMBL83894 10.4 Ki 0.04 Clinical
CHEMBL253878 10.4 Ki 0.04 Preclinical
Distribution

pChEMBL Value Distribution

342
5.0
756
5.5
1158
6.0
1215
6.5
1197
7.0
1412
7.5
1088
8.0
760
8.5
493
9.0
174
9.5
pChEMBL
Approved Drugs

Approved Drugs

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

Assay Landscape

1,406
Total Assays
5,562
Tested Compounds
4
Assay Types
Binding — 1,070 assays, 5,562 compounds
BAO Format Assays Compounds Avg pChEMBL
single protein format 661 1,570 7.1
cell-based format 343 2,806 7.2
cell membrane format 28 271 7.3
assay format 27 850 8.1
tissue-based format 9 5 8.7
microsome format 1 5 8.1
organism-based format 1 55 7.0
Functional — 295 assays, 908 compounds
BAO Format Assays Compounds Avg pChEMBL
cell-based format 208 692 7.0
assay format 72 125 7.1
single protein format 8 83 7.0
cell membrane format 4 4 8.3
tissue-based format 3 4 8.0
ADME — 40 assays, 112 compounds
BAO Format Assays Compounds Avg pChEMBL
cell-based format 32 99 6.7
single protein format 8 13 6.0
Toxicity — 1 assays, 0 compounds
BAO Format Assays Compounds Avg pChEMBL
assay format 1 0

Confidence Score Distribution

Source · ChEMBL 36 via Core Engine