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Target Snapshot

CHEMBL214 Target Snapshot

5-hydroxytryptamine receptor 1A · SINGLE PROTEIN · Homo sapiens

9,808Compounds
1,664Assays
84Approved Drugs
9,071.0Activities
Free Research Context

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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

5-hydroxytryptamine receptor 1A shows approved-linked disease relevance led by major depressive disorder. 5 more disease programs remain visible in the same review block. 8 linked drugs keep the current disease frame grounded. Protein identity stays anchored to UniProt P08908. Start with major depressive disorder, then reuse UniProt P08908 as the stable protein anchor across project notes and exports.

Review focus
Review-ready target frame

Start with major depressive disorder, then reuse UniProt P08908 as the stable protein anchor across project notes and exports.

ChEMBL component mapping + Open Targets-ready proxy + ChEMBL 36 via Core Engine 2026-09-13 8 linked drugs
Open source guide
Disease program
major depressive disorder

5-hydroxytryptamine receptor 1A shows approved-linked disease relevance led by major depressive disorder. 5 more disease programs remain visible in the same review block. 8 linked drugs remain visible in the same block.

Start review with major depressive disorder because it currently carries approved-linked support. Linked drugs include ARIPIPRAZOLE, BREXPIPRAZOLE, GEPIRONE HYDROCHLORIDE, GSK163090. 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 8 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 1A as ChEMBL target CHEMBL214, mapped to UniProt P08908. Disease framing currently uses the Open Targets-ready proxy contract.

Review anchor
5-hydroxytryptamine receptor 1A
SINGLE PROTEIN · Homo sapiens
As of 2026-09-13
ChEMBL target ID
CHEMBL214
Primary anchor for compounds, assays, approvals, and exports
ChEMBL 36 via Core Engine As of 2026-09-13
www.ebi.ac.uk
UniProt accession
P08908
5-hydroxytryptamine receptor 1A
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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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 1A is the right protein anchor across sources, using UniProt P08908 as the stable mapping.

Jump to Protein Context
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Disease Relevance & Evidence Level
ChEMBL drug mechanism + indication proxy

Use this block first when you need to confirm why major depressive disorder is currently framed as approved-linked support. It currently carries 8 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 1A
UniProt AccessionP08908
Component TypeProtein
Sequence Length422 aa

5-hydroxytryptamine receptor 1A

Source · UniProt accession via ChEMBL component mapping
Review Cue

How to read this target

Review this target as 5-hydroxytryptamine receptor 1A, mapped to UniProt P08908. Sequence length is 422 aa.

Mapped IDP08908
Review name5-hydroxytryptamine receptor 1A
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 1A shows approved-linked disease relevance led by major depressive disorder. 5 more disease programs remain visible in the same review block.

Approved-linked Approved
major depressive disorder
8 linked drugs · 8 direct · 8 efficacy
Linked drugARIPIPRAZOLE
Linked drugBREXPIPRAZOLE
Linked drugGEPIRONE HYDROCHLORIDE
Linked drugGSK163090
Approved-linked Approved
depressive disorder
6 linked drugs · 6 direct · 6 efficacy
Linked drugARIPIPRAZOLE
Linked drugBIFEPRUNOX
Linked drugBREXPIPRAZOLE
Linked drugBUSPIRONE HYDROCHLORIDE
Approved-linked Approved
schizophrenia
6 linked drugs · 6 direct · 6 efficacy
Linked drugARIPIPRAZOLE
Linked drugARIPIPRAZOLE LAUROXIL
Linked drugBIFEPRUNOX
Linked drugBREXPIPRAZOLE
Approved-linked Approved
schizoaffective disorder
5 linked drugs · 5 direct · 5 efficacy
Linked drugARIPIPRAZOLE
Linked drugARIPIPRAZOLE LAUROXIL
Linked drugBIFEPRUNOX
Linked drugBREXPIPRAZOLE
Approved-linked Approved
bipolar disorder
3 linked drugs · 3 direct · 3 efficacy
Linked drugARIPIPRAZOLE
Linked drugBIFEPRUNOX
Linked drugBREXPIPRAZOLE
Approved-linked Approved
bipolar I disorder
3 linked drugs · 3 direct · 3 efficacy
Linked drugARIPIPRAZOLE
Linked drugBIFEPRUNOX
Linked drugBREXPIPRAZOLE
Source · ChEMBL drug mechanism + indication proxy
Review Cue

How to read disease relevance

Start review with major depressive disorder because it currently carries approved-linked support. Linked drugs include ARIPIPRAZOLE, BREXPIPRAZOLE, GEPIRONE HYDROCHLORIDE, GSK163090. This disease block keeps the Open Targets-ready contract explicit while current evidence comes from ChEMBL mechanism and indication mappings.

Lead diseasemajor depressive disorder
Strongest levelApproved-linked
Block modeOpen Targets-ready proxy
Clinical Profile

Clinical Phase Distribution

84
Approved
25
Phase III
58
Phase II
Assay Mix

Activity Type Distribution

IC50832.0
KI6,925.0
EC501,242.0
KD72.0
Lead Set

Top Inhibitors (by pChEMBL)

ChEMBL IDpChEMBLTypeValue (nM)Phase
CHEMBL199824 11.0 EC50 0.01 Preclinical
CHEMBL4790600 11.0 Ki 0.01 Preclinical
CHEMBL4790600 10.99 EC50 0.01023 Preclinical
CHEMBL4746386 10.89 Ki 0.01288 Preclinical
CHEMBL4757755 10.88 EC50 0.01318 Preclinical
CHEMBL4755058 10.86 EC50 0.0138 Preclinical
CHEMBL1258761 10.85 Ki 0.0141 Preclinical
CHEMBL4742112 10.83 Ki 0.01479 Preclinical
CHEMBL1258533 10.82 Ki 0.0152 Preclinical
CHEMBL4760271 10.8 Ki 0.01585 Preclinical
Distribution

pChEMBL Value Distribution

297
5.0
428
5.5
847
6.0
1023
6.5
1236
7.0
1218
7.5
1091
8.0
825
8.5
489
9.0
212
9.5
pChEMBL
Approved Drugs

Approved Drugs

GEPIRONE
CHEMBL284092
Approved 2023
LOFEXIDINE
CHEMBL17860
Approved 2018
FLIBANSERIN
CHEMBL231068
Approved 2015
CARIPRAZINE HYDROCHLORIDE
CHEMBL2024517
Approved 2015
CARIPRAZINE
CHEMBL2028019
Approved 2015
BREXPIPRAZOLE
CHEMBL2105760
Approved 2015
VORTIOXETINE
CHEMBL2104993
Approved 2013
VILAZODONE
CHEMBL439849
Approved 2011
VILAZODONE HYDROCHLORIDE
CHEMBL1615374
Approved 2011
LURASIDONE
CHEMBL1237021
Approved 2010
SILODOSIN
CHEMBL24778
Approved 2008
TEGASEROD MALEATE
CHEMBL1516474
Approved 2002
ARIPIPRAZOLE
CHEMBL1112
Approved 2002
FROVATRIPTAN
CHEMBL1279
Approved 2001
APOMORPHINE
CHEMBL53
Approved 2001
ZIPRASIDONE
CHEMBL708
Approved 2001
RIZATRIPTAN
CHEMBL905
Approved 1998
NARATRIPTAN
CHEMBL1278
Approved 1998
ZOLMITRIPTAN
CHEMBL1185
Approved 1997
TAMSULOSIN
CHEMBL836
Approved 1997
QUETIAPINE
CHEMBL716
Approved 1997
MIRTAZAPINE
CHEMBL654
Approved 1996
SERTINDOLE
CHEMBL12713
Approved 1996
OLANZAPINE
CHEMBL715
Approved 1996
NEFAZODONE
CHEMBL623
Approved 1994
CISAPRIDE
CHEMBL1729
Approved 1993
RISPERIDONE
CHEMBL85
Approved 1993
SUMATRIPTAN
CHEMBL128
Approved 1992
EBASTINE
CHEMBL305660
Approved 1990
CLOZAPINE
CHEMBL42
Approved 1989
PERGOLIDE
CHEMBL531
Approved 1988
OXYMETAZOLINE HYDROCHLORIDE
CHEMBL1200791
Approved 1986
BUSPIRONE
CHEMBL49
Approved 1986
PINDOLOL
CHEMBL500
Approved 1982
TRAZODONE
CHEMBL621
Approved 1981
AMOXAPINE
CHEMBL1113
Approved 1980
BROMOCRIPTINE
CHEMBL493
Approved 1978
PROPRANOLOL HYDROCHLORIDE
CHEMBL1671
Approved 1967
METHYSERGIDE MALEATE
CHEMBL1200938
Approved 1962
FLUPHENAZINE
CHEMBL726
Approved 1959
CHLORPROMAZINE
CHEMBL71
Approved 1957
CHLORPROMAZINE HYDROCHLORIDE
CHEMBL1713
Approved 1957
DIHYDROERGOTAMINE MESYLATE
CHEMBL1200517
Approved 1946
Assay Landscape

Assay Landscape

1,664
Total Assays
5,595
Tested Compounds
4
Assay Types
Binding — 1,194 assays, 5,595 compounds
BAO Format Assays Compounds Avg pChEMBL
single protein format 671 1,668 7.2
cell-based format 417 2,989 7.5
tissue-based format 43 163 7.5
assay format 37 593 8.2
cell membrane format 24 147 7.1
organism-based format 2 35 8.0
Functional — 460 assays, 976 compounds
BAO Format Assays Compounds Avg pChEMBL
cell-based format 309 586 7.6
assay format 130 286 7.5
single protein format 11 87 7.5
cell membrane format 6 7 7.5
organism-based format 2 0
tissue-based format 2 10 6.5
ADME — 9 assays, 9 compounds
BAO Format Assays Compounds Avg pChEMBL
cell-based format 4 3 5.7
single protein format 3 0
cell membrane format 2 6 6.5
Toxicity — 1 assays, 0 compounds
BAO Format Assays Compounds Avg pChEMBL
cell-based format 1 0

Confidence Score Distribution

Source · ChEMBL 36 via Core Engine