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Target Snapshot

CHEMBL231 Target Snapshot

Histamine H1 receptor · SINGLE PROTEIN · Homo sapiens

5,025Compounds
832Assays
140Approved Drugs
4,411.0Activities
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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

Histamine H1 receptor shows approved-linked disease relevance led by allergic disease. 5 more disease programs remain visible in the same review block. 24 linked drugs keep the current disease frame grounded. Protein identity stays anchored to UniProt P35367. Start with allergic disease, then reuse UniProt P35367 as the stable protein anchor across project notes and exports.

Review focus
Review-ready target frame

Start with allergic disease, then reuse UniProt P35367 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 24 linked drugs
Open source guide
Disease program
allergic disease

Histamine H1 receptor shows approved-linked disease relevance led by allergic disease. 5 more disease programs remain visible in the same review block. 24 linked drugs remain visible in the same block.

Start review with allergic disease because it currently carries approved-linked support. Linked drugs include ACRIVASTINE, ASTEMIZOLE, BILASTINE, BROMPHENIRAMINE MALEATE. 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 24 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 Histamine H1 receptor as ChEMBL target CHEMBL231, mapped to UniProt P35367. Disease framing currently uses the Open Targets-ready proxy contract.

Review anchor
Histamine H1 receptor
SINGLE PROTEIN · Homo sapiens
As of 2026-09-13
ChEMBL target ID
CHEMBL231
Primary anchor for compounds, assays, approvals, and exports
ChEMBL 36 via Core Engine As of 2026-09-13
www.ebi.ac.uk
UniProt accession
P35367
Histamine H1 receptor
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

Start with the right source

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UniProt Target Context
UniProt accession via ChEMBL component mapping

Start here when your first question is whether Histamine H1 receptor is the right protein anchor across sources, using UniProt P35367 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 allergic disease is currently framed as approved-linked support. It currently carries 24 linked drugs in the same disease frame.

Jump to Disease Context
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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 LabelHistamine H1 receptor
UniProt AccessionP35367
Component TypeProtein
Sequence Length487 aa

Histamine H1 receptor

Source · UniProt accession via ChEMBL component mapping
Review Cue

How to read this target

Review this target as Histamine H1 receptor, mapped to UniProt P35367. Sequence length is 487 aa.

Mapped IDP35367
Review nameHistamine H1 receptor
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

Histamine H1 receptor shows approved-linked disease relevance led by allergic disease. 5 more disease programs remain visible in the same review block.

Approved-linked Approved
allergic disease
24 linked drugs · 24 direct · 24 efficacy
Linked drugACRIVASTINE
Linked drugASTEMIZOLE
Linked drugBILASTINE
Linked drugBROMPHENIRAMINE MALEATE
Approved-linked Approved
seasonal allergic rhinitis
20 linked drugs · 20 direct · 20 efficacy
Linked drugAZELASTINE HYDROCHLORIDE
Linked drugBILASTINE
Linked drugBROMPHENIRAMINE MALEATE
Linked drugCARBINOXAMINE MALEATE
Approved-linked Approved
allergic conjunctivitis
14 linked drugs · 14 direct · 14 efficacy
Linked drugALCAFTADINE
Linked drugAZELASTINE HYDROCHLORIDE
Linked drugBEPOTASTINE BESYLATE
Linked drugBILASTINE
Approved-linked Approved
urticaria
14 linked drugs · 14 direct · 14 efficacy
Linked drugBILASTINE
Linked drugCARBINOXAMINE MALEATE
Linked drugCETIRIZINE HYDROCHLORIDE
Linked drugCLEMASTINE FUMARATE
Approved-linked Approved
Rhinitis, Allergic, Perennial
12 linked drugs · 12 direct · 12 efficacy
Linked drugAZELASTINE HYDROCHLORIDE
Linked drugBEPOTASTINE BESYLATE
Linked drugBILASTINE
Linked drugCARBINOXAMINE MALEATE
Approved-linked Approved
allergic rhinitis
11 linked drugs · 11 direct · 11 efficacy
Linked drugAZELASTINE HYDROCHLORIDE
Linked drugCETIRIZINE HYDROCHLORIDE
Linked drugCHLORPHENIRAMINE MALEATE
Linked drugDESLORATADINE
Source · ChEMBL drug mechanism + indication proxy
Review Cue

How to read disease relevance

Start review with allergic disease because it currently carries approved-linked support. Linked drugs include ACRIVASTINE, ASTEMIZOLE, BILASTINE, BROMPHENIRAMINE MALEATE. This disease block keeps the Open Targets-ready contract explicit while current evidence comes from ChEMBL mechanism and indication mappings.

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

Clinical Phase Distribution

140
Approved
8
Phase III
28
Phase II
1
Phase I
Assay Mix

Activity Type Distribution

IC501,296.0
KI2,834.0
EC5084.0
KD197.0
Lead Set

Top Inhibitors (by pChEMBL)

ChEMBL IDpChEMBLTypeValue (nM)Phase
CHEMBL511 10.85 IC50 0.014 Approved
CHEMBL2146802 10.4 Kd 0.03981 Preclinical
CHEMBL1626 10.31 Ki 0.049 Approved
CHEMBL1628227 10.18 Ki 0.066 Approved
CHEMBL715 10.06 Kd 0.087 Approved
CHEMBL2146806 10.0 Kd 0.1 Preclinical
CHEMBL1767136 10.0 Kd 0.1 Preclinical
CHEMBL5284242 10.0 Kd 0.1 Preclinical
CHEMBL1767137 10.0 Ki 0.1 Preclinical
CHEMBL5275284 9.88 Kd 0.1318 Preclinical
Distribution

pChEMBL Value Distribution

213
5.0
242
5.5
298
6.0
250
6.5
268
7.0
253
7.5
303
8.0
153
8.5
101
9.0
37
9.5
pChEMBL
Approved Drugs

Approved Drugs

BREXPIPRAZOLE
CHEMBL2105760
Approved 2015
CARIPRAZINE HYDROCHLORIDE
CHEMBL2024517
Approved 2015
CARIPRAZINE
CHEMBL2028019
Approved 2015
VILAZODONE HYDROCHLORIDE
CHEMBL1615374
Approved 2011
ASENAPINE
CHEMBL3187365
Approved 2009
LEVOCETIRIZINE DIHYDROCHLORIDE
CHEMBL1201190
Approved 2007
PALIPERIDONE
CHEMBL1621
Approved 2006
TIOTROPIUM BROMIDE
CHEMBL3545181
Approved 2004
ARIPIPRAZOLE
CHEMBL1112
Approved 2002
ZIPRASIDONE
CHEMBL708
Approved 2001
RUPATADINE
CHEMBL91397
Approved 2001
DESLORATADINE
CHEMBL1172
Approved 2001
KETOTIFEN
CHEMBL534
Approved 1999
KETOTIFEN FUMARATE
CHEMBL1633
Approved 1999
CITALOPRAM
CHEMBL549
Approved 1998
MIZOLASTINE
CHEMBL94454
Approved 1998
TOLTERODINE TARTRATE
CHEMBL1722209
Approved 1998
QUETIAPINE
CHEMBL716
Approved 1997
PRAMIPEXOLE
CHEMBL301265
Approved 1997
SERTINDOLE
CHEMBL12713
Approved 1996
OLANZAPINE
CHEMBL715
Approved 1996
AZELASTINE
CHEMBL639
Approved 1996
FEXOFENADINE
CHEMBL914
Approved 1996
MIRTAZAPINE
CHEMBL654
Approved 1996
FEXOFENADINE HYDROCHLORIDE
CHEMBL1200618
Approved 1996
AZELASTINE HYDROCHLORIDE
CHEMBL1200809
Approved 1996
CETIRIZINE
CHEMBL1000
Approved 1995
NEFAZODONE HYDROCHLORIDE
CHEMBL1200492
Approved 1994
LORATADINE
CHEMBL998
Approved 1993
RISPERIDONE
CHEMBL85
Approved 1993
EBASTINE
CHEMBL305660
Approved 1990
CLOMIPRAMINE
CHEMBL415
Approved 1989
CLOZAPINE
CHEMBL42
Approved 1989
ASTEMIZOLE
CHEMBL296419
Approved 1988
TERFENADINE
CHEMBL17157
Approved 1985
TRIPROLIDINE
CHEMBL855
Approved 1982
CYCLIZINE
CHEMBL648
Approved 1982
TRAZODONE
CHEMBL621
Approved 1981
DEXCHLORPHENIRAMINE
CHEMBL1201353
Approved 1981
AMOXAPINE
CHEMBL1113
Approved 1980
MAPROTILINE
CHEMBL21731
Approved 1980
CLEMASTINE
CHEMBL1626
Approved 1977
PYRILAMINE
CHEMBL511
Approved 1973
DIMENHYDRINATE
CHEMBL1200406
Approved 1972
DROPERIDOL
CHEMBL1108
Approved 1970
DOXEPIN
CHEMBL1628227
Approved 1969
HALOPERIDOL
CHEMBL54
Approved 1967
CHLORPROTHIXENE
CHEMBL908
Approved 1967
NORTRIPTYLINE
CHEMBL445
Approved 1964
THIORIDAZINE
CHEMBL479
Approved 1962
Assay Landscape

Assay Landscape

832
Total Assays
1,456
Tested Compounds
3
Assay Types
Binding — 702 assays, 1,456 compounds
BAO Format Assays Compounds Avg pChEMBL
single protein format 505 589 6.8
cell-based format 178 637 7.1
cell membrane format 10 146 6.9
assay format 6 82 5.7
tissue-based format 3 2 8.2
Functional — 113 assays, 349 compounds
BAO Format Assays Compounds Avg pChEMBL
cell-based format 66 208 7.7
assay format 38 128 7.1
tissue-based format 8 0
organism-based format 1 13 5.8
ADME — 17 assays, 42 compounds
BAO Format Assays Compounds Avg pChEMBL
single protein format 11 41 6.5
cell-based format 6 1 7.0

Confidence Score Distribution

Source · ChEMBL 36 via Core Engine