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Target Snapshot

CHEMBL264 Target Snapshot

Histamine H3 receptor · SINGLE PROTEIN · Homo sapiens

7,468Compounds
876Assays
20Approved Drugs
6,943.0Activities
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

Histamine H3 receptor shows approved-linked disease relevance led by narcolepsy-cataplexy syndrome. 5 more disease programs remain visible in the same review block. 2 linked drugs keep the current disease frame grounded. Protein identity stays anchored to UniProt Q9Y5N1. Start with narcolepsy-cataplexy syndrome, then reuse UniProt Q9Y5N1 as the stable protein anchor across project notes and exports.

Review focus
Review-ready target frame

Start with narcolepsy-cataplexy syndrome, then reuse UniProt Q9Y5N1 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 2 linked drugs
Open source guide
Disease program
narcolepsy-cataplexy syndrome

Histamine H3 receptor shows approved-linked disease relevance led by narcolepsy-cataplexy syndrome. 5 more disease programs remain visible in the same review block. 2 linked drugs remain visible in the same block.

Start review with narcolepsy-cataplexy syndrome because it currently carries approved-linked support. Linked drugs include PITOLISANT, PITOLISANT HYDROCHLORIDE. 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 2 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 H3 receptor as ChEMBL target CHEMBL264, mapped to UniProt Q9Y5N1. Disease framing currently uses the Open Targets-ready proxy contract.

Review anchor
Histamine H3 receptor
SINGLE PROTEIN · Homo sapiens
As of 2026-09-13
ChEMBL target ID
CHEMBL264
Primary anchor for compounds, assays, approvals, and exports
ChEMBL 36 via Core Engine As of 2026-09-13
www.ebi.ac.uk
UniProt accession
Q9Y5N1
Histamine H3 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

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Choose the first block or source based on the question you are trying to answer.

Need stable target naming and protein identity?
UniProt Target Context
UniProt accession via ChEMBL component mapping

Start here when your first question is whether Histamine H3 receptor is the right protein anchor across sources, using UniProt Q9Y5N1 as the stable mapping.

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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 narcolepsy-cataplexy syndrome is currently framed as approved-linked support. It currently carries 2 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 LabelHistamine H3 receptor
UniProt AccessionQ9Y5N1
Component TypeProtein
Sequence Length445 aa

Histamine H3 receptor

Source · UniProt accession via ChEMBL component mapping
Review Cue

How to read this target

Review this target as Histamine H3 receptor, mapped to UniProt Q9Y5N1. Sequence length is 445 aa.

Mapped IDQ9Y5N1
Review nameHistamine H3 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 H3 receptor shows approved-linked disease relevance led by narcolepsy-cataplexy syndrome. 5 more disease programs remain visible in the same review block.

Approved-linked Approved
narcolepsy-cataplexy syndrome
2 linked drugs · 2 direct · 2 efficacy
Linked drugPITOLISANT
Linked drugPITOLISANT HYDROCHLORIDE
Approved-linked Approved
obstructive sleep apnea
2 linked drugs · 2 direct · 2 efficacy
Linked drugMK-0249
Linked drugPITOLISANT HYDROCHLORIDE
Approved-linked Approved
hypersomnia
1 linked drug · 1 direct · 1 efficacy
Linked drugPITOLISANT HYDROCHLORIDE
Approved-linked Approved
Vertigo
1 linked drug · 1 direct · 1 efficacy
Linked drugBETAHISTINE
Late clinical Phase III
narcolepsy
4 linked drugs · 4 direct · 4 efficacy
Linked drugGSK189254
Linked drugJNJ-17216498
Linked drugPITOLISANT
Linked drugSUVN-G3031
Late clinical Phase III
idiopathic hypersomnia
1 linked drug · 1 direct · 1 efficacy
Linked drugPITOLISANT
Source · ChEMBL drug mechanism + indication proxy
Review Cue

How to read disease relevance

Start review with narcolepsy-cataplexy syndrome because it currently carries approved-linked support. Linked drugs include PITOLISANT, PITOLISANT HYDROCHLORIDE. This disease block keeps the Open Targets-ready contract explicit while current evidence comes from ChEMBL mechanism and indication mappings.

Lead diseasenarcolepsy-cataplexy syndrome
Strongest levelApproved-linked
Block modeOpen Targets-ready proxy
Clinical Profile

Clinical Phase Distribution

20
Approved
1
Phase III
22
Phase II
Assay Mix

Activity Type Distribution

IC501,022.0
KI5,133.0
EC50485.0
KD303.0
Lead Set

Top Inhibitors (by pChEMBL)

ChEMBL IDpChEMBLTypeValue (nM)Phase
CHEMBL272077 10.72 Kd 0.01905 Preclinical
CHEMBL401683 10.7 Kd 0.01995 Preclinical
CHEMBL258349 10.65 Kd 0.02239 Preclinical
CHEMBL3094128 10.6 Ki 0.02512 Preclinical
CHEMBL3753475 10.52 Ki 0.03 Preclinical
CHEMBL508712 10.51 Ki 0.03125 Preclinical
CHEMBL257208 10.44 Kd 0.03631 Preclinical
CHEMBL18661 10.4 EC50 0.03981 Preclinical
CHEMBL272699 10.4 Kd 0.03981 Preclinical
CHEMBL455288 10.38 Ki 0.042 Preclinical
Distribution

pChEMBL Value Distribution

188
5.0
248
5.5
404
6.0
565
6.5
868
7.0
923
7.5
1044
8.0
988
8.5
689
9.0
296
9.5
pChEMBL
Approved Drugs

Approved Drugs

PITOLISANT HYDROCHLORIDE
CHEMBL4164059
Approved 2016
PITOLISANT
CHEMBL462605
Approved 2016
HISTAMINE DIHYDROCHLORIDE
CHEMBL1533310
Approved 2008
PLERIXAFOR
CHEMBL18442
Approved 2008
MELATONIN
CHEMBL45
Approved 2007
DONEPEZIL
CHEMBL502
Approved 1996
AZELASTINE
CHEMBL639
Approved 1996
CLOZAPINE
CHEMBL42
Approved 1989
DECAMETHONIUM
CHEMBL1190
Approved 1982
HISTAMINE
CHEMBL90
Approved 1939
Assay Landscape

Assay Landscape

876
Total Assays
3,917
Tested Compounds
3
Assay Types
Binding — 641 assays, 3,917 compounds
BAO Format Assays Compounds Avg pChEMBL
cell-based format 314 2,401 7.7
single protein format 297 1,184 7.8
assay format 16 203 7.6
cell membrane format 11 128 6.6
tissue-based format 2 0
organism-based format 1 1 7.4
Functional — 231 assays, 1,380 compounds
BAO Format Assays Compounds Avg pChEMBL
cell-based format 154 922 8.2
assay format 70 450 8.0
cell membrane format 3 6 9.2
organism-based format 2 0
single protein format 2 2 8.9
ADME — 4 assays, 1 compounds
BAO Format Assays Compounds Avg pChEMBL
cell-based format 3 1 6.0
single protein format 1 0

Confidence Score Distribution

Source · ChEMBL 36 via Core Engine