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Evidence Snapshot

Histamine H3 receptor

CHEMBL264 SINGLE PROTEIN Homo sapiens
Source Header

ChEMBL 36 via Core Engine

Target Snapshot 2026-09-13T21:24:35Z
Source · ChEMBL 36 via Core Engine
ChEMBL ChEMBL 36 CHEMBL264
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.

Review-ready Target Rationale

Why Histamine H3 receptor matters

As of 2026-09-13

Histamine H3 receptor is reviewed as Histamine H3 receptor (UniProt Q9Y5N1); 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 this evidence frame grounded.; the current evidence base includes 20 approved drugs, 7468 compounds, and 876 assays, with lead potency reaching pChEMBL 10.7.

Disease context
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 keep the rationale reviewable. 5 additional disease programs remain visible in the same card. Linked drugs include PITOLISANT, PITOLISANT HYDROCHLORIDE.

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.

ChEMBL target record
Approved-linked 2 linked drugs
Activity base
Portfolio and assay base

ChEMBL currently tracks 20 approved drugs, 7468 compounds, and 876 assays for this target. The dominant activity type is KI. CHEMBL272077 is the current potency anchor at pChEMBL 10.7.

Use CHEMBL272077 as the tractability anchor when discussing potency (pChEMBL 10.7).

Activity source · ChEMBL 36 via Core Engine
20 approved pChEMBL 10.7
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 Histamine H3 receptor 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 Q9Y5N1, 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 narcolepsy-cataplexy syndrome is currently treated as approved-linked support.

Open Disease Context

Snapshot State

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

7468
Total Compounds
876
Total Assays
20
Approved Drugs
IC50: 1022.0, KI: 5133.0, EC50: 485.0, KD: 303.0
Activity Types

pChEMBL Activity Distribution

Top 5 Inhibitors (by pChEMBL)

Structure Compound pChEMBL Type Phase
No preferred name
CHEMBL272077
 10.7 Kd —
No preferred name
CHEMBL401683
 10.7 Kd —
No preferred name
CHEMBL258349
 10.7 Kd —
No preferred name
CHEMBL3094128
 10.6 Ki —
No preferred name
CHEMBL3753475
 10.5 Ki —

Approved Drugs

Structure Compound First Approval
PITOLISANT HYDROCHLORIDE
CHEMBL4164059
 2016
PITOLISANT
CHEMBL462605
 2016
HISTAMINE DIHYDROCHLORIDE
CHEMBL1533310
 2008
PLERIXAFOR
CHEMBL18442
 2008
MELATONIN
CHEMBL45
 2007
DONEPEZIL
CHEMBL502
 1996
AZELASTINE
CHEMBL639
 1996
CLOZAPINE
CHEMBL42
 1989
DECAMETHONIUM
CHEMBL1190
 1982
HISTAMINE
CHEMBL90
 1939
← Target Page
Source Header

ChEMBL 36 via Core Engine

Target Snapshot 2026-09-13T21:24:35Z
Source · ChEMBL 36 via Core Engine
ChEMBL ChEMBL 36 CHEMBL264