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Target Snapshot

CHEMBL4654 Target Snapshot

Histamine H2 receptor · SINGLE PROTEIN · Rattus norvegicus

132Compounds
25Assays
2Approved Drugs
99.0Activities
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

Protein identity stays anchored to UniProt P25102. Use UniProt P25102 as the stable identity anchor, then attach disease evidence before program review.

Review focus
Protein anchor ready

Use UniProt P25102 as the stable identity anchor, then attach disease evidence before program review.

ChEMBL component mapping + Open Targets-ready proxy + ChEMBL 36 via Core Engine 2026-09-13
Open source guide
Identity Layer

Cross-source identity

Keep the review anchor, source IDs, and context contract aligned before reusing this target elsewhere.

This review treats Histamine H2 receptor as ChEMBL target CHEMBL4654, mapped to UniProt P25102. Disease framing currently uses the Open Targets-ready proxy contract.

Review anchor
Histamine H2 receptor
SINGLE PROTEIN · Rattus norvegicus
As of 2026-09-13
ChEMBL target ID
CHEMBL4654
Primary anchor for compounds, assays, approvals, and exports
ChEMBL 36 via Core Engine As of 2026-09-13
www.ebi.ac.uk
UniProt accession
P25102
Histamine H2 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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UniProt Target Context
UniProt accession via ChEMBL component mapping

Start here when your first question is whether Histamine H2 receptor is the right protein anchor across sources, using UniProt P25102 as the stable mapping.

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Disease Relevance & Evidence Level
ChEMBL drug mechanism + indication proxy

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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 H2 receptor
UniProt AccessionP25102
Component TypeProtein
Sequence Length358 aa

Histamine H2 receptor

Source · UniProt accession via ChEMBL component mapping
Review Cue

How to read this target

Review this target as Histamine H2 receptor, mapped to UniProt P25102. Sequence length is 358 aa.

Mapped IDP25102
Review nameHistamine H2 receptor
OrganismRattus norvegicus
Clinical Profile

Clinical Phase Distribution

2
Approved
1
Phase II
Assay Mix

Activity Type Distribution

IC5025.0
KI3.0
EC5022.0
KD49.0
Lead Set

Top Inhibitors (by pChEMBL)

ChEMBL IDpChEMBLTypeValue (nM)Phase
CHEMBL285556 7.8 Kd 15.85 Preclinical
CHEMBL284374 7.3 Kd 50.12 Preclinical
CHEMBL33398 6.8 Kd 158.49 Preclinical
CHEMBL33698 6.6 Kd 251.19 Preclinical
CHEMBL265987 6.6 Kd 251.19 Preclinical
CHEMBL30 6.6 Kd 251.19 Approved
CHEMBL285719 6.5 Kd 316.23 Preclinical
CHEMBL406844 6.5 Kd 316.23 Preclinical
CHEMBL282645 6.5 Kd 316.23 Preclinical
CHEMBL30917 6.4 Kd 398.11 Preclinical
Distribution

pChEMBL Value Distribution

5
5.0
5
5.5
21
6.0
8
6.5
1
7.0
1
7.5
0
8.0
0
8.5
0
9.0
0
9.5
pChEMBL
Approved Drugs

Approved Drugs

CIMETIDINE
CHEMBL30
Approved 1977
Assay Landscape

Assay Landscape

25
Total Assays
39
Tested Compounds
2
Assay Types
Binding — 13 assays, 26 compounds
BAO Format Assays Compounds Avg pChEMBL
single protein format 10 23 4.3
cell-based format 2 3 5.0
tissue-based format 1 0
Functional — 12 assays, 39 compounds
BAO Format Assays Compounds Avg pChEMBL
organism-based format 10 0
assay format 2 39 6.2

Confidence Score Distribution

Source · ChEMBL 36 via Core Engine