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Target Snapshot

CHEMBL1941 Target Snapshot

Histamine H2 receptor · SINGLE PROTEIN · Homo sapiens

3,142Compounds
500Assays
91Approved Drugs
2,787.0Activities
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 H2 receptor shows approved-linked disease relevance led by gastroesophageal reflux disease. 5 more disease programs remain visible in the same review block. 6 linked drugs keep the current disease frame grounded. Protein identity stays anchored to UniProt P25021. Start with gastroesophageal reflux disease, then reuse UniProt P25021 as the stable protein anchor across project notes and exports.

Review focus
Review-ready target frame

Start with gastroesophageal reflux disease, then reuse UniProt P25021 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 6 linked drugs
Open source guide
Disease program
gastroesophageal reflux disease

Histamine H2 receptor shows approved-linked disease relevance led by gastroesophageal reflux disease. 5 more disease programs remain visible in the same review block. 6 linked drugs remain visible in the same block.

Start review with gastroesophageal reflux disease because it currently carries approved-linked support. Linked drugs include CIMETIDINE, FAMOTIDINE, LAFUTIDINE, NIZATIDINE. 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 6 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 H2 receptor as ChEMBL target CHEMBL1941, mapped to UniProt P25021. Disease framing currently uses the Open Targets-ready proxy contract.

Review anchor
Histamine H2 receptor
SINGLE PROTEIN · Homo sapiens
As of 2026-09-13
ChEMBL target ID
CHEMBL1941
Primary anchor for compounds, assays, approvals, and exports
ChEMBL 36 via Core Engine As of 2026-09-13
www.ebi.ac.uk
UniProt accession
P25021
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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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 H2 receptor is the right protein anchor across sources, using UniProt P25021 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 gastroesophageal reflux disease is currently framed as approved-linked support. It currently carries 6 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 H2 receptor
UniProt AccessionP25021
Component TypeProtein
Sequence Length359 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 P25021. Sequence length is 359 aa.

Mapped IDP25021
Review nameHistamine H2 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 H2 receptor shows approved-linked disease relevance led by gastroesophageal reflux disease. 5 more disease programs remain visible in the same review block.

Approved-linked Approved
gastroesophageal reflux disease
6 linked drugs · 6 direct · 6 efficacy
Linked drugCIMETIDINE
Linked drugFAMOTIDINE
Linked drugLAFUTIDINE
Linked drugNIZATIDINE
Approved-linked Approved
Peptic ulcer
6 linked drugs · 6 direct · 6 efficacy
Linked drugCIMETIDINE
Linked drugFAMOTIDINE
Linked drugLAFUTIDINE
Linked drugNIZATIDINE
Approved-linked Approved
duodenal ulcer
4 linked drugs · 4 direct · 4 efficacy
Linked drugCIMETIDINE
Linked drugFAMOTIDINE
Linked drugNIZATIDINE
Linked drugRANITIDINE HYDROCHLORIDE
Approved-linked Approved
dyspepsia
4 linked drugs · 4 direct · 4 efficacy
Linked drugCIMETIDINE
Linked drugFAMOTIDINE
Linked drugNIZATIDINE
Linked drugRANITIDINE HYDROCHLORIDE
Approved-linked Approved
gastric ulcer
4 linked drugs · 4 direct · 4 efficacy
Linked drugFAMOTIDINE
Linked drugLAFUTIDINE
Linked drugRANITIDINE
Linked drugRANITIDINE HYDROCHLORIDE
Approved-linked Approved
ulcer disease
3 linked drugs · 3 direct · 3 efficacy
Linked drugCIMETIDINE
Linked drugFAMOTIDINE
Linked drugRANITIDINE HYDROCHLORIDE
Source · ChEMBL drug mechanism + indication proxy
Review Cue

How to read disease relevance

Start review with gastroesophageal reflux disease because it currently carries approved-linked support. Linked drugs include CIMETIDINE, FAMOTIDINE, LAFUTIDINE, NIZATIDINE. This disease block keeps the Open Targets-ready contract explicit while current evidence comes from ChEMBL mechanism and indication mappings.

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

Clinical Phase Distribution

91
Approved
7
Phase III
8
Phase II
Assay Mix

Activity Type Distribution

IC50935.0
KI1,530.0
EC50248.0
KD74.0
Lead Set

Top Inhibitors (by pChEMBL)

ChEMBL IDpChEMBLTypeValue (nM)Phase
CHEMBL194837 9.06 IC50 0.87 Preclinical
CHEMBL1627 8.77 Ki 1.7 Preclinical
CHEMBL5276441 8.7 Ki 2.0 Preclinical
CHEMBL4875600 8.69 Ki 2.042 Preclinical
CHEMBL5207281 8.52 Ki 3.02 Preclinical
CHEMBL5206565 8.48 EC50 3.311 Preclinical
CHEMBL4860528 8.35 Ki 4.467 Preclinical
CHEMBL1090526 8.35 Ki 4.5 Preclinical
CHEMBL5173079 8.32 Ki 4.786 Preclinical
CHEMBL5178472 8.31 EC50 4.898 Preclinical
Distribution

pChEMBL Value Distribution

153
5.0
162
5.5
133
6.0
115
6.5
89
7.0
104
7.5
24
8.0
4
8.5
1
9.0
0
9.5
pChEMBL
Approved Drugs

Approved Drugs

ASENAPINE MALEATE
CHEMBL3544974
Approved 2009
PRAMIPEXOLE
CHEMBL301265
Approved 1997
FAMOTIDINE
CHEMBL902
Approved 1986
RANITIDINE
CHEMBL1790041
Approved 1983
MAPROTILINE
CHEMBL21731
Approved 1980
SULOCTIDIL
CHEMBL404849
Approved 1979
CIMETIDINE
CHEMBL30
Approved 1977
CLEMASTINE
CHEMBL1626
Approved 1977
THIORIDAZINE
CHEMBL479
Approved 1962
CYPROHEPTADINE
CHEMBL516
Approved 1961
AMITRIPTYLINE
CHEMBL629
Approved 1961
HISTAMINE
CHEMBL90
Approved 1939
Assay Landscape

Assay Landscape

500
Total Assays
587
Tested Compounds
3
Assay Types
Binding — 422 assays, 587 compounds
BAO Format Assays Compounds Avg pChEMBL
single protein format 315 220 5.5
cell-based format 97 115 6.2
cell membrane format 7 199 6.5
assay format 2 53 4.6
tissue-based format 1 0
Functional — 73 assays, 145 compounds
BAO Format Assays Compounds Avg pChEMBL
cell-based format 50 105 6.7
assay format 16 4 5.9
cell membrane format 7 36 6.9
ADME — 5 assays, 3 compounds
BAO Format Assays Compounds Avg pChEMBL
cell-based format 4 3 6.2
single protein format 1 0

Confidence Score Distribution

Source · ChEMBL 36 via Core Engine