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Evidence Snapshot

Histamine H1 receptor

CHEMBL231 SINGLE PROTEIN Homo sapiens
Source Header

ChEMBL 36 via Core Engine

Target Snapshot 2026-09-13T10:19:16Z
Source · ChEMBL 36 via Core Engine
ChEMBL ChEMBL 36 CHEMBL231
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.

Review-ready Target Rationale

Why Histamine H1 receptor matters

As of 2026-09-13

Histamine H1 receptor is reviewed as Histamine H1 receptor (UniProt P35367); 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 this evidence frame grounded.; the current evidence base includes 140 approved drugs, 5025 compounds, and 832 assays, with lead potency reaching pChEMBL 10.8.

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

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.

ChEMBL target record
Approved-linked 24 linked drugs
Activity base
Portfolio and assay base

ChEMBL currently tracks 140 approved drugs, 5025 compounds, and 832 assays for this target. The dominant activity type is KI. CHEMBL511 is the current potency anchor at pChEMBL 10.8.

Use CHEMBL511 as the tractability anchor when discussing potency (pChEMBL 10.8).

Activity source · ChEMBL 36 via Core Engine
140 approved pChEMBL 10.8
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 H1 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 P35367, 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 allergic disease is currently treated as approved-linked support.

Open Disease Context

Snapshot State

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

5025
Total Compounds
832
Total Assays
140
Approved Drugs
IC50: 1296.0, KI: 2834.0, EC50: 84.0, KD: 197.0
Activity Types

pChEMBL Activity Distribution

Top 5 Inhibitors (by pChEMBL)

Structure Compound pChEMBL Type Phase
No preferred name
CHEMBL511
 10.8 IC50 Approved
No preferred name
CHEMBL2146802
 10.4 Kd —
No preferred name
CHEMBL1626
 10.3 Ki Approved
No preferred name
CHEMBL1628227
 10.2 Ki Approved
No preferred name
CHEMBL715
 10.1 Kd Approved

Approved Drugs

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

ChEMBL 36 via Core Engine

Target Snapshot 2026-09-13T10:19:16Z
Source · ChEMBL 36 via Core Engine
ChEMBL ChEMBL 36 CHEMBL231