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Atlas / Drug / Histamine

Histamine

drug
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Also known as .beta.-aminoethylglyoxalineErgamineErgotidineNSC-33792SID11111275SID26753351SID26753352SID8139979SID90341171SID104171171SID124880328SID170465001SID144203717[3H]Histamine[3H]-HistamineHistamine dihydrochlorideÊHistamine dihydrochlorideÂ

Summary

Histamine (CHEMBL90) is an approved small-molecule neurotransmitter targeting CA1, HRH1, and HRH2; indicated across 10 conditions including pterygium and osteoarthritis, knee.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • Targets: 7 (CA1, HRH1, HRH2…)
  • Indications: 10 conditions
  • Clinical trials: 36
  • Chemistry: 111.15 Da · C5H9N3

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL90
NameHistamine
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID774
ChEBICHEBI:18295
Molecular formulaC5H9N3
Molecular weight111.15
InChIKeyNTYJJOPFIAHURM-UHFFFAOYSA-N

SMILES: C1=C(NC=N1)CCN

IUPAC name: 2-(1H-imidazol-5-yl)ethanamine

ChEBI definition: A member of the class of imidazoles that is 1H-imidazole substituted at position C-4 by a 2-aminoethyl group.

Pharmacological roles (ChEBI): neurotransmitter.

Other ChEBI roles (chemical / environmental): human metabolite, mouse metabolite.

Also known as: .beta.-aminoethylglyoxaline, Ergamine, Ergotidine, Histamine, NSC-33792, histamine, SID11111275, SID26753351, SID26753352, SID8139979, SID90341171, SID104171171

Parent form; salt/anhydrous children: CHEMBL544208, CHEMBL535166, CHEMBL1533310, CHEMBL3989520

Patent coverage: 66,050 distinct patent families (169,677 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 169,200 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
CA1carbonic anhydrase 1Activation0%P00915
HRH1H1 receptorFull agonist5.90%P35367
HRH2H2 receptorFull agonist3.8P25021
HRH3H3 receptorFull agonist8.30.5%Q9Y5N1
HRH4H4 receptorFull agonist8.30%Q9H3N8
CA7carbonic anhydrase 7Activation1.6%P43166
CA5Acarbonic anhydrase 5AActivation29.6%P35218

Broader ChEMBL bioactivity targets: 17 (assay-derived). Sample: Prelamin-A/C, 4’-phosphopantetheinyl transferase ffp, Histamine H2 receptor, Thyrotropin receptor, Beta-lactamase, Macrophage migration inhibitory factor, Histamine H1 receptor, Histamine H3 receptor, Histamine H2 receptor, Histamine H3 receptor.

Bioactivity

ChEMBL activities: 162 potent at pChembl ≥ 5 of 179 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
Q9JI359.84Ki0.14nMCHEMBL_ACT_971259
P313899.11Kd0.78nMCHEMBL_ACT_277694
P313899.11Kd0.78nMCHEMBL_ACT_681572
P313899.07Kd0.85nMCHEMBL_ACT_277690
P313899.07Kd0.85nMCHEMBL_ACT_681570
P313899Kd1nMCHEMBL_ACT_1148003
HRH49Ki1nMCHEMBL_ACT_22485408
P313899Kd1nMCHEMBL_ACT_681574
HRH48.8Ki1.6nMCHEMBL_ACT_16766681
HRH38.6EC502.51nMCHEMBL_ACT_19054808
HRH38.6Ki2.51nMCHEMBL_ACT_22485425
HRH38.52Kd3nMCHEMBL_ACT_24864949
HRH38.4EC504nMCHEMBL_ACT_22472425
HRH38.39EC504.07nMCHEMBL_ACT_997564
HRH18.35Kd4.5nMCHEMBL_ACT_24864807
HRH48.32Ki4.8nMCHEMBL_ACT_15742102
HRH48.3Kd5nMCHEMBL_ACT_18972948
HRH38.3EC505.01nMCHEMBL_ACT_19054887
HRH38.3EC505.01nMCHEMBL_ACT_5100536
HRH38.28Ki5.2nMCHEMBL_ACT_3297785
Q9QYN88.2Ki6.31nMCHEMBL_ACT_565755
HRH38.2Ki6.31nMCHEMBL_ACT_7956247
HRH48.13EC507.41nMCHEMBL_ACT_18972952
HRH48.1Ki7.94nMCHEMBL_ACT_1454475
HRH48.1Ki8nMCHEMBL_ACT_15742107
HRH48.1EC507.94nMCHEMBL_ACT_16441243
HRH48.1Ki7.94nMCHEMBL_ACT_5100496
HRH48.05Ki9nMCHEMBL_ACT_7982165
HRH38.04AC509.1nMCHEMBL_ACT_25199640
HRH48.04EC509.12nMCHEMBL_ACT_3286686

Target pathways

Aggregated over 7 target gene(s): CA1, HRH1, HRH2, HRH3, HRH4, CA7, CA5A.

Top Reactome pathways

16 total, by targets touching each:

PathwayTargetsGenes
Histamine receptors4HRH1, HRH2, HRH3, HRH4
Metabolism3CA1, CA5A, CA7
Reversible hydration of carbon dioxide3CA1, CA5A, CA7
Erythrocytes take up carbon dioxide and release oxygen1CA1
Erythrocytes take up oxygen and release carbon dioxide1CA1
Cytokine Signaling in Immune system1CA1
O2/CO2 exchange in erythrocytes1CA1
Immune System1CA1
Transport of small molecules1CA1
G alpha (q) signalling events1HRH1
G alpha (s) signalling events1HRH2
G alpha (i) signalling events1HRH4
Interleukin-12 family signaling1CA1
Signaling by Interleukins1CA1
Gene and protein expression by JAK-STAT signaling after Interleukin-12 stimulation1CA1
Interleukin-12 signaling1CA1

Dominant GO biological processes

GO termTargets
G protein-coupled receptor signaling pathway4
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger4
chemical synaptic transmission4
signal transduction4
inflammatory response2
positive regulation of vasoconstriction2
adenylate cyclase-activating G protein-coupled receptor signaling pathway2
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway2
response to fructose1
phospholipase C-activating G protein-coupled receptor signaling pathway1
memory1
visual learning1
regulation of vascular permeability1
regulation of synaptic plasticity1
cellular response to histamine1

Indications & clinical

Indications

10 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
pterygium3MONDO:0005085EFO:0000678
osteoarthritis, knee3MONDO:0005416EFO:0004616
non-Hodgkin lymphoma3MONDO:0018908EFO:0005952
seasonal allergic rhinitis2MONDO:0005324EFO:0003956
allergic rhinitis2MONDO:0011786EFO:0005854
multiple sclerosis2MONDO:0005301MONDO:0005301
asthma1MONDO:0004979MONDO:0004979
allergic disease0MONDO:0005271MONDO:0005271

2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 36.

Phase distribution

PhaseTrials
Not specified29
PHASE24
PHASE12
PHASE31

Top trials by phase / activity

NCTPhaseStatusTitle
NCT01112722PHASE3COMPLETEDApitox, Honeybee Toxin for Pain and Inflammation of Osteoarthritis
NCT00387738PHASE2TERMINATEDEfficacy and Safety Study of TOLAMBA™ in Ragweed-Allergic Adults
NCT00537355PHASE2COMPLETEDAn Evaluation of the Efficacy and Safety of TOLAMBA™ for Ragweed-Allergic Rhinitis in an Environmental Exposure Chamber
NCT00630383PHASE2WITHDRAWNImmunoregulation by Controlled Parasite Exposure in Multiple Sclerosis.
NCT01689363PHASE2COMPLETEDEvaluation of the Allergenicity of AMPHADASE INJECTION (Hyaluronidase Injection USP)
NCT01719133PHASE1COMPLETEDSkin Prick Tests With AllerT in Subjects Allergic to Birch Pollen
NCT01925729PHASE1COMPLETEDTransMEM Gas Exchange – Project 1, Aim 2
NCT06081946Not specifiedRECRUITINGInvestigation of the Effects of Sleep Fragmentation on Itch and Pain Sensitivity
NCT06081998Not specifiedRECRUITINGInvestigation of the Effects of Sleep Deprivation on Itch and Pain Sensitivity
NCT06328530Not specifiedRECRUITINGItch Sensation Induced by Simultaneous Application of Pruritogens (Spatial Summation)
NCT06328543Not specifiedRECRUITINGItch Sensation Induced by Multiple Applications of Pruritogens (temporal Summation)
NCT06340438Not specifiedRECRUITINGInvestigate the Relationship Between Catastrophizing and the Perception of Itch Intensity in Healthy Individuals
NCT06503510Not specifiedRECRUITINGRole of Interleukin-13 Pathways on Pain and Itch Sensitivity
NCT06503523Not specifiedRECRUITINGThe Effects of Performing a Motor Imagery Task on Cortical Excitability During Acute Experimental Muscle Pain and Acute Itch
NCT07122973Not specifiedRECRUITINGTopographical Distribution of Itch and Pain Receptors
NCT07247695Not specifiedRECRUITINGMechanisms Underlying the Placebo Effect in Both Histaminergic and Non-histaminergic Itch
NCT07255092Not specifiedNOT_YET_RECRUITINGMechanisms Underlying the Nocibo Effect of Contagious Itch. in Both Histaminergic and Nonhistaminergic Itch
NCT07395882Not specifiedNOT_YET_RECRUITINGA New Model to Induce Itch and Inflammation
NCT00795496Not specifiedCOMPLETEDBronchial Hyperreactivity in Atopic Dermatitis Patients - a 10 Year Follow-up
NCT01777464Not specifiedTERMINATEDRole of the Central Nervous System in Allergic Rhinitis
NCT01963741Not specifiedCOMPLETEDLeukotriene D4 Nasal Provocation Test in Allergic Rhinitis
NCT03576053Not specifiedCOMPLETEDA Mechanistic Evaluation of the Interactions Between Thermoceptive and Pruriceptive Sensory Processing
NCT03587220Not specifiedCOMPLETEDA Mechanistic Evaluation of the Nociceptive Desensitizing Properties of Topical Capsaicin
NCT03943407Not specifiedWITHDRAWNCharacterization of the Toll-like Receptor 7-agonist Imiquimod 3.75% As a New Surrogate Model of Itch
NCT04058054Not specifiedCOMPLETEDSkin Prick Test of KeraStat® Cream
NCT04115462Not specifiedCOMPLETEDA Relation of Morphine-induced Itch and Pain Processing
NCT04396977Not specifiedCOMPLETEDInter-arm and Inter-period Reproducability of the Dermal Blood Flow Response After a Histamine Skin Prick.
NCT04554888Not specifiedCOMPLETEDCharacterization of New Human Models of Non-histaminergic Itch and Their Interaction With the TRPM8 Receptor
NCT04588532Not specifiedCOMPLETEDCharacterization of BAM8-22 as a New Surrogate Model of Non-histaminergic Itch
NCT04635254Not specifiedCOMPLETEDThe Effect of Halophyte-based Cream on Pain and Itch
NCT04676763Not specifiedCOMPLETEDSubstance P Challenge in Healthy Participants
NCT04700007Not specifiedCOMPLETEDEvaluation of Peripheral Itch Mechanisms Following Injection of Morphine (Second Sub-Project)
NCT04711044Not specifiedCOMPLETEDInvestigation of a New Human Model for Itch
NCT06154824Not specifiedCOMPLETEDRepetitive Applications of Pruritogens and Effects of a Cutaneous-induced Pain Stimulation on Nonhistaminergic Itch Perception
NCT06245564Not specifiedCOMPLETEDEffect of Ketamine, Amitriptyline and Their Combination on Itch
NCT06470737Not specifiedCOMPLETEDInvestigation of Corticospinal Excitability Aspects of Itch and Pain

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

558 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
CLOZAPINEChEMBL + PubChemPhase 4 (approved)HRH1, HRH2, HRH3, HRH4
PIMOZIDEChEMBL + PubChemPhase 4 (approved)HRH1, HRH2, HRH3, HRH4
ASTEMIZOLEChEMBLPhase 4 (approved)HRH1, HRH2, HRH3, HRH4
FAMOTIDINEChEMBLPhase 4 (approved)CA1, CA5A, CA7, HRH2
IMATINIBChEMBLPhase 4 (approved)CA1, CA5A, CA7, HRH2
VERALIPRIDEChEMBLPhase 4 (approved)CA1, CA5A, CA7, HRH3
GSK-1004723ChEMBLPhase 2HRH1, HRH2, HRH3, HRH4
ACETAMINOPHENChEMBL + PubChemPhase 4 (approved)CA1, CA5A, CA7
ACETAZOLAMIDEChEMBL + PubChemPhase 4 (approved)CA1, CA5A, CA7
ACLIDINIUM BROMIDEChEMBL + PubChemPhase 4 (approved)HRH1, HRH2, HRH3
DESLORATADINEChEMBL + PubChemPhase 4 (approved)HRH1, HRH2, HRH4
DIHYDROERGOTAMINEChEMBL + PubChemPhase 4 (approved)HRH1, HRH2, HRH3
GefitinibChEMBL + PubChemPhase 4 (approved)HRH1, HRH2, HRH3
LinagliptinChEMBL + PubChemPhase 4 (approved)HRH1, HRH2, HRH3
PRAMIPEXOLEChEMBL + PubChemPhase 4 (approved)HRH1, HRH2, HRH4
PropoxypheneChEMBL + PubChemPhase 4 (approved)HRH1, HRH2, HRH3
RIFAMPINChEMBL + PubChemPhase 4 (approved)HRH1, HRH2, HRH3
RufinamideChEMBL + PubChemPhase 4 (approved)CA5A, HRH1, HRH2
AMIODARONEChEMBLPhase 4 (approved)HRH1, HRH2, HRH3
AMITRIPTYLINEChEMBLPhase 4 (approved)HRH1, HRH2, HRH3
ARIPIPRAZOLEChEMBLPhase 4 (approved)HRH1, HRH2, HRH3
BORTEZOMIBChEMBLPhase 4 (approved)CA1, CA5A, CA7
BRINZOLAMIDEChEMBLPhase 4 (approved)CA1, CA5A, CA7
CELECOXIBChEMBLPhase 4 (approved)CA1, CA5A, CA7
CHLORPHENIRAMINEChEMBLPhase 4 (approved)HRH1, HRH2, HRH3
CHLORTHALIDONEChEMBLPhase 4 (approved)CA1, CA5A, CA7
CLEMASTINEChEMBLPhase 4 (approved)HRH1, HRH2, HRH3
CLOMIPRAMINEChEMBLPhase 4 (approved)HRH1, HRH2, HRH3
COUMARINChEMBLPhase 4 (approved)CA1, CA5A, CA7
DEXCHLORPHENIRAMINEChEMBLPhase 4 (approved)HRH1, HRH2, HRH3
DICHLORPHENAMIDEChEMBLPhase 4 (approved)CA1, CA5A, CA7
DIPHENHYDRAMINEChEMBLPhase 4 (approved)HRH1, HRH2, HRH4
DOBUTAMINEChEMBLPhase 4 (approved)CA1, CA5A, CA7
DORZOLAMIDEChEMBLPhase 4 (approved)CA1, CA5A, CA7
DYCLONINEChEMBLPhase 4 (approved)HRH1, HRH2, HRH3
ETHOXZOLAMIDEChEMBLPhase 4 (approved)CA1, CA5A, CA7
FLUOXETINEChEMBLPhase 4 (approved)HRH1, HRH2, HRH3
FUROSEMIDEChEMBLPhase 4 (approved)CA1, CA5A, CA7
INDAPAMIDEChEMBLPhase 4 (approved)CA1, CA5A, CA7
INDOCYANINE GREEN ACID FORMChEMBLPhase 4 (approved)HRH1, HRH2, HRH3
IPRINDOLEChEMBLPhase 4 (approved)HRH1, HRH2, HRH3
KETOTIFENChEMBLPhase 4 (approved)HRH1, HRH2, HRH4
LACOSAMIDEChEMBLPhase 4 (approved)CA1, CA5A, CA7
LEVETIRACETAMChEMBLPhase 4 (approved)CA1, CA5A, CA7
LOXAPINEChEMBLPhase 4 (approved)HRH1, HRH2, HRH4
MAFENIDEChEMBLPhase 4 (approved)CA1, CA5A, CA7
METHAZOLAMIDEChEMBLPhase 4 (approved)CA1, CA5A, CA7
NILOTINIBChEMBLPhase 4 (approved)CA1, CA5A, CA7
RISPERIDONEChEMBLPhase 4 (approved)HRH1, HRH2, HRH3
SULFANILAMIDEChEMBLPhase 4 (approved)CA1, CA5A, CA7
SULOCTIDILChEMBLPhase 4 (approved)HRH1, HRH2, HRH3
SULPIRIDEChEMBLPhase 4 (approved)CA1, CA5A, CA7
TETRACAINEChEMBLPhase 4 (approved)HRH1, HRH2, HRH3
TOPIRAMATEChEMBLPhase 4 (approved)CA1, CA5A, CA7
TRICHLORMETHIAZIDEChEMBLPhase 4 (approved)CA1, CA5A, CA7
TRIENTINEChEMBLPhase 4 (approved)CA1, CA5A, CA7
TRIFLUOPERAZINEChEMBLPhase 4 (approved)HRH1, HRH2, HRH3
VALDECOXIBChEMBLPhase 4 (approved)CA1, CA5A, CA7
ZONISAMIDEChEMBLPhase 4 (approved)CA1, CA5A, CA7
CAFFEIC ACIDChEMBLPhase 3CA1, CA5A, CA7

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot