Details of the Target

General Information of Target

Target ID LDTP11875
Target Name Histamine H4 receptor (HRH4)
Gene Name HRH4
Gene ID 59340
Synonyms
GPCR105; Histamine H4 receptor; H4R; HH4R; AXOR35; G-protein coupled receptor 105; GPRv53; Pfi-013; SP9144
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAPSGSLAVPLAVLVLLLWGAPWTHGRRSNVRVITDENWRELLEGDWMIEFYAPWCPACQ
NLQPEWESFAEWGEDLEVNIAKVDVTEQPGLSGRFIITALPTIYHCKDGEFRRYQGPRTK
KDFINFISDKEWKSIEPVSSWFGPGSVLMSSMSALFQLSMWIRTCHNYFIEDLGLPVWGS
YTVFALATLFSGLLLGLCMIFVADCLCPSKRRRPQPYPYPSKKLLSESAQPLKKVEEEQE
ADEEDVSEEEAESKEGTNKDFPQNAIRQRSLGPSLATDKS
Target Type
Clinical trial
Target Bioclass
GPCR
Family
G-protein coupled receptor 1 family
Subcellular location
Cell membrane
Function
The H4 subclass of histamine receptors could mediate the histamine signals in peripheral tissues. Displays a significant level of constitutive activity (spontaneous activity in the absence of agonist).
TTD ID
T26500
Uniprot ID
Q9H3N8
DrugMap ID
TTXJ178
Ensemble ID
ENST00000256906.5
HGNC ID
HGNC:17383
ChEMBL ID
CHEMBL3759

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
JHH1 SNV: p.S247C .
KASUMI1 SNV: p.A306S .
KPNYN SNV: p.E163K .
MCC13 SNV: p.E171K .
NCIH1793 SNV: p.A58T .
NCIH1993 SNV: p.L57F .
RKO Deletion: p.S170RfsTer15
SNV: p.P379H		 .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Acrolein
 Probe Info  		N.A.  LDD0229  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0109  NEM HeLa N.A.  LDD0229  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 10 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Amitriptyline Small molecular drug DB00321
Amoxapine Small molecular drug DB00543
Aripiprazole Small molecular drug DB01238
Chlorpromazine Small molecular drug DB00477
Clozapine Small molecular drug DB00363
Doxepin Small molecular drug DB01142
Histamine Small molecular drug DB05381
Loxapine Small molecular drug DB00408
Mianserin Small molecular drug DB06148
Pheniramine Small molecular drug DB01620
Phase 2
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pf-3893787 Small molecular drug D02DTQ
Jnj-38518168 . D04VBF
Ur-63325 . D05GYL
Investigative
Click To Hide/Show 31 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(1h-indol-2-yl)(Piperazin-1-yl)Methanone Small molecular drug D0H2KD
(R)-3-(1h-imidazol-4-yl)Propyl Sec-butylcarbamate Small molecular drug D0C8IB
(R)-alpha-methylhistamine Small molecular drug D03SAM
(S)-alpha-methylhistamine Small molecular drug D0Q8BS
2-(3-bromophenyl)Histamine Small molecular drug D0G6AQ
2-methylhistamine Small molecular drug D0TC5E
4-methylhistamine Small molecular drug D02SQF
6-(4-methylpiperazin-1-yl)-9h-purin-2-amine Small molecular drug D0G3RZ
6-(4-methylpiperazin-1-yl)-9hpurine Small molecular drug D0QT2F
6-(4-methylpiperazin-1-yl)Pyrimidine-2,4-diamine Small molecular drug D0UK0F
9-benzyl-6-(4-methylpiperazin-1-yl)-9h-purine Small molecular drug D08BLM
A-846714 Small molecular drug D08DOG
A-943931 Small molecular drug D0P8DW
Burimamide Small molecular drug D06RNM
Clobenpropit Small molecular drug D0T8OD
Htmt Small molecular drug D09UVB
Imetit Small molecular drug D02RAN
Improgan Small molecular drug D04EDO
Impromidine Small molecular drug D0B4SF
Jnj-10191584 Small molecular drug D00XJR
N,N-dimethylhistamine Small molecular drug D0IF3N
N-ethylhistamine Small molecular drug D05OIF
N-methylhistamine Small molecular drug D0T6SC
N-[3h]Alpha-methylhistamine Small molecular drug D08ECP
N-[3h]Methylhistamine Small molecular drug D0A4XL
Vuf 8430 Small molecular drug D0MP8E
[125i]Iodophenpropit Small molecular drug D03ECU
[3h]Jnj 7777120 Small molecular drug D0E9SR
2-(2-(4-tert-butylphenylthio)Ethyl)-1h-imidazole . D01JXM
Rev131 . DB05032
Ur-60427 . D09HUF
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Thioperamide Small molecular drug D05FYA

References

1 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.