U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
This repository is under review for potential modification in compliance with Administration directives.

Approval Year

Substance Class Protein
Created
by admin
on Tue Apr 01 18:33:56 GMT 2025
Edited
by admin
on Tue Apr 01 18:33:56 GMT 2025
Protein Sub Type
Sequence Type COMPLETE
Record UNII
28XBT591QG
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
HISTAMINE H1 RECEPTOR
Common Name English
H1R
Preferred Name English
HRH1
Common Name English
H1
Common Name English
HH1R
Common Name English
Code System Code Type Description
UNIPROT
P35367
Created by admin on Tue Apr 01 18:33:56 GMT 2025 , Edited by admin on Tue Apr 01 18:33:56 GMT 2025
PRIMARY
FDA UNII
28XBT591QG
Created by admin on Tue Apr 01 18:33:56 GMT 2025 , Edited by admin on Tue Apr 01 18:33:56 GMT 2025
PRIMARY
From To
1_100 1_180
1_441 1_444
Glycosylation Type HUMAN
Glycosylation Link Type Site
N 1_5
N 1_18
Related Record Type Details
INHIBITOR -> TARGET
RADIOLIGAND->TARGET
Kd
INHIBITOR -> TARGET
INHIBITOR
Ki
INHIBITOR -> TARGET
IC50
INHIBITOR -> TARGET
AGONIST -> TARGET
CHO-H1 cells, histamine stimulation resulted in a concentration-dependent increase in [Ca2+]i with an EC50 of 170±30 nM.
EC50
INHIBITOR -> TARGET
Ki
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR->OFF-TARGET
IC50
INHIBITOR -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
IC50
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR
Ki
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
Long acting slowly dissociates.
BINDING
Ki
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
ANTAGONIST->TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
Ki
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
Alcaftadine is a H1 histamine receptor antagonist and inhibitor of the release of histamine from mast cells.
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
TARGET -> INHIBITOR
INHIBITOR -> TARGET
Binds stronger than R-isomer
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET

Structural Modifications

Modification Type Location Site Location Type Residue Modified Extent Fragment Name Fragment Approval
AMINO ACID SUBSTITUTION [1_140] [1_142] [1_279] THREONINE PHOSPHATE 3L4WX7B1EI
AMINO ACID SUBSTITUTION [1_344] [1_347] [1_380] [1_396] [1_398] DEXFOSFOSERINE VI4F0K069V
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT CHEMICAL
Molecular Formula CHEMICAL