Details of the Target

General Information of Target

Target ID LDTP13819
Target Name Cysteinyl leukotriene receptor 1 (CYSLTR1)
Gene Name CYSLTR1
Gene ID 10800
Synonyms
CYSLT1; Cysteinyl leukotriene receptor 1; CysLTR1; Cysteinyl leukotriene D4 receptor; LTD4 receptor; G-protein coupled receptor HG55; HMTMF81
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAGEENFKEELRSQDASRNLNQHEVAGHPHSWSLEMLLRRLRAVHTKQDDKFANLLDAVG
EFGTFQQRLVALTFIPSIMSAFFMFADHFVFTAQKPYCNTSWILAVGPHLSKAEQLNLTI
PQAPNGSFLTCFMYLPVPWNLDSIIQFGLNDTDTCQDGWIYPDAKKRSLINEFDLVCGME
TKKDTAQIMFMAGLPIGSLIFRLITDKMGRYPAILLSLLGLIIFGFGTAFMNSFHLYLFF
RFGISQSVVGYAISSISLATEWLVGEHRAHAIILGHCFFAVGAVLLTGIAYSLPHWQLLF
LVGGILVIPFISYIWILPESPRWLMMKGKVKEAKQVLCYAASVNKKTIPSNLLDELQLPR
KKVTRASVLDFCKNRQLCKVTLVMSCVWFTVSYTYFTLSLRMRELGVSVHFRHVVPSIME
VPARLCCIFLLQQIGRKWSLAVTLLQAIIWCLLLLFLPEGEDGLRLKWPRCPATELKSMT
ILVLMLREFSLAATVTVFFLYTAELLPTVLRATGLGLVSLASVAGAILSLTIISQTPSLL
PIFLCCVLAIVAFSLSSLLPETRDQPLSESLNHSSQIRNKVKDMKTKETSSDDV
Target Type
Successful
Target Bioclass
GPCR
Family
G-protein coupled receptor 1 family
Subcellular location
Cell membrane
Function
Receptor for cysteinyl leukotrienes mediating bronchoconstriction of individuals with and without asthma. Stimulation by LTD4 results in the contraction and proliferation of smooth muscle, edema, eosinophil migration and damage to the mucus layer in the lung. This response is mediated via a G-protein that activates a phosphatidylinositol-calcium second messenger system. The rank order of affinities for the leukotrienes is LTD4 >> LTE4 = LTC4 >> LTB4.
TTD ID
T71192
Uniprot ID
Q9Y271
DrugMap ID
TTGKOY9
Ensemble ID
ENST00000373304.4
HGNC ID
HGNC:17451
ChEMBL ID
CHEMBL1798

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
N1
 Probe Info  		H256(0.00); H258(0.00)  LDD0245  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cinalukast Small molecular drug D06PEB
Hydroquinone Small molecular drug DB09526
Montelukast Small molecular drug D00QET
Nedocromil Small molecular drug DB00716
Pranlukast Small molecular drug D08QIP
Zafirlukast Small molecular drug D05DVP
Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Claritin/Singulair . D0C2XI
Phase 2
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bay-x-7195 Small molecular drug D0GY0O
Iralukast Small molecular drug D0X9LK
Masilukast Small molecular drug D05BHF
Kp-496 . D07JKY
Lm-1507.Na . D0OG6N
Phase 1
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ym-57158 Small molecular drug D0K2NA
Cr-3465 . D07ZUX
Investigative
Click To Hide/Show 12 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Baycyslt2 Small molecular drug D09JQU
Bayu9773 Small molecular drug D05CNT
Cgp-57698 Small molecular drug D04CZQ
Leukotriene D4 Small molecular drug DB11858
Ltc4 Small molecular drug D0EW6H
Ltd4 Small molecular drug D03YBH
Lte4 Small molecular drug D0C0KJ
N-methyl Ltc4 Small molecular drug D03VGR
Pobilukast Small molecular drug D0G7OZ
Wy-46016 Small molecular drug D0R8IQ
Leukotriene C4 . DB08855
Xgp-510 . D0X8PD
Discontinued
Click To Hide/Show 17 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ablukast Small molecular drug D09DIG
As-35 Small molecular drug D0B6EU
Ds-4574 Small molecular drug D0F4IG
Fpl-55712 Small molecular drug D0ZE5V
Ici-198615 Small molecular drug D0J7UI
L-648051 Small molecular drug D0J4EG
L-660771 Small molecular drug D07GTB
Mci-826 Small molecular drug D0AB7G
Mdl-43291 Small molecular drug D09ZVR
Rg-7152 Small molecular drug D0B7KF
Sulukast Small molecular drug D0G8UG
Tomelukast Small molecular drug D0S8YL
Fk-011 . D04HHW
Lm-1376 . D00YOW
Ly-2300559 . D09RON
Ly-290154 . D0D0XX
Ot-4003 . D0PL5F

References

1 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.