Details of the Target

General Information of Target

Target ID LDTP03310
Target Name Endothelin-1 receptor (EDNRA)
Gene Name EDNRA
Gene ID 1909
Synonyms
ETA; ETRA; Endothelin-1 receptor; Endothelin receptor type A; ET-A; ETA-R; hET-AR
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
METLCLRASFWLALVGCVISDNPERYSTNLSNHVDDFTTFRGTELSFLVTTHQPTNLVLP
SNGSMHNYCPQQTKITSAFKYINTVISCTIFIVGMVGNATLLRIIYQNKCMRNGPNALIA
SLALGDLIYVVIDLPINVFKLLAGRWPFDHNDFGVFLCKLFPFLQKSSVGITVLNLCALS
VDRYRAVASWSRVQGIGIPLVTAIEIVSIWILSFILAIPEAIGFVMVPFEYRGEQHKTCM
LNATSKFMEFYQDVKDWWLFGFYFCMPLVCTAIFYTLMTCEMLNRRNGSLRIALSEHLKQ
RREVAKTVFCLVVIFALCWFPLHLSRILKKTVYNEMDKNRCELLSFLLLMDYIGINLATM
NSCINPIALYFVSKKFKNCFQSCLCCCCYQSKSLMTSVPMNGTSIQWKNHDQNNHNTDRS
SHKDSMN
Target Type
Successful
Target Bioclass
GPCR
Family
G-protein coupled receptor 1 family, Endothelin receptor subfamily, EDNRA sub-subfamily
Subcellular location
Cell membrane
Function
Receptor for endothelin-1. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of binding affinities for ET-A is: ET1 > ET2 >> ET3.
TTD ID
T23499
Uniprot ID
P25101
DrugMap ID
TTKRD0G
Ensemble ID
ENST00000324300.10
HGNC ID
HGNC:3179
ChEMBL ID
CHEMBL252

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A375 SNV: p.S31N .
HS578T SNV: p.I136L .
HT115 SNV: p.F315V .
IM95 SNV: p.R232G .
JEKO1 SNV: p.K306N .
MEWO SNV: p.G197R .
NCIH1650 SNV: p.S289I .

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
DBIA
 Probe Info  		C158(1.00)  LDD1507  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C158(1.00)  LDD1507  [1]
 LDCM0215  AC10 HEK-293T C158(0.93)  LDD1508  [1]
 LDCM0226  AC11 HEK-293T C158(1.01)  LDD1509  [1]
 LDCM0237  AC12 HEK-293T C158(1.15)  LDD1510  [1]
 LDCM0259  AC14 HEK-293T C158(0.86)  LDD1512  [1]
 LDCM0270  AC15 HEK-293T C158(1.06)  LDD1513  [1]
 LDCM0276  AC17 HEK-293T C158(1.16)  LDD1515  [1]
 LDCM0277  AC18 HEK-293T C158(0.88)  LDD1516  [1]
 LDCM0278  AC19 HEK-293T C158(1.01)  LDD1517  [1]
 LDCM0279  AC2 HEK-293T C158(1.02)  LDD1518  [1]
 LDCM0280  AC20 HEK-293T C158(1.06)  LDD1519  [1]
 LDCM0281  AC21 HEK-293T C158(0.90)  LDD1520  [1]
 LDCM0282  AC22 HEK-293T C158(0.60)  LDD1521  [1]
 LDCM0283  AC23 HEK-293T C158(0.96)  LDD1522  [1]
 LDCM0285  AC25 HEK-293T C158(0.70)  LDD1524  [1]
 LDCM0286  AC26 HEK-293T C158(1.03)  LDD1525  [1]
 LDCM0287  AC27 HEK-293T C158(0.93)  LDD1526  [1]
 LDCM0288  AC28 HEK-293T C158(0.86)  LDD1527  [1]
 LDCM0289  AC29 HEK-293T C158(0.94)  LDD1528  [1]
 LDCM0290  AC3 HEK-293T C158(0.87)  LDD1529  [1]
 LDCM0291  AC30 HEK-293T C158(0.93)  LDD1530  [1]
 LDCM0292  AC31 HEK-293T C158(0.85)  LDD1531  [1]
 LDCM0294  AC33 HEK-293T C158(0.80)  LDD1533  [1]
 LDCM0295  AC34 HEK-293T C158(0.87)  LDD1534  [1]
 LDCM0296  AC35 HEK-293T C158(0.87)  LDD1535  [1]
 LDCM0297  AC36 HEK-293T C158(0.88)  LDD1536  [1]
 LDCM0298  AC37 HEK-293T C158(0.94)  LDD1537  [1]
 LDCM0299  AC38 HEK-293T C158(1.09)  LDD1538  [1]
 LDCM0300  AC39 HEK-293T C158(1.02)  LDD1539  [1]
 LDCM0301  AC4 HEK-293T C158(0.74)  LDD1540  [1]
 LDCM0303  AC41 HEK-293T C158(0.96)  LDD1542  [1]
 LDCM0304  AC42 HEK-293T C158(0.87)  LDD1543  [1]
 LDCM0305  AC43 HEK-293T C158(0.87)  LDD1544  [1]
 LDCM0306  AC44 HEK-293T C158(0.97)  LDD1545  [1]
 LDCM0307  AC45 HEK-293T C158(1.02)  LDD1546  [1]
 LDCM0308  AC46 HEK-293T C158(0.63)  LDD1547  [1]
 LDCM0309  AC47 HEK-293T C158(0.95)  LDD1548  [1]
 LDCM0311  AC49 HEK-293T C158(0.79)  LDD1550  [1]
 LDCM0312  AC5 HEK-293T C158(0.74)  LDD1551  [1]
 LDCM0313  AC50 HEK-293T C158(0.94)  LDD1552  [1]
 LDCM0314  AC51 HEK-293T C158(0.96)  LDD1553  [1]
 LDCM0315  AC52 HEK-293T C158(0.87)  LDD1554  [1]
 LDCM0316  AC53 HEK-293T C158(0.78)  LDD1555  [1]
 LDCM0317  AC54 HEK-293T C158(0.64)  LDD1556  [1]
 LDCM0318  AC55 HEK-293T C158(1.13)  LDD1557  [1]
 LDCM0320  AC57 HEK-293T C158(0.95)  LDD1559  [1]
 LDCM0321  AC58 HEK-293T C158(0.99)  LDD1560  [1]
 LDCM0322  AC59 HEK-293T C158(0.96)  LDD1561  [1]
 LDCM0323  AC6 HEK-293T C158(0.72)  LDD1562  [1]
 LDCM0324  AC60 HEK-293T C158(1.06)  LDD1563  [1]
 LDCM0325  AC61 HEK-293T C158(0.91)  LDD1564  [1]
 LDCM0326  AC62 HEK-293T C158(0.73)  LDD1565  [1]
 LDCM0327  AC63 HEK-293T C158(1.13)  LDD1566  [1]
 LDCM0334  AC7 HEK-293T C158(1.02)  LDD1568  [1]
 LDCM0248  AKOS034007472 HEK-293T C158(0.81)  LDD1511  [1]
 LDCM0356  AKOS034007680 HEK-293T C158(0.69)  LDD1570  [1]
 LDCM0367  CL1 HEK-293T C158(1.53)  LDD1571  [1]
 LDCM0368  CL10 HEK-293T C158(1.90)  LDD1572  [1]
 LDCM0369  CL100 HEK-293T C158(0.98)  LDD1573  [1]
 LDCM0370  CL101 HEK-293T C158(1.10)  LDD1574  [1]
 LDCM0372  CL103 HEK-293T C158(0.98)  LDD1576  [1]
 LDCM0373  CL104 HEK-293T C158(0.77)  LDD1577  [1]
 LDCM0374  CL105 HEK-293T C158(1.01)  LDD1578  [1]
 LDCM0376  CL107 HEK-293T C158(1.02)  LDD1580  [1]
 LDCM0377  CL108 HEK-293T C158(0.98)  LDD1581  [1]
 LDCM0378  CL109 HEK-293T C158(1.05)  LDD1582  [1]
 LDCM0379  CL11 HEK-293T C158(1.16)  LDD1583  [1]
 LDCM0381  CL111 HEK-293T C158(1.04)  LDD1585  [1]
 LDCM0382  CL112 HEK-293T C158(1.16)  LDD1586  [1]
 LDCM0383  CL113 HEK-293T C158(0.90)  LDD1587  [1]
 LDCM0385  CL115 HEK-293T C158(1.21)  LDD1589  [1]
 LDCM0386  CL116 HEK-293T C158(0.80)  LDD1590  [1]
 LDCM0387  CL117 HEK-293T C158(1.00)  LDD1591  [1]
 LDCM0389  CL119 HEK-293T C158(0.90)  LDD1593  [1]
 LDCM0391  CL120 HEK-293T C158(0.81)  LDD1595  [1]
 LDCM0392  CL121 HEK-293T C158(1.05)  LDD1596  [1]
 LDCM0394  CL123 HEK-293T C158(1.20)  LDD1598  [1]
 LDCM0395  CL124 HEK-293T C158(0.87)  LDD1599  [1]
 LDCM0396  CL125 HEK-293T C158(1.18)  LDD1600  [1]
 LDCM0398  CL127 HEK-293T C158(1.24)  LDD1602  [1]
 LDCM0399  CL128 HEK-293T C158(1.08)  LDD1603  [1]
 LDCM0400  CL13 HEK-293T C158(1.46)  LDD1604  [1]
 LDCM0402  CL15 HEK-293T C158(1.38)  LDD1606  [1]
 LDCM0403  CL16 HEK-293T C158(1.04)  LDD1607  [1]
 LDCM0404  CL17 HEK-293T C158(1.42)  LDD1608  [1]
 LDCM0405  CL18 HEK-293T C158(0.97)  LDD1609  [1]
 LDCM0406  CL19 HEK-293T C158(1.10)  LDD1610  [1]
 LDCM0408  CL20 HEK-293T C158(1.40)  LDD1612  [1]
 LDCM0409  CL21 HEK-293T C158(1.26)  LDD1613  [1]
 LDCM0410  CL22 HEK-293T C158(1.02)  LDD1614  [1]
 LDCM0411  CL23 HEK-293T C158(1.26)  LDD1615  [1]
 LDCM0413  CL25 HEK-293T C158(1.22)  LDD1617  [1]
 LDCM0415  CL27 HEK-293T C158(1.09)  LDD1619  [1]
 LDCM0416  CL28 HEK-293T C158(0.98)  LDD1620  [1]
 LDCM0417  CL29 HEK-293T C158(0.82)  LDD1621  [1]
 LDCM0418  CL3 HEK-293T C158(1.33)  LDD1622  [1]
 LDCM0419  CL30 HEK-293T C158(0.99)  LDD1623  [1]
 LDCM0420  CL31 HEK-293T C158(1.01)  LDD1624  [1]
 LDCM0421  CL32 HEK-293T C158(1.04)  LDD1625  [1]
 LDCM0422  CL33 HEK-293T C158(1.54)  LDD1626  [1]
 LDCM0423  CL34 HEK-293T C158(0.92)  LDD1627  [1]
 LDCM0424  CL35 HEK-293T C158(1.19)  LDD1628  [1]
 LDCM0426  CL37 HEK-293T C158(1.08)  LDD1630  [1]
 LDCM0428  CL39 HEK-293T C158(0.95)  LDD1632  [1]
 LDCM0429  CL4 HEK-293T C158(1.12)  LDD1633  [1]
 LDCM0430  CL40 HEK-293T C158(0.84)  LDD1634  [1]
 LDCM0431  CL41 HEK-293T C158(0.93)  LDD1635  [1]
 LDCM0432  CL42 HEK-293T C158(0.82)  LDD1636  [1]
 LDCM0433  CL43 HEK-293T C158(0.87)  LDD1637  [1]
 LDCM0434  CL44 HEK-293T C158(0.80)  LDD1638  [1]
 LDCM0435  CL45 HEK-293T C158(1.09)  LDD1639  [1]
 LDCM0436  CL46 HEK-293T C158(0.75)  LDD1640  [1]
 LDCM0437  CL47 HEK-293T C158(1.16)  LDD1641  [1]
 LDCM0439  CL49 HEK-293T C158(0.93)  LDD1643  [1]
 LDCM0440  CL5 HEK-293T C158(1.16)  LDD1644  [1]
 LDCM0443  CL52 HEK-293T C158(1.02)  LDD1646  [1]
 LDCM0444  CL53 HEK-293T C158(1.00)  LDD1647  [1]
 LDCM0445  CL54 HEK-293T C158(1.26)  LDD1648  [1]
 LDCM0446  CL55 HEK-293T C158(0.93)  LDD1649  [1]
 LDCM0447  CL56 HEK-293T C158(1.00)  LDD1650  [1]
 LDCM0448  CL57 HEK-293T C158(1.22)  LDD1651  [1]
 LDCM0449  CL58 HEK-293T C158(0.70)  LDD1652  [1]
 LDCM0450  CL59 HEK-293T C158(1.14)  LDD1653  [1]
 LDCM0451  CL6 HEK-293T C158(1.08)  LDD1654  [1]
 LDCM0453  CL61 HEK-293T C158(1.06)  LDD1656  [1]
 LDCM0455  CL63 HEK-293T C158(0.92)  LDD1658  [1]
 LDCM0456  CL64 HEK-293T C158(0.83)  LDD1659  [1]
 LDCM0457  CL65 HEK-293T C158(0.88)  LDD1660  [1]
 LDCM0458  CL66 HEK-293T C158(0.95)  LDD1661  [1]
 LDCM0459  CL67 HEK-293T C158(1.16)  LDD1662  [1]
 LDCM0460  CL68 HEK-293T C158(0.90)  LDD1663  [1]
 LDCM0461  CL69 HEK-293T C158(0.92)  LDD1664  [1]
 LDCM0462  CL7 HEK-293T C158(1.21)  LDD1665  [1]
 LDCM0463  CL70 HEK-293T C158(1.19)  LDD1666  [1]
 LDCM0464  CL71 HEK-293T C158(1.06)  LDD1667  [1]
 LDCM0466  CL73 HEK-293T C158(1.13)  LDD1669  [1]
 LDCM0469  CL76 HEK-293T C158(0.87)  LDD1672  [1]
 LDCM0470  CL77 HEK-293T C158(0.93)  LDD1673  [1]
 LDCM0471  CL78 HEK-293T C158(0.88)  LDD1674  [1]
 LDCM0472  CL79 HEK-293T C158(0.99)  LDD1675  [1]
 LDCM0473  CL8 HEK-293T C158(2.27)  LDD1676  [1]
 LDCM0474  CL80 HEK-293T C158(1.13)  LDD1677  [1]
 LDCM0475  CL81 HEK-293T C158(1.24)  LDD1678  [1]
 LDCM0476  CL82 HEK-293T C158(0.76)  LDD1679  [1]
 LDCM0477  CL83 HEK-293T C158(0.95)  LDD1680  [1]
 LDCM0479  CL85 HEK-293T C158(1.35)  LDD1682  [1]
 LDCM0481  CL87 HEK-293T C158(1.35)  LDD1684  [1]
 LDCM0482  CL88 HEK-293T C158(0.89)  LDD1685  [1]
 LDCM0483  CL89 HEK-293T C158(1.05)  LDD1686  [1]
 LDCM0484  CL9 HEK-293T C158(1.25)  LDD1687  [1]
 LDCM0485  CL90 HEK-293T C158(1.32)  LDD1688  [1]
 LDCM0486  CL91 HEK-293T C158(1.05)  LDD1689  [1]
 LDCM0487  CL92 HEK-293T C158(1.27)  LDD1690  [1]
 LDCM0488  CL93 HEK-293T C158(1.14)  LDD1691  [1]
 LDCM0489  CL94 HEK-293T C158(0.89)  LDD1692  [1]
 LDCM0490  CL95 HEK-293T C158(1.29)  LDD1693  [1]
 LDCM0492  CL97 HEK-293T C158(1.55)  LDD1695  [1]
 LDCM0494  CL99 HEK-293T C158(1.03)  LDD1697  [1]
 LDCM0495  E2913 HEK-293T C158(1.02)  LDD1698  [1]
 LDCM0468  Fragment33 HEK-293T C158(1.05)  LDD1671  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Beta-arrestin-1 (ARRB1) Arrestin family P49407
Beta-arrestin-2 (ARRB2) Arrestin family P32121
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Endothelin-1 (EDN1) Endothelin/sarafotoxin family P05305

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
Acetylsalicylic Acid Small molecular drug DB00945
Ambrisentan Small molecular drug D0X5ZI
Bosentan Small molecular drug D0U4CE
Macitentan Small molecular drug D0S7JH
Sitaxentan Small molecular drug DB06268
Lu302146 . D0Y7OJ
Phase 3
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Atrasentan Small molecular drug D0Y6UU
Clazosentan Small molecular drug D0H2RJ
Darusentan Small molecular drug D0R7YY
Pf-1228305 Small molecular drug D08JWJ
Sparsentan Small molecular drug D0YS1U
Phase 2
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bq-123 Small molecular drug D09LQK
Fr139317 Small molecular drug D09XLS
Pd-145065 Small molecular drug D0OW4A
Tbc-3711 Small molecular drug D03LAB
Ym-598 . D0XR7C
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmz-2123 . D04OXG
Clinical trial
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Et-1 . D05OEO
Investigative
Click To Hide/Show 25 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
2-hydroxy-3,5-diiodobenzoic Acid Small molecular drug D0A8MD
2-hydroxy-35-diiodobenzoic Acid Small molecular drug DB04674
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Small molecular drug D0T2RY
Asterric Acid Small molecular drug D0I7OD
Bms-187308 Small molecular drug D0W4UX
Endothelin-2 Small molecular drug D0F6TS
Enrasentan Small molecular drug DB06460
Lu302872 Small molecular drug D0X1XM
Pd-163140 Small molecular drug D07OMS
Pd164333 Small molecular drug D0W1HZ
Sarafotoxin S6b Small molecular drug D0OC1W
Sparsentan Small molecular drug DB12548
[125i]Pd151242 Small molecular drug D0M2YL
[3h]Bq123 Small molecular drug D02OPG
[3h]S0139 Small molecular drug D0NA5S
Ac-bhg-f-n-y-y-w . D0F8BZ
Ac-w-f-f-n-y-y-w . D0Y8UY
Actelion-1 . DB05367
Bhg-f-n-y-y-w . D06OSN
Hjp-272 . D07QBJ
Spp 301 . DB05290
Tezosentan . DB06558
Trp-ile-ile-asp-leu-hisc(Cys-ser-val-tyr-phe-cys) . D0M2TB
Trp-ile-ile-asp-leu-hisc(Cys-val-tyr-phe-cys) . D0NI1W
W-f-f-n--y-y-w . D00RGL
Withdrawn from market
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Sitaxsentan Small molecular drug D0T1RG
Tbc 11251 (Tbc) Small molecular drug D02EAS
Discontinued
Click To Hide/Show 19 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
A-216546 Small molecular drug D02QQB
Avosentan Small molecular drug D0J2IH
Bms-182874 Small molecular drug D01VUE
Bms-193884 Small molecular drug D0B5PU
Bq-518 Small molecular drug D07DGM
Bq610 Small molecular drug D0Q9XI
Enrasentan Small molecular drug D07YHT
J-104132 Small molecular drug D05VZJ
Pd-155080 Small molecular drug D0H0KK
Pd142893 Small molecular drug D0S9JH
Pd156707 Small molecular drug D0L3AR
Sb-209670 Small molecular drug D0W6XL
Sb-234551 Small molecular drug D08AMQ
Zibotentan Small molecular drug D02HVW
50-235 . D0P5UE
97-139 . D03FVI
Edonentan Hydrate . D03MUM
Mx-6120 . D0NC1D
Zd-1611 . D04NPX

References

1 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402