Details of the Target

General Information of Target

Target ID LDTP03009
Target Name Sodium/hydrogen exchanger 1 (SLC9A1)
Gene Name SLC9A1
Gene ID 6548
Synonyms
APNH1; NHE1; Sodium/hydrogen exchanger 1; APNH; Na(+)/H(+) antiporter, amiloride-sensitive; Na(+)/H(+) exchanger 1; NHE-1; Solute carrier family 9 member 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MVLRSGICGLSPHRIFPSLLVVVALVGLLPVLRSHGLQLSPTASTIRSSEPPRERSIGDV
TTAPPEVTPESRPVNHSVTDHGMKPRKAFPVLGIDYTHVRTPFEISLWILLACLMKIGFH
VIPTISSIVPESCLLIVVGLLVGGLIKGVGETPPFLQSDVFFLFLLPPIILDAGYFLPLR
QFTENLGTILIFAVVGTLWNAFFLGGLMYAVCLVGGEQINNIGLLDNLLFGSIISAVDPV
AVLAVFEEIHINELLHILVFGESLLNDAVTVVLYHLFEEFANYEHVGIVDIFLGFLSFFV
VALGGVLVGVVYGVIAAFTSRFTSHIRVIEPLFVFLYSYMAYLSAELFHLSGIMALIASG
VVMRPYVEANISHKSHTTIKYFLKMWSSVSETLIFIFLGVSTVAGSHHWNWTFVISTLLF
CLIARVLGVLGLTWFINKFRIVKLTPKDQFIIAYGGLRGAIAFSLGYLLDKKHFPMCDLF
LTAIITVIFFTVFVQGMTIRPLVDLLAVKKKQETKRSINEEIHTQFLDHLLTGIEDICGH
YGHHHWKDKLNRFNKKYVKKCLIAGERSKEPQLIAFYHKMEMKQAIELVESGGMGKIPSA
VSTVSMQNIHPKSLPSERILPALSKDKEEEIRKILRNNLQKTRQRLRSYNRHTLVADPYE
EAWNQMLLRRQKARQLEQKINNYLTVPAHKLDSPTMSRARIGSDPLAYEPKEDLPVITID
PASPQSPESVDLVNEELKGKVLGLSRDPAKVAEEDEDDDGGIMMRSKETSSPGTDDVFTP
APSDSPSSQRIQRCLSDPGPHPEPGEGEPFFPKGQ
Target Type
Clinical trial
Target Bioclass
Transporter and channel
Family
Monovalent cation:proton antiporter 1 (CPA1) transporter (TC 2.A.36) family
Subcellular location
Membrane
Function
Electroneutral Na(+) /H(+) antiporter that extrudes Na(+) in exchange for external protons driven by the inward sodium ion chemical gradient, protecting cells from acidification that occurs from metabolism. Exchanges intracellular H(+) ions for extracellular Na(+) in 1:1 stoichiometry. Plays a key role in maintening intracellular pH neutral and cell volume, and thus is important for cell growth, proliferation, migration and survival. In addition, can transport lithium Li(+) and functions also as a Na(+)/Li(+) antiporter. SLC9A1 also functions in membrane anchoring and organization of scaffolding complexes that coordinate signaling inputs.
TTD ID
T82028
Uniprot ID
P19634
DrugMap ID
TTGSEFH
Ensemble ID
ENST00000263980.8
HGNC ID
HGNC:11071
ChEMBL ID
CHEMBL2781

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
DOTC24510 SNV: p.A707V DBIA    Probe Info 
DU145 SNV: p.R180W .
HCT116 Deletion: p.F155SfsTer36 .
HCT15 SNV: p.K560R; p.R645W; p.L742F .
KELLY SNV: p.P694L .
MDAMB436 SNV: p.P724L .
OVK18 Deletion: p.F155SfsTer36 .
RKO Deletion: p.K612SfsTer24 .
SW480 SNV: p.A236T .
SW620 SNV: p.A236T .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 7 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C561(4.76)  LDD3311  [1]
BTD
 Probe Info  		C561(1.04)  LDD2137  [2]
NAIA_4
 Probe Info  		N.A.  LDD2226  [3]
NAIA_5
 Probe Info  		C794(0.00); C561(0.00)  LDD2224  [3]
IPM
 Probe Info  		N.A.  LDD0147  [4]
TFBX
 Probe Info  		N.A.  LDD0148  [4]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [5]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C794(1.08)  LDD1507  [6]
 LDCM0215  AC10 HEK-293T C794(0.99)  LDD1508  [6]
 LDCM0226  AC11 HEK-293T C561(1.12); C794(1.03)  LDD1509  [6]
 LDCM0237  AC12 HEK-293T C561(1.09); C794(1.02)  LDD1510  [6]
 LDCM0259  AC14 HEK-293T C561(1.11); C794(0.95)  LDD1512  [6]
 LDCM0270  AC15 HEK-293T C794(0.94)  LDD1513  [6]
 LDCM0276  AC17 HEK-293T C794(1.08)  LDD1515  [6]
 LDCM0277  AC18 HEK-293T C794(1.06)  LDD1516  [6]
 LDCM0278  AC19 HEK-293T C561(0.97); C794(0.98)  LDD1517  [6]
 LDCM0279  AC2 HEK-293T C794(1.04)  LDD1518  [6]
 LDCM0280  AC20 HEK-293T C561(1.10); C794(0.91)  LDD1519  [6]
 LDCM0281  AC21 HEK-293T C561(1.28); C794(1.03)  LDD1520  [6]
 LDCM0282  AC22 HEK-293T C561(1.10); C794(0.99)  LDD1521  [6]
 LDCM0283  AC23 HEK-293T C794(1.02)  LDD1522  [6]
 LDCM0284  AC24 HEK-293T C561(1.02); C794(1.04)  LDD1523  [6]
 LDCM0285  AC25 HEK-293T C794(1.13)  LDD1524  [6]
 LDCM0286  AC26 HEK-293T C794(1.07)  LDD1525  [6]
 LDCM0287  AC27 HEK-293T C561(1.15); C794(0.99)  LDD1526  [6]
 LDCM0288  AC28 HEK-293T C561(1.00); C794(0.95)  LDD1527  [6]
 LDCM0289  AC29 HEK-293T C561(1.01); C794(1.06)  LDD1528  [6]
 LDCM0290  AC3 HEK-293T C561(1.11); C794(1.05)  LDD1529  [6]
 LDCM0291  AC30 HEK-293T C561(0.97); C794(0.96)  LDD1530  [6]
 LDCM0292  AC31 HEK-293T C794(0.95)  LDD1531  [6]
 LDCM0293  AC32 HEK-293T C561(1.08); C794(0.96)  LDD1532  [6]
 LDCM0294  AC33 HEK-293T C794(0.98)  LDD1533  [6]
 LDCM0295  AC34 HEK-293T C794(0.99)  LDD1534  [6]
 LDCM0296  AC35 HEK-293T C561(1.18); C794(1.02)  LDD1535  [6]
 LDCM0297  AC36 HEK-293T C561(1.12); C794(1.00)  LDD1536  [6]
 LDCM0298  AC37 HEK-293T C561(1.15); C794(1.13)  LDD1537  [6]
 LDCM0299  AC38 HEK-293T C561(0.97); C794(0.92)  LDD1538  [6]
 LDCM0300  AC39 HEK-293T C794(0.88)  LDD1539  [6]
 LDCM0301  AC4 HEK-293T C561(1.07); C794(0.95)  LDD1540  [6]
 LDCM0302  AC40 HEK-293T C561(0.91); C794(0.91)  LDD1541  [6]
 LDCM0303  AC41 HEK-293T C794(1.01)  LDD1542  [6]
 LDCM0304  AC42 HEK-293T C794(1.02)  LDD1543  [6]
 LDCM0305  AC43 HEK-293T C561(1.05); C794(1.03)  LDD1544  [6]
 LDCM0306  AC44 HEK-293T C561(1.07); C794(1.02)  LDD1545  [6]
 LDCM0307  AC45 HEK-293T C561(1.20); C794(1.04)  LDD1546  [6]
 LDCM0308  AC46 HEK-293T C561(0.92); C794(0.94)  LDD1547  [6]
 LDCM0309  AC47 HEK-293T C794(0.95)  LDD1548  [6]
 LDCM0310  AC48 HEK-293T C561(1.04); C794(0.95)  LDD1549  [6]
 LDCM0311  AC49 HEK-293T C794(1.15)  LDD1550  [6]
 LDCM0312  AC5 HEK-293T C561(1.08); C794(1.02)  LDD1551  [6]
 LDCM0313  AC50 HEK-293T C794(1.03)  LDD1552  [6]
 LDCM0314  AC51 HEK-293T C561(1.04); C794(1.05)  LDD1553  [6]
 LDCM0315  AC52 HEK-293T C561(1.08); C794(0.87)  LDD1554  [6]
 LDCM0316  AC53 HEK-293T C561(1.05); C794(1.04)  LDD1555  [6]
 LDCM0317  AC54 HEK-293T C561(1.03); C794(0.95)  LDD1556  [6]
 LDCM0318  AC55 HEK-293T C794(0.90)  LDD1557  [6]
 LDCM0319  AC56 HEK-293T C561(1.16); C794(0.95)  LDD1558  [6]
 LDCM0320  AC57 HEK-293T C794(1.04)  LDD1559  [6]
 LDCM0321  AC58 HEK-293T C794(1.01)  LDD1560  [6]
 LDCM0322  AC59 HEK-293T C561(0.99); C794(1.04)  LDD1561  [6]
 LDCM0323  AC6 HEK-293T C561(1.04); C794(1.00)  LDD1562  [6]
 LDCM0324  AC60 HEK-293T C561(0.97); C794(0.92)  LDD1563  [6]
 LDCM0325  AC61 HEK-293T C561(0.97); C794(0.98)  LDD1564  [6]
 LDCM0326  AC62 HEK-293T C561(0.93); C794(0.98)  LDD1565  [6]
 LDCM0327  AC63 HEK-293T C794(0.94)  LDD1566  [6]
 LDCM0328  AC64 HEK-293T C561(0.98); C794(0.97)  LDD1567  [6]
 LDCM0334  AC7 HEK-293T C794(1.04)  LDD1568  [6]
 LDCM0345  AC8 HEK-293T C561(1.02); C794(0.98)  LDD1569  [6]
 LDCM0248  AKOS034007472 HEK-293T C561(1.14); C794(1.02)  LDD1511  [6]
 LDCM0356  AKOS034007680 HEK-293T C794(1.14)  LDD1570  [6]
 LDCM0275  AKOS034007705 HEK-293T C561(0.92); C794(0.94)  LDD1514  [6]
 LDCM0367  CL1 HEK-293T C561(1.13); C794(0.90)  LDD1571  [6]
 LDCM0368  CL10 HEK-293T C561(1.30); C794(0.86)  LDD1572  [6]
 LDCM0369  CL100 HEK-293T C561(1.11); C794(1.06)  LDD1573  [6]
 LDCM0370  CL101 HEK-293T C561(0.98); C794(0.98)  LDD1574  [6]
 LDCM0371  CL102 HEK-293T C561(1.04); C794(1.08)  LDD1575  [6]
 LDCM0372  CL103 HEK-293T C561(0.88); C794(1.02)  LDD1576  [6]
 LDCM0373  CL104 HEK-293T C561(0.97); C794(0.86)  LDD1577  [6]
 LDCM0374  CL105 HEK-293T C561(1.00); C794(0.99)  LDD1578  [6]
 LDCM0375  CL106 HEK-293T C561(0.96); C794(1.05)  LDD1579  [6]
 LDCM0376  CL107 HEK-293T C561(1.02); C794(1.03)  LDD1580  [6]
 LDCM0377  CL108 HEK-293T C561(1.12); C794(1.13)  LDD1581  [6]
 LDCM0378  CL109 HEK-293T C561(1.03); C794(0.93)  LDD1582  [6]
 LDCM0379  CL11 HEK-293T C794(0.95)  LDD1583  [6]
 LDCM0380  CL110 HEK-293T C561(0.96); C794(0.99)  LDD1584  [6]
 LDCM0381  CL111 HEK-293T C561(1.09); C794(1.08)  LDD1585  [6]
 LDCM0382  CL112 HEK-293T C561(0.99); C794(1.10)  LDD1586  [6]
 LDCM0383  CL113 HEK-293T C561(0.91); C794(1.01)  LDD1587  [6]
 LDCM0384  CL114 HEK-293T C561(0.95); C794(1.06)  LDD1588  [6]
 LDCM0385  CL115 HEK-293T C561(1.02); C794(1.04)  LDD1589  [6]
 LDCM0386  CL116 HEK-293T C561(1.16); C794(0.80)  LDD1590  [6]
 LDCM0387  CL117 HEK-293T C561(0.96); C794(1.01)  LDD1591  [6]
 LDCM0388  CL118 HEK-293T C561(0.76); C794(1.01)  LDD1592  [6]
 LDCM0389  CL119 HEK-293T C561(1.10); C794(1.01)  LDD1593  [6]
 LDCM0390  CL12 HEK-293T C561(1.20); C794(0.83)  LDD1594  [6]
 LDCM0391  CL120 HEK-293T C561(1.10); C794(1.06)  LDD1595  [6]
 LDCM0392  CL121 HEK-293T C561(0.94); C794(1.04)  LDD1596  [6]
 LDCM0393  CL122 HEK-293T C561(0.89); C794(1.01)  LDD1597  [6]
 LDCM0394  CL123 HEK-293T C561(1.55); C794(0.92)  LDD1598  [6]
 LDCM0395  CL124 HEK-293T C561(0.94); C794(1.21)  LDD1599  [6]
 LDCM0396  CL125 HEK-293T C561(1.00); C794(0.95)  LDD1600  [6]
 LDCM0397  CL126 HEK-293T C561(0.94); C794(0.97)  LDD1601  [6]
 LDCM0398  CL127 HEK-293T C561(1.02); C794(0.97)  LDD1602  [6]
 LDCM0399  CL128 HEK-293T C561(0.93); C794(0.93)  LDD1603  [6]
 LDCM0400  CL13 HEK-293T C561(0.97); C794(0.96)  LDD1604  [6]
 LDCM0401  CL14 HEK-293T C561(0.92); C794(1.05)  LDD1605  [6]
 LDCM0402  CL15 HEK-293T C561(1.14); C794(0.88)  LDD1606  [6]
 LDCM0403  CL16 HEK-293T C561(0.96); C794(1.16)  LDD1607  [6]
 LDCM0404  CL17 HEK-293T C794(0.95)  LDD1608  [6]
 LDCM0405  CL18 HEK-293T C794(0.99)  LDD1609  [6]
 LDCM0406  CL19 HEK-293T C561(1.17); C794(1.14)  LDD1610  [6]
 LDCM0407  CL2 HEK-293T C561(1.00); C794(0.97)  LDD1611  [6]
 LDCM0408  CL20 HEK-293T C561(1.11); C794(1.03)  LDD1612  [6]
 LDCM0409  CL21 HEK-293T C561(1.31); C794(0.99)  LDD1613  [6]
 LDCM0410  CL22 HEK-293T C561(0.97); C794(0.99)  LDD1614  [6]
 LDCM0411  CL23 HEK-293T C794(1.01)  LDD1615  [6]
 LDCM0412  CL24 HEK-293T C561(0.98); C794(0.97)  LDD1616  [6]
 LDCM0413  CL25 HEK-293T C561(1.06); C794(0.91)  LDD1617  [6]
 LDCM0414  CL26 HEK-293T C561(0.87); C794(1.16)  LDD1618  [6]
 LDCM0415  CL27 HEK-293T C561(1.15); C794(1.00)  LDD1619  [6]
 LDCM0416  CL28 HEK-293T C561(1.18); C794(1.03)  LDD1620  [6]
 LDCM0417  CL29 HEK-293T C794(1.13)  LDD1621  [6]
 LDCM0418  CL3 HEK-293T C561(1.41); C794(0.95)  LDD1622  [6]
 LDCM0419  CL30 HEK-293T C794(0.98)  LDD1623  [6]
 LDCM0420  CL31 HEK-293T C561(1.16); C794(1.01)  LDD1624  [6]
 LDCM0421  CL32 HEK-293T C561(1.12); C794(1.05)  LDD1625  [6]
 LDCM0422  CL33 HEK-293T C561(1.62); C794(0.90)  LDD1626  [6]
 LDCM0423  CL34 HEK-293T C561(1.15); C794(1.04)  LDD1627  [6]
 LDCM0424  CL35 HEK-293T C794(0.97)  LDD1628  [6]
 LDCM0425  CL36 HEK-293T C561(1.10); C794(1.06)  LDD1629  [6]
 LDCM0426  CL37 HEK-293T C561(0.95); C794(0.85)  LDD1630  [6]
 LDCM0428  CL39 HEK-293T C561(1.26); C794(1.00)  LDD1632  [6]
 LDCM0429  CL4 HEK-293T C561(1.20); C794(1.02)  LDD1633  [6]
 LDCM0430  CL40 HEK-293T C561(1.03); C794(0.85)  LDD1634  [6]
 LDCM0431  CL41 HEK-293T C794(1.05)  LDD1635  [6]
 LDCM0432  CL42 HEK-293T C794(1.02)  LDD1636  [6]
 LDCM0433  CL43 HEK-293T C561(1.16); C794(0.98)  LDD1637  [6]
 LDCM0434  CL44 HEK-293T C561(1.13); C794(1.01)  LDD1638  [6]
 LDCM0435  CL45 HEK-293T C561(1.42); C794(1.06)  LDD1639  [6]
 LDCM0436  CL46 HEK-293T C561(1.11); C794(0.92)  LDD1640  [6]
 LDCM0437  CL47 HEK-293T C794(1.14)  LDD1641  [6]
 LDCM0438  CL48 HEK-293T C561(0.87); C794(1.00)  LDD1642  [6]
 LDCM0439  CL49 HEK-293T C561(1.17); C794(0.93)  LDD1643  [6]
 LDCM0440  CL5 HEK-293T C794(1.09)  LDD1644  [6]
 LDCM0441  CL50 HEK-293T C561(0.95); C794(0.92)  LDD1645  [6]
 LDCM0443  CL52 HEK-293T C561(1.09); C794(0.85)  LDD1646  [6]
 LDCM0444  CL53 HEK-293T C794(1.11)  LDD1647  [6]
 LDCM0445  CL54 HEK-293T C794(0.90)  LDD1648  [6]
 LDCM0446  CL55 HEK-293T C561(1.22); C794(1.10)  LDD1649  [6]
 LDCM0447  CL56 HEK-293T C561(1.28); C794(0.93)  LDD1650  [6]
 LDCM0448  CL57 HEK-293T C561(1.23); C794(0.91)  LDD1651  [6]
 LDCM0449  CL58 HEK-293T C561(1.34); C794(0.94)  LDD1652  [6]
 LDCM0450  CL59 HEK-293T C794(0.95)  LDD1653  [6]
 LDCM0451  CL6 HEK-293T C794(1.00)  LDD1654  [6]
 LDCM0452  CL60 HEK-293T C561(0.91); C794(1.04)  LDD1655  [6]
 LDCM0453  CL61 HEK-293T C561(1.07); C794(0.98)  LDD1656  [6]
 LDCM0454  CL62 HEK-293T C561(0.85); C794(1.00)  LDD1657  [6]
 LDCM0455  CL63 HEK-293T C561(1.07); C794(0.87)  LDD1658  [6]
 LDCM0456  CL64 HEK-293T C561(1.16); C794(1.03)  LDD1659  [6]
 LDCM0457  CL65 HEK-293T C794(1.23)  LDD1660  [6]
 LDCM0458  CL66 HEK-293T C794(1.02)  LDD1661  [6]
 LDCM0459  CL67 HEK-293T C561(1.16); C794(1.04)  LDD1662  [6]
 LDCM0460  CL68 HEK-293T C561(1.28); C794(1.00)  LDD1663  [6]
 LDCM0461  CL69 HEK-293T C561(1.22); C794(1.02)  LDD1664  [6]
 LDCM0462  CL7 HEK-293T C561(1.00); C794(1.10)  LDD1665  [6]
 LDCM0463  CL70 HEK-293T C561(0.97); C794(1.00)  LDD1666  [6]
 LDCM0464  CL71 HEK-293T C794(0.95)  LDD1667  [6]
 LDCM0465  CL72 HEK-293T C561(0.98); C794(0.92)  LDD1668  [6]
 LDCM0466  CL73 HEK-293T C561(0.94); C794(0.95)  LDD1669  [6]
 LDCM0467  CL74 HEK-293T C561(0.93); C794(1.07)  LDD1670  [6]
 LDCM0469  CL76 HEK-293T C561(1.02); C794(0.94)  LDD1672  [6]
 LDCM0470  CL77 HEK-293T C794(1.08)  LDD1673  [6]
 LDCM0471  CL78 HEK-293T C794(1.01)  LDD1674  [6]
 LDCM0472  CL79 HEK-293T C561(1.14); C794(1.02)  LDD1675  [6]
 LDCM0473  CL8 HEK-293T C561(1.68); C794(0.80)  LDD1676  [6]
 LDCM0474  CL80 HEK-293T C561(1.02); C794(0.95)  LDD1677  [6]
 LDCM0475  CL81 HEK-293T C561(1.25); C794(1.04)  LDD1678  [6]
 LDCM0476  CL82 HEK-293T C561(1.00); C794(0.97)  LDD1679  [6]
 LDCM0477  CL83 HEK-293T C794(0.99)  LDD1680  [6]
 LDCM0478  CL84 HEK-293T C561(1.03); C794(0.88)  LDD1681  [6]
 LDCM0479  CL85 HEK-293T C561(0.96); C794(0.88)  LDD1682  [6]
 LDCM0480  CL86 HEK-293T C561(0.76); C794(1.01)  LDD1683  [6]
 LDCM0481  CL87 HEK-293T C561(1.04); C794(0.94)  LDD1684  [6]
 LDCM0482  CL88 HEK-293T C561(0.86); C794(0.85)  LDD1685  [6]
 LDCM0483  CL89 HEK-293T C794(1.02)  LDD1686  [6]
 LDCM0484  CL9 HEK-293T C561(1.29); C794(1.07)  LDD1687  [6]
 LDCM0485  CL90 HEK-293T C794(0.86)  LDD1688  [6]
 LDCM0486  CL91 HEK-293T C561(1.07); C794(0.98)  LDD1689  [6]
 LDCM0487  CL92 HEK-293T C561(1.21); C794(0.94)  LDD1690  [6]
 LDCM0488  CL93 HEK-293T C561(1.16); C794(1.00)  LDD1691  [6]
 LDCM0489  CL94 HEK-293T C561(1.15); C794(1.02)  LDD1692  [6]
 LDCM0490  CL95 HEK-293T C794(0.86)  LDD1693  [6]
 LDCM0491  CL96 HEK-293T C561(1.26); C794(0.80)  LDD1694  [6]
 LDCM0492  CL97 HEK-293T C561(1.24); C794(0.92)  LDD1695  [6]
 LDCM0493  CL98 HEK-293T C561(0.95); C794(0.97)  LDD1696  [6]
 LDCM0494  CL99 HEK-293T C561(1.17); C794(0.99)  LDD1697  [6]
 LDCM0495  E2913 HEK-293T C561(1.04); C794(1.03)  LDD1698  [6]
 LDCM0468  Fragment33 HEK-293T C561(0.96); C794(0.92)  LDD1671  [6]
 LDCM0427  Fragment51 HEK-293T C561(0.83); C794(1.03)  LDD1631  [6]
 LDCM0022  KB02 HEK-293T C794(0.93)  LDD1492  [6]
 LDCM0023  KB03 HEK-293T C794(1.17)  LDD1497  [6]
 LDCM0024  KB05 G361 C561(4.76)  LDD3311  [1]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C561(1.04)  LDD2137  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Calcineurin B homologous protein 1 (CHP1) Calcineurin regulatory subunit family Q99653
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Calcineurin B homologous protein 2 (CHP2) Calcineurin regulatory subunit family O43745
Calcineurin B homologous protein 3 (TESC) Calcineurin regulatory subunit family Q96BS2

The Drug(s) Related To This Target

Approved
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Amiloride Small molecular drug DB00594
Memantine Small molecular drug DB01043
Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Zoniporide Hydrochloride Small molecular drug D0C8PI
Investigative
Click To Hide/Show 17 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
5'-(N-ethyl-n-isopropyl)Amiloride Small molecular drug D0V5NZ
Biib-513 Small molecular drug D0NS9C
Cariporide Small molecular drug DB06468
Homoserine Lactone Small molecular drug D07WXS
N-(3-methanesulfonyl-4-methoxy-benzoyl)-guanidine Small molecular drug D07DUW
N-(3-methanesulfonyl-4-methyl-benzoyl)-guanidine Small molecular drug D03AGV
N-(4-bromo-3-methanesulfonyl-benzoyl)-guanidine Small molecular drug D05CQR
N-(4-chloro-3-methanesulfonyl-benzoyl)-guanidine Small molecular drug D04OTF
N-(4-cyano-3-methanesulfonyl-benzoyl)-guanidine Small molecular drug D04UMY
N-(5-m-tolyl-furan-2-carbonyl)-guanidine Small molecular drug D06AKW
N-(5-methanesulfonyl-2-methyl-benzoyl)-guanidine Small molecular drug D0T1OG
N-(5-o-tolyl-furan-2-carbonyl)-guanidine Small molecular drug D08BDI
N-(5-phenyl-furan-2-carbonyl)-guanidine Small molecular drug D09ZSK
N-[2-(1h-benzoimidazol-2-yl)-benzoyl]-guanidine Small molecular drug D01RDB
N-[4-(1h-benzoimidazol-2-yl)-benzoyl]-guanidine Small molecular drug D0Y4CC
N-[5-(2-ethyl-phenyl)-furan-2-carbonyl]-guanidine Small molecular drug D01ZIP
N-[5-(2-nitro-phenyl)-furan-2-carbonyl]-guanidine Small molecular drug D0D3OX
Discontinued
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cariporide Small molecular drug D0N8QQ
Eniporide Small molecular drug D0V9RU
Hoe-694 Small molecular drug D0K2CV

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
2 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
3 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
4 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
5 DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling. Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202205348. doi: 10.1002/anie.202205348. Epub 2022 Aug 22.
Mass spectrometry data entry: PXD033004
6 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