Details of the Target

General Information of Target

Target ID LDTP01398
Target Name Organic cation/carnitine transporter 2 (SLC22A5)
Gene Name SLC22A5
Gene ID 6584
Synonyms
OCTN2; Organic cation/carnitine transporter 2; High-affinity sodium-dependent carnitine cotransporter; Solute carrier family 22 member 5
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MRDYDEVTAFLGEWGPFQRLIFFLLSASIIPNGFTGLSSVFLIATPEHRCRVPDAANLSS
AWRNHTVPLRLRDGREVPHSCRRYRLATIANFSALGLEPGRDVDLGQLEQESCLDGWEFS
QDVYLSTIVTEWNLVCEDDWKAPLTISLFFVGVLLGSFISGQLSDRFGRKNVLFVTMGMQ
TGFSFLQIFSKNFEMFVVLFVLVGMGQISNYVAAFVLGTEILGKSVRIIFSTLGVCIFYA
FGYMVLPLFAYFIRDWRMLLVALTMPGVLCVALWWFIPESPRWLISQGRFEEAEVIIRKA
AKANGIVVPSTIFDPSELQDLSSKKQQSHNILDLLRTWNIRMVTIMSIMLWMTISVGYFG
LSLDTPNLHGDIFVNCFLSAMVEVPAYVLAWLLLQYLPRRYSMATALFLGGSVLLFMQLV
PPDLYYLATVLVMVGKFGVTAAFSMVYVYTAELYPTVVRNMGVGVSSTASRLGSILSPYF
VYLGAYDRFLPYILMGSLTILTAILTLFLPESFGTPLPDTIDQMLRVKGMKHRKTPSHTR
MLKDGQERPTILKSTAF
Target Bioclass
Transporter and channel
Family
Major facilitator (TC 2.A.1) superfamily, Organic cation transporter (TC 2.A.1.19) family
Subcellular location
Endoplasmic reticulum; Cell membrane
Function
Sodium-ion dependent, high affinity carnitine transporter. Involved in the active cellular uptake of carnitine. Transports one sodium ion with one molecule of carnitine . Also transports organic cations such as tetraethylammonium (TEA) without the involvement of sodium. Relative uptake activity ratio of carnitine to TEA is 11.3. In intestinal epithelia, transports the quorum-sensing pentapeptide CSF (competence and sporulation factor) from Bacillus Subtilis wich induces cytoprotective heat shock proteins contributing to intestinal homeostasis. May also contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable).; [Isoform 3]: Retained in the ER, unable to perform carnitine uptake.
Uniprot ID
O76082
Ensemble ID
ENST00000245407.8
HGNC ID
HGNC:10969
ChEMBL ID
CHEMBL2073693

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 SNV: p.V268G .
HT115 SNV: p.L415P .
SKMEL2 SNV: p.G96V .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C81(2.70)  LDD3310  [1]
IA-alkyne
 Probe Info  		N.A.  LDD0162  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C81(1.07)  LDD1507  [3]
 LDCM0215  AC10 HEK-293T C81(1.01)  LDD1508  [3]
 LDCM0226  AC11 HEK-293T C81(1.00)  LDD1509  [3]
 LDCM0237  AC12 HEK-293T C81(0.93)  LDD1510  [3]
 LDCM0259  AC14 HEK-293T C81(1.03)  LDD1512  [3]
 LDCM0270  AC15 HEK-293T C81(1.10)  LDD1513  [3]
 LDCM0276  AC17 HEK-293T C81(1.26)  LDD1515  [3]
 LDCM0277  AC18 HEK-293T C81(1.02)  LDD1516  [3]
 LDCM0278  AC19 HEK-293T C81(1.56)  LDD1517  [3]
 LDCM0279  AC2 HEK-293T C81(1.06)  LDD1518  [3]
 LDCM0280  AC20 HEK-293T C81(1.02)  LDD1519  [3]
 LDCM0281  AC21 HEK-293T C81(1.03)  LDD1520  [3]
 LDCM0282  AC22 HEK-293T C81(1.11)  LDD1521  [3]
 LDCM0283  AC23 HEK-293T C81(1.07)  LDD1522  [3]
 LDCM0284  AC24 HEK-293T C81(0.98)  LDD1523  [3]
 LDCM0285  AC25 HEK-293T C81(1.01)  LDD1524  [3]
 LDCM0286  AC26 HEK-293T C81(0.97)  LDD1525  [3]
 LDCM0287  AC27 HEK-293T C81(0.98)  LDD1526  [3]
 LDCM0288  AC28 HEK-293T C81(0.93)  LDD1527  [3]
 LDCM0289  AC29 HEK-293T C81(0.85)  LDD1528  [3]
 LDCM0290  AC3 HEK-293T C81(1.05)  LDD1529  [3]
 LDCM0291  AC30 HEK-293T C81(1.14)  LDD1530  [3]
 LDCM0292  AC31 HEK-293T C81(0.94)  LDD1531  [3]
 LDCM0293  AC32 HEK-293T C81(0.94)  LDD1532  [3]
 LDCM0294  AC33 HEK-293T C81(1.10)  LDD1533  [3]
 LDCM0295  AC34 HEK-293T C81(1.03)  LDD1534  [3]
 LDCM0296  AC35 HEK-293T C81(1.09)  LDD1535  [3]
 LDCM0297  AC36 HEK-293T C81(1.00)  LDD1536  [3]
 LDCM0298  AC37 HEK-293T C81(1.06)  LDD1537  [3]
 LDCM0299  AC38 HEK-293T C81(1.01)  LDD1538  [3]
 LDCM0300  AC39 HEK-293T C81(1.00)  LDD1539  [3]
 LDCM0301  AC4 HEK-293T C81(0.91)  LDD1540  [3]
 LDCM0302  AC40 HEK-293T C81(0.90)  LDD1541  [3]
 LDCM0303  AC41 HEK-293T C81(1.16)  LDD1542  [3]
 LDCM0304  AC42 HEK-293T C81(1.06)  LDD1543  [3]
 LDCM0305  AC43 HEK-293T C81(1.09)  LDD1544  [3]
 LDCM0306  AC44 HEK-293T C81(0.99)  LDD1545  [3]
 LDCM0307  AC45 HEK-293T C81(0.89)  LDD1546  [3]
 LDCM0308  AC46 HEK-293T C81(1.18)  LDD1547  [3]
 LDCM0309  AC47 HEK-293T C81(0.98)  LDD1548  [3]
 LDCM0310  AC48 HEK-293T C81(0.92)  LDD1549  [3]
 LDCM0311  AC49 HEK-293T C81(1.09)  LDD1550  [3]
 LDCM0312  AC5 HEK-293T C81(0.83)  LDD1551  [3]
 LDCM0313  AC50 HEK-293T C81(0.98)  LDD1552  [3]
 LDCM0314  AC51 HEK-293T C81(0.99)  LDD1553  [3]
 LDCM0315  AC52 HEK-293T C81(0.98)  LDD1554  [3]
 LDCM0316  AC53 HEK-293T C81(0.99)  LDD1555  [3]
 LDCM0317  AC54 HEK-293T C81(1.01)  LDD1556  [3]
 LDCM0318  AC55 HEK-293T C81(0.94)  LDD1557  [3]
 LDCM0319  AC56 HEK-293T C81(0.97)  LDD1558  [3]
 LDCM0320  AC57 HEK-293T C81(1.06)  LDD1559  [3]
 LDCM0321  AC58 HEK-293T C81(1.09)  LDD1560  [3]
 LDCM0322  AC59 HEK-293T C81(0.97)  LDD1561  [3]
 LDCM0323  AC6 HEK-293T C81(1.02)  LDD1562  [3]
 LDCM0324  AC60 HEK-293T C81(0.99)  LDD1563  [3]
 LDCM0325  AC61 HEK-293T C81(1.22)  LDD1564  [3]
 LDCM0326  AC62 HEK-293T C81(1.14)  LDD1565  [3]
 LDCM0327  AC63 HEK-293T C81(1.18)  LDD1566  [3]
 LDCM0328  AC64 HEK-293T C81(0.87)  LDD1567  [3]
 LDCM0334  AC7 HEK-293T C81(1.08)  LDD1568  [3]
 LDCM0345  AC8 HEK-293T C81(0.89)  LDD1569  [3]
 LDCM0248  AKOS034007472 HEK-293T C81(1.05)  LDD1511  [3]
 LDCM0356  AKOS034007680 HEK-293T C81(1.05)  LDD1570  [3]
 LDCM0275  AKOS034007705 HEK-293T C81(0.94)  LDD1514  [3]
 LDCM0368  CL10 HEK-293T C81(1.20)  LDD1572  [3]
 LDCM0369  CL100 HEK-293T C81(1.16)  LDD1573  [3]
 LDCM0371  CL102 HEK-293T C81(1.09)  LDD1575  [3]
 LDCM0372  CL103 HEK-293T C81(0.97)  LDD1576  [3]
 LDCM0373  CL104 HEK-293T C81(1.03)  LDD1577  [3]
 LDCM0375  CL106 HEK-293T C81(0.97)  LDD1579  [3]
 LDCM0376  CL107 HEK-293T C81(0.96)  LDD1580  [3]
 LDCM0377  CL108 HEK-293T C81(1.06)  LDD1581  [3]
 LDCM0379  CL11 HEK-293T C81(1.18)  LDD1583  [3]
 LDCM0380  CL110 HEK-293T C81(1.19)  LDD1584  [3]
 LDCM0381  CL111 HEK-293T C81(0.92)  LDD1585  [3]
 LDCM0382  CL112 HEK-293T C81(1.01)  LDD1586  [3]
 LDCM0384  CL114 HEK-293T C81(1.37)  LDD1588  [3]
 LDCM0385  CL115 HEK-293T C81(0.94)  LDD1589  [3]
 LDCM0386  CL116 HEK-293T C81(1.04)  LDD1590  [3]
 LDCM0388  CL118 HEK-293T C81(1.07)  LDD1592  [3]
 LDCM0389  CL119 HEK-293T C81(1.00)  LDD1593  [3]
 LDCM0390  CL12 HEK-293T C81(0.90)  LDD1594  [3]
 LDCM0391  CL120 HEK-293T C81(1.22)  LDD1595  [3]
 LDCM0393  CL122 HEK-293T C81(1.20)  LDD1597  [3]
 LDCM0394  CL123 HEK-293T C81(0.98)  LDD1598  [3]
 LDCM0395  CL124 HEK-293T C81(1.19)  LDD1599  [3]
 LDCM0397  CL126 HEK-293T C81(1.21)  LDD1601  [3]
 LDCM0398  CL127 HEK-293T C81(1.04)  LDD1602  [3]
 LDCM0399  CL128 HEK-293T C81(1.09)  LDD1603  [3]
 LDCM0401  CL14 HEK-293T C81(1.26)  LDD1605  [3]
 LDCM0402  CL15 HEK-293T C81(1.22)  LDD1606  [3]
 LDCM0403  CL16 HEK-293T C81(1.13)  LDD1607  [3]
 LDCM0404  CL17 HEK-293T C81(1.29)  LDD1608  [3]
 LDCM0405  CL18 HEK-293T C81(1.13)  LDD1609  [3]
 LDCM0406  CL19 HEK-293T C81(1.07)  LDD1610  [3]
 LDCM0407  CL2 HEK-293T C81(0.99)  LDD1611  [3]
 LDCM0408  CL20 HEK-293T C81(1.13)  LDD1612  [3]
 LDCM0409  CL21 HEK-293T C81(1.16)  LDD1613  [3]
 LDCM0410  CL22 HEK-293T C81(1.08)  LDD1614  [3]
 LDCM0411  CL23 HEK-293T C81(1.04)  LDD1615  [3]
 LDCM0412  CL24 HEK-293T C81(1.00)  LDD1616  [3]
 LDCM0414  CL26 HEK-293T C81(1.06)  LDD1618  [3]
 LDCM0415  CL27 HEK-293T C81(0.91)  LDD1619  [3]
 LDCM0416  CL28 HEK-293T C81(1.08)  LDD1620  [3]
 LDCM0417  CL29 HEK-293T C81(1.03)  LDD1621  [3]
 LDCM0418  CL3 HEK-293T C81(0.92)  LDD1622  [3]
 LDCM0419  CL30 HEK-293T C81(1.04)  LDD1623  [3]
 LDCM0420  CL31 HEK-293T C81(1.23)  LDD1624  [3]
 LDCM0421  CL32 HEK-293T C81(1.11)  LDD1625  [3]
 LDCM0422  CL33 HEK-293T C81(1.25)  LDD1626  [3]
 LDCM0423  CL34 HEK-293T C81(1.12)  LDD1627  [3]
 LDCM0424  CL35 HEK-293T C81(1.13)  LDD1628  [3]
 LDCM0425  CL36 HEK-293T C81(1.00)  LDD1629  [3]
 LDCM0428  CL39 HEK-293T C81(1.10)  LDD1632  [3]
 LDCM0429  CL4 HEK-293T C81(1.09)  LDD1633  [3]
 LDCM0430  CL40 HEK-293T C81(1.02)  LDD1634  [3]
 LDCM0431  CL41 HEK-293T C81(1.06)  LDD1635  [3]
 LDCM0432  CL42 HEK-293T C81(1.03)  LDD1636  [3]
 LDCM0433  CL43 HEK-293T C81(1.07)  LDD1637  [3]
 LDCM0434  CL44 HEK-293T C81(1.04)  LDD1638  [3]
 LDCM0435  CL45 HEK-293T C81(0.91)  LDD1639  [3]
 LDCM0436  CL46 HEK-293T C81(1.25)  LDD1640  [3]
 LDCM0437  CL47 HEK-293T C81(1.15)  LDD1641  [3]
 LDCM0438  CL48 HEK-293T C81(0.92)  LDD1642  [3]
 LDCM0440  CL5 HEK-293T C81(1.04)  LDD1644  [3]
 LDCM0441  CL50 HEK-293T C81(1.27)  LDD1645  [3]
 LDCM0443  CL52 HEK-293T C81(1.15)  LDD1646  [3]
 LDCM0444  CL53 HEK-293T C81(1.23)  LDD1647  [3]
 LDCM0445  CL54 HEK-293T C81(1.06)  LDD1648  [3]
 LDCM0446  CL55 HEK-293T C81(1.03)  LDD1649  [3]
 LDCM0447  CL56 HEK-293T C81(1.05)  LDD1650  [3]
 LDCM0448  CL57 HEK-293T C81(1.26)  LDD1651  [3]
 LDCM0449  CL58 HEK-293T C81(1.27)  LDD1652  [3]
 LDCM0450  CL59 HEK-293T C81(1.24)  LDD1653  [3]
 LDCM0451  CL6 HEK-293T C81(1.16)  LDD1654  [3]
 LDCM0452  CL60 HEK-293T C81(1.08)  LDD1655  [3]
 LDCM0454  CL62 HEK-293T C81(1.15)  LDD1657  [3]
 LDCM0455  CL63 HEK-293T C81(1.05)  LDD1658  [3]
 LDCM0456  CL64 HEK-293T C81(1.30)  LDD1659  [3]
 LDCM0457  CL65 HEK-293T C81(1.11)  LDD1660  [3]
 LDCM0458  CL66 HEK-293T C81(1.17)  LDD1661  [3]
 LDCM0459  CL67 HEK-293T C81(1.06)  LDD1662  [3]
 LDCM0460  CL68 HEK-293T C81(1.02)  LDD1663  [3]
 LDCM0461  CL69 HEK-293T C81(1.21)  LDD1664  [3]
 LDCM0462  CL7 HEK-293T C81(1.18)  LDD1665  [3]
 LDCM0463  CL70 HEK-293T C81(0.98)  LDD1666  [3]
 LDCM0464  CL71 HEK-293T C81(1.17)  LDD1667  [3]
 LDCM0465  CL72 HEK-293T C81(1.10)  LDD1668  [3]
 LDCM0467  CL74 HEK-293T C81(1.03)  LDD1670  [3]
 LDCM0469  CL76 HEK-293T C81(0.94)  LDD1672  [3]
 LDCM0470  CL77 HEK-293T C81(1.07)  LDD1673  [3]
 LDCM0471  CL78 HEK-293T C81(1.10)  LDD1674  [3]
 LDCM0472  CL79 HEK-293T C81(1.14)  LDD1675  [3]
 LDCM0473  CL8 HEK-293T C81(1.40)  LDD1676  [3]
 LDCM0474  CL80 HEK-293T C81(1.14)  LDD1677  [3]
 LDCM0475  CL81 HEK-293T C81(0.91)  LDD1678  [3]
 LDCM0476  CL82 HEK-293T C81(1.06)  LDD1679  [3]
 LDCM0477  CL83 HEK-293T C81(1.02)  LDD1680  [3]
 LDCM0478  CL84 HEK-293T C81(0.92)  LDD1681  [3]
 LDCM0480  CL86 HEK-293T C81(1.14)  LDD1683  [3]
 LDCM0481  CL87 HEK-293T C81(0.92)  LDD1684  [3]
 LDCM0482  CL88 HEK-293T C81(1.15)  LDD1685  [3]
 LDCM0483  CL89 HEK-293T C81(1.12)  LDD1686  [3]
 LDCM0484  CL9 HEK-293T C81(0.91)  LDD1687  [3]
 LDCM0485  CL90 HEK-293T C81(1.55)  LDD1688  [3]
 LDCM0486  CL91 HEK-293T C81(1.01)  LDD1689  [3]
 LDCM0487  CL92 HEK-293T C81(1.05)  LDD1690  [3]
 LDCM0488  CL93 HEK-293T C81(0.97)  LDD1691  [3]
 LDCM0489  CL94 HEK-293T C81(1.04)  LDD1692  [3]
 LDCM0490  CL95 HEK-293T C81(1.35)  LDD1693  [3]
 LDCM0491  CL96 HEK-293T C81(1.07)  LDD1694  [3]
 LDCM0493  CL98 HEK-293T C81(1.16)  LDD1696  [3]
 LDCM0494  CL99 HEK-293T C81(0.95)  LDD1697  [3]
 LDCM0495  E2913 HEK-293T C81(1.11)  LDD1698  [3]
 LDCM0468  Fragment33 HEK-293T C81(1.18)  LDD1671  [3]
 LDCM0427  Fragment51 HEK-293T C81(1.09)  LDD1631  [3]
 LDCM0022  KB02 HEK-293T C81(1.15)  LDD1492  [3]
 LDCM0023  KB03 HEK-293T C81(1.08)  LDD1497  [3]
 LDCM0024  KB05 COLO792 C81(2.70)  LDD3310  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Keratin, type I cuticular Ha4 (KRT34) Intermediate filament family O76011
Keratin, type I cytoskeletal 27 (KRT27) Intermediate filament family Q7Z3Y8
Notch homolog 2 N-terminal-like protein C (NOTCH2NLC) NOTCH family P0DPK4

The Drug(s) Related To This Target

Approved
Click To Hide/Show 52 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Acetylcholine Small molecular drug DB03128
Amphetamine Small molecular drug DB00182
Ampicillin Small molecular drug DB00415
Benzylpenicillin Small molecular drug DB01053
Cefadroxil Small molecular drug DB01140
Cefalotin Small molecular drug DB00456
Cefdinir Small molecular drug DB00535
Cefepime Small molecular drug DB01413
Cefixime Small molecular drug DB00671
Cefradine Small molecular drug DB01333
Cephalexin Small molecular drug DB00567
Cephaloglycin Small molecular drug DB00689
Choline Small molecular drug DB00122
Choline Salicylate Small molecular drug DB14006
Cimetidine Small molecular drug DB00501
Clonidine Small molecular drug DB00575
Creatine Small molecular drug DB00148
Cyclacillin Small molecular drug DB01000
Dactinomycin Small molecular drug DB00970
Desipramine Small molecular drug DB01151
Diphenhydramine Small molecular drug DB01075
Dopamine Small molecular drug DB00988
Formoterol Small molecular drug DB00983
Furosemide Small molecular drug DB00695
Grepafloxacin Small molecular drug DB00365
Guanidine Small molecular drug DB00536
Histamine Small molecular drug DB05381
Imatinib Small molecular drug DB00619
Ipratropium Small molecular drug DB00332
Levamlodipine Small molecular drug DB09237
Levocarnitine Small molecular drug DB00583
Lidocaine Small molecular drug DB00281
Lomefloxacin Small molecular drug DB00978
Mepyramine Small molecular drug DB06691
Metamfetamine Small molecular drug DB01577
Methacholine Small molecular drug DB06709
Niacin Small molecular drug DB00627
Nicotine Small molecular drug DB00184
Norepinephrine Small molecular drug DB00368
Norfloxacin Small molecular drug DB01059
Ofloxacin Small molecular drug DB01165
Probenecid Small molecular drug DB01032
Procainamide Small molecular drug DB01035
Quinidine Small molecular drug DB00908
Quinine Small molecular drug DB00468
Sparfloxacin Small molecular drug DB01208
Terbutaline Small molecular drug DB00871
Thiamine Small molecular drug DB00152
Tiotropium Small molecular drug DB01409
Valproic Acid Small molecular drug DB00313
Verapamil Small molecular drug DB00661
Solriamfetol . DB14754
Investigative
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Aldosterone Small molecular drug DB04630
Arginine Small molecular drug DB00125
Azidocillin Small molecular drug DB08795
Degraded Cephaloridine Small molecular drug DB04133
Tetraethylammonium Small molecular drug DB08837

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 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
3 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