Details of the Target

General Information of Target

Target ID LDTP05408
Target Name Antigen peptide transporter 1 (TAP1)
Gene Name TAP1
Gene ID 6890
Synonyms
ABCB2; PSF1; RING4; Y3; Antigen peptide transporter 1; APT1; EC 7.4.2.14; ATP-binding cassette sub-family B member 2; Peptide supply factor 1; Peptide transporter PSF1; PSF-1; Peptide transporter TAP1; Peptide transporter involved in antigen processing 1; Really interesting new gene 4 protein; RING4
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MASSRCPAPRGCRCLPGASLAWLGTVLLLLADWVLLRTALPRIFSLLVPTALPLLRVWAV
GLSRWAVLWLGACGVLRATVGSKSENAGAQGWLAALKPLAAALGLALPGLALFRELISWG
APGSADSTRLLHWGSHPTAFVVSYAAALPAAALWHKLGSLWVPGGQGGSGNPVRRLLGCL
GSETRRLSLFLVLVVLSSLGEMAIPFFTGRLTDWILQDGSADTFTRNLTLMSILTIASAV
LEFVGDGIYNNTMGHVHSHLQGEVFGAVLRQETEFFQQNQTGNIMSRVTEDTSTLSDSLS
ENLSLFLWYLVRGLCLLGIMLWGSVSLTMVTLITLPLLFLLPKKVGKWYQLLEVQVRESL
AKSSQVAIEALSAMPTVRSFANEEGEAQKFREKLQEIKTLNQKEAVAYAVNSWTTSISGM
LLKVGILYIGGQLVTSGAVSSGNLVTFVLYQMQFTQAVEVLLSIYPRVQKAVGSSEKIFE
YLDRTPRCPPSGLLTPLHLEGLVQFQDVSFAYPNRPDVLVLQGLTFTLRPGEVTALVGPN
GSGKSTVAALLQNLYQPTGGQLLLDGKPLPQYEHRYLHRQVAAVGQEPQVFGRSLQENIA
YGLTQKPTMEEITAAAVKSGAHSFISGLPQGYDTEVDEAGSQLSGGQRQAVALARALIRK
PCVLILDDATSALDANSQLQVEQLLYESPERYSRSVLLITQHLSLVEQADHILFLEGGAI
REGGTHQQLMEKKGCYWAMVQAPADAPE
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
ABC transporter superfamily, ABCB family, MHC peptide exporter (TC 3.A.1.209) subfamily
Subcellular location
Endoplasmic reticulum membrane
Function
ABC transporter associated with antigen processing. In complex with TAP2 mediates unidirectional translocation of peptide antigens from cytosol to endoplasmic reticulum (ER) for loading onto MHC class I (MHCI) molecules. Uses the chemical energy of ATP to export peptides against the concentration gradient. During the transport cycle alternates between 'inward-facing' state with peptide binding site facing the cytosol to 'outward-facing' state with peptide binding site facing the ER lumen. Peptide antigen binding to ATP-loaded TAP1-TAP2 induces a switch to hydrolysis-competent 'outward-facing' conformation ready for peptide loading onto nascent MHCI molecules. Subsequently ATP hydrolysis resets the transporter to the 'inward facing' state for a new cycle. Typically transports intracellular peptide antigens of 8 to 13 amino acids that arise from cytosolic proteolysis via IFNG-induced immunoproteasome. Binds peptides with free N- and C-termini, the first three and the C-terminal residues being critical. Preferentially selects peptides having a highly hydrophobic residue at position 3 and hydrophobic or charged residues at the C-terminal anchor. Proline at position 2 has the most destabilizing effect. As a component of the peptide loading complex (PLC), acts as a molecular scaffold essential for peptide-MHCI assembly and antigen presentation.
TTD ID
T22945
Uniprot ID
Q03518
DrugMap ID
TT7JZI8
Ensemble ID
ENST00000354258.5
HGNC ID
HGNC:43
ChEMBL ID
CHEMBL4523275

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
8505C SNV: p.P98T .
CHL1 SNV: p.R185P .
HT SNV: p.L335R; p.Y481C .
L428 SNV: p.V366G .
NCIH82 SNV: p.R56W .
P31FUJ SNV: p.G109V .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 18 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
CY-1
 Probe Info  		100.00  LDD0243  [1]
CY4
 Probe Info  		100.00  LDD0244  [1]
N1
 Probe Info  		100.00  LDD0242  [1]
YN-4
 Probe Info  		100.00  LDD0445  [2]
STPyne
 Probe Info  		K458(7.04); K530(8.33); K537(7.69)  LDD0277  [3]
IPM
 Probe Info  		N.A.  LDD0241  [4]
m-APA
 Probe Info  		11.43  LDD0403  [5]
BTD
 Probe Info  		C239(1.49)  LDD2136  [6]
Johansson_61
 Probe Info  		_(7.53)  LDD1490  [7]
YY4-yne
 Probe Info  		3.87  LDD0400  [8]
HPAP
 Probe Info  		3.37  LDD0064  [9]
DBIA
 Probe Info  		C795(0.88)  LDD0078  [10]
4-Iodoacetamidophenylacetylene
 Probe Info  		C662(0.00); C179(0.00)  LDD0038  [11]
IA-alkyne
 Probe Info  		C662(0.00); C179(0.00)  LDD0036  [11]
Lodoacetamide azide
 Probe Info  		C179(0.00); C662(0.00)  LDD0037  [11]
TFBX
 Probe Info  		N.A.  LDD0027  [12]
W1
 Probe Info  		N.A.  LDD0236  [4]
AOyne
 Probe Info  		10.50  LDD0443  [13]
PAL-AfBPP Probe
Click To Hide/Show 43 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C001
 Probe Info  		5.24  LDD1711  [14]
C004
 Probe Info  		6.23  LDD1714  [14]
C007
 Probe Info  		5.10  LDD1716  [14]
C022
 Probe Info  		12.13  LDD1728  [14]
C026
 Probe Info  		5.70  LDD1732  [14]
C106
 Probe Info  		20.25  LDD1793  [14]
C107
 Probe Info  		6.96  LDD1794  [14]
C112
 Probe Info  		20.25  LDD1799  [14]
C134
 Probe Info  		23.92  LDD1816  [14]
C138
 Probe Info  		16.00  LDD1820  [14]
C140
 Probe Info  		16.56  LDD1822  [14]
C141
 Probe Info  		9.85  LDD1823  [14]
C143
 Probe Info  		13.45  LDD1825  [14]
C145
 Probe Info  		8.51  LDD1827  [14]
C158
 Probe Info  		21.41  LDD1838  [14]
C159
 Probe Info  		8.34  LDD1839  [14]
C161
 Probe Info  		10.41  LDD1841  [14]
C177
 Probe Info  		8.57  LDD1856  [14]
C210
 Probe Info  		46.21  LDD1884  [14]
C218
 Probe Info  		38.85  LDD1892  [14]
C219
 Probe Info  		14.72  LDD1893  [14]
C220
 Probe Info  		23.59  LDD1894  [14]
C231
 Probe Info  		11.79  LDD1904  [14]
C240
 Probe Info  		11.39  LDD1913  [14]
C242
 Probe Info  		5.13  LDD1915  [14]
C243
 Probe Info  		12.55  LDD1916  [14]
C244
 Probe Info  		16.91  LDD1917  [14]
C246
 Probe Info  		25.99  LDD1919  [14]
C249
 Probe Info  		12.82  LDD1922  [14]
C252
 Probe Info  		8.57  LDD1925  [14]
C265
 Probe Info  		16.68  LDD1936  [14]
C271
 Probe Info  		4.92  LDD1941  [14]
C285
 Probe Info  		20.97  LDD1955  [14]
C287
 Probe Info  		10.78  LDD1957  [14]
C288
 Probe Info  		6.73  LDD1958  [14]
C289
 Probe Info  		37.01  LDD1959  [14]
C290
 Probe Info  		5.66  LDD1960  [14]
C293
 Probe Info  		18.13  LDD1963  [14]
C310
 Probe Info  		11.88  LDD1977  [14]
C403
 Probe Info  		14.22  LDD2061  [14]
STS-1
 Probe Info  		N.A.  LDD0137  [15]
STS-2
 Probe Info  		N.A.  LDD0139  [15]
OEA-DA
 Probe Info  		5.54  LDD0046  [16]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HCT 116 C239(1.08); C795(0.87)  LDD0531  [10]
 LDCM0215  AC10 HCT 116 C239(0.80); C795(0.89)  LDD0532  [10]
 LDCM0216  AC100 HCT 116 C239(0.92); C795(0.93)  LDD0533  [10]
 LDCM0217  AC101 HCT 116 C239(0.95); C795(0.90)  LDD0534  [10]
 LDCM0218  AC102 HCT 116 C239(0.78); C795(0.88)  LDD0535  [10]
 LDCM0219  AC103 HCT 116 C239(0.89); C795(0.97)  LDD0536  [10]
 LDCM0220  AC104 HCT 116 C239(0.94); C795(0.93)  LDD0537  [10]
 LDCM0221  AC105 HCT 116 C239(1.04); C795(0.83)  LDD0538  [10]
 LDCM0222  AC106 HCT 116 C239(0.83); C795(0.87)  LDD0539  [10]
 LDCM0223  AC107 HCT 116 C239(0.86); C795(0.87)  LDD0540  [10]
 LDCM0224  AC108 HCT 116 C239(0.93); C795(0.85)  LDD0541  [10]
 LDCM0225  AC109 HCT 116 C239(1.03); C795(1.01)  LDD0542  [10]
 LDCM0226  AC11 HCT 116 C239(0.88); C795(1.08)  LDD0543  [10]
 LDCM0227  AC110 HCT 116 C239(1.00); C795(1.05)  LDD0544  [10]
 LDCM0228  AC111 HCT 116 C239(0.92); C795(1.04)  LDD0545  [10]
 LDCM0229  AC112 HCT 116 C239(0.87); C795(0.91)  LDD0546  [10]
 LDCM0230  AC113 HCT 116 C795(0.91)  LDD0547  [10]
 LDCM0231  AC114 HCT 116 C795(0.92)  LDD0548  [10]
 LDCM0232  AC115 HCT 116 C795(0.95)  LDD0549  [10]
 LDCM0233  AC116 HCT 116 C795(0.88)  LDD0550  [10]
 LDCM0234  AC117 HCT 116 C795(0.94)  LDD0551  [10]
 LDCM0235  AC118 HCT 116 C795(0.86)  LDD0552  [10]
 LDCM0236  AC119 HCT 116 C795(1.04)  LDD0553  [10]
 LDCM0237  AC12 HCT 116 C239(0.86); C795(0.98)  LDD0554  [10]
 LDCM0238  AC120 HCT 116 C795(1.01)  LDD0555  [10]
 LDCM0239  AC121 HCT 116 C795(0.92)  LDD0556  [10]
 LDCM0240  AC122 HCT 116 C795(0.97)  LDD0557  [10]
 LDCM0241  AC123 HCT 116 C795(1.02)  LDD0558  [10]
 LDCM0242  AC124 HCT 116 C795(0.90)  LDD0559  [10]
 LDCM0243  AC125 HCT 116 C795(0.94)  LDD0560  [10]
 LDCM0244  AC126 HCT 116 C795(1.03)  LDD0561  [10]
 LDCM0245  AC127 HCT 116 C795(0.94)  LDD0562  [10]
 LDCM0246  AC128 HCT 116 C239(1.62); C795(1.02)  LDD0563  [10]
 LDCM0247  AC129 HCT 116 C239(1.00); C795(0.85)  LDD0564  [10]
 LDCM0249  AC130 HCT 116 C239(1.05); C795(1.01)  LDD0566  [10]
 LDCM0250  AC131 HCT 116 C239(1.04); C795(0.89)  LDD0567  [10]
 LDCM0251  AC132 HCT 116 C239(1.04); C795(1.07)  LDD0568  [10]
 LDCM0252  AC133 HCT 116 C239(1.34); C795(0.97)  LDD0569  [10]
 LDCM0253  AC134 HCT 116 C239(1.09); C795(1.01)  LDD0570  [10]
 LDCM0254  AC135 HCT 116 C239(1.21); C795(0.82)  LDD0571  [10]
 LDCM0255  AC136 HCT 116 C239(1.22); C795(1.03)  LDD0572  [10]
 LDCM0256  AC137 HCT 116 C239(1.12); C795(0.90)  LDD0573  [10]
 LDCM0257  AC138 HCT 116 C239(1.01); C795(1.26)  LDD0574  [10]
 LDCM0258  AC139 HCT 116 C239(1.06); C795(1.11)  LDD0575  [10]
 LDCM0259  AC14 HCT 116 C239(1.00); C795(0.92)  LDD0576  [10]
 LDCM0260  AC140 HCT 116 C239(1.91); C795(1.08)  LDD0577  [10]
 LDCM0261  AC141 HCT 116 C239(1.19); C795(1.20)  LDD0578  [10]
 LDCM0262  AC142 HCT 116 C239(1.71); C795(0.88)  LDD0579  [10]
 LDCM0263  AC143 HCT 116 C239(1.01); C795(1.09)  LDD0580  [10]
 LDCM0264  AC144 HCT 116 C795(0.96); C239(0.97)  LDD0581  [10]
 LDCM0265  AC145 HCT 116 C795(0.94); C239(1.00)  LDD0582  [10]
 LDCM0266  AC146 HCT 116 C239(1.10); C795(1.13)  LDD0583  [10]
 LDCM0267  AC147 HCT 116 C239(0.91); C795(1.10)  LDD0584  [10]
 LDCM0268  AC148 HCT 116 C795(1.57); C239(2.70)  LDD0585  [10]
 LDCM0269  AC149 HCT 116 C795(1.07); C239(1.58)  LDD0586  [10]
 LDCM0270  AC15 HCT 116 C239(0.93); C795(1.02)  LDD0587  [10]
 LDCM0271  AC150 HCT 116 C239(1.02); C795(1.05)  LDD0588  [10]
 LDCM0272  AC151 HCT 116 C239(0.91); C795(1.01)  LDD0589  [10]
 LDCM0273  AC152 HCT 116 C239(1.06); C795(1.22)  LDD0590  [10]
 LDCM0274  AC153 HCT 116 C795(1.39); C239(1.40)  LDD0591  [10]
 LDCM0621  AC154 HCT 116 C239(0.91); C795(1.03)  LDD2158  [10]
 LDCM0622  AC155 HCT 116 C239(1.06); C795(1.10)  LDD2159  [10]
 LDCM0623  AC156 HCT 116 C239(0.95); C795(1.21)  LDD2160  [10]
 LDCM0624  AC157 HCT 116 C239(0.97); C795(1.15)  LDD2161  [10]
 LDCM0276  AC17 HCT 116 C239(1.02); C795(1.09)  LDD0593  [10]
 LDCM0277  AC18 HCT 116 C239(0.99); C795(1.10)  LDD0594  [10]
 LDCM0278  AC19 HCT 116 C239(0.96); C795(1.02)  LDD0595  [10]
 LDCM0279  AC2 HCT 116 C795(0.87); C239(1.22)  LDD0596  [10]
 LDCM0280  AC20 HCT 116 C239(0.95); C795(1.18)  LDD0597  [10]
 LDCM0281  AC21 HCT 116 C239(0.93); C795(1.14)  LDD0598  [10]
 LDCM0282  AC22 HCT 116 C239(0.95); C795(1.20)  LDD0599  [10]
 LDCM0283  AC23 HCT 116 C239(0.87); C795(1.01)  LDD0600  [10]
 LDCM0284  AC24 HCT 116 C239(1.11); C795(1.14)  LDD0601  [10]
 LDCM0285  AC25 HCT 116 C239(1.11); C795(1.23)  LDD0602  [10]
 LDCM0286  AC26 HCT 116 C795(1.23); C239(1.32)  LDD0603  [10]
 LDCM0287  AC27 HCT 116 C795(1.12); C239(1.16)  LDD0604  [10]
 LDCM0288  AC28 HCT 116 C795(1.34); C239(1.58)  LDD0605  [10]
 LDCM0289  AC29 HCT 116 C795(1.19); C239(1.24)  LDD0606  [10]
 LDCM0290  AC3 HCT 116 C795(0.92); C239(1.06)  LDD0607  [10]
 LDCM0291  AC30 HCT 116 C239(1.11); C795(1.24)  LDD0608  [10]
 LDCM0292  AC31 HCT 116 C239(1.19); C795(1.23)  LDD0609  [10]
 LDCM0293  AC32 HCT 116 C795(1.12); C239(1.32)  LDD0610  [10]
 LDCM0294  AC33 HCT 116 C239(1.03); C795(1.56)  LDD0611  [10]
 LDCM0295  AC34 HCT 116 C239(0.97); C795(1.40)  LDD0612  [10]
 LDCM0296  AC35 HCT 116 C795(0.77); C239(0.99)  LDD0613  [10]
 LDCM0297  AC36 HCT 116 C239(0.91); C795(0.95)  LDD0614  [10]
 LDCM0298  AC37 HCT 116 C795(0.77); C239(0.96)  LDD0615  [10]
 LDCM0299  AC38 HCT 116 C795(0.96); C239(0.97)  LDD0616  [10]
 LDCM0300  AC39 HCT 116 C795(0.84); C239(0.93)  LDD0617  [10]
 LDCM0301  AC4 HCT 116 C239(0.86); C795(0.89)  LDD0618  [10]
 LDCM0302  AC40 HCT 116 C795(0.90); C239(0.91)  LDD0619  [10]
 LDCM0303  AC41 HCT 116 C239(0.89); C795(0.99)  LDD0620  [10]
 LDCM0304  AC42 HCT 116 C795(0.93); C239(0.95)  LDD0621  [10]
 LDCM0305  AC43 HCT 116 C239(0.84); C795(1.04)  LDD0622  [10]
 LDCM0306  AC44 HCT 116 C239(0.97); C795(1.06)  LDD0623  [10]
 LDCM0307  AC45 HCT 116 C239(0.96); C795(0.98)  LDD0624  [10]
 LDCM0308  AC46 HCT 116 C239(0.91); C795(1.09)  LDD0625  [10]
 LDCM0309  AC47 HCT 116 C795(1.10); C239(1.16)  LDD0626  [10]
 LDCM0310  AC48 HCT 116 C795(0.91); C239(1.28)  LDD0627  [10]
 LDCM0311  AC49 HCT 116 C239(1.13); C795(1.33)  LDD0628  [10]
 LDCM0312  AC5 HCT 116 C795(0.86); C239(1.03)  LDD0629  [10]
 LDCM0313  AC50 HCT 116 C239(1.06); C795(1.21)  LDD0630  [10]
 LDCM0314  AC51 HCT 116 C795(0.93); C239(1.05)  LDD0631  [10]
 LDCM0315  AC52 HCT 116 C239(0.89); C795(1.03)  LDD0632  [10]
 LDCM0316  AC53 HCT 116 C795(1.11); C239(1.21)  LDD0633  [10]
 LDCM0317  AC54 HCT 116 C239(1.16); C795(1.19)  LDD0634  [10]
 LDCM0318  AC55 HCT 116 C239(1.16); C795(1.19)  LDD0635  [10]
 LDCM0319  AC56 HCT 116 C239(1.16); C795(1.57)  LDD0636  [10]
 LDCM0320  AC57 HCT 116 C795(1.02)  LDD0637  [10]
 LDCM0321  AC58 HCT 116 C795(1.18)  LDD0638  [10]
 LDCM0322  AC59 HCT 116 C795(1.11)  LDD0639  [10]
 LDCM0323  AC6 HCT 116 C239(0.86); C795(1.05)  LDD0640  [10]
 LDCM0324  AC60 HCT 116 C795(1.27)  LDD0641  [10]
 LDCM0325  AC61 HCT 116 C795(1.12)  LDD0642  [10]
 LDCM0326  AC62 HCT 116 C795(1.10)  LDD0643  [10]
 LDCM0327  AC63 HCT 116 C795(1.09)  LDD0644  [10]
 LDCM0328  AC64 HCT 116 C795(1.18)  LDD0645  [10]
 LDCM0329  AC65 HCT 116 C795(1.05)  LDD0646  [10]
 LDCM0330  AC66 HCT 116 C795(1.04)  LDD0647  [10]
 LDCM0331  AC67 HCT 116 C795(1.22)  LDD0648  [10]
 LDCM0332  AC68 HCT 116 C795(0.89)  LDD0649  [10]
 LDCM0333  AC69 HCT 116 C795(0.97)  LDD0650  [10]
 LDCM0334  AC7 HCT 116 C795(0.90); C239(0.95)  LDD0651  [10]
 LDCM0335  AC70 HCT 116 C795(0.94)  LDD0652  [10]
 LDCM0336  AC71 HCT 116 C795(1.05)  LDD0653  [10]
 LDCM0337  AC72 HCT 116 C795(1.14)  LDD0654  [10]
 LDCM0338  AC73 HCT 116 C795(1.25)  LDD0655  [10]
 LDCM0339  AC74 HCT 116 C795(1.24)  LDD0656  [10]
 LDCM0340  AC75 HCT 116 C795(1.27)  LDD0657  [10]
 LDCM0341  AC76 HCT 116 C795(1.14)  LDD0658  [10]
 LDCM0342  AC77 HCT 116 C795(1.02)  LDD0659  [10]
 LDCM0343  AC78 HCT 116 C795(1.05)  LDD0660  [10]
 LDCM0344  AC79 HCT 116 C795(1.12)  LDD0661  [10]
 LDCM0345  AC8 HCT 116 C239(0.90); C795(0.97)  LDD0662  [10]
 LDCM0346  AC80 HCT 116 C795(1.21)  LDD0663  [10]
 LDCM0347  AC81 HCT 116 C795(1.26)  LDD0664  [10]
 LDCM0348  AC82 HCT 116 C795(1.38)  LDD0665  [10]
 LDCM0349  AC83 HCT 116 C239(1.14); C795(1.22)  LDD0666  [10]
 LDCM0350  AC84 HCT 116 C239(1.03); C795(1.10)  LDD0667  [10]
 LDCM0351  AC85 HCT 116 C795(1.02); C239(1.25)  LDD0668  [10]
 LDCM0352  AC86 HCT 116 C795(0.97); C239(1.07)  LDD0669  [10]
 LDCM0353  AC87 HCT 116 C795(0.84); C239(1.09)  LDD0670  [10]
 LDCM0354  AC88 HCT 116 C795(0.92); C239(1.32)  LDD0671  [10]
 LDCM0355  AC89 HCT 116 C795(1.03); C239(1.27)  LDD0672  [10]
 LDCM0357  AC90 HCT 116 C795(0.92); C239(1.24)  LDD0674  [10]
 LDCM0358  AC91 HCT 116 C239(0.93); C795(1.22)  LDD0675  [10]
 LDCM0359  AC92 HCT 116 C795(1.06); C239(1.28)  LDD0676  [10]
 LDCM0360  AC93 HCT 116 C795(1.01); C239(1.18)  LDD0677  [10]
 LDCM0361  AC94 HCT 116 C239(0.92); C795(1.09)  LDD0678  [10]
 LDCM0362  AC95 HCT 116 C795(0.95); C239(1.20)  LDD0679  [10]
 LDCM0363  AC96 HCT 116 C795(0.94); C239(1.18)  LDD0680  [10]
 LDCM0364  AC97 HCT 116 C795(1.01); C239(1.20)  LDD0681  [10]
 LDCM0365  AC98 HCT 116 C239(1.00); C795(1.09)  LDD0682  [10]
 LDCM0366  AC99 HCT 116 C239(0.83); C795(0.91)  LDD0683  [10]
 LDCM0248  AKOS034007472 HCT 116 C239(0.88); C795(0.98)  LDD0565  [10]
 LDCM0356  AKOS034007680 HCT 116 C239(0.90); C795(0.94)  LDD0673  [10]
 LDCM0275  AKOS034007705 HCT 116 C239(0.95); C795(1.02)  LDD0592  [10]
 LDCM0156  Aniline NCI-H1299 11.43  LDD0403  [5]
 LDCM0020  ARS-1620 HCC44 C795(0.88)  LDD0078  [10]
 LDCM0367  CL1 HCT 116 C795(0.87); C239(0.95)  LDD0684  [10]
 LDCM0368  CL10 HCT 116 C795(1.10); C239(1.15)  LDD0685  [10]
 LDCM0369  CL100 HCT 116 C795(0.78); C239(0.86)  LDD0686  [10]
 LDCM0370  CL101 HCT 116 C239(0.95); C795(1.03)  LDD0687  [10]
 LDCM0371  CL102 HCT 116 C795(0.88); C239(1.01)  LDD0688  [10]
 LDCM0372  CL103 HCT 116 C239(0.85); C795(1.05)  LDD0689  [10]
 LDCM0373  CL104 HCT 116 C239(0.82); C795(0.90)  LDD0690  [10]
 LDCM0374  CL105 HCT 116 C239(1.00); C795(1.05)  LDD0691  [10]
 LDCM0375  CL106 HCT 116 C239(0.92); C795(1.24)  LDD0692  [10]
 LDCM0376  CL107 HCT 116 C239(0.88); C795(1.21)  LDD0693  [10]
 LDCM0377  CL108 HCT 116 C239(0.99); C795(1.31)  LDD0694  [10]
 LDCM0378  CL109 HCT 116 C239(0.87); C795(1.11)  LDD0695  [10]
 LDCM0379  CL11 HCT 116 C239(1.08); C795(1.39)  LDD0696  [10]
 LDCM0380  CL110 HCT 116 C239(1.05); C795(1.13)  LDD0697  [10]
 LDCM0381  CL111 HCT 116 C239(0.97); C795(1.12)  LDD0698  [10]
 LDCM0382  CL112 HCT 116 C795(0.92); C239(1.07)  LDD0699  [10]
 LDCM0383  CL113 HCT 116 C239(1.07); C795(1.27)  LDD0700  [10]
 LDCM0384  CL114 HCT 116 C239(1.17); C795(1.35)  LDD0701  [10]
 LDCM0385  CL115 HCT 116 C795(1.12); C239(1.18)  LDD0702  [10]
 LDCM0386  CL116 HCT 116 C239(0.99); C795(1.44)  LDD0703  [10]
 LDCM0387  CL117 HCT 116 C239(0.98); C795(1.16)  LDD0704  [10]
 LDCM0388  CL118 HCT 116 C239(0.92); C795(1.00)  LDD0705  [10]
 LDCM0389  CL119 HCT 116 C795(0.90); C239(1.03)  LDD0706  [10]
 LDCM0390  CL12 HCT 116 C239(1.05); C795(1.43)  LDD0707  [10]
 LDCM0391  CL120 HCT 116 C795(0.89); C239(0.94)  LDD0708  [10]
 LDCM0392  CL121 HCT 116 C795(0.67); C239(1.22)  LDD0709  [10]
 LDCM0393  CL122 HCT 116 C795(1.02); C239(1.97)  LDD0710  [10]
 LDCM0394  CL123 HCT 116 C795(1.06); C239(1.75)  LDD0711  [10]
 LDCM0395  CL124 HCT 116 C795(1.17); C239(1.23)  LDD0712  [10]
 LDCM0396  CL125 HCT 116 C795(0.93)  LDD0713  [10]
 LDCM0397  CL126 HCT 116 C795(1.06)  LDD0714  [10]
 LDCM0398  CL127 HCT 116 C795(0.96)  LDD0715  [10]
 LDCM0399  CL128 HCT 116 C795(0.98)  LDD0716  [10]
 LDCM0400  CL13 HCT 116 C795(1.02); C239(1.06)  LDD0717  [10]
 LDCM0401  CL14 HCT 116 C795(0.85); C239(1.08)  LDD0718  [10]
 LDCM0402  CL15 HCT 116 C795(0.91); C239(0.99)  LDD0719  [10]
 LDCM0403  CL16 HCT 116 C795(1.10); C239(1.15)  LDD0720  [10]
 LDCM0404  CL17 HCT 116 C239(1.00); C795(1.13)  LDD0721  [10]
 LDCM0405  CL18 HCT 116 C239(1.09); C795(1.17)  LDD0722  [10]
 LDCM0406  CL19 HCT 116 C239(1.00); C795(1.11)  LDD0723  [10]
 LDCM0407  CL2 HCT 116 C795(0.95); C239(1.00)  LDD0724  [10]
 LDCM0408  CL20 HCT 116 C239(1.03); C795(1.19)  LDD0725  [10]
 LDCM0409  CL21 HCT 116 C795(1.00); C239(1.19)  LDD0726  [10]
 LDCM0410  CL22 HCT 116 C239(1.23); C795(1.48)  LDD0727  [10]
 LDCM0411  CL23 HCT 116 C239(0.99); C795(1.15)  LDD0728  [10]
 LDCM0412  CL24 HCT 116 C239(1.18); C795(1.38)  LDD0729  [10]
 LDCM0413  CL25 HCT 116 C239(1.31); C795(1.33)  LDD0730  [10]
 LDCM0414  CL26 HCT 116 C239(1.19); C795(1.07)  LDD0731  [10]
 LDCM0415  CL27 HCT 116 C239(1.13); C795(1.18)  LDD0732  [10]
 LDCM0416  CL28 HCT 116 C239(1.07); C795(1.23)  LDD0733  [10]
 LDCM0417  CL29 HCT 116 C239(1.13); C795(1.27)  LDD0734  [10]
 LDCM0418  CL3 HCT 116 C239(1.06); C795(0.95)  LDD0735  [10]
 LDCM0419  CL30 HCT 116 C239(1.10); C795(1.07)  LDD0736  [10]
 LDCM0420  CL31 HCT 116 C239(1.36); C795(1.15)  LDD0737  [10]
 LDCM0421  CL32 HCT 116 C239(1.02); C795(1.30)  LDD0738  [10]
 LDCM0422  CL33 HCT 116 C239(1.03); C795(0.98)  LDD0739  [10]
 LDCM0423  CL34 HCT 116 C239(1.12); C795(1.34)  LDD0740  [10]
 LDCM0424  CL35 HCT 116 C239(1.05); C795(1.30)  LDD0741  [10]
 LDCM0425  CL36 HCT 116 C239(0.88); C795(1.19)  LDD0742  [10]
 LDCM0426  CL37 HCT 116 C239(1.00); C795(1.34)  LDD0743  [10]
 LDCM0428  CL39 HCT 116 C239(1.04); C795(1.18)  LDD0745  [10]
 LDCM0429  CL4 HCT 116 C239(1.05); C795(0.86)  LDD0746  [10]
 LDCM0430  CL40 HCT 116 C239(0.81); C795(1.35)  LDD0747  [10]
 LDCM0431  CL41 HCT 116 C239(1.15); C795(1.24)  LDD0748  [10]
 LDCM0432  CL42 HCT 116 C239(0.83); C795(1.71)  LDD0749  [10]
 LDCM0433  CL43 HCT 116 C239(0.99); C795(1.51)  LDD0750  [10]
 LDCM0434  CL44 HCT 116 C239(1.07); C795(1.27)  LDD0751  [10]
 LDCM0435  CL45 HCT 116 C239(1.22); C795(1.29)  LDD0752  [10]
 LDCM0436  CL46 HCT 116 C239(1.28); C795(0.86)  LDD0753  [10]
 LDCM0437  CL47 HCT 116 C239(1.02); C795(0.93)  LDD0754  [10]
 LDCM0438  CL48 HCT 116 C239(1.08); C795(0.86)  LDD0755  [10]
 LDCM0439  CL49 HCT 116 C239(1.18); C795(1.07)  LDD0756  [10]
 LDCM0440  CL5 HCT 116 C239(0.88); C795(1.03)  LDD0757  [10]
 LDCM0441  CL50 HCT 116 C239(1.05); C795(0.79)  LDD0758  [10]
 LDCM0442  CL51 HCT 116 C239(1.23); C795(0.85)  LDD0759  [10]
 LDCM0443  CL52 HCT 116 C239(1.28); C795(0.86)  LDD0760  [10]
 LDCM0444  CL53 HCT 116 C239(0.95); C795(1.02)  LDD0761  [10]
 LDCM0445  CL54 HCT 116 C239(1.29); C795(0.83)  LDD0762  [10]
 LDCM0446  CL55 HCT 116 C239(1.07); C795(0.88)  LDD0763  [10]
 LDCM0447  CL56 HCT 116 C239(1.03); C795(0.97)  LDD0764  [10]
 LDCM0448  CL57 HCT 116 C239(0.98); C795(0.96)  LDD0765  [10]
 LDCM0449  CL58 HCT 116 C239(1.15); C795(0.92)  LDD0766  [10]
 LDCM0450  CL59 HCT 116 C239(1.31); C795(0.99)  LDD0767  [10]
 LDCM0451  CL6 HCT 116 C239(1.09); C795(1.09)  LDD0768  [10]
 LDCM0452  CL60 HCT 116 C239(1.22); C795(0.99)  LDD0769  [10]
 LDCM0453  CL61 HCT 116 C239(1.00); C795(1.23)  LDD0770  [10]
 LDCM0454  CL62 HCT 116 C239(0.92); C795(1.25)  LDD0771  [10]
 LDCM0455  CL63 HCT 116 C239(1.15); C795(1.34)  LDD0772  [10]
 LDCM0456  CL64 HCT 116 C239(0.92); C795(1.33)  LDD0773  [10]
 LDCM0457  CL65 HCT 116 C239(0.85); C795(1.17)  LDD0774  [10]
 LDCM0458  CL66 HCT 116 C239(0.93); C795(1.49)  LDD0775  [10]
 LDCM0459  CL67 HCT 116 C239(0.90); C795(1.56)  LDD0776  [10]
 LDCM0460  CL68 HCT 116 C239(0.93); C795(1.53)  LDD0777  [10]
 LDCM0461  CL69 HCT 116 C239(1.27); C795(1.27)  LDD0778  [10]
 LDCM0462  CL7 HCT 116 C239(1.13); C795(1.04)  LDD0779  [10]
 LDCM0463  CL70 HCT 116 C239(1.14); C795(1.45)  LDD0780  [10]
 LDCM0464  CL71 HCT 116 C239(0.93); C795(1.42)  LDD0781  [10]
 LDCM0465  CL72 HCT 116 C239(0.85); C795(1.27)  LDD0782  [10]
 LDCM0466  CL73 HCT 116 C239(1.08); C795(1.51)  LDD0783  [10]
 LDCM0467  CL74 HCT 116 C239(0.99); C795(1.39)  LDD0784  [10]
 LDCM0469  CL76 HCT 116 C795(0.89)  LDD0786  [10]
 LDCM0470  CL77 HCT 116 C795(1.01)  LDD0787  [10]
 LDCM0471  CL78 HCT 116 C795(0.97)  LDD0788  [10]
 LDCM0472  CL79 HCT 116 C795(0.95)  LDD0789  [10]
 LDCM0473  CL8 HCT 116 C239(1.26); C795(1.00)  LDD0790  [10]
 LDCM0474  CL80 HCT 116 C795(1.00)  LDD0791  [10]
 LDCM0475  CL81 HCT 116 C795(1.07)  LDD0792  [10]
 LDCM0476  CL82 HCT 116 C795(0.90)  LDD0793  [10]
 LDCM0477  CL83 HCT 116 C795(0.94)  LDD0794  [10]
 LDCM0478  CL84 HCT 116 C795(0.99)  LDD0795  [10]
 LDCM0479  CL85 HCT 116 C795(1.04)  LDD0796  [10]
 LDCM0480  CL86 HCT 116 C795(1.02)  LDD0797  [10]
 LDCM0481  CL87 HCT 116 C795(0.92)  LDD0798  [10]
 LDCM0482  CL88 HCT 116 C795(1.07)  LDD0799  [10]
 LDCM0483  CL89 HCT 116 C795(1.01)  LDD0800  [10]
 LDCM0484  CL9 HCT 116 C239(1.04); C795(1.00)  LDD0801  [10]
 LDCM0485  CL90 HCT 116 C795(1.05)  LDD0802  [10]
 LDCM0486  CL91 HCT 116 C239(0.94); C795(1.01)  LDD0803  [10]
 LDCM0487  CL92 HCT 116 C239(1.17); C795(0.81)  LDD0804  [10]
 LDCM0488  CL93 HCT 116 C239(1.02); C795(0.97)  LDD0805  [10]
 LDCM0489  CL94 HCT 116 C239(1.22); C795(0.95)  LDD0806  [10]
 LDCM0490  CL95 HCT 116 C239(1.08); C795(0.92)  LDD0807  [10]
 LDCM0491  CL96 HCT 116 C239(0.99); C795(0.86)  LDD0808  [10]
 LDCM0492  CL97 HCT 116 C239(1.10); C795(0.82)  LDD0809  [10]
 LDCM0493  CL98 HCT 116 C239(1.15); C795(0.92)  LDD0810  [10]
 LDCM0494  CL99 HCT 116 C239(0.95); C795(0.94)  LDD0811  [10]
 LDCM0495  E2913 HEK-293T C239(0.98); C722(1.15)  LDD1698  [17]
 LDCM0625  F8 Ramos C179(2.37); C735(1.00)  LDD2187  [18]
 LDCM0573  Fragment11 Ramos C179(0.38); C735(0.05)  LDD2190  [18]
 LDCM0576  Fragment14 Ramos C735(1.53)  LDD2193  [18]
 LDCM0580  Fragment21 Ramos C179(0.98)  LDD2195  [18]
 LDCM0582  Fragment23 Ramos C179(1.24); C735(0.49)  LDD2196  [18]
 LDCM0578  Fragment27 Ramos C179(0.90); C735(0.33)  LDD2197  [18]
 LDCM0586  Fragment28 Ramos C735(0.78)  LDD2198  [18]
 LDCM0588  Fragment30 Ramos C735(0.99)  LDD2199  [18]
 LDCM0589  Fragment31 Ramos C179(1.18); C735(1.06)  LDD2200  [18]
 LDCM0468  Fragment33 HCT 116 C239(1.00); C795(1.42)  LDD0785  [10]
 LDCM0596  Fragment38 Ramos C735(0.72)  LDD2203  [18]
 LDCM0566  Fragment4 Ramos C735(0.86)  LDD2184  [18]
 LDCM0427  Fragment51 HCT 116 C239(0.90); C795(1.38)  LDD0744  [10]
 LDCM0610  Fragment52 Ramos C735(0.85)  LDD2204  [18]
 LDCM0614  Fragment56 Ramos C179(1.34)  LDD2205  [18]
 LDCM0617  Fragment63-S Jurkat _(7.53)  LDD1490  [7]
 LDCM0569  Fragment7 Ramos C735(1.75)  LDD2186  [18]
 LDCM0022  KB02 HEK-293T C722(0.86)  LDD1492  [17]
 LDCM0023  KB03 HEK-293T C722(0.96)  LDD1497  [17]
 LDCM0024  KB05 COLO792 C239(2.32)  LDD3310  [19]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C239(1.49)  LDD2136  [6]
 LDCM0014  Panhematin hPBMC 3.37  LDD0064  [9]
 LDCM0131  RA190 MM1.R C239(2.13)  LDD0304  [20]
 LDCM0021  THZ1 HCT 116 C795(1.19)  LDD2173  [10]
 LDCM0154  YY4 T cell 3.87  LDD0400  [8]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Antigen peptide transporter 2 (TAP2) ABCB family Q03519
Protein disulfide-isomerase (P4HB) Protein disulfide isomerase family P07237
Protein disulfide-isomerase A3 (PDIA3) Protein disulfide isomerase family P30101
E3 ubiquitin-protein ligase RNF19B (RNF19B) RBR family Q6ZMZ0
Transporter and channel
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Hepatic sodium/bile acid cotransporter (SLC10A1) Bile acid:sodium symporter (BASS) family Q14973
Sodium-dependent organic anion transporter (SLC10A6) Bile acid:sodium symporter (BASS) family Q3KNW5
Calreticulin (CALR) Calreticulin family P27797
Syncytin-2 (ERVFRD-1) Gamma type-C retroviral envelope protein family P60508
Aquaporin-6 (AQP6) MIP/aquaporin (TC 1.A.8) family Q13520
THO complex subunit 5 homolog (THOC5) THOC5 family Q13769
Transmembrane protein 14B (TMEM14B) TMEM14 family Q9NUH8
GPCR
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Probable G-protein coupled receptor 152 (GPR152) G-protein coupled receptor 1 family Q8TDT2
Immunoglobulin
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Tapasin (TAPBP) . O15533
Other
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Endoplasmic reticulum-Golgi intermediate compartment protein 3 (ERGIC3) ERGIC family Q9Y282
Late cornified envelope protein 2C (LCE2C) LCE family Q5TA81
Gem-associated protein 4 (GEMIN4) . P57678
Serine-rich single-pass membrane protein 1 (SSMEM1) . Q8WWF3

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Lapatinib Small molecular drug DB01259

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.
2 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
3 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
4 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
5 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
6 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
7 Proteome-wide covalent ligand discovery in native biological systems. Nature. 2016 Jun 23;534(7608):570-4. doi: 10.1038/nature18002. Epub 2016 Jun 15.
8 A Chemical Proteomic Probe for the Mitochondrial Pyruvate Carrier Complex. Angew Chem Int Ed Engl. 2020 Mar 2;59(10):3896-3899. doi: 10.1002/anie.201914391. Epub 2020 Feb 11.
9 A Chemical Proteomic Map of Heme-Protein Interactions. J Am Chem Soc. 2022 Aug 24;144(33):15013-15019. doi: 10.1021/jacs.2c06104. Epub 2022 Aug 12.
Mass spectrometry data entry: PXD034651
10 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
11 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
12 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
13 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
14 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
15 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.
16 Mapping Protein Targets of Bioactive Small Molecules Using Lipid-Based Chemical Proteomics. ACS Chem Biol. 2017 Oct 20;12(10):2671-2681. doi: 10.1021/acschembio.7b00581. Epub 2017 Sep 20.
Mass spectrometry data entry: PXD007570
17 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
18 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578
19 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
20 Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190. Cell Chem Biol. 2020 Nov 19;27(11):1371-1382.e6. doi: 10.1016/j.chembiol.2020.08.007. Epub 2020 Aug 27.