Details of the Target

General Information of Target

Target ID LDTP06462
Target Name Neutral amino acid transporter B(0) (SLC1A5)
Gene Name SLC1A5
Gene ID 6510
Synonyms
ASCT2; M7V1; RDR; RDRC; Neutral amino acid transporter B(0; ATB(0); Baboon M7 virus receptor; RD114/simian type D retrovirus receptor; Sodium-dependent neutral amino acid transporter type 2; Solute carrier family 1 member 5
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MVADPPRDSKGLAAAEPTANGGLALASIEDQGAAAGGYCGSRDQVRRCLRANLLVLLTVV
AVVAGVALGLGVSGAGGALALGPERLSAFVFPGELLLRLLRMIILPLVVCSLIGGAASLD
PGALGRLGAWALLFFLVTTLLASALGVGLALALQPGAASAAINASVGAAGSAENAPSKEV
LDSFLDLARNIFPSNLVSAAFRSYSTTYEERNITGTRVKVPVGQEVEGMNILGLVVFAIV
FGVALRKLGPEGELLIRFFNSFNEATMVLVSWIMWYAPVGIMFLVAGKIVEMEDVGLLFA
RLGKYILCCLLGHAIHGLLVLPLIYFLFTRKNPYRFLWGIVTPLATAFGTSSSSATLPLM
MKCVEENNGVAKHISRFILPIGATVNMDGAALFQCVAAVFIAQLSQQSLDFVKIITILVT
ATASSVGAAGIPAGGVLTLAIILEAVNLPVDHISLILAVDWLVDRSCTVLNVEGDALGAG
LLQNYVDRTESRSTEPELIQVKSELPLDPLPVPTEEGNPLLKHYRGPAGDATVASEKESV
M
Target Type
Literature-reported
Target Bioclass
Transporter and channel
Family
Dicarboxylate/amino acid:cation symporter (DAACS) (TC 2.A.23) family, SLC1A5 subfamily
Subcellular location
Cell membrane
Function
Sodium-coupled antiporter of neutral amino acids. In a tri-substrate transport cycle, exchanges neutral amino acids between the extracellular and intracellular compartments, coupled to the inward cotransport of at least one sodium ion . The preferred substrate is the essential amino acid L-glutamine, a precursor for biosynthesis of proteins, nucleotides and amine sugars as well as an alternative fuel for mitochondrial oxidative phosphorylation. Exchanges L-glutamine with other neutral amino acids such as L-serine, L-threonine and L-asparagine in a bidirectional way. Provides L-glutamine to proliferating stem and activated cells driving the metabolic switch toward cell differentiation. The transport cycle is usually pH-independent, with the exception of L-glutamate. Transports extracellular L-glutamate coupled to the cotransport of one proton and one sodium ion in exchange for intracellular L-glutamine counter-ion. May provide for L-glutamate uptake in glial cells regulating glutamine/glutamate cycle in the nervous system. Can transport D-amino acids. Mediates D-serine release from the retinal glia potentially affecting NMDA receptor function in retinal neurons. Displays sodium- and amino acid-dependent but uncoupled channel-like anion conductance with a preference SCN(-) >> NO3(-) > I(-) > Cl(-). Through binding of the fusogenic protein syncytin-1/ERVW-1 may mediate trophoblasts syncytialization, the spontaneous fusion of their plasma membranes, an essential process in placental development.; (Microbial infection) Acts as a cell surface receptor for Feline endogenous virus RD114.; (Microbial infection) Acts as a cell surface receptor for Baboon M7 endogenous virus.; (Microbial infection) Acts as a cell surface receptor for type D simian retroviruses.
TTD ID
T59493
Uniprot ID
Q15758
DrugMap ID
TTF7WRM
Ensemble ID
ENST00000412532.6
HGNC ID
HGNC:10943
ChEMBL ID
CHEMBL3562162

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HEC1 SNV: p.V268A .
MELHO SNV: p.V66A; p.G69Ter DBIA    Probe Info 
MFE319 SNV: p.V320A DBIA    Probe Info 
MOLT4 SNV: p.L105F; p.A152V; p.F377S IA-alkyne    Probe Info 
PANC0403 Substitution: p.E253M .
RH30 SNV: p.A429T .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 35 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
HDSF-alk
 Probe Info  		1.54  LDD0197  [1]
11RK72
 Probe Info  		2.01  LDD0327  [2]
FBPP2
 Probe Info  		4.18  LDD0318  [3]
CHEMBL5175495
 Probe Info  		10.93  LDD0196  [4]
CY4
 Probe Info  		100.00  LDD0244  [5]
FBP2
 Probe Info  		2.22  LDD0317  [3]
YN-4
 Probe Info  		100.00  LDD0445  [6]
AZ-9
 Probe Info  		E536(1.25)  LDD2208  [7]
ONAyne
 Probe Info  		N.A.  LDD0273  [8]
JZ128-DTB
 Probe Info  		C39(0.00); C363(0.00)  LDD0462  [9]
THZ1-DTB
 Probe Info  		C39(0.99)  LDD0460  [9]
AHL-Pu-1
 Probe Info  		C39(4.00); C363(2.47)  LDD0168  [10]
Alkyne-RA190
 Probe Info  		2.06  LDD0299  [11]
EA-probe
 Probe Info  		C39(1.34); C467(1.02); C467(1.23)  LDD2210  [12]
DBIA
 Probe Info  		C39(1.19)  LDD0078  [13]
ATP probe
 Probe Info  		K522(0.00); K372(0.00)  LDD0199  [14]
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [15]
IA-alkyne
 Probe Info  		C363(0.00); C467(0.00)  LDD0036  [15]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [15]
JW-RF-010
 Probe Info  		N.A.  LDD0026  [16]
TFBX
 Probe Info  		N.A.  LDD0027  [16]
WYneN
 Probe Info  		N.A.  LDD0021  [17]
WYneO
 Probe Info  		N.A.  LDD0022  [17]
1d-yne
 Probe Info  		N.A.  LDD0356  [18]
ENE
 Probe Info  		N.A.  LDD0006  [17]
IPM
 Probe Info  		N.A.  LDD0005  [17]
NHS
 Probe Info  		K247(0.00); K522(0.00); K537(0.00)  LDD0010  [17]
NPM
 Probe Info  		N.A.  LDD0016  [17]
SF
 Probe Info  		N.A.  LDD0028  [19]
STPyne
 Probe Info  		N.A.  LDD0009  [17]
VSF
 Probe Info  		C467(0.00); C39(0.00); C363(0.00)  LDD0007  [17]
1c-yne
 Probe Info  		K522(0.00); K502(0.00)  LDD0228  [18]
Acrolein
 Probe Info  		C363(0.00); C467(0.00)  LDD0217  [20]
AOyne
 Probe Info  		8.60  LDD0443  [21]
NAIA_5
 Probe Info  		N.A.  LDD2223  [22]
PAL-AfBPP Probe
Click To Hide/Show 12 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FFF probe11
 Probe Info  		16.70  LDD0471  [23]
FFF probe12
 Probe Info  		20.00  LDD0473  [23]
FFF probe13
 Probe Info  		9.57  LDD0475  [23]
FFF probe14
 Probe Info  		17.66  LDD0477  [23]
FFF probe2
 Probe Info  		11.15  LDD0463  [23]
FFF probe3
 Probe Info  		16.76  LDD0464  [23]
JN0003
 Probe Info  		11.64  LDD0469  [23]
STS-1
 Probe Info  		N.A.  LDD0136  [24]
STS-2
 Probe Info  		N.A.  LDD0138  [24]
VE-P
 Probe Info  		N.A.  LDD0396  [25]
DA-2
 Probe Info  		N.A.  LDD0073  [26]
KIRA6 AfBP
 Probe Info  		N.A.  LDD0378  [27]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0025  4SU-RNA HEK-293T C39(4.00); C363(2.47)  LDD0168  [10]
 LDCM0214  AC1 HCT 116 C39(0.82)  LDD0531  [13]
 LDCM0215  AC10 HCT 116 C363(0.75); C39(0.71)  LDD0532  [13]
 LDCM0216  AC100 HCT 116 C363(0.71); C39(0.84)  LDD0533  [13]
 LDCM0217  AC101 HCT 116 C363(0.88); C39(0.83)  LDD0534  [13]
 LDCM0218  AC102 HCT 116 C363(0.66); C39(0.84)  LDD0535  [13]
 LDCM0219  AC103 HCT 116 C363(0.56); C39(0.96)  LDD0536  [13]
 LDCM0220  AC104 HCT 116 C363(0.68); C39(1.19)  LDD0537  [13]
 LDCM0221  AC105 HCT 116 C363(0.73); C39(0.92)  LDD0538  [13]
 LDCM0222  AC106 HCT 116 C363(0.70); C39(0.90)  LDD0539  [13]
 LDCM0223  AC107 HCT 116 C363(0.63); C39(1.00)  LDD0540  [13]
 LDCM0224  AC108 HCT 116 C363(0.61); C39(0.82)  LDD0541  [13]
 LDCM0225  AC109 HCT 116 C363(0.72); C39(0.79)  LDD0542  [13]
 LDCM0226  AC11 HCT 116 C363(0.83); C39(0.72)  LDD0543  [13]
 LDCM0227  AC110 HCT 116 C363(0.66); C39(0.82)  LDD0544  [13]
 LDCM0228  AC111 HCT 116 C363(0.85); C39(0.97)  LDD0545  [13]
 LDCM0229  AC112 HCT 116 C363(0.52); C39(0.88)  LDD0546  [13]
 LDCM0230  AC113 HCT 116 C363(0.78); C39(0.94)  LDD0547  [13]
 LDCM0231  AC114 HCT 116 C363(0.87); C39(1.04)  LDD0548  [13]
 LDCM0232  AC115 HCT 116 C363(0.90); C39(1.10)  LDD0549  [13]
 LDCM0233  AC116 HCT 116 C363(0.73); C39(0.93)  LDD0550  [13]
 LDCM0234  AC117 HCT 116 C363(0.77); C39(0.87)  LDD0551  [13]
 LDCM0235  AC118 HCT 116 C363(0.82); C39(0.79)  LDD0552  [13]
 LDCM0236  AC119 HCT 116 C363(0.90); C39(0.82)  LDD0553  [13]
 LDCM0237  AC12 HCT 116 C363(0.84); C39(0.75)  LDD0554  [13]
 LDCM0238  AC120 HCT 116 C363(0.78); C39(0.95)  LDD0555  [13]
 LDCM0239  AC121 HCT 116 C363(1.31); C39(0.81)  LDD0556  [13]
 LDCM0240  AC122 HCT 116 C363(0.80); C39(0.73)  LDD0557  [13]
 LDCM0241  AC123 HCT 116 C363(0.89); C39(0.94)  LDD0558  [13]
 LDCM0242  AC124 HCT 116 C363(0.83); C39(0.88)  LDD0559  [13]
 LDCM0243  AC125 HCT 116 C363(0.86); C39(0.81)  LDD0560  [13]
 LDCM0244  AC126 HCT 116 C363(0.68); C39(1.28)  LDD0561  [13]
 LDCM0245  AC127 HCT 116 C363(0.79); C39(1.01)  LDD0562  [13]
 LDCM0246  AC128 HEK-293T C39(0.80); C363(1.31)  LDD0844  [13]
 LDCM0247  AC129 HEK-293T C39(0.89); C363(1.05)  LDD0845  [13]
 LDCM0249  AC130 HEK-293T C39(1.15); C363(0.74)  LDD0847  [13]
 LDCM0250  AC131 HEK-293T C39(0.89); C363(1.23)  LDD0848  [13]
 LDCM0251  AC132 HEK-293T C39(0.86); C363(1.04)  LDD0849  [13]
 LDCM0252  AC133 HEK-293T C39(0.85); C363(0.82)  LDD0850  [13]
 LDCM0253  AC134 HEK-293T C39(0.93); C363(0.82)  LDD0851  [13]
 LDCM0254  AC135 HEK-293T C39(1.28); C363(0.77)  LDD0852  [13]
 LDCM0255  AC136 HEK-293T C39(0.90); C363(0.70)  LDD0853  [13]
 LDCM0256  AC137 HEK-293T C39(1.28); C363(0.78)  LDD0854  [13]
 LDCM0257  AC138 HEK-293T C39(1.21); C363(0.89)  LDD0855  [13]
 LDCM0258  AC139 HEK-293T C39(1.12); C363(0.78)  LDD0856  [13]
 LDCM0259  AC14 HCT 116 C363(0.79); C39(0.64)  LDD0576  [13]
 LDCM0260  AC140 HEK-293T C39(0.77); C363(1.13)  LDD0858  [13]
 LDCM0261  AC141 HEK-293T C39(1.03); C363(0.95)  LDD0859  [13]
 LDCM0262  AC142 HEK-293T C39(0.94); C363(0.85)  LDD0860  [13]
 LDCM0263  AC143 HCT 116 C39(0.84); C363(0.97)  LDD0580  [13]
 LDCM0264  AC144 HCT 116 C363(0.80); C39(1.36)  LDD0581  [13]
 LDCM0265  AC145 HCT 116 C363(0.88); C39(1.24)  LDD0582  [13]
 LDCM0266  AC146 HCT 116 C363(0.66); C39(0.88)  LDD0583  [13]
 LDCM0267  AC147 HCT 116 C363(1.05); C39(1.54)  LDD0584  [13]
 LDCM0268  AC148 HCT 116 C363(0.63); C39(1.78)  LDD0585  [13]
 LDCM0269  AC149 HCT 116 C363(0.64); C39(1.17)  LDD0586  [13]
 LDCM0270  AC15 HCT 116 C39(0.68); C363(0.85)  LDD0587  [13]
 LDCM0271  AC150 HCT 116 C363(0.85); C39(1.11)  LDD0588  [13]
 LDCM0272  AC151 HCT 116 C363(0.79); C39(1.20)  LDD0589  [13]
 LDCM0273  AC152 HCT 116 C363(0.72); C39(1.41)  LDD0590  [13]
 LDCM0274  AC153 HCT 116 C363(0.68); C39(2.23)  LDD0591  [13]
 LDCM0621  AC154 HCT 116 C363(0.83); C39(0.99)  LDD2158  [13]
 LDCM0622  AC155 HCT 116 C363(0.68); C39(2.22)  LDD2159  [13]
 LDCM0623  AC156 HCT 116 C363(0.74); C39(1.64)  LDD2160  [13]
 LDCM0624  AC157 HCT 116 C363(0.78); C39(3.07)  LDD2161  [13]
 LDCM0276  AC17 HCT 116 C363(0.91); C39(1.52)  LDD0593  [13]
 LDCM0277  AC18 HCT 116 C363(0.54); C39(0.92)  LDD0594  [13]
 LDCM0278  AC19 HCT 116 C363(1.07); C39(1.57)  LDD0595  [13]
 LDCM0279  AC2 HCT 116 C39(0.85)  LDD0596  [13]
 LDCM0280  AC20 HCT 116 C363(0.97); C39(1.40)  LDD0597  [13]
 LDCM0281  AC21 HCT 116 C363(0.94); C39(1.57)  LDD0598  [13]
 LDCM0282  AC22 HCT 116 C363(0.65); C39(1.13)  LDD0599  [13]
 LDCM0283  AC23 HCT 116 C363(1.00); C39(1.35)  LDD0600  [13]
 LDCM0284  AC24 HCT 116 C39(1.47); C363(1.78)  LDD0601  [13]
 LDCM0285  AC25 HCT 116 C363(0.51); C39(1.07)  LDD0602  [13]
 LDCM0286  AC26 HCT 116 C363(0.53); C39(1.37)  LDD0603  [13]
 LDCM0287  AC27 HCT 116 C363(0.41); C39(1.34)  LDD0604  [13]
 LDCM0288  AC28 HCT 116 C363(0.71); C39(1.61)  LDD0605  [13]
 LDCM0289  AC29 HCT 116 C363(0.48); C39(1.70)  LDD0606  [13]
 LDCM0290  AC3 HCT 116 C39(0.80)  LDD0607  [13]
 LDCM0291  AC30 HCT 116 C363(0.52); C39(1.44)  LDD0608  [13]
 LDCM0292  AC31 HCT 116 C363(0.58); C39(1.35)  LDD0609  [13]
 LDCM0293  AC32 HCT 116 C363(0.58); C39(1.33)  LDD0610  [13]
 LDCM0294  AC33 HCT 116 C363(0.40); C39(1.42)  LDD0611  [13]
 LDCM0295  AC34 HCT 116 C363(0.61); C39(2.09)  LDD0612  [13]
 LDCM0296  AC35 HCT 116 C39(0.84)  LDD0613  [13]
 LDCM0297  AC36 HCT 116 C39(0.75)  LDD0614  [13]
 LDCM0298  AC37 HCT 116 C39(0.85)  LDD0615  [13]
 LDCM0299  AC38 HCT 116 C39(0.82)  LDD0616  [13]
 LDCM0300  AC39 HCT 116 C39(0.72)  LDD0617  [13]
 LDCM0301  AC4 HCT 116 C39(0.80)  LDD0618  [13]
 LDCM0302  AC40 HCT 116 C39(0.82)  LDD0619  [13]
 LDCM0303  AC41 HCT 116 C39(0.75)  LDD0620  [13]
 LDCM0304  AC42 HCT 116 C39(0.78)  LDD0621  [13]
 LDCM0305  AC43 HCT 116 C39(0.78)  LDD0622  [13]
 LDCM0306  AC44 HCT 116 C39(0.70)  LDD0623  [13]
 LDCM0307  AC45 HCT 116 C39(0.87)  LDD0624  [13]
 LDCM0308  AC46 HCT 116 C39(1.10)  LDD0625  [13]
 LDCM0309  AC47 HCT 116 C39(0.90)  LDD0626  [13]
 LDCM0310  AC48 HCT 116 C39(0.75)  LDD0627  [13]
 LDCM0311  AC49 HCT 116 C39(1.28)  LDD0628  [13]
 LDCM0312  AC5 HCT 116 C39(0.62)  LDD0629  [13]
 LDCM0313  AC50 HCT 116 C39(1.59)  LDD0630  [13]
 LDCM0314  AC51 HCT 116 C39(0.87)  LDD0631  [13]
 LDCM0315  AC52 HCT 116 C39(0.97)  LDD0632  [13]
 LDCM0316  AC53 HCT 116 C39(1.18)  LDD0633  [13]
 LDCM0317  AC54 HCT 116 C39(1.04)  LDD0634  [13]
 LDCM0318  AC55 HCT 116 C39(1.20)  LDD0635  [13]
 LDCM0319  AC56 HCT 116 C39(1.22)  LDD0636  [13]
 LDCM0320  AC57 HCT 116 C39(0.78)  LDD0637  [13]
 LDCM0321  AC58 HCT 116 C39(0.85)  LDD0638  [13]
 LDCM0322  AC59 HCT 116 C39(0.75)  LDD0639  [13]
 LDCM0323  AC6 HCT 116 C39(0.78); C363(0.89)  LDD0640  [13]
 LDCM0324  AC60 HCT 116 C39(0.60)  LDD0641  [13]
 LDCM0325  AC61 HCT 116 C39(0.67)  LDD0642  [13]
 LDCM0326  AC62 HCT 116 C39(0.78)  LDD0643  [13]
 LDCM0327  AC63 HCT 116 C39(0.79)  LDD0644  [13]
 LDCM0328  AC64 HCT 116 C39(0.71)  LDD0645  [13]
 LDCM0329  AC65 HCT 116 C39(0.65)  LDD0646  [13]
 LDCM0330  AC66 HCT 116 C39(0.82)  LDD0647  [13]
 LDCM0331  AC67 HCT 116 C39(0.67)  LDD0648  [13]
 LDCM0332  AC68 HCT 116 C39(0.70); C363(1.01)  LDD0649  [13]
 LDCM0333  AC69 HCT 116 C363(0.70); C39(1.10)  LDD0650  [13]
 LDCM0334  AC7 HCT 116 C39(0.65); C363(0.88)  LDD0651  [13]
 LDCM0335  AC70 HCT 116 C363(0.68); C39(0.88)  LDD0652  [13]
 LDCM0336  AC71 HCT 116 C39(0.63); C363(1.00)  LDD0653  [13]
 LDCM0337  AC72 HCT 116 C363(0.97); C39(1.01)  LDD0654  [13]
 LDCM0338  AC73 HCT 116 C363(0.79); C39(1.27)  LDD0655  [13]
 LDCM0339  AC74 HCT 116 C363(0.61); C39(1.06)  LDD0656  [13]
 LDCM0340  AC75 HCT 116 C363(0.71); C39(1.56)  LDD0657  [13]
 LDCM0341  AC76 HCT 116 C39(0.96); C363(1.04)  LDD0658  [13]
 LDCM0342  AC77 HCT 116 C363(0.89); C39(0.98)  LDD0659  [13]
 LDCM0343  AC78 HCT 116 C363(0.67); C39(0.92)  LDD0660  [13]
 LDCM0344  AC79 HCT 116 C39(0.93); C363(1.22)  LDD0661  [13]
 LDCM0345  AC8 HCT 116 C39(0.65); C363(0.82)  LDD0662  [13]
 LDCM0346  AC80 HCT 116 C39(0.98); C363(1.01)  LDD0663  [13]
 LDCM0347  AC81 HCT 116 C39(0.86); C363(1.07)  LDD0664  [13]
 LDCM0348  AC82 HCT 116 C363(0.38); C39(0.76)  LDD0665  [13]
 LDCM0349  AC83 HCT 116 C363(0.71); C39(1.10)  LDD0666  [13]
 LDCM0350  AC84 HCT 116 C363(0.70); C39(1.25)  LDD0667  [13]
 LDCM0351  AC85 HCT 116 C363(0.62); C39(0.86)  LDD0668  [13]
 LDCM0352  AC86 HCT 116 C363(1.03); C39(1.19)  LDD0669  [13]
 LDCM0353  AC87 HCT 116 C363(0.93); C39(1.09)  LDD0670  [13]
 LDCM0354  AC88 HCT 116 C363(0.77); C39(1.17)  LDD0671  [13]
 LDCM0355  AC89 HCT 116 C363(0.83); C39(1.74)  LDD0672  [13]
 LDCM0357  AC90 HCT 116 C39(0.98); C363(1.29)  LDD0674  [13]
 LDCM0358  AC91 HCT 116 C363(0.76); C39(1.35)  LDD0675  [13]
 LDCM0359  AC92 HCT 116 C363(0.79); C39(1.52)  LDD0676  [13]
 LDCM0360  AC93 HCT 116 C363(0.78); C39(1.26)  LDD0677  [13]
 LDCM0361  AC94 HCT 116 C363(0.75); C39(1.37)  LDD0678  [13]
 LDCM0362  AC95 HCT 116 C363(0.93); C39(1.37)  LDD0679  [13]
 LDCM0363  AC96 HCT 116 C363(0.71); C39(1.51)  LDD0680  [13]
 LDCM0364  AC97 HCT 116 C363(0.79); C39(1.31)  LDD0681  [13]
 LDCM0365  AC98 HCT 116 C363(0.28); C39(0.84)  LDD0682  [13]
 LDCM0366  AC99 HCT 116 C363(0.73); C39(0.88)  LDD0683  [13]
 LDCM0248  AKOS034007472 HCT 116 C363(1.33); C39(0.64)  LDD0565  [13]
 LDCM0356  AKOS034007680 HCT 116 C39(0.69); C363(1.09)  LDD0673  [13]
 LDCM0275  AKOS034007705 HCT 116 C39(0.83); C363(0.96)  LDD0592  [13]
 LDCM0020  ARS-1620 HCC44 C39(1.19)  LDD0078  [13]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [20]
 LDCM0367  CL1 HCT 116 C363(0.85); C39(1.08)  LDD0684  [13]
 LDCM0368  CL10 HCT 116 C363(0.88); C39(1.27)  LDD0685  [13]
 LDCM0369  CL100 HCT 116 C39(0.97)  LDD0686  [13]
 LDCM0370  CL101 HCT 116 C39(0.66); C363(0.90)  LDD0687  [13]
 LDCM0371  CL102 HCT 116 C39(0.62); C363(1.13)  LDD0688  [13]
 LDCM0372  CL103 HCT 116 C39(0.97); C363(1.21)  LDD0689  [13]
 LDCM0373  CL104 HCT 116 C363(0.88); C39(1.02)  LDD0690  [13]
 LDCM0374  CL105 HCT 116 C363(0.81); C39(1.01)  LDD0691  [13]
 LDCM0375  CL106 HCT 116 C363(0.49); C39(1.18)  LDD0692  [13]
 LDCM0376  CL107 HCT 116 C363(0.96); C39(1.03)  LDD0693  [13]
 LDCM0377  CL108 HCT 116 C363(0.86); C39(1.35)  LDD0694  [13]
 LDCM0378  CL109 HCT 116 C363(0.79); C39(1.46)  LDD0695  [13]
 LDCM0379  CL11 HCT 116 C363(0.84); C39(1.44)  LDD0696  [13]
 LDCM0380  CL110 HCT 116 C363(0.78); C39(1.49)  LDD0697  [13]
 LDCM0381  CL111 HCT 116 C363(0.75); C39(1.42)  LDD0698  [13]
 LDCM0382  CL112 HCT 116 C363(0.77); C39(0.88)  LDD0699  [13]
 LDCM0383  CL113 HCT 116 C363(0.59); C39(1.71)  LDD0700  [13]
 LDCM0384  CL114 HCT 116 C363(0.80); C39(1.41)  LDD0701  [13]
 LDCM0385  CL115 HCT 116 C363(0.58); C39(1.37)  LDD0702  [13]
 LDCM0386  CL116 HCT 116 C363(0.67); C39(1.09)  LDD0703  [13]
 LDCM0387  CL117 HCT 116 C39(0.90)  LDD0704  [13]
 LDCM0388  CL118 HCT 116 C39(0.77)  LDD0705  [13]
 LDCM0389  CL119 HCT 116 C39(0.95)  LDD0706  [13]
 LDCM0390  CL12 HCT 116 C363(0.77); C39(1.37)  LDD0707  [13]
 LDCM0391  CL120 HCT 116 C39(0.75)  LDD0708  [13]
 LDCM0392  CL121 HCT 116 C39(0.95)  LDD0709  [13]
 LDCM0393  CL122 HCT 116 C39(0.92)  LDD0710  [13]
 LDCM0394  CL123 HCT 116 C39(1.80)  LDD0711  [13]
 LDCM0395  CL124 HCT 116 C39(1.12)  LDD0712  [13]
 LDCM0396  CL125 HCT 116 C39(0.58)  LDD0713  [13]
 LDCM0397  CL126 HCT 116 C39(0.70)  LDD0714  [13]
 LDCM0398  CL127 HCT 116 C39(0.83)  LDD0715  [13]
 LDCM0399  CL128 HCT 116 C39(0.73)  LDD0716  [13]
 LDCM0400  CL13 HCT 116 C363(0.90); C39(1.20)  LDD0717  [13]
 LDCM0401  CL14 HCT 116 C363(0.98); C39(1.53)  LDD0718  [13]
 LDCM0402  CL15 HCT 116 C363(0.94); C39(0.95)  LDD0719  [13]
 LDCM0403  CL16 HCT 116 C39(1.07)  LDD0720  [13]
 LDCM0404  CL17 HCT 116 C39(1.07)  LDD0721  [13]
 LDCM0405  CL18 HCT 116 C39(1.42)  LDD0722  [13]
 LDCM0406  CL19 HCT 116 C39(1.01)  LDD0723  [13]
 LDCM0407  CL2 HCT 116 C39(0.85); C363(0.88)  LDD0724  [13]
 LDCM0408  CL20 HCT 116 C39(1.31)  LDD0725  [13]
 LDCM0409  CL21 HCT 116 C39(1.39)  LDD0726  [13]
 LDCM0410  CL22 HCT 116 C39(1.55)  LDD0727  [13]
 LDCM0411  CL23 HCT 116 C39(1.51)  LDD0728  [13]
 LDCM0412  CL24 HCT 116 C39(1.58)  LDD0729  [13]
 LDCM0413  CL25 HCT 116 C39(1.46)  LDD0730  [13]
 LDCM0414  CL26 HCT 116 C39(1.25)  LDD0731  [13]
 LDCM0415  CL27 HCT 116 C39(0.90)  LDD0732  [13]
 LDCM0416  CL28 HCT 116 C39(1.39)  LDD0733  [13]
 LDCM0417  CL29 HCT 116 C39(1.24)  LDD0734  [13]
 LDCM0418  CL3 HCT 116 C363(0.93); C39(1.00)  LDD0735  [13]
 LDCM0419  CL30 HCT 116 C39(1.09)  LDD0736  [13]
 LDCM0420  CL31 HCT 116 C39(1.13)  LDD0737  [13]
 LDCM0421  CL32 HCT 116 C39(1.51)  LDD0738  [13]
 LDCM0422  CL33 HCT 116 C39(3.26)  LDD0739  [13]
 LDCM0423  CL34 HCT 116 C39(1.53)  LDD0740  [13]
 LDCM0424  CL35 HCT 116 C39(1.81)  LDD0741  [13]
 LDCM0425  CL36 HCT 116 C39(1.79)  LDD0742  [13]
 LDCM0426  CL37 HCT 116 C39(1.77)  LDD0743  [13]
 LDCM0428  CL39 HCT 116 C39(1.47)  LDD0745  [13]
 LDCM0429  CL4 HCT 116 C363(1.02); C39(2.57)  LDD0746  [13]
 LDCM0430  CL40 HCT 116 C39(1.49)  LDD0747  [13]
 LDCM0431  CL41 HCT 116 C39(1.54)  LDD0748  [13]
 LDCM0432  CL42 HCT 116 C39(1.54)  LDD0749  [13]
 LDCM0433  CL43 HCT 116 C39(1.89)  LDD0750  [13]
 LDCM0434  CL44 HCT 116 C39(1.53)  LDD0751  [13]
 LDCM0435  CL45 HCT 116 C39(1.57)  LDD0752  [13]
 LDCM0436  CL46 HCT 116 C39(1.21)  LDD0753  [13]
 LDCM0437  CL47 HCT 116 C39(1.25)  LDD0754  [13]
 LDCM0438  CL48 HCT 116 C39(1.16)  LDD0755  [13]
 LDCM0439  CL49 HCT 116 C39(1.72)  LDD0756  [13]
 LDCM0440  CL5 HCT 116 C363(1.00); C39(0.93)  LDD0757  [13]
 LDCM0441  CL50 HCT 116 C39(1.01)  LDD0758  [13]
 LDCM0442  CL51 HCT 116 C39(1.41)  LDD0759  [13]
 LDCM0443  CL52 HCT 116 C39(1.18)  LDD0760  [13]
 LDCM0444  CL53 HCT 116 C39(3.03)  LDD0761  [13]
 LDCM0445  CL54 HCT 116 C39(2.03)  LDD0762  [13]
 LDCM0446  CL55 HCT 116 C39(1.68)  LDD0763  [13]
 LDCM0447  CL56 HCT 116 C39(1.15)  LDD0764  [13]
 LDCM0448  CL57 HCT 116 C39(1.29)  LDD0765  [13]
 LDCM0449  CL58 HCT 116 C39(1.51)  LDD0766  [13]
 LDCM0450  CL59 HCT 116 C39(1.27)  LDD0767  [13]
 LDCM0451  CL6 HCT 116 C363(1.03); C39(1.20)  LDD0768  [13]
 LDCM0452  CL60 HCT 116 C39(1.70)  LDD0769  [13]
 LDCM0453  CL61 HCT 116 C39(0.85)  LDD0770  [13]
 LDCM0454  CL62 HCT 116 C39(0.87)  LDD0771  [13]
 LDCM0455  CL63 HCT 116 C39(0.68)  LDD0772  [13]
 LDCM0456  CL64 HCT 116 C39(0.91)  LDD0773  [13]
 LDCM0457  CL65 HCT 116 C39(0.61)  LDD0774  [13]
 LDCM0458  CL66 HCT 116 C39(0.97)  LDD0775  [13]
 LDCM0459  CL67 HCT 116 C39(0.87)  LDD0776  [13]
 LDCM0460  CL68 HCT 116 C39(0.54)  LDD0777  [13]
 LDCM0461  CL69 HCT 116 C39(0.96)  LDD0778  [13]
 LDCM0462  CL7 HCT 116 C363(1.09); C39(1.07)  LDD0779  [13]
 LDCM0463  CL70 HCT 116 C39(0.84)  LDD0780  [13]
 LDCM0464  CL71 HCT 116 C39(0.58)  LDD0781  [13]
 LDCM0465  CL72 HCT 116 C39(0.46)  LDD0782  [13]
 LDCM0466  CL73 HCT 116 C39(0.76)  LDD0783  [13]
 LDCM0467  CL74 HCT 116 C39(0.68)  LDD0784  [13]
 LDCM0469  CL76 HCT 116 C39(1.24)  LDD0786  [13]
 LDCM0470  CL77 HCT 116 C39(1.60)  LDD0787  [13]
 LDCM0471  CL78 HCT 116 C39(1.01)  LDD0788  [13]
 LDCM0472  CL79 HCT 116 C39(1.60)  LDD0789  [13]
 LDCM0473  CL8 HCT 116 C363(0.95); C39(1.34)  LDD0790  [13]
 LDCM0474  CL80 HCT 116 C39(1.43)  LDD0791  [13]
 LDCM0475  CL81 HCT 116 C39(1.16)  LDD0792  [13]
 LDCM0476  CL82 HCT 116 C39(1.87)  LDD0793  [13]
 LDCM0477  CL83 HCT 116 C39(1.82)  LDD0794  [13]
 LDCM0478  CL84 HCT 116 C39(1.37)  LDD0795  [13]
 LDCM0479  CL85 HCT 116 C39(1.33)  LDD0796  [13]
 LDCM0480  CL86 HCT 116 C39(1.33)  LDD0797  [13]
 LDCM0481  CL87 HCT 116 C39(1.10)  LDD0798  [13]
 LDCM0482  CL88 HCT 116 C39(1.61)  LDD0799  [13]
 LDCM0483  CL89 HCT 116 C39(1.90)  LDD0800  [13]
 LDCM0484  CL9 HCT 116 C363(0.96); C39(1.16)  LDD0801  [13]
 LDCM0485  CL90 HCT 116 C39(2.41)  LDD0802  [13]
 LDCM0486  CL91 HCT 116 C39(0.70)  LDD0803  [13]
 LDCM0487  CL92 HCT 116 C39(0.78)  LDD0804  [13]
 LDCM0488  CL93 HCT 116 C39(1.12)  LDD0805  [13]
 LDCM0489  CL94 HCT 116 C39(0.91)  LDD0806  [13]
 LDCM0490  CL95 HCT 116 C39(0.72)  LDD0807  [13]
 LDCM0491  CL96 HCT 116 C39(0.81)  LDD0808  [13]
 LDCM0492  CL97 HCT 116 C39(1.06)  LDD0809  [13]
 LDCM0493  CL98 HCT 116 C39(0.76)  LDD0810  [13]
 LDCM0494  CL99 HCT 116 C39(0.84)  LDD0811  [13]
 LDCM0495  E2913 HEK-293T C39(1.02); C467(0.80); C363(0.93)  LDD1698  [28]
 LDCM0175  Ethacrynic acid HeLa C39(1.34); C467(1.02); C467(1.23)  LDD2210  [12]
 LDCM0625  F8 Ramos C363(1.78); C467(0.80); C110(0.84); C39(1.08)  LDD2187  [29]
 LDCM0572  Fragment10 Ramos C363(13.74); C467(2.16); C110(0.56); C39(1.27)  LDD2189  [29]
 LDCM0573  Fragment11 Ramos C363(0.21); C467(2.53); C110(0.15); C39(1.09)  LDD2190  [29]
 LDCM0574  Fragment12 Ramos C363(20.00); C467(1.43); C110(1.37)  LDD2191  [29]
 LDCM0575  Fragment13 Ramos C363(1.21); C467(0.89); C110(1.34); C39(0.82)  LDD2192  [29]
 LDCM0576  Fragment14 Ramos C363(11.72); C467(1.72); C110(1.97); C39(1.32)  LDD2193  [29]
 LDCM0579  Fragment20 Ramos C363(20.00); C467(3.80); C39(3.09)  LDD2194  [29]
 LDCM0580  Fragment21 Ramos C363(1.44); C467(1.16); C110(1.06); C39(1.37)  LDD2195  [29]
 LDCM0582  Fragment23 Ramos C363(2.02); C467(0.99); C39(1.33)  LDD2196  [29]
 LDCM0578  Fragment27 Ramos C363(0.85); C467(0.90); C39(0.95)  LDD2197  [29]
 LDCM0586  Fragment28 Ramos C363(0.69); C467(1.05); C110(0.53); C39(0.69)  LDD2198  [29]
 LDCM0588  Fragment30 Ramos C363(2.55); C467(1.13); C110(0.56); C39(1.14)  LDD2199  [29]
 LDCM0589  Fragment31 Ramos C363(2.00); C467(1.06); C39(1.16)  LDD2200  [29]
 LDCM0590  Fragment32 Ramos C363(18.29); C467(0.99); C110(0.62); C39(0.76)  LDD2201  [29]
 LDCM0468  Fragment33 HCT 116 C39(0.55)  LDD0785  [13]
 LDCM0596  Fragment38 Ramos C363(3.31); C467(0.87); C39(1.12)  LDD2203  [29]
 LDCM0566  Fragment4 Ramos C363(7.95); C467(1.73); C110(0.57)  LDD2184  [29]
 LDCM0427  Fragment51 HCT 116 C39(1.58)  LDD0744  [13]
 LDCM0610  Fragment52 Ramos C363(2.64); C467(0.92); C110(0.86); C39(0.94)  LDD2204  [29]
 LDCM0614  Fragment56 Ramos C363(4.05); C467(1.12); C110(0.29); C39(0.87)  LDD2205  [29]
 LDCM0569  Fragment7 Ramos C363(12.60); C467(1.74); C110(0.40); C39(1.55)  LDD2186  [29]
 LDCM0571  Fragment9 Ramos C363(20.00); C467(1.66)  LDD2188  [29]
 LDCM0179  JZ128 PC-3 C39(0.00); C363(0.00)  LDD0462  [9]
 LDCM0022  KB02 Ramos 5.08  LDD0431  [30]
 LDCM0023  KB03 HEK-293T C363(1.16); C39(0.91); C467(1.10)  LDD1497  [28]
 LDCM0024  KB05 G361 C363(3.06)  LDD3311  [31]
 LDCM0627  NUDT7-COV-1 HEK-293T C467(4.92); C363(1.07)  LDD2206  [32]
 LDCM0628  OTUB2-COV-1 HEK-293T C363(0.73); C467(0.71)  LDD2207  [32]
 LDCM0131  RA190 MM1.R 2.06  LDD0299  [11]
 LDCM0021  THZ1 HeLa S3 C39(0.99)  LDD0460  [9]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
E3 ubiquitin-protein ligase RNF5 (RNF5) RNF5 family Q99942

The Drug(s) Related To This Target

Approved
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Asparagine Small molecular drug DB00174
L-glutamine Small molecular drug DB00130
Fluciclovine (18f) . DB13146
Investigative
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Benzylserine Small molecular drug D0VX9R
P-nitrophenyl Glutamyl Anilide Small molecular drug D00IWH

References

1 Fatty Acyl Sulfonyl Fluoride as an Activity-Based Probe for Profiling Fatty Acid-Associated Proteins in Living Cells. Chembiochem. 2022 Feb 16;23(4):e202100628. doi: 10.1002/cbic.202100628. Epub 2021 Dec 30.
2 Small-Molecule Activity-Based Probe for Monitoring Ubiquitin C-Terminal Hydrolase L1 (UCHL1) Activity in Live Cells and Zebrafish Embryos. J Am Chem Soc. 2020 Sep 30;142(39):16825-16841. doi: 10.1021/jacs.0c07726. Epub 2020 Sep 18.
Mass spectrometry data entry: PXD021557 , PXD015828
3 Tranylcypromine specificity for monoamine oxidase is limited by promiscuous protein labelling and lysosomal trapping. RSC Chem Biol. 2020 Aug 12;1(4):209-213. doi: 10.1039/d0cb00048e. eCollection 2020 Oct 1.
Mass spectrometry data entry: PXD018580
4 Charting the Chemical Space of Acrylamide-Based Inhibitors of zDHHC20. ACS Med Chem Lett. 2022 Sep 26;13(10):1648-1654. doi: 10.1021/acsmedchemlett.2c00336. eCollection 2022 Oct 13.
5 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.
6 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.
7 2H-Azirine-Based Reagents for Chemoselective Bioconjugation at Carboxyl Residues Inside Live Cells. J Am Chem Soc. 2020 Apr 1;142(13):6051-6059. doi: 10.1021/jacs.9b12116. Epub 2020 Mar 23.
8 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
9 A Chemoproteomic Strategy for Direct and Proteome-Wide Covalent Inhibitor Target-Site Identification. J Am Chem Soc. 2019 Jan 9;141(1):191-203. doi: 10.1021/jacs.8b07911. Epub 2018 Dec 20.
10 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
11 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.
12 Chemoproteomic Profiling Reveals Ethacrynic Acid Targets Adenine Nucleotide Translocases to Impair Mitochondrial Function. Mol Pharm. 2018 Jun 4;15(6):2413-2422. doi: 10.1021/acs.molpharmaceut.8b00250. Epub 2018 May 15.
13 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.
14 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
15 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
16 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
17 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
18 Tunable Amine-Reactive Electrophiles for Selective Profiling of Lysine. Angew Chem Int Ed Engl. 2022 Jan 26;61(5):e202112107. doi: 10.1002/anie.202112107. Epub 2021 Dec 16.
19 Solid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows. bioRxiv [Preprint]. 2023 Feb 18:2023.02.17.529022. doi: 10.1101/2023.02.17.529022.
Mass spectrometry data entry: PXD039931
20 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
21 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.
22 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
23 Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017 Jan 26;168(3):527-541.e29. doi: 10.1016/j.cell.2016.12.029. Epub 2017 Jan 19.
24 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.
25 Pharmacological Targeting of Vacuolar H(+)-ATPase via Subunit V1G Combats Multidrug-Resistant Cancer. Cell Chem Biol. 2020 Nov 19;27(11):1359-1370.e8. doi: 10.1016/j.chembiol.2020.06.011. Epub 2020 Jul 9.
26 Cell-based proteome profiling of potential dasatinib targets by use of affinity-based probes. J Am Chem Soc. 2012 Feb 15;134(6):3001-14. doi: 10.1021/ja208518u. Epub 2012 Feb 1.
27 Kinase Photoaffinity Labeling Reveals Low Selectivity Profile of the IRE1 Targeting Imidazopyrazine-Based KIRA6 Inhibitor. ACS Chem Biol. 2020 Dec 18;15(12):3106-3111. doi: 10.1021/acschembio.0c00802. Epub 2020 Dec 8.
Mass spectrometry data entry: PXD022628
28 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
29 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
30 2-Sulfonylpyridines as Tunable, Cysteine-Reactive Electrophiles. J Am Chem Soc. 2020 May 13;142(19):8972-8979. doi: 10.1021/jacs.0c02721. Epub 2020 Apr 29.
31 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
32 Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22.