Details of the Target

General Information of Target

Target ID LDTP02679
Target Name Prolyl 4-hydroxylase subunit alpha-1 (P4HA1)
Gene Name P4HA1
Gene ID 5033
Synonyms
P4HA; Prolyl 4-hydroxylase subunit alpha-1; 4-PH alpha-1; EC 1.14.11.2; Procollagen-proline,2-oxoglutarate-4-dioxygenase subunit alpha-1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MIWYILIIGILLPQSLAHPGFFTSIGQMTDLIHTEKDLVTSLKDYIKAEEDKLEQIKKWA
EKLDRLTSTATKDPEGFVGHPVNAFKLMKRLNTEWSELENLVLKDMSDGFISNLTIQRQY
FPNDEDQVGAAKALLRLQDTYNLDTDTISKGNLPGVKHKSFLTAEDCFELGKVAYTEADY
YHTELWMEQALRQLDEGEISTIDKVSVLDYLSYAVYQQGDLDKALLLTKKLLELDPEHQR
ANGNLKYFEYIMAKEKDVNKSASDDQSDQKTTPKKKGVAVDYLPERQKYEMLCRGEGIKM
TPRRQKKLFCRYHDGNRNPKFILAPAKQEDEWDKPRIIRFHDIISDAEIEIVKDLAKPRL
RRATISNPITGDLETVHYRISKSAWLSGYENPVVSRINMRIQDLTGLDVSTAEELQVANY
GVGGQYEPHFDFARKDEPDAFKELGTGNRIATWLFYMSDVSAGGATVFPEVGASVWPKKG
TAVFWYNLFASGEGDYSTRHAACPVLVGNKWVSNKWLHERGQEFRRPCTLSELE
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
P4HA family
Subcellular location
Endoplasmic reticulum lumen
Function Catalyzes the post-translational formation of 4-hydroxyproline in -Xaa-Pro-Gly- sequences in collagens and other proteins.
TTD ID
T61729
Uniprot ID
P13674
DrugMap ID
TTNH25W
Ensemble ID
ENST00000263556.3
HGNC ID
HGNC:8546
ChEMBL ID
CHEMBL1250350

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
42MGBA SNV: p.E54Q DBIA    Probe Info 
MEWO SNV: p.E443K DBIA    Probe Info 
RKO Deletion: p.T271LfsTer30 DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 28 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Alkylaryl probe 1
 Probe Info  		15.00  LDD0387  [1]
Alkylaryl probe 3
 Probe Info  		12.92  LDD0381  [1]
TH211
 Probe Info  		Y289(7.65)  LDD0257  [2]
TH216
 Probe Info  		Y389(6.84)  LDD0259  [2]
ONAyne
 Probe Info  		K299(1.10)  LDD0274  [3]
STPyne
 Probe Info  		K132(10.00); K230(10.00); K288(2.97); K299(10.00)  LDD0277  [3]
IPM
 Probe Info  		N.A.  LDD0241  [4]
Probe 1
 Probe Info  		Y120(20.00); Y141(139.08)  LDD3495  [5]
Alkylaryl probe 2
 Probe Info  		3.00  LDD0390  [1]
BTD
 Probe Info  		C503(0.90)  LDD1700  [6]
HHS-475
 Probe Info  		Y216(1.30); Y389(1.72); Y250(8.00)  LDD0264  [7]
HHS-465
 Probe Info  		Y250(6.22); Y389(10.00)  LDD2237  [8]
Acrolein
 Probe Info  		H500(0.00); H80(0.00)  LDD0221  [9]
DBIA
 Probe Info  		C528(1.52)  LDD0080  [10]
5E-2FA
 Probe Info  		N.A.  LDD2235  [11]
m-APA
 Probe Info  		N.A.  LDD2231  [11]
4-Iodoacetamidophenylacetylene
 Probe Info  		C503(0.00); C528(0.00); C167(0.00)  LDD0038  [12]
IA-alkyne
 Probe Info  		N.A.  LDD0032  [13]
Lodoacetamide azide
 Probe Info  		C503(0.00); C293(0.00); C528(0.00); C167(0.00)  LDD0037  [12]
PPMS
 Probe Info  		N.A.  LDD0008  [14]
SF
 Probe Info  		Y250(0.00); Y378(0.00)  LDD0028  [15]
TFBX
 Probe Info  		N.A.  LDD0148  [16]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [17]
Ox-W18
 Probe Info  		N.A.  LDD2175  [18]
1c-yne
 Probe Info  		K150(0.00); K353(0.00)  LDD0228  [19]
Crotonaldehyde
 Probe Info  		C503(0.00); C167(0.00)  LDD0219  [9]
Methacrolein
 Probe Info  		N.A.  LDD0218  [9]
NAIA_5
 Probe Info  		N.A.  LDD2223  [20]
PAL-AfBPP Probe
Click To Hide/Show 45 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IMP2070
 Probe Info  		1.79  LDD0367  [21]
C017
 Probe Info  		10.85  LDD1725  [22]
C040
 Probe Info  		7.57  LDD1740  [22]
C053
 Probe Info  		5.98  LDD1751  [22]
C063
 Probe Info  		10.13  LDD1760  [22]
C087
 Probe Info  		8.34  LDD1779  [22]
C091
 Probe Info  		12.64  LDD1782  [22]
C106
 Probe Info  		16.68  LDD1793  [22]
C122
 Probe Info  		7.73  LDD1808  [22]
C129
 Probe Info  		5.03  LDD1811  [22]
C130
 Probe Info  		7.41  LDD1812  [22]
C134
 Probe Info  		20.82  LDD1816  [22]
C165
 Probe Info  		12.30  LDD1845  [22]
C191
 Probe Info  		10.63  LDD1868  [22]
C214
 Probe Info  		5.74  LDD1888  [22]
C218
 Probe Info  		14.52  LDD1892  [22]
C220
 Probe Info  		17.63  LDD1894  [22]
C228
 Probe Info  		18.38  LDD1901  [22]
C239
 Probe Info  		5.82  LDD1912  [22]
C244
 Probe Info  		20.53  LDD1917  [22]
C249
 Probe Info  		12.64  LDD1922  [22]
C252
 Probe Info  		9.00  LDD1925  [22]
C280
 Probe Info  		10.13  LDD1950  [22]
C287
 Probe Info  		10.13  LDD1957  [22]
C289
 Probe Info  		28.05  LDD1959  [22]
C296
 Probe Info  		17.63  LDD1966  [22]
C303
 Probe Info  		5.24  LDD1972  [22]
C305
 Probe Info  		11.96  LDD1974  [22]
C313
 Probe Info  		25.99  LDD1980  [22]
C314
 Probe Info  		39.95  LDD1981  [22]
C320
 Probe Info  		7.11  LDD1986  [22]
C322
 Probe Info  		5.98  LDD1988  [22]
C338
 Probe Info  		10.48  LDD2001  [22]
C353
 Probe Info  		12.30  LDD2014  [22]
C363
 Probe Info  		20.39  LDD2024  [22]
C382
 Probe Info  		8.88  LDD2041  [22]
C413
 Probe Info  		12.55  LDD2069  [22]
C420
 Probe Info  		12.91  LDD2075  [22]
FFF probe11
 Probe Info  		14.57  LDD0472  [23]
FFF probe13
 Probe Info  		19.62  LDD0475  [23]
FFF probe2
 Probe Info  		20.00  LDD0463  [23]
FFF probe3
 Probe Info  		16.59  LDD0465  [23]
FFF probe6
 Probe Info  		6.71  LDD0468  [23]
JN0003
 Probe Info  		16.95  LDD0469  [23]
STS-1
 Probe Info  		N.A.  LDD0136  [24]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C528(0.39)  LDD2112  [6]
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C503(1.12)  LDD2130  [6]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C503(1.45); C293(0.83)  LDD2117  [6]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C503(1.20)  LDD2152  [6]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C503(0.72)  LDD2132  [6]
 LDCM0538  4-(Cyanoacetyl)morpholine MDA-MB-231 C503(0.75)  LDD2131  [6]
 LDCM0214  AC1 HCT 116 C503(0.74); C528(1.38)  LDD0531  [10]
 LDCM0215  AC10 HCT 116 C503(1.00); C528(1.20)  LDD0532  [10]
 LDCM0216  AC100 HEK-293T C503(0.91)  LDD0814  [10]
 LDCM0217  AC101 HEK-293T C503(0.95)  LDD0815  [10]
 LDCM0218  AC102 HEK-293T C503(0.81)  LDD0816  [10]
 LDCM0219  AC103 HEK-293T C503(0.99)  LDD0817  [10]
 LDCM0220  AC104 HEK-293T C503(0.98)  LDD0818  [10]
 LDCM0221  AC105 HEK-293T C503(0.87)  LDD0819  [10]
 LDCM0222  AC106 HEK-293T C503(1.05)  LDD0820  [10]
 LDCM0223  AC107 HEK-293T C503(0.98)  LDD0821  [10]
 LDCM0224  AC108 HEK-293T C503(0.98)  LDD0822  [10]
 LDCM0225  AC109 HEK-293T C503(0.99)  LDD0823  [10]
 LDCM0226  AC11 HCT 116 C503(0.97); C528(1.10)  LDD0543  [10]
 LDCM0227  AC110 HEK-293T C503(1.12)  LDD0825  [10]
 LDCM0228  AC111 HEK-293T C503(1.32)  LDD0826  [10]
 LDCM0229  AC112 HEK-293T C503(1.12)  LDD0827  [10]
 LDCM0230  AC113 HEK-293T C503(0.90); C528(1.28)  LDD0828  [10]
 LDCM0231  AC114 HEK-293T C503(0.94); C528(1.39)  LDD0829  [10]
 LDCM0232  AC115 HEK-293T C503(0.85); C528(1.19)  LDD0830  [10]
 LDCM0233  AC116 HEK-293T C503(0.81); C528(1.14)  LDD0831  [10]
 LDCM0234  AC117 HEK-293T C503(0.79); C528(1.11)  LDD0832  [10]
 LDCM0235  AC118 HEK-293T C503(0.85); C528(1.33)  LDD0833  [10]
 LDCM0236  AC119 HEK-293T C503(0.89); C528(1.34)  LDD0834  [10]
 LDCM0237  AC12 HCT 116 C503(1.08); C528(1.22)  LDD0554  [10]
 LDCM0238  AC120 HEK-293T C503(0.72); C528(1.39)  LDD0836  [10]
 LDCM0239  AC121 HEK-293T C503(0.76); C528(1.43)  LDD0837  [10]
 LDCM0240  AC122 HEK-293T C503(0.82); C528(1.03)  LDD0838  [10]
 LDCM0241  AC123 HEK-293T C503(0.80); C528(1.26)  LDD0839  [10]
 LDCM0242  AC124 HEK-293T C503(0.83); C528(1.17)  LDD0840  [10]
 LDCM0243  AC125 HEK-293T C503(0.86); C528(1.19)  LDD0841  [10]
 LDCM0244  AC126 HEK-293T C503(1.04); C528(1.22)  LDD0842  [10]
 LDCM0245  AC127 HEK-293T C503(1.07); C528(1.00)  LDD0843  [10]
 LDCM0259  AC14 HCT 116 C503(1.16); C528(0.96)  LDD0576  [10]
 LDCM0263  AC143 HCT 116 C528(1.10)  LDD0580  [10]
 LDCM0264  AC144 HCT 116 C528(1.21)  LDD0581  [10]
 LDCM0265  AC145 HCT 116 C528(1.11)  LDD0582  [10]
 LDCM0266  AC146 HCT 116 C528(0.89)  LDD0583  [10]
 LDCM0267  AC147 HCT 116 C528(1.05)  LDD0584  [10]
 LDCM0268  AC148 HCT 116 C528(1.17)  LDD0585  [10]
 LDCM0269  AC149 HCT 116 C528(1.08)  LDD0586  [10]
 LDCM0270  AC15 HCT 116 C503(0.99); C528(1.15)  LDD0587  [10]
 LDCM0271  AC150 HCT 116 C528(1.11)  LDD0588  [10]
 LDCM0272  AC151 HCT 116 C528(0.98)  LDD0589  [10]
 LDCM0273  AC152 HCT 116 C528(0.87)  LDD0590  [10]
 LDCM0274  AC153 HCT 116 C528(0.95)  LDD0591  [10]
 LDCM0621  AC154 HCT 116 C528(1.02)  LDD2158  [10]
 LDCM0622  AC155 HCT 116 C528(1.26)  LDD2159  [10]
 LDCM0623  AC156 HCT 116 C528(0.94)  LDD2160  [10]
 LDCM0624  AC157 HCT 116 C528(0.99)  LDD2161  [10]
 LDCM0276  AC17 HCT 116 C503(0.92)  LDD0593  [10]
 LDCM0277  AC18 HCT 116 C503(0.43)  LDD0594  [10]
 LDCM0278  AC19 HCT 116 C503(0.89)  LDD0595  [10]
 LDCM0279  AC2 HCT 116 C503(0.84); C528(1.06)  LDD0596  [10]
 LDCM0280  AC20 HCT 116 C503(1.04)  LDD0597  [10]
 LDCM0281  AC21 HCT 116 C503(0.88)  LDD0598  [10]
 LDCM0282  AC22 HCT 116 C503(0.92)  LDD0599  [10]
 LDCM0283  AC23 HCT 116 C503(0.95)  LDD0600  [10]
 LDCM0284  AC24 HCT 116 C503(1.02)  LDD0601  [10]
 LDCM0285  AC25 HEK-293T C503(0.84)  LDD0883  [10]
 LDCM0286  AC26 HEK-293T C503(0.83)  LDD0884  [10]
 LDCM0287  AC27 HEK-293T C503(0.76)  LDD0885  [10]
 LDCM0288  AC28 HEK-293T C503(0.64)  LDD0886  [10]
 LDCM0289  AC29 HEK-293T C503(0.79)  LDD0887  [10]
 LDCM0290  AC3 HCT 116 C503(0.89); C528(0.98)  LDD0607  [10]
 LDCM0291  AC30 HEK-293T C503(0.85)  LDD0889  [10]
 LDCM0292  AC31 HEK-293T C503(0.97)  LDD0890  [10]
 LDCM0293  AC32 HEK-293T C503(0.81)  LDD0891  [10]
 LDCM0294  AC33 HEK-293T C503(0.78)  LDD0892  [10]
 LDCM0295  AC34 HEK-293T C503(1.00)  LDD0893  [10]
 LDCM0296  AC35 HCT 116 C503(2.01)  LDD0613  [10]
 LDCM0297  AC36 HCT 116 C503(1.75)  LDD0614  [10]
 LDCM0298  AC37 HCT 116 C503(1.50)  LDD0615  [10]
 LDCM0299  AC38 HCT 116 C503(1.57)  LDD0616  [10]
 LDCM0300  AC39 HCT 116 C503(1.13)  LDD0617  [10]
 LDCM0301  AC4 HCT 116 C503(0.76); C528(1.19)  LDD0618  [10]
 LDCM0302  AC40 HCT 116 C503(0.71)  LDD0619  [10]
 LDCM0303  AC41 HCT 116 C503(1.18)  LDD0620  [10]
 LDCM0304  AC42 HCT 116 C503(0.89)  LDD0621  [10]
 LDCM0305  AC43 HCT 116 C503(1.27)  LDD0622  [10]
 LDCM0306  AC44 HCT 116 C503(0.85)  LDD0623  [10]
 LDCM0307  AC45 HCT 116 C503(0.68)  LDD0624  [10]
 LDCM0308  AC46 HCT 116 C528(0.76); C503(1.25)  LDD0625  [10]
 LDCM0309  AC47 HCT 116 C528(0.76); C503(0.98)  LDD0626  [10]
 LDCM0310  AC48 HCT 116 C528(0.75); C503(1.42)  LDD0627  [10]
 LDCM0311  AC49 HCT 116 C503(0.61); C528(0.86)  LDD0628  [10]
 LDCM0312  AC5 HCT 116 C503(0.71); C528(1.06)  LDD0629  [10]
 LDCM0313  AC50 HCT 116 C503(0.58); C528(0.94)  LDD0630  [10]
 LDCM0314  AC51 HCT 116 C528(0.97); C503(1.82)  LDD0631  [10]
 LDCM0315  AC52 HCT 116 C528(0.99); C503(1.04)  LDD0632  [10]
 LDCM0316  AC53 HCT 116 C503(0.65); C528(0.88)  LDD0633  [10]
 LDCM0317  AC54 HCT 116 C503(0.61); C528(1.02)  LDD0634  [10]
 LDCM0318  AC55 HCT 116 C503(0.60); C528(1.37)  LDD0635  [10]
 LDCM0319  AC56 HCT 116 C503(0.67); C528(1.00)  LDD0636  [10]
 LDCM0320  AC57 HCT 116 C528(0.92)  LDD0637  [10]
 LDCM0321  AC58 HCT 116 C528(0.75)  LDD0638  [10]
 LDCM0322  AC59 HCT 116 C528(0.86)  LDD0639  [10]
 LDCM0323  AC6 HCT 116 C503(0.99); C528(1.06)  LDD0640  [10]
 LDCM0324  AC60 HCT 116 C528(0.98)  LDD0641  [10]
 LDCM0325  AC61 HCT 116 C528(0.86)  LDD0642  [10]
 LDCM0326  AC62 HCT 116 C528(0.92)  LDD0643  [10]
 LDCM0327  AC63 HCT 116 C528(1.00)  LDD0644  [10]
 LDCM0328  AC64 HCT 116 C528(1.04)  LDD0645  [10]
 LDCM0329  AC65 HCT 116 C528(1.03)  LDD0646  [10]
 LDCM0330  AC66 HCT 116 C528(0.90)  LDD0647  [10]
 LDCM0331  AC67 HCT 116 C528(0.97)  LDD0648  [10]
 LDCM0332  AC68 HCT 116 C528(0.96)  LDD0649  [10]
 LDCM0333  AC69 HCT 116 C528(0.94)  LDD0650  [10]
 LDCM0334  AC7 HCT 116 C503(0.99); C528(1.05)  LDD0651  [10]
 LDCM0335  AC70 HCT 116 C528(1.03)  LDD0652  [10]
 LDCM0336  AC71 HCT 116 C528(1.03)  LDD0653  [10]
 LDCM0337  AC72 HCT 116 C528(1.10)  LDD0654  [10]
 LDCM0338  AC73 HCT 116 C528(1.00)  LDD0655  [10]
 LDCM0339  AC74 HCT 116 C528(1.02)  LDD0656  [10]
 LDCM0340  AC75 HCT 116 C528(1.03)  LDD0657  [10]
 LDCM0341  AC76 HCT 116 C528(1.06)  LDD0658  [10]
 LDCM0342  AC77 HCT 116 C528(1.10)  LDD0659  [10]
 LDCM0343  AC78 HCT 116 C528(0.91)  LDD0660  [10]
 LDCM0344  AC79 HCT 116 C528(1.05)  LDD0661  [10]
 LDCM0345  AC8 HCT 116 C503(1.01); C528(1.05)  LDD0662  [10]
 LDCM0346  AC80 HCT 116 C528(0.98)  LDD0663  [10]
 LDCM0347  AC81 HCT 116 C528(1.01)  LDD0664  [10]
 LDCM0348  AC82 HCT 116 C528(1.02)  LDD0665  [10]
 LDCM0349  AC83 HEK-293T C503(1.26); C528(1.24)  LDD0947  [10]
 LDCM0350  AC84 HEK-293T C503(0.86); C528(1.23)  LDD0948  [10]
 LDCM0351  AC85 HEK-293T C503(0.87); C528(1.26)  LDD0949  [10]
 LDCM0352  AC86 HEK-293T C503(0.90); C528(1.31)  LDD0950  [10]
 LDCM0353  AC87 HEK-293T C503(0.89); C528(1.37)  LDD0951  [10]
 LDCM0354  AC88 HEK-293T C503(0.90); C528(1.37)  LDD0952  [10]
 LDCM0355  AC89 HEK-293T C503(0.87); C528(1.33)  LDD0953  [10]
 LDCM0357  AC90 HEK-293T C503(0.79); C528(1.32)  LDD0955  [10]
 LDCM0358  AC91 HEK-293T C503(0.96); C528(1.35)  LDD0956  [10]
 LDCM0359  AC92 HEK-293T C503(0.99); C528(1.11)  LDD0957  [10]
 LDCM0360  AC93 HEK-293T C503(0.74); C528(1.17)  LDD0958  [10]
 LDCM0361  AC94 HEK-293T C503(0.85); C528(1.14)  LDD0959  [10]
 LDCM0362  AC95 HEK-293T C503(0.87); C528(1.20)  LDD0960  [10]
 LDCM0363  AC96 HEK-293T C503(0.72); C528(1.02)  LDD0961  [10]
 LDCM0364  AC97 HEK-293T C503(0.98); C528(1.09)  LDD0962  [10]
 LDCM0365  AC98 HEK-293T C503(0.96)  LDD0963  [10]
 LDCM0366  AC99 HEK-293T C503(0.93)  LDD0964  [10]
 LDCM0545  Acetamide MDA-MB-231 C528(0.72); C503(0.34)  LDD2138  [6]
 LDCM0248  AKOS034007472 HCT 116 C503(1.03); C528(1.06)  LDD0565  [10]
 LDCM0356  AKOS034007680 HCT 116 C503(1.17); C528(1.20)  LDD0673  [10]
 LDCM0275  AKOS034007705 HCT 116 C503(0.53); C528(0.99)  LDD0592  [10]
 LDCM0020  ARS-1620 HCC44 C503(1.06); C528(1.01)  LDD2171  [10]
 LDCM0498  BS-3668 MDA-MB-231 C528(0.61); C503(0.40)  LDD2091  [6]
 LDCM0108  Chloroacetamide HeLa C167(0.00); C503(0.00); H80(0.00)  LDD0222  [9]
 LDCM0367  CL1 HEK-293T C503(0.64)  LDD0965  [10]
 LDCM0368  CL10 HEK-293T C503(0.65)  LDD0966  [10]
 LDCM0369  CL100 HCT 116 C503(0.73); C528(1.29)  LDD0686  [10]
 LDCM0370  CL101 HCT 116 C503(0.99); C528(1.06)  LDD0687  [10]
 LDCM0371  CL102 HCT 116 C528(0.95); C503(1.06)  LDD0688  [10]
 LDCM0372  CL103 HCT 116 C503(0.99); C528(1.15)  LDD0689  [10]
 LDCM0373  CL104 HCT 116 C503(1.05); C528(1.14)  LDD0690  [10]
 LDCM0374  CL105 HCT 116 C503(0.78)  LDD0691  [10]
 LDCM0375  CL106 HCT 116 C503(0.48)  LDD0692  [10]
 LDCM0376  CL107 HCT 116 C503(0.44)  LDD0693  [10]
 LDCM0377  CL108 HCT 116 C503(0.30)  LDD0694  [10]
 LDCM0378  CL109 HCT 116 C503(0.72)  LDD0695  [10]
 LDCM0379  CL11 HEK-293T C503(0.70)  LDD0977  [10]
 LDCM0380  CL110 HCT 116 C503(0.51)  LDD0697  [10]
 LDCM0381  CL111 HCT 116 C503(0.85)  LDD0698  [10]
 LDCM0382  CL112 HEK-293T C503(0.71)  LDD0980  [10]
 LDCM0383  CL113 HEK-293T C503(0.87)  LDD0981  [10]
 LDCM0384  CL114 HEK-293T C503(0.81)  LDD0982  [10]
 LDCM0385  CL115 HEK-293T C503(0.74)  LDD0983  [10]
 LDCM0386  CL116 HEK-293T C503(0.79)  LDD0984  [10]
 LDCM0387  CL117 HCT 116 C503(0.76)  LDD0704  [10]
 LDCM0388  CL118 HCT 116 C503(0.96)  LDD0705  [10]
 LDCM0389  CL119 HCT 116 C503(0.74)  LDD0706  [10]
 LDCM0390  CL12 HEK-293T C503(0.66)  LDD0988  [10]
 LDCM0391  CL120 HCT 116 C503(1.32)  LDD0708  [10]
 LDCM0392  CL121 HCT 116 C503(0.60); C528(1.05)  LDD0709  [10]
 LDCM0393  CL122 HCT 116 C528(0.88); C503(1.00)  LDD0710  [10]
 LDCM0394  CL123 HCT 116 C503(0.61); C528(0.87)  LDD0711  [10]
 LDCM0395  CL124 HCT 116 C503(0.60); C528(1.40)  LDD0712  [10]
 LDCM0396  CL125 HCT 116 C528(0.85)  LDD0713  [10]
 LDCM0397  CL126 HCT 116 C528(0.82)  LDD0714  [10]
 LDCM0398  CL127 HCT 116 C528(0.91)  LDD0715  [10]
 LDCM0399  CL128 HCT 116 C528(0.80)  LDD0716  [10]
 LDCM0400  CL13 HEK-293T C503(0.55)  LDD0998  [10]
 LDCM0401  CL14 HEK-293T C503(0.56)  LDD0999  [10]
 LDCM0402  CL15 HEK-293T C503(0.50)  LDD1000  [10]
 LDCM0403  CL16 HCT 116 C503(0.67); C528(1.01)  LDD0720  [10]
 LDCM0404  CL17 HCT 116 C503(0.76); C528(0.99)  LDD0721  [10]
 LDCM0405  CL18 HCT 116 C503(0.50); C528(0.92)  LDD0722  [10]
 LDCM0406  CL19 HCT 116 C503(0.74); C528(0.91)  LDD0723  [10]
 LDCM0407  CL2 HEK-293T C503(0.60)  LDD1005  [10]
 LDCM0408  CL20 HCT 116 C503(0.38); C528(0.96)  LDD0725  [10]
 LDCM0409  CL21 HCT 116 C503(0.37); C528(0.77)  LDD0726  [10]
 LDCM0410  CL22 HCT 116 C503(0.41); C528(1.02)  LDD0727  [10]
 LDCM0411  CL23 HCT 116 C503(0.46); C528(0.99)  LDD0728  [10]
 LDCM0412  CL24 HCT 116 C503(0.34); C528(0.93)  LDD0729  [10]
 LDCM0413  CL25 HCT 116 C503(0.38); C528(1.02)  LDD0730  [10]
 LDCM0414  CL26 HCT 116 C503(0.54); C528(1.44)  LDD0731  [10]
 LDCM0415  CL27 HCT 116 C503(0.57); C528(0.95)  LDD0732  [10]
 LDCM0416  CL28 HCT 116 C503(0.48); C528(1.02)  LDD0733  [10]
 LDCM0417  CL29 HCT 116 C503(0.47); C528(0.93)  LDD0734  [10]
 LDCM0418  CL3 HEK-293T C503(0.86)  LDD1016  [10]
 LDCM0419  CL30 HCT 116 C503(0.68); C528(0.98)  LDD0736  [10]
 LDCM0420  CL31 HCT 116 C503(0.78)  LDD0737  [10]
 LDCM0421  CL32 HCT 116 C503(0.83)  LDD0738  [10]
 LDCM0422  CL33 HCT 116 C503(0.69)  LDD0739  [10]
 LDCM0423  CL34 HCT 116 C503(0.41)  LDD0740  [10]
 LDCM0424  CL35 HCT 116 C503(0.40)  LDD0741  [10]
 LDCM0425  CL36 HCT 116 C503(0.49)  LDD0742  [10]
 LDCM0426  CL37 HCT 116 C503(0.42)  LDD0743  [10]
 LDCM0428  CL39 HCT 116 C503(0.41)  LDD0745  [10]
 LDCM0429  CL4 HEK-293T C503(0.57)  LDD1027  [10]
 LDCM0430  CL40 HCT 116 C503(0.42)  LDD0747  [10]
 LDCM0431  CL41 HCT 116 C503(0.55)  LDD0748  [10]
 LDCM0432  CL42 HCT 116 C503(0.38)  LDD0749  [10]
 LDCM0433  CL43 HCT 116 C503(0.47)  LDD0750  [10]
 LDCM0434  CL44 HCT 116 C503(0.56)  LDD0751  [10]
 LDCM0435  CL45 HCT 116 C503(0.55)  LDD0752  [10]
 LDCM0436  CL46 HCT 116 C528(0.91)  LDD0753  [10]
 LDCM0437  CL47 HCT 116 C528(0.96)  LDD0754  [10]
 LDCM0438  CL48 HCT 116 C528(0.98)  LDD0755  [10]
 LDCM0439  CL49 HCT 116 C528(0.93)  LDD0756  [10]
 LDCM0440  CL5 HEK-293T C503(0.65)  LDD1038  [10]
 LDCM0441  CL50 HCT 116 C528(0.88)  LDD0758  [10]
 LDCM0442  CL51 HCT 116 C528(0.95)  LDD0759  [10]
 LDCM0443  CL52 HCT 116 C528(0.95)  LDD0760  [10]
 LDCM0444  CL53 HCT 116 C528(1.01)  LDD0761  [10]
 LDCM0445  CL54 HCT 116 C528(0.89)  LDD0762  [10]
 LDCM0446  CL55 HCT 116 C528(0.99)  LDD0763  [10]
 LDCM0447  CL56 HCT 116 C528(1.07)  LDD0764  [10]
 LDCM0448  CL57 HCT 116 C528(0.91)  LDD0765  [10]
 LDCM0449  CL58 HCT 116 C528(0.94)  LDD0766  [10]
 LDCM0450  CL59 HCT 116 C528(0.93)  LDD0767  [10]
 LDCM0451  CL6 HEK-293T C503(0.63)  LDD1049  [10]
 LDCM0452  CL60 HCT 116 C528(1.00)  LDD0769  [10]
 LDCM0453  CL61 HEK-293T C503(1.07); C528(1.02); C167(1.04)  LDD1656  [25]
 LDCM0454  CL62 HEK-293T C503(0.98); C528(1.20)  LDD1657  [25]
 LDCM0455  CL63 HEK-293T C503(1.04); C528(1.13); C167(1.01)  LDD1658  [25]
 LDCM0456  CL64 HEK-293T C503(1.12); C528(1.22); C167(0.97)  LDD1659  [25]
 LDCM0457  CL65 HEK-293T C503(1.02); C528(0.94)  LDD1660  [25]
 LDCM0458  CL66 HEK-293T C503(0.98); C528(1.04); C167(1.13)  LDD1661  [25]
 LDCM0459  CL67 HEK-293T C503(1.02); C528(1.01)  LDD1662  [25]
 LDCM0460  CL68 HEK-293T C503(1.00); C167(1.13)  LDD1663  [25]
 LDCM0461  CL69 HEK-293T C503(0.86); C528(1.05)  LDD1664  [25]
 LDCM0462  CL7 HEK-293T C503(0.54)  LDD1060  [10]
 LDCM0463  CL70 HEK-293T C503(0.82); C528(1.14)  LDD1666  [25]
 LDCM0464  CL71 HEK-293T C503(0.99); C528(1.07); C167(1.29)  LDD1667  [25]
 LDCM0465  CL72 HEK-293T C503(1.02); C528(1.16); C167(1.12)  LDD1668  [25]
 LDCM0466  CL73 HEK-293T C503(1.35); C528(1.18); C167(0.94)  LDD1669  [25]
 LDCM0467  CL74 HEK-293T C503(1.01); C528(1.07)  LDD1670  [25]
 LDCM0469  CL76 HCT 116 C503(0.87)  LDD0786  [10]
 LDCM0470  CL77 HCT 116 C503(0.78)  LDD0787  [10]
 LDCM0471  CL78 HCT 116 C503(0.71)  LDD0788  [10]
 LDCM0472  CL79 HCT 116 C503(0.41)  LDD0789  [10]
 LDCM0473  CL8 HEK-293T C503(1.27)  LDD1071  [10]
 LDCM0474  CL80 HCT 116 C503(0.73)  LDD0791  [10]
 LDCM0475  CL81 HCT 116 C503(0.69)  LDD0792  [10]
 LDCM0476  CL82 HCT 116 C503(0.40)  LDD0793  [10]
 LDCM0477  CL83 HCT 116 C503(0.44)  LDD0794  [10]
 LDCM0478  CL84 HCT 116 C503(0.40)  LDD0795  [10]
 LDCM0479  CL85 HCT 116 C503(0.70)  LDD0796  [10]
 LDCM0480  CL86 HCT 116 C503(0.87)  LDD0797  [10]
 LDCM0481  CL87 HCT 116 C503(0.72)  LDD0798  [10]
 LDCM0482  CL88 HCT 116 C503(0.40)  LDD0799  [10]
 LDCM0483  CL89 HCT 116 C503(0.45)  LDD0800  [10]
 LDCM0484  CL9 HEK-293T C503(1.09)  LDD1082  [10]
 LDCM0485  CL90 HCT 116 C503(0.96)  LDD0802  [10]
 LDCM0486  CL91 HCT 116 C503(0.84); C528(1.04)  LDD0803  [10]
 LDCM0487  CL92 HCT 116 C503(0.84); C528(1.20)  LDD0804  [10]
 LDCM0488  CL93 HCT 116 C503(0.78); C528(1.19)  LDD0805  [10]
 LDCM0489  CL94 HCT 116 C503(0.74); C528(1.19)  LDD0806  [10]
 LDCM0490  CL95 HCT 116 C503(0.69); C528(1.11)  LDD0807  [10]
 LDCM0491  CL96 HCT 116 C503(0.78); C528(1.13)  LDD0808  [10]
 LDCM0492  CL97 HCT 116 C503(0.71); C528(1.08)  LDD0809  [10]
 LDCM0493  CL98 HCT 116 C503(0.67); C528(1.12)  LDD0810  [10]
 LDCM0494  CL99 HCT 116 C503(0.75); C528(1.28)  LDD0811  [10]
 LDCM0495  E2913 HEK-293T C503(1.13); C528(1.05); C167(1.04)  LDD1698  [25]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C293(2.37); C528(0.98)  LDD1702  [6]
 LDCM0468  Fragment33 HEK-293T C503(1.01); C528(1.12); C167(1.03)  LDD1671  [25]
 LDCM0427  Fragment51 HCT 116 C503(0.44)  LDD0744  [10]
 LDCM0116  HHS-0101 DM93 Y216(1.30); Y389(1.72); Y250(8.00)  LDD0264  [7]
 LDCM0117  HHS-0201 DM93 Y389(1.24); Y250(1.50); Y216(1.79)  LDD0265  [7]
 LDCM0118  HHS-0301 DM93 Y175(0.17); Y389(0.64); Y216(0.74); Y250(1.40)  LDD0266  [7]
 LDCM0119  HHS-0401 DM93 Y389(1.13); Y216(1.51); Y250(2.15)  LDD0267  [7]
 LDCM0120  HHS-0701 DM93 Y175(0.12); Y389(0.82); Y216(1.01); Y250(2.03)  LDD0268  [7]
 LDCM0107  IAA HeLa H500(0.00); H80(0.00)  LDD0221  [9]
 LDCM0022  KB02 HCT 116 C528(1.52)  LDD0080  [10]
 LDCM0023  KB03 HCT 116 C528(1.30)  LDD0081  [10]
 LDCM0024  KB05 HCT 116 C528(1.16)  LDD0082  [10]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C528(0.85); C503(0.39)  LDD2121  [6]
 LDCM0109  NEM HeLa C167(0.00); H341(0.00); H500(0.00)  LDD0223  [9]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C503(0.31)  LDD2089  [6]
 LDCM0497  Nucleophilic fragment 11b MDA-MB-231 C528(1.17)  LDD2090  [6]
 LDCM0499  Nucleophilic fragment 12b MDA-MB-231 C503(1.02)  LDD2092  [6]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C503(1.03)  LDD2093  [6]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C503(0.98)  LDD2094  [6]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C528(1.54); C503(1.18)  LDD2098  [6]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C528(0.83); C503(0.97)  LDD2099  [6]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C528(0.38)  LDD2100  [6]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C528(0.56); C503(0.82)  LDD2104  [6]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C503(1.13)  LDD2105  [6]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C528(0.41)  LDD2106  [6]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C528(0.94); C503(0.92); C293(0.96)  LDD2107  [6]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C528(0.55)  LDD2108  [6]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C503(0.93)  LDD2109  [6]
 LDCM0517  Nucleophilic fragment 21b MDA-MB-231 C528(0.41)  LDD2110  [6]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C528(0.98)  LDD2118  [6]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C503(2.17)  LDD2119  [6]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C503(0.88)  LDD2120  [6]
 LDCM0529  Nucleophilic fragment 27b MDA-MB-231 C528(0.54)  LDD2122  [6]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C528(0.84); C503(0.71)  LDD2123  [6]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C528(1.02); C503(0.73)  LDD2125  [6]
 LDCM0533  Nucleophilic fragment 29b MDA-MB-231 C528(1.57)  LDD2126  [6]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C503(0.86)  LDD2127  [6]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C503(0.92)  LDD2128  [6]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C528(1.40)  LDD2129  [6]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C528(1.67); C503(0.99)  LDD2135  [6]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C528(1.21); C503(0.96); C293(1.57)  LDD2136  [6]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C528(1.05); C503(1.03)  LDD2137  [6]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C503(0.90)  LDD1700  [6]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C503(0.64)  LDD2140  [6]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C528(0.97); C503(0.97)  LDD2143  [6]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C528(2.64); C503(2.66)  LDD2144  [6]
 LDCM0551  Nucleophilic fragment 5b MDA-MB-231 C528(0.56)  LDD2145  [6]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C528(1.43); C503(0.70)  LDD2146  [6]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C528(0.71); C503(0.22)  LDD2150  [6]
 LDCM0099  Phenelzine HEK-293T 3.00  LDD0390  [1]
 LDCM0021  THZ1 HCT 116 C503(1.06); C528(1.01)  LDD2173  [10]

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
Prolyl 4-hydroxylase subunit alpha-1 (P4HA1) P4HA family P13674
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Huntingtin (HTT) Huntingtin family P42858

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
Ascorbic Acid Small molecular drug DB00126
Hydralazine Small molecular drug DB01275
Succinic Acid Small molecular drug DB00139
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Lufironil Small molecular drug D01NCH
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Safironil Small molecular drug D0P2BD
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Proline Small molecular drug DB00172

References

1 Hydrazines as versatile chemical biology probes and drug-discovery tools for cofactor-dependent enzymes. bioRxiv, 2020-06.
2 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
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 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
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 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
8 Global targeting of functional tyrosines using sulfur-triazole exchange chemistry. Nat Chem Biol. 2020 Feb;16(2):150-159. doi: 10.1038/s41589-019-0404-5. Epub 2019 Nov 25.
9 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.
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 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
12 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
13 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
14 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
15 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
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 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
18 Oxidative cyclization reagents reveal tryptophan cation- interactions. Nature. 2024 Mar;627(8004):680-687. doi: 10.1038/s41586-024-07140-6. Epub 2024 Mar 6.
Mass spectrometry data entry: PXD001377 , PXD005252
19 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.
20 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
21 A Probe for NLRP3 Inflammasome Inhibitor MCC950 Identifies Carbonic Anhydrase 2 as a Novel Target. ACS Chem Biol. 2021 Jun 18;16(6):982-990. doi: 10.1021/acschembio.1c00218. Epub 2021 May 18.
Mass spectrometry data entry: PXD024915 , PXD024913
22 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
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.
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Mass spectrometry data entry: PXD044402