Details of the Target

General Information of Target

Target ID LDTP08352
Target Name Histone-arginine methyltransferase CARM1 (CARM1)
Gene Name CARM1
Gene ID 10498
Synonyms
PRMT4; Histone-arginine methyltransferase CARM1; EC 2.1.1.319; Coactivator-associated arginine methyltransferase 1; Protein arginine N-methyltransferase 4
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAAAAAAVGPGAGGAGSAVPGGAGPCATVSVFPGARLLTIGDANGEIQRHAEQQALRLEV
RAGPDSAGIALYSHEDVCVFKCSVSRETECSRVGKQSFIITLGCNSVLIQFATPNDFCSF
YNILKTCRGHTLERSVFSERTEESSAVQYFQFYGYLSQQQNMMQDYVRTGTYQRAILQNH
TDFKDKIVLDVGCGSGILSFFAAQAGARKIYAVEASTMAQHAEVLVKSNNLTDRIVVIPG
KVEEVSLPEQVDIIISEPMGYMLFNERMLESYLHAKKYLKPSGNMFPTIGDVHLAPFTDE
QLYMEQFTKANFWYQPSFHGVDLSALRGAAVDEYFRQPVVDTFDIRILMAKSVKYTVNFL
EAKEGDLHRIEIPFKFHMLHSGLVHGLAFWFDVAFIGSIMTVWLSTAPTEPLTHWYQVRC
LFQSPLFAKAGDTLSGTCLLIANKRQSYDISIVAQVDQTGSKSSNLLDLKNPFFRYTGTT
PSPPPGSHYTSPSENMWNTGSTYNLSSGMAVAGMPTAYDLSSVIASGSSVGHNNLIPLAN
TGIVNHTHSRMGSIMSTGIVQGSSGAQGSGGGSTSAHYAVNSQFTMGGPAISMASPMSIP
TNTMHYGS
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Class I-like SAM-binding methyltransferase superfamily, Protein arginine N-methyltransferase family
Subcellular location
Nucleus
Function
Methylates (mono- and asymmetric dimethylation) the guanidino nitrogens of arginyl residues in several proteins involved in DNA packaging, transcription regulation, pre-mRNA splicing, and mRNA stability. Recruited to promoters upon gene activation together with histone acetyltransferases from EP300/P300 and p160 families, methylates histone H3 at 'Arg-17' (H3R17me), forming mainly asymmetric dimethylarginine (H3R17me2a), leading to activates transcription via chromatin remodeling. During nuclear hormone receptor activation and TCF7L2/TCF4 activation, acts synergically with EP300/P300 and either one of the p160 histone acetyltransferases NCOA1/SRC1, NCOA2/GRIP1 and NCOA3/ACTR or CTNNB1/beta-catenin to activate transcription. During myogenic transcriptional activation, acts together with NCOA3/ACTR as a coactivator for MEF2C. During monocyte inflammatory stimulation, acts together with EP300/P300 as a coactivator for NF-kappa-B. Acts as a coactivator for PPARG, promotes adipocyte differentiation and the accumulation of brown fat tissue. Plays a role in the regulation of pre-mRNA alternative splicing by methylation of splicing factors. Also seems to be involved in p53/TP53 transcriptional activation. Methylates EP300/P300, both at 'Arg-2142', which may loosen its interaction with NCOA2/GRIP1, and at 'Arg-580' and 'Arg-604' in the KIX domain, which impairs its interaction with CREB and inhibits CREB-dependent transcriptional activation. Also methylates arginine residues in RNA-binding proteins PABPC1, ELAVL1 and ELAV4, which may affect their mRNA-stabilizing properties and the half-life of their target mRNAs. Acts as a transcriptional coactivator of ACACA/acetyl-CoA carboxylase by enriching H3R17 methylation at its promoter, thereby positively regulating fatty acid synthesis. Independently of its methyltransferase activity, involved in replication fork progression: promotes PARP1 recruitment to replication forks, leading to poly-ADP-ribosylation of chromatin at replication forks and reduced fork speed.
TTD ID
T12837
Uniprot ID
Q86X55
DrugMap ID
TTIZQFJ
Ensemble ID
ENST00000327064.9
HGNC ID
HGNC:23393
ChEMBL ID
CHEMBL5406

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 22 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
TH211
 Probe Info  		Y272(6.90); Y314(6.54)  LDD0257  [2]
STPyne
 Probe Info  		K241(0.74)  LDD2217  [3]
Probe 1
 Probe Info  		Y334(44.04)  LDD3495  [4]
BTD
 Probe Info  		C438(1.40)  LDD2107  [5]
Sulforaphane-probe2
 Probe Info  		2.52  LDD0160  [6]
EA-probe
 Probe Info  		N.A.  LDD0440  [7]
HHS-475
 Probe Info  		Y314(0.64)  LDD0264  [8]
Acrolein
 Probe Info  		N.A.  LDD0221  [9]
DBIA
 Probe Info  		C420(1.15)  LDD0531  [10]
ATP probe
 Probe Info  		N.A.  LDD0199  [11]
4-Iodoacetamidophenylacetylene
 Probe Info  		C438(0.00); C193(0.00); C420(0.00)  LDD0038  [12]
IA-alkyne
 Probe Info  		C26(0.00); C420(0.00)  LDD0032  [13]
IPIAA_L
 Probe Info  		N.A.  LDD0031  [14]
Lodoacetamide azide
 Probe Info  		C438(0.00); C420(0.00); C193(0.00)  LDD0037  [12]
IPM
 Probe Info  		N.A.  LDD0025  [15]
JW-RF-010
 Probe Info  		N.A.  LDD0026  [15]
TFBX
 Probe Info  		N.A.  LDD0027  [15]
PF-06672131
 Probe Info  		N.A.  LDD0017  [16]
VSF
 Probe Info  		N.A.  LDD0007  [17]
AOyne
 Probe Info  		5.90  LDD0443  [18]
NAIA_5
 Probe Info  		C438(0.00); C78(0.00); C420(0.00); C127(0.00)  LDD2223  [19]
PAL-AfBPP Probe
Click To Hide/Show 11 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C059
 Probe Info  		8.34  LDD1756  [20]
C278
 Probe Info  		61.39  LDD1948  [20]
C280
 Probe Info  		9.99  LDD1950  [20]
C281
 Probe Info  		4.99  LDD1951  [20]
C282
 Probe Info  		17.15  LDD1952  [20]
C284
 Probe Info  		39.40  LDD1954  [20]
FFF probe11
 Probe Info  		13.51  LDD0471  [21]
FFF probe14
 Probe Info  		12.13  LDD0477  [21]
FFF probe2
 Probe Info  		20.00  LDD0463  [21]
FFF probe3
 Probe Info  		8.48  LDD0465  [21]
VE-P
 Probe Info  		N.A.  LDD0396  [22]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HCT 116 C420(1.15)  LDD0531  [10]
 LDCM0215  AC10 HCT 116 C420(0.96)  LDD0532  [10]
 LDCM0216  AC100 HCT 116 C420(0.80); C438(0.72)  LDD0533  [10]
 LDCM0217  AC101 HCT 116 C420(0.67); C438(0.70)  LDD0534  [10]
 LDCM0218  AC102 HCT 116 C420(0.82); C438(0.70)  LDD0535  [10]
 LDCM0219  AC103 HCT 116 C420(0.67); C438(0.56)  LDD0536  [10]
 LDCM0220  AC104 HCT 116 C420(0.83); C438(0.81)  LDD0537  [10]
 LDCM0221  AC105 HCT 116 C420(0.78); C438(0.63)  LDD0538  [10]
 LDCM0222  AC106 HCT 116 C420(0.71); C438(0.67)  LDD0539  [10]
 LDCM0223  AC107 HCT 116 C420(0.76); C438(0.75)  LDD0540  [10]
 LDCM0224  AC108 HCT 116 C420(0.70); C438(0.60)  LDD0541  [10]
 LDCM0225  AC109 HCT 116 C420(0.90); C438(0.71)  LDD0542  [10]
 LDCM0226  AC11 HCT 116 C420(0.94)  LDD0543  [10]
 LDCM0227  AC110 HCT 116 C420(0.80); C438(0.61)  LDD0544  [10]
 LDCM0228  AC111 HCT 116 C420(0.62); C438(0.50)  LDD0545  [10]
 LDCM0229  AC112 HCT 116 C420(0.58); C438(0.63)  LDD0546  [10]
 LDCM0230  AC113 HCT 116 C420(1.19); C438(1.16)  LDD0547  [10]
 LDCM0231  AC114 HCT 116 C420(0.98); C438(1.20)  LDD0548  [10]
 LDCM0232  AC115 HCT 116 C420(0.95); C438(1.15)  LDD0549  [10]
 LDCM0233  AC116 HCT 116 C420(1.05); C438(0.95)  LDD0550  [10]
 LDCM0234  AC117 HCT 116 C420(1.23); C438(1.20)  LDD0551  [10]
 LDCM0235  AC118 HCT 116 C420(1.23); C438(1.05)  LDD0552  [10]
 LDCM0236  AC119 HCT 116 C420(1.16); C438(1.02)  LDD0553  [10]
 LDCM0237  AC12 HCT 116 C420(1.19)  LDD0554  [10]
 LDCM0238  AC120 HCT 116 C420(1.11); C438(0.91)  LDD0555  [10]
 LDCM0239  AC121 HCT 116 C420(1.68); C438(1.18)  LDD0556  [10]
 LDCM0240  AC122 HCT 116 C420(1.14); C438(1.18)  LDD0557  [10]
 LDCM0241  AC123 HCT 116 C420(1.66); C438(1.38)  LDD0558  [10]
 LDCM0242  AC124 HCT 116 C420(1.54); C438(1.06)  LDD0559  [10]
 LDCM0243  AC125 HCT 116 C420(1.26); C438(0.98)  LDD0560  [10]
 LDCM0244  AC126 HCT 116 C420(1.35); C438(0.93)  LDD0561  [10]
 LDCM0245  AC127 HCT 116 C420(1.56); C438(1.08)  LDD0562  [10]
 LDCM0246  AC128 HCT 116 C420(1.64)  LDD0563  [10]
 LDCM0247  AC129 HCT 116 C420(1.44)  LDD0564  [10]
 LDCM0249  AC130 HCT 116 C420(1.47)  LDD0566  [10]
 LDCM0250  AC131 HCT 116 C420(1.11)  LDD0567  [10]
 LDCM0251  AC132 HCT 116 C420(0.88)  LDD0568  [10]
 LDCM0252  AC133 HCT 116 C420(1.23)  LDD0569  [10]
 LDCM0253  AC134 HCT 116 C420(0.79)  LDD0570  [10]
 LDCM0254  AC135 HCT 116 C420(0.87)  LDD0571  [10]
 LDCM0255  AC136 HCT 116 C420(0.85)  LDD0572  [10]
 LDCM0256  AC137 HCT 116 C420(0.72)  LDD0573  [10]
 LDCM0257  AC138 HCT 116 C420(0.49)  LDD0574  [10]
 LDCM0258  AC139 HCT 116 C420(0.58)  LDD0575  [10]
 LDCM0259  AC14 HCT 116 C420(1.21)  LDD0576  [10]
 LDCM0260  AC140 HCT 116 C420(0.47)  LDD0577  [10]
 LDCM0261  AC141 HCT 116 C420(0.47)  LDD0578  [10]
 LDCM0262  AC142 HCT 116 C420(0.64)  LDD0579  [10]
 LDCM0263  AC143 HCT 116 C420(0.84)  LDD0580  [10]
 LDCM0264  AC144 HCT 116 C420(0.76)  LDD0581  [10]
 LDCM0265  AC145 HCT 116 C420(0.88)  LDD0582  [10]
 LDCM0266  AC146 HCT 116 C420(0.73)  LDD0583  [10]
 LDCM0267  AC147 HCT 116 C420(0.71)  LDD0584  [10]
 LDCM0268  AC148 HCT 116 C420(0.82)  LDD0585  [10]
 LDCM0269  AC149 HCT 116 C420(0.77)  LDD0586  [10]
 LDCM0270  AC15 HCT 116 C420(1.07)  LDD0587  [10]
 LDCM0271  AC150 HCT 116 C420(0.87)  LDD0588  [10]
 LDCM0272  AC151 HCT 116 C420(0.85)  LDD0589  [10]
 LDCM0273  AC152 HCT 116 C420(0.75)  LDD0590  [10]
 LDCM0274  AC153 HCT 116 C420(0.64)  LDD0591  [10]
 LDCM0621  AC154 HCT 116 C420(0.72)  LDD2158  [10]
 LDCM0622  AC155 HCT 116 C420(0.80)  LDD2159  [10]
 LDCM0623  AC156 HCT 116 C420(0.90)  LDD2160  [10]
 LDCM0624  AC157 HCT 116 C420(0.90)  LDD2161  [10]
 LDCM0276  AC17 HCT 116 C420(1.06)  LDD0593  [10]
 LDCM0277  AC18 HCT 116 C420(0.90)  LDD0594  [10]
 LDCM0278  AC19 HCT 116 C420(1.00)  LDD0595  [10]
 LDCM0279  AC2 HCT 116 C420(0.98)  LDD0596  [10]
 LDCM0280  AC20 HCT 116 C420(0.89)  LDD0597  [10]
 LDCM0281  AC21 HCT 116 C420(0.91)  LDD0598  [10]
 LDCM0282  AC22 HCT 116 C420(1.05)  LDD0599  [10]
 LDCM0283  AC23 HCT 116 C420(1.05)  LDD0600  [10]
 LDCM0284  AC24 HCT 116 C420(1.13)  LDD0601  [10]
 LDCM0285  AC25 HCT 116 C420(1.09)  LDD0602  [10]
 LDCM0286  AC26 HCT 116 C420(0.76)  LDD0603  [10]
 LDCM0287  AC27 HCT 116 C420(0.70)  LDD0604  [10]
 LDCM0288  AC28 HCT 116 C420(0.70)  LDD0605  [10]
 LDCM0289  AC29 HCT 116 C420(0.65)  LDD0606  [10]
 LDCM0290  AC3 HCT 116 C420(1.17)  LDD0607  [10]
 LDCM0291  AC30 HCT 116 C420(0.59)  LDD0608  [10]
 LDCM0292  AC31 HCT 116 C420(0.66)  LDD0609  [10]
 LDCM0293  AC32 HCT 116 C420(0.51)  LDD0610  [10]
 LDCM0294  AC33 HCT 116 C420(0.80)  LDD0611  [10]
 LDCM0295  AC34 HCT 116 C420(0.74)  LDD0612  [10]
 LDCM0296  AC35 HCT 116 C420(0.98)  LDD0613  [10]
 LDCM0297  AC36 HCT 116 C420(1.07)  LDD0614  [10]
 LDCM0298  AC37 HCT 116 C420(1.03)  LDD0615  [10]
 LDCM0299  AC38 HCT 116 C420(1.10)  LDD0616  [10]
 LDCM0300  AC39 HCT 116 C420(0.87)  LDD0617  [10]
 LDCM0301  AC4 HCT 116 C420(1.08)  LDD0618  [10]
 LDCM0302  AC40 HCT 116 C420(0.80)  LDD0619  [10]
 LDCM0303  AC41 HCT 116 C420(0.95)  LDD0620  [10]
 LDCM0304  AC42 HCT 116 C420(0.92)  LDD0621  [10]
 LDCM0305  AC43 HCT 116 C420(0.77)  LDD0622  [10]
 LDCM0306  AC44 HCT 116 C420(0.86)  LDD0623  [10]
 LDCM0307  AC45 HCT 116 C420(0.78)  LDD0624  [10]
 LDCM0308  AC46 HCT 116 C420(0.87)  LDD0625  [10]
 LDCM0309  AC47 HCT 116 C420(0.85)  LDD0626  [10]
 LDCM0310  AC48 HCT 116 C420(0.78)  LDD0627  [10]
 LDCM0311  AC49 HCT 116 C420(0.65)  LDD0628  [10]
 LDCM0312  AC5 HCT 116 C420(1.09)  LDD0629  [10]
 LDCM0313  AC50 HCT 116 C420(0.65)  LDD0630  [10]
 LDCM0314  AC51 HCT 116 C420(0.98)  LDD0631  [10]
 LDCM0315  AC52 HCT 116 C420(0.81)  LDD0632  [10]
 LDCM0316  AC53 HCT 116 C420(0.76)  LDD0633  [10]
 LDCM0317  AC54 HCT 116 C420(0.79)  LDD0634  [10]
 LDCM0318  AC55 HCT 116 C420(0.66)  LDD0635  [10]
 LDCM0319  AC56 HCT 116 C420(0.42)  LDD0636  [10]
 LDCM0320  AC57 HCT 116 C420(0.89)  LDD0637  [10]
 LDCM0321  AC58 HCT 116 C420(0.72)  LDD0638  [10]
 LDCM0322  AC59 HCT 116 C420(0.88)  LDD0639  [10]
 LDCM0323  AC6 HCT 116 C420(0.76)  LDD0640  [10]
 LDCM0324  AC60 HCT 116 C420(0.72)  LDD0641  [10]
 LDCM0325  AC61 HCT 116 C420(0.77)  LDD0642  [10]
 LDCM0326  AC62 HCT 116 C420(0.73)  LDD0643  [10]
 LDCM0327  AC63 HCT 116 C420(0.83)  LDD0644  [10]
 LDCM0328  AC64 HCT 116 C420(0.81)  LDD0645  [10]
 LDCM0329  AC65 HCT 116 C420(0.77)  LDD0646  [10]
 LDCM0330  AC66 HCT 116 C420(0.88)  LDD0647  [10]
 LDCM0331  AC67 HCT 116 C420(0.56)  LDD0648  [10]
 LDCM0332  AC68 HCT 116 C420(0.80)  LDD0649  [10]
 LDCM0333  AC69 HCT 116 C420(0.74)  LDD0650  [10]
 LDCM0334  AC7 HCT 116 C420(0.98)  LDD0651  [10]
 LDCM0335  AC70 HCT 116 C420(0.55)  LDD0652  [10]
 LDCM0336  AC71 HCT 116 C420(1.03)  LDD0653  [10]
 LDCM0337  AC72 HCT 116 C420(0.70)  LDD0654  [10]
 LDCM0338  AC73 HCT 116 C420(0.53)  LDD0655  [10]
 LDCM0339  AC74 HCT 116 C420(0.82)  LDD0656  [10]
 LDCM0340  AC75 HCT 116 C420(0.42)  LDD0657  [10]
 LDCM0341  AC76 HCT 116 C420(0.88)  LDD0658  [10]
 LDCM0342  AC77 HCT 116 C420(0.63)  LDD0659  [10]
 LDCM0343  AC78 HCT 116 C420(0.72)  LDD0660  [10]
 LDCM0344  AC79 HCT 116 C420(0.76)  LDD0661  [10]
 LDCM0345  AC8 HCT 116 C420(0.90)  LDD0662  [10]
 LDCM0346  AC80 HCT 116 C420(1.02)  LDD0663  [10]
 LDCM0347  AC81 HCT 116 C420(0.77)  LDD0664  [10]
 LDCM0348  AC82 HCT 116 C420(0.60)  LDD0665  [10]
 LDCM0349  AC83 HCT 116 C420(0.80); C438(0.96)  LDD0666  [10]
 LDCM0350  AC84 HCT 116 C420(0.65); C438(0.86)  LDD0667  [10]
 LDCM0351  AC85 HCT 116 C420(0.66); C438(1.05)  LDD0668  [10]
 LDCM0352  AC86 HCT 116 C420(0.63); C438(0.83)  LDD0669  [10]
 LDCM0353  AC87 HCT 116 C438(0.70); C420(0.73)  LDD0670  [10]
 LDCM0354  AC88 HCT 116 C438(0.64); C420(0.70)  LDD0671  [10]
 LDCM0355  AC89 HCT 116 C420(0.59); C438(0.86)  LDD0672  [10]
 LDCM0357  AC90 HCT 116 C438(0.62); C420(0.65)  LDD0674  [10]
 LDCM0358  AC91 HCT 116 C420(0.75); C438(0.94)  LDD0675  [10]
 LDCM0359  AC92 HCT 116 C420(0.71); C438(0.93)  LDD0676  [10]
 LDCM0360  AC93 HCT 116 C420(0.71); C438(0.73)  LDD0677  [10]
 LDCM0361  AC94 HCT 116 C420(1.14); C438(1.37)  LDD0678  [10]
 LDCM0362  AC95 HCT 116 C438(0.64); C420(0.79)  LDD0679  [10]
 LDCM0363  AC96 HCT 116 C420(1.04); C438(1.20)  LDD0680  [10]
 LDCM0364  AC97 HCT 116 C420(0.55); C438(0.69)  LDD0681  [10]
 LDCM0365  AC98 HCT 116 C438(0.39); C420(0.65)  LDD0682  [10]
 LDCM0366  AC99 HCT 116 C420(0.63); C438(0.66)  LDD0683  [10]
 LDCM0248  AKOS034007472 HCT 116 C420(1.09)  LDD0565  [10]
 LDCM0356  AKOS034007680 HCT 116 C420(1.02)  LDD0673  [10]
 LDCM0275  AKOS034007705 HCT 116 C420(0.75)  LDD0592  [10]
 LDCM0156  Aniline NCI-H1299 11.89  LDD0403  [1]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [9]
 LDCM0632  CL-Sc Hep-G2 C26(3.00)  LDD2227  [19]
 LDCM0367  CL1 HCT 116 C420(1.12)  LDD0684  [10]
 LDCM0368  CL10 HCT 116 C420(0.70)  LDD0685  [10]
 LDCM0369  CL100 HCT 116 C420(1.04)  LDD0686  [10]
 LDCM0370  CL101 HCT 116 C420(0.89)  LDD0687  [10]
 LDCM0371  CL102 HCT 116 C420(1.05)  LDD0688  [10]
 LDCM0372  CL103 HCT 116 C420(1.35)  LDD0689  [10]
 LDCM0373  CL104 HCT 116 C420(1.13)  LDD0690  [10]
 LDCM0374  CL105 HCT 116 C420(1.01)  LDD0691  [10]
 LDCM0375  CL106 HCT 116 C420(0.90)  LDD0692  [10]
 LDCM0376  CL107 HCT 116 C420(0.91)  LDD0693  [10]
 LDCM0377  CL108 HCT 116 C420(0.90)  LDD0694  [10]
 LDCM0378  CL109 HCT 116 C420(0.86)  LDD0695  [10]
 LDCM0379  CL11 HCT 116 C420(0.74)  LDD0696  [10]
 LDCM0380  CL110 HCT 116 C420(0.79)  LDD0697  [10]
 LDCM0381  CL111 HCT 116 C420(0.78)  LDD0698  [10]
 LDCM0382  CL112 HCT 116 C420(0.88)  LDD0699  [10]
 LDCM0383  CL113 HCT 116 C420(0.57)  LDD0700  [10]
 LDCM0384  CL114 HCT 116 C420(0.65)  LDD0701  [10]
 LDCM0385  CL115 HCT 116 C420(0.71)  LDD0702  [10]
 LDCM0386  CL116 HCT 116 C420(0.78)  LDD0703  [10]
 LDCM0387  CL117 HCT 116 C420(0.60)  LDD0704  [10]
 LDCM0388  CL118 HCT 116 C420(0.87)  LDD0705  [10]
 LDCM0389  CL119 HCT 116 C420(0.82)  LDD0706  [10]
 LDCM0390  CL12 HCT 116 C420(0.71)  LDD0707  [10]
 LDCM0391  CL120 HCT 116 C420(1.02)  LDD0708  [10]
 LDCM0392  CL121 HCT 116 C420(0.75)  LDD0709  [10]
 LDCM0393  CL122 HCT 116 C420(0.68)  LDD0710  [10]
 LDCM0394  CL123 HCT 116 C420(0.72)  LDD0711  [10]
 LDCM0395  CL124 HCT 116 C420(0.64)  LDD0712  [10]
 LDCM0396  CL125 HCT 116 C420(1.06)  LDD0713  [10]
 LDCM0397  CL126 HCT 116 C420(0.95)  LDD0714  [10]
 LDCM0398  CL127 HCT 116 C420(0.92)  LDD0715  [10]
 LDCM0399  CL128 HCT 116 C420(0.85)  LDD0716  [10]
 LDCM0400  CL13 HCT 116 C420(0.88)  LDD0717  [10]
 LDCM0401  CL14 HCT 116 C420(1.01)  LDD0718  [10]
 LDCM0402  CL15 HCT 116 C420(0.93)  LDD0719  [10]
 LDCM0403  CL16 HCT 116 C420(0.79)  LDD0720  [10]
 LDCM0404  CL17 HCT 116 C420(0.88)  LDD0721  [10]
 LDCM0405  CL18 HCT 116 C420(0.85)  LDD0722  [10]
 LDCM0406  CL19 HCT 116 C420(0.69)  LDD0723  [10]
 LDCM0407  CL2 HCT 116 C420(1.16)  LDD0724  [10]
 LDCM0408  CL20 HCT 116 C420(0.69)  LDD0725  [10]
 LDCM0409  CL21 HCT 116 C420(0.64)  LDD0726  [10]
 LDCM0410  CL22 HCT 116 C420(0.58)  LDD0727  [10]
 LDCM0411  CL23 HCT 116 C420(0.76)  LDD0728  [10]
 LDCM0412  CL24 HCT 116 C420(0.64)  LDD0729  [10]
 LDCM0413  CL25 HCT 116 C420(0.71)  LDD0730  [10]
 LDCM0414  CL26 HCT 116 C420(0.73)  LDD0731  [10]
 LDCM0415  CL27 HCT 116 C420(0.83)  LDD0732  [10]
 LDCM0416  CL28 HCT 116 C420(0.64)  LDD0733  [10]
 LDCM0417  CL29 HCT 116 C420(0.69)  LDD0734  [10]
 LDCM0418  CL3 HCT 116 C420(1.08)  LDD0735  [10]
 LDCM0419  CL30 HCT 116 C420(0.86)  LDD0736  [10]
 LDCM0420  CL31 HCT 116 C420(0.78)  LDD0737  [10]
 LDCM0421  CL32 HCT 116 C420(0.68)  LDD0738  [10]
 LDCM0422  CL33 HCT 116 C420(0.57)  LDD0739  [10]
 LDCM0423  CL34 HCT 116 C420(0.47)  LDD0740  [10]
 LDCM0424  CL35 HCT 116 C420(0.56)  LDD0741  [10]
 LDCM0425  CL36 HCT 116 C420(0.61)  LDD0742  [10]
 LDCM0426  CL37 HCT 116 C420(0.57)  LDD0743  [10]
 LDCM0428  CL39 HCT 116 C420(0.56)  LDD0745  [10]
 LDCM0429  CL4 HCT 116 C420(1.12)  LDD0746  [10]
 LDCM0430  CL40 HCT 116 C420(0.57)  LDD0747  [10]
 LDCM0431  CL41 HCT 116 C420(0.67)  LDD0748  [10]
 LDCM0432  CL42 HCT 116 C420(0.53)  LDD0749  [10]
 LDCM0433  CL43 HCT 116 C420(0.51)  LDD0750  [10]
 LDCM0434  CL44 HCT 116 C420(0.62)  LDD0751  [10]
 LDCM0435  CL45 HCT 116 C420(0.52)  LDD0752  [10]
 LDCM0436  CL46 HCT 116 C420(1.55); C438(0.97)  LDD0753  [10]
 LDCM0437  CL47 HCT 116 C420(1.41); C438(0.94)  LDD0754  [10]
 LDCM0438  CL48 HCT 116 C420(1.37); C438(0.81)  LDD0755  [10]
 LDCM0439  CL49 HCT 116 C420(1.28); C438(1.15)  LDD0756  [10]
 LDCM0440  CL5 HCT 116 C420(1.05)  LDD0757  [10]
 LDCM0441  CL50 HCT 116 C420(1.40); C438(0.99)  LDD0758  [10]
 LDCM0442  CL51 HCT 116 C420(1.40); C438(1.15)  LDD0759  [10]
 LDCM0443  CL52 HCT 116 C420(1.20); C438(0.84)  LDD0760  [10]
 LDCM0444  CL53 HCT 116 C420(1.28); C438(0.70)  LDD0761  [10]
 LDCM0445  CL54 HCT 116 C420(1.32); C438(0.72)  LDD0762  [10]
 LDCM0446  CL55 HCT 116 C420(1.40); C438(0.92)  LDD0763  [10]
 LDCM0447  CL56 HCT 116 C420(1.16); C438(0.73)  LDD0764  [10]
 LDCM0448  CL57 HCT 116 C420(1.40); C438(0.92)  LDD0765  [10]
 LDCM0449  CL58 HCT 116 C420(1.39); C438(0.79)  LDD0766  [10]
 LDCM0450  CL59 HCT 116 C420(1.26); C438(1.04)  LDD0767  [10]
 LDCM0451  CL6 HCT 116 C420(0.87)  LDD0768  [10]
 LDCM0452  CL60 HCT 116 C420(1.21); C438(0.91)  LDD0769  [10]
 LDCM0453  CL61 HCT 116 C420(0.87)  LDD0770  [10]
 LDCM0454  CL62 HCT 116 C420(0.87)  LDD0771  [10]
 LDCM0455  CL63 HCT 116 C420(0.88)  LDD0772  [10]
 LDCM0456  CL64 HCT 116 C420(0.74)  LDD0773  [10]
 LDCM0457  CL65 HCT 116 C420(0.95)  LDD0774  [10]
 LDCM0458  CL66 HCT 116 C420(0.74)  LDD0775  [10]
 LDCM0459  CL67 HCT 116 C420(0.75)  LDD0776  [10]
 LDCM0460  CL68 HCT 116 C420(0.63)  LDD0777  [10]
 LDCM0461  CL69 HCT 116 C420(0.84)  LDD0778  [10]
 LDCM0462  CL7 HCT 116 C420(0.94)  LDD0779  [10]
 LDCM0463  CL70 HCT 116 C420(0.59)  LDD0780  [10]
 LDCM0464  CL71 HCT 116 C420(0.70)  LDD0781  [10]
 LDCM0465  CL72 HCT 116 C420(0.78)  LDD0782  [10]
 LDCM0466  CL73 HCT 116 C420(0.70)  LDD0783  [10]
 LDCM0467  CL74 HCT 116 C420(0.70)  LDD0784  [10]
 LDCM0469  CL76 HCT 116 C420(0.89)  LDD0786  [10]
 LDCM0470  CL77 HCT 116 C420(0.76)  LDD0787  [10]
 LDCM0471  CL78 HCT 116 C420(0.83)  LDD0788  [10]
 LDCM0472  CL79 HCT 116 C420(0.78)  LDD0789  [10]
 LDCM0473  CL8 HCT 116 C420(0.59)  LDD0790  [10]
 LDCM0474  CL80 HCT 116 C420(1.06)  LDD0791  [10]
 LDCM0475  CL81 HCT 116 C420(0.86)  LDD0792  [10]
 LDCM0476  CL82 HCT 116 C420(0.63)  LDD0793  [10]
 LDCM0477  CL83 HCT 116 C420(0.65)  LDD0794  [10]
 LDCM0478  CL84 HCT 116 C420(0.54)  LDD0795  [10]
 LDCM0479  CL85 HCT 116 C420(0.72)  LDD0796  [10]
 LDCM0480  CL86 HCT 116 C420(0.93)  LDD0797  [10]
 LDCM0481  CL87 HCT 116 C420(0.89)  LDD0798  [10]
 LDCM0482  CL88 HCT 116 C420(0.67)  LDD0799  [10]
 LDCM0483  CL89 HCT 116 C420(0.50)  LDD0800  [10]
 LDCM0484  CL9 HCT 116 C420(0.88)  LDD0801  [10]
 LDCM0485  CL90 HCT 116 C420(0.97)  LDD0802  [10]
 LDCM0486  CL91 HCT 116 C420(0.94)  LDD0803  [10]
 LDCM0487  CL92 HCT 116 C420(1.03)  LDD0804  [10]
 LDCM0488  CL93 HCT 116 C420(1.20)  LDD0805  [10]
 LDCM0489  CL94 HCT 116 C420(1.02)  LDD0806  [10]
 LDCM0490  CL95 HCT 116 C420(0.93)  LDD0807  [10]
 LDCM0491  CL96 HCT 116 C420(0.98)  LDD0808  [10]
 LDCM0492  CL97 HCT 116 C420(0.92)  LDD0809  [10]
 LDCM0493  CL98 HCT 116 C420(0.86)  LDD0810  [10]
 LDCM0494  CL99 HCT 116 C420(0.95)  LDD0811  [10]
 LDCM0634  CY-0357 Hep-G2 C26(0.54)  LDD2228  [19]
 LDCM0495  E2913 HEK-293T C78(0.97); C438(1.00); C193(0.98)  LDD1698  [23]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C420(1.73)  LDD1702  [5]
 LDCM0175  Ethacrynic acid HeLa N.A.  LDD0440  [7]
 LDCM0625  F8 Ramos C420(0.39)  LDD2187  [24]
 LDCM0572  Fragment10 Ramos C420(0.51)  LDD2189  [24]
 LDCM0574  Fragment12 Ramos C420(0.58)  LDD2191  [24]
 LDCM0575  Fragment13 Ramos C420(1.19)  LDD2192  [24]
 LDCM0576  Fragment14 Ramos C420(0.76)  LDD2193  [24]
 LDCM0579  Fragment20 Ramos C420(0.69)  LDD2194  [24]
 LDCM0580  Fragment21 Ramos C420(0.81)  LDD2195  [24]
 LDCM0582  Fragment23 Ramos C420(1.14)  LDD2196  [24]
 LDCM0578  Fragment27 Ramos C420(1.06)  LDD2197  [24]
 LDCM0586  Fragment28 Ramos C420(0.83)  LDD2198  [24]
 LDCM0588  Fragment30 Ramos C420(1.28)  LDD2199  [24]
 LDCM0589  Fragment31 Ramos C420(1.47)  LDD2200  [24]
 LDCM0590  Fragment32 Ramos C420(0.56)  LDD2201  [24]
 LDCM0468  Fragment33 HCT 116 C420(0.77)  LDD0785  [10]
 LDCM0596  Fragment38 Ramos C420(0.63)  LDD2203  [24]
 LDCM0566  Fragment4 Ramos C420(0.54)  LDD2184  [24]
 LDCM0427  Fragment51 HCT 116 C420(0.50)  LDD0744  [10]
 LDCM0610  Fragment52 Ramos C420(2.02)  LDD2204  [24]
 LDCM0614  Fragment56 Ramos C420(1.40)  LDD2205  [24]
 LDCM0569  Fragment7 Ramos C420(0.35)  LDD2186  [24]
 LDCM0571  Fragment9 Ramos C420(0.49)  LDD2188  [24]
 LDCM0116  HHS-0101 DM93 Y314(0.64)  LDD0264  [8]
 LDCM0117  HHS-0201 DM93 Y314(1.36)  LDD0265  [8]
 LDCM0118  HHS-0301 DM93 Y314(3.40)  LDD0266  [8]
 LDCM0119  HHS-0401 DM93 Y314(0.81)  LDD0267  [8]
 LDCM0120  HHS-0701 DM93 Y314(1.25)  LDD0268  [8]
 LDCM0107  IAA HeLa N.A.  LDD0221  [9]
 LDCM0022  KB02 HEK-293T C193(1.02); C78(0.99)  LDD1492  [23]
 LDCM0023  KB03 HEK-293T C193(0.98); C78(1.06)  LDD1497  [23]
 LDCM0024  KB05 COLO792 C193(1.94)  LDD3310  [25]
 LDCM0109  NEM HeLa N.A.  LDD0223  [9]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C438(1.40)  LDD2107  [5]
 LDCM0529  Nucleophilic fragment 27b MDA-MB-231 C438(0.14)  LDD2122  [5]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C438(0.38)  LDD2148  [5]
 LDCM0557  Nucleophilic fragment 8b MDA-MB-231 C438(0.12)  LDD2151  [5]
 LDCM0627  NUDT7-COV-1 HEK-293T C26(0.83)  LDD2206  [26]
 LDCM0628  OTUB2-COV-1 HEK-293T C26(0.47)  LDD2207  [26]
 LDCM0003  Sulforaphane MDA-MB-231 2.52  LDD0160  [6]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Bifunctional arginine demethylase and lysyl-hydroxylase JMJD6 (JMJD6) JMJD6 family Q6NYC1
Cleavage and polyadenylation specificity factor subunit 5 (NUDT21) Nudix hydrolase family O43809
Nuclear receptor coactivator 3 (NCOA3) SRC/p160 nuclear receptor coactivator family Q9Y6Q9
Transcription factor
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
CCAAT/enhancer-binding protein beta (CEBPB) BZIP family P17676
SWI/SNF complex subunit SMARCC1 (SMARCC1) SMARCC family Q92922
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
DnaJ homolog subfamily A member 3, mitochondrial (DNAJA3) . Q96EY1
KH domain-containing RNA-binding protein QKI (QKI) . Q96PU8

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bms Pyrazole Inhibitor 7f Small molecular drug D0BU8W
Pmid19632837c17f Small molecular drug D0Q3FY

References

1 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.
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 Global profiling of lysine reactivity and ligandability in the human proteome. Nat Chem. 2017 Dec;9(12):1181-1190. doi: 10.1038/nchem.2826. Epub 2017 Jul 31.
4 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.
5 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
6 Competition-based, quantitative chemical proteomics in breast cancer cells identifies new target profiles for sulforaphane. Chem Commun (Camb). 2017 May 4;53(37):5182-5185. doi: 10.1039/c6cc08797c.
Mass spectrometry data entry: PXD006279
7 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.
8 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.
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 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.
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 SP3-Enabled Rapid and High Coverage Chemoproteomic Identification of Cell-State-Dependent Redox-Sensitive Cysteines. Mol Cell Proteomics. 2022 Apr;21(4):100218. doi: 10.1016/j.mcpro.2022.100218. Epub 2022 Feb 25.
Mass spectrometry data entry: PXD029500 , PXD031647
15 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
16 Site-Specific Activity-Based Protein Profiling Using Phosphonate Handles. Mol Cell Proteomics. 2023 Jan;22(1):100455. doi: 10.1016/j.mcpro.2022.100455. Epub 2022 Nov 24.
Mass spectrometry data entry: PXD036569
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 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.
19 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
20 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
21 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.
22 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.
23 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
24 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
25 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
26 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.