Details of the Target

General Information of Target

Target ID LDTP05539
Target Name Serine/arginine-rich splicing factor 1 (SRSF1)
Gene Name SRSF1
Gene ID 6426
Synonyms
ASF; SF2; SF2P33; SFRS1; Serine/arginine-rich splicing factor 1; Alternative-splicing factor 1; ASF-1; Splicing factor, arginine/serine-rich 1; pre-mRNA-splicing factor SF2, P33 subunit
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSGGGVIRGPAGNNDCRIYVGNLPPDIRTKDIEDVFYKYGAIRDIDLKNRRGGPPFAFVE
FEDPRDAEDAVYGRDGYDYDGYRLRVEFPRSGRGTGRGGGGGGGGGAPRGRYGPPSRRSE
NRVVVSGLPPSGSWQDLKDHMREAGDVCYADVYRDGTGVVEFVRKEDMTYAVRKLDNTKF
RSHEGETAYIRVKVDGPRSPSYGRSRSRSRSRSRSRSRSNSRSRSYSPRRSRGSPRYSPR
HSRSRSRT
Target Bioclass
Other
Family
Splicing factor SR family
Subcellular location
Cytoplasm
Function
Plays a role in preventing exon skipping, ensuring the accuracy of splicing and regulating alternative splicing. Interacts with other spliceosomal components, via the RS domains, to form a bridge between the 5'- and 3'-splice site binding components, U1 snRNP and U2AF. Can stimulate binding of U1 snRNP to a 5'-splice site-containing pre-mRNA. Binds to purine-rich RNA sequences, either the octamer, 5'-RGAAGAAC-3' (r=A or G) or the decamers, AGGACAGAGC/AGGACGAAGC. Binds preferentially to the 5'-CGAGGCG-3' motif in vitro. Three copies of the octamer constitute a powerful splicing enhancer in vitro, the ASF/SF2 splicing enhancer (ASE) which can specifically activate ASE-dependent splicing. Isoform ASF-2 and isoform ASF-3 act as splicing repressors. May function as export adapter involved in mRNA nuclear export through the TAP/NXF1 pathway.
Uniprot ID
Q07955
Ensemble ID
ENST00000258962.5
HGNC ID
HGNC:10780
ChEMBL ID
CHEMBL4295805

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
Ishikawa (Heraklio) 02 ER Deletion: p.G102VfsTer36 DBIA    Probe Info 
MFE296 SNV: p.K138N DBIA    Probe Info 
NCIH1048 SNV: p.G9D DBIA    Probe Info 
OCUM1 SNV: p.S126P DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 37 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C-Sul
 Probe Info  		6.09  LDD0066  [1]
YN-1
 Probe Info  		100.00  LDD0444  [2]
STPyne
 Probe Info  		K165(7.34); K174(5.73); K179(7.47); K193(0.97)  LDD0277  [3]
ONAyne
 Probe Info  		K174(0.00); K193(0.00); K165(0.00); K30(0.00)  LDD0273  [3]
Probe 1
 Probe Info  		Y37(90.00); Y72(27.75); Y77(5.79); Y79(54.41)  LDD3495  [4]
DBIA
 Probe Info  		C16(0.86); C148(0.91)  LDD3310  [5]
JZ128-DTB
 Probe Info  		N.A.  LDD0462  [6]
5E-2FA
 Probe Info  		N.A.  LDD2235  [7]
ATP probe
 Probe Info  		K30(0.00); K38(0.00)  LDD0199  [8]
m-APA
 Probe Info  		N.A.  LDD2233  [7]
4-Iodoacetamidophenylacetylene
 Probe Info  		C148(0.00); C16(0.00)  LDD0038  [9]
IA-alkyne
 Probe Info  		C148(0.00); C16(0.00)  LDD0032  [10]
IPIAA_H
 Probe Info  		N.A.  LDD0030  [11]
IPIAA_L
 Probe Info  		N.A.  LDD0031  [11]
Lodoacetamide azide
 Probe Info  		C148(0.00); C16(0.00)  LDD0037  [9]
BTD
 Probe Info  		N.A.  LDD0004  [12]
IPM
 Probe Info  		C148(0.00); C16(0.00)  LDD0025  [13]
JW-RF-010
 Probe Info  		C148(0.00); C16(0.00)  LDD0026  [13]
TFBX
 Probe Info  		N.A.  LDD0027  [13]
WYneN
 Probe Info  		N.A.  LDD0021  [12]
WYneO
 Probe Info  		N.A.  LDD0022  [12]
ENE
 Probe Info  		N.A.  LDD0006  [12]
NHS
 Probe Info  		K30(0.00); K165(0.00)  LDD0010  [12]
PF-06672131
 Probe Info  		N.A.  LDD0152  [14]
SF
 Probe Info  		Y112(0.00); Y189(0.00); Y37(0.00); Y72(0.00)  LDD0028  [15]
VSF
 Probe Info  		N.A.  LDD0007  [12]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [16]
Acrolein
 Probe Info  		H183(0.00); C148(0.00); C16(0.00)  LDD0217  [17]
Cinnamaldehyde
 Probe Info  		C148(0.00); C16(0.00)  LDD0220  [17]
Crotonaldehyde
 Probe Info  		C148(0.00); C16(0.00); H183(0.00)  LDD0219  [17]
Methacrolein
 Probe Info  		C148(0.00); H183(0.00); C16(0.00)  LDD0218  [17]
W1
 Probe Info  		C148(0.00); C16(0.00)  LDD0236  [18]
AOyne
 Probe Info  		6.70  LDD0443  [19]
NAIA_5
 Probe Info  		C148(0.00); C16(0.00)  LDD2223  [20]
HHS-465
 Probe Info  		N.A.  LDD2240  [21]
HHS-475
 Probe Info  		Y37(1.03)  LDD2238  [22]
HHS-482
 Probe Info  		Y37(0.86)  LDD2239  [22]
PAL-AfBPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C338
 Probe Info  		14.42  LDD2001  [23]
STS-2
 Probe Info  		N.A.  LDD0138  [24]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0548  1-(4-(Benzo[d][1,3]dioxol-5-ylmethyl)piperazin-1-yl)-2-nitroethan-1-one MDA-MB-231 C16(0.44)  LDD2142  [25]
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C16(0.60)  LDD2112  [25]
 LDCM0502  1-(Cyanoacetyl)piperidine MDA-MB-231 C16(0.46)  LDD2095  [25]
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C16(0.95)  LDD2130  [25]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C16(0.73); C148(0.97)  LDD2117  [25]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C16(1.21)  LDD2152  [25]
 LDCM0510  3-(4-(Hydroxydiphenylmethyl)piperidin-1-yl)-3-oxopropanenitrile MDA-MB-231 C16(1.05)  LDD2103  [25]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C16(0.53)  LDD2132  [25]
 LDCM0538  4-(Cyanoacetyl)morpholine MDA-MB-231 C16(0.80)  LDD2131  [25]
 LDCM0214  AC1 HEK-293T C148(0.89); C16(0.88)  LDD1507  [26]
 LDCM0215  AC10 HEK-293T C148(0.93); C16(0.94)  LDD1508  [26]
 LDCM0226  AC11 HEK-293T C148(1.02); C16(1.03)  LDD1509  [26]
 LDCM0237  AC12 HEK-293T C16(1.14)  LDD1510  [26]
 LDCM0259  AC14 HEK-293T C148(0.94); C16(0.94)  LDD1512  [26]
 LDCM0270  AC15 HEK-293T C148(1.02); C16(1.02)  LDD1513  [26]
 LDCM0276  AC17 HEK-293T C148(0.93); C16(0.84)  LDD1515  [26]
 LDCM0277  AC18 HEK-293T C148(0.93); C16(1.02)  LDD1516  [26]
 LDCM0278  AC19 HEK-293T C148(0.76); C16(0.82)  LDD1517  [26]
 LDCM0279  AC2 HEK-293T C148(0.96); C16(0.98)  LDD1518  [26]
 LDCM0280  AC20 HEK-293T C16(0.96)  LDD1519  [26]
 LDCM0281  AC21 HEK-293T C148(0.93); C16(0.89)  LDD1520  [26]
 LDCM0282  AC22 HEK-293T C148(0.89); C16(0.98)  LDD1521  [26]
 LDCM0283  AC23 HEK-293T C148(1.02); C16(0.92)  LDD1522  [26]
 LDCM0284  AC24 HEK-293T C148(1.00); C16(0.98)  LDD1523  [26]
 LDCM0285  AC25 HEK-293T C148(0.94); C16(0.89)  LDD1524  [26]
 LDCM0286  AC26 HEK-293T C148(0.94); C16(1.06)  LDD1525  [26]
 LDCM0287  AC27 HEK-293T C148(0.94); C16(1.00)  LDD1526  [26]
 LDCM0288  AC28 HEK-293T C16(1.08)  LDD1527  [26]
 LDCM0289  AC29 HEK-293T C148(0.97); C16(1.02)  LDD1528  [26]
 LDCM0290  AC3 HEK-293T C148(1.09); C16(0.96)  LDD1529  [26]
 LDCM0291  AC30 HEK-293T C148(0.95); C16(1.08)  LDD1530  [26]
 LDCM0292  AC31 HEK-293T C148(0.95); C16(1.04)  LDD1531  [26]
 LDCM0293  AC32 HEK-293T C148(0.97); C16(0.99)  LDD1532  [26]
 LDCM0294  AC33 HEK-293T C148(0.82); C16(0.87)  LDD1533  [26]
 LDCM0295  AC34 HEK-293T C148(0.94); C16(1.00)  LDD1534  [26]
 LDCM0296  AC35 HEK-293T C148(1.00); C16(0.97)  LDD1535  [26]
 LDCM0297  AC36 HEK-293T C16(0.89)  LDD1536  [26]
 LDCM0298  AC37 HEK-293T C148(1.06); C16(1.07)  LDD1537  [26]
 LDCM0299  AC38 HEK-293T C148(1.03); C16(0.93)  LDD1538  [26]
 LDCM0300  AC39 HEK-293T C148(1.02); C16(0.91)  LDD1539  [26]
 LDCM0301  AC4 HEK-293T C16(0.97)  LDD1540  [26]
 LDCM0302  AC40 HEK-293T C148(0.97); C16(0.90)  LDD1541  [26]
 LDCM0303  AC41 HEK-293T C148(0.95); C16(0.91)  LDD1542  [26]
 LDCM0304  AC42 HEK-293T C148(0.91); C16(0.89)  LDD1543  [26]
 LDCM0305  AC43 HEK-293T C148(0.90); C16(0.94)  LDD1544  [26]
 LDCM0306  AC44 HEK-293T C16(0.95)  LDD1545  [26]
 LDCM0307  AC45 HEK-293T C148(0.97); C16(0.93)  LDD1546  [26]
 LDCM0308  AC46 HEK-293T C148(0.92); C16(0.87)  LDD1547  [26]
 LDCM0309  AC47 HEK-293T C148(1.00); C16(1.06)  LDD1548  [26]
 LDCM0310  AC48 HEK-293T C148(1.11); C16(0.90)  LDD1549  [26]
 LDCM0311  AC49 HEK-293T C148(0.88); C16(0.84)  LDD1550  [26]
 LDCM0312  AC5 HEK-293T C148(0.93); C16(1.02)  LDD1551  [26]
 LDCM0313  AC50 HEK-293T C148(0.95); C16(0.99)  LDD1552  [26]
 LDCM0314  AC51 HEK-293T C148(1.05); C16(0.94)  LDD1553  [26]
 LDCM0315  AC52 HEK-293T C16(0.96)  LDD1554  [26]
 LDCM0316  AC53 HEK-293T C148(0.98); C16(0.93)  LDD1555  [26]
 LDCM0317  AC54 HEK-293T C148(0.90); C16(0.90)  LDD1556  [26]
 LDCM0318  AC55 HEK-293T C148(0.92); C16(0.95)  LDD1557  [26]
 LDCM0319  AC56 HEK-293T C148(0.98); C16(0.90)  LDD1558  [26]
 LDCM0320  AC57 HEK-293T C148(0.86); C16(0.81)  LDD1559  [26]
 LDCM0321  AC58 HEK-293T C148(0.90); C16(0.94)  LDD1560  [26]
 LDCM0322  AC59 HEK-293T C148(0.96); C16(0.97)  LDD1561  [26]
 LDCM0323  AC6 HEK-293T C148(0.89); C16(0.88)  LDD1562  [26]
 LDCM0324  AC60 HEK-293T C16(0.83)  LDD1563  [26]
 LDCM0325  AC61 HEK-293T C148(0.94); C16(0.88)  LDD1564  [26]
 LDCM0326  AC62 HEK-293T C148(0.89); C16(0.92)  LDD1565  [26]
 LDCM0327  AC63 HEK-293T C148(0.97); C16(0.93)  LDD1566  [26]
 LDCM0328  AC64 HEK-293T C148(1.04); C16(0.89)  LDD1567  [26]
 LDCM0334  AC7 HEK-293T C148(1.00); C16(1.05)  LDD1568  [26]
 LDCM0345  AC8 HEK-293T C148(1.07); C16(1.01)  LDD1569  [26]
 LDCM0545  Acetamide MDA-MB-231 C16(0.35)  LDD2138  [25]
 LDCM0520  AKOS000195272 MDA-MB-231 C16(0.78)  LDD2113  [25]
 LDCM0248  AKOS034007472 HEK-293T C148(1.03); C16(0.91)  LDD1511  [26]
 LDCM0356  AKOS034007680 HEK-293T C148(0.92); C16(0.93)  LDD1570  [26]
 LDCM0275  AKOS034007705 HEK-293T C148(1.02); C16(0.95)  LDD1514  [26]
 LDCM0020  ARS-1620 HCC44 C16(1.45); C148(1.04)  LDD2171  [27]
 LDCM0498  BS-3668 MDA-MB-231 C16(0.80)  LDD2091  [25]
 LDCM0108  Chloroacetamide HeLa C148(0.00); H183(0.00); C16(0.00)  LDD0222  [17]
 LDCM0367  CL1 HEK-293T C148(0.89); C16(0.98)  LDD1571  [26]
 LDCM0368  CL10 HEK-293T C148(0.82); C16(0.65)  LDD1572  [26]
 LDCM0369  CL100 HEK-293T C148(1.01); C16(0.96)  LDD1573  [26]
 LDCM0370  CL101 HEK-293T C148(0.97); C16(1.01)  LDD1574  [26]
 LDCM0371  CL102 HEK-293T C148(0.81); C16(0.85)  LDD1575  [26]
 LDCM0372  CL103 HEK-293T C148(0.98); C16(1.07)  LDD1576  [26]
 LDCM0373  CL104 HEK-293T C148(0.97); C16(0.96)  LDD1577  [26]
 LDCM0374  CL105 HEK-293T C148(0.94); C16(1.01)  LDD1578  [26]
 LDCM0375  CL106 HEK-293T C148(0.75); C16(0.89)  LDD1579  [26]
 LDCM0376  CL107 HEK-293T C148(1.00); C16(1.04)  LDD1580  [26]
 LDCM0377  CL108 HEK-293T C148(0.92); C16(0.89)  LDD1581  [26]
 LDCM0378  CL109 HEK-293T C148(0.98); C16(0.97)  LDD1582  [26]
 LDCM0379  CL11 HEK-293T C148(0.90); C16(0.81)  LDD1583  [26]
 LDCM0380  CL110 HEK-293T C148(0.69); C16(0.83)  LDD1584  [26]
 LDCM0381  CL111 HEK-293T C148(0.95); C16(0.99)  LDD1585  [26]
 LDCM0382  CL112 HEK-293T C148(0.92); C16(0.92)  LDD1586  [26]
 LDCM0383  CL113 HEK-293T C148(0.99); C16(1.04)  LDD1587  [26]
 LDCM0384  CL114 HEK-293T C148(0.70); C16(0.85)  LDD1588  [26]
 LDCM0385  CL115 HEK-293T C148(0.98); C16(1.06)  LDD1589  [26]
 LDCM0386  CL116 HEK-293T C148(0.97); C16(0.94)  LDD1590  [26]
 LDCM0387  CL117 HEK-293T C148(0.92); C16(1.00)  LDD1591  [26]
 LDCM0388  CL118 HEK-293T C148(0.81); C16(0.91)  LDD1592  [26]
 LDCM0389  CL119 HEK-293T C148(0.90); C16(1.04)  LDD1593  [26]
 LDCM0390  CL12 HEK-293T C148(0.96); C16(0.78)  LDD1594  [26]
 LDCM0391  CL120 HEK-293T C148(1.03); C16(0.85)  LDD1595  [26]
 LDCM0392  CL121 HEK-293T C148(0.93); C16(0.96)  LDD1596  [26]
 LDCM0393  CL122 HEK-293T C148(0.80); C16(0.91)  LDD1597  [26]
 LDCM0394  CL123 HEK-293T C148(0.83); C16(0.89)  LDD1598  [26]
 LDCM0395  CL124 HEK-293T C148(0.87); C16(0.88)  LDD1599  [26]
 LDCM0396  CL125 HEK-293T C148(0.92); C16(0.91)  LDD1600  [26]
 LDCM0397  CL126 HEK-293T C148(0.78); C16(0.86)  LDD1601  [26]
 LDCM0398  CL127 HEK-293T C148(0.87); C16(0.95)  LDD1602  [26]
 LDCM0399  CL128 HEK-293T C148(0.90); C16(0.95)  LDD1603  [26]
 LDCM0400  CL13 HEK-293T C148(0.97); C16(1.05)  LDD1604  [26]
 LDCM0401  CL14 HEK-293T C148(0.89); C16(0.96)  LDD1605  [26]
 LDCM0402  CL15 HEK-293T C148(0.81); C16(0.91)  LDD1606  [26]
 LDCM0403  CL16 HEK-293T C148(1.10); C16(0.93)  LDD1607  [26]
 LDCM0404  CL17 HEK-293T C148(0.76); C16(0.70)  LDD1608  [26]
 LDCM0405  CL18 HEK-293T C148(1.05); C16(0.90)  LDD1609  [26]
 LDCM0406  CL19 HEK-293T C148(0.91); C16(0.93)  LDD1610  [26]
 LDCM0407  CL2 HEK-293T C148(0.90); C16(0.91)  LDD1611  [26]
 LDCM0408  CL20 HEK-293T C16(1.09)  LDD1612  [26]
 LDCM0409  CL21 HEK-293T C148(0.89); C16(0.71)  LDD1613  [26]
 LDCM0410  CL22 HEK-293T C148(1.04); C16(0.86)  LDD1614  [26]
 LDCM0411  CL23 HEK-293T C148(0.95); C16(0.94)  LDD1615  [26]
 LDCM0412  CL24 HEK-293T C148(0.93); C16(0.84)  LDD1616  [26]
 LDCM0413  CL25 HEK-293T C148(0.96); C16(1.00)  LDD1617  [26]
 LDCM0414  CL26 HEK-293T C148(0.85); C16(0.99)  LDD1618  [26]
 LDCM0415  CL27 HEK-293T C148(1.03); C16(1.04)  LDD1619  [26]
 LDCM0416  CL28 HEK-293T C148(1.06); C16(1.11)  LDD1620  [26]
 LDCM0417  CL29 HEK-293T C148(1.00); C16(1.07)  LDD1621  [26]
 LDCM0418  CL3 HEK-293T C148(0.94); C16(1.04)  LDD1622  [26]
 LDCM0419  CL30 HEK-293T C148(1.12); C16(1.05)  LDD1623  [26]
 LDCM0420  CL31 HEK-293T C148(0.95); C16(0.97)  LDD1624  [26]
 LDCM0421  CL32 HEK-293T C16(0.98)  LDD1625  [26]
 LDCM0422  CL33 HEK-293T C148(0.85); C16(0.79)  LDD1626  [26]
 LDCM0423  CL34 HEK-293T C148(1.00); C16(0.97)  LDD1627  [26]
 LDCM0424  CL35 HEK-293T C148(1.08); C16(0.91)  LDD1628  [26]
 LDCM0425  CL36 HEK-293T C148(0.99); C16(0.91)  LDD1629  [26]
 LDCM0426  CL37 HEK-293T C148(1.05); C16(1.03)  LDD1630  [26]
 LDCM0428  CL39 HEK-293T C148(0.97); C16(0.96)  LDD1632  [26]
 LDCM0429  CL4 HEK-293T C148(0.99); C16(0.92)  LDD1633  [26]
 LDCM0430  CL40 HEK-293T C148(1.04); C16(0.98)  LDD1634  [26]
 LDCM0431  CL41 HEK-293T C148(0.92); C16(0.92)  LDD1635  [26]
 LDCM0432  CL42 HEK-293T C148(1.08); C16(1.06)  LDD1636  [26]
 LDCM0433  CL43 HEK-293T C148(1.17); C16(1.03)  LDD1637  [26]
 LDCM0434  CL44 HEK-293T C16(0.92)  LDD1638  [26]
 LDCM0435  CL45 HEK-293T C148(0.90); C16(0.82)  LDD1639  [26]
 LDCM0436  CL46 HEK-293T C148(1.04); C16(0.91)  LDD1640  [26]
 LDCM0437  CL47 HEK-293T C148(0.98); C16(0.99)  LDD1641  [26]
 LDCM0438  CL48 HEK-293T C148(1.04); C16(0.93)  LDD1642  [26]
 LDCM0439  CL49 HEK-293T C148(0.98); C16(1.13)  LDD1643  [26]
 LDCM0440  CL5 HEK-293T C148(0.91); C16(0.83)  LDD1644  [26]
 LDCM0441  CL50 HEK-293T C148(0.79); C16(0.97)  LDD1645  [26]
 LDCM0443  CL52 HEK-293T C148(0.99); C16(0.96)  LDD1646  [26]
 LDCM0444  CL53 HEK-293T C148(0.85); C16(0.78)  LDD1647  [26]
 LDCM0445  CL54 HEK-293T C148(0.86); C16(0.82)  LDD1648  [26]
 LDCM0446  CL55 HEK-293T C148(0.97); C16(1.01)  LDD1649  [26]
 LDCM0447  CL56 HEK-293T C16(0.91)  LDD1650  [26]
 LDCM0448  CL57 HEK-293T C148(0.86); C16(0.75)  LDD1651  [26]
 LDCM0449  CL58 HEK-293T C148(0.91); C16(0.79)  LDD1652  [26]
 LDCM0450  CL59 HEK-293T C148(1.00); C16(0.89)  LDD1653  [26]
 LDCM0451  CL6 HEK-293T C148(0.89); C16(0.80)  LDD1654  [26]
 LDCM0452  CL60 HEK-293T C148(0.96); C16(0.88)  LDD1655  [26]
 LDCM0453  CL61 HEK-293T C148(1.07); C16(1.13)  LDD1656  [26]
 LDCM0454  CL62 HEK-293T C148(0.93); C16(0.95)  LDD1657  [26]
 LDCM0455  CL63 HEK-293T C148(1.00); C16(1.16)  LDD1658  [26]
 LDCM0456  CL64 HEK-293T C148(0.98); C16(0.82)  LDD1659  [26]
 LDCM0457  CL65 HEK-293T C148(0.90); C16(0.93)  LDD1660  [26]
 LDCM0458  CL66 HEK-293T C148(0.97); C16(0.96)  LDD1661  [26]
 LDCM0459  CL67 HEK-293T C148(0.95); C16(1.01)  LDD1662  [26]
 LDCM0460  CL68 HEK-293T C16(0.98)  LDD1663  [26]
 LDCM0461  CL69 HEK-293T C148(0.98); C16(0.83)  LDD1664  [26]
 LDCM0462  CL7 HEK-293T C148(0.85); C16(0.95)  LDD1665  [26]
 LDCM0463  CL70 HEK-293T C148(1.00); C16(0.91)  LDD1666  [26]
 LDCM0464  CL71 HEK-293T C148(0.95); C16(0.99)  LDD1667  [26]
 LDCM0465  CL72 HEK-293T C148(1.03); C16(0.97)  LDD1668  [26]
 LDCM0466  CL73 HEK-293T C148(0.99); C16(0.97)  LDD1669  [26]
 LDCM0467  CL74 HEK-293T C148(0.85); C16(0.89)  LDD1670  [26]
 LDCM0469  CL76 HEK-293T C148(0.93); C16(0.92)  LDD1672  [26]
 LDCM0470  CL77 HEK-293T C148(0.79); C16(0.79)  LDD1673  [26]
 LDCM0471  CL78 HEK-293T C148(1.03); C16(1.03)  LDD1674  [26]
 LDCM0472  CL79 HEK-293T C148(1.00); C16(0.98)  LDD1675  [26]
 LDCM0473  CL8 HEK-293T C16(0.63)  LDD1676  [26]
 LDCM0474  CL80 HEK-293T C16(1.05)  LDD1677  [26]
 LDCM0475  CL81 HEK-293T C148(1.02); C16(0.89)  LDD1678  [26]
 LDCM0476  CL82 HEK-293T C148(1.00); C16(0.91)  LDD1679  [26]
 LDCM0477  CL83 HEK-293T C148(0.97); C16(0.91)  LDD1680  [26]
 LDCM0478  CL84 HEK-293T C148(0.95); C16(0.85)  LDD1681  [26]
 LDCM0479  CL85 HEK-293T C148(0.95); C16(1.08)  LDD1682  [26]
 LDCM0480  CL86 HEK-293T C148(0.77); C16(0.93)  LDD1683  [26]
 LDCM0481  CL87 HEK-293T C148(0.96); C16(0.95)  LDD1684  [26]
 LDCM0482  CL88 HEK-293T C148(0.97); C16(0.95)  LDD1685  [26]
 LDCM0483  CL89 HEK-293T C148(0.89); C16(0.94)  LDD1686  [26]
 LDCM0484  CL9 HEK-293T C148(0.94); C16(0.85)  LDD1687  [26]
 LDCM0485  CL90 HEK-293T C148(0.77); C16(0.71)  LDD1688  [26]
 LDCM0486  CL91 HEK-293T C148(1.16); C16(1.03)  LDD1689  [26]
 LDCM0487  CL92 HEK-293T C16(0.96)  LDD1690  [26]
 LDCM0488  CL93 HEK-293T C148(0.92); C16(0.82)  LDD1691  [26]
 LDCM0489  CL94 HEK-293T C148(0.95); C16(0.87)  LDD1692  [26]
 LDCM0490  CL95 HEK-293T C148(0.77); C16(0.67)  LDD1693  [26]
 LDCM0491  CL96 HEK-293T C148(0.89); C16(0.81)  LDD1694  [26]
 LDCM0492  CL97 HEK-293T C148(0.90); C16(1.00)  LDD1695  [26]
 LDCM0493  CL98 HEK-293T C148(0.78); C16(0.97)  LDD1696  [26]
 LDCM0494  CL99 HEK-293T C148(0.89); C16(1.02)  LDD1697  [26]
 LDCM0495  E2913 HEK-293T C148(0.99); C16(1.10)  LDD1698  [26]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C148(0.99)  LDD1702  [25]
 LDCM0625  F8 Ramos C16(0.82); C148(0.69)  LDD2187  [28]
 LDCM0572  Fragment10 Ramos C16(0.56); C148(0.99)  LDD2189  [28]
 LDCM0573  Fragment11 Ramos C16(2.62); C148(0.30)  LDD2190  [28]
 LDCM0574  Fragment12 Ramos C16(0.67); C148(0.99)  LDD2191  [28]
 LDCM0575  Fragment13 Ramos C16(1.06); C148(0.80)  LDD2192  [28]
 LDCM0576  Fragment14 Ramos C16(1.01); C148(0.63)  LDD2193  [28]
 LDCM0579  Fragment20 Ramos C16(0.56); C148(0.71)  LDD2194  [28]
 LDCM0580  Fragment21 Ramos C16(1.07); C148(0.75)  LDD2195  [28]
 LDCM0582  Fragment23 Ramos C16(1.26); C148(1.56)  LDD2196  [28]
 LDCM0578  Fragment27 Ramos C16(1.17); C148(0.90)  LDD2197  [28]
 LDCM0586  Fragment28 Ramos C16(0.61); C148(0.68)  LDD2198  [28]
 LDCM0588  Fragment30 Ramos C16(1.40); C148(0.91)  LDD2199  [28]
 LDCM0589  Fragment31 Ramos C16(1.22); C148(0.93)  LDD2200  [28]
 LDCM0590  Fragment32 Ramos C16(0.69); C148(0.55)  LDD2201  [28]
 LDCM0468  Fragment33 HEK-293T C148(0.95); C16(1.05)  LDD1671  [26]
 LDCM0596  Fragment38 Ramos C16(1.09); C148(0.69)  LDD2203  [28]
 LDCM0566  Fragment4 Ramos C16(0.60); C148(0.79)  LDD2184  [28]
 LDCM0427  Fragment51 HEK-293T C148(0.83); C16(1.01)  LDD1631  [26]
 LDCM0610  Fragment52 Ramos C16(1.63); C148(0.76)  LDD2204  [28]
 LDCM0614  Fragment56 Ramos C16(1.52); C148(0.78)  LDD2205  [28]
 LDCM0569  Fragment7 Ramos C16(0.55); C148(0.61)  LDD2186  [28]
 LDCM0571  Fragment9 Ramos C16(0.52); C148(0.73)  LDD2188  [28]
 LDCM0107  IAA HeLa C148(0.00); H183(0.00); C16(0.00)  LDD0221  [17]
 LDCM0179  JZ128 PC-3 N.A.  LDD0462  [6]
 LDCM0022  KB02 HEK-293T C16(0.99); C148(1.16)  LDD1492  [26]
 LDCM0023  KB03 HEK-293T C16(0.97); C148(1.12)  LDD1497  [26]
 LDCM0024  KB05 COLO792 C16(0.86); C148(0.91)  LDD3310  [5]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C16(1.28)  LDD2102  [25]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C16(0.75)  LDD2121  [25]
 LDCM0109  NEM HeLa N.A.  LDD0223  [17]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C16(0.62); C148(0.94)  LDD2089  [25]
 LDCM0497  Nucleophilic fragment 11b MDA-MB-231 C16(1.05)  LDD2090  [25]
 LDCM0499  Nucleophilic fragment 12b MDA-MB-231 C16(1.14)  LDD2092  [25]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C16(0.69)  LDD2093  [25]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C16(2.17)  LDD2094  [25]
 LDCM0503  Nucleophilic fragment 14b MDA-MB-231 C16(0.30)  LDD2096  [25]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C16(0.77)  LDD2097  [25]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C16(0.90); C148(1.50)  LDD2099  [25]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C16(0.40)  LDD2100  [25]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C16(0.76)  LDD2101  [25]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C16(0.43)  LDD2104  [25]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C16(1.79)  LDD2105  [25]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C16(0.46)  LDD2106  [25]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C16(1.10); C148(1.52)  LDD2107  [25]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C16(0.64)  LDD2108  [25]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C16(0.50); C148(0.64)  LDD2109  [25]
 LDCM0517  Nucleophilic fragment 21b MDA-MB-231 C16(0.55)  LDD2110  [25]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C16(0.75)  LDD2111  [25]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C16(0.45)  LDD2115  [25]
 LDCM0523  Nucleophilic fragment 24b MDA-MB-231 C16(0.72)  LDD2116  [25]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C16(0.65)  LDD2118  [25]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C16(1.60)  LDD2119  [25]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C16(0.87)  LDD2120  [25]
 LDCM0529  Nucleophilic fragment 27b MDA-MB-231 C16(0.37)  LDD2122  [25]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C16(0.54); C148(0.80)  LDD2123  [25]
 LDCM0531  Nucleophilic fragment 28b MDA-MB-231 C16(0.49)  LDD2124  [25]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C16(0.57); C148(0.86)  LDD2125  [25]
 LDCM0533  Nucleophilic fragment 29b MDA-MB-231 C16(0.44)  LDD2126  [25]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C16(0.61)  LDD2127  [25]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C16(0.92)  LDD2128  [25]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C16(1.18); C148(1.96)  LDD2129  [25]
 LDCM0540  Nucleophilic fragment 35 MDA-MB-231 C16(0.46)  LDD2133  [25]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C16(0.41)  LDD2134  [25]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C16(1.60); C148(2.02)  LDD2135  [25]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C16(0.80); C148(0.90)  LDD2136  [25]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C16(0.78); C148(1.07)  LDD2137  [25]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C16(1.80)  LDD1700  [25]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C16(0.49); C148(0.95)  LDD2140  [25]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C16(0.63)  LDD2141  [25]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C16(0.99)  LDD2143  [25]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C16(2.61)  LDD2144  [25]
 LDCM0551  Nucleophilic fragment 5b MDA-MB-231 C16(0.35)  LDD2145  [25]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C16(0.70)  LDD2146  [25]
 LDCM0553  Nucleophilic fragment 6b MDA-MB-231 C16(3.59)  LDD2147  [25]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C16(0.40)  LDD2148  [25]
 LDCM0555  Nucleophilic fragment 7b MDA-MB-231 C16(0.43)  LDD2149  [25]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C16(0.47)  LDD2150  [25]
 LDCM0557  Nucleophilic fragment 8b MDA-MB-231 C16(0.40)  LDD2151  [25]
 LDCM0131  RA190 MM1.R C148(1.07)  LDD0304  [29]
 LDCM0021  THZ1 HCT 116 C16(1.45); C148(1.04)  LDD2173  [27]

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
SRSF protein kinase 1 (SRPK1) CMGC Ser/Thr protein kinase family Q96SB4
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Nuclear RNA export factor 1 (NXF1) NXF family Q9UBU9
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Nuclear transcription factor Y subunit alpha (NFYA) NFYA/HAP2 subunit family P23511
Other
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Ribosomal RNA processing protein 1 homolog B (RRP1B) RRP1 family Q14684
Splicing factor U2AF 35 kDa subunit (U2AF1) Splicing factor SR family Q01081
Transformer-2 protein homolog beta (TRA2B) Splicing factor SR family P62995
TNF receptor-associated factor 5 (TRAF5) TNF receptor-associated factor family O00463
Corepressor interacting with RBPJ 1 (CIR1) . Q86X95
U1 small nuclear ribonucleoprotein 70 kDa (SNRNP70) . P08621

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Copper . DB09130

References

1 Low-Toxicity Sulfonium-Based Probes for Cysteine-Specific Profiling in Live Cells. Anal Chem. 2022 Mar 15;94(10):4366-4372. doi: 10.1021/acs.analchem.1c05129. Epub 2022 Mar 4.
2 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
3 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
4 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 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
6 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.
7 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
8 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.
9 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
10 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
11 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
12 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
13 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
14 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
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 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
17 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.
18 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.
19 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.
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 Global profiling identifies a stress-responsive tyrosine site on EDC3 regulating biomolecular condensate formation. Cell Chem Biol. 2022 Dec 15;29(12):1709-1720.e7. doi: 10.1016/j.chembiol.2022.11.008. Epub 2022 Dec 6.
Mass spectrometry data entry: PXD038010
22 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.
23 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
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 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
26 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
27 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.
28 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
29 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.