General Information of Target

Target ID LDTP06384
Target Name Ribosomal protein S6 kinase alpha-1 (RPS6KA1)
Gene Name RPS6KA1
Gene ID 6195
Synonyms
MAPKAPK1A; RSK1; Ribosomal protein S6 kinase alpha-1; S6K-alpha-1; EC 2.7.11.1; 90 kDa ribosomal protein S6 kinase 1; p90-RSK 1; p90RSK1; p90S6K; MAP kinase-activated protein kinase 1a; MAPK-activated protein kinase 1a; MAPKAP kinase 1a; MAPKAPK-1a; Ribosomal S6 kinase 1; RSK-1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MPLAQLKEPWPLMELVPLDPENGQTSGEEAGLQPSKDEGVLKEISITHHVKAGSEKADPS
HFELLKVLGQGSFGKVFLVRKVTRPDSGHLYAMKVLKKATLKVRDRVRTKMERDILADVN
HPFVVKLHYAFQTEGKLYLILDFLRGGDLFTRLSKEVMFTEEDVKFYLAELALGLDHLHS
LGIIYRDLKPENILLDEEGHIKLTDFGLSKEAIDHEKKAYSFCGTVEYMAPEVVNRQGHS
HSADWWSYGVLMFEMLTGSLPFQGKDRKETMTLILKAKLGMPQFLSTEAQSLLRALFKRN
PANRLGSGPDGAEEIKRHVFYSTIDWNKLYRREIKPPFKPAVAQPDDTFYFDTEFTSRTP
KDSPGIPPSAGAHQLFRGFSFVATGLMEDDGKPRAPQAPLHSVVQQLHGKNLVFSDGYVV
KETIGVGSYSECKRCVHKATNMEYAVKVIDKSKRDPSEEIEILLRYGQHPNIITLKDVYD
DGKHVYLVTELMRGGELLDKILRQKFFSEREASFVLHTIGKTVEYLHSQGVVHRDLKPSN
ILYVDESGNPECLRICDFGFAKQLRAENGLLMTPCYTANFVAPEVLKRQGYDEGCDIWSL
GILLYTMLAGYTPFANGPSDTPEEILTRIGSGKFTLSGGNWNTVSETAKDLVSKMLHVDP
HQRLTAKQVLQHPWVTQKDKLPQSQLSHQDLQLVKGAMAATYSALNSSKPTPQLKPIESS
ILAQRRVRKLPSTTL
Target Type
Patented-recorded
Target Bioclass
Enzyme
Family
Protein kinase superfamily, AGC Ser/Thr protein kinase family, S6 kinase subfamily
Subcellular location
Nucleus
Function
Serine/threonine-protein kinase that acts downstream of ERK (MAPK1/ERK2 and MAPK3/ERK1) signaling and mediates mitogenic and stress-induced activation of the transcription factors CREB1, ETV1/ER81 and NR4A1/NUR77, regulates translation through RPS6 and EIF4B phosphorylation, and mediates cellular proliferation, survival, and differentiation by modulating mTOR signaling and repressing pro-apoptotic function of BAD and DAPK1. In fibroblast, is required for EGF-stimulated phosphorylation of CREB1, which results in the subsequent transcriptional activation of several immediate-early genes. In response to mitogenic stimulation (EGF and PMA), phosphorylates and activates NR4A1/NUR77 and ETV1/ER81 transcription factors and the cofactor CREBBP. Upon insulin-derived signal, acts indirectly on the transcription regulation of several genes by phosphorylating GSK3B at 'Ser-9' and inhibiting its activity. Phosphorylates RPS6 in response to serum or EGF via an mTOR-independent mechanism and promotes translation initiation by facilitating assembly of the pre-initiation complex. In response to insulin, phosphorylates EIF4B, enhancing EIF4B affinity for the EIF3 complex and stimulating cap-dependent translation. Is involved in the mTOR nutrient-sensing pathway by directly phosphorylating TSC2 at 'Ser-1798', which potently inhibits TSC2 ability to suppress mTOR signaling, and mediates phosphorylation of RPTOR, which regulates mTORC1 activity and may promote rapamycin-sensitive signaling independently of the PI3K/AKT pathway. Also involved in feedback regulation of mTORC1 and mTORC2 by phosphorylating DEPTOR. Mediates cell survival by phosphorylating the pro-apoptotic proteins BAD and DAPK1 and suppressing their pro-apoptotic function. Promotes the survival of hepatic stellate cells by phosphorylating CEBPB in response to the hepatotoxin carbon tetrachloride (CCl4). Mediates induction of hepatocyte prolifration by TGFA through phosphorylation of CEBPB. Is involved in cell cycle regulation by phosphorylating the CDK inhibitor CDKN1B, which promotes CDKN1B association with 14-3-3 proteins and prevents its translocation to the nucleus and inhibition of G1 progression. Phosphorylates EPHA2 at 'Ser-897', the RPS6KA-EPHA2 signaling pathway controls cell migration. In response to mTORC1 activation, phosphorylates EIF4B at 'Ser-406' and 'Ser-422' which stimulates bicarbonate cotransporter SLC4A7 mRNA translation, increasing SLC4A7 protein abundance and function.; (Microbial infection) Promotes the late transcription and translation of viral lytic genes during Kaposi's sarcoma-associated herpesvirus/HHV-8 infection, when constitutively activated.
TTD ID
T83202
Uniprot ID
Q15418
DrugMap ID
TTIXKA4
Ensemble ID
ENST00000374168.7
HGNC ID
HGNC:10430
ChEMBL ID
CHEMBL2553

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CAL33 Substitution: p.A169V DBIA    Probe Info 
CAL78 SNV: p.L329I .
CORL23 SNV: p.A52P .
G402 SNV: p.Q397L .
HEC1 SNV: p.R588H DBIA    Probe Info 
HT SNV: p.R726Ter .
HT115 SNV: p.D187N .
JHH7 SNV: p.S72A .
MCC26 SNV: p.S457L .
MDAMB453 SNV: p.Q671Ter .
SF295 SNV: p.T440N .
SNU1 SNV: p.R588C DBIA    Probe Info 
SW1783 SNV: p.R434H .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 31 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
A-EBA
 Probe Info 
50.00  LDD0214  [1]
m-APA
 Probe Info 
15.00  LDD0402  [2]
N1
 Probe Info 
100.00  LDD0242  [3]
TH211
 Probe Info 
Y321(20.00); Y576(20.00)  LDD0257  [4]
STPyne
 Probe Info 
K66(6.77)  LDD0277  [5]
ONAyne
 Probe Info 
K210(6.50)  LDD0275  [5]
JZ128-DTB
 Probe Info 
N.A.  LDD0462  [6]
Sulforaphane-probe2
 Probe Info 
1.78  LDD0160  [7]
AHL-Pu-1
 Probe Info 
C552(2.40)  LDD0168  [8]
DBIA
 Probe Info 
C432(9.11)  LDD0209  [9]
HHS-475
 Probe Info 
Y429(1.23)  LDD0264  [10]
AMP probe
 Probe Info 
K94(0.00); K97(0.00)  LDD0200  [11]
ATP probe
 Probe Info 
K537(0.00); K210(0.00); K217(0.00); K453(0.00)  LDD0199  [11]
4-Iodoacetamidophenylacetylene
 Probe Info 
C575(0.00); C223(0.00); C552(0.00); C556(0.00)  LDD0038  [12]
IA-alkyne
 Probe Info 
N.A.  LDD0032  [13]
IPIAA_L
 Probe Info 
N.A.  LDD0031  [14]
Lodoacetamide azide
 Probe Info 
C575(0.00); C223(0.00); C552(0.00); C556(0.00)  LDD0037  [12]
ATP probe
 Probe Info 
K537(0.00); K210(0.00)  LDD0035  [15]
JW-RF-010
 Probe Info 
C435(0.00); C575(0.00)  LDD0026  [16]
NAIA_4
 Probe Info 
C575(0.00); C223(0.00); C432(0.00)  LDD2226  [17]
TFBX
 Probe Info 
C575(0.00); C432(0.00)  LDD0027  [16]
WYneN
 Probe Info 
C575(0.00); C432(0.00); C556(0.00)  LDD0021  [18]
1d-yne
 Probe Info 
N.A.  LDD0356  [19]
Compound 10
 Probe Info 
N.A.  LDD2216  [20]
Compound 11
 Probe Info 
N.A.  LDD2213  [20]
IPM
 Probe Info 
C432(0.00); C556(0.00); C223(0.00)  LDD0005  [18]
VSF
 Probe Info 
C575(0.00); C432(0.00)  LDD0007  [18]
1c-yne
 Probe Info 
N.A.  LDD0228  [19]
Acrolein
 Probe Info 
C223(0.00); C575(0.00)  LDD0217  [21]
AOyne
 Probe Info 
9.40  LDD0443  [22]
NAIA_5
 Probe Info 
N.A.  LDD2223  [17]
PAL-AfBPP Probe
Click To Hide/Show 39 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
PARPYnD
 Probe Info 
1.61  LDD0374  [23]
C040
 Probe Info 
7.21  LDD1740  [24]
C051
 Probe Info 
5.28  LDD1749  [24]
C106
 Probe Info 
26.72  LDD1793  [24]
C112
 Probe Info 
22.32  LDD1799  [24]
C131
 Probe Info 
7.26  LDD1813  [24]
C138
 Probe Info 
7.84  LDD1820  [24]
C145
 Probe Info 
10.70  LDD1827  [24]
C158
 Probe Info 
9.13  LDD1838  [24]
C174
 Probe Info 
8.17  LDD1854  [24]
C178
 Probe Info 
15.24  LDD1857  [24]
C196
 Probe Info 
10.41  LDD1872  [24]
C218
 Probe Info 
22.63  LDD1892  [24]
C225
 Probe Info 
5.74  LDD1898  [24]
C226
 Probe Info 
6.19  LDD1899  [24]
C235
 Probe Info 
17.75  LDD1908  [24]
C238
 Probe Info 
25.81  LDD1911  [24]
C288
 Probe Info 
6.92  LDD1958  [24]
C289
 Probe Info 
26.54  LDD1959  [24]
C348
 Probe Info 
10.78  LDD2009  [24]
C361
 Probe Info 
23.43  LDD2022  [24]
C382
 Probe Info 
10.20  LDD2041  [24]
C391
 Probe Info 
16.80  LDD2050  [24]
C407
 Probe Info 
12.64  LDD2064  [24]
C418
 Probe Info 
24.42  LDD2073  [24]
C424
 Probe Info 
10.85  LDD2079  [24]
C429
 Probe Info 
11.55  LDD2084  [24]
C433
 Probe Info 
10.06  LDD2088  [24]
FFF probe12
 Probe Info 
12.29  LDD0473  [25]
FFF probe13
 Probe Info 
20.00  LDD0475  [25]
FFF probe14
 Probe Info 
20.00  LDD0477  [25]
FFF probe3
 Probe Info 
20.00  LDD0464  [25]
FFF probe6
 Probe Info 
13.91  LDD0467  [25]
FFF probe9
 Probe Info 
14.16  LDD0470  [25]
JN0003
 Probe Info 
14.88  LDD0469  [25]
Kambe_26
 Probe Info 
8.04  LDD0127  [26]
Diazir
 Probe Info 
N.A.  LDD0011  [18]
OEA-DA
 Probe Info 
17.93  LDD0046  [27]
Probe 12
 Probe Info 
N.A.  LDD0420  [28]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0025  4SU-RNA HEK-293T C552(2.40)  LDD0168  [8]
 LDCM0026  4SU-RNA+native RNA HEK-293T C556(2.29); C223(2.79)  LDD0169  [8]
 LDCM0214  AC1 HEK-293T C432(0.94); C552(1.16)  LDD1507  [29]
 LDCM0215  AC10 HEK-293T C432(1.01); C552(1.16)  LDD1508  [29]
 LDCM0226  AC11 HEK-293T C432(1.04); C552(1.36)  LDD1509  [29]
 LDCM0237  AC12 HEK-293T C432(1.01); C552(1.13)  LDD1510  [29]
 LDCM0259  AC14 HEK-293T C432(1.00); C552(1.43)  LDD1512  [29]
 LDCM0270  AC15 HEK-293T C432(1.05); C552(1.13)  LDD1513  [29]
 LDCM0276  AC17 HEK-293T C432(1.06); C552(1.19)  LDD1515  [29]
 LDCM0277  AC18 HEK-293T C432(1.04); C552(0.86)  LDD1516  [29]
 LDCM0278  AC19 HEK-293T C432(0.93); C552(1.07)  LDD1517  [29]
 LDCM0279  AC2 HEK-293T C432(0.93); C552(1.15)  LDD1518  [29]
 LDCM0280  AC20 HEK-293T C432(0.98); C552(1.40)  LDD1519  [29]
 LDCM0281  AC21 HEK-293T C432(0.99); C552(1.01)  LDD1520  [29]
 LDCM0282  AC22 HEK-293T C432(0.99); C552(1.10)  LDD1521  [29]
 LDCM0283  AC23 HEK-293T C432(1.00); C552(1.22)  LDD1522  [29]
 LDCM0284  AC24 HEK-293T C432(0.99); C552(1.04)  LDD1523  [29]
 LDCM0285  AC25 HEK-293T C432(0.94); C552(1.57)  LDD1524  [29]
 LDCM0286  AC26 HEK-293T C432(1.01); C552(1.16)  LDD1525  [29]
 LDCM0287  AC27 HEK-293T C432(0.98); C552(1.15)  LDD1526  [29]
 LDCM0288  AC28 HEK-293T C432(0.94); C552(1.21)  LDD1527  [29]
 LDCM0289  AC29 HEK-293T C432(1.04); C552(1.05)  LDD1528  [29]
 LDCM0290  AC3 HEK-293T C432(1.06); C552(1.29)  LDD1529  [29]
 LDCM0291  AC30 HEK-293T C432(0.95); C552(1.27)  LDD1530  [29]
 LDCM0292  AC31 HEK-293T C432(1.01); C552(1.20)  LDD1531  [29]
 LDCM0293  AC32 HEK-293T C432(1.00); C552(1.13)  LDD1532  [29]
 LDCM0294  AC33 HEK-293T C432(0.93); C552(1.19)  LDD1533  [29]
 LDCM0295  AC34 HEK-293T C432(0.98); C552(1.13)  LDD1534  [29]
 LDCM0296  AC35 HEK-293T C432(1.04); C552(1.82)  LDD1535  [29]
 LDCM0297  AC36 HEK-293T C432(0.93); C552(1.29)  LDD1536  [29]
 LDCM0298  AC37 HEK-293T C432(1.02); C552(1.48)  LDD1537  [29]
 LDCM0299  AC38 HEK-293T C432(0.91); C552(1.31)  LDD1538  [29]
 LDCM0300  AC39 HEK-293T C432(1.03); C552(1.05)  LDD1539  [29]
 LDCM0301  AC4 HEK-293T C432(0.99); C552(1.04)  LDD1540  [29]
 LDCM0302  AC40 HEK-293T C432(0.94); C552(1.04)  LDD1541  [29]
 LDCM0303  AC41 HEK-293T C432(0.96); C552(1.25)  LDD1542  [29]
 LDCM0304  AC42 HEK-293T C432(1.03); C552(1.42)  LDD1543  [29]
 LDCM0305  AC43 HEK-293T C432(1.03); C552(1.46)  LDD1544  [29]
 LDCM0306  AC44 HEK-293T C432(1.03); C552(1.51)  LDD1545  [29]
 LDCM0307  AC45 HEK-293T C432(0.95); C552(1.11)  LDD1546  [29]
 LDCM0308  AC46 HEK-293T C432(0.97); C552(1.34)  LDD1547  [29]
 LDCM0309  AC47 HEK-293T C432(1.03); C552(1.14)  LDD1548  [29]
 LDCM0310  AC48 HEK-293T C432(0.91); C552(0.98)  LDD1549  [29]
 LDCM0311  AC49 HEK-293T C432(0.95); C552(1.28)  LDD1550  [29]
 LDCM0312  AC5 HEK-293T C432(1.00); C552(1.23)  LDD1551  [29]
 LDCM0313  AC50 HEK-293T C432(1.00); C552(1.05)  LDD1552  [29]
 LDCM0314  AC51 HEK-293T C432(1.02); C552(1.44)  LDD1553  [29]
 LDCM0315  AC52 HEK-293T C432(1.00); C552(1.16)  LDD1554  [29]
 LDCM0316  AC53 HEK-293T C432(1.00); C552(1.00)  LDD1555  [29]
 LDCM0317  AC54 HEK-293T C432(0.93); C552(1.01)  LDD1556  [29]
 LDCM0318  AC55 HEK-293T C432(0.99); C552(1.15)  LDD1557  [29]
 LDCM0319  AC56 HEK-293T C432(0.93); C552(1.03)  LDD1558  [29]
 LDCM0320  AC57 HEK-293T C432(1.00); C552(1.62)  LDD1559  [29]
 LDCM0321  AC58 HEK-293T C432(1.01); C552(1.41)  LDD1560  [29]
 LDCM0322  AC59 HEK-293T C432(0.96); C552(1.87)  LDD1561  [29]
 LDCM0323  AC6 HEK-293T C432(0.93); C552(1.31)  LDD1562  [29]
 LDCM0324  AC60 HEK-293T C432(0.98); C552(1.20)  LDD1563  [29]
 LDCM0325  AC61 HEK-293T C432(0.99); C552(1.17)  LDD1564  [29]
 LDCM0326  AC62 HEK-293T C432(0.91); C552(1.14)  LDD1565  [29]
 LDCM0327  AC63 HEK-293T C432(1.02); C552(1.19)  LDD1566  [29]
 LDCM0328  AC64 HEK-293T C432(0.91); C552(0.98)  LDD1567  [29]
 LDCM0334  AC7 HEK-293T C432(1.00); C552(1.29)  LDD1568  [29]
 LDCM0345  AC8 HEK-293T C432(1.00); C552(1.07)  LDD1569  [29]
 LDCM0248  AKOS034007472 HEK-293T C432(1.03); C552(1.07)  LDD1511  [29]
 LDCM0356  AKOS034007680 HEK-293T C432(0.94); C552(1.40)  LDD1570  [29]
 LDCM0275  AKOS034007705 HEK-293T C432(0.93); C552(1.06)  LDD1514  [29]
 LDCM0156  Aniline NCI-H1299 11.59  LDD0403  [2]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [21]
 LDCM0632  CL-Sc Hep-G2 C575(1.29); C575(0.96); C432(0.88)  LDD2227  [17]
 LDCM0367  CL1 HEK-293T C432(0.92); C552(1.18)  LDD1571  [29]
 LDCM0368  CL10 HEK-293T C432(14.06); C552(0.61)  LDD1572  [29]
 LDCM0369  CL100 HEK-293T C432(0.93)  LDD1573  [29]
 LDCM0370  CL101 HEK-293T C432(1.62); C552(1.11)  LDD1574  [29]
 LDCM0371  CL102 HEK-293T C432(1.29); C552(1.10)  LDD1575  [29]
 LDCM0372  CL103 HEK-293T C432(0.91); C552(1.42)  LDD1576  [29]
 LDCM0373  CL104 HEK-293T C432(1.08)  LDD1577  [29]
 LDCM0374  CL105 HEK-293T C432(1.04); C552(0.99)  LDD1578  [29]
 LDCM0375  CL106 HEK-293T C432(1.34); C552(1.15)  LDD1579  [29]
 LDCM0376  CL107 HEK-293T C432(0.97); C552(1.32)  LDD1580  [29]
 LDCM0377  CL108 HEK-293T C432(1.21)  LDD1581  [29]
 LDCM0378  CL109 HEK-293T C432(1.30); C552(1.08)  LDD1582  [29]
 LDCM0379  CL11 HEK-293T C432(3.33); C552(0.54)  LDD1583  [29]
 LDCM0380  CL110 HEK-293T C432(1.36); C552(1.05)  LDD1584  [29]
 LDCM0381  CL111 HEK-293T C432(1.14); C552(1.12)  LDD1585  [29]
 LDCM0382  CL112 HEK-293T C432(5.40)  LDD1586  [29]
 LDCM0383  CL113 HEK-293T C432(1.03); C552(1.18)  LDD1587  [29]
 LDCM0384  CL114 HEK-293T C432(2.45); C552(0.92)  LDD1588  [29]
 LDCM0385  CL115 HEK-293T C432(1.13); C552(1.38)  LDD1589  [29]
 LDCM0386  CL116 HEK-293T C432(0.85)  LDD1590  [29]
 LDCM0387  CL117 HEK-293T C432(1.08); C552(1.06)  LDD1591  [29]
 LDCM0388  CL118 HEK-293T C432(0.97); C552(1.17)  LDD1592  [29]
 LDCM0389  CL119 HEK-293T C432(0.98); C552(1.04)  LDD1593  [29]
 LDCM0390  CL12 HEK-293T C432(1.40); C552(0.69)  LDD1594  [29]
 LDCM0391  CL120 HEK-293T C432(0.93)  LDD1595  [29]
 LDCM0392  CL121 HEK-293T C432(1.28); C552(1.16)  LDD1596  [29]
 LDCM0393  CL122 HEK-293T C432(0.98); C552(1.12)  LDD1597  [29]
 LDCM0394  CL123 HEK-293T C432(1.10); C552(1.00)  LDD1598  [29]
 LDCM0395  CL124 HEK-293T C432(1.10)  LDD1599  [29]
 LDCM0396  CL125 HEK-293T C432(1.08); C552(1.14)  LDD1600  [29]
 LDCM0397  CL126 HEK-293T C432(0.96); C552(1.21)  LDD1601  [29]
 LDCM0398  CL127 HEK-293T C432(0.93); C552(1.11)  LDD1602  [29]
 LDCM0399  CL128 HEK-293T C432(0.92)  LDD1603  [29]
 LDCM0400  CL13 HEK-293T C432(5.25); C552(1.11)  LDD1604  [29]
 LDCM0401  CL14 HEK-293T C432(1.77); C552(1.18)  LDD1605  [29]
 LDCM0402  CL15 HEK-293T C432(0.95); C552(0.98)  LDD1606  [29]
 LDCM0403  CL16 HEK-293T C432(1.10)  LDD1607  [29]
 LDCM0404  CL17 HEK-293T C432(1.16); C552(0.98)  LDD1608  [29]
 LDCM0405  CL18 HEK-293T C432(1.08); C552(0.92)  LDD1609  [29]
 LDCM0406  CL19 HEK-293T C432(1.17); C552(1.06)  LDD1610  [29]
 LDCM0407  CL2 HEK-293T C432(1.08); C552(1.14)  LDD1611  [29]
 LDCM0408  CL20 HEK-293T C432(1.33); C552(0.81)  LDD1612  [29]
 LDCM0409  CL21 HEK-293T C432(8.35); C552(0.54)  LDD1613  [29]
 LDCM0410  CL22 HEK-293T C432(1.70); C552(0.79)  LDD1614  [29]
 LDCM0411  CL23 HEK-293T C432(1.56); C552(0.61)  LDD1615  [29]
 LDCM0412  CL24 HEK-293T C432(1.48); C552(0.61)  LDD1616  [29]
 LDCM0413  CL25 HEK-293T C432(0.97); C552(1.04)  LDD1617  [29]
 LDCM0414  CL26 HEK-293T C432(1.05); C552(1.05)  LDD1618  [29]
 LDCM0415  CL27 HEK-293T C432(1.04); C552(1.25)  LDD1619  [29]
 LDCM0416  CL28 HEK-293T C432(1.28)  LDD1620  [29]
 LDCM0417  CL29 HEK-293T C432(1.02); C552(0.94)  LDD1621  [29]
 LDCM0418  CL3 HEK-293T C432(0.96); C552(1.28)  LDD1622  [29]
 LDCM0419  CL30 HEK-293T C432(1.07); C552(0.77)  LDD1623  [29]
 LDCM0420  CL31 HEK-293T C432(1.22); C552(0.85)  LDD1624  [29]
 LDCM0421  CL32 HEK-293T C432(1.22); C552(0.74)  LDD1625  [29]
 LDCM0422  CL33 HEK-293T C432(1.17); C552(0.56)  LDD1626  [29]
 LDCM0423  CL34 HEK-293T C432(1.52); C552(0.72)  LDD1627  [29]
 LDCM0424  CL35 HEK-293T C432(1.48); C552(0.53)  LDD1628  [29]
 LDCM0425  CL36 HEK-293T C432(1.57); C552(0.56)  LDD1629  [29]
 LDCM0426  CL37 HEK-293T C432(0.84); C552(1.00)  LDD1630  [29]
 LDCM0428  CL39 HEK-293T C432(2.25); C552(1.43)  LDD1632  [29]
 LDCM0429  CL4 HEK-293T C432(0.93)  LDD1633  [29]
 LDCM0430  CL40 HEK-293T C432(1.08)  LDD1634  [29]
 LDCM0431  CL41 HEK-293T C432(1.93); C552(1.02)  LDD1635  [29]
 LDCM0432  CL42 HEK-293T C432(1.33); C552(0.61)  LDD1636  [29]
 LDCM0433  CL43 HEK-293T C432(1.42); C552(0.82)  LDD1637  [29]
 LDCM0434  CL44 HEK-293T C432(1.22); C552(0.70)  LDD1638  [29]
 LDCM0435  CL45 HEK-293T C432(5.07); C552(0.55)  LDD1639  [29]
 LDCM0436  CL46 HEK-293T C432(1.47); C552(0.77)  LDD1640  [29]
 LDCM0437  CL47 HEK-293T C432(1.81); C552(0.56)  LDD1641  [29]
 LDCM0438  CL48 HEK-293T C432(1.31); C552(0.55)  LDD1642  [29]
 LDCM0439  CL49 HEK-293T C432(0.92); C552(1.16)  LDD1643  [29]
 LDCM0440  CL5 HEK-293T C432(0.98); C552(0.94)  LDD1644  [29]
 LDCM0441  CL50 HEK-293T C432(2.06); C552(1.17)  LDD1645  [29]
 LDCM0443  CL52 HEK-293T C432(0.86)  LDD1646  [29]
 LDCM0444  CL53 HEK-293T C432(1.26); C552(1.04)  LDD1647  [29]
 LDCM0445  CL54 HEK-293T C432(1.15); C552(0.85)  LDD1648  [29]
 LDCM0446  CL55 HEK-293T C432(1.16); C552(0.96)  LDD1649  [29]
 LDCM0447  CL56 HEK-293T C432(1.47); C552(0.75)  LDD1650  [29]
 LDCM0448  CL57 HEK-293T C432(2.66); C552(0.57)  LDD1651  [29]
 LDCM0449  CL58 HEK-293T C432(1.31); C552(0.70)  LDD1652  [29]
 LDCM0450  CL59 HEK-293T C432(1.63); C552(0.52)  LDD1653  [29]
 LDCM0451  CL6 HEK-293T C432(1.19); C552(0.89)  LDD1654  [29]
 LDCM0452  CL60 HEK-293T C432(1.69); C552(0.66)  LDD1655  [29]
 LDCM0453  CL61 HEK-293T C432(0.95); C552(1.12)  LDD1656  [29]
 LDCM0454  CL62 HEK-293T C432(2.12); C552(1.35)  LDD1657  [29]
 LDCM0455  CL63 HEK-293T C432(2.70); C552(1.18)  LDD1658  [29]
 LDCM0456  CL64 HEK-293T C432(1.17)  LDD1659  [29]
 LDCM0457  CL65 HEK-293T C432(0.95); C552(1.16)  LDD1660  [29]
 LDCM0458  CL66 HEK-293T C432(1.51); C552(0.70)  LDD1661  [29]
 LDCM0459  CL67 HEK-293T C432(1.11); C552(1.00)  LDD1662  [29]
 LDCM0460  CL68 HEK-293T C432(1.15); C552(0.80)  LDD1663  [29]
 LDCM0461  CL69 HEK-293T C432(1.48); C552(0.60)  LDD1664  [29]
 LDCM0462  CL7 HEK-293T C432(1.51); C552(0.86)  LDD1665  [29]
 LDCM0463  CL70 HEK-293T C432(1.50); C552(0.86)  LDD1666  [29]
 LDCM0464  CL71 HEK-293T C432(2.57); C552(0.63)  LDD1667  [29]
 LDCM0465  CL72 HEK-293T C432(1.24); C552(0.72)  LDD1668  [29]
 LDCM0466  CL73 HEK-293T C432(0.93); C552(1.28)  LDD1669  [29]
 LDCM0467  CL74 HEK-293T C432(1.57); C552(1.27)  LDD1670  [29]
 LDCM0469  CL76 HEK-293T C432(0.95)  LDD1672  [29]
 LDCM0470  CL77 HEK-293T C432(1.60); C552(1.08)  LDD1673  [29]
 LDCM0471  CL78 HEK-293T C432(1.07); C552(0.95)  LDD1674  [29]
 LDCM0472  CL79 HEK-293T C432(1.04); C552(0.97)  LDD1675  [29]
 LDCM0473  CL8 HEK-293T C432(12.37); C552(0.61)  LDD1676  [29]
 LDCM0474  CL80 HEK-293T C432(1.17); C552(0.82)  LDD1677  [29]
 LDCM0475  CL81 HEK-293T C432(1.43); C552(0.68)  LDD1678  [29]
 LDCM0476  CL82 HEK-293T C432(1.20); C552(0.81)  LDD1679  [29]
 LDCM0477  CL83 HEK-293T C432(1.22); C552(0.62)  LDD1680  [29]
 LDCM0478  CL84 HEK-293T C432(1.13); C552(0.66)  LDD1681  [29]
 LDCM0479  CL85 HEK-293T C432(0.92); C552(1.35)  LDD1682  [29]
 LDCM0480  CL86 HEK-293T C432(1.25); C552(1.48)  LDD1683  [29]
 LDCM0481  CL87 HEK-293T C432(1.26); C552(1.50)  LDD1684  [29]
 LDCM0482  CL88 HEK-293T C432(0.91)  LDD1685  [29]
 LDCM0483  CL89 HEK-293T C432(0.92); C552(1.29)  LDD1686  [29]
 LDCM0484  CL9 HEK-293T C432(1.49); C552(0.65)  LDD1687  [29]
 LDCM0485  CL90 HEK-293T C432(1.40); C552(0.91)  LDD1688  [29]
 LDCM0486  CL91 HEK-293T C432(1.14); C552(1.01)  LDD1689  [29]
 LDCM0487  CL92 HEK-293T C432(1.12); C552(0.79)  LDD1690  [29]
 LDCM0488  CL93 HEK-293T C432(1.22); C552(0.79)  LDD1691  [29]
 LDCM0489  CL94 HEK-293T C432(1.86); C552(0.83)  LDD1692  [29]
 LDCM0490  CL95 HEK-293T C432(16.16); C552(0.59)  LDD1693  [29]
 LDCM0491  CL96 HEK-293T C432(1.80); C552(0.84)  LDD1694  [29]
 LDCM0492  CL97 HEK-293T C432(1.38); C552(1.10)  LDD1695  [29]
 LDCM0493  CL98 HEK-293T C432(1.44); C552(1.36)  LDD1696  [29]
 LDCM0494  CL99 HEK-293T C432(3.52); C552(1.16)  LDD1697  [29]
 LDCM0189  Compound 16 HEK-293T 15.15  LDD0492  [25]
 LDCM0182  Compound 18 HEK-293T 7.52  LDD0501  [25]
 LDCM0191  Compound 21 HEK-293T 11.11  LDD0493  [25]
 LDCM0190  Compound 34 HEK-293T 16.81  LDD0497  [25]
 LDCM0192  Compound 35 HEK-293T 7.66  LDD0491  [25]
 LDCM0193  Compound 36 HEK-293T 6.60  LDD0494  [25]
 LDCM0194  Compound 37 HEK-293T 14.81  LDD0498  [25]
 LDCM0195  Compound 38 HEK-293T 7.60  LDD0499  [25]
 LDCM0196  Compound 39 HEK-293T 10.99  LDD0496  [25]
 LDCM0197  Compound 40 HEK-293T 9.01  LDD0495  [25]
 LDCM0181  Compound 41 HEK-293T 13.16  LDD0502  [25]
 LDCM0165  Compound 9 HL-60 N.A.  LDD0420  [28]
 LDCM0495  E2913 HEK-293T C432(1.12); C552(1.07)  LDD1698  [29]
 LDCM0625  F8 Ramos C575(1.03); C432(1.02); C223(0.64)  LDD2187  [30]
 LDCM0572  Fragment10 Ramos C575(1.74); C432(2.15)  LDD2189  [30]
 LDCM0573  Fragment11 Ramos C575(0.34)  LDD2190  [30]
 LDCM0574  Fragment12 Ramos C575(1.10); C432(1.18)  LDD2191  [30]
 LDCM0575  Fragment13 Ramos C575(1.04); C432(1.05)  LDD2192  [30]
 LDCM0576  Fragment14 Ramos C575(0.75); C432(0.36); C223(1.25)  LDD2193  [30]
 LDCM0579  Fragment20 Ramos C575(0.92); C432(0.66)  LDD2194  [30]
 LDCM0580  Fragment21 Ramos C575(0.95); C432(0.90)  LDD2195  [30]
 LDCM0582  Fragment23 Ramos C575(0.92); C432(1.44)  LDD2196  [30]
 LDCM0578  Fragment27 Ramos C575(0.93); C432(0.91)  LDD2197  [30]
 LDCM0586  Fragment28 Ramos C575(1.14); C432(0.76)  LDD2198  [30]
 LDCM0588  Fragment30 Ramos C575(1.20); C432(2.69)  LDD2199  [30]
 LDCM0589  Fragment31 Ramos C575(0.86); C432(0.92)  LDD2200  [30]
 LDCM0590  Fragment32 Ramos C575(2.32); C432(3.46)  LDD2201  [30]
 LDCM0468  Fragment33 HEK-293T C432(0.97); C552(1.38)  LDD1671  [29]
 LDCM0596  Fragment38 Ramos C575(0.61); C432(0.92)  LDD2203  [30]
 LDCM0566  Fragment4 Ramos C575(0.91); C432(0.85)  LDD2184  [30]
 LDCM0427  Fragment51 HEK-293T C432(3.51); C552(0.90)  LDD1631  [29]
 LDCM0610  Fragment52 Ramos C575(1.06); C432(1.04)  LDD2204  [30]
 LDCM0614  Fragment56 Ramos C575(1.03); C432(1.03)  LDD2205  [30]
 LDCM0569  Fragment7 Ramos C575(1.21); C432(1.45); C223(0.93)  LDD2186  [30]
 LDCM0571  Fragment9 Ramos C575(1.39); C432(2.31)  LDD2188  [30]
 LDCM0116  HHS-0101 DM93 Y429(1.23)  LDD0264  [10]
 LDCM0117  HHS-0201 DM93 Y429(1.23)  LDD0265  [10]
 LDCM0118  HHS-0301 DM93 Y429(0.80)  LDD0266  [10]
 LDCM0119  HHS-0401 DM93 Y429(4.22)  LDD0267  [10]
 LDCM0120  HHS-0701 DM93 Y429(0.61)  LDD0268  [10]
 LDCM0179  JZ128 PC-3 N.A.  LDD0462  [6]
 LDCM0073  Kambe_cp3 PC-3 8.04  LDD0127  [26]
 LDCM0022  KB02 HEK-293T C432(0.59); C575(1.06)  LDD1492  [29]
 LDCM0023  KB03 Jurkat C432(9.11)  LDD0209  [9]
 LDCM0024  KB05 MEL167 C441(2.16)  LDD3316  [31]
 LDCM0109  NEM HeLa H200(0.00); H657(0.00); H533(0.00); H527(0.00)  LDD0223  [21]
 LDCM0628  OTUB2-COV-1 HEK-293T C575(0.87)  LDD2207  [32]
 LDCM0170  Structure8 Ramos 12.81  LDD0433  [33]
 LDCM0003  Sulforaphane MDA-MB-231 1.78  LDD0160  [7]

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
Mitogen-activated protein kinase 1 (MAPK1) CMGC Ser/Thr protein kinase family P28482
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Heat shock protein HSP 90-beta (HSP90AB1) Heat shock protein 90 family P08238
Protein S100-B (S100B) S-100 family P04271
Other
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
A-kinase anchor protein 8 (AKAP8) AKAP95 family O43823
Cyclin-dependent kinase inhibitor 1B (CDKN1B) CDI family P46527
Vasodilator-stimulated phosphoprotein (VASP) Ena/VASP family P50552
Protein scribble homolog (SCRIB) LAP (LRR and PDZ) protein family Q14160

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
Fostamatinib Small molecular drug DB12010
Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bi-d1870 Small molecular drug D02VBF
Investigative
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Gsk-1838705a Small molecular drug D06PJW
Pmid19364658c33 Small molecular drug D01YWE
Purvalanol A Small molecular drug DB04751
Patented
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1,6-diazanaphthalenes And Pyrido[2,3-d] Pyrimidine Derivative 1 Small molecular drug D00RPW
1,6-diazanaphthalenes And Pyrido[2,3-d] Pyrimidine Derivative 2 Small molecular drug D0I3YK
Heterocyclic Derivative 26 Small molecular drug D08QMJ
Pyrrolo[2,3-d]Pyrimidine Derivative 1 Small molecular drug D0R0DW
Pyrrolo[2,3-d]Pyrimidine Derivative 2 Small molecular drug D0T2CA

References

1 2-Ethynylbenzaldehyde-Based, Lysine-Targeting Irreversible Covalent Inhibitors for Protein Kinases and Nonkinases. J Am Chem Soc. 2023 Feb 12. doi: 10.1021/jacs.2c11595. Online ahead of print.
Mass spectrometry data entry: PXD037665
2 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.
3 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
4 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.
5 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
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 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
8 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
9 Covalent Inhibition by a Natural Product-Inspired Latent Electrophile. J Am Chem Soc. 2023 May 24;145(20):11097-11109. doi: 10.1021/jacs.3c00598. Epub 2023 May 15.
10 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.
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 Comparison of Quantitative Mass Spectrometry Platforms for Monitoring Kinase ATP Probe Uptake in Lung Cancer. J Proteome Res. 2018 Jan 5;17(1):63-75. doi: 10.1021/acs.jproteome.7b00329. Epub 2017 Nov 22.
Mass spectrometry data entry: PXD006095 , PXD006096
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 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
18 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
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 Multiplexed CuAAC Suzuki-Miyaura Labeling for Tandem Activity-Based Chemoproteomic Profiling. Anal Chem. 2021 Feb 2;93(4):2610-2618. doi: 10.1021/acs.analchem.0c04726. Epub 2021 Jan 20.
Mass spectrometry data entry: PXD022279
21 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.
22 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.
23 Structure-Guided Design and In-Cell Target Profiling of a Cell-Active Target Engagement Probe for PARP Inhibitors. ACS Chem Biol. 2020 Feb 21;15(2):325-333. doi: 10.1021/acschembio.9b00963. Epub 2020 Feb 10.
24 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
25 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.
26 Mapping the protein interaction landscape for fully functionalized small-molecule probes in human cells. J Am Chem Soc. 2014 Jul 30;136(30):10777-82. doi: 10.1021/ja505517t. Epub 2014 Jul 21.
27 Mapping Protein Targets of Bioactive Small Molecules Using Lipid-Based Chemical Proteomics. ACS Chem Biol. 2017 Oct 20;12(10):2671-2681. doi: 10.1021/acschembio.7b00581. Epub 2017 Sep 20.
Mass spectrometry data entry: PXD007570
28 A Photoaffinity Displacement Assay and Probes to Study the Cyclin-Dependent Kinase Family. Angew Chem Int Ed Engl. 2019 Nov 25;58(48):17322-17327. doi: 10.1002/anie.201906321. Epub 2019 Oct 31.
29 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
30 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
31 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
32 Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22.
33 2-Sulfonylpyridines as Tunable, Cysteine-Reactive Electrophiles. J Am Chem Soc. 2020 May 13;142(19):8972-8979. doi: 10.1021/jacs.0c02721. Epub 2020 Apr 29.