Details of the Target

General Information of Target

Target ID LDTP02002
Target Name RAF proto-oncogene serine/threonine-protein kinase (RAF1)
Gene Name RAF1
Gene ID 5894
Synonyms
RAF; RAF proto-oncogene serine/threonine-protein kinase; EC 2.7.11.1; Proto-oncogene c-RAF; cRaf; Raf-1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MEHIQGAWKTISNGFGFKDAVFDGSSCISPTIVQQFGYQRRASDDGKLTDPSKTSNTIRV
FLPNKQRTVVNVRNGMSLHDCLMKALKVRGLQPECCAVFRLLHEHKGKKARLDWNTDAAS
LIGEELQVDFLDHVPLTTHNFARKTFLKLAFCDICQKFLLNGFRCQTCGYKFHEHCSTKV
PTMCVDWSNIRQLLLFPNSTIGDSGVPALPSLTMRRMRESVSRMPVSSQHRYSTPHAFTF
NTSSPSSEGSLSQRQRSTSTPNVHMVSTTLPVDSRMIEDAIRSHSESASPSALSSSPNNL
SPTGWSQPKTPVPAQRERAPVSGTQEKNKIRPRGQRDSSYYWEIEASEVMLSTRIGSGSF
GTVYKGKWHGDVAVKILKVVDPTPEQFQAFRNEVAVLRKTRHVNILLFMGYMTKDNLAIV
TQWCEGSSLYKHLHVQETKFQMFQLIDIARQTAQGMDYLHAKNIIHRDMKSNNIFLHEGL
TVKIGDFGLATVKSRWSGSQQVEQPTGSVLWMAPEVIRMQDNNPFSFQSDVYSYGIVLYE
LMTGELPYSHINNRDQIIFMVGRGYASPDLSKLYKNCPKAMKRLVADCVKKVKEERPLFP
QILSSIELLQHSLPKINRSASEPSLHRAAHTEDINACTLTTSPRLPVF
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, TKL Ser/Thr protein kinase family, RAF subfamily
Subcellular location
Cytoplasm
Function
Serine/threonine-protein kinase that acts as a regulatory link between the membrane-associated Ras GTPases and the MAPK/ERK cascade, and this critical regulatory link functions as a switch determining cell fate decisions including proliferation, differentiation, apoptosis, survival and oncogenic transformation. RAF1 activation initiates a mitogen-activated protein kinase (MAPK) cascade that comprises a sequential phosphorylation of the dual-specific MAPK kinases (MAP2K1/MEK1 and MAP2K2/MEK2) and the extracellular signal-regulated kinases (MAPK3/ERK1 and MAPK1/ERK2). The phosphorylated form of RAF1 (on residues Ser-338 and Ser-339, by PAK1) phosphorylates BAD/Bcl2-antagonist of cell death at 'Ser-75'. Phosphorylates adenylyl cyclases: ADCY2, ADCY5 and ADCY6, resulting in their activation. Phosphorylates PPP1R12A resulting in inhibition of the phosphatase activity. Phosphorylates TNNT2/cardiac muscle troponin T. Can promote NF-kB activation and inhibit signal transducers involved in motility (ROCK2), apoptosis (MAP3K5/ASK1 and STK3/MST2), proliferation and angiogenesis (RB1). Can protect cells from apoptosis also by translocating to the mitochondria where it binds BCL2 and displaces BAD/Bcl2-antagonist of cell death. Regulates Rho signaling and migration, and is required for normal wound healing. Plays a role in the oncogenic transformation of epithelial cells via repression of the TJ protein, occludin (OCLN) by inducing the up-regulation of a transcriptional repressor SNAI2/SLUG, which induces down-regulation of OCLN. Restricts caspase activation in response to selected stimuli, notably Fas stimulation, pathogen-mediated macrophage apoptosis, and erythroid differentiation.
TTD ID
T23673
Uniprot ID
P04049
DrugMap ID
TTB18GJ
Ensemble ID
ENST00000251849.9
HGNC ID
HGNC:9829
ChEMBL ID
CHEMBL1906

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
COLO792 Substitution: p.S352L DBIA    Probe Info 
EFO27 SNV: p.V403A .
HDMYZ SNV: p.E343G DBIA    Probe Info 
OCIAML2 Insertion: p.A118CfsTer9 DBIA    Probe Info 
RL952 SNV: p.R73Ter .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 24 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
Jackson_1
 Probe Info  		20.00  LDD0122  [2]
STPyne
 Probe Info  		K106(7.33); K493(10.00)  LDD0277  [3]
BTD
 Probe Info  		C637(1.07)  LDD2098  [4]
DA-P3
 Probe Info  		4.68  LDD0183  [5]
AHL-Pu-1
 Probe Info  		C637(5.35); C27(3.68)  LDD0169  [6]
EA-probe
 Probe Info  		N.A.  LDD0440  [7]
DBIA
 Probe Info  		C588(10.36)  LDD0209  [8]
HHS-475
 Probe Info  		Y565(1.00)  LDD0265  [9]
ATP probe
 Probe Info  		K470(0.00); K493(0.00)  LDD0199  [10]
4-Iodoacetamidophenylacetylene
 Probe Info  		C637(0.00); C588(0.00); C184(0.00)  LDD0038  [11]
IA-alkyne
 Probe Info  		N.A.  LDD0162  [12]
Lodoacetamide azide
 Probe Info  		C637(0.00); C588(0.00)  LDD0037  [11]
JW-RF-010
 Probe Info  		N.A.  LDD0026  [13]
NAIA_4
 Probe Info  		C27(0.00); C637(0.00); 0.00  LDD2226  [14]
TFBX
 Probe Info  		C637(0.00); C95(0.00); C588(0.00); C96(0.00)  LDD0027  [13]
WYneN
 Probe Info  		N.A.  LDD0021  [15]
aHNE
 Probe Info  		N.A.  LDD0001  [15]
Compound 10
 Probe Info  		C637(0.00); C95(0.00)  LDD2216  [16]
Compound 11
 Probe Info  		C637(0.00); C95(0.00)  LDD2213  [16]
IPM
 Probe Info  		C637(0.00); C96(0.00); C588(0.00)  LDD0005  [15]
VSF
 Probe Info  		N.A.  LDD0007  [15]
AOyne
 Probe Info  		13.80  LDD0443  [17]
NAIA_5
 Probe Info  		C637(0.00); C176(0.00); C184(0.00)  LDD2223  [14]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C637(0.95)  LDD2152  [4]
 LDCM0025  4SU-RNA HEK-293T C637(2.97); C81(2.82)  LDD0371  [6]
 LDCM0026  4SU-RNA+native RNA HEK-293T C637(5.35); C27(3.68)  LDD0169  [6]
 LDCM0214  AC1 HEK-293T C637(1.07); C588(0.96); C81(0.94); C96(1.17)  LDD1507  [18]
 LDCM0215  AC10 HEK-293T C637(1.01); C588(0.98); C81(1.03); C152(1.22)  LDD1508  [18]
 LDCM0226  AC11 HEK-293T C637(1.07); C588(1.03); C152(1.11); C95(0.77)  LDD1509  [18]
 LDCM0237  AC12 HEK-293T C637(1.04); C588(0.98); C81(1.04); C424(1.05)  LDD1510  [18]
 LDCM0259  AC14 HEK-293T C637(0.98); C588(0.95); C27(0.98); C152(0.89)  LDD1512  [18]
 LDCM0270  AC15 HEK-293T C637(1.21); C588(1.01); C184(1.11); C152(1.05)  LDD1513  [18]
 LDCM0276  AC17 HEK-293T C637(1.10); C588(1.00); C81(1.12); C96(1.10)  LDD1515  [18]
 LDCM0277  AC18 HEK-293T C637(0.95); C588(0.93); C81(0.91); C152(1.24)  LDD1516  [18]
 LDCM0278  AC19 HEK-293T C637(1.21); C588(1.16); C152(0.93); C95(1.00)  LDD1517  [18]
 LDCM0279  AC2 HEK-293T C637(1.11); C588(1.05); C81(0.98); C152(1.00)  LDD1518  [18]
 LDCM0280  AC20 HEK-293T C637(1.06); C588(1.06); C81(1.05); C424(0.90)  LDD1519  [18]
 LDCM0281  AC21 HEK-293T C637(0.96); C81(0.94)  LDD1520  [18]
 LDCM0282  AC22 HEK-293T C637(0.98); C588(1.01); C27(0.82); C152(0.95)  LDD1521  [18]
 LDCM0283  AC23 HEK-293T C637(1.02); C588(1.00); C184(1.00); C152(0.86)  LDD1522  [18]
 LDCM0284  AC24 HEK-293T C637(0.97); C588(0.99); C27(1.09); C81(1.05)  LDD1523  [18]
 LDCM0285  AC25 HEK-293T C637(1.08); C588(1.02); C81(0.94); C96(1.13)  LDD1524  [18]
 LDCM0286  AC26 HEK-293T C637(1.07); C588(1.02); C81(1.05); C152(1.30)  LDD1525  [18]
 LDCM0287  AC27 HEK-293T C637(1.07); C588(0.96); C152(0.92); C95(0.96)  LDD1526  [18]
 LDCM0288  AC28 HEK-293T C637(1.00); C588(0.97); C81(0.95); C424(0.92)  LDD1527  [18]
 LDCM0289  AC29 HEK-293T C637(1.14); C81(1.09)  LDD1528  [18]
 LDCM0290  AC3 HEK-293T C637(0.99); C588(0.99); C152(1.15); C95(0.95)  LDD1529  [18]
 LDCM0291  AC30 HEK-293T C637(1.00); C588(0.91); C27(0.91); C152(1.11)  LDD1530  [18]
 LDCM0292  AC31 HEK-293T C637(0.99); C588(0.98); C184(0.97); C152(1.11)  LDD1531  [18]
 LDCM0293  AC32 HEK-293T C637(1.02); C588(1.06); C27(1.09); C81(1.09)  LDD1532  [18]
 LDCM0294  AC33 HEK-293T C637(1.04); C588(1.02); C81(1.11); C96(1.07)  LDD1533  [18]
 LDCM0295  AC34 HEK-293T C637(1.01); C588(1.01); C81(1.14); C152(1.01)  LDD1534  [18]
 LDCM0296  AC35 HEK-293T C637(1.01); C588(1.05); C152(1.00); C95(0.90)  LDD1535  [18]
 LDCM0297  AC36 HEK-293T C637(1.13); C588(1.05); C81(1.10); C424(1.15)  LDD1536  [18]
 LDCM0298  AC37 HEK-293T C637(1.03); C81(1.31)  LDD1537  [18]
 LDCM0299  AC38 HEK-293T C637(1.11); C588(0.99); C27(1.06); C152(0.97)  LDD1538  [18]
 LDCM0300  AC39 HEK-293T C637(1.01); C588(1.03); C184(1.03); C152(1.03)  LDD1539  [18]
 LDCM0301  AC4 HEK-293T C637(0.82); C588(0.99); C81(1.01); C424(1.05)  LDD1540  [18]
 LDCM0302  AC40 HEK-293T C637(0.95); C588(0.95); C27(1.01); C81(1.21)  LDD1541  [18]
 LDCM0303  AC41 HEK-293T C637(1.14); C588(1.01); C81(1.11); C96(1.13)  LDD1542  [18]
 LDCM0304  AC42 HEK-293T C637(1.19); C588(1.01); C81(1.05); C152(0.98)  LDD1543  [18]
 LDCM0305  AC43 HEK-293T C637(1.06); C588(1.02); C152(1.06); C95(0.80)  LDD1544  [18]
 LDCM0306  AC44 HEK-293T C637(1.09); C588(0.97); C81(1.08); C424(1.22)  LDD1545  [18]
 LDCM0307  AC45 HEK-293T C637(0.96); C81(1.09)  LDD1546  [18]
 LDCM0308  AC46 HEK-293T C637(0.97); C588(0.99); C27(0.98); C152(0.96)  LDD1547  [18]
 LDCM0309  AC47 HEK-293T C637(1.13); C588(1.04); C184(1.09); C152(0.85)  LDD1548  [18]
 LDCM0310  AC48 HEK-293T C637(0.98); C588(0.97); C27(1.00); C81(1.21)  LDD1549  [18]
 LDCM0311  AC49 HEK-293T C637(1.01); C588(0.97); C81(1.08); C96(1.03)  LDD1550  [18]
 LDCM0312  AC5 HEK-293T C637(1.03); C81(0.98)  LDD1551  [18]
 LDCM0313  AC50 HEK-293T C637(1.01); C588(0.98); C81(1.05); C152(1.05)  LDD1552  [18]
 LDCM0314  AC51 HEK-293T C637(1.09); C588(0.97); C152(1.13); C95(0.91)  LDD1553  [18]
 LDCM0315  AC52 HEK-293T C637(1.10); C588(1.03); C81(1.07); C424(1.10)  LDD1554  [18]
 LDCM0316  AC53 HEK-293T C637(1.01); C81(1.00)  LDD1555  [18]
 LDCM0317  AC54 HEK-293T C637(1.07); C588(0.94); C27(1.04); C152(0.86)  LDD1556  [18]
 LDCM0318  AC55 HEK-293T C637(1.06); C588(1.07); C184(1.01); C152(1.04)  LDD1557  [18]
 LDCM0319  AC56 HEK-293T C637(1.09); C588(1.03); C27(1.15); C81(1.16)  LDD1558  [18]
 LDCM0320  AC57 HEK-293T C637(1.05); C588(0.99); C81(1.00); C96(0.95)  LDD1559  [18]
 LDCM0321  AC58 HEK-293T C637(1.01); C588(0.97); C81(0.98); C152(1.02)  LDD1560  [18]
 LDCM0322  AC59 HEK-293T C637(1.15); C588(1.01); C152(1.00); C95(0.83)  LDD1561  [18]
 LDCM0323  AC6 HEK-293T C637(1.11); C588(0.89); C27(1.01); C152(1.04)  LDD1562  [18]
 LDCM0324  AC60 HEK-293T C637(1.04); C588(0.98); C81(1.00); C424(1.01)  LDD1563  [18]
 LDCM0325  AC61 HEK-293T C637(1.08); C81(0.98)  LDD1564  [18]
 LDCM0326  AC62 HEK-293T C637(1.09); C588(0.87); C27(1.18); C152(0.97)  LDD1565  [18]
 LDCM0327  AC63 HEK-293T C637(1.00); C588(1.02); C184(0.94); C152(1.05)  LDD1566  [18]
 LDCM0328  AC64 HEK-293T C637(1.08); C588(0.99); C27(1.28); C81(1.02)  LDD1567  [18]
 LDCM0334  AC7 HEK-293T C637(1.14); C588(1.03); C184(0.91); C152(1.15)  LDD1568  [18]
 LDCM0345  AC8 HEK-293T C637(0.90); C588(1.08); C27(0.97); C81(1.04)  LDD1569  [18]
 LDCM0248  AKOS034007472 HEK-293T C637(1.00); C81(0.97)  LDD1511  [18]
 LDCM0356  AKOS034007680 HEK-293T C637(1.10); C588(1.01); C81(1.09); C96(1.04)  LDD1570  [18]
 LDCM0275  AKOS034007705 HEK-293T C637(1.01); C588(0.95); C27(1.09); C81(1.03)  LDD1514  [18]
 LDCM0156  Aniline NCI-H1299 10.58  LDD0403  [1]
 LDCM0630  CCW28-3 231MFP C637(2.82); C27(1.19)  LDD2214  [19]
 LDCM0632  CL-Sc Hep-G2 C637(5.67)  LDD2227  [14]
 LDCM0367  CL1 HEK-293T C637(1.01); C588(0.87); C27(0.93)  LDD1571  [18]
 LDCM0368  CL10 HEK-293T C637(0.91); C588(1.07); C27(1.27); C152(1.13)  LDD1572  [18]
 LDCM0369  CL100 HEK-293T C637(1.00); C588(0.96); C81(0.98); C152(0.84)  LDD1573  [18]
 LDCM0370  CL101 HEK-293T C637(1.01); C588(0.93); C27(1.02)  LDD1574  [18]
 LDCM0371  CL102 HEK-293T C637(1.12); C588(0.93); C27(1.13); C81(0.99)  LDD1575  [18]
 LDCM0372  CL103 HEK-293T C637(1.00); C588(1.02); C152(0.94); C96(1.15)  LDD1576  [18]
 LDCM0373  CL104 HEK-293T C637(1.01); C588(0.95); C81(1.01); C152(0.78)  LDD1577  [18]
 LDCM0374  CL105 HEK-293T C637(0.94); C588(0.92); C27(0.90)  LDD1578  [18]
 LDCM0375  CL106 HEK-293T C637(0.99); C588(0.99); C27(0.88); C81(1.05)  LDD1579  [18]
 LDCM0376  CL107 HEK-293T C637(0.84); C588(0.96); C152(0.99); C96(0.82)  LDD1580  [18]
 LDCM0377  CL108 HEK-293T C637(1.00); C588(0.95); C81(0.97); C152(0.92)  LDD1581  [18]
 LDCM0378  CL109 HEK-293T C637(1.01); C588(0.92); C27(1.12)  LDD1582  [18]
 LDCM0379  CL11 HEK-293T C637(0.99); C588(1.20); C184(1.18); C152(1.23)  LDD1583  [18]
 LDCM0380  CL110 HEK-293T C637(1.00); C588(1.13); C27(1.22); C81(1.10)  LDD1584  [18]
 LDCM0381  CL111 HEK-293T C637(0.77); C588(0.92); C152(0.90); C96(1.12)  LDD1585  [18]
 LDCM0382  CL112 HEK-293T C637(0.99); C588(0.95); C81(1.00); C152(0.90)  LDD1586  [18]
 LDCM0383  CL113 HEK-293T C637(1.02); C588(0.92); C27(0.86)  LDD1587  [18]
 LDCM0384  CL114 HEK-293T C637(0.97); C588(1.05); C27(1.48); C81(1.15)  LDD1588  [18]
 LDCM0385  CL115 HEK-293T C637(0.81); C588(1.00); C152(0.97); C96(1.32)  LDD1589  [18]
 LDCM0386  CL116 HEK-293T C637(1.10); C588(1.01); C81(1.15); C152(1.01)  LDD1590  [18]
 LDCM0387  CL117 HEK-293T C637(0.97); C588(0.91); C27(0.98)  LDD1591  [18]
 LDCM0388  CL118 HEK-293T C637(1.14); C588(1.02); C27(1.11); C81(1.13)  LDD1592  [18]
 LDCM0389  CL119 HEK-293T C637(0.94); C588(1.08); C152(0.98); C96(0.95)  LDD1593  [18]
 LDCM0390  CL12 HEK-293T C637(1.08); C588(1.01); C27(1.06); C81(0.94)  LDD1594  [18]
 LDCM0391  CL120 HEK-293T C637(1.20); C588(1.00); C81(1.12); C152(0.92)  LDD1595  [18]
 LDCM0392  CL121 HEK-293T C637(1.07); C588(0.92); C27(0.94)  LDD1596  [18]
 LDCM0393  CL122 HEK-293T C637(1.09); C588(0.93); C27(1.17); C81(1.13)  LDD1597  [18]
 LDCM0394  CL123 HEK-293T C637(0.95); C588(0.99); C152(1.08); C96(1.10)  LDD1598  [18]
 LDCM0395  CL124 HEK-293T C637(1.09); C588(0.94); C81(1.11); C152(0.75)  LDD1599  [18]
 LDCM0396  CL125 HEK-293T C637(1.12); C588(0.83); C27(1.33)  LDD1600  [18]
 LDCM0397  CL126 HEK-293T C637(1.04); C588(0.98); C27(1.15); C81(0.98)  LDD1601  [18]
 LDCM0398  CL127 HEK-293T C637(0.90); C588(0.96); C152(1.05); C96(1.25)  LDD1602  [18]
 LDCM0399  CL128 HEK-293T C637(1.03); C588(0.92); C81(0.94); C152(0.86)  LDD1603  [18]
 LDCM0400  CL13 HEK-293T C637(1.01); C588(0.92); C27(1.10)  LDD1604  [18]
 LDCM0401  CL14 HEK-293T C637(1.06); C588(1.07); C27(1.42); C81(1.12)  LDD1605  [18]
 LDCM0402  CL15 HEK-293T C637(0.88); C588(1.03); C152(0.99); C96(0.80)  LDD1606  [18]
 LDCM0403  CL16 HEK-293T C637(1.09); C588(0.98); C81(0.97); C152(0.90)  LDD1607  [18]
 LDCM0404  CL17 HEK-293T C637(1.09); C588(1.04); C81(0.94); C96(1.21)  LDD1608  [18]
 LDCM0405  CL18 HEK-293T C637(1.07); C588(1.16); C81(1.01); C152(0.97)  LDD1609  [18]
 LDCM0406  CL19 HEK-293T C637(1.22); C588(1.08); C152(1.03); C95(0.91)  LDD1610  [18]
 LDCM0407  CL2 HEK-293T C637(1.05); C588(1.06); C27(1.11); C81(1.14)  LDD1611  [18]
 LDCM0408  CL20 HEK-293T C637(1.01); C588(1.14); C81(0.95); C424(1.25)  LDD1612  [18]
 LDCM0409  CL21 HEK-293T C637(0.91); C81(0.88)  LDD1613  [18]
 LDCM0410  CL22 HEK-293T C637(0.98); C588(1.13); C27(0.91); C152(1.21)  LDD1614  [18]
 LDCM0411  CL23 HEK-293T C637(0.98); C588(1.21); C184(1.16); C152(1.24)  LDD1615  [18]
 LDCM0412  CL24 HEK-293T C637(1.16); C588(1.08); C27(1.14); C81(0.88)  LDD1616  [18]
 LDCM0413  CL25 HEK-293T C637(0.91); C588(0.87); C27(1.00)  LDD1617  [18]
 LDCM0414  CL26 HEK-293T C637(1.06); C588(0.97); C27(1.10); C81(1.08)  LDD1618  [18]
 LDCM0415  CL27 HEK-293T C637(0.80); C588(0.96); C152(1.05); C96(1.17)  LDD1619  [18]
 LDCM0416  CL28 HEK-293T C637(1.04); C588(0.96); C81(0.94); C152(0.86)  LDD1620  [18]
 LDCM0417  CL29 HEK-293T C637(1.04); C588(0.94); C81(1.07); C96(1.09)  LDD1621  [18]
 LDCM0418  CL3 HEK-293T C637(0.95); C588(0.99); C152(1.06); C96(0.97)  LDD1622  [18]
 LDCM0419  CL30 HEK-293T C637(1.10); C588(1.00); C81(1.00); C152(1.10)  LDD1623  [18]
 LDCM0420  CL31 HEK-293T C637(1.10); C588(1.04); C152(0.88); C95(0.83)  LDD1624  [18]
 LDCM0421  CL32 HEK-293T C637(1.10); C588(1.07); C81(0.82); C424(1.30)  LDD1625  [18]
 LDCM0422  CL33 HEK-293T C637(0.84); C81(0.87)  LDD1626  [18]
 LDCM0423  CL34 HEK-293T C637(0.98); C588(0.97); C27(1.02); C152(1.19)  LDD1627  [18]
 LDCM0424  CL35 HEK-293T C637(0.97); C588(1.11); C184(1.08); C152(1.10)  LDD1628  [18]
 LDCM0425  CL36 HEK-293T C637(1.01); C588(0.93); C27(1.20); C81(0.88)  LDD1629  [18]
 LDCM0426  CL37 HEK-293T C637(0.93); C588(0.88); C27(0.91)  LDD1630  [18]
 LDCM0428  CL39 HEK-293T C637(0.99); C588(0.98); C152(0.99); C96(1.22)  LDD1632  [18]
 LDCM0429  CL4 HEK-293T C637(1.05); C588(0.94); C81(0.81); C152(1.10)  LDD1633  [18]
 LDCM0430  CL40 HEK-293T C637(0.98); C588(0.97); C81(0.87); C152(0.97)  LDD1634  [18]
 LDCM0431  CL41 HEK-293T C637(1.13); C588(0.99); C81(1.12); C96(1.33)  LDD1635  [18]
 LDCM0432  CL42 HEK-293T C637(0.86); C588(1.00); C81(0.89); C152(1.05)  LDD1636  [18]
 LDCM0433  CL43 HEK-293T C637(1.03); C588(1.08); C152(1.10); C95(0.87)  LDD1637  [18]
 LDCM0434  CL44 HEK-293T C637(1.18); C588(1.10); C81(0.76); C424(1.07)  LDD1638  [18]
 LDCM0435  CL45 HEK-293T C637(0.96); C81(0.93)  LDD1639  [18]
 LDCM0436  CL46 HEK-293T C637(1.03); C588(1.01); C27(0.97); C152(1.08)  LDD1640  [18]
 LDCM0437  CL47 HEK-293T C637(1.08); C588(1.18); C184(1.16); C152(1.05)  LDD1641  [18]
 LDCM0438  CL48 HEK-293T C637(1.07); C588(1.05); C27(1.22); C81(0.83)  LDD1642  [18]
 LDCM0439  CL49 HEK-293T C637(0.96); C588(0.84); C27(1.06)  LDD1643  [18]
 LDCM0440  CL5 HEK-293T C637(1.06); C588(1.00); C81(0.93); C96(1.20)  LDD1644  [18]
 LDCM0441  CL50 HEK-293T C637(1.15); C588(1.09); C27(1.14); C81(1.11)  LDD1645  [18]
 LDCM0443  CL52 HEK-293T C637(1.12); C588(0.98); C81(1.20); C152(0.96)  LDD1646  [18]
 LDCM0444  CL53 HEK-293T C637(1.10); C588(0.93); C81(0.94); C96(1.45)  LDD1647  [18]
 LDCM0445  CL54 HEK-293T C637(1.05); C588(1.05); C81(0.97); C152(1.23)  LDD1648  [18]
 LDCM0446  CL55 HEK-293T C637(1.09); C588(1.11); C152(1.01); C95(0.80)  LDD1649  [18]
 LDCM0447  CL56 HEK-293T C637(0.99); C588(0.97); C81(0.90); C424(1.19)  LDD1650  [18]
 LDCM0448  CL57 HEK-293T C637(0.93); C81(1.03)  LDD1651  [18]
 LDCM0449  CL58 HEK-293T C637(0.99); C588(0.87); C27(0.93); C152(0.95)  LDD1652  [18]
 LDCM0450  CL59 HEK-293T C637(1.08); C588(1.10); C184(1.06); C152(1.13)  LDD1653  [18]
 LDCM0451  CL6 HEK-293T C637(1.11); C588(1.14); C81(0.85); C152(1.12)  LDD1654  [18]
 LDCM0452  CL60 HEK-293T C637(0.99); C588(1.02); C27(1.19); C81(0.93)  LDD1655  [18]
 LDCM0453  CL61 HEK-293T C637(1.04); C588(0.85); C27(1.06)  LDD1656  [18]
 LDCM0454  CL62 HEK-293T C637(0.98); C588(1.04); C27(1.22); C81(1.02)  LDD1657  [18]
 LDCM0455  CL63 HEK-293T C637(0.96); C588(0.95); C152(1.03); C96(1.00)  LDD1658  [18]
 LDCM0456  CL64 HEK-293T C637(1.04); C588(1.04); C81(1.01); C152(1.10)  LDD1659  [18]
 LDCM0457  CL65 HEK-293T C637(0.99); C588(0.93); C81(1.14); C96(1.17)  LDD1660  [18]
 LDCM0458  CL66 HEK-293T C637(1.10); C588(1.03); C81(0.98); C152(1.26)  LDD1661  [18]
 LDCM0459  CL67 HEK-293T C637(1.11); C588(1.03); C152(1.05); C95(0.83)  LDD1662  [18]
 LDCM0460  CL68 HEK-293T C637(0.98); C588(1.01); C81(0.87); C424(1.38)  LDD1663  [18]
 LDCM0461  CL69 HEK-293T C637(0.99); C81(1.01)  LDD1664  [18]
 LDCM0462  CL7 HEK-293T C637(1.12); C588(1.00); C152(0.95); C95(0.85)  LDD1665  [18]
 LDCM0463  CL70 HEK-293T C637(1.03); C588(0.97); C27(0.85); C152(1.02)  LDD1666  [18]
 LDCM0464  CL71 HEK-293T C637(1.12); C588(1.10); C184(1.12); C152(1.14)  LDD1667  [18]
 LDCM0465  CL72 HEK-293T C637(1.04); C588(1.01); C27(1.02); C81(0.94)  LDD1668  [18]
 LDCM0466  CL73 HEK-293T C637(0.90); C588(0.86); C27(1.03)  LDD1669  [18]
 LDCM0467  CL74 HEK-293T C637(1.01); C588(0.95); C27(0.91); C81(1.12)  LDD1670  [18]
 LDCM0469  CL76 HEK-293T C637(1.04); C588(0.94); C81(0.99); C152(0.92)  LDD1672  [18]
 LDCM0470  CL77 HEK-293T C637(1.19); C588(0.88); C81(0.90); C96(1.23)  LDD1673  [18]
 LDCM0471  CL78 HEK-293T C637(1.08); C588(1.03); C81(1.02); C152(1.09)  LDD1674  [18]
 LDCM0472  CL79 HEK-293T C637(1.15); C588(1.06); C152(1.09); C95(0.81)  LDD1675  [18]
 LDCM0473  CL8 HEK-293T C637(0.98); C588(1.20); C81(0.85); C424(1.14)  LDD1676  [18]
 LDCM0474  CL80 HEK-293T C637(1.17); C588(1.00); C81(0.88); C424(1.27)  LDD1677  [18]
 LDCM0475  CL81 HEK-293T C637(1.04); C81(0.99)  LDD1678  [18]
 LDCM0476  CL82 HEK-293T C637(1.18); C588(0.97); C27(0.97); C152(1.08)  LDD1679  [18]
 LDCM0477  CL83 HEK-293T C637(1.05); C588(0.96); C184(1.14); C152(1.00)  LDD1680  [18]
 LDCM0478  CL84 HEK-293T C637(1.13); C588(0.93); C27(1.17); C81(0.85)  LDD1681  [18]
 LDCM0479  CL85 HEK-293T C637(1.03); C588(0.84); C27(0.81)  LDD1682  [18]
 LDCM0480  CL86 HEK-293T C637(1.09); C588(0.97); C27(0.95); C81(1.02)  LDD1683  [18]
 LDCM0481  CL87 HEK-293T C637(0.78); C588(0.97); C152(1.04); C96(1.39)  LDD1684  [18]
 LDCM0482  CL88 HEK-293T C637(1.03); C588(0.93); C81(0.84); C152(0.96)  LDD1685  [18]
 LDCM0483  CL89 HEK-293T C637(1.09); C588(0.93); C81(0.95); C96(1.05)  LDD1686  [18]
 LDCM0484  CL9 HEK-293T C637(0.98); C81(0.97)  LDD1687  [18]
 LDCM0485  CL90 HEK-293T C637(0.99); C588(1.10); C81(0.84); C152(1.11)  LDD1688  [18]
 LDCM0486  CL91 HEK-293T C637(1.16); C588(1.07); C152(0.93); C95(1.03)  LDD1689  [18]
 LDCM0487  CL92 HEK-293T C637(1.25); C588(1.11); C81(0.81); C424(1.20)  LDD1690  [18]
 LDCM0488  CL93 HEK-293T C637(1.03); C81(0.98)  LDD1691  [18]
 LDCM0489  CL94 HEK-293T C637(1.15); C588(0.98); C27(1.21); C152(0.92)  LDD1692  [18]
 LDCM0490  CL95 HEK-293T C637(1.04); C588(1.11); C184(0.97); C152(1.41)  LDD1693  [18]
 LDCM0491  CL96 HEK-293T C637(1.05); C588(0.97); C27(0.99); C81(0.80)  LDD1694  [18]
 LDCM0492  CL97 HEK-293T C637(0.98); C588(0.92); C27(1.18)  LDD1695  [18]
 LDCM0493  CL98 HEK-293T C637(1.05); C588(0.99); C27(1.25); C81(1.15)  LDD1696  [18]
 LDCM0494  CL99 HEK-293T C637(0.95); C588(0.93); C152(1.12); C96(1.50)  LDD1697  [18]
 LDCM0634  CY-0357 Hep-G2 C637(0.98)  LDD2228  [14]
 LDCM0495  E2913 HEK-293T C637(1.02); C588(0.96); C152(1.02); C96(1.12)  LDD1698  [18]
 LDCM0031  Epigallocatechin gallate HEK-293T 4.68  LDD0183  [5]
 LDCM0175  Ethacrynic acid HeLa N.A.  LDD0440  [7]
 LDCM0625  F8 Ramos C637(1.81)  LDD2187  [20]
 LDCM0572  Fragment10 Ramos C637(1.16)  LDD2189  [20]
 LDCM0573  Fragment11 Ramos C637(0.42)  LDD2190  [20]
 LDCM0574  Fragment12 Ramos C637(1.09)  LDD2191  [20]
 LDCM0575  Fragment13 Ramos C637(0.76)  LDD2192  [20]
 LDCM0576  Fragment14 Ramos C637(1.42)  LDD2193  [20]
 LDCM0580  Fragment21 Ramos C637(0.76)  LDD2195  [20]
 LDCM0582  Fragment23 Ramos C637(0.67)  LDD2196  [20]
 LDCM0578  Fragment27 Ramos C637(0.69)  LDD2197  [20]
 LDCM0586  Fragment28 Ramos C637(0.73)  LDD2198  [20]
 LDCM0588  Fragment30 Ramos C637(1.15)  LDD2199  [20]
 LDCM0589  Fragment31 Ramos C637(0.70)  LDD2200  [20]
 LDCM0468  Fragment33 HEK-293T C637(0.73); C588(0.92); C152(1.07); C96(0.96)  LDD1671  [18]
 LDCM0596  Fragment38 Ramos C637(0.64)  LDD2203  [20]
 LDCM0427  Fragment51 HEK-293T C637(1.02); C588(1.02); C27(1.47); C81(1.03)  LDD1631  [18]
 LDCM0610  Fragment52 Ramos C637(0.61)  LDD2204  [20]
 LDCM0614  Fragment56 Ramos C637(0.90)  LDD2205  [20]
 LDCM0117  HHS-0201 DM93 Y565(1.00)  LDD0265  [9]
 LDCM0118  HHS-0301 DM93 Y565(0.94)  LDD0266  [9]
 LDCM0119  HHS-0401 DM93 Y565(1.11)  LDD0267  [9]
 LDCM0022  KB02 HEK-293T C637(0.99); C588(0.95); C27(1.07)  LDD1492  [18]
 LDCM0023  KB03 Jurkat C588(10.36)  LDD0209  [8]
 LDCM0024  KB05 MKN-1 C657(3.64)  LDD3331  [21]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C637(1.07)  LDD2098  [4]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C637(0.90)  LDD2105  [4]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C637(2.09)  LDD2144  [4]
 LDCM0627  NUDT7-COV-1 HEK-293T C637(0.95)  LDD2206  [22]
 LDCM0628  OTUB2-COV-1 HEK-293T C637(0.89)  LDD2207  [22]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 20 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Endoplasmic reticulum chaperone BiP (HSPA5) Heat shock protein 70 family P11021
Heat shock protein HSP 90-alpha (HSP90AA1) Heat shock protein 90 family P07900
M-phase inducer phosphatase 1 (CDC25A) MPI phosphatase family P30304
Caspase-8 (CASP8) Peptidase C14A family Q14790
Serine/threonine-protein phosphatase 2A 56 kDa regulatory subunit gamma isoform (PPP2R5C) Phosphatase 2A regulatory subunit B56 family Q13362
Serine/threonine-protein phosphatase 2A catalytic subunit alpha isoform (PPP2CA) PPP phosphatase family P67775
Dual specificity mitogen-activated protein kinase kinase 1 (MAP2K1) STE Ser/Thr protein kinase family Q02750
Dual specificity mitogen-activated protein kinase kinase 2 (MAP2K2) STE Ser/Thr protein kinase family P36507
Serine/threonine-protein kinase 3 (STK3) STE Ser/Thr protein kinase family Q13188
Serine/threonine-protein kinase PAK 2 (PAK2) STE Ser/Thr protein kinase family Q13177
RAF proto-oncogene serine/threonine-protein kinase (RAF1) TKL Ser/Thr protein kinase family P04049
Serine/threonine-protein kinase B-raf (BRAF) TKL Ser/Thr protein kinase family P15056
Pyruvate kinase PKM (PKM) Pyruvate kinase family P14618
GTPase HRas (HRAS) Ras family P01112
GTPase KRas (KRAS) Ras family P01116
GTPase NRas (NRAS) Ras family P01111
Ras-related protein Rap-1A (RAP1A) Ras family P62834
Mitochondrial import inner membrane translocase subunit TIM50 (TIMM50) TIM50 family Q3ZCQ8
Carbamoyl-phosphate synthase [ammonia], mitochondrial (CPS1) . P31327
Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (PIN1) . Q13526
Transporter and channel
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
14-3-3 protein epsilon (YWHAE) 14-3-3 family P62258
14-3-3 protein gamma (YWHAG) 14-3-3 family P61981
14-3-3 protein theta (YWHAQ) 14-3-3 family P27348
14-3-3 protein zeta/delta (YWHAZ) 14-3-3 family P63104
Amyloid-beta precursor protein (APP) APP family P05067
Hsp90 co-chaperone Cdc37 (CDC37) CDC37 family Q16543
Heat shock protein HSP 90-beta (HSP90AB1) Heat shock protein 90 family P08238
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Nuclear factor of activated T-cells, cytoplasmic 3 (NFATC3) . Q12968
GPCR
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Progestin and adipoQ receptor family member 3 (PAQR3) ADIPOR family Q6TCH7
Other
Click To Hide/Show 9 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
14-3-3 protein beta/alpha (YWHAB) 14-3-3 family P31946
14-3-3 protein eta (YWHAH) 14-3-3 family Q04917
14-3-3 protein sigma (SFN) 14-3-3 family P31947
Protein Mis18-beta (OIP5) Mis18 family O43482
Phosphatidylethanolamine-binding protein 1 (PEBP1) Phosphatidylethanolamine-binding protein family P30086
Phosphatidylethanolamine-binding protein 4 (PEBP4) Phosphatidylethanolamine-binding protein family Q96S96
Retinoblastoma-associated protein (RB1) Retinoblastoma protein (RB) family P06400
T-complex protein 1 subunit gamma (CCT3) TCP-1 chaperonin family P49368
BAG family molecular chaperone regulator 2 (BAG2) . O95816

The Drug(s) Related To This Target

Approved
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dabrafenib Small molecular drug DB08912
Fostamatinib Small molecular drug DB12010
Regorafenib Small molecular drug DB08896
Sorafenib Small molecular drug DB00398
Cholecystokinin . DB08862
Phase 2
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bgb-3245 Small molecular drug DMYS25
Semapimod Small molecular drug D01WKE
Phase 1
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Belvarafenib Small molecular drug DU98JH
Gdc-5573 . D0VS9E
Investigative
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ico-007 Antisense drug DB05268
Lerafaon Antisense drug DB04973
Xl281 . DB05190

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 Appendage and Scaffold Diverse Fully Functionalized Small-Molecule Probes via a Minimalist Terminal Alkyne-Aliphatic Diazirine Isocyanide. J Org Chem. 2018 Sep 21;83(18):11245-11253. doi: 10.1021/acs.joc.8b01831. Epub 2018 Aug 31.
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 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
5 A chemical probe unravels the reactive proteome of health-associated catechols. Chem Sci. 2023 Jul 22;14(32):8635-8643. doi: 10.1039/d3sc00888f. eCollection 2023 Aug 16.
Mass spectrometry data entry: PXD043348
6 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
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 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.
9 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.
10 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.
11 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
12 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
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 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
15 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
16 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
17 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.
18 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
19 Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications. ACS Chem Biol. 2019 Nov 15;14(11):2430-2440. doi: 10.1021/acschembio.8b01083. Epub 2019 May 13.
20 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
21 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
22 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.