Details of the Target

General Information of Target

Target ID LDTP04504
Target Name Rap1 GTPase-GDP dissociation stimulator 1 (RAP1GDS1)
Gene Name RAP1GDS1
Gene ID 5910
Synonyms
SMGGDS; Rap1 GTPase-GDP dissociation stimulator 1; Exchange factor smgGDS; SMG GDS protein; SMG P21 stimulatory GDP/GTP exchange protein
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDNLSDTLKKLKITAVDKTEDSLEGCLDCLLQALAQNNTETSEKIQASGILQLFASLLTP
QSSCKAKVANIIAEVAKNEFMRIPCVDAGLISPLVQLLNSKDQEVLLQTGRALGNICYDS
HEGRSAVDQAGGAQIVIDHLRSLCSITDPANEKLLTVFCGMLMNYSNENDSLQAQLINMG
VIPTLVKLLGIHCQNAALTEMCLVAFGNLAELESSKEQFASTNIAEELVKLFKKQIEHDK
REMIFEVLAPLAENDAIKLQLVEAGLVECLLEIVQQKVDSDKEDDITELKTGSDLMVLLL
LGDESMQKLFEGGKGSVFQRVLSWIPSNNHQLQLAGALAIANFARNDANCIHMVDNGIVE
KLMDLLDRHVEDGNVTVQHAALSALRNLAIPVINKAKMLSAGVTEAVLKFLKSEMPPVQF
KLLGTLRMLIDAQAEAAEQLGKNVKLVERLVEWCEAKDHAGVMGESNRLLSALIRHSKSK
DVIKTIVQSGGIKHLVTMATSEHVIMQNEALVALALIAALELGTAEKDLESAKLVQILHR
LLADERSAPEIKYNSMVLICALMGSECLHKEVQDLAFLDVVSKLRSHENKSVAQQASLTE
QRLTVES
Target Bioclass
Other
Subcellular location
Cytoplasm, cytosol
Function
Acts as a GEF (guanine nucleotide exchange factor) for the Rho family of small GTP-binding proteins (G proteins) that stimulates the dissociation of GDP to enable subsequent binding of GTP. Additionally, appears to chaperone the processing and/or trafficking of small GTPases containing a C-terminal polybasic region independently of GEF activity. Targets include RAP1A/RAP1B, RHOA, RHOB, RHOC, RAC1 and KRAS. Regulates mitochondrial dynamics by controlling RHOT function to promote mitochondrial fission during high calcium conditions. Able to promote the Ca(2+) release from the endoplasmic reticulum via both inositol trisphosphate (Ins3P) and ryanodine sensitive receptors leading to a enhanced mitochondrial Ca(2+) uptake.; [Isoform 1]: Acts as a GEF (guanine nucleotide exchange factor) for unprenylated RHOA. Chaperones the entry and passage of small GTPases through the prenylation pathway. Recognizes the last amino acid in the GTPase C-terminal CAAX motif with a preference for 'Leu' over 'Met', indicating involvement in the geranylgeranylation pathway.; [Isoform 2]: Acts as a GEF (guanine nucleotide exchange factor) for prenylated RHOA. Acts as a GEF for RHOC. Chaperones the downstream trafficking and/or processing of small newly prenylated GTPases. Escorts RAC1 to the nucleus.
Uniprot ID
P52306
Ensemble ID
ENST00000264572.11
HGNC ID
HGNC:9859

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HUH1 SNV: p.E414V DBIA    Probe Info 
LU65 SNV: p.R320M DBIA    Probe Info 
MFE319 SNV: p.S501G DBIA    Probe Info 
NCIH1975 SNV: p.A510V DBIA    Probe Info 
SH4 SNV: p.S327L DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 27 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		11.59  LDD0402  [1]
TH211
 Probe Info  		Y118(9.35)  LDD0260  [2]
YN-1
 Probe Info  		100.00  LDD0444  [3]
STPyne
 Probe Info  		K234(10.00); K421(3.88); K583(1.08); K67(6.51)  LDD0277  [4]
IPM
 Probe Info  		N.A.  LDD0241  [5]
BTD
 Probe Info  		C117(1.72)  LDD1700  [6]
MCL-4
 Probe Info  		1.50  LDD0049  [7]
AHL-Pu-1
 Probe Info  		C26(2.82)  LDD0170  [8]
EA-probe
 Probe Info  		C85(0.64); C85(0.92)  LDD2210  [9]
DBIA
 Probe Info  		C85(5.69)  LDD0209  [10]
HHS-475
 Probe Info  		Y118(2.97)  LDD0264  [11]
5E-2FA
 Probe Info  		H121(0.00); H459(0.00); H139(0.00)  LDD2235  [12]
ATP probe
 Probe Info  		N.A.  LDD0199  [13]
4-Iodoacetamidophenylacetylene
 Probe Info  		C117(0.00); C85(0.00); C64(0.00); C269(0.00)  LDD0038  [14]
IA-alkyne
 Probe Info  		C117(0.00); C85(0.00); C64(0.00); C202(0.00)  LDD0036  [14]
IPIAA_H
 Probe Info  		N.A.  LDD0030  [15]
IPIAA_L
 Probe Info  		C117(0.00); C269(0.00); C85(0.00); C454(0.00)  LDD0031  [15]
Lodoacetamide azide
 Probe Info  		C117(0.00); C85(0.00); C64(0.00); C269(0.00)  LDD0037  [14]
NAIA_4
 Probe Info  		C64(0.00); C85(0.00); C117(0.00)  LDD2226  [16]
TFBX
 Probe Info  		N.A.  LDD0027  [17]
Compound 10
 Probe Info  		C117(0.00); C454(0.00)  LDD2216  [18]
NHS
 Probe Info  		N.A.  LDD0010  [19]
Acrolein
 Probe Info  		C350(0.00); C117(0.00); C454(0.00)  LDD0217  [20]
Methacrolein
 Probe Info  		C117(0.00); C350(0.00)  LDD0218  [20]
W1
 Probe Info  		N.A.  LDD0236  [5]
AOyne
 Probe Info  		10.50  LDD0443  [21]
NAIA_5
 Probe Info  		C117(0.00); C85(0.00); C64(0.00); C350(0.00)  LDD2223  [16]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
VE-P
 Probe Info  		N.A.  LDD0396  [22]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C350(1.03)  LDD2117  [6]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C117(1.36)  LDD2152  [6]
 LDCM0025  4SU-RNA DM93 C26(2.82)  LDD0170  [8]
 LDCM0026  4SU-RNA+native RNA DM93 C29(2.63); C26(2.16)  LDD0171  [8]
 LDCM0214  AC1 HEK-293T C117(0.94); C350(1.01); C193(0.98); C144(0.91)  LDD1507  [23]
 LDCM0215  AC10 HEK-293T C117(1.03); C350(1.07); C193(0.96); C144(0.87)  LDD1508  [23]
 LDCM0226  AC11 HEK-293T C117(0.99); C350(1.17); C193(0.98); C144(1.02)  LDD1509  [23]
 LDCM0237  AC12 HEK-293T C117(0.98); C350(1.11); C193(1.04); C144(0.98)  LDD1510  [23]
 LDCM0259  AC14 HEK-293T C117(1.01); C350(1.04); C193(0.90); C144(0.98)  LDD1512  [23]
 LDCM0270  AC15 HEK-293T C117(1.11); C350(1.02); C193(0.89); C144(1.00)  LDD1513  [23]
 LDCM0276  AC17 HEK-293T C117(0.96); C350(1.12); C193(0.94); C144(0.89)  LDD1515  [23]
 LDCM0277  AC18 HEK-293T C117(0.99); C350(1.01); C193(0.91); C144(0.91)  LDD1516  [23]
 LDCM0278  AC19 HEK-293T C117(0.95); C350(1.03); C193(1.02); C144(1.20)  LDD1517  [23]
 LDCM0279  AC2 HEK-293T C117(1.07); C350(1.15); C193(0.97); C144(1.00)  LDD1518  [23]
 LDCM0280  AC20 HEK-293T C117(1.01); C350(1.12); C193(0.95); C144(0.85)  LDD1519  [23]
 LDCM0281  AC21 HEK-293T C117(0.99); C350(1.13); C193(0.98); C144(1.02)  LDD1520  [23]
 LDCM0282  AC22 HEK-293T C117(1.04); C350(1.08); C193(0.91); C144(1.02)  LDD1521  [23]
 LDCM0283  AC23 HEK-293T C117(0.96); C350(1.03); C193(1.01); C144(0.97)  LDD1522  [23]
 LDCM0284  AC24 HEK-293T C117(1.04); C350(1.08); C193(0.95); C144(1.00)  LDD1523  [23]
 LDCM0285  AC25 HEK-293T C117(0.97); C350(1.08); C193(0.95); C144(0.97)  LDD1524  [23]
 LDCM0286  AC26 HEK-293T C117(0.99); C350(1.06); C193(0.98); C144(0.91)  LDD1525  [23]
 LDCM0287  AC27 HEK-293T C117(0.95); C350(1.05); C193(1.01); C144(1.01)  LDD1526  [23]
 LDCM0288  AC28 HEK-293T C117(1.03); C350(1.11); C193(0.95); C144(1.06)  LDD1527  [23]
 LDCM0289  AC29 HEK-293T C117(1.03); C350(1.03); C193(0.95); C144(1.02)  LDD1528  [23]
 LDCM0290  AC3 HEK-293T C117(0.94); C350(1.00); C193(1.03); C144(1.08)  LDD1529  [23]
 LDCM0291  AC30 HEK-293T C117(0.95); C350(1.03); C193(0.96); C144(0.97)  LDD1530  [23]
 LDCM0292  AC31 HEK-293T C117(1.00); C350(0.96); C193(1.09); C144(1.00)  LDD1531  [23]
 LDCM0293  AC32 HEK-293T C117(1.05); C350(1.09); C193(1.03); C144(1.00)  LDD1532  [23]
 LDCM0294  AC33 HEK-293T C117(1.00); C350(1.12); C193(1.01); C144(0.92)  LDD1533  [23]
 LDCM0295  AC34 HEK-293T C117(0.96); C350(1.06); C193(0.98); C144(1.04)  LDD1534  [23]
 LDCM0296  AC35 HEK-293T C117(0.98); C350(1.08); C193(1.02); C144(1.03)  LDD1535  [23]
 LDCM0297  AC36 HEK-293T C117(0.97); C350(1.13); C193(1.06); C144(0.90)  LDD1536  [23]
 LDCM0298  AC37 HEK-293T C117(1.00); C350(0.94); C193(0.96); C144(1.13)  LDD1537  [23]
 LDCM0299  AC38 HEK-293T C117(1.00); C350(1.15); C193(1.00); C144(1.04)  LDD1538  [23]
 LDCM0300  AC39 HEK-293T C117(1.02); C350(1.06); C193(0.93); C144(1.00)  LDD1539  [23]
 LDCM0301  AC4 HEK-293T C117(1.06); C350(1.12); C193(1.01); C144(0.94)  LDD1540  [23]
 LDCM0302  AC40 HEK-293T C117(0.98); C350(1.08); C193(1.12); C144(0.93)  LDD1541  [23]
 LDCM0303  AC41 HEK-293T C117(1.02); C350(1.14); C193(0.98); C144(0.90)  LDD1542  [23]
 LDCM0304  AC42 HEK-293T C117(0.96); C350(1.09); C193(0.92); C144(0.91)  LDD1543  [23]
 LDCM0305  AC43 HEK-293T C117(1.04); C350(1.05); C193(0.99); C144(1.10)  LDD1544  [23]
 LDCM0306  AC44 HEK-293T C117(1.04); C350(1.20); C193(1.01); C144(0.96)  LDD1545  [23]
 LDCM0307  AC45 HEK-293T C117(1.06); C350(1.02); C193(1.00); C144(1.00)  LDD1546  [23]
 LDCM0308  AC46 HEK-293T C117(0.95); C350(1.16); C193(0.94); C144(0.86)  LDD1547  [23]
 LDCM0309  AC47 HEK-293T C117(1.07); C350(1.12); C193(0.94); C144(0.99)  LDD1548  [23]
 LDCM0310  AC48 HEK-293T C117(1.06); C350(1.17); C193(1.05); C144(1.02)  LDD1549  [23]
 LDCM0311  AC49 HEK-293T C117(0.95); C350(1.12); C193(0.82); C144(0.94)  LDD1550  [23]
 LDCM0312  AC5 HEK-293T C117(1.08); C350(1.11); C193(0.94); C144(1.05)  LDD1551  [23]
 LDCM0313  AC50 HEK-293T C117(1.04); C350(1.03); C193(0.98); C144(0.99)  LDD1552  [23]
 LDCM0314  AC51 HEK-293T C117(1.07); C350(1.12); C193(0.97); C144(0.93)  LDD1553  [23]
 LDCM0315  AC52 HEK-293T C117(1.06); C350(1.15); C193(0.97); C144(0.96)  LDD1554  [23]
 LDCM0316  AC53 HEK-293T C117(1.04); C350(1.03); C193(1.02); C144(1.06)  LDD1555  [23]
 LDCM0317  AC54 HEK-293T C117(0.96); C350(1.21); C193(0.90); C144(0.92)  LDD1556  [23]
 LDCM0318  AC55 HEK-293T C117(1.03); C350(1.15); C193(0.92); C144(0.94)  LDD1557  [23]
 LDCM0319  AC56 HEK-293T C117(1.05); C350(1.07); C193(1.10); C144(0.99)  LDD1558  [23]
 LDCM0320  AC57 HEK-293T C117(0.96); C350(1.09); C193(1.03); C144(0.92)  LDD1559  [23]
 LDCM0321  AC58 HEK-293T C117(1.03); C350(1.11); C193(1.03); C144(0.93)  LDD1560  [23]
 LDCM0322  AC59 HEK-293T C117(1.04); C350(1.12); C193(1.02); C144(0.94)  LDD1561  [23]
 LDCM0323  AC6 HEK-293T C117(0.99); C350(1.10); C193(0.97); C144(0.93)  LDD1562  [23]
 LDCM0324  AC60 HEK-293T C117(1.02); C350(1.13); C193(1.00); C144(0.95)  LDD1563  [23]
 LDCM0325  AC61 HEK-293T C117(1.02); C350(1.11); C193(1.04); C144(0.98)  LDD1564  [23]
 LDCM0326  AC62 HEK-293T C117(1.07); C350(1.13); C193(0.96); C144(0.95)  LDD1565  [23]
 LDCM0327  AC63 HEK-293T C117(1.06); C350(1.06); C193(0.97); C144(1.01)  LDD1566  [23]
 LDCM0328  AC64 HEK-293T C117(1.04); C350(1.10); C193(1.11); C144(0.97)  LDD1567  [23]
 LDCM0334  AC7 HEK-293T C117(1.00); C350(1.01); C193(0.86); C144(1.07)  LDD1568  [23]
 LDCM0345  AC8 HEK-293T C117(1.04); C350(1.00); C193(1.13); C144(0.97)  LDD1569  [23]
 LDCM0545  Acetamide MDA-MB-231 C350(0.67)  LDD2138  [6]
 LDCM0520  AKOS000195272 MDA-MB-231 C117(0.99)  LDD2113  [6]
 LDCM0248  AKOS034007472 HEK-293T C117(0.99); C350(0.96); C193(1.02); C144(1.08)  LDD1511  [23]
 LDCM0356  AKOS034007680 HEK-293T C117(0.97); C350(1.12); C193(0.98); C144(0.98)  LDD1570  [23]
 LDCM0275  AKOS034007705 HEK-293T C117(1.06); C350(1.05); C193(1.02); C144(0.96)  LDD1514  [23]
 LDCM0156  Aniline NCI-H1299 11.48  LDD0403  [1]
 LDCM0498  BS-3668 MDA-MB-231 C117(1.10)  LDD2091  [6]
 LDCM0108  Chloroacetamide HeLa C117(0.00); C454(0.00); C144(0.00); C350(0.00)  LDD0222  [20]
 LDCM0367  CL1 HEK-293T C117(0.98); C350(1.02); C193(0.89); C144(0.92)  LDD1571  [23]
 LDCM0368  CL10 HEK-293T C117(0.72); C350(1.04); C193(0.99); C144(0.98)  LDD1572  [23]
 LDCM0369  CL100 HEK-293T C117(1.07); C350(1.04); C193(1.02); C144(0.94)  LDD1573  [23]
 LDCM0370  CL101 HEK-293T C117(0.91); C350(1.01); C193(0.86); C144(1.00)  LDD1574  [23]
 LDCM0371  CL102 HEK-293T C117(1.02); C350(1.09); C193(0.93); C144(0.89)  LDD1575  [23]
 LDCM0372  CL103 HEK-293T C117(1.09); C350(1.09); C193(1.01); C144(0.95)  LDD1576  [23]
 LDCM0373  CL104 HEK-293T C117(1.02); C350(1.16); C193(0.96); C144(1.02)  LDD1577  [23]
 LDCM0374  CL105 HEK-293T C117(1.05); C350(1.00); C193(0.87); C144(0.97)  LDD1578  [23]
 LDCM0375  CL106 HEK-293T C117(1.05); C350(1.14); C193(1.01); C144(0.85)  LDD1579  [23]
 LDCM0376  CL107 HEK-293T C117(1.16); C350(1.11); C193(1.01); C144(0.87)  LDD1580  [23]
 LDCM0377  CL108 HEK-293T C117(1.18); C350(1.12); C193(0.93); C144(1.01)  LDD1581  [23]
 LDCM0378  CL109 HEK-293T C117(0.86); C350(0.98); C193(0.86); C144(0.94)  LDD1582  [23]
 LDCM0379  CL11 HEK-293T C117(0.95); C350(0.98); C193(0.94); C144(1.02)  LDD1583  [23]
 LDCM0380  CL110 HEK-293T C117(0.99); C350(1.07); C193(1.00); C144(0.90)  LDD1584  [23]
 LDCM0381  CL111 HEK-293T C117(0.96); C350(1.03); C193(0.88); C144(1.03)  LDD1585  [23]
 LDCM0382  CL112 HEK-293T C117(1.01); C350(1.09); C193(0.97); C144(0.93)  LDD1586  [23]
 LDCM0383  CL113 HEK-293T C117(1.00); C350(1.03); C193(0.81); C144(0.90)  LDD1587  [23]
 LDCM0384  CL114 HEK-293T C117(0.91); C350(1.12); C193(1.02); C144(0.95)  LDD1588  [23]
 LDCM0385  CL115 HEK-293T C117(1.05); C350(1.14); C193(0.98); C144(0.94)  LDD1589  [23]
 LDCM0386  CL116 HEK-293T C117(1.02); C350(1.13); C193(0.88); C144(0.94)  LDD1590  [23]
 LDCM0387  CL117 HEK-293T C117(0.98); C350(1.08); C193(0.93); C144(0.92)  LDD1591  [23]
 LDCM0388  CL118 HEK-293T C117(1.07); C350(1.10); C193(1.01); C144(1.03)  LDD1592  [23]
 LDCM0389  CL119 HEK-293T C117(1.09); C350(1.16); C193(0.97); C144(0.94)  LDD1593  [23]
 LDCM0390  CL12 HEK-293T C117(1.14); C350(1.08); C193(1.05); C144(1.18)  LDD1594  [23]
 LDCM0391  CL120 HEK-293T C117(1.05); C350(1.09); C193(0.92); C144(0.94)  LDD1595  [23]
 LDCM0392  CL121 HEK-293T C117(0.96); C350(1.01); C193(0.91); C144(0.91)  LDD1596  [23]
 LDCM0393  CL122 HEK-293T C117(1.07); C350(1.20); C193(0.96); C144(1.02)  LDD1597  [23]
 LDCM0394  CL123 HEK-293T C117(0.89); C350(1.15); C193(0.95); C144(1.08)  LDD1598  [23]
 LDCM0395  CL124 HEK-293T C117(0.93); C350(1.23); C193(0.90); C144(0.98)  LDD1599  [23]
 LDCM0396  CL125 HEK-293T C117(0.97); C350(0.99); C193(1.16); C144(1.05)  LDD1600  [23]
 LDCM0397  CL126 HEK-293T C117(0.97); C350(1.14); C193(1.14); C144(1.00)  LDD1601  [23]
 LDCM0398  CL127 HEK-293T C117(1.03); C350(1.05); C193(1.07); C144(1.05)  LDD1602  [23]
 LDCM0399  CL128 HEK-293T C117(1.08); C350(1.15); C193(1.05); C144(1.05)  LDD1603  [23]
 LDCM0400  CL13 HEK-293T C117(1.03); C350(0.98); C193(0.94); C144(0.90)  LDD1604  [23]
 LDCM0401  CL14 HEK-293T C117(1.17); C350(1.11); C193(1.01); C144(0.93)  LDD1605  [23]
 LDCM0402  CL15 HEK-293T C117(0.88); C350(1.03); C193(1.05); C144(0.97)  LDD1606  [23]
 LDCM0403  CL16 HEK-293T C117(1.06); C350(1.09); C193(0.99); C144(1.06)  LDD1607  [23]
 LDCM0404  CL17 HEK-293T C117(0.83); C350(1.04); C193(0.91); C144(0.86)  LDD1608  [23]
 LDCM0405  CL18 HEK-293T C117(1.07); C350(1.10); C193(0.84); C144(1.14)  LDD1609  [23]
 LDCM0406  CL19 HEK-293T C117(0.96); C350(1.11); C193(1.03); C144(1.19)  LDD1610  [23]
 LDCM0407  CL2 HEK-293T C117(1.06); C350(1.05); C193(1.03); C144(1.02)  LDD1611  [23]
 LDCM0408  CL20 HEK-293T C117(1.04); C350(0.99); C193(1.11); C144(1.13)  LDD1612  [23]
 LDCM0409  CL21 HEK-293T C117(0.92); C350(0.84); C193(1.03); C144(1.16)  LDD1613  [23]
 LDCM0410  CL22 HEK-293T C117(1.01); C350(1.17); C193(1.05); C144(0.93)  LDD1614  [23]
 LDCM0411  CL23 HEK-293T C117(1.07); C350(0.97); C193(1.00); C144(1.14)  LDD1615  [23]
 LDCM0412  CL24 HEK-293T C117(1.07); C350(1.04); C193(1.08); C144(1.17)  LDD1616  [23]
 LDCM0413  CL25 HEK-293T C117(0.82); C350(1.05); C193(0.98); C144(0.96)  LDD1617  [23]
 LDCM0414  CL26 HEK-293T C117(1.23); C350(1.08); C193(0.95); C144(0.93)  LDD1618  [23]
 LDCM0415  CL27 HEK-293T C117(1.21); C350(1.04); C193(0.96); C144(0.97)  LDD1619  [23]
 LDCM0416  CL28 HEK-293T C117(0.97); C350(0.99); C193(0.96); C144(1.07)  LDD1620  [23]
 LDCM0417  CL29 HEK-293T C117(0.98); C350(1.05); C193(0.88); C144(1.02)  LDD1621  [23]
 LDCM0418  CL3 HEK-293T C117(1.08); C350(1.03); C193(1.06); C144(1.06)  LDD1622  [23]
 LDCM0419  CL30 HEK-293T C117(1.03); C350(1.23); C193(0.88); C144(1.09)  LDD1623  [23]
 LDCM0420  CL31 HEK-293T C117(0.96); C350(1.13); C193(0.94); C144(1.18)  LDD1624  [23]
 LDCM0421  CL32 HEK-293T C117(1.01); C350(1.06); C193(1.06); C144(1.12)  LDD1625  [23]
 LDCM0422  CL33 HEK-293T C117(0.81); C350(0.81); C193(0.98); C144(1.03)  LDD1626  [23]
 LDCM0423  CL34 HEK-293T C117(1.07); C350(1.20); C193(0.92); C144(0.93)  LDD1627  [23]
 LDCM0424  CL35 HEK-293T C117(1.04); C350(1.03); C193(1.08); C144(1.14)  LDD1628  [23]
 LDCM0425  CL36 HEK-293T C117(1.01); C350(0.98); C193(1.12); C144(1.11)  LDD1629  [23]
 LDCM0426  CL37 HEK-293T C117(1.06); C350(0.98); C193(1.03); C144(0.94)  LDD1630  [23]
 LDCM0428  CL39 HEK-293T C117(1.10); C350(1.07); C193(0.95); C144(0.90)  LDD1632  [23]
 LDCM0429  CL4 HEK-293T C117(1.07); C350(1.02); C193(0.99); C144(1.02)  LDD1633  [23]
 LDCM0430  CL40 HEK-293T C117(0.99); C350(1.05); C193(0.91); C144(1.01)  LDD1634  [23]
 LDCM0431  CL41 HEK-293T C117(0.93); C350(1.07); C193(0.87); C144(0.90)  LDD1635  [23]
 LDCM0432  CL42 HEK-293T C117(1.10); C350(1.04); C193(0.94); C144(1.17)  LDD1636  [23]
 LDCM0433  CL43 HEK-293T C117(1.01); C350(1.03); C193(0.99); C144(1.06)  LDD1637  [23]
 LDCM0434  CL44 HEK-293T C117(0.89); C350(0.97); C193(1.00); C144(1.02)  LDD1638  [23]
 LDCM0435  CL45 HEK-293T C117(0.89); C350(0.84); C193(0.98); C144(1.07)  LDD1639  [23]
 LDCM0436  CL46 HEK-293T C117(0.97); C350(1.05); C193(0.96); C144(1.14)  LDD1640  [23]
 LDCM0437  CL47 HEK-293T C117(0.97); C350(1.03); C193(1.02); C144(0.97)  LDD1641  [23]
 LDCM0438  CL48 HEK-293T C117(1.08); C350(1.00); C193(1.26); C144(1.17)  LDD1642  [23]
 LDCM0439  CL49 HEK-293T C117(1.06); C350(1.00); C193(0.98); C144(1.07)  LDD1643  [23]
 LDCM0440  CL5 HEK-293T C117(1.00); C350(0.96); C193(1.10); C144(0.98)  LDD1644  [23]
 LDCM0441  CL50 HEK-293T C117(1.11); C350(1.09); C193(0.93); C144(0.94)  LDD1645  [23]
 LDCM0443  CL52 HEK-293T C117(0.95); C350(0.98); C193(0.94); C144(0.95)  LDD1646  [23]
 LDCM0444  CL53 HEK-293T C117(0.90); C350(0.97); C193(0.85); C144(1.04)  LDD1647  [23]
 LDCM0445  CL54 HEK-293T C117(0.86); C350(1.07); C193(0.99); C144(1.01)  LDD1648  [23]
 LDCM0446  CL55 HEK-293T C117(1.03); C350(1.14); C193(0.98); C144(1.04)  LDD1649  [23]
 LDCM0447  CL56 HEK-293T C117(1.15); C350(1.04); C193(1.08); C144(1.07)  LDD1650  [23]
 LDCM0448  CL57 HEK-293T C117(0.96); C350(1.00); C193(0.89); C144(1.09)  LDD1651  [23]
 LDCM0449  CL58 HEK-293T C117(0.92); C350(1.14); C193(1.07); C144(1.15)  LDD1652  [23]
 LDCM0450  CL59 HEK-293T C117(1.00); C350(1.12); C193(0.92); C144(1.11)  LDD1653  [23]
 LDCM0451  CL6 HEK-293T C117(0.99); C350(1.03); C193(0.99); C144(1.18)  LDD1654  [23]
 LDCM0452  CL60 HEK-293T C117(1.05); C350(1.04); C193(0.98); C144(1.10)  LDD1655  [23]
 LDCM0453  CL61 HEK-293T C117(0.94); C350(0.99); C193(0.97); C144(0.98)  LDD1656  [23]
 LDCM0454  CL62 HEK-293T C117(1.09); C350(1.05); C193(1.04); C144(0.89)  LDD1657  [23]
 LDCM0455  CL63 HEK-293T C117(1.07); C350(1.10); C193(1.11); C144(0.96)  LDD1658  [23]
 LDCM0456  CL64 HEK-293T C117(0.89); C350(0.98); C193(0.93); C144(1.00)  LDD1659  [23]
 LDCM0457  CL65 HEK-293T C117(1.11); C350(1.12); C193(0.89); C144(1.03)  LDD1660  [23]
 LDCM0458  CL66 HEK-293T C117(0.92); C350(1.10); C193(0.97); C144(1.04)  LDD1661  [23]
 LDCM0459  CL67 HEK-293T C117(0.93); C350(1.01); C193(0.98); C144(1.18)  LDD1662  [23]
 LDCM0460  CL68 HEK-293T C117(1.13); C350(1.04); C193(1.02); C144(1.03)  LDD1663  [23]
 LDCM0461  CL69 HEK-293T C117(0.99); C350(0.92); C193(0.97); C144(1.14)  LDD1664  [23]
 LDCM0462  CL7 HEK-293T C117(0.96); C350(0.93); C193(1.18); C144(1.23)  LDD1665  [23]
 LDCM0463  CL70 HEK-293T C117(1.01); C350(1.06); C193(1.20); C144(0.88)  LDD1666  [23]
 LDCM0464  CL71 HEK-293T C117(0.98); C350(1.05); C193(0.94); C144(1.05)  LDD1667  [23]
 LDCM0465  CL72 HEK-293T C117(1.00); C350(1.00); C193(1.21); C144(1.13)  LDD1668  [23]
 LDCM0466  CL73 HEK-293T C117(0.95); C350(1.06); C193(0.92); C144(1.04)  LDD1669  [23]
 LDCM0467  CL74 HEK-293T C117(1.17); C350(1.13); C193(1.06); C144(0.92)  LDD1670  [23]
 LDCM0469  CL76 HEK-293T C117(0.94); C350(1.06); C193(0.93); C144(1.01)  LDD1672  [23]
 LDCM0470  CL77 HEK-293T C117(0.90); C350(1.01); C193(0.89); C144(0.98)  LDD1673  [23]
 LDCM0471  CL78 HEK-293T C117(1.05); C350(1.19); C193(0.96); C144(1.06)  LDD1674  [23]
 LDCM0472  CL79 HEK-293T C117(0.97); C350(1.12); C193(1.04); C144(1.34)  LDD1675  [23]
 LDCM0473  CL8 HEK-293T C117(0.70); C350(0.92); C193(1.53); C144(1.73)  LDD1676  [23]
 LDCM0474  CL80 HEK-293T C117(1.19); C350(1.07); C193(1.04); C144(1.08)  LDD1677  [23]
 LDCM0475  CL81 HEK-293T C117(1.02); C350(0.87); C193(1.11); C144(1.17)  LDD1678  [23]
 LDCM0476  CL82 HEK-293T C117(0.91); C350(1.04); C193(1.03); C144(0.91)  LDD1679  [23]
 LDCM0477  CL83 HEK-293T C117(1.00); C350(0.99); C193(0.94); C144(1.11)  LDD1680  [23]
 LDCM0478  CL84 HEK-293T C117(0.94); C350(1.16); C193(1.04); C144(1.09)  LDD1681  [23]
 LDCM0479  CL85 HEK-293T C117(1.04); C350(1.05); C193(1.07); C144(0.99)  LDD1682  [23]
 LDCM0480  CL86 HEK-293T C117(1.11); C350(1.11); C193(1.14); C144(1.01)  LDD1683  [23]
 LDCM0481  CL87 HEK-293T C117(1.11); C350(1.06); C193(1.07); C144(1.08)  LDD1684  [23]
 LDCM0482  CL88 HEK-293T C117(1.09); C350(1.03); C193(1.07); C144(1.00)  LDD1685  [23]
 LDCM0483  CL89 HEK-293T C117(0.98); C350(1.14); C193(0.99); C144(0.91)  LDD1686  [23]
 LDCM0484  CL9 HEK-293T C117(0.97); C350(0.82); C193(1.05); C144(1.22)  LDD1687  [23]
 LDCM0485  CL90 HEK-293T C117(0.72); C350(1.05); C193(1.30); C144(0.90)  LDD1688  [23]
 LDCM0486  CL91 HEK-293T C117(1.17); C350(1.09); C193(1.03); C144(1.04)  LDD1689  [23]
 LDCM0487  CL92 HEK-293T C117(1.01); C350(1.08); C193(1.07); C144(1.03)  LDD1690  [23]
 LDCM0488  CL93 HEK-293T C117(1.01); C350(0.86); C193(0.98); C144(1.15)  LDD1691  [23]
 LDCM0489  CL94 HEK-293T C117(0.95); C350(0.98); C193(0.95); C144(0.93)  LDD1692  [23]
 LDCM0490  CL95 HEK-293T C117(0.84); C350(0.98); C193(0.95); C144(1.01)  LDD1693  [23]
 LDCM0491  CL96 HEK-293T C117(0.96); C350(1.10); C193(1.15); C144(1.03)  LDD1694  [23]
 LDCM0492  CL97 HEK-293T C117(0.92); C350(0.98); C193(0.91); C144(0.92)  LDD1695  [23]
 LDCM0493  CL98 HEK-293T C117(1.05); C350(1.02); C193(0.91); C144(0.85)  LDD1696  [23]
 LDCM0494  CL99 HEK-293T C117(1.06); C350(0.94); C193(0.96); C144(0.93)  LDD1697  [23]
 LDCM0495  E2913 HEK-293T C117(1.18); C350(1.12); C193(0.93); C144(0.96)  LDD1698  [23]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C117(5.84)  LDD1702  [6]
 LDCM0175  Ethacrynic acid HeLa C85(0.64); C85(0.92)  LDD2210  [9]
 LDCM0625  F8 Ramos C117(1.33); C454(0.79); C144(1.08); C85(0.94)  LDD2187  [24]
 LDCM0572  Fragment10 Ramos C117(1.38); C454(0.48); C144(1.18); C350(0.57)  LDD2189  [24]
 LDCM0573  Fragment11 Ramos C117(0.15); C144(0.59); C350(17.04); C85(0.30)  LDD2190  [24]
 LDCM0574  Fragment12 Ramos C117(2.59); C454(0.53); C144(2.79)  LDD2191  [24]
 LDCM0575  Fragment13 Ramos C117(1.07); C454(0.88); C144(0.91); C85(1.10)  LDD2192  [24]
 LDCM0576  Fragment14 Ramos C117(8.04); C64(0.59)  LDD2193  [24]
 LDCM0579  Fragment20 Ramos C117(5.89); C454(0.62); C350(0.77)  LDD2194  [24]
 LDCM0580  Fragment21 Ramos C117(1.25); C454(0.78); C144(1.06); C85(1.24)  LDD2195  [24]
 LDCM0582  Fragment23 Ramos C117(2.82); C454(0.69); C144(2.24); C350(0.36)  LDD2196  [24]
 LDCM0578  Fragment27 Ramos C117(1.07); C454(0.88); C144(0.94); C350(0.93)  LDD2197  [24]
 LDCM0586  Fragment28 Ramos C117(0.66); C454(0.58); C144(0.57); C350(0.67)  LDD2198  [24]
 LDCM0588  Fragment30 Ramos C117(1.31); C454(0.76); C144(0.98); C85(1.40)  LDD2199  [24]
 LDCM0589  Fragment31 Ramos C117(1.96); C454(0.71); C144(1.27); C350(0.87)  LDD2200  [24]
 LDCM0590  Fragment32 Ramos C117(1.35); C454(0.53); C144(1.39); C85(3.99)  LDD2201  [24]
 LDCM0468  Fragment33 HEK-293T C117(1.04); C350(1.09); C193(0.97); C144(0.96)  LDD1671  [23]
 LDCM0596  Fragment38 Ramos C117(1.43); C454(0.87); C144(0.70); C350(0.58)  LDD2203  [24]
 LDCM0566  Fragment4 Ramos C117(1.33); C454(0.79); C144(1.49); C350(0.86)  LDD2184  [24]
 LDCM0427  Fragment51 HEK-293T C117(1.14); C350(1.09); C193(0.99); C144(0.94)  LDD1631  [23]
 LDCM0610  Fragment52 Ramos C117(1.63); C144(1.59); C350(1.01); C85(2.55)  LDD2204  [24]
 LDCM0614  Fragment56 Ramos C117(1.60); C454(0.83); C144(1.03); C350(0.80)  LDD2205  [24]
 LDCM0569  Fragment7 Ramos C117(1.68); C454(0.97); C144(1.37); C350(0.74)  LDD2186  [24]
 LDCM0571  Fragment9 Ramos C117(4.63); C454(0.49); C350(0.79)  LDD2188  [24]
 LDCM0116  HHS-0101 DM93 Y118(2.97)  LDD0264  [11]
 LDCM0117  HHS-0201 DM93 Y118(4.05)  LDD0265  [11]
 LDCM0118  HHS-0301 DM93 Y118(3.88)  LDD0266  [11]
 LDCM0119  HHS-0401 DM93 Y118(1.04)  LDD0267  [11]
 LDCM0120  HHS-0701 DM93 Y118(4.85)  LDD0268  [11]
 LDCM0015  HNE MDA-MB-231 C85(1.10)  LDD0346  [24]
 LDCM0107  IAA HeLa C117(0.00); C144(0.00); C454(0.00)  LDD0221  [20]
 LDCM0022  KB02 HEK-293T C117(1.10); C350(1.10); C144(1.04); C454(0.88)  LDD1492  [23]
 LDCM0023  KB03 Jurkat C85(5.69)  LDD0209  [10]
 LDCM0024  KB05 G361 C86(2.49); C455(2.12); C145(3.24)  LDD3311  [25]
 LDCM0006  Micheliolide M9-ENL1 1.50  LDD0049  [7]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C117(0.89); C350(0.91)  LDD2121  [6]
 LDCM0109  NEM HeLa H459(0.00); H139(0.00)  LDD0223  [20]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C117(0.99)  LDD2097  [6]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C144(0.94)  LDD2107  [6]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C117(0.97)  LDD2108  [6]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C117(1.10); C350(0.89)  LDD2109  [6]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C117(1.03)  LDD2119  [6]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C350(0.93)  LDD2123  [6]
 LDCM0531  Nucleophilic fragment 28b MDA-MB-231 C350(0.84)  LDD2124  [6]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C117(0.91)  LDD2125  [6]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C117(1.08); C350(1.14)  LDD2127  [6]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C117(0.99)  LDD2129  [6]
 LDCM0540  Nucleophilic fragment 35 MDA-MB-231 C117(1.06)  LDD2133  [6]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C117(0.94)  LDD2135  [6]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C117(1.88); C350(1.38)  LDD2136  [6]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C350(1.21)  LDD2137  [6]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C117(1.72)  LDD1700  [6]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C117(0.99); C144(1.40)  LDD2140  [6]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C117(0.66)  LDD2143  [6]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C117(1.07)  LDD2146  [6]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C117(0.54)  LDD2148  [6]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C117(0.83); C350(0.57)  LDD2150  [6]
 LDCM0627  NUDT7-COV-1 HEK-293T C117(0.56)  LDD2206  [26]
 LDCM0628  OTUB2-COV-1 HEK-293T C117(0.07)  LDD2207  [26]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 9 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
E3 ubiquitin-protein ligase RNF19B (RNF19B) RBR family Q6ZMZ0
GTP-binding protein Di-Ras1 (DIRAS1) Di-Ras family O95057
GTP-binding protein Di-Ras2 (DIRAS2) Di-Ras family Q96HU8
Ras-related protein Rab-6B (RAB6B) Rab family Q9NRW1
GTPase NRas (NRAS) Ras family P01111
Ras-related protein R-Ras (RRAS) Ras family P10301
Ras-related protein R-Ras2 (RRAS2) Ras family P62070
Ras-related protein Rap-2b (RAP2B) Ras family P61225
Ras-related protein Rap-2c (RAP2C) Ras family Q9Y3L5
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Optineurin (OPTN) . Q96CV9
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Pleckstrin homology domain-containing family B member 1 (PLEKHB1) . Q9UF11

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
2 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
3 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.
4 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
5 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.
6 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
7 Comprehensive Structure-Activity Profiling of Micheliolide and its Targeted Proteome in Leukemia Cells via Probe-Guided Late-Stage C-H Functionalization. ACS Cent Sci. 2021 May 26;7(5):841-857. doi: 10.1021/acscentsci.0c01624. Epub 2021 Apr 28.
Mass spectrometry data entry: PXD024455
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 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.
10 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.
11 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.
12 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
13 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.
14 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
15 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
16 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
17 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
18 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
19 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
20 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.
21 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.
22 Pharmacological Targeting of Vacuolar H(+)-ATPase via Subunit V1G Combats Multidrug-Resistant Cancer. Cell Chem Biol. 2020 Nov 19;27(11):1359-1370.e8. doi: 10.1016/j.chembiol.2020.06.011. Epub 2020 Jul 9.
23 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402
24 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578
25 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
26 Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22.