General Information of Target

Target ID LDTP03012
Target Name Retinoic acid receptor RXR-alpha (RXRA)
Gene Name RXRA
Gene ID 6256
Synonyms
NR2B1; Retinoic acid receptor RXR-alpha; Nuclear receptor subfamily 2 group B member 1; Retinoid X receptor alpha
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDTKHFLPLDFSTQVNSSLTSPTGRGSMAAPSLHPSLGPGIGSPGQLHSPISTLSSPING
MGPPFSVISSPMGPHSMSVPTTPTLGFSTGSPQLSSPMNPVSSSEDIKPPLGLNGVLKVP
AHPSGNMASFTKHICAICGDRSSGKHYGVYSCEGCKGFFKRTVRKDLTYTCRDNKDCLID
KRQRNRCQYCRYQKCLAMGMKREAVQEERQRGKDRNENEVESTSSANEDMPVERILEAEL
AVEPKTETYVEANMGLNPSSPNDPVTNICQAADKQLFTLVEWAKRIPHFSELPLDDQVIL
LRAGWNELLIASFSHRSIAVKDGILLATGLHVHRNSAHSAGVGAIFDRVLTELVSKMRDM
QMDKTELGCLRAIVLFNPDSKGLSNPAEVEALREKVYASLEAYCKHKYPEQPGRFAKLLL
RLPALRSIGLKCLEHLFFFKLIGDTPIDTFLMEMLEAPHQMT
Target Type
Successful
Target Bioclass
Transcription factor
Family
Nuclear hormone receptor family, NR2 subfamily
Subcellular location
Nucleus
Function
Receptor for retinoic acid that acts as a transcription factor. Forms homo- or heterodimers with retinoic acid receptors (RARs) and binds to target response elements in response to their ligands, all-trans or 9-cis retinoic acid, to regulate gene expression in various biological processes. The RAR/RXR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5 to regulate transcription. The high affinity ligand for retinoid X receptors (RXRs) is 9-cis retinoic acid. In the absence of ligand, the RXR-RAR heterodimers associate with a multiprotein complex containing transcription corepressors that induce histone deacetylation, chromatin condensation and transcriptional suppression. On ligand binding, the corepressors dissociate from the receptors and coactivators are recruited leading to transcriptional activation. Serves as a common heterodimeric partner for a number of nuclear receptors, such as RARA, RARB and PPARA. The RXRA/RARB heterodimer can act as a transcriptional repressor or transcriptional activator, depending on the RARE DNA element context. The RXRA/PPARA heterodimer is required for PPARA transcriptional activity on fatty acid oxidation genes such as ACOX1 and the P450 system genes. Together with RARA, positively regulates microRNA-10a expression, thereby inhibiting the GATA6/VCAM1 signaling response to pulsatile shear stress in vascular endothelial cells. Acts as an enhancer of RARA binding to RARE DNA element. May facilitate the nuclear import of heterodimerization partners such as VDR and NR4A1. Promotes myelin debris phagocytosis and remyelination by macrophages. Plays a role in the attenuation of the innate immune system in response to viral infections, possibly by negatively regulating the transcription of antiviral genes such as type I IFN genes. Involved in the regulation of calcium signaling by repressing ITPR2 gene expression, thereby controlling cellular senescence.
TTD ID
T13726
Uniprot ID
P19793
DrugMap ID
TT6PEUO
Ensemble ID
ENST00000481739.2
HGNC ID
HGNC:10477
ChEMBL ID
CHEMBL2061

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HT1197 SNV: p.S427F DBIA    Probe Info 
Ishikawa (Heraklio) 02 ER SNV: p.T162M .
LS180 SNV: p.R25Ter .
MFE296 Deletion: p.L111WfsTer57 DBIA    Probe Info 
MFE319 SNV: p.K165N .
NUGC3 SNV: p.P50S .
WM115 SNV: p.S66L .
WM2664 SNV: p.S66L .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 7 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info 
K356(0.34)  LDD0277  [1]
BTD
 Probe Info 
C369(0.75)  LDD2109  [2]
DBIA
 Probe Info 
C135(1.14); C138(1.14); C171(1.01)  LDD0078  [3]
IA-alkyne
 Probe Info 
C369(0.00); C432(0.00)  LDD0165  [4]
TFBX
 Probe Info 
N.A.  LDD0027  [5]
IPM
 Probe Info 
N.A.  LDD2156  [6]
NAIA_5
 Probe Info 
C195(0.00); C432(0.00); C177(0.00); C404(0.00)  LDD2223  [7]

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 C369(1.16)  LDD2117  [2]
 LDCM0215  AC10 HCT 116 C135(0.92); C138(0.92); C404(0.96)  LDD0532  [3]
 LDCM0216  AC100 HCT 116 C135(1.05); C138(1.05)  LDD0533  [3]
 LDCM0217  AC101 HCT 116 C135(1.13); C138(1.13)  LDD0534  [3]
 LDCM0218  AC102 HCT 116 C135(0.95); C138(0.95)  LDD0535  [3]
 LDCM0219  AC103 HCT 116 C135(1.01); C138(1.01)  LDD0536  [3]
 LDCM0220  AC104 HCT 116 C135(1.04); C138(1.04)  LDD0537  [3]
 LDCM0221  AC105 HCT 116 C135(1.03); C138(1.03)  LDD0538  [3]
 LDCM0222  AC106 HCT 116 C135(1.16); C138(1.16)  LDD0539  [3]
 LDCM0223  AC107 HCT 116 C135(0.98); C138(0.98)  LDD0540  [3]
 LDCM0224  AC108 HCT 116 C135(1.19); C138(1.19)  LDD0541  [3]
 LDCM0225  AC109 HCT 116 C135(1.00); C138(1.00)  LDD0542  [3]
 LDCM0226  AC11 HCT 116 C135(1.18); C138(1.18); C404(1.05)  LDD0543  [3]
 LDCM0227  AC110 HCT 116 C135(1.18); C138(1.18)  LDD0544  [3]
 LDCM0228  AC111 HCT 116 C135(1.17); C138(1.17)  LDD0545  [3]
 LDCM0229  AC112 HCT 116 C135(1.22); C138(1.22)  LDD0546  [3]
 LDCM0230  AC113 HCT 116 C135(1.09); C138(1.09)  LDD0547  [3]
 LDCM0231  AC114 HCT 116 C135(0.91); C138(0.91)  LDD0548  [3]
 LDCM0232  AC115 HCT 116 C135(0.95); C138(0.95)  LDD0549  [3]
 LDCM0233  AC116 HCT 116 C135(0.91); C138(0.91)  LDD0550  [3]
 LDCM0234  AC117 HCT 116 C135(0.85); C138(0.85)  LDD0551  [3]
 LDCM0235  AC118 HCT 116 C135(1.05); C138(1.05)  LDD0552  [3]
 LDCM0236  AC119 HCT 116 C135(1.10); C138(1.10)  LDD0553  [3]
 LDCM0237  AC12 HCT 116 C135(0.93); C138(0.93); C404(0.96)  LDD0554  [3]
 LDCM0238  AC120 HCT 116 C135(0.93); C138(0.93)  LDD0555  [3]
 LDCM0239  AC121 HCT 116 C135(0.88); C138(0.88)  LDD0556  [3]
 LDCM0240  AC122 HCT 116 C135(0.94); C138(0.94)  LDD0557  [3]
 LDCM0241  AC123 HCT 116 C135(0.77); C138(0.77)  LDD0558  [3]
 LDCM0242  AC124 HCT 116 C135(0.91); C138(0.91)  LDD0559  [3]
 LDCM0243  AC125 HCT 116 C135(1.00); C138(1.00)  LDD0560  [3]
 LDCM0244  AC126 HCT 116 C135(0.99); C138(0.99)  LDD0561  [3]
 LDCM0245  AC127 HCT 116 C135(0.93); C138(0.93)  LDD0562  [3]
 LDCM0246  AC128 HCT 116 C135(0.78); C138(0.78); C404(1.28)  LDD0563  [3]
 LDCM0247  AC129 HCT 116 C135(0.82); C138(0.82); C404(1.04)  LDD0564  [3]
 LDCM0249  AC130 HCT 116 C135(0.80); C138(0.80); C404(1.16)  LDD0566  [3]
 LDCM0250  AC131 HCT 116 C135(0.82); C138(0.82); C404(1.01)  LDD0567  [3]
 LDCM0251  AC132 HCT 116 C135(0.81); C138(0.81); C404(1.32)  LDD0568  [3]
 LDCM0252  AC133 HCT 116 C135(0.88); C138(0.88); C404(1.40)  LDD0569  [3]
 LDCM0253  AC134 HCT 116 C135(0.83); C138(0.83); C404(1.37)  LDD0570  [3]
 LDCM0254  AC135 HCT 116 C135(0.87); C138(0.87); C404(1.52)  LDD0571  [3]
 LDCM0255  AC136 HCT 116 C135(0.74); C138(0.74); C404(1.29)  LDD0572  [3]
 LDCM0256  AC137 HCT 116 C135(0.76); C138(0.76); C404(1.07)  LDD0573  [3]
 LDCM0257  AC138 HCT 116 C135(0.81); C138(0.81); C404(1.19)  LDD0574  [3]
 LDCM0258  AC139 HCT 116 C135(0.86); C138(0.86); C404(1.11)  LDD0575  [3]
 LDCM0259  AC14 HCT 116 C135(0.91); C138(0.91); C404(1.31)  LDD0576  [3]
 LDCM0260  AC140 HCT 116 C135(0.96); C138(0.96); C404(1.11)  LDD0577  [3]
 LDCM0261  AC141 HCT 116 C135(0.98); C138(0.98); C404(1.10)  LDD0578  [3]
 LDCM0262  AC142 HCT 116 C135(0.82); C138(0.82); C404(1.35)  LDD0579  [3]
 LDCM0263  AC143 HCT 116 C404(1.14)  LDD0580  [3]
 LDCM0264  AC144 HCT 116 C404(0.72)  LDD0581  [3]
 LDCM0265  AC145 HCT 116 C404(0.79)  LDD0582  [3]
 LDCM0266  AC146 HCT 116 C404(0.83)  LDD0583  [3]
 LDCM0267  AC147 HCT 116 C404(0.82)  LDD0584  [3]
 LDCM0268  AC148 HCT 116 C404(0.91)  LDD0585  [3]
 LDCM0269  AC149 HCT 116 C404(0.88)  LDD0586  [3]
 LDCM0270  AC15 HCT 116 C404(0.91); C135(0.95); C138(0.95)  LDD0587  [3]
 LDCM0271  AC150 HCT 116 C404(0.84)  LDD0588  [3]
 LDCM0272  AC151 HCT 116 C404(0.83)  LDD0589  [3]
 LDCM0273  AC152 HCT 116 C404(0.82)  LDD0590  [3]
 LDCM0274  AC153 HCT 116 C404(0.96)  LDD0591  [3]
 LDCM0621  AC154 HCT 116 C404(0.75)  LDD2158  [3]
 LDCM0622  AC155 HCT 116 C404(0.80)  LDD2159  [3]
 LDCM0623  AC156 HCT 116 C404(0.90)  LDD2160  [3]
 LDCM0624  AC157 HCT 116 C404(0.84)  LDD2161  [3]
 LDCM0277  AC18 HEK-293T C195(0.94); C269(0.94)  LDD1516  [8]
 LDCM0279  AC2 HEK-293T C195(0.94); C269(0.93)  LDD1518  [8]
 LDCM0282  AC22 HEK-293T C171(0.95); C138(1.08)  LDD1521  [8]
 LDCM0283  AC23 HEK-293T C195(0.96)  LDD1522  [8]
 LDCM0285  AC25 HCT 116 C404(0.80); C135(0.98); C138(0.98)  LDD0602  [3]
 LDCM0286  AC26 HCT 116 C404(0.73); C135(1.22); C138(1.22)  LDD0603  [3]
 LDCM0287  AC27 HCT 116 C404(0.77); C135(1.06); C138(1.06)  LDD0604  [3]
 LDCM0288  AC28 HCT 116 C404(0.71); C135(1.08); C138(1.08)  LDD0605  [3]
 LDCM0289  AC29 HCT 116 C404(0.69); C135(1.21); C138(1.21)  LDD0606  [3]
 LDCM0291  AC30 HCT 116 C404(0.76); C135(1.25); C138(1.25)  LDD0608  [3]
 LDCM0292  AC31 HCT 116 C404(0.66); C135(1.20); C138(1.20)  LDD0609  [3]
 LDCM0293  AC32 HCT 116 C404(0.68); C135(1.38); C138(1.38)  LDD0610  [3]
 LDCM0294  AC33 HCT 116 C404(0.70); C135(0.98); C138(0.98)  LDD0611  [3]
 LDCM0295  AC34 HCT 116 C404(0.70); C135(0.97); C138(0.97)  LDD0612  [3]
 LDCM0299  AC38 HEK-293T C171(1.20); C138(1.07)  LDD1538  [8]
 LDCM0300  AC39 HEK-293T C195(0.94)  LDD1539  [8]
 LDCM0304  AC42 HEK-293T C195(0.98); C269(1.12)  LDD1543  [8]
 LDCM0308  AC46 HCT 116 C404(0.75)  LDD0625  [3]
 LDCM0309  AC47 HCT 116 C404(0.75)  LDD0626  [3]
 LDCM0310  AC48 HCT 116 C404(0.78)  LDD0627  [3]
 LDCM0311  AC49 HCT 116 C404(0.65)  LDD0628  [3]
 LDCM0313  AC50 HCT 116 C404(0.73)  LDD0630  [3]
 LDCM0314  AC51 HCT 116 C404(0.68)  LDD0631  [3]
 LDCM0315  AC52 HCT 116 C404(0.80)  LDD0632  [3]
 LDCM0316  AC53 HCT 116 C404(0.86)  LDD0633  [3]
 LDCM0317  AC54 HCT 116 C404(0.78)  LDD0634  [3]
 LDCM0318  AC55 HCT 116 C404(0.89)  LDD0635  [3]
 LDCM0319  AC56 HCT 116 C404(0.75)  LDD0636  [3]
 LDCM0320  AC57 HCT 116 C404(1.08)  LDD0637  [3]
 LDCM0321  AC58 HCT 116 C404(1.21)  LDD0638  [3]
 LDCM0322  AC59 HCT 116 C404(0.91)  LDD0639  [3]
 LDCM0323  AC6 HCT 116 C404(0.93); C135(1.08); C138(1.08)  LDD0640  [3]
 LDCM0324  AC60 HCT 116 C404(0.81)  LDD0641  [3]
 LDCM0325  AC61 HCT 116 C404(1.20)  LDD0642  [3]
 LDCM0326  AC62 HCT 116 C404(0.91)  LDD0643  [3]
 LDCM0327  AC63 HCT 116 C404(0.92)  LDD0644  [3]
 LDCM0328  AC64 HCT 116 C404(1.12)  LDD0645  [3]
 LDCM0329  AC65 HCT 116 C404(0.95)  LDD0646  [3]
 LDCM0330  AC66 HCT 116 C404(1.03)  LDD0647  [3]
 LDCM0331  AC67 HCT 116 C404(0.97)  LDD0648  [3]
 LDCM0334  AC7 HCT 116 C404(0.95); C135(0.99); C138(0.99)  LDD0651  [3]
 LDCM0345  AC8 HCT 116 C135(0.99); C138(0.99); C404(1.04)  LDD0662  [3]
 LDCM0349  AC83 HCT 116 C404(1.00); C135(4.16); C138(4.16)  LDD0666  [3]
 LDCM0350  AC84 HCT 116 C404(1.03); C135(3.48); C138(3.48)  LDD0667  [3]
 LDCM0351  AC85 HCT 116 C404(0.95); C135(3.56); C138(3.56)  LDD0668  [3]
 LDCM0352  AC86 HCT 116 C404(0.81); C135(4.62); C138(4.62)  LDD0669  [3]
 LDCM0353  AC87 HCT 116 C404(0.85); C135(4.16); C138(4.16)  LDD0670  [3]
 LDCM0354  AC88 HCT 116 C404(0.91); C135(3.66); C138(3.66)  LDD0671  [3]
 LDCM0355  AC89 HCT 116 C404(0.82); C135(4.95); C138(4.95)  LDD0672  [3]
 LDCM0357  AC90 HCT 116 C404(0.94); C135(4.68); C138(4.68)  LDD0674  [3]
 LDCM0358  AC91 HCT 116 C404(0.93); C135(4.50); C138(4.50)  LDD0675  [3]
 LDCM0359  AC92 HCT 116 C404(0.81); C135(4.71); C138(4.71)  LDD0676  [3]
 LDCM0360  AC93 HCT 116 C404(0.87); C135(3.21); C138(3.21)  LDD0677  [3]
 LDCM0361  AC94 HCT 116 C404(0.99); C135(3.87); C138(3.87)  LDD0678  [3]
 LDCM0362  AC95 HCT 116 C404(0.90); C135(4.77); C138(4.77)  LDD0679  [3]
 LDCM0363  AC96 HCT 116 C404(0.78); C135(3.27); C138(3.27)  LDD0680  [3]
 LDCM0364  AC97 HCT 116 C404(0.83); C135(4.79); C138(4.79)  LDD0681  [3]
 LDCM0365  AC98 HCT 116 C135(1.14); C138(1.14)  LDD0682  [3]
 LDCM0366  AC99 HCT 116 C135(0.98); C138(0.98)  LDD0683  [3]
 LDCM0248  AKOS034007472 HCT 116 C135(0.89); C138(0.89); C404(1.09)  LDD0565  [3]
 LDCM0356  AKOS034007680 HCT 116 C135(0.95); C138(0.95); C404(1.59)  LDD0673  [3]
 LDCM0275  AKOS034007705 HCT 116 C135(0.97); C138(0.97); C404(1.02)  LDD0592  [3]
 LDCM0020  ARS-1620 HCC44 C135(1.14); C138(1.14); C171(1.01)  LDD0078  [3]
 LDCM0632  CL-Sc Hep-G2 C432(2.17)  LDD2227  [7]
 LDCM0368  CL10 HEK-293T C171(1.12); C138(1.30)  LDD1572  [8]
 LDCM0369  CL100 HEK-293T C195(0.92)  LDD1573  [8]
 LDCM0370  CL101 HCT 116 C404(0.95); C135(0.96); C138(0.96)  LDD0687  [3]
 LDCM0371  CL102 HCT 116 C135(0.95); C138(0.95); C404(1.07)  LDD0688  [3]
 LDCM0372  CL103 HCT 116 C135(1.01); C138(1.01); C404(1.06)  LDD0689  [3]
 LDCM0373  CL104 HCT 116 C404(0.90); C135(1.00); C138(1.00)  LDD0690  [3]
 LDCM0375  CL106 HEK-293T C195(0.85)  LDD1579  [8]
 LDCM0377  CL108 HEK-293T C195(1.05)  LDD1581  [8]
 LDCM0379  CL11 HEK-293T C195(0.90)  LDD1583  [8]
 LDCM0380  CL110 HEK-293T C195(0.79)  LDD1584  [8]
 LDCM0382  CL112 HCT 116 C404(0.94); C135(0.95); C138(0.95)  LDD0699  [3]
 LDCM0383  CL113 HCT 116 C404(0.72); C135(1.29); C138(1.29)  LDD0700  [3]
 LDCM0384  CL114 HCT 116 C404(0.77); C135(1.17); C138(1.17)  LDD0701  [3]
 LDCM0385  CL115 HCT 116 C404(0.75); C135(1.10); C138(1.10)  LDD0702  [3]
 LDCM0386  CL116 HCT 116 C404(0.71); C135(1.10); C138(1.10)  LDD0703  [3]
 LDCM0388  CL118 HEK-293T C195(0.95)  LDD1592  [8]
 LDCM0391  CL120 HEK-293T C195(0.98)  LDD1595  [8]
 LDCM0392  CL121 HCT 116 C404(0.80)  LDD0709  [3]
 LDCM0393  CL122 HCT 116 C404(0.85)  LDD0710  [3]
 LDCM0394  CL123 HCT 116 C404(0.85)  LDD0711  [3]
 LDCM0395  CL124 HCT 116 C404(0.79)  LDD0712  [3]
 LDCM0396  CL125 HCT 116 C404(1.21)  LDD0713  [3]
 LDCM0397  CL126 HCT 116 C404(0.84)  LDD0714  [3]
 LDCM0398  CL127 HCT 116 C404(0.96)  LDD0715  [3]
 LDCM0399  CL128 HCT 116 C404(1.41)  LDD0716  [3]
 LDCM0401  CL14 HEK-293T C195(0.87)  LDD1605  [8]
 LDCM0403  CL16 HCT 116 C135(1.12); C138(1.12)  LDD0720  [3]
 LDCM0404  CL17 HCT 116 C135(0.84); C138(0.84)  LDD0721  [3]
 LDCM0405  CL18 HCT 116 C135(1.14); C138(1.14)  LDD0722  [3]
 LDCM0406  CL19 HCT 116 C135(0.99); C138(0.99)  LDD0723  [3]
 LDCM0407  CL2 HEK-293T C195(0.91)  LDD1611  [8]
 LDCM0408  CL20 HCT 116 C135(0.97); C138(0.97)  LDD0725  [3]
 LDCM0409  CL21 HCT 116 C135(0.77); C138(0.77)  LDD0726  [3]
 LDCM0410  CL22 HCT 116 C135(0.98); C138(0.98)  LDD0727  [3]
 LDCM0411  CL23 HCT 116 C135(0.99); C138(0.99)  LDD0728  [3]
 LDCM0412  CL24 HCT 116 C135(1.11); C138(1.11)  LDD0729  [3]
 LDCM0413  CL25 HCT 116 C135(1.25); C138(1.25)  LDD0730  [3]
 LDCM0414  CL26 HCT 116 C135(1.04); C138(1.04)  LDD0731  [3]
 LDCM0415  CL27 HCT 116 C135(1.12); C138(1.12)  LDD0732  [3]
 LDCM0416  CL28 HCT 116 C135(1.12); C138(1.12)  LDD0733  [3]
 LDCM0417  CL29 HCT 116 C135(1.12); C138(1.12)  LDD0734  [3]
 LDCM0419  CL30 HCT 116 C135(1.16); C138(1.16)  LDD0736  [3]
 LDCM0423  CL34 HEK-293T C171(1.08); C138(1.25)  LDD1627  [8]
 LDCM0424  CL35 HEK-293T C195(1.01)  LDD1628  [8]
 LDCM0429  CL4 HEK-293T C195(0.94)  LDD1633  [8]
 LDCM0430  CL40 HEK-293T C195(0.99)  LDD1634  [8]
 LDCM0432  CL42 HEK-293T C195(0.97); C269(0.83)  LDD1636  [8]
 LDCM0436  CL46 HCT 116 C135(0.85); C138(0.85)  LDD0753  [3]
 LDCM0437  CL47 HCT 116 C135(0.85); C138(0.85)  LDD0754  [3]
 LDCM0438  CL48 HCT 116 C135(0.80); C138(0.80)  LDD0755  [3]
 LDCM0439  CL49 HCT 116 C135(0.75); C138(0.75)  LDD0756  [3]
 LDCM0441  CL50 HCT 116 C135(0.84); C138(0.84)  LDD0758  [3]
 LDCM0442  CL51 HCT 116 C135(0.85); C138(0.85)  LDD0759  [3]
 LDCM0443  CL52 HCT 116 C135(0.87); C138(0.87)  LDD0760  [3]
 LDCM0444  CL53 HCT 116 C135(0.88); C138(0.88)  LDD0761  [3]
 LDCM0445  CL54 HCT 116 C135(0.89); C138(0.89)  LDD0762  [3]
 LDCM0446  CL55 HCT 116 C135(1.00); C138(1.00)  LDD0763  [3]
 LDCM0447  CL56 HCT 116 C135(0.83); C138(0.83)  LDD0764  [3]
 LDCM0448  CL57 HCT 116 C135(0.73); C138(0.73)  LDD0765  [3]
 LDCM0449  CL58 HCT 116 C135(0.93); C138(0.93)  LDD0766  [3]
 LDCM0450  CL59 HCT 116 C135(1.02); C138(1.02)  LDD0767  [3]
 LDCM0451  CL6 HEK-293T C195(0.89); C269(1.52)  LDD1654  [8]
 LDCM0452  CL60 HCT 116 C135(0.92); C138(0.92)  LDD0769  [3]
 LDCM0453  CL61 HCT 116 C135(0.62); C138(0.62); C404(1.00)  LDD0770  [3]
 LDCM0454  CL62 HCT 116 C135(1.12); C138(1.12); C404(1.02)  LDD0771  [3]
 LDCM0455  CL63 HCT 116 C135(0.98); C138(0.98); C404(0.88)  LDD0772  [3]
 LDCM0456  CL64 HCT 116 C135(0.69); C138(0.69); C404(0.83)  LDD0773  [3]
 LDCM0457  CL65 HCT 116 C135(0.83); C138(0.83); C404(0.92)  LDD0774  [3]
 LDCM0458  CL66 HCT 116 C135(0.90); C138(0.90); C404(0.93)  LDD0775  [3]
 LDCM0459  CL67 HCT 116 C135(0.58); C138(0.58); C404(0.97)  LDD0776  [3]
 LDCM0460  CL68 HCT 116 C135(0.58); C138(0.58); C404(0.93)  LDD0777  [3]
 LDCM0461  CL69 HCT 116 C135(0.74); C138(0.74); C404(0.92)  LDD0778  [3]
 LDCM0463  CL70 HCT 116 C135(0.45); C138(0.45); C404(0.84)  LDD0780  [3]
 LDCM0464  CL71 HCT 116 C135(0.66); C138(0.66); C404(0.86)  LDD0781  [3]
 LDCM0465  CL72 HCT 116 C135(0.78); C138(0.78); C404(1.10)  LDD0782  [3]
 LDCM0466  CL73 HCT 116 C135(1.27); C138(1.27); C404(0.90)  LDD0783  [3]
 LDCM0467  CL74 HCT 116 C135(0.66); C138(0.66); C404(0.93)  LDD0784  [3]
 LDCM0469  CL76 HCT 116 C135(0.81); C138(0.81)  LDD0786  [3]
 LDCM0470  CL77 HCT 116 C135(0.67); C138(0.67)  LDD0787  [3]
 LDCM0471  CL78 HCT 116 C135(0.89); C138(0.89)  LDD0788  [3]
 LDCM0472  CL79 HCT 116 C135(0.79); C138(0.79)  LDD0789  [3]
 LDCM0474  CL80 HCT 116 C135(0.81); C138(0.81)  LDD0791  [3]
 LDCM0475  CL81 HCT 116 C135(0.70); C138(0.70)  LDD0792  [3]
 LDCM0476  CL82 HCT 116 C135(0.69); C138(0.69)  LDD0793  [3]
 LDCM0477  CL83 HCT 116 C135(0.79); C138(0.79)  LDD0794  [3]
 LDCM0478  CL84 HCT 116 C135(0.90); C138(0.90)  LDD0795  [3]
 LDCM0479  CL85 HCT 116 C135(0.99); C138(0.99)  LDD0796  [3]
 LDCM0480  CL86 HCT 116 C135(0.72); C138(0.72)  LDD0797  [3]
 LDCM0481  CL87 HCT 116 C135(0.73); C138(0.73)  LDD0798  [3]
 LDCM0482  CL88 HCT 116 C135(0.74); C138(0.74)  LDD0799  [3]
 LDCM0483  CL89 HCT 116 C135(0.89); C138(0.89)  LDD0800  [3]
 LDCM0485  CL90 HCT 116 C135(0.65); C138(0.65)  LDD0802  [3]
 LDCM0489  CL94 HEK-293T C171(1.12); C138(1.24)  LDD1692  [8]
 LDCM0490  CL95 HEK-293T C195(0.89)  LDD1693  [8]
 LDCM0493  CL98 HEK-293T C195(0.96)  LDD1696  [8]
 LDCM0468  Fragment33 HCT 116 C135(0.63); C138(0.63); C404(0.95)  LDD0785  [3]
 LDCM0427  Fragment51 HEK-293T C195(0.95)  LDD1631  [8]
 LDCM0022  KB02 HCT 116 C138(1.44); C135(1.44); C171(1.19)  LDD0080  [3]
 LDCM0023  KB03 HCT 116 C138(1.98); C135(1.98); C171(1.23)  LDD0081  [3]
 LDCM0024  KB05 HCT 116 C138(1.48); C135(1.48); C171(1.32)  LDD0082  [3]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C369(0.75)  LDD2109  [2]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C369(0.83)  LDD2125  [2]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C369(1.06)  LDD2136  [2]

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
Nuclear receptor coactivator 1 (NCOA1) SRC/p160 nuclear receptor coactivator family Q15788
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Oxysterols receptor LXR-alpha (NR1H3) Nuclear hormone receptor family Q13133
Vitamin D3 receptor (VDR) Nuclear hormone receptor family P11473
Transcription factor
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Oxysterols receptor LXR-beta (NR1H2) Nuclear hormone receptor family P55055
Peroxisome proliferator-activated receptor gamma (PPARG) Nuclear hormone receptor family P37231
Retinoic acid receptor alpha (RARA) Nuclear hormone receptor family P10276
Nuclear receptor coactivator 2 (NCOA2) SRC/p160 nuclear receptor coactivator family Q15596
Signal transducer and activator of transcription 1-alpha/beta (STAT1) Transcription factor STAT family P42224
Class E basic helix-loop-helix protein 40 (BHLHE40) . O14503
Other
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Mediator of RNA polymerase II transcription subunit 1 (MED1) Mediator complex subunit 1 family Q15648
Mediator of RNA polymerase II transcription subunit 25 (MED25) Mediator complex subunit 25 family Q71SY5
Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1) PI3K p85 subunit family P27986
RNA-binding protein FUS (FUS) RRM TET family P35637

The Drug(s) Related To This Target

Approved
Click To Hide/Show 12 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Acitretin Small molecular drug DB00459
Adapalene Small molecular drug DB00210
Alfacalcidol Small molecular drug DB01436
Alitretinoin Small molecular drug D0G3PI
Alpha-linolenic Acid Small molecular drug DB00132
Bexarotene Small molecular drug D0N0RU
Bezafibrate Small molecular drug DB01393
Doconexent Small molecular drug DB03756
Etodolac Small molecular drug DB00749
Oleic Acid Small molecular drug DB04224
Rosiglitazone Small molecular drug DB00412
Tretinoin Small molecular drug DB00755
Investigative
Click To Hide/Show 17 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(5beta)-pregnane-3,20-dione Small molecular drug D05DMH
2-chloro-5-nitro-n-phenylbenzamide Small molecular drug D00ACX
320-pregnanedione Small molecular drug DB07557
Agn-34 Small molecular drug D0GR9O
Arachidonic Acid Small molecular drug DB04557
Cd3254 Small molecular drug D03ZEL
Evt-101 Small molecular drug DB05956
Lg100754 Small molecular drug D0Q9FZ
Methoprene Acid Small molecular drug D0CT1F
Pa451 Small molecular drug D0IY9H
Phthalic Acid Small molecular drug DB02746
Phytanic Acid Small molecular drug D05JXE
Tributylstannanyl Small molecular drug D0CQ3A
Tributyltin Small molecular drug DB08601
Uvi3003 Small molecular drug D09IEN
1-benzyl-3-(4-methoxyphenylamino)-4-phenylpyrrole-25-dione . DB08063
2-[(24-dichlorobenzoyl)Amino]-5-(Pyrimidin-2-yloxy)Benzoic Acid . DB08402
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Etretinate Small molecular drug DB00926

References

1 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
2 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
3 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
4 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
5 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
6 Benchmarking Cleavable Biotin Tags for Peptide-Centric Chemoproteomics. J Proteome Res. 2022 May 6;21(5):1349-1358. doi: 10.1021/acs.jproteome.2c00174. Epub 2022 Apr 25.
Mass spectrometry data entry: PXD031019
7 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
8 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