Details of the Target

General Information of Target

Target ID LDTP00351
Target Name Class E basic helix-loop-helix protein 40 (BHLHE40)
Gene Name BHLHE40
Gene ID 8553
Synonyms
BHLHB2; DEC1; SHARP2; STRA13; Class E basic helix-loop-helix protein 40; bHLHe40; Class B basic helix-loop-helix protein 2; bHLHb2; Differentially expressed in chondrocytes protein 1; DEC1; Enhancer-of-split and hairy-related protein 2; SHARP-2; Stimulated by retinoic acid gene 13 protein
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MERIPSAQPPPACLPKAPGLEHGDLPGMYPAHMYQVYKSRRGIKRSEDSKETYKLPHRLI
EKKRRDRINECIAQLKDLLPEHLKLTTLGHLEKAVVLELTLKHVKALTNLIDQQQQKIIA
LQSGLQAGELSGRNVETGQEMFCSGFQTCAREVLQYLAKHENTRDLKSSQLVTHLHRVVS
ELLQGGTSRKPSDPAPKVMDFKEKPSSPAKGSEGPGKNCVPVIQRTFAHSSGEQSGSDTD
TDSGYGGESEKGDLRSEQPCFKSDHGRRFTMGERIGAIKQESEEPPTKKNRMQLSDDEGH
FTSSDLISSPFLGPHPHQPPFCLPFYLIPPSATAYLPMLEKCWYPTSVPVLYPGLNASAA
ALSSFMNPDKISAPLLMPQRLPSPLPAHPSVDSSVLLQALKPIPPLNLETKD
Target Bioclass
Transcription factor
Subcellular location
Cytoplasm
Function
Transcriptional repressor involved in the regulation of the circadian rhythm by negatively regulating the activity of the clock genes and clock-controlled genes. Acts as the negative limb of a novel autoregulatory feedback loop (DEC loop) which differs from the one formed by the PER and CRY transcriptional repressors (PER/CRY loop). Both these loops are interlocked as it represses the expression of PER1/2 and in turn is repressed by PER1/2 and CRY1/2. Represses the activity of the circadian transcriptional activator: CLOCK-BMAL1|BMAL2 heterodimer by competing for the binding to E-box elements (5'-CACGTG-3') found within the promoters of its target genes. Negatively regulates its own expression and the expression of DBP and BHLHE41/DEC2. Acts as a corepressor of RXR and the RXR-LXR heterodimers and represses the ligand-induced RXRA and NR1H3/LXRA transactivation activity. May be involved in the regulation of chondrocyte differentiation via the cAMP pathway. Represses the transcription of NR0B2 and attentuates the transactivation of NR0B2 by the CLOCK-BMAL1 complex. Drives the circadian rhythm of blood pressure through transcriptional repression of ATP1B1 in the cardiovascular system.
Uniprot ID
O14503
Ensemble ID
ENST00000256495.4
HGNC ID
HGNC:1046

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C13(2.93)  LDD3419  [1]
Alkyne-RA190
 Probe Info  		2.10  LDD0303  [2]
IA-alkyne
 Probe Info  		C219(5.09)  LDD1706  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0216  AC100 PaTu 8988t C143(1.12); C149(1.12)  LDD1095  [4]
 LDCM0217  AC101 PaTu 8988t C143(1.15); C149(1.15)  LDD1096  [4]
 LDCM0218  AC102 PaTu 8988t C143(1.11); C149(1.11)  LDD1097  [4]
 LDCM0219  AC103 PaTu 8988t C143(1.21); C149(1.21)  LDD1098  [4]
 LDCM0220  AC104 PaTu 8988t C143(1.06); C149(1.06)  LDD1099  [4]
 LDCM0221  AC105 PaTu 8988t C143(1.12); C149(1.12)  LDD1100  [4]
 LDCM0222  AC106 PaTu 8988t C143(1.28); C149(1.28)  LDD1101  [4]
 LDCM0223  AC107 PaTu 8988t C143(1.05); C149(1.05)  LDD1102  [4]
 LDCM0224  AC108 PaTu 8988t C143(1.08); C149(1.08)  LDD1103  [4]
 LDCM0225  AC109 PaTu 8988t C143(1.29); C149(1.29)  LDD1104  [4]
 LDCM0227  AC110 PaTu 8988t C143(1.11); C149(1.11)  LDD1106  [4]
 LDCM0228  AC111 PaTu 8988t C143(1.50); C149(1.50)  LDD1107  [4]
 LDCM0229  AC112 PaTu 8988t C143(1.12); C149(1.12)  LDD1108  [4]
 LDCM0230  AC113 PaTu 8988t C143(0.93); C149(0.93)  LDD1109  [4]
 LDCM0231  AC114 PaTu 8988t C143(1.03); C149(1.03)  LDD1110  [4]
 LDCM0232  AC115 PaTu 8988t C143(1.24); C149(1.24)  LDD1111  [4]
 LDCM0233  AC116 PaTu 8988t C143(0.91); C149(0.91)  LDD1112  [4]
 LDCM0234  AC117 PaTu 8988t C143(0.88); C149(0.88)  LDD1113  [4]
 LDCM0235  AC118 PaTu 8988t C143(1.39); C149(1.39)  LDD1114  [4]
 LDCM0236  AC119 PaTu 8988t C143(0.89); C149(0.89)  LDD1115  [4]
 LDCM0238  AC120 PaTu 8988t C143(0.70); C149(0.70)  LDD1117  [4]
 LDCM0239  AC121 PaTu 8988t C143(0.80); C149(0.80)  LDD1118  [4]
 LDCM0240  AC122 PaTu 8988t C143(0.89); C149(0.89)  LDD1119  [4]
 LDCM0241  AC123 PaTu 8988t C143(0.73); C149(0.73)  LDD1120  [4]
 LDCM0242  AC124 PaTu 8988t C143(1.05); C149(1.05)  LDD1121  [4]
 LDCM0243  AC125 PaTu 8988t C143(1.53); C149(1.53)  LDD1122  [4]
 LDCM0244  AC126 PaTu 8988t C143(1.07); C149(1.07)  LDD1123  [4]
 LDCM0245  AC127 PaTu 8988t C143(0.91); C149(0.91)  LDD1124  [4]
 LDCM0246  AC128 PaTu 8988t C143(1.17); C149(1.17)  LDD1125  [4]
 LDCM0247  AC129 PaTu 8988t C143(1.09); C149(1.09)  LDD1126  [4]
 LDCM0249  AC130 PaTu 8988t C143(0.95); C149(0.95)  LDD1128  [4]
 LDCM0250  AC131 PaTu 8988t C143(1.15); C149(1.15)  LDD1129  [4]
 LDCM0251  AC132 PaTu 8988t C143(1.00); C149(1.00)  LDD1130  [4]
 LDCM0252  AC133 PaTu 8988t C143(1.18); C149(1.18)  LDD1131  [4]
 LDCM0253  AC134 PaTu 8988t C143(0.97); C149(0.97)  LDD1132  [4]
 LDCM0254  AC135 PaTu 8988t C143(1.04); C149(1.04)  LDD1133  [4]
 LDCM0255  AC136 PaTu 8988t C143(1.15); C149(1.15)  LDD1134  [4]
 LDCM0256  AC137 PaTu 8988t C143(1.13); C149(1.13)  LDD1135  [4]
 LDCM0257  AC138 PaTu 8988t C143(1.09); C149(1.09)  LDD1136  [4]
 LDCM0258  AC139 PaTu 8988t C143(1.07); C149(1.07)  LDD1137  [4]
 LDCM0260  AC140 PaTu 8988t C143(1.19); C149(1.19)  LDD1139  [4]
 LDCM0261  AC141 PaTu 8988t C143(1.12); C149(1.12)  LDD1140  [4]
 LDCM0262  AC142 PaTu 8988t C143(1.15); C149(1.15)  LDD1141  [4]
 LDCM0263  AC143 PaTu 8988t C143(1.06); C149(1.06)  LDD1142  [4]
 LDCM0264  AC144 PaTu 8988t C143(1.12); C149(1.12)  LDD1143  [4]
 LDCM0265  AC145 PaTu 8988t C143(1.24); C149(1.24)  LDD1144  [4]
 LDCM0266  AC146 PaTu 8988t C143(1.00); C149(1.00)  LDD1145  [4]
 LDCM0267  AC147 PaTu 8988t C143(1.26); C149(1.26)  LDD1146  [4]
 LDCM0268  AC148 PaTu 8988t C143(1.00); C149(1.00)  LDD1147  [4]
 LDCM0269  AC149 PaTu 8988t C143(1.28); C149(1.28)  LDD1148  [4]
 LDCM0271  AC150 PaTu 8988t C143(1.57); C149(1.57)  LDD1150  [4]
 LDCM0272  AC151 PaTu 8988t C143(1.77); C149(1.77)  LDD1151  [4]
 LDCM0273  AC152 PaTu 8988t C143(1.52); C149(1.52)  LDD1152  [4]
 LDCM0274  AC153 PaTu 8988t C143(1.75); C149(1.75)  LDD1153  [4]
 LDCM0621  AC154 PaTu 8988t C143(2.17); C149(2.17)  LDD2166  [4]
 LDCM0622  AC155 PaTu 8988t C143(1.87); C149(1.87)  LDD2167  [4]
 LDCM0623  AC156 PaTu 8988t C143(1.62); C149(1.62)  LDD2168  [4]
 LDCM0624  AC157 PaTu 8988t C143(1.71); C149(1.71)  LDD2169  [4]
 LDCM0276  AC17 PaTu 8988t C143(1.39); C149(1.39)  LDD1155  [4]
 LDCM0277  AC18 PaTu 8988t C143(0.87); C149(0.87)  LDD1156  [4]
 LDCM0278  AC19 PaTu 8988t C143(0.93); C149(0.93)  LDD1157  [4]
 LDCM0280  AC20 PaTu 8988t C143(0.98); C149(0.98)  LDD1159  [4]
 LDCM0281  AC21 PaTu 8988t C143(0.95); C149(0.95)  LDD1160  [4]
 LDCM0282  AC22 PaTu 8988t C143(1.10); C149(1.10)  LDD1161  [4]
 LDCM0283  AC23 PaTu 8988t C143(1.03); C149(1.03)  LDD1162  [4]
 LDCM0284  AC24 PaTu 8988t C143(1.08); C149(1.08)  LDD1163  [4]
 LDCM0365  AC98 PaTu 8988t C143(1.20); C149(1.20)  LDD1244  [4]
 LDCM0366  AC99 PaTu 8988t C143(1.09); C149(1.09)  LDD1245  [4]
 LDCM0374  CL105 PaTu 8988t C143(0.83); C149(0.83)  LDD1253  [4]
 LDCM0375  CL106 PaTu 8988t C143(1.15); C149(1.15)  LDD1254  [4]
 LDCM0376  CL107 PaTu 8988t C143(1.05); C149(1.05)  LDD1255  [4]
 LDCM0377  CL108 PaTu 8988t C143(0.83); C149(0.83)  LDD1256  [4]
 LDCM0378  CL109 PaTu 8988t C143(1.14); C149(1.14)  LDD1257  [4]
 LDCM0380  CL110 PaTu 8988t C143(1.26); C149(1.26)  LDD1259  [4]
 LDCM0381  CL111 PaTu 8988t C143(1.25); C149(1.25)  LDD1260  [4]
 LDCM0420  CL31 PaTu 8988t C143(1.19); C149(1.19)  LDD1299  [4]
 LDCM0421  CL32 PaTu 8988t C143(1.76); C149(1.76)  LDD1300  [4]
 LDCM0422  CL33 PaTu 8988t C143(1.67); C149(1.67)  LDD1301  [4]
 LDCM0423  CL34 PaTu 8988t C143(1.22); C149(1.22)  LDD1302  [4]
 LDCM0424  CL35 PaTu 8988t C143(1.43); C149(1.43)  LDD1303  [4]
 LDCM0425  CL36 PaTu 8988t C143(1.23); C149(1.23)  LDD1304  [4]
 LDCM0426  CL37 PaTu 8988t C143(1.86); C149(1.86)  LDD1305  [4]
 LDCM0428  CL39 PaTu 8988t C143(1.79); C149(1.79)  LDD1307  [4]
 LDCM0430  CL40 PaTu 8988t C143(1.63); C149(1.63)  LDD1309  [4]
 LDCM0431  CL41 PaTu 8988t C143(1.49); C149(1.49)  LDD1310  [4]
 LDCM0432  CL42 PaTu 8988t C143(1.93); C149(1.93)  LDD1311  [4]
 LDCM0433  CL43 PaTu 8988t C143(2.27); C149(2.27)  LDD1312  [4]
 LDCM0434  CL44 PaTu 8988t C143(1.53); C149(1.53)  LDD1313  [4]
 LDCM0435  CL45 PaTu 8988t C143(2.04); C149(2.04)  LDD1314  [4]
 LDCM0469  CL76 PaTu 8988t C143(1.82); C149(1.82)  LDD1348  [4]
 LDCM0470  CL77 PaTu 8988t C143(1.52); C149(1.52)  LDD1349  [4]
 LDCM0471  CL78 PaTu 8988t C143(1.01); C149(1.01)  LDD1350  [4]
 LDCM0472  CL79 PaTu 8988t C143(0.96); C149(0.96)  LDD1351  [4]
 LDCM0474  CL80 PaTu 8988t C143(1.19); C149(1.19)  LDD1353  [4]
 LDCM0475  CL81 PaTu 8988t C143(1.02); C149(1.02)  LDD1354  [4]
 LDCM0476  CL82 PaTu 8988t C143(0.98); C149(0.98)  LDD1355  [4]
 LDCM0477  CL83 PaTu 8988t C143(1.12); C149(1.12)  LDD1356  [4]
 LDCM0478  CL84 PaTu 8988t C143(1.15); C149(1.15)  LDD1357  [4]
 LDCM0479  CL85 PaTu 8988t C143(1.06); C149(1.06)  LDD1358  [4]
 LDCM0480  CL86 PaTu 8988t C143(2.10); C149(2.10)  LDD1359  [4]
 LDCM0481  CL87 PaTu 8988t C143(1.34); C149(1.34)  LDD1360  [4]
 LDCM0482  CL88 PaTu 8988t C143(1.29); C149(1.29)  LDD1361  [4]
 LDCM0483  CL89 PaTu 8988t C143(0.96); C149(0.96)  LDD1362  [4]
 LDCM0485  CL90 PaTu 8988t C143(1.14); C149(1.14)  LDD1364  [4]
 LDCM0427  Fragment51 PaTu 8988t C143(1.72); C149(1.72)  LDD1306  [4]
 LDCM0022  KB02 BRX211 C13(2.55); C219(1.74)  LDD2268  [1]
 LDCM0023  KB03 BRX211 C13(5.87)  LDD2685  [1]
 LDCM0024  KB05 SH-4 C13(2.93)  LDD3419  [1]
 LDCM0131  RA190 SK-MEL-5 2.10  LDD0303  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 14 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Serotonin N-acetyltransferase (AANAT) Acetyltransferase family Q16613
N-alpha-acetyltransferase 50 (NAA50) Acetyltransferase family Q9GZZ1
Histone-lysine N-methyltransferase SMYD1 (SMYD1) Class V-like SAM-binding methyltransferase superfamily Q8NB12
Thioredoxin-like protein 4B (TXNL4B) DIM1 family Q9NX01
Peroxisomal bifunctional enzyme (EHHADH) Enoyl-CoA hydratase/isomerase family; 3-hydroxyacyl-CoA dehydrogenase family Q08426
5'-AMP-activated protein kinase catalytic subunit alpha-1 (PRKAA1) CAMK Ser/Thr protein kinase family Q13131
Tyrosine-protein kinase transmembrane receptor ROR2 (ROR2) Tyr protein kinase family Q01974
Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma (PDE6G) Rod/cone cGMP-PDE gamma subunit family P18545
Rho-related GTP-binding protein RhoJ (RHOJ) Rho family Q9H4E5
Helicase ARIP4 (RAD54L2) SNF2/RAD54 helicase family Q9Y4B4
Terminal nucleotidyltransferase 5B (TENT5B) TENT family Q96A09
SUMO-conjugating enzyme UBC9 (UBE2I) Ubiquitin-conjugating enzyme family P63279
Germ cell-less protein-like 2 (GMCL2) . Q8NEA9
Rho-related BTB domain-containing protein 3 (RHOBTB3) . O94955
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cytochrome c oxidase subunit 5B, mitochondrial (COX5B) Cytochrome c oxidase subunit 5B family P10606
Cellular tumor antigen p53 (TP53) P53 family P04637
Transcription factor
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Retinoic acid receptor RXR-alpha (RXRA) Nuclear hormone receptor family P19793
PHD finger protein 1 (PHF1) Polycomblike family O43189
POU domain, class 6, transcription factor 2 (POU6F2) POU transcription factor family P78424
Homeobox protein VENTX (VENTX) . O95231
Protein SOX-15 (SOX15) . O60248
Other
Click To Hide/Show 31 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Ataxin-1 (ATXN1) ATXN1 family P54253
Protein Tob2 (TOB2) BTG family Q14106
Bystin (BYSL) Bystin family Q13895
Nucleolar complex protein 4 homolog (NOC4L) CBF/MAK21 family Q9BVI4
Cysteine-rich DPF motif domain-containing protein 1 (CDPF1) CDPF1 family Q6NVV7
Cyclin-K (CCNK) Cyclin family O75909
Segment polarity protein dishevelled homolog DVL-3 (DVL3) DSH family Q92997
Protein FAM83A (FAM83A) FAM83 family Q86UY5
Keratin-associated protein 1-3 (KRTAP1-3) KRTAP type 1 family Q8IUG1
Keratin-associated protein 19-1 (KRTAP19-1) KRTAP type 19 family Q8IUB9
Keratin-associated protein 19-5 (KRTAP19-5) KRTAP type 19 family Q3LI72
Keratin-associated protein 19-7 (KRTAP19-7) KRTAP type 19 family Q3SYF9
Keratin-associated protein 6-1 (KRTAP6-1) KRTAP type 6 family Q3LI64
Keratin-associated protein 6-2 (KRTAP6-2) KRTAP type 6 family Q3LI66
Keratin-associated protein 8-1 (KRTAP8-1) KRTAP type 8 family Q8IUC2
Prefoldin subunit 5 (PFDN5) Prefoldin subunit alpha family Q99471
Proline-rich protein 20D (PRR20D) PRR20 family P86480
Probable RNA-binding protein 23 (RBM23) Splicing factor SR family Q86U06
Protein VAC14 homolog (VAC14) VAC14 family Q08AM6
TLE family member 5 (TLE5) WD repeat Groucho/TLE family Q08117
DAZ-associated protein 2 (DAZAP2) . Q15038
Disabled homolog 1 (DAB1) . O75553
Kelch domain-containing protein 7B (KLHDC7B) . Q96G42
Keratin-associated protein 23-1 (KRTAP23-1) . A1A580
Melanoma-associated antigen D1 (MAGED1) . Q9Y5V3
Microspherule protein 1 (MCRS1) . Q96EZ8
Pleckstrin homology domain-containing family B member 2 (PLEKHB2) . Q96CS7
RNA-binding protein with multiple splicing (RBPMS) . Q93062
RNA-binding protein with multiple splicing 2 (RBPMS2) . Q6ZRY4
Stromal membrane-associated protein 2 (SMAP2) . Q8WU79
Tetratricopeptide repeat protein 23 (TTC23) . Q5W5X9

References

1 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
2 Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190. Cell Chem Biol. 2020 Nov 19;27(11):1371-1382.e6. doi: 10.1016/j.chembiol.2020.08.007. Epub 2020 Aug 27.
3 An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.
4 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.