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Target
Protein-glutamine gamma-glutamyltransferase 2/Receptor protein-tyrosine kinase
Ligand
BDBM4363
Substrate
n/a
Meas. Tech.
BP Incorporation Assay
Temperature
310.15±0 K
IC50
3e+3± 3e+3 nM
Citation
 Lai, TS; Liu, Y; Tucker, T; Daniel, KR; Sane, DC; Toone, E; Burke, JR; Strittmatter, WJ; Greenberg, CS Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug libraries. Chem Biol 15:969-78 (2008) [PubMed]  Article 
Target
Name:
Protein-glutamine gamma-glutamyltransferase 2/Receptor protein-tyrosine kinase
Synonyms:
TGM2/ EGFR
Type:
Protein
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
Protein-glutamine gamma-glutamyltransferase 2
Synonyms:
Protein-glutamine gamma-glutamyltransferase | Protein-glutamine gamma-glutamyltransferase 2 (TG2) | TGM2 | TGM2_HUMAN | Tissue transglutaminase | Tissue transglutaminase (TG2) | Transglutaminase 2 (TGM2) | Transglutaminase C | Transglutaminase-2
Type:
Protein
Mol. Mass.:
77309.30
Organism:
Homo sapiens (Human)
Description:
P21980
Residue:
687
Sequence:
MAEELVLERCDLELETNGRDHHTADLCREKLVVRRGQPFWLTLHFEGRNYEASVDSLTFSVVTGPAPSQEAGTKARFPLRDAVEEGDWTATVVDQQDCTLSLQLTTPANAPIGLYRLSLEASTGYQGSSFVLGHFILLFNAWCPADAVYLDSEEERQEYVLTQQGFIYQGSAKFIKNIPWNFGQFEDGILDICLILLDVNPKFLKNAGRDCSRRSSPVYVGRVVSGMVNCNDDQGVLLGRWDNNYGDGVSPMSWIGSVDILRRWKNHGCQRVKYGQCWVFAAVACTVLRCLGIPTRVVTNYNSAHDQNSNLLIEYFRNEFGEIQGDKSEMIWNFHCWVESWMTRPDLQPGYEGWQALDPTPQEKSEGTYCCGPVPVRAIKEGDLSTKYDAPFVFAEVNADVVDWIQQDDGSVHKSINRSLIVGLKISTKSVGRDEREDITHTYKYPEGSSEEREAFTRANHLNKLAEKEETGMAMRIRVGQSMNMGSDFDVFAHITNNTAEEYVCRLLLCARTVSYNGILGPECGTKYLLNLNLEPFSEKSVPLCILYEKYRDCLTESNLIKVRALLVEPVINSYLLAERDLYLENPEIKIRILGEPKQKRKLVAEVSLQNPLPVALEGCTFTVEGAGLTEEQKTVEIPDPVEAGEEVKVRMDLLPLHMGLHKLVVNFESDKLKAVKGFRNVIIGPA
  
Component 2
Name:
Receptor protein-tyrosine kinase
Synonyms:
EGFR | Q504U8_HUMAN
Type:
Protein
Mol. Mass.:
120695.83
Organism:
Homo sapiens (Human)
Description:
Q504U8
Residue:
1091
Sequence:
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQGQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFKNCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAFENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKLFGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCNLLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVMGENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVVALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSIDDTFLPVPGEWLVWKQSCSSTSSTHSAAASLQCPSQVLPPASPEGETVADLQTQ
  
Inhibitor
Name:
BDBM4363
Synonyms:
(2E)-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enethioamide | AG 213 | CHEMBL77030 | RG-50864 | T7540 (Tyrphostin 47) | Tyrphostin A47 | alpha-Cyano-(3,4-dihydroxy)thiocinnamide | benzylidenemalononitrile (BMN) deriv. 47
Type:
Small organic molecule
Emp. Form.:
C10H8N2O2S
Mol. Mass.:
220.248
SMILES:
NC(=S)C(=C\c1ccc(O)c(O)c1)\C#N
Structure:
Search PDB for entries with ligand similarity: