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Target
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM50051826
Substrate
n/a
Meas. Tech.
ChEMBL_163505 (CHEMBL772416)
IC50
500±n/a nM
Citation
 Williams, TM; Ciccarone, TM; MacTough, SC; Bock, RL; Conner, MW; Davide, JP; Hamilton, K; Koblan, KS; Kohl, NE; Kral, AM; Mosser, SD; Omer, CA; Pompliano, DL; Rands, E; Schaber, MD; Shah, D; Wilson, FR; Gibbs, JB; Graham, SL; Hartman, GD; Oliff, AI; Smith, RL 2-substituted piperazines as constrained amino acids. Application to the synthesis of potent, non carboxylic acid inhibitors of farnesyltransferase. J Med Chem 39:1345-8 (1996) [PubMed]  Article 
Target
Name:
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
Protein Farnesyltransferase (PFT)/farnesyltransferase beta subunit | Protein farnesyltransferase
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of EBI is 69815
Components:
This complex has 2 components.
Component 1
Name:
Protein farnesyltransferase subunit beta
Synonyms:
CAAX farnesyltransferase subunit beta | FNTB_RAT | FTase-beta | Fntb | Protein farnesyltransferase | Protein farnesyltransferase subunit beta | Ras proteins prenyltransferase subunit beta
Type:
PROTEIN
Mol. Mass.:
48666.41
Organism:
Rattus norvegicus
Description:
EBI_10573
Residue:
437
Sequence:
MASSSSFTYYCPPSSSPVWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFSSYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQIVATDVCQFLELCQSPDGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYNVINREKLLQYLYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIGGVPGMEAHGGYTFCGLAALVILKKERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCYSFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDFYHTCYCLSGLSIAQHFGSGAMLHDVVMGVPENVLQPTHPVYNIGPDKVIQATTHFLQKPVPGFEECEDAVTSDPATD
  
Component 2
Name:
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
CAAX farnesyltransferase alpha subunit | FNTA_RAT | FTase-alpha | Fnta | GGTase-I-alpha | Protein farnesyltransferase | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Ras proteins prenyltransferase alpha | Type I protein geranyl-geranyltransferase alpha subunit | geranylgeranyltransferase type-I
Type:
Enzyme
Mol. Mass.:
44030.14
Organism:
Rattus norvegicus (rat)
Description:
Recombinant rat enzyme.
Residue:
377
Sequence:
MAATEGVGESAPGGEPGQPEQPPPPPPPPPAQQPQEEEMAAEAGEAAASPMDDGFLSLDSPTYVLYRDRAEWADIDPVPQNDGPSPVVQIIYSEKFRDVYDYFRAVLQRDERSERAFKLTRDAIELNAANYTVWHFRRVLLRSLQKDLQEEMNYIIAIIEEQPKNYQVWHHRRVLVEWLKDPSQELEFIADILNQDAKNYHAWQHRQWVIQEFRLWDNELQYVDQLLKEDVRNNSVWNQRHFVISNTTGYSDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSRYPNLLNQLLDLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQSKHSRESDIPASV
  
Inhibitor
Name:
BDBM50051826
Synonyms:
CHEMBL27486 | [(S)-4-((R)-2-Amino-3-mercapto-propyl)-3-butyl-piperazin-1-yl]-naphthalen-1-yl-methanone | [4-((R)-2-Amino-3-mercapto-propyl)-3-butyl-piperazin-1-yl]-naphthalen-1-yl-methanone
Type:
Small organic molecule
Emp. Form.:
C22H31N3OS
Mol. Mass.:
385.566
SMILES:
CCCC[C@H]1CN(CCN1C[C@@H](N)CS)C(=O)c1cccc2ccccc12
Structure:
Search PDB for entries with ligand similarity: