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Target
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM50100305
Substrate
n/a
Meas. Tech.
ChEMBL_70734 (CHEMBL680527)
IC50
260±n/a nM
Citation
 Mactough, SC; Desolms, SJ; Shaw, AW; Abrams, MT; Ciccarone, TM; Davide, JP; Hamilton, KA; Hutchinson, JH; Koblan, KS; Kohl, NE; Lobell, RB; Robinson, RG; Graham, SL Diaryl ether inhibitors of farnesyl-protein transferase. Bioorg Med Chem Lett 11:1257-60 (2001) [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:
BDBM50100305
Synonyms:
2-(2,4-Dichloro-phenoxy)-4-imidazol-1-ylmethyl-benzonitrile | CHEMBL22319
Type:
Small organic molecule
Emp. Form.:
C17H11Cl2N3O
Mol. Mass.:
344.195
SMILES:
Clc1ccc(Oc2cc(Cn3ccnc3)ccc2C#N)c(Cl)c1
Structure:
Search PDB for entries with ligand similarity: