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Target
Dimer of Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM50059876
Substrate
n/a
Meas. Tech.
ChEMBL_71979 (CHEMBL683532)
IC50
1250±n/a nM
Citation
 Leonard, DM; Shuler, KR; Poulter, CJ; Eaton, SR; Sawyer, TK; Hodges, JC; Su, TZ; Scholten, JD; Gowan, RC; Sebolt-Leopold, JS; Doherty, AM Structure-activity relationships of cysteine-lacking pentapeptide derivatives that inhibit ras farnesyltransferase. J Med Chem 40:192-200 (1997) [PubMed]  Article 
Target
Name:
Dimer of Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
geranylgeranyltransferase type-I
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of EBI is 71979
Components:
This complex has 2 components.
Component 1
Name:
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
Type I protein geranyl-geranyltransferase alpha subunit | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | FTase-alpha | CAAX farnesyltransferase alpha subunit | GGTase-I-alpha | Ras proteins prenyltransferase alpha | FNTA_RAT | Fnta | geranylgeranyltransferase type-I | Protein farnesyltransferase
Type:
Enzyme
Mol. Mass.:
44030.14
Organism:
Rat
Description:
Recombinant rat enzyme.
Residue:
377
Sequence:
MAATEGVGESAPGGEPGQPEQPPPPPPPPPAQQPQEEEMAAEAGEAAASPMDDGFLSLDSPTYVLYRDRAEWADIDPVPQNDGPSPVVQIIYSEKFRDVYDYFRAVLQRDERSERAFKLTRDAIELNAANYTVWHFRRVLLRSLQKDLQEEMNYIIAIIEEQPKNYQVWHHRRVLVEWLKDPSQELEFIADILNQDAKNYHAWQHRQWVIQEFRLWDNELQYVDQLLKEDVRNNSVWNQRHFVISNTTGYSDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSRYPNLLNQLLDLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQSKHSRESDIPASV
  
Component 2
Name:
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
Type I protein geranyl-geranyltransferase alpha subunit | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | FTase-alpha | CAAX farnesyltransferase alpha subunit | GGTase-I-alpha | Ras proteins prenyltransferase alpha | FNTA_RAT | Fnta | geranylgeranyltransferase type-I | Protein farnesyltransferase
Type:
Enzyme
Mol. Mass.:
44030.14
Organism:
Rat
Description:
Recombinant rat enzyme.
Residue:
377
Sequence:
MAATEGVGESAPGGEPGQPEQPPPPPPPPPAQQPQEEEMAAEAGEAAASPMDDGFLSLDSPTYVLYRDRAEWADIDPVPQNDGPSPVVQIIYSEKFRDVYDYFRAVLQRDERSERAFKLTRDAIELNAANYTVWHFRRVLLRSLQKDLQEEMNYIIAIIEEQPKNYQVWHHRRVLVEWLKDPSQELEFIADILNQDAKNYHAWQHRQWVIQEFRLWDNELQYVDQLLKEDVRNNSVWNQRHFVISNTTGYSDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSRYPNLLNQLLDLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQSKHSRESDIPASV
  
Inhibitor
Name:
BDBM50059876
Synonyms:
[(S)-1-[(S)-1-{(S)-2-Benzyloxy-1-[(S)-1-((R)-1-carbamoyl-ethylcarbamoyl)-2-(1H-indol-3-yl)-ethylcarbamoyl]-ethylcarbamoyl}-2-(4-benzyloxy-phenyl)-ethylcarbamoyl]-2-(3H-imidazol-4-yl)-ethyl]-carbamic acid benzyl ester | [(S)-1-[(S)-1-{(S)-2-Benzyloxy-1-[(S)-1-((R)-1-carbamoyl-ethylcarbamoyl)-2-(1H-indol-3-yl)-ethylcarbamoyl]-ethylcarbamoyl}-2-(4-benzyloxy-phenyl)-ethylcarbamoyl]-2-(1H-imidazol-4-yl)-ethyl]-carbamic acid benzyl ester | CHEMBL217423
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
C[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](COCc1ccccc1)NC(=O)[C@H](Cc1ccc(OCc2ccccc2)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)OCc1ccccc1)C(N)=O
Structure:
Search PDB for entries with ligand similarity: