Target
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM50062252
Substrate
n/a
Meas. Tech.
ChEMBL_70742 (CHEMBL681453)
IC50
6±n/a nM
Citation
 Aoyama, TSatoh, TYonemoto, MShibata, JNonoshita, KArai, SKawakami, KIwasawa, YSano, HTanaka, KMonden, YKodera, TArakawa, HSuzuki-Takahashi, IKamei, TTomimoto, K A new class of highly potent farnesyl diphosphate-competitive inhibitors of farnesyltransferase. J Med Chem 41:143-7 (1998) [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:
BDBM50062252
Synonyms:
CHEMBL36339 | trisodium 5-[2-benzo[d][1,3]dioxol-5-yl-5-benzo[d][1,3]oxazol-2-yl-1-methyl-(1R,2S,4E)-4-pentenyl(2-naphthylmethyl)carbamoyl]-(4S,5R)-1,3-dioxolane-2,2,4-tricarboxylate
Type:
Small organic molecule
Emp. Form.:
C38H29N2O12
Mol. Mass.:
705.6447
SMILES:
C[C@H]([C@@H](C\C=C\c1nc2ccccc2o1)c1ccc2OCOc2c1)N(Cc1ccc2ccccc2c1)C(=O)[C@@H]1OC(O[C@@H]1C([O-])=O)(C([O-])=O)C([O-])=O
Structure:
Search PDB for entries with ligand similarity: