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Target
Geranylgeranyl transferase type-1 subunit beta/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM50134557
Substrate
n/a
Meas. Tech.
ChEMBL_71791 (CHEMBL686002)
IC50
124±n/a nM
Citation
 Lin, NH; Wang, L; Cohen, J; Gu, WZ; Frost, D; Zhang, H; Rosenberg, S; Sham, H Synthesis and biological evaluation of 4-[(3-methyl-3H-imidazol-4-yl)-(2-phenylethynyl-benzyloxy)-methyl]-benzonitrile as novel farnesyltransferase inhibitor. Bioorg Med Chem Lett 13:3821-5 (2003) [PubMed]  Article 
Target
Name:
Geranylgeranyl transferase type-1 subunit beta/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
Geranylgeranyl transferase type I | Geranylgeranyl transferase type I beta subunit/Protein Farnesyltransferase (PFT) | Geranylgeranyl transferase type I beta/Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of EBI is 70196
Components:
This complex has 2 components.
Component 1
Name:
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
CAAX farnesyltransferase alpha subunit | FNTA | FNTA_HUMAN | FTase-1-alpha | FTase-alpha | GGTase-I-alpha | Geranylgeranyl Transferase (GGTase-I) Chain A | Geranylgeranyl transferase type I | Protein Farnesyltransferase (PFT) Chain A | Protein farnesyl/geranylgeranyl transferase | Protein farnesyltransferase | Protein farnesyltransferase subunit alpha | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Ras proteins prenyltransferase alpha
Type:
Enzyme
Mol. Mass.:
44392.46
Organism:
Homo sapiens (Human)
Description:
Recombinant human FTase.
Residue:
379
Sequence:
MAATEGVGEAAQGGEPGQPAQPPPQPHPPPPQQQHKEEMAAEAGEAVASPMDDGFVSLDSPSYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSDKFRDVYDYFRAVLQRDERSERAFKLTRDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYITAIIEEQPKNYQVWHHRRVLVEWLRDPSQELEFIADILNQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQRYFVISNTTGYNDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLLDLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQSKHSTENDSPTNVQQ
  
Component 2
Name:
Geranylgeranyl transferase type-1 subunit beta
Synonyms:
2.5.1.59 | GGTase-I-beta | Geranylgeranyl transferase type I | Geranylgeranyl transferase type I beta subunit | Geranylgeranyl transferase type I subunit beta | Geranylgeranyl transferase type-1 subunit beta | PGGT1B | PGTB1_HUMAN | Protein farnesyl/geranylgeranyl transferase | Type I protein geranyl-geranyltransferase subunit beta
Type:
n/a
Mol. Mass.:
42369.84
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
377
Sequence:
MAATEDERLAGSGEGERLDFLRDRHVRFFQRCLQVLPERYSSLETSRLTIAFFALSGLDMLDSLDVVNKDDIIEWIYSLQVLPTEDRSNLNRCGFRGSSYLGIPFNPSKAPGTAHPYDSGHIAMTYTGLSCLVILGDDLSRVNKEACLAGLRALQLEDGSFCAVPEGSENDMRFVYCASCICYMLNNWSGMDMKKAITYIRRSMSYDNGLAQGAGLESHGGSTFCGIASLCLMGKLEEVFSEKELNRIKRWCIMRQQNGYHGRPNKPVDTCYSFWVGATLKLLKIFQYTNFEKNRNYILSTQDRLVGGFAKWPDSHPDALHAYFGICGLSLMEESGICKVHPALNVSTRTSERLLDLHQSWKTKDSKQCSENVHIST
  
Inhibitor
Name:
BDBM50134557
Synonyms:
3-(4-Cyano-phenylethynyl)-4-[(4-cyano-phenyl)-(3-methyl-3H-imidazol-4-yl)-methoxymethyl]-benzonitrile | CHEMBL124081
Type:
Small organic molecule
Emp. Form.:
C29H19N5O
Mol. Mass.:
453.4941
SMILES:
Cn1cncc1C(OCc1ccc(cc1C#Cc1ccc(cc1)C#N)C#N)c1ccc(cc1)C#N
Structure:
Search PDB for entries with ligand similarity: