Reaction Details Report a problem with these data
Target
Geranylgeranyl transferase type-1 subunit beta/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM50115914
Substrate
n/a
Meas. Tech.
ChEMBL_71676 (CHEMBL681668)
IC50
0.680000±n/a nM
Citation
 Tucker, TJ; Abrams, MT; Buser, CA; Davide, JP; Ellis-Hutchings, M; Fernandes, C; Gibbs, JB; Graham, SL; Hartman, GD; Huber, HE; Liu, D; Lobell, RB; Lumma, WC; Robinson, RG; Sisko, JT; Smith, AM The synthesis and biological evaluation of a series of potent dual inhibitors of farnesyl and geranyl-Geranyl protein transferases. Bioorg Med Chem Lett 12:2027-30 (2002) [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:
Protein Farnesyltransferase (PFT) Chain A | GGTase-I-alpha | FTase-alpha | FTase-1-alpha | Protein farnesyltransferase | Ras proteins prenyltransferase alpha | CAAX farnesyltransferase alpha subunit | Protein farnesyltransferase subunit alpha | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Geranylgeranyl Transferase (GGTase-I) Chain A | FNTA_HUMAN | FNTA | Geranylgeranyl transferase type I | Protein farnesyl/geranylgeranyl transferase
Type:
Enzyme
Mol. Mass.:
44392.46
Organism:
Human
Description:
Recombinant human FTase.
Residue:
379
Sequence:
MAATEGVGEAAQGGEPGQPAQPPPQPHPPPPQQQHKEEMAAEAGEAVASPMDDGFVSLDSPSYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSDKFRDVYDYFRAVLQRDERSERAFKLTRDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYITAIIEEQPKNYQVWHHRRVLVEWLRDPSQELEFIADILNQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQRYFVISNTTGYNDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLLDLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQSKHSTENDSPTNVQQ
  
Component 2
Name:
Geranylgeranyl transferase type-1 subunit beta
Synonyms:
Geranylgeranyl transferase type I beta subunit | GGTase-I-beta | Geranylgeranyl transferase type-1 subunit beta | Protein farnesyl/geranylgeranyl transferase | Type I protein geranyl-geranyltransferase subunit beta | Geranylgeranyl transferase type I subunit beta | 2.5.1.59 | PGTB1_HUMAN | PGGT1B | Geranylgeranyl transferase type I
Type:
n/a
Mol. Mass.:
42369.84
Organism:
Human
Description:
n/a
Residue:
377
Sequence:
MAATEDERLAGSGEGERLDFLRDRHVRFFQRCLQVLPERYSSLETSRLTIAFFALSGLDMLDSLDVVNKDDIIEWIYSLQVLPTEDRSNLNRCGFRGSSYLGIPFNPSKAPGTAHPYDSGHIAMTYTGLSCLVILGDDLSRVNKEACLAGLRALQLEDGSFCAVPEGSENDMRFVYCASCICYMLNNWSGMDMKKAITYIRRSMSYDNGLAQGAGLESHGGSTFCGIASLCLMGKLEEVFSEKELNRIKRWCIMRQQNGYHGRPNKPVDTCYSFWVGATLKLLKIFQYTNFEKNRNYILSTQDRLVGGFAKWPDSHPDALHAYFGICGLSLMEESGICKVHPALNVSTRTSERLLDLHQSWKTKDSKQCSENVHIST
  
Inhibitor
Name:
BDBM50115914
Synonyms:
4-[3-(4-Cyano-benzyl)-3H-imidazol-4-ylmethyl]-piperazine-1-carboxylic acid 2-chloro-benzyl ester | CHEMBL291580
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
Clc1ccccc1COC(=O)N1CCN(Cc2cncn2Cc2ccc(cc2)C#N)CC1
Structure:
Search PDB for entries with ligand similarity: