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TargetGeranylgeranyl transferase type I beta subunit/Protein Farnesyltransferase (PFT)
LigandBDBM50115916
Substrate/Competitorn/a
Meas. Tech.ChEMBL_71676
IC50 0.160000±n/a nM
Citation Tucker TJAbrams MTBuser CADavide JPEllis-Hutchings MFernandes CGibbs JBGraham SLHartman GDHuber HELiu DLobell RBLumma WCRobinson RGSisko JTSmith 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]
More Info.:Get all data from this article,  Assay Method
 
Geranylgeranyl transferase type I beta subunit/Protein Farnesyltransferase (PFT)
Name:Geranylgeranyl transferase type I beta subunit/Protein Farnesyltransferase (PFT)
Synonyms:Geranylgeranyl transferase type I | 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:Geranylgeranyl transferase type I
Synonyms:CAAX farnesyltransferase alpha subunit | FTase-1-alpha | FTase-alpha | GGTase-I-alpha | Geranylgeranyl Transferase (GGTase-I) Chain A | Protein Farnesyltransferase (PFT) Chain A | 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:
MAATEGVGEAAQGGEPGQPAQPPPQPHPPPPQQQHKEEMAAEAGEAVASPMDDGFVSLDS
PSYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSDKFRDVYDYFRAVLQRDERSERAFKLT
RDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYITAIIEEQPKNYQVWHHRRVLVEWLR
DPSQELEFIADILNQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQR
YFVISNTTGYNDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLL
DLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIG
RSLQSKHSTENDSPTNVQQ
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Component 2
Name:Geranylgeranyl transferase type I
Synonyms:GGTase-I-beta | Geranylgeranyl transferase type I beta subunit | Geranylgeranyl transferase type I subunit beta | Geranylgeranyl transferase type-1 subunit beta | PGGT1B | 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:
MAATEDERLAGSGEGERLDFLRDRHVRFFQRCLQVLPERYSSLETSRLTIAFFALSGLDM
LDSLDVVNKDDIIEWIYSLQVLPTEDRSNLNRCGFRGSSYLGIPFNPSKAPGTAHPYDSG
HIAMTYTGLSCLVILGDDLSRVNKEACLAGLRALQLEDGSFCAVPEGSENDMRFVYCASC
ICYMLNNWSGMDMKKAITYIRRSMSYDNGLAQGAGLESHGGSTFCGIASLCLMGKLEEVF
SEKELNRIKRWCIMRQQNGYHGRPNKPVDTCYSFWVGATLKLLKIFQYTNFEKNRNYILS
TQDRLVGGFAKWPDSHPDALHAYFGICGLSLMEESGICKVHPALNVSTRTSERLLDLHQS
WKTKDSKQCSENVHIST
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BDBM50115916
n/a
NameBDBM50115916
Synonyms:4-[3-(4-Cyano-benzyl)-3H-imidazol-4-ylmethyl]-piperazine-1-carboxylic acid 2-trifluoromethoxy-benzyl ester | CHEMBL64183
TypeSmall organic molecule
Emp. Form.C25H24F3N5O3
Mol. Mass.499.485
SMILESFC(F)(F)Oc1ccccc1COC(=O)N1CCN(Cc2cncn2Cc2ccc(cc2)C#N)CC1
Structure
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