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TargetGeranylgeranyl transferase type-1 subunit beta/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
LigandBDBM50115912
Substrate/Competitorn/a
Meas. Tech.ChEMBL_71676 (CHEMBL681668)
IC50 8.7±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 Lett12:2027-30 (2002) [PubMed]
More Info.:Get all data from this article,  Assay Method
 
Geranylgeranyl transferase type-1 subunit beta/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
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:
MAATEGVGEAAQGGEPGQPAQPPPQPHPPPPQQQHKEEMAAEAGEAVASPMDDGFVSLDS
PSYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSDKFRDVYDYFRAVLQRDERSERAFKLT
RDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYITAIIEEQPKNYQVWHHRRVLVEWLR
DPSQELEFIADILNQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQR
YFVISNTTGYNDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLL
DLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIG
RSLQSKHSTENDSPTNVQQ
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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:
MAATEDERLAGSGEGERLDFLRDRHVRFFQRCLQVLPERYSSLETSRLTIAFFALSGLDM
LDSLDVVNKDDIIEWIYSLQVLPTEDRSNLNRCGFRGSSYLGIPFNPSKAPGTAHPYDSG
HIAMTYTGLSCLVILGDDLSRVNKEACLAGLRALQLEDGSFCAVPEGSENDMRFVYCASC
ICYMLNNWSGMDMKKAITYIRRSMSYDNGLAQGAGLESHGGSTFCGIASLCLMGKLEEVF
SEKELNRIKRWCIMRQQNGYHGRPNKPVDTCYSFWVGATLKLLKIFQYTNFEKNRNYILS
TQDRLVGGFAKWPDSHPDALHAYFGICGLSLMEESGICKVHPALNVSTRTSERLLDLHQS
WKTKDSKQCSENVHIST
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BDBM50115912
n/a
NameBDBM50115912
Synonyms:4-[3-(4-Cyano-benzyl)-3H-imidazol-4-ylmethyl]-piperazine-1-carboxylic acid 2-ethoxy-pyridin-3-ylmethyl ester | CHEMBL418513
TypeSmall organic molecule
Emp. Form.C25H28N6O3
Mol. Mass.460.5282
SMILESCCOc1ncccc1COC(=O)N1CCN(Cc2cncn2Cc2ccc(cc2)C#N)CC1
Structure
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