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Target
Geranylgeranyl transferase type-1 subunit beta/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM50126335
Substrate
n/a
Meas. Tech.
ChEMBL_305246 (CHEMBL833504)
IC50
1100±n/a nM
Citation
 Li, Q; Wang, GT; Li, T; Gwaltney, SL; Woods, KW; Claiborne, A; Wang, X; Gu, W; Cohen, J; Stoll, VS; Hutchins, C; Frost, D; Rosenberg, SH; Sham, HL Synthesis and activity of 1-aryl-1'-imidazolyl methyl ethers as non-thiol farnesyltransferase inhibitors. Bioorg Med Chem Lett 14:5371-6 (2004) [PubMed]  Article 
Target
Name:
Geranylgeranyl transferase type-1 subunit beta/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
Geranylgeranyl Transferase (GGTase-I) | Geranylgeranyl Transferase (GGTase-I)/Protein Farnesyltransferase (PFT) | Geranylgeranyl transferase type I
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
CAAX farnesyltransferase alpha subunit | FNTA | FNTA_BOVIN | FTase-alpha | GGTase-I-alpha | Geranylgeranyl Transferase (GGTase-I) Chain A | Protein Farnesyltransferase (PFT) Chain A | Protein farnesyltransferase | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Ras proteins prenyltransferase alpha | Type I protein geranyl-geranyltransferase alpha subunit
Type:
Enzyme
Mol. Mass.:
43827.38
Organism:
Bos taurus (bovine)
Description:
The enzyme was purified from a bovine brain homogenate by sequential ammonium sulfate fractionation and affinity chromatography.
Residue:
375
Sequence:
MAAADGVGEAAQGGDPGQPEPPPPPQPHPPPPPPQPPQEEAAAASPIDDGFLSLDSPTYVLYRDRPEWADIDPVPQNDGPNPVVQIIYSEKFQDVYDYFRAVLQRDERSERAFKLTRDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYISAIIEEQPKNYQVWHHRRVLVEWLRDPSQELEFIADILTQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQRYFVISNTTGYNDRAILEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLLDLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQSKHSTESDPPTNVQQ
  
Component 2
Name:
Geranylgeranyl transferase type-1 subunit beta
Synonyms:
GGTase-I-beta | Geranylgeranyl transferase type I | Geranylgeranyl transferase type-1 subunit beta | PGGT1B | PGTB1_BOVIN | Type I protein geranyl-geranyltransferase subunit beta
Type:
Enzyme
Mol. Mass.:
42483.88
Organism:
Bos taurus (bovine)
Description:
Purified from bovine brain
Residue:
377
Sequence:
MAATEDERPTGSGEGERLDFLRDRHVRFFQRCLQVLPERYSSLETSRLTIAFFALSGLDMLDSLDVVNKDDIIEWIYSLQVLPTEDRSNLNRCGFRGSSYLGIPFNPSKNPGTAHPYDSGHIAMTYTGLSCLVILGDDLSRVNKEACLAGLRALQLEDGSFCAVPEGSENDMRFVYCASCICYMLNNWSGMDMKKAINYIRRSMSYDNGLAQGAGLESHGGSTFCGIASLCLMGKLEEVFSEKELNRIKRWCIMRQQNGYHGRPNKPVDTCYSFWVGATLKLLKIFQYTNFEKNRNYILSTQDRLVGGFAKWPDSHPDALHAYFGICGLSLMEESGICKVHPALNVSTRTSERLRDLHQSWKTKDSKQCSENVHIST
  
Inhibitor
Name:
BDBM50126335
Synonyms:
6-[(R)-Amino-(4-chloro-phenyl)-(3-methyl-3H-imidazol-4-yl)-methyl]-4-(3-chloro-phenyl)-1-methyl-1H-quinolin-2-one | 6-[(R)-Amino-(4-chloro-phenyl)-(3-methyl-4,5-dihydro-3H-imidazol-4-yl)-methyl]-4-(3-chloro-phenyl)-1-methyl-1H-quinolin-2-one | 6-[(S)-AMINO(4-CHLOROPHENYL)(1-METHYL-1H-IMIDAZOL-5-YL)METHYL]-4-(3-CHLOROPHENYL)-1-METHYLQUINOLIN-2(1H)-ONE | 6-[Amino-(4-chloro-phenyl)-(1-methyl-1H-imidazol-2-yl)-methyl]-4-(3-chloro-phenyl)-1-methyl-1H-quinolin-2-one | 6-[Amino-(4-chloro-phenyl)-(3-methyl-3H-imidazol-4-yl)-methyl]-4-(3-chloro-phenyl)-1-methyl-1H-quinolin-2-one | CHEMBL289228 | R-11577 | R-115777 | Tipifarnib
Type:
Small organic molecule
Emp. Form.:
C27H22Cl2N4O
Mol. Mass.:
489.396
SMILES:
Cn1ccnc1C(N)(c1ccc(Cl)cc1)c1ccc2n(C)c(=O)cc(-c3cccc(Cl)c3)c2c1
Structure:
Search PDB for entries with ligand similarity: