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Target
Geranylgeranyl transferase type-1 subunit beta/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM50327998
Substrate
n/a
Meas. Tech.
ChEBML_665230
IC50
2700±n/a nM
Citation
 Fletcher, S; Keaney, EP; Cummings, CG; Blaskovich, MA; Hast, MA; Glenn, MP; Chang, SY; Bucher, CJ; Floyd, RJ; Katt, WP; Gelb, MH; Van Voorhis, WC; Beese, LS; Sebti, SM; Hamilton, AD Structure-based design and synthesis of potent, ethylenediamine-based, mammalian farnesyltransferase inhibitors as anticancer agents. J Med Chem 53:6867-88 (2010) [PubMed]  Article 
Target
Name:
Geranylgeranyl transferase type-1 subunit beta/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
Geranylgeranyl transferase type 1
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of ChEMBL is 665230
Components:
This complex has 2 components.
Component 1
Name:
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
CAAX farnesyltransferase subunit alpha | FNTA_MOUSE | FTase-alpha | Fnta | GGTase-I-alpha | Geranylgeranyl transferase type 1 | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Ras proteins prenyltransferase subunit alpha | Type I protein geranyl-geranyltransferase subunit alpha
Type:
PROTEIN
Mol. Mass.:
43994.09
Organism:
Mus musculus
Description:
EBI_10570
Residue:
377
Sequence:
MAATEGVGESAAGGEPGQPEQPPPPPPPPPAQQPQEEEMAAEAGEAAASPMDDGFLSLDSPTYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSEKFRDVYDYFRAVLQRDERSERAFKLTRDAIELNAANYTVWHFRRVLLRSLQKDLQEEMNYITAIIEEQPKNYQVWHHRRVLVEWLKDPSQELEFIADILSQDAKNYHAWQHRQWVIQEFRLWDNELQYVDQLLKEDVRNNSVWNQRHFVISNTTGYSDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSRYPNLLNQLLDLQPSHSSPYLIAFLVDVYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQSKHCRESDIPASV
  
Component 2
Name:
Geranylgeranyl transferase type-1 subunit beta
Synonyms:
GGTase-I-beta | Geranylgeranyl transferase type 1 | Geranylgeranyl transferase type I subunit beta | Geranylgeranyl transferase type-1 subunit beta | PGTB1_MOUSE | Pggt1b | Type I protein geranyl-geranyltransferase subunit beta
Type:
PROTEIN
Mol. Mass.:
42355.77
Organism:
Mus musculus
Description:
ChEMBL_108428
Residue:
377
Sequence:
MATTEDDRLAGSGEGERLDFLRDRHVRFFQRCLQVLPERYSSLETSRLTIAFFALSGLDMLDSLDVVNKDDIIEWIYSLQVLPTEDRSNLSRCGFRGSSYLGIPFNPSKNPGAAHPYDSGHIAMTYTGLSCLIILGDDLGRVDKEACLAGLRALQLEDGSFCAVPEGSENDMRFVYCASCICYMLNNWSGMDMKKAISYIRRSMSYDNGLAQGAGLESHGGSTFCGIASLCLMGKLEEVFSEKELNRIKRWCIMRQQNGYHGRPNKPVDTCYSFWVGATLKLLKIFQYTNFEKNRNYILSTQDRLVGGFAKWPDSHPDALHAYFGICGLSLMEESGICKVHPALNVSTRTSERLRDLHQSWKTKDSKQCSDNVHIAT
  
Inhibitor
Name:
BDBM50327998
Synonyms:
CHEMBL1258350 | N-(2-((4-cyano-2-fluorophenyl)((1-methyl-1H-imidazol-5-yl)methyl)amino)ethyl)-N-(cyclohexylmethyl)pyridine-2-sulfonamide
Type:
Small organic molecule
Emp. Form.:
C26H31FN6O2S
Mol. Mass.:
510.627
SMILES:
Cn1cncc1CN(CCN(CC1CCCCC1)S(=O)(=O)c1ccccn1)c1ccc(cc1F)C#N
Structure:
Search PDB for entries with ligand similarity: