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Target
Geranylgeranyl transferase type-1 subunit beta/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM50098037
Substrate
n/a
Meas. Tech.
ChEMBL_71826 (CHEMBL683657)
IC50
0.200000±n/a nM
Citation
 Trotter, BW; Quigley, AG; Lumma, WC; Sisko, JT; Walsh, ES; Hamann, CS; Robinson, RG; Bhimnathwala, H; Kolodin, DG; Zheng, W; Buser, CA; Huber, HE; Lobell, RB; Kohl, NE; Williams, TM; Graham, SL; Dinsmore, CJ 2-Arylindole-3-acetamides: FPP-competitive inhibitors of farnesyl protein transferase. Bioorg Med Chem Lett 11:865-9 (2001) [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:
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:
MAATEGVGEAAQGGEPGQPAQPPPQPHPPPPQQQHKEEMAAEAGEAVASPMDDGFVSLDSPSYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSDKFRDVYDYFRAVLQRDERSERAFKLTRDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYITAIIEEQPKNYQVWHHRRVLVEWLRDPSQELEFIADILNQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQRYFVISNTTGYNDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLLDLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQSKHSTENDSPTNVQQ
  
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:
MAATEDERLAGSGEGERLDFLRDRHVRFFQRCLQVLPERYSSLETSRLTIAFFALSGLDMLDSLDVVNKDDIIEWIYSLQVLPTEDRSNLNRCGFRGSSYLGIPFNPSKAPGTAHPYDSGHIAMTYTGLSCLVILGDDLSRVNKEACLAGLRALQLEDGSFCAVPEGSENDMRFVYCASCICYMLNNWSGMDMKKAITYIRRSMSYDNGLAQGAGLESHGGSTFCGIASLCLMGKLEEVFSEKELNRIKRWCIMRQQNGYHGRPNKPVDTCYSFWVGATLKLLKIFQYTNFEKNRNYILSTQDRLVGGFAKWPDSHPDALHAYFGICGLSLMEESGICKVHPALNVSTRTSERLLDLHQSWKTKDSKQCSENVHIST
  
Inhibitor
Name:
BDBM50098037
Synonyms:
4-[3-(4-Cyano-benzyl)-3H-imidazol-4-ylmethyl]-piperazine-1-carboxylic acid adamantan-1-ylamide | CHEMBL424564
Type:
Small organic molecule
Emp. Form.:
C27H34N6O
Mol. Mass.:
458.5985
SMILES:
O=C(NC12CC3CC(CC(C3)C1)C2)N1CCN(Cc2cncn2Cc2ccc(cc2)C#N)CC1 |TLB:10:9:12:5.4.6,THB:8:9:4:7.12.6|
Structure:
Search PDB for entries with ligand similarity: