| Reaction Details |
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 | Report a problem with these data |
| Target | Protein farnesyltransferase alpha subunit/subunit beta |
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| Ligand | BDBM50067584 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | T. brucei FTase Assay |
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| IC50 | 10.0±2.0 nM |
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| Citation |  Lethu, S; Bosc, D; Mouray, E; Grellier, P; Dubois, J New protein farnesyltransferase inhibitors in the 3-arylthiophene 2-carboxylic acid series: diversification of the aryl moiety by solid-phase synthesis. J Enzyme Inhib Med Chem28:163-71 (2013) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Protein farnesyltransferase alpha subunit/subunit beta |
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| Name: | Protein farnesyltransferase alpha subunit/subunit beta |
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| Synonyms: | Farnesyltransferase (FTase) |
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| Type: | Enzyme |
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| Mol. Mass.: | n/a |
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| Description: | T. brucei FTase |
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| Components: | This complex has 2 components. |
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| Component 1 |
| Name: | Protein farnesyltransferase alpha subunit |
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| Synonyms: | Protein farnesyltransferase subunit alpha |
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| Type: | Protein |
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| Mol. Mass.: | 70116.60 |
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| Organism: | Trypanosoma brucei brucei |
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| Description: | Q9NC77 |
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| Residue: | 612 |
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| Sequence: | MNKSAVRSEESRQSSSLPSTYSSSSLNSEDERLALLSDINALQALFPGVTPKEETPLIKH
PNMTPAVFSKKFDYVMGIYRAVGVTFKGTRVGPSTPQWLLLTSFVIQQNASHYSAWKDRR
DVFLQPSRLVTSTRDAFMAENGQQCCGDKTDSLAKVSQEWLPAQCDVQGPTGECSVWRAI
RWELKAMERFALMNPKNFQVWHHRREMLREALMHANPVVTGSRSAFDGYLLTCHNMQFSD
IDERVFCDAALDDDGKNYHAWLYRSWFVHSFPFLLHPPSWDSLLGGDQGTEDKHSELRAA
PFRSFTVEEDWLHKCLQPIIPECPLSDELTSTAKRILHDCMNNSAWCHRFYVFEHDLIVP
LIRVIPPQQTEEAKLILKRLCECEMFYALQWCAYEPCNESAFVHARCVAVLHQAVAIHLC
LSSHGDAPHVFLRGDETIQVAGSSSLRHINLRDKLRWGAFLETFRLLLCQVNVLSDVITP
RAEEFRSGGEGRDNATISVIHKRRSQFLLDNTHQVYTARYRCLFTILEYMWRCYFTVSDR
ANVAAALPPEVYAGGDAEAAALAQQQSDDCVKFFLEAELQALRLARRLVVEDDIRRKYWK
HEMNIVMNRDYV
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| Component 2 |
| Name: | Protein farnesyltransferase subunit beta |
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| Synonyms: | n/a |
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| Type: | Protein |
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| Mol. Mass.: | 65426.56 |
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| Organism: | Trypanosoma brucei brucei |
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| Description: | Q9NC76 |
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| Residue: | 585 |
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| Sequence: | MSFVPPPASSTTHAQREVELTLLRFLEKYRPEVCDLWGTHSDIHLHADSNEKEEEMCTID
NEEGIVHSLNRESHEKYLKSRLVKLPEYAQRLYNAQPWMVYWTLQAAEMLGITEKLYEQI
SQDALGEFILSCLQEQPVEDEQKGCWGSEEGGKHGKGSMPQQCGNVYDFLRRCDADHTCA
IGFSGGNYGQIPHLATSYAGVCSLCILGCPEYLQALPRSAIKRWLLSLRCADGSFRMHIG
GEADIRASYCVAVITTLLQLQDVDVRSGDILREQEAQFVASCQTHEGGFACGRFASEAHG
AYTQCGLAALILMKRPELCNYTALRGWLAARQLRFEGGFNGRTNKLVDSCYAHWVGASHV
LLRVGESLAKITTCGETKRSLTSREMLLLDHAQLVDISNLHPESFEAWSQHEEEKQERAS
RVEAYLSATPLAASWSSSGVPNVLDDDAGDFYFNQRRLQLYILACCQNREEGGLMDKPNY
PNDFYHTCYSLSGMSSAQNLQGMQVNRDGRDLSGNSFYAAALSRGYIPGRRDSYGIVLPS
DERSGVSSELHLSKNCLRPTNPIFNINQSKVLFALRTWGAKTFMC
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| BDBM50067584 |
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| n/a |
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| Name | BDBM50067584 |
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| Synonyms: | (S)-2-{[5-((R)-2-Amino-3-mercapto-propylamino)-biphenyl-2-carbonyl]-amino}-4-methylsulfanyl-butyric acid | 2-{[5-((R)-2-Amino-3-mercapto-propylamino)-biphenyl-2-carbonyl]-amino}-4-methylsulfanyl-butyric acid | 2-{[5-(2-Amino-3-mercapto-propylamino)-biphenyl-2-carbonyl]-amino}-4-methylsulfanyl-butyric acid | CHEMBL54044 | FTI-276 |
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| Type | Small organic molecule |
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| Emp. Form. | C21H27N3O3S2 |
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| Mol. Mass. | 433.587 |
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| SMILES | CSCC[C@H](NC(=O)c1ccc(NC[C@@H](N)CS)cc1-c1ccccc1)C(O)=O |
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| Structure | 
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