| Reaction Details |
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 | Report a problem with these data |
| Target | Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha |
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| Ligand | BDBM16180 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_70735 (CHEMBL680528) |
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| IC50 | 0.2±n/a nM |
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| Citation |  Henry, KJ; Wasicak, J; Tasker, AS; Cohen, J; Ewing, P; Mitten, M; Larsen, JJ; Kalvin, DM; Swenson, R; Ng, SC; Saeed, B; Cherian, S; Sham, H; Rosenberg, SH Discovery of a series of cyclohexylethylamine-containing protein farnesyltransferase inhibitors exhibiting potent cellular activity. J Med Chem42:4844-52 (1999) [PubMed] |
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| More Info.: | Get all data from this article, Assay Method |
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| Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha |
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| Name: | Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha |
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| Synonyms: | Protein Farnesyltransferase (PFT)/farnesyltransferase beta subunit | Protein farnesyltransferase |
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| Type: | n/a |
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| Mol. Mass.: | n/a |
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| Description: | ASSAY_ID of EBI is 69815 |
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| Components: | This complex has 2 components. |
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| Component 1 |
| Name: | Protein farnesyltransferase subunit beta |
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| Synonyms: | CAAX farnesyltransferase subunit beta | FNTB_RAT | FTase-beta | Fntb | Protein farnesyltransferase | Protein farnesyltransferase subunit beta | Ras proteins prenyltransferase subunit beta |
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| Type: | PROTEIN |
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| Mol. Mass.: | 48666.41 |
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| Organism: | Rattus norvegicus |
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| Description: | EBI_10573 |
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| Residue: | 437 |
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| Sequence: | MASSSSFTYYCPPSSSPVWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFS
SYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQ
IVATDVCQFLELCQSPDGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYNVINREKLLQY
LYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIG
GVPGMEAHGGYTFCGLAALVILKKERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCY
SFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDF
YHTCYCLSGLSIAQHFGSGAMLHDVVMGVPENVLQPTHPVYNIGPDKVIQATTHFLQKPV
PGFEECEDAVTSDPATD
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| Component 2 |
| Name: | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
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| Synonyms: | CAAX farnesyltransferase alpha subunit | FNTA_RAT | FTase-alpha | Fnta | GGTase-I-alpha | Protein farnesyltransferase | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Ras proteins prenyltransferase alpha | Type I protein geranyl-geranyltransferase alpha subunit | geranylgeranyltransferase type-I |
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| Type: | Enzyme |
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| Mol. Mass.: | 44030.14 |
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| Organism: | Rattus norvegicus (rat) |
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| Description: | Recombinant rat enzyme. |
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| Residue: | 377 |
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| Sequence: | MAATEGVGESAPGGEPGQPEQPPPPPPPPPAQQPQEEEMAAEAGEAAASPMDDGFLSLDS
PTYVLYRDRAEWADIDPVPQNDGPSPVVQIIYSEKFRDVYDYFRAVLQRDERSERAFKLT
RDAIELNAANYTVWHFRRVLLRSLQKDLQEEMNYIIAIIEEQPKNYQVWHHRRVLVEWLK
DPSQELEFIADILNQDAKNYHAWQHRQWVIQEFRLWDNELQYVDQLLKEDVRNNSVWNQR
HFVISNTTGYSDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSRYPNLLNQLL
DLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIG
RSLQSKHSRESDIPASV
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| BDBM16180 |
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| n/a |
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| Name | BDBM16180 |
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| Synonyms: | (2S)-2-{[4-({[(2S)-1-cyclohexyl-3-(ethylsulfanyl)propan-2-yl]amino}methyl)-2-(2-methylphenyl)phenyl]formamido}-4-(methylsulfanyl)butanoic acid | A197574 | CHEMBL344100 | N-({5-[({(1S)-2-cyclohexyl-1-[(ethylsulfanyl)methyl]ethyl}amino)methyl]-2 -methylbiphenyl-2-yl}carbonyl)-L-methionine |
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| Type | Small organic molecule |
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| Emp. Form. | C31H44N2O3S2 |
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| Mol. Mass. | 556.823 |
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| SMILES | CCSC[C@H](CC1CCCCC1)NCc1ccc(C(=O)N[C@@H](CCSC)C(O)=O)c(c1)-c1ccccc1C |r| |
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| Structure | 
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