Reaction Details |
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Target | Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha |
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Ligand | BDBM50126335 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_310131 (CHEMBL838112) |
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EC50 | 1.6±n/a nM |
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Citation | Li, Q; Claiborne, A; Li, T; Hasvold, L; Stoll, VS; Muchmore, S; Jakob, CG; Gu, W; Cohen, J; Hutchins, C; Frost, D; Rosenberg, SH; Sham, HL Design, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors. Bioorg Med Chem Lett14:5367-70 (2004) [PubMed] Article |
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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 |
Synonyms: | Protein farnesyltransferase | Protein farnesyltransferase beta/geranylgeranyltransferase type I alpha subunit |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of EBI is 38702 |
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: | MAATEGVGESAAGGEPGQPEQPPPPPPPPPAQQPQEEEMAAEAGEAAASPMDDGFLSLDS
PTYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSEKFRDVYDYFRAVLQRDERSERAFKLT
RDAIELNAANYTVWHFRRVLLRSLQKDLQEEMNYITAIIEEQPKNYQVWHHRRVLVEWLK
DPSQELEFIADILSQDAKNYHAWQHRQWVIQEFRLWDNELQYVDQLLKEDVRNNSVWNQR
HFVISNTTGYSDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSRYPNLLNQLL
DLQPSHSSPYLIAFLVDVYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIG
RSLQSKHCRESDIPASV
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Component 2 |
Name: | Protein farnesyltransferase subunit beta |
Synonyms: | FNTB_MOUSE | Fntb | Protein farnesyltransferase |
Type: | PROTEIN |
Mol. Mass.: | 48811.61 |
Organism: | Mus musculus |
Description: | EBI_12341 |
Residue: | 437 |
Sequence: | MASSSSFTYYCPPSSSPVWSEPLYSLRPEHVRERLQDDSVETVTSIEQAKVEEKIQEVFS
SYKFNHLVPRLILQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQ
IVATDVCQFLELCQSPDGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYNVINREKLLQY
LYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIG
GVPGMEAHGGYTFCGLAALVILKKERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCY
SFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDF
YHTCYCLSGLSIAQHFGSGAMLHDMVMGVPENVLQPTHPVYNIGPEKVIQATTHFLQKPV
PGFEECEDEVTSDPATD
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BDBM50126335 |
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n/a |
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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 |
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