| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha |
|---|
| Ligand | BDBM50109870 |
|---|
| Substrate/Competitor | n/a |
|---|
| Meas. Tech. | ChEBML_69830 |
|---|
| IC50 | 1.7±n/a nM |
|---|
| Citation |  Cooper, AB; Strickland, CL; Wang, J; Desai, J; Kirschmeier, P; Patton, R; Bishop, WR; Weber, PC; Girijavallabhan, V Synthesis of 5,6-dihydro-11H-benzo[5,6]-cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidine-N-cyanoguanidine derivatives as inhibitors of ras farnesyl protein transferase. Bioorg Med Chem Lett12:601-5 (2002) [PubMed] |
|---|
| More Info.: | Get all data from this article, Assay Method |
|---|
| |
| Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha |
|---|
| Name: | Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha |
|---|
| Synonyms: | Farnesyltransferase (FTase) | Protein Farnesyltransferase (PFT) | Protein Farnesyltransferase (PFT) Chain B | Protein farnesyltransferase |
|---|
| Type: | Protein Complex |
|---|
| Mol. Mass.: | n/a |
|---|
| Description: | To express recombinant enzyme in E. coli, the cloned human alpha and beta subunits were co-expressed from a plasmid, in which their expression was translationally coupled. |
|---|
| Components: | This complex has 2 components. |
|---|
| Component 1 |
| Name: | Protein farnesyltransferase subunit beta |
|---|
| Synonyms: | CAAX farnesyltransferase subunit alpha | CAAX farnesyltransferase subunit beta | FNTB | FNTB_HUMAN | FTase-alpha | FTase-beta | GGTase-I-alpha | Protein Farnesyltransferase (PFT) Chain B | Protein farnesyl/geranylgeranyl transferase | Protein farnesyltransferase beta subunit | Protein farnesyltransferase subunit beta | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Ras proteins prenyltransferase subunit alpha | Ras proteins prenyltransferase subunit beta | Type I protein geranyl-geranyltransferase subunit alpha |
|---|
| Type: | Enzyme Subunit |
|---|
| Mol. Mass.: | 48766.02 |
|---|
| Organism: | Homo sapiens (Human) |
|---|
| Description: | Protein farnesyltransferase subunit beta |
|---|
| Residue: | 437 |
|---|
| Sequence: | MASPSSFTYYCPPSSSPVWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFS
SYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQ
IVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDIINREKLLQY
LYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIG
GVPGMEAHGGYTFCGLAALVILKRERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCY
SFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDF
YHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATTYFLQKPV
PGFEELKDETSAEPATD
|
|
|
|---|
| Component 2 |
| 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: | MAATEGVGEAAQGGEPGQPAQPPPQPHPPPPQQQHKEEMAAEAGEAVASPMDDGFVSLDS
PSYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSDKFRDVYDYFRAVLQRDERSERAFKLT
RDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYITAIIEEQPKNYQVWHHRRVLVEWLR
DPSQELEFIADILNQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQR
YFVISNTTGYNDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLL
DLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIG
RSLQSKHSTENDSPTNVQQ
|
|
|
|---|
| BDBM50109870 |
|---|
| n/a |
|---|
| Name | BDBM50109870 |
|---|
| Synonyms: | 4-((R)-3,10-Dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-N-cyano-N'-(1-oxy-pyridin-3-ylmethyl)-piperidine-1-carboxamidine | CHEMBL348647 |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C27H25Br2ClN6O |
|---|
| Mol. Mass. | 644.788 |
|---|
| SMILES | [O-][n+]1cccc(CNC(=NC#N)N2CCC(CC2)[C@H]2c3ncc(Br)cc3CCc3cc(Cl)cc(Br)c23)c1 |w:9.9| |
|---|
| Structure | 
|
|---|
Search and Browse
