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Target
Dimer of Protein farnesyltransferase subunit beta
Ligand
BDBM50077853
Substrate
n/a
Meas. Tech.
ChEMBL_70294 (CHEMBL679531)
IC50
3.9±n/a nM
Citation
 Strickland, CL; Weber, PC; Windsor, WT; Wu, Z; Le, HV; Albanese, MM; Alvarez, CS; Cesarz, D; del Rosario, J; Deskus, J; Mallams, AK; Njoroge, FG; Piwinski, JJ; Remiszewski, S; Rossman, RR; Taveras, AG; Vibulbhan, B; Doll, RJ; Girijavallabhan, VM; Ganguly, AK Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships. J Med Chem 42:2125-35 (1999) [PubMed]  Article 
Target
Name:
Dimer of Protein farnesyltransferase subunit beta
Synonyms:
Protein Farnesyltransferase (PFT) Chain B
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of EBI is 51428
Components:
This complex has 3 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:
MASPSSFTYYCPPSSSPVWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFSSYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQIVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDIINREKLLQYLYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIGGVPGMEAHGGYTFCGLAALVILKRERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCYSFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDFYHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATTYFLQKPVPGFEELKDETSAEPATD
  
Component 2
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:
MASPSSFTYYCPPSSSPVWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFSSYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQIVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDIINREKLLQYLYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIGGVPGMEAHGGYTFCGLAALVILKRERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCYSFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDFYHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATTYFLQKPVPGFEELKDETSAEPATD
  
Inhibitor
Name:
BDBM50077853
Synonyms:
1-[4-(3,10-Dibromo-8-chloro-5,6-dihydro-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-piperidin-1-yl]-2-(1-oxy-pyridin-4-yl)-ethanone | CHEMBL66462
Type:
Small organic molecule
Emp. Form.:
C26H22Br2ClN3O2
Mol. Mass.:
603.733
SMILES:
[#8-]-[n+]1ccc(-[#6]-[#6](=O)-[#7]-2-[#6]-[#6]\[#6](-[#6]-[#6]-2)=[#6]-2/c3ncc(Br)cc3-[#6]-[#6]-c3cc(Cl)cc(Br)c-23)cc1
Structure:
Search PDB for entries with ligand similarity: