Reaction Details | |||
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Target | Geranylgeranyl transferase type-1 subunit beta/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | ||
Ligand | BDBM50139194 | ||
Substrate/Competitor | n/a | ||
Meas. Tech. | ChEMBL_71972 (CHEMBL684165) | ||
IC50 | 43±n/a nM | ||
Citation | Dinsmore, CJ; Zartman, CB; Bergman, JM; Abrams, MT; Buser, CA; Culberson, JC; Davide, JP; Ellis-Hutchings, M; Fernandes, C; Graham, SL; Hartman, GD; Huber, HE; Lobell, RB; Mosser, SD; Robinson, RG; Williams, TM Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I. Bioorg Med Chem Lett14:639-43 (2004) [PubMed] | ||
More Info.: | Get all data from this article, Assay Method | ||
Geranylgeranyl transferase type-1 subunit beta/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | |||
Name: | Geranylgeranyl transferase type-1 subunit beta/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | ||
Synonyms: | Geranylgeranyl transferase type I | Geranylgeranyl transferase type I beta subunit/Protein Farnesyltransferase (PFT) | Geranylgeranyl transferase type I beta/Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | ||
Type: | n/a | ||
Mol. Mass.: | n/a | ||
Description: | ASSAY_ID of EBI is 70196 | ||
Components: | This complex has 2 components. | ||
Component 1 | |||
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: |
| ||
Component 2 | |||
Name: | Geranylgeranyl transferase type-1 subunit beta | ||
Synonyms: | 2.5.1.59 | GGTase-I-beta | Geranylgeranyl transferase type I | Geranylgeranyl transferase type I beta subunit | Geranylgeranyl transferase type I subunit beta | Geranylgeranyl transferase type-1 subunit beta | PGGT1B | PGTB1_HUMAN | Protein farnesyl/geranylgeranyl transferase | Type I protein geranyl-geranyltransferase subunit beta | ||
Type: | n/a | ||
Mol. Mass.: | 42369.84 | ||
Organism: | Homo sapiens (Human) | ||
Description: | n/a | ||
Residue: | 377 | ||
Sequence: |
| ||
BDBM50139194 | |||
n/a | |||
Name | BDBM50139194 | ||
Synonyms: | CHEMBL345474 | N-(adamantan-2-yl)-10-cyano-23-oxo-8-oxa-1,15,17,21-tetraazapentacyclo[19.2.2.1^{3,7}.1^{9,13}.0^{15,19}]heptacosa-3(27),4,6,9(26),10,12,16,18-octaene-4-carboxamide | ||
Type | Small organic molecule | ||
Emp. Form. | C34H36N6O3 | ||
Mol. Mass. | 576.688 | ||
SMILES | O=C(NC1C2CC3CC(C2)CC1C3)c1ccc2Oc3cc(Cn4cncc4CN4CCN(Cc1c2)C(=O)C4)ccc3C#N |TLB:2:3:5:8.9.7,THB:2:3:6.5.12:8.10.9,7:6:3:8.10.9,7:8:3:6.5.12,10:11:5:8.9.7,10:8:5:3.11.12,(8.51,2.5,;9.26,1.16,;10.81,1.15,;11.58,2.49,;13.07,2.91,;14.48,2.35,;15.5,3.62,;15.51,5.16,;14.1,5.74,;13.07,4.5,;12.75,5.25,;12.77,3.78,;14.1,3.29,;8.47,-.19,;9.24,-1.53,;8.47,-2.86,;6.93,-2.86,;4.87,-5.99,;3.4,-5.55,;3.05,-4.04,;1.57,-3.58,;1.22,-2.09,;-.25,-1.64,;-1.44,-2.62,;-2.73,-1.78,;-2.35,-.29,;-.81,-.19,;-.04,1.14,;1.5,1.14,;2.28,2.48,;3.83,2.48,;4.6,1.14,;6.16,1.14,;6.93,-.19,;6.16,-1.53,;3.83,-.19,;4.63,-1.54,;2.28,-.19,;.45,-4.64,;.79,-6.13,;2.28,-6.59,;2.62,-8.1,;2.95,-9.62,)| | ||
Structure |