| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Geranylgeranyl transferase type-1 subunit beta/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
|---|
| Ligand | BDBM50127256 |
|---|
| Substrate/Competitor | n/a |
|---|
| Meas. Tech. | ChEMBL_72096 (CHEMBL680222) |
|---|
| IC50 | 32000±n/a nM |
|---|
| Citation |  Angibaud, P; Bourdrez, X; Devine, A; End, DW; Freyne, E; Ligny, Y; Muller, P; Mannens, G; Pilatte, I; Poncelet, V; Skrzat, S; Smets, G; Van Dun, J; Van Remoortere, P; Venet, M; Wouters, W 5-imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors. Bioorg Med Chem Lett13:1543-7 (2003) [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: | MAATEGVGEAAQGGEPGQPAQPPPQPHPPPPQQQHKEEMAAEAGEAVASPMDDGFVSLDS
PSYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSDKFRDVYDYFRAVLQRDERSERAFKLT
RDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYITAIIEEQPKNYQVWHHRRVLVEWLR
DPSQELEFIADILNQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQR
YFVISNTTGYNDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLL
DLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIG
RSLQSKHSTENDSPTNVQQ
|
|
|
|---|
| 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: | MAATEDERLAGSGEGERLDFLRDRHVRFFQRCLQVLPERYSSLETSRLTIAFFALSGLDM
LDSLDVVNKDDIIEWIYSLQVLPTEDRSNLNRCGFRGSSYLGIPFNPSKAPGTAHPYDSG
HIAMTYTGLSCLVILGDDLSRVNKEACLAGLRALQLEDGSFCAVPEGSENDMRFVYCASC
ICYMLNNWSGMDMKKAITYIRRSMSYDNGLAQGAGLESHGGSTFCGIASLCLMGKLEEVF
SEKELNRIKRWCIMRQQNGYHGRPNKPVDTCYSFWVGATLKLLKIFQYTNFEKNRNYILS
TQDRLVGGFAKWPDSHPDALHAYFGICGLSLMEESGICKVHPALNVSTRTSERLLDLHQS
WKTKDSKQCSENVHIST
|
|
|
|---|
| BDBM50127256 |
|---|
| n/a |
|---|
| Name | BDBM50127256 |
|---|
| Synonyms: | 7-[Amino-(4-chloro-phenyl)-(3-methyl-3H-imidazol-4-yl)-methyl]-5-(3-chloro-phenyl)-1-methyl-1,3-dihydro-benzo[e][1,4]diazepin-2-one | CHEMBL39618 |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C27H23Cl2N5O |
|---|
| Mol. Mass. | 504.41 |
|---|
| SMILES | CN1c2ccc(cc2C(=NCC1=O)c1cccc(Cl)c1)C(N)(c1cncn1C)c1ccc(Cl)cc1 |c:9| |
|---|
| Structure | 
|
|---|
Search and Browse
