Reaction Details |
| Report a problem with these data |
Target | Histone-lysine N-methyltransferase EZH2 |
---|
Ligand | BDBM50205637 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_1628509 (CHEMBL3871094) |
---|
IC50 | 15200±n/a nM |
---|
Citation | Ansari, A; Satalkar, S; Patil, V; Shete, AS; Kaur, S; Gupta, A; Singh, S; Raja, M; Severance, DL; Bernales, S; Chakravarty, S; Hung, DT; Pham, SM; Herrera, FJ; Rai, R Novel 3-methylindoline inhibitors of EZH2: Design, synthesis and SAR. Bioorg Med Chem Lett27:217-222 (2017) [PubMed] Article |
---|
More Info.: | Get all data from this article, Assay Method |
---|
|
Histone-lysine N-methyltransferase EZH2 |
---|
Name: | Histone-lysine N-methyltransferase EZH2 |
Synonyms: | ENX-1 | EZH2 | EZH2_HUMAN | Enhancer of zeste homolog 2 (EZH2) | Histone-lysine N-methyltransferase EZH2 | KMT6 | Lysine N-methyltransferase 6 |
Type: | Protein |
Mol. Mass.: | 85367.84 |
Organism: | Homo sapiens (Human) |
Description: | Q15910 |
Residue: | 746 |
Sequence: | MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEW
KQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNF
MVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQ
YNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEEL
KEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFH
ATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPN
NSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKM
KPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPA
PAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQ
NFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVS
CKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDK
YMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGE
ELFFDYRYSQADALKYVGIEREMEIP
|
|
|
BDBM50205637 |
---|
n/a |
---|
Name | BDBM50205637 |
Synonyms: | CHEMBL3896239 |
Type | Small organic molecule |
Emp. Form. | C33H40N4O3 |
Mol. Mass. | 540.6957 |
SMILES | CC1CN(CC2CC2)c2cc(cc(C(=O)NCc3c(C)cc(C)[nH]c3=O)c12)-c1ccc(CN2CCOCC2)cc1 |
Structure |
|