Details of the Biological Target of DIG (DBT)
| General Information of DBT (ID: ET0O3EP) | |||||
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| Name |
G9a-like protein 1 (EHMT1)
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| Synonyms |
Click to Show/Hide the Synonyms of This DBT
Histone-lysine N-methyltransferase EHMT1; Euchromatic histone-lysine N-methyltransferase 1; G9a-like protein 1; GLP; GLP1; H3-K9-HMTase 5; EHMT1; Eu-HMTase1; Histone H3-K9 methyltransferase 5; Lysine N-methyltransferase 1D
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| Family | Transferase (TFase) >> Methylase (EC 2.1) | ||||
| Organism |
Homo sapiens (Human)
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| Gene Name | EHMT1 | Gene ID | |||
| UniProt ID | EHMT1_HUMAN | (click to find more protein-related data of this DBT) | |||
| TTD ID | T39996 | (click to find more therapeutic target data of this DBT) | |||
| Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target | |||||
| Sequence |
MAAADAEAVPARGEPQQDCCVKTELLGEETPMAADEGSAEKQAGEAHMAADGETNGSCEN
SDASSHANAAKHTQDSARVNPQDGTNTLTRIAENGVSERDSEAAKQNHVTADDFVQTSVI GSNGYILNKPALQAQPLRTTSTLASSLPGHAAKTLPGGAGKGRTPSAFPQTPAAPPATLG EGSADTEDRKLPAPGADVKVHRARKTMPKSVVGLHAASKDPREVREARDHKEPKEEINKN ISDFGRQQLLPPFPSLHQSLPQNQCYMATTKSQTACLPFVLAAAVSRKKKRRMGTYSLVP KKKTKVLKQRTVIEMFKSITHSTVGSKGEKDLGASSLHVNGESLEMDSDEDDSEELEEDD GHGAEQAAAFPTEDSRTSKESMSEADRAQKMDGESEEEQESVDTGEEEEGGDESDLSSES SIKKKFLKRKGKTDSPWIKPARKRRRRSRKKPSGALGSESYKSSAGSAEQTAPGDSTGYM EVSLDSLDLRVKGILSSQAEGLANGPDVLETDGLQEVPLCSCRMETPKSREITTLANNQC MATESVDHELGRCTNSVVKYELMRPSNKAPLLVLCEDHRGRMVKHQCCPGCGYFCTAGNF MECQPESSISHRFHKDCASRVNNASYCPHCGEESSKAKEVTIAKADTTSTVTPVPGQEKG SALEGRADTTTGSAAGPPLSEDDKLQGAASHVPEGFDPTGPAGLGRPTPGLSQGPGKETL ESALIALDSEKPKKLRFHPKQLYFSARQGELQKVLLMLVDGIDPNFKMEHQNKRSPLHAA AEAGHVDICHMLVQAGANIDTCSEDQRTPLMEAAENNHLEAVKYLIKAGALVDPKDAEGS TCLHLAAKKGHYEVVQYLLSNGQMDVNCQDDGGWTPMIWATEYKHVDLVKLLLSKGSDIN IRDNEENICLHWAAFSGCVDIAEILLAAKCDLHAVNIHGDSPLHIAARENRYDCVVLFLS RDSDVTLKNKEGETPLQCASLNSQVWSALQMSKALQDSAPDRPSPVERIVSRDIARGYER IPIPCVNAVDSEPCPSNYKYVSQNCVTSPMNIDRNITHLQYCVCIDDCSSSNCMCGQLSM RCWYDKDGRLLPEFNMAEPPLIFECNHACSCWRNCRNRVVQNGLRARLQLYRTRDMGWGV RSLQDIPPGTFVCEYVGELISDSEADVREEDSYLFDLDNKDGEVYCIDARFYGNVSRFIN HHCEPNLVPVRVFMAHQDLRFPRIAFFSTRLIEAGEQLGFDYGERFWDIKGKLFSCRCGS PKCRHSSAALAQRQASAAQEAQEDGLPDTSSAAAADPL |
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| Function |
Histone methyltransferase that specifically mono- and dimethylates 'Lys-9' of histone H3 (H3K9me1 and H3K9me2, respectively) in euchromatin. H3K9me represents a specific tag for epigenetic transcriptional repression by recruiting HP1 proteins to methylated histones. Also weakly methylates 'Lys-27' of histone H3 (H3K27me). Also required for DNA methylation, the histone methyltransferase activity is not required for DNA methylation, suggesting that these 2 activities function independently.
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| Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT | ||||||
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| DIG Name: Phenylmercuric acetate | Click to Show/Hide | |||||
| Detailed Information |
DIG Info
 click to show the detail info of this DIG
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| Functional Class | Click to Show/Hide the Functional Class of This DIG
Antimicrobial preservative
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| Experiment for Assessing the Biological Activity of This DIG on the Studied DBT | ||||||
| Biological Activity | IC50 = 4900 nM (estimated based on the structural similarity with CHEMBL39469 ) | [1] | ||||
| Structural Similarity | Tanimoto coefficient = 0.766666667 | |||||
| Tested Species | Homo sapiens (Human) | |||||
| UniProt ID | EHMT1_HUMAN | |||||
| References | |||||
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| 1 | Inhibition of histone lysine methyltransferases G9a and GLP by ejection of structural Zn(II). Bioorg Med Chem Lett. 2018 Apr 15; 28(7):1234-1238. | ||||
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