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Target
MAP/microtubule affinity-regulating kinase 3
Ligand
BDBM50208926
Substrate
n/a
Meas. Tech.
ChEMBL_1633686 (CHEMBL3876478)
IC50
61±n/a nM
Citation
 Haidle, AM; Childers, KK; Zabierek, AA; Katz, JD; Jewell, JP; Hou, Y; Altman, MD; Szewczak, A; Chen, D; Harsch, A; Hayashi, M; Warren, L; Hutton, M; Nuthall, H; Stanton, MG; Davies, IW; Munoz, B; Northrup, A MARK inhibitors: Declaring a No-Go decision on a chemical series based on extensive DMPK experimentation. Bioorg Med Chem Lett 27:109-113 (2017) [PubMed]  Article 
Target
Name:
MAP/microtubule affinity-regulating kinase 3
Synonyms:
2.7.11.1 | C-TAK1 | CTAK1 | Cdc25C-associated protein kinase 1 | ELKL motif kinase 2 | EMK-2 | EMK2 | MAP/microtubule affinity-regulating kinase 3 | MAP/microtubule affinity-regulating kinase 3 (MARK 3) | MARK3 | MARK3_HUMAN | Par-1a | Protein kinase STK10 | Ser/Thr protein kinase PAR-1 | Serine/threonine-protein kinase c-TAK1 | Serine/threonine-protein kinase p78
Type:
Protein
Mol. Mass.:
84525.94
Organism:
Homo sapiens (Human)
Description:
P27448
Residue:
753
Sequence:
MSTRTPLPTVNERDTENHTSHGDGRQEVTSRTSRSGARCRNSIASCADEQPHIGNYRLLKTIGKGNFAKVKLARHILTGREVAIKIIDKTQLNPTSLQKLFREVRIMKILNHPNIVKLFEVIETEKTLYLIMEYASGGEVFDYLVAHGRMKEKEARSKFRQIVSAVQYCHQKRIVHRDLKAENLLLDADMNIKIADFGFSNEFTVGGKLDTFCGSPPYAAPELFQGKKYDGPEVDVWSLGVILYTLVSGSLPFDGQNLKELRERVLRGKYRIPFYMSTDCENLLKRFLVLNPIKRGTLEQIMKDRWINAGHEEDELKPFVEPELDISDQKRIDIMVGMGYSQEEIQESLSKMKYDEITATYLLLGRKSSELDASDSSSSSNLSLAKVRPSSDLNNSTGQSPHHKVQRSVSSSQKQRRYSDHAGPAIPSVVAYPKRSQTSTADSDLKEDGISSRKSSGSAVGGKGIAPASPMLGNASNPNKADIPERKKSSTVPSSNTASGGMTRRNTYVCSERTTADRHSVIQNGKENSTIPDQRTPVASTHSISSAATPDRIRFPRGTASRSTFHGQPRERRTATYNGPPASPSLSHEATPLSQTRSRGSTNLFSKLTSKLTRRNMSFRFIKRLPTEYERNGRYEGSSRNVSAEQKDENKEAKPRSLRFTWSMKTTSSMDPGDMMREIRKVLDANNCDYEQRERFLLFCVHGDGHAENLVQWEMEVCKLPRLSLNGVRFKRISGTSIAFKNIASKIANELKL
  
Inhibitor
Name:
BDBM50208926
Synonyms:
CHEMBL3884179
Type:
Small organic molecule
Emp. Form.:
C21H20FN5O
Mol. Mass.:
377.4148
SMILES:
C[C@H](N1C(=O)C(C)(C)c2cnc(Nc3cccnc3)nc12)c1ccc(F)cc1 |r|
Structure:
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