Reaction Details |
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Target | MAP/microtubule affinity-regulating kinase 3 |
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Ligand | BDBM50208912 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1633686 (CHEMBL3876478) |
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IC50 | 738±n/a nM |
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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 Lett27:109-113 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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MAP/microtubule affinity-regulating kinase 3 |
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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: | MSTRTPLPTVNERDTENHTSHGDGRQEVTSRTSRSGARCRNSIASCADEQPHIGNYRLLK
TIGKGNFAKVKLARHILTGREVAIKIIDKTQLNPTSLQKLFREVRIMKILNHPNIVKLFE
VIETEKTLYLIMEYASGGEVFDYLVAHGRMKEKEARSKFRQIVSAVQYCHQKRIVHRDLK
AENLLLDADMNIKIADFGFSNEFTVGGKLDTFCGSPPYAAPELFQGKKYDGPEVDVWSLG
VILYTLVSGSLPFDGQNLKELRERVLRGKYRIPFYMSTDCENLLKRFLVLNPIKRGTLEQ
IMKDRWINAGHEEDELKPFVEPELDISDQKRIDIMVGMGYSQEEIQESLSKMKYDEITAT
YLLLGRKSSELDASDSSSSSNLSLAKVRPSSDLNNSTGQSPHHKVQRSVSSSQKQRRYSD
HAGPAIPSVVAYPKRSQTSTADSDLKEDGISSRKSSGSAVGGKGIAPASPMLGNASNPNK
ADIPERKKSSTVPSSNTASGGMTRRNTYVCSERTTADRHSVIQNGKENSTIPDQRTPVAS
THSISSAATPDRIRFPRGTASRSTFHGQPRERRTATYNGPPASPSLSHEATPLSQTRSRG
STNLFSKLTSKLTRRNMSFRFIKRLPTEYERNGRYEGSSRNVSAEQKDENKEAKPRSLRF
TWSMKTTSSMDPGDMMREIRKVLDANNCDYEQRERFLLFCVHGDGHAENLVQWEMEVCKL
PRLSLNGVRFKRISGTSIAFKNIASKIANELKL
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BDBM50208912 |
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n/a |
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Name | BDBM50208912 |
Synonyms: | CHEMBL3883766 |
Type | Small organic molecule |
Emp. Form. | C17H21N5O |
Mol. Mass. | 311.3815 |
SMILES | CC[C@@H](C)N1C(=O)C(C)(C)c2cnc(Nc3cccnc3)nc12 |r| |
Structure |
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