Reaction Details |
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Target | MAP kinase-activated protein kinase 2 |
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Ligand | BDBM158154 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1577179 |
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IC50 | >10000±n/a nM |
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Citation | Menichincheri, M; Ardini, E; Magnaghi, P; Avanzi, N; Banfi, P; Bossi, R; Buffa, L; Canevari, G; Ceriani, L; Colombo, M; Corti, L; Donati, D; Fasolini, M; Felder, E; Fiorelli, C; Fiorentini, F; Galvani, A; Isacchi, A; Borgia, AL; Marchionni, C; Nesi, M; Orrenius, C; Panzeri, A; Pesenti, E; Rusconi, L; Saccardo, MB; Vanotti, E; Perrone, E; Orsini, P Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor. J Med Chem59:3392-408 (2016) [PubMed] |
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More Info.: | Get all data from this article, Assay Method |
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MAP kinase-activated protein kinase 2 |
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Name: | MAP kinase-activated protein kinase 2 |
Synonyms: | MAP kinase-activated protein kinase 2 (MAPKAPK2) | MAP kinase-activated protein kinase 2 (MK2) | MAP kinase-activated protein kinase 2 (p38/MK2) | MAPK-Activated Protein Kinase 2 (MK2) | MAPK-activated protein kinase 2 | MAPKAP kinase 2 | MAPKAPK-2 | MAPKAPK2 | MK2 |
Type: | Serine/threonine-protein kinase |
Mol. Mass.: | 45579.87 |
Organism: | Homo sapiens (human) |
Description: | MK2 was pre-activated in kinase buffer containing active human p38alpha for 30 min at room temperature before assays.
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Residue: | 400 |
Sequence: | MLSNSQGQSPPVPFPAPAPPPQPPTPALPHPPAQPPPPPPQQFPQFHVKSGLQIKKNAII
DDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRI
VDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSI
NIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSHNSLTTPCYTPYYVAPEVLGPEKY
DKSCDMWSLGVIMYILLCGYPPFYSNHGLAISPGMKTRIRMGQYEFPNPEWSEVSEEVKM
LIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLKEDKERWEDVKEEMTSAL
ATMRVDYEQIKIKKIEDASNPLLLKRRKKARALEAAALAH
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BDBM158154 |
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Name | BDBM158154 |
Synonyms: | US9029356, 11 | US9255087, 11 |
Type | Small organic molecule |
Emp. Form. | C31H34F2N6O2 |
Mol. Mass. | 560.6375 |
SMILES | CN1CCN(CC1)c1ccc(C(=O)Nc2n[nH]c3ccc(Cc4cc(F)cc(F)c4)cc23)c(NC2CCOCC2)c1 |
Structure |
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n/a |
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