Reaction Details |
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Target | [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial |
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Ligand | BDBM50021626 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1368016 (CHEMBL3300861) |
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IC50 | >10000±n/a nM |
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Citation | Casuscelli, F; Ardini, E; Avanzi, N; Casale, E; Cervi, G; D'Anello, M; Donati, D; Faiardi, D; Ferguson, RD; Fogliatto, G; Galvani, A; Marsiglio, A; Mirizzi, DG; Montemartini, M; Orrenius, C; Papeo, G; Piutti, C; Salom, B; Felder, ER Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases. Bioorg Med Chem21:7364-80 (2013) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial |
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Name: | [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial |
Synonyms: | PDHK1 | PDK1 | PDK1_HUMAN | Pyruvate dehydrogenase kinase | Pyruvate dehydrogenase kinase 1 (PDK1) | Pyruvate dehydrogenase kinase isoform 1 |
Type: | Protein |
Mol. Mass.: | 49255.23 |
Organism: | Homo sapiens (Human) |
Description: | Q15118 |
Residue: | 436 |
Sequence: | MRLARLLRGAALAGPGPGLRAAGFSRSFSSDSGSSPASERGVPGQVDFYARFSPSPLSMK
QFLDFGSVNACEKTSFMFLRQELPVRLANIMKEISLLPDNLLRTPSVQLVQSWYIQSLQE
LLDFKDKSAEDAKAIYDFTDTVIRIRNRHNDVIPTMAQGVIEYKESFGVDPVTSQNVQYF
LDRFYMSRISIRMLLNQHSLLFGGKGKGSPSHRKHIGSINPNCNVLEVIKDGYENARRLC
DLYYINSPELELEELNAKSPGQPIQVVYVPSHLYHMVFELFKNAMRATMEHHANRGVYPP
IQVHVTLGNEDLTVKMSDRGGGVPLRKIDRLFNYMYSTAPRPRVETSRAVPLAGFGYGLP
ISRLYAQYFQGDLKLYSLEGYGTDAVIYIKALSTDSIERLPVYNKAAWKHYNTNHEADDW
CVPSREPKDMTTFRSA
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BDBM50021626 |
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n/a |
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Name | BDBM50021626 |
Synonyms: | CHEMBL3298400 |
Type | Small organic molecule |
Emp. Form. | C18H23N3O2S |
Mol. Mass. | 345.459 |
SMILES | CC(C)(C)CNC(=O)CC1CNC(=O)c2cc(cn12)-c1ccsc1 |
Structure |
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