Reaction Details |
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Target | Cyclin-T1/Cyclin-dependent kinase 9 |
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Ligand | BDBM454567 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2025111 (CHEMBL4678924) |
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IC50 | 3.0±n/a nM |
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Citation | Barlaam, B; Casella, R; Cidado, J; Cook, C; De Savi, C; Dishington, A; Donald, CS; Drew, L; Ferguson, AD; Ferguson, D; Glossop, S; Grebe, T; Gu, C; Hande, S; Hawkins, J; Hird, AW; Holmes, J; Horstick, J; Jiang, Y; Lamb, ML; McGuire, TM; Moore, JE; O'Connell, N; Pike, A; Pike, KG; Proia, T; Roberts, B; San Martin, M; Sarkar, U; Shao, W; Stead, D; Sumner, N; Thakur, K; Vasbinder, MM; Varnes, JG; Wang, J; Wang, L; Wu, D; Wu, L; Yang, B; Yao, T Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies. J Med Chem63:15564-15590 (2020) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Cyclin-T1/Cyclin-dependent kinase 9 |
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Name: | Cyclin-T1/Cyclin-dependent kinase 9 |
Synonyms: | CDK9/ Cyclin-T1 | CDK9/CycT1 | CDK9/Cyclin T | CDK9/Cyclin T1 | Cyclin T1/dependent kinase 9 | Cyclin-Dependent Kinase 9 (CDK9) |
Type: | Protein Complex |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 2 components. |
Component 1 |
Name: | Cyclin-T1 |
Synonyms: | CCNT1 | CCNT1_HUMAN | CycT | CycT1 | Cyclin T | Cyclin T1 | Cyclin-T |
Type: | Enzyme Subunit |
Mol. Mass.: | 80712.40 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 726 |
Sequence: | MEGERKNNNKRWYFTREQLENSPSRRFGVDPDKELSYRQQAANLLQDMGQRLNVSQLTIN
TAIVYMHRFYMIQSFTQFPGNSVAPAALFLAAKVEEQPKKLEHVIKVAHTCLHPQESLPD
TRSEAYLQQVQDLVILESIILQTLGFELTIDHPHTHVVKCTQLVRASKDLAQTSYFMATN
SLHLTTFSLQYTPPVVACVCIHLACKWSNWEIPVSTDGKHWWEYVDATVTLELLDELTHE
FLQILEKTPNRLKRIWNWRACEAAKKTKADDRGTDEKTSEQTILNMISQSSSDTTIAGLM
SMSTSTTSAVPSLPVSEESSSNLTSVEMLPGKRWLSSQPSFKLEPTQGHRTSENLALTGV
DHSLPQDGSNAFISQKQNSKSVPSAKVSLKEYRAKHAEELAAQKRQLENMEANVKSQYAY
AAQNLLSHHDSHSSVILKMPIEGSENPERPFLEKADKTALKMRIPVAGGDKAASSKPEEI
KMRIKVHAAADKHNSVEDSVTKSREHKEKHKTHPSNHHHHHNHHSHKHSHSQLPVGTGNK
RPGDPKHSSQTSNLAHKTYSLSSSFSSSSSTRKRGPSEETGGAVFDHPAKIAKSTKSSSL
NFSFPSLPTMGQMPGHSSDTSGLSFSQPSCKTRVPHSKLDKGPTGANGHNTTQTIDYQDT
VNMLHSLLSAQGVQPTQPTAFEFVRPYSDYLNPRSGGISSRSGNTDKPRPPPLPSEPPPP
LPPLPK
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Component 2 |
Name: | Cyclin-dependent kinase 9 |
Synonyms: | C-2K | CDC2L4 | CDK9 | CDK9_HUMAN | Cell division cycle 2-like protein kinase 4 | Cell division protein kinase 9 | Cyclin-Dependent Kinase 9 (CDK9) | Cyclin-dependent kinase 9 (CDK9) | Serine/threonine-protein kinase PITALRE | TAK | Tat-associated kinase complex catalytic subunit |
Type: | Enzyme Subunit |
Mol. Mass.: | 42789.13 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 372 |
Sequence: | MAKQYDSVECPFCDEVSKYEKLAKIGQGTFGEVFKARHRKTGQKVALKKVLMENEKEGFP
ITALREIKILQLLKHENVVNLIEICRTKASPYNRCKGSIYLVFDFCEHDLAGLLSNVLVK
FTLSEIKRVMQMLLNGLYYIHRNKILHRDMKAANVLITRDGVLKLADFGLARAFSLAKNS
QPNRYTNRVVTLWYRPPELLLGERDYGPPIDLWGAGCIMAEMWTRSPIMQGNTEQHQLAL
ISQLCGSITPEVWPNVDNYELYEKLELVKGQKRKVKDRLKAYVRDPYALDLIDKLLVLDP
AQRIDSDDALNHDFFWSDPMPSDLKGMLSTHLTSMFEYLAPPRRKGSQITQQSTNQSRNP
ATTNQTEFERVF
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BDBM454567 |
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n/a |
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Name | BDBM454567 |
Synonyms: | US10717746, Example 48 |
Type | Small organic molecule |
Emp. Form. | C21H26ClN5O2 |
Mol. Mass. | 415.916 |
SMILES | CC(=O)N[C@@H]1CC[C@@H](C1)C(=O)Nc1cc(-c2cnn3CC(C)(C)Cc23)c(Cl)cn1 |r| |
Structure |
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