Reaction Details |
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Target | Transcription factor p65 |
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Ligand | BDBM158531 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1701708 (CHEMBL4052941) |
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IC50 | >20000±n/a nM |
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Citation | Castanedo, GM; Blaquiere, N; Beresini, M; Bravo, B; Brightbill, H; Chen, J; Cui, HF; Eigenbrot, C; Everett, C; Feng, J; Godemann, R; Gogol, E; Hymowitz, S; Johnson, A; Kayagaki, N; Kohli, PB; Knüppel, K; Kraemer, J; Krüger, S; Loke, P; McEwan, P; Montalbetti, C; Roberts, DA; Smith, M; Steinbacher, S; Sujatha-Bhaskar, S; Takahashi, R; Wang, X; Wu, LC; Zhang, Y; Staben, ST Structure-Based Design of Tricyclic NF-?B Inducing Kinase (NIK) Inhibitors That Have High Selectivity over Phosphoinositide-3-kinase (PI3K). J Med Chem60:627-640 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Transcription factor p65 |
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Name: | Transcription factor p65 |
Synonyms: | NFKB3 | Nuclear factor NF-kappa-B | Nuclear factor NF-kappa-B p65 subunit | RELA | TF65_HUMAN | v-rel reticuloendotheliosis viral oncogene homolog A isoform 1 |
Type: | Enzyme |
Mol. Mass.: | 60211.92 |
Organism: | Homo sapiens (Human) |
Description: | Q04206 |
Residue: | 551 |
Sequence: | MDELFPLIFPAEPAQASGPYVEIIEQPKQRGMRFRYKCEGRSAGSIPGERSTDTTKTHPT
IKINGYTGPGTVRISLVTKDPPHRPHPHELVGKDCRDGFYEAELCPDRCIHSFQNLGIQC
VKKRDLEQAISQRIQTNNNPFQVPIEEQRGDYDLNAVRLCFQVTVRDPSGRPLRLPPVLS
HPIFDNRAPNTAELKICRVNRNSGSCLGGDEIFLLCDKVQKEDIEVYFTGPGWEARGSFS
QADVHRQVAIVFRTPPYADPSLQAPVRVSMQLRRPSDRELSEPMEFQYLPDTDDRHRIEE
KRKRTYETFKSIMKKSPFSGPTDPRPPPRRIAVPSRSSASVPKPAPQPYPFTSSLSTINY
DEFPTMVFPSGQISQASALAPAPPQVLPQAPAPAPAPAMVSALAQAPAPVPVLAPGPPQA
VAPPAPKPTQAGEGTLSEALLQLQFDDEDLGALLGNSTDPAVFTDLASVDNSEFQQLLNQ
GIPVAPHTTEPMLMEYPEAITRLVTGAQRPPDPAPAPLGAPGLPNGLLSGDEDFSSIADM
DFSALLSQISS
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BDBM158531 |
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n/a |
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Name | BDBM158531 |
Synonyms: | US9034866, 6 |
Type | Small organic molecule |
Emp. Form. | C20H17FN4O4 |
Mol. Mass. | 396.3718 |
SMILES | Cc1cc(no1)[C@](C)(O)C#Cc1cc2-c3nc(cn3CCOc2cc1F)C(N)=O |r| |
Structure |
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