Reaction Details |
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Target | Interleukin-1 receptor-associated kinase 4 |
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Ligand | BDBM50239494 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1666148 (CHEMBL4015944) |
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IC50 | 12±n/a nM |
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Citation | Lee, KL; Ambler, CM; Anderson, DR; Boscoe, BP; Bree, AG; Brodfuehrer, JI; Chang, JS; Choi, C; Chung, S; Curran, KJ; Day, JE; Dehnhardt, CM; Dower, K; Drozda, SE; Frisbie, RK; Gavrin, LK; Goldberg, JA; Han, S; Hegen, M; Hepworth, D; Hope, HR; Kamtekar, S; Kilty, IC; Lee, A; Lin, LL; Lovering, FE; Lowe, MD; Mathias, JP; Morgan, HM; Murphy, EA; Papaioannou, N; Patny, A; Pierce, BS; Rao, VR; Saiah, E; Samardjiev, IJ; Samas, BM; Shen, MWH; Shin, JH; Soutter, HH; Strohbach, JW; Symanowicz, PT; Thomason, JR; Trzupek, JD; Vargas, R; Vincent, F; Yan, J; Zapf, CW; Wright, SW Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design. J Med Chem60:5521-5542 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Interleukin-1 receptor-associated kinase 4 |
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Name: | Interleukin-1 receptor-associated kinase 4 |
Synonyms: | IRAK-4 | IRAK4 | IRAK4_HUMAN | Interleukin-1 receptor-associated kinase 4 (IRAK-4) | Interleukin-1 receptor-associated kinase 4 (IRAK4) | Renal carcinoma antigen NY-REN-64 |
Type: | Protein |
Mol. Mass.: | 51519.08 |
Organism: | Homo sapiens (Human) |
Description: | Q9NWZ3 |
Residue: | 460 |
Sequence: | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALL
QTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITV
QQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNF
DERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKC
QHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGIN
FLHENHHIHRDIKSANILLDEAFTAKISDFGLARASEKFAQTVMTSRIVGTTAYMAPEAL
RGEITPKSDIYSFGVVLLEIITGLPAVDEHREPQLLLDIKEEIEDEEKTIEDYIDKKMND
ADSTSVEAMYSVASQCLHEKKNKRPDIKKVQQLLQEMTAS
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BDBM50239494 |
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n/a |
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Name | BDBM50239494 |
Synonyms: | CHEMBL4079243 | US10329302, Example 340 | US10793579, Example 340 | US11702424, Example 340 |
Type | Small organic molecule |
Emp. Form. | C18H21N3O5 |
Mol. Mass. | 359.3764 |
SMILES | COC[C@@H]1CC(=O)N[C@@H]1COc1nccc2cc(C(N)=O)c(OC)cc12 |r| |
Structure |
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