Reaction Details |
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Target | Tyrosine-protein kinase JAK3 |
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Ligand | BDBM99611 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_833042 (CHEMBL2067181) |
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IC50 | 105±n/a nM |
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Citation | Dugan, BJ; Gingrich, DE; Mesaros, EF; Milkiewicz, KL; Curry, MA; Zulli, AL; Dobrzanski, P; Serdikoff, C; Jan, M; Angeles, TS; Albom, MS; Mason, JL; Aimone, LD; Meyer, SL; Huang, Z; Wells-Knecht, KJ; Ator, MA; Ruggeri, BA; Dorsey, BD A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of Janus kinase 2 for use in anticancer therapy: discovery of CEP-33779. J Med Chem55:5243-54 (2012) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Tyrosine-protein kinase JAK3 |
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Name: | Tyrosine-protein kinase JAK3 |
Synonyms: | JAK-3 | JAK3 | JAK3_HUMAN | Janus kinase 3 | Janus kinase 3 (JAK3) | Janus kinase 3 JAK3 | L-JAK | Leukocyte janus kinase |
Type: | Protein |
Mol. Mass.: | 125111.08 |
Organism: | Homo sapiens (Human) |
Description: | P52333 |
Residue: | 1124 |
Sequence: | MAPPSEETPLIPQRSCSLLSTEAGALHVLLPARGPGPPQRLSFSFGDHLAEDLCVQAAKA
SGILPVYHSLFALATEDLSCWFPPSHIFSVEDASTQVLLYRIRFYFPNWFGLEKCHRFGL
RKDLASAILDLPVLEHLFAQHRSDLVSGRLPVGLSLKEQGECLSLAVLDLARMAREQAQR
PGELLKTVSYKACLPPSLRDLIQGLSFVTRRRIRRTVRRALRRVAACQADRHSLMAKYIM
DLERLDPAGAAETFHVGLPGALGGHDGLGLLRVAGDGGIAWTQGEQEVLQPFCDFPEIVD
ISIKQAPRVGPAGEHRLVTVTRTDNQILEAEFPGLPEALSFVALVDGYFRLTTDSQHFFC
KEVAPPRLLEEVAEQCHGPITLDFAINKLKTGGSRPGSYVLRRSPQDFDSFLLTVCVQNP
LGPDYKGCLIRRSPTGTFLLVGLSRPHSSLRELLATCWDGGLHVDGVAVTLTSCCIPRPK
EKSNLIVVQRGHSPPTSSLVQPQSQYQLSQMTFHKIPADSLEWHENLGHGSFTKIYRGCR
HEVVDGEARKTEVLLKVMDAKHKNCMESFLEAASLMSQVSYRHLVLLHGVCMAGDSTMVQ
EFVHLGAIDMYLRKRGHLVPASWKLQVVKQLAYALNYLEDKGLPHGNVSARKVLLAREGA
DGSPPFIKLSDPGVSPAVLSLEMLTDRIPWVAPECLREAQTLSLEADKWGFGATVWEVFS
GVTMPISALDPAKKLQFYEDRQQLPAPKWTELALLIQQCMAYEPVQRPSFRAVIRDLNSL
ISSDYELLSDPTPGALAPRDGLWNGAQLYACQDPTIFEERHLKYISQLGKGNFGSVELCR
YDPLGDNTGALVAVKQLQHSGPDQQRDFQREIQILKALHSDFIVKYRGVSYGPGRQSLRL
VMEYLPSGCLRDFLQRHRARLDASRLLLYSSQICKGMEYLGSRRCVHRDLAARNILVESE
AHVKIADFGLAKLLPLDKDYYVVREPGQSPIFWYAPESLSDNIFSRQSDVWSFGVVLYEL
FTYCDKSCSPSAEFLRMMGCERDVPALCRLLELLEEGQRLPAPPACPAEVHELMKLCWAP
SPQDRPSFSALGPQLDMLWSGSRGCETHAFTAHPEGKHHSLSFS
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BDBM99611 |
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n/a |
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Name | BDBM99611 |
Synonyms: | CHEMBL2062801 | US8501936, 112 |
Type | Small organic molecule |
Emp. Form. | C20H18N4O4S2 |
Mol. Mass. | 442.511 |
SMILES | CS(=O)(=O)c1ccc(Nc2nc3c(cccn3n2)-c2ccc(cc2)S(C)(=O)=O)cc1 |
Structure |
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