Reaction Details |
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Target | Tyrosine-protein kinase JAK3 |
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Ligand | BDBM50377357 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_479566 (CHEMBL929430) |
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IC50 | >50000±n/a nM |
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Citation | Ruel, R; Thibeault, C; L'Heureux, A; Martel, A; Cai, ZW; Wei, D; Qian, L; Barrish, JC; Mathur, A; D'Arienzo, C; Hunt, JT; Kamath, A; Marathe, P; Zhang, Y; Derbin, G; Wautlet, B; Mortillo, S; Jeyaseelan, R; Henley, B; Tejwani, R; Bhide, RS; Trainor, GL; Fargnoli, J; Lombardo, LJ Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor. Bioorg Med Chem Lett18:2985-9 (2008) [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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BDBM50377357 |
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n/a |
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Name | BDBM50377357 |
Synonyms: | CHEMBL258694 |
Type | Small organic molecule |
Emp. Form. | C19H18N8O |
Mol. Mass. | 374.3992 |
SMILES | CC(C)c1c(cn2ncnc(Nc3cnc4[nH]ccc4c3)c12)-c1nnc(C)o1 |
Structure |
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