Target
Tyrosine-protein kinase JAK3
Ligand
BDBM50348880
Substrate
n/a
Meas. Tech.
ChEMBL_758501 (CHEMBL1811579)
IC50
>25000±n/a nM
Citation
 Dyckman, AJLi, TPitt, SZhang, RShen, DRMcIntyre, KWGillooly, KMShuster, DJDoweyko, AMSack, JSKish, KKiefer, SENewitt, JAZhang, HMarathe, PHMcKinnon, MBarrish, JCDodd, JHSchieven, GLLeftheris, K Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors. Bioorg Med Chem Lett 21:4633-7 (2011) [PubMed]  Article
Target
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:
MAPPSEETPLIPQRSCSLLSTEAGALHVLLPARGPGPPQRLSFSFGDHLAEDLCVQAAKASGILPVYHSLFALATEDLSCWFPPSHIFSVEDASTQVLLYRIRFYFPNWFGLEKCHRFGLRKDLASAILDLPVLEHLFAQHRSDLVSGRLPVGLSLKEQGECLSLAVLDLARMAREQAQRPGELLKTVSYKACLPPSLRDLIQGLSFVTRRRIRRTVRRALRRVAACQADRHSLMAKYIMDLERLDPAGAAETFHVGLPGALGGHDGLGLLRVAGDGGIAWTQGEQEVLQPFCDFPEIVDISIKQAPRVGPAGEHRLVTVTRTDNQILEAEFPGLPEALSFVALVDGYFRLTTDSQHFFCKEVAPPRLLEEVAEQCHGPITLDFAINKLKTGGSRPGSYVLRRSPQDFDSFLLTVCVQNPLGPDYKGCLIRRSPTGTFLLVGLSRPHSSLRELLATCWDGGLHVDGVAVTLTSCCIPRPKEKSNLIVVQRGHSPPTSSLVQPQSQYQLSQMTFHKIPADSLEWHENLGHGSFTKIYRGCRHEVVDGEARKTEVLLKVMDAKHKNCMESFLEAASLMSQVSYRHLVLLHGVCMAGDSTMVQEFVHLGAIDMYLRKRGHLVPASWKLQVVKQLAYALNYLEDKGLPHGNVSARKVLLAREGADGSPPFIKLSDPGVSPAVLSLEMLTDRIPWVAPECLREAQTLSLEADKWGFGATVWEVFSGVTMPISALDPAKKLQFYEDRQQLPAPKWTELALLIQQCMAYEPVQRPSFRAVIRDLNSLISSDYELLSDPTPGALAPRDGLWNGAQLYACQDPTIFEERHLKYISQLGKGNFGSVELCRYDPLGDNTGALVAVKQLQHSGPDQQRDFQREIQILKALHSDFIVKYRGVSYGPGRQSLRLVMEYLPSGCLRDFLQRHRARLDASRLLLYSSQICKGMEYLGSRRCVHRDLAARNILVESEAHVKIADFGLAKLLPLDKDYYVVREPGQSPIFWYAPESLSDNIFSRQSDVWSFGVVLYELFTYCDKSCSPSAEFLRMMGCERDVPALCRLLELLEEGQRLPAPPACPAEVHELMKLCWAPSPQDRPSFSALGPQLDMLWSGSRGCETHAFTAHPEGKHHSLSFS
  
Inhibitor
Name:
BDBM50348880
Synonyms:
CHEMBL1807446
Type:
Small organic molecule
Emp. Form.:
C25H23N5O2
Mol. Mass.:
425.4824
SMILES:
Cc1c(cn2ncnc(Nc3cc(ccc3C)C(=O)NC3CC3)c12)C(=O)c1ccccc1
Structure:
Search PDB for entries with ligand similarity: