Target
Tyrosine-protein kinase JAK3
Ligand
BDBM325438
Substrate
n/a
Meas. Tech.
JAK3 Inhibition Assay
IC50
5500±n/a nM
Citation
 Allen, SBoys, MLChicarelli, MJFell, JBFischer, JPGaudino, JHicken, EJHinklin, RJKraser, CFLaird, ERobinson, JETang, TPBurgess, LERieger, RAPheneger, JSatoh, YLeftheris, KRaheja, RKBennett, BL 4,6-substituted-pyrazolo[1,5-a]pyrazines as Janus kinase inhibitors US Patent  US10730880 Publication Date 8/4/2020 
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:
BDBM325438
Synonyms:
(R)-1-(methylamino)-3- (4-(4-(1-(pentan-3-yl)- 1H-pyrazol-4- yl)pyrazolo[1,5- a]pyrazin-6-yl)-1H- pyrazol-1-yl)propan-2-ol | US10189845, Example 100 | US10730880, Example 100 | US11028093, Example 100
Type:
Small organic molecule
Emp. Form.:
C21H28N8O
Mol. Mass.:
408.5
SMILES:
CCC(CC)n1cc(cn1)-c1nc(cn2nccc12)-c1cnn(C[C@H](O)CNC)c1 |r|
Structure:
Search PDB for entries with ligand similarity: