Target
Tyrosine-protein kinase JAK1
Ligand
BDBM262166
Substrate
n/a
Meas. Tech.
Enzyme Assay
IC50
<10±n/a nM
Citation
 Zhou, JQiao, LWeng, L Process for the synthesis of a phosphoinositide 3-kinase inhibitor US Patent  US9732097 Publication Date 8/15/2017 
Target
Name:
Tyrosine-protein kinase JAK1
Synonyms:
JAK-1 | JAK1 | JAK1A | JAK1B | JAK1_HUMAN | Janus kinase 1 | Janus kinase 1 (JAK1) | Janus kinase 1 JAK1
Type:
Protein
Mol. Mass.:
133293.73
Organism:
Homo sapiens (Human)
Description:
P23458
Residue:
1154
Sequence:
MQYLNIKEDCNAMAFCAKMRSSKKTEVNLEAPEPGVEVIFYLSDREPLRLGSGEYTAEELCIRAAQACRISPLCHNLFALYDENTKLWYAPNRTITVDDKMSLRLHYRMRFYFTNWHGTNDNEQSVWRHSPKKQKNGYEKKKIPDATPLLDASSLEYLFAQGQYDLVKCLAPIRDPKTEQDGHDIENECLGMAVLAISHYAMMKKMQLPELPKDISYKRYIPETLNKSIRQRNLLTRMRINNVFKDFLKEFNNKTICDSSVSTHDLKVKYLATLETLTKHYGAEIFETSMLLISSENEMNWFHSNDGGNVLYYEVMVTGNLGIQWRHKPNVVSVEKEKNKLKRKKLENKHKKDEEKNKIREEWNNFSYFPEITHIVIKESVVSINKQDNKKMELKLSSHEEALSFVSLVDGYFRLTADAHHYLCTDVAPPLIVHNIQNGCHGPICTEYAINKLRQEGSEEGMYVLRWSCTDFDNILMTVTCFEKSEQVQGAQKQFKNFQIEVQKGRYSLHGSDRSFPSLGDLMSHLKKQILRTDNISFMLKRCCQPKPREISNLLVATKKAQEWQPVYPMSQLSFDRILKKDLVQGEHLGRGTRTHIYSGTLMDYKDDEGTSEEKKIKVILKVLDPSHRDISLAFFEAASMMRQVSHKHIVYLYGVCVRDVENIMVEEFVEGGPLDLFMHRKSDVLTTPWKFKVAKQLASALSYLEDKDLVHGNVCTKNLLLAREGIDSECGPFIKLSDPGIPITVLSRQECIERIPWIAPECVEDSKNLSVAADKWSFGTTLWEICYNGEIPLKDKTLIEKERFYESRCRPVTPSCKELADLMTRCMNYDPNQRPFFRAIMRDINKLEEQNPDIVSEKKPATEVDPTHFEKRFLKRIRDLGEGHFGKVELCRYDPEGDNTGEQVAVKSLKPESGGNHIADLKKEIEILRNLYHENIVKYKGICTEDGGNGIKLIMEFLPSGSLKEYLPKNKNKINLKQQLKYAVQICKGMDYLGSRQYVHRDLAARNVLVESEHQVKIGDFGLTKAIETDKEYYTVKDDRDSPVFWYAPECLMQSKFYIASDVWSFGVTLHELLTYCDSDSSPMALFLKMIGPTHGQMTVTRLVNTLKEGKRLPCPPNCPDEVYQLMRKCWEFQPSNRTSFQNLIEGFEALLK
  
Inhibitor
Name:
BDBM262166
Synonyms:
5-{3-(cyanomethyl)- 3-[4-(1H-pyrrolo[2,3- b]pyridin-4-yl)-1H- pyrazol-1-yl] azetidin-1-yl}-N- isopropylpyrazine- 2-carboxamide | US10065963, Compound 17 | US10125150, Example 17 | US10336759, # 17 | US10479803, Example 17 | US10513522, Example 34 | US10675284, Example 17 | US11084822, Example 17 | US11130767, # 17 | US11136326, Example 17 | US11214573, Example 34 | US11304949, Compound 17 | US11324749, Comp. No. 17 | US11406640, Comp. No. 17 | US11596632, Comp. No. 17 | US20240058343, Compound 17 | US9611269, Example 34 | US9708333, 17 | US9732097, Example 17
Type:
Small organic molecule
Emp. Form.:
C23H23N9O
Mol. Mass.:
441.4884
SMILES:
CC(C)NC(=O)c1cnc(cn1)N1CC(CC#N)(C1)n1cc(cn1)-c1ccnc2[nH]ccc12
Structure:
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