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Target
Tyrosine-protein kinase JAK1
Ligand
BDBM543516
Substrate
n/a
Meas. Tech.
HotSpot Kinase Assay
IC50
2.70±n/a nM
Citation
 Schönbrunn, E; Lawrence, NJ; Lawrence, HR BRD4-kinase inhibitors as cancer therapeutics US Patent  US11643396 Publication Date 5/9/2023 
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:
BDBM543516
Synonyms:
US11279703, TABLE 6.119 | US11279703, TABLE 6.128 | US11279703, TABLE 6.149 | US11279703, TABLE 6.154 | US11279703, TABLE 6.168 | US11279703, TABLE 6.181 | US11279703, TABLE 6.194 | US11279703, TABLE 6.199 | US11279703, TABLE 6.204 | US11279703, TABLE 6.215 | US11279703, TABLE 6.244 | US11279703, TABLE 6.262 | US11279703, TABLE 6.276 | US11279703, TABLE 6.298 | US11279703, TABLE 6.307 | US11279703, TABLE 6.314 | US11279703, TABLE 6.319 | US11279703, TABLE 6.328 | US11279703, TABLE 6.37 | US11643396, Example MA2-014
Type:
Small organic molecule
Emp. Form.:
C26H35N7O2S
Mol. Mass.:
509.667
SMILES:
CN1CCN(CC1)c1ccc(Nc2ncc(C)c(Nc3cccc(NS(=O)(=O)C(C)(C)C)c3)n2)cc1
Structure:
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