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Target
Tyrosine-protein kinase JAK1
Ligand
BDBM390999
Substrate
n/a
Meas. Tech.
Biochemical HTRF Assay
IC50
0.070±n/a nM
Citation
Childers, ML; Fuller, P; Guerin, D; Katz, JD; Pu, Q; Scott, ME; Thompson, CF; Martinez, M; Falcone, D; Torres, L; Deng, Y; Kurukulasuriya, R; Zeng, H; Bai, Y; Kong, N; Liu, Y; Zheng, Z Geminally substituted cyanoethylpyrazolo pyridones as Janus kinase inhibitors US Patent US9957264 Publication Date 5/1/2018
More Info.:
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:
BDBM390999
Synonyms:
US9957264, Example 5-70 | methyl 4-(cyanomethyl)-4- [3-[(2-methyl-1,1-dioxo-2,3- dihydro-1,2-benzothiazol-5- yl)amino]-4-oxo-1H,4H,5H- pyrazolo[4,3-c]pyridin-1- yl]piperidine-1-carboxylate
Type:
Small organic molecule
Emp. Form.:
C23H25N7O5S
Mol. Mass.:
511.554
SMILES:
COC(=O)N1CCC(CC#N)(CC1)n1nc(Nc2ccc3c(CN(C)S3(=O)=O)c2)c2c1cc[nH]c2=O