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Target
Tyrosine-protein kinase JAK1
Ligand
BDBM4313
Substrate
n/a
Meas. Tech.
ChEMBL_542085 (CHEMBL1016954)
IC50
3380±n/a nM
Citation
 Changelian, PS; Flanagan, ME; Ball, DJ; Kent, CR; Magnuson, KS; Martin, WH; Rizzuti, BJ; Sawyer, PS; Perry, BD; Brissette, WH; McCurdy, SP; Kudlacz, EM; Conklyn, MJ; Elliott, EA; Koslov, ER; Fisher, MB; Strelevitz, TJ; Yoon, K; Whipple, DA; Sun, J; Munchhof, MJ; Doty, JL; Casavant, JM; Blumenkopf, TA; Hines, M; Brown, MF; Lillie, BM; Subramanyam, C; Shang-Poa, C; Milici, AJ; Beckius, GE; Moyer, JD; Su, C; Woodworth, TG; Gaweco, AS; Beals, CR; Littman, BH; Fisher, DA; Smith, JF; Zagouras, P; Magna, HA; Saltarelli, MJ; Johnson, KS; Nelms, LF; Des Etages, SG; Hayes, LS; Kawabata, TT; Finco-Kent, D; Baker, DL; Larson, M; Si, MS; Paniagua, R; Higgins, J; Holm, B; Reitz, B; Zhou, YJ; Morris, RE; O'Shea, JJ; Borie, DC Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. Science 302:875-878 (2003) [PubMed]  Article 
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:
BDBM4313
Synonyms:
(2E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide | AG 490 | AG-490 | CHEMBL56543 | Tyrphostin AG 490 | Tyrphostin B42 | Tyrphostin deriv. 42
Type:
Small organic molecule
Emp. Form.:
C17H14N2O3
Mol. Mass.:
294.3047
SMILES:
Oc1ccc(\C=C(/C#N)C(=O)NCc2ccccc2)cc1O
Structure:
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