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Target
Tyrosine-protein kinase JAK1
Ligand
BDBM26198
Substrate
n/a
Meas. Tech.
ChEBML_91943
IC50
15±n/a nM
Citation
 Thompson, JE; Cubbon, RM; Cummings, RT; Wicker, LS; Frankshun, R; Cunningham, BR; Cameron, PM; Meinke, PT; Liverton, N; Weng, Y; DeMartino, JA Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor. Bioorg Med Chem Lett 12:1219-23 (2002) [PubMed]  Article 
Target
Name:
Tyrosine-protein kinase JAK1
Synonyms:
JAK-1 | JAK1_MOUSE | Jak1 | Janus kinase 1 | Tyrosine-protein kinase JAK1 | Tyrosine-protein kinase JAK1/JAK3
Type:
PROTEIN
Mol. Mass.:
133384.57
Organism:
Mus musculus
Description:
ChEMBL_1291227
Residue:
1153
Sequence:
MQYLNIKEDCNAMAFCAKMRSFKKTEVKQVVPEPGVEVTFYLLDREPLRLGSGEYTAEELCIRAAQECSISPLCHNLFALYDESTKLWYAPNRIITVDDKTSLRLHYRMRFYFTNWHGTNDNEQSVWRHSPKKQKNGYEKKRVPEATPLLDASSLEYLFAQGQYDLIKCLAPIRDPKTEQDGHDIENECLGMAVLAISHYAMMKKMQLPELPKDISYKRYIPETLNKSIRQRNLLTRMRINNVFKDFLKEFNNKTICDSSVHDLKVKYLATLETSTLTKHYGAEIFETSMLLISSENELSRCHSNDSGNVLYEVMVTGNLGIQWRQKPNVVPVEKEKNKLKRKKLEYNKHKKDDERNKLREEWNNFSYFPEITHIVIKESVVSINKQDNKNMELKLSSREEALSFVSLVDGYFRLTADAHHYLCTDVAPPLIVHNIQNGCHGPICTEYAINKLRQEGSEEGMYVLRWSCTDFDNILMTVTCFEKSEVLGGQKQFKNFQIEVQKGRYSLHGSMDHFPSLRDLMNHLKKQILRTDNISFVLKRCCQPKPREISNLLVATKKAQEWQPVYSMSQLSFDRILKKDIIQGEHLGRGTRTHIYSGTLLDYKDEEGIAEEKKIKVILKVLDPSHRDISLAFFEAASMMRQVSHKHIVYLYGVCVRDVENIMVEEFVEGGPLDLFMHRKSDALTTPWKFKVAKQLASALSYLEDKDLVHGNVCTKNLLLAREGIDSDIGPFIKLSDPGIPVSVLTRQECIERIPWIAPECVEDSKNLSVAADKWSFGTTLWEICYNGEIPLKDKTLIEKERFYESRCRPVTPSCKELADLMTRCMNYDPNQRPFFRAIMRDINKLEEQNPDIVSEKQPTTEVDPTHFEKRFLKRIRDLGEGHFGKVELCRYDPEGDNTGEQVAVKSLKPESGGNHIADLKKEIEILRNLYHENIVKYKGICMEDGGNGIKLIMEFLPSGSLKEYLPKNKNKINLKQQLKYAIQICKGMDYLGSRQYVHRDLAARNVLVESEHQVKIGDFGLTKAIETDKEYYTVKDDRDSPVFWYAPECLIQCKFYIASDVWSFGVTLHELLTYCDSDFSPMALFLKMIGPTHGQMTVTRLVKTLKEGKRLPCPPNCPDEVYQLMRKCWEFQPSNRTTFQNLIEGFEALLK
  
Inhibitor
Name:
BDBM26198
Synonyms:
4-tert-butyl-15-fluoro-3,5,10-triazatetracyclo[11.4.0.0^{2,6}.0^{7,12}]heptadeca-1(13),2(6),3,7(12),8,14,16-heptaen-11-one | CHEMBL21156 | Compound # 2 | Jak Inhibitor 1 | PDK1 inhibitor, 1 | Tetracyclic Pyridone, 1
Type:
Small organic molecule
Emp. Form.:
C18H16FN3O
Mol. Mass.:
309.3375
SMILES:
CC(C)(C)c1nc2c([nH]1)c1ccc(F)cc1c1c2cc[nH]c1=O
Structure:
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