Ki Summary

Reaction Details

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Target

Tyrosine-protein kinase JAK2

Ligand

BDBM50545982

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_2013357 (CHEMBL4666935)

0.160000±n/a nM

Citation

Zak, M; Hanan, EJ; Lupardus, P; Brown, DG; Robinson, C; Siu, M; Lyssikatos, JP; Romero, FA; Zhao, G; Kellar, T; Mendonca, R; Ray, NC; Goodacre, SC; Crackett, PH; McLean, N; Hurley, CA; Yuen, PW; Cheng, YX; Liu, X; Liimatta, M; Kohli, PB; Nonomiya, J; Salmon, G; Buckley, G; Lloyd, J; Gibbons, P; Ghilardi, N; Kenny, JR; Johnson, A Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling. Bioorg Med Chem Lett29:1522-1531 (2019) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

Tyrosine-protein kinase JAK2

Name:

Tyrosine-protein kinase JAK2

Synonyms:

Type:

Protein

Mol. Mass.:

130684.68

Organism:

Homo sapiens (Human)

Description:

O60674

Residue:

1132

Sequence:

MGMACLTMTEMEGTSTSSIYQNGDISGNANSMKQIDPVLQVYLYHSLGKSEADYLTFPSG
EYVAEEICIAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHNVLYRIRFYF
PRWYCSGSNRAYRHGISRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLG
MAVLDMMRIAKENDQTPLAIYNSISYKTFLPKCIRAKIQDYHILTRKRIRYRFRRFIQQF
SQCKATARNLKLKYLINLETLQSAFYTEKFEVKEPGSGPSGEEIFATIIITGNGGIQWSR
GKHKESETLTEQDLQLYCDFPNIIDVSIKQANQEGSNESRVVTIHKQDGKNLEIELSSLR
EALSFVSLIDGYYRLTADAHHYLCKEVAPPAVLENIQSNCHGPISMDFAISKLKKAGNQT
GLYVLRCSPKDFNKYFLTFAVERENVIEYKHCLITKNENEEYNLSGTKKNFSSLKDLLNC
YQMETVRSDNIIFQFTKCCPPKPKDKSNLLVFRTNGVSDVPTSPTLQRPTHMNQMVFHKI
RNEDLIFNESLGQGTFTKIFKGVRREVGDYGQLHETEVLLKVLDKAHRNYSESFFEAASM
MSKLSHKHLVLNYGVCVCGDENILVQEFVKFGSLDTYLKKNKNCINILWKLEVAKQLAWA
MHFLEENTLIHGNVCAKNILLIREEDRKTGNPPFIKLSDPGISITVLPKDILQERIPWVP
PECIENPKNLNLATDKWSFGTTLWEICSGGDKPLSALDSQRKLQFYEDRHQLPAPKWAEL
ANLINNCMDYEPDFRPSFRAIIRDLNSLFTPDYELLTENDMLPNMRIGALGFSGAFEDRD
PTQFEERHLKFLQQLGKGNFGSVEMCRYDPLQDNTGEVVAVKKLQHSTEEHLRDFEREIE
ILKSLQHDNIVKYKGVCYSAGRRNLKLIMEYLPYGSLRDYLQKHKERIDHIKLLQYTSQI
CKGMEYLGTKRYIHRDLATRNILVENENRVKIGDFGLTKVLPQDKEYYKVKEPGESPIFW
YAPESLTESKFSVASDVWSFGVVLYELFTYIEKSKSPPAEFMRMIGNDKQGQMIVFHLIE
LLKNNGRLPRPDGCPDEIYMIMTECWNNNVNQRPSFRDLALRVDQIRDNMAG

BDBM50545982

n/a

Name

BDBM50545982

Synonyms:

CHEMBL4756876

Type

Small organic molecule

Emp. Form.

C17H10ClF3N6O2

Mol. Mass.

422.749

SMILES

FC(F)Oc1ccc(Cl)c(F)c1-c1n[nH]cc1NC(=O)c1cnn2cccnc12 |(22.91,-36.82,;23.68,-35.49,;25.22,-35.48,;22.91,-34.15,;23.67,-32.82,;25.21,-32.82,;25.98,-31.48,;25.19,-30.15,;25.95,-28.81,;23.66,-30.16,;22.88,-28.84,;22.91,-31.49,;21.37,-31.5,;20.87,-32.96,;19.33,-32.95,;18.86,-31.48,;20.12,-30.58,;20.13,-29.04,;18.8,-28.25,;17.45,-29.02,;18.81,-26.71,;17.56,-25.79,;18.05,-24.33,;19.59,-24.34,;20.63,-23.21,;22.12,-23.54,;22.59,-25.01,;21.55,-26.14,;20.05,-25.81,)|

Structure