Ki Summary

Reaction Details

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Target

Tyrosine-protein kinase JAK2

Ligand

BDBM324634

Substrate/Competitor

n/a

Meas. Tech.

JAK Enzyme Assays

0.300±n/a nM

Citation

Cheng, Y; Hua, R; Kellar, T; Li, W; Gibbons, P; Zak, ME Therapeutic compounds, compositions and methods of use thereof US Patent US10189836 Publication Date 1/29/2019

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

BDBM324634

n/a

Name

BDBM324634

Synonyms:

1-[4-(2- methylsulfanylethyl)- piperazin-1-yl]-2-[4-[[8- [8-[3-(trifluoromethyl)- cyclobutanecarbonyl]-3,8- diazabicyclo[3.2.1]octan- 3-yl]-[1,2,4]triazolo[1,5-a] pyridin-2- yl]amino]pyrazol-1- yl]ethanone | US10189836, Example 197 | US10189836, Example 198

Type

Small organic molecule

Emp. Form.

C30H39F3N10O2S

Mol. Mass.

660.757

SMILES

CSCCN1CCN(CC1)C(=O)Cn1cc(Nc2nc3c(cccn3n2)N2CC3CCC(C2)N3C(=O)C2CC(C2)C(F)(F)F)cn1 |(-12.99,1.1,;-11.75,.19,;-10.34,.81,;-9.1,-.11,;-7.69,.51,;-6.45,-.4,;-5.04,.21,;-4.87,1.74,;-6.11,2.66,;-7.52,2.04,;-3.45,2.36,;-3.28,3.89,;-2.21,1.45,;-.8,2.07,;-.47,3.57,;1.06,3.72,;1.84,5.05,;3.38,5.05,;4.29,3.81,;5.75,4.28,;7.08,3.52,;8.42,4.29,;8.41,5.83,;7.08,6.6,;5.75,5.82,;4.28,6.3,;7.09,1.98,;5.76,1.2,;5.76,-.34,;6.37,.51,;7.82,.52,;8.43,-.33,;8.42,1.21,;7.09,-1.1,;7.1,-2.64,;5.77,-3.42,;8.43,-3.41,;8.84,-4.9,;10.32,-4.49,;9.92,-3.01,;11.66,-5.26,;10.89,-6.6,;12.43,-3.93,;12.99,-6.03,;1.68,2.31,;.53,1.29,)|

Structure