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Target
Mitogen-activated protein kinase kinase kinase kinase 1
Ligand
BDBM503999
Substrate
n/a
Meas. Tech.
Binding Assay
Ki
0.021±n/a nM
Citation
 Chan, B; Daniels, B; Drobnick, J; Gazzard, L; Heffron, T; Huestis, M; Liang, J; Malhotra, S; Mendonca, R; Rajapaksa, N; Siu, M; Stivala, C; Tellis, J; Wang, W; Wei, B; Zhou, A; Cartwright, MW; Gancia, E; Jones, G; Lainchbury, M; Madin, A; Seward, E; Favor, D; Fong, KC; Good, A; Hu, Y; Hu, B; Lu, A Naphthyridines as inhibitors of HPK1 US Patent  US11034692 Publication Date 6/15/2021 
Target
Name:
Mitogen-activated protein kinase kinase kinase kinase 1
Synonyms:
HPK1 | M4K1_HUMAN | MAP4K1
Type:
PROTEIN
Mol. Mass.:
91316.07
Organism:
Homo sapiens (Human)
Description:
ChEMBL_586597
Residue:
833
Sequence:
MDVVDPDIFNRDPRDHYDLLQRLGGGTYGEVFKARDKVSGDLVALKMVKMEPDDDVSTLQKEILILKTCRHANIVAYHGSYLWLQKLWICMEFCGAGSLQDIYQVTGSLSELQISYVCREVLQGLAYLHSQKKIHRDIKGANILINDAGEVRLADFGISAQIGATLARRLSFIGTPYWMAPEVAAVALKGGYNELCDIWSLGITAIELAELQPPLFDVHPLRVLFLMTKSGYQPPRLKEKGKWSAAFHNFIKVTLTKSPKKRPSATKMLSHQLVSQPGLNRGLILDLLDKLKNPGKGPSIGDIEDEEPELPPAIPRRIRSTHRSSSLGIPDADCCRRHMEFRKLRGMETRPPANTARLQPPRDLRSSSPRKQLSESSDDDYDDVDIPTPAEDTPPPLPPKPKFRSPSDEGPGSMGDDGQLSPGVLVRCASGPPPNSPRPGPPPSTSSPHLTAHSEPSLWNPPSRELDKPPLLPPKKEKMKRKGCALLVKLFNGCPLRIHSTAAWTHPSTKDQHLLLGAEEGIFILNRNDQEATLEMLFPSRTTWVYSINNVLMSLSGKTPHLYSHSILGLLERKETRAGNPIAHISPHRLLARKNMVSTKIQDTKGCRACCVAEGASSGGPFLCGALETSVVLLQWYQPMNKFLLVRQVLFPLPTPLSVFALLTGPGSELPAVCIGVSPGRPGKSVLFHTVRFGALSCWLGEMSTEHRGPVQVTQVEEDMVMVLMDGSVKLVTPEGSPVRGLRTPEIPMTEAVEAVAMVGGQLQAFWKHGVQVWALGSDQLLQELRDPTLTFRLLGSPRLECSGTISPHCNLLLPGSSNSPASASRVAGITGL
  
Inhibitor
Name:
BDBM503999
Synonyms:
3-[[8-Amino-6-(4-methylpyridin-3-yl)-2,7- naphthyridin-3-yl]amino]-N,1-dimethyl- 1H-pyrazole-5-carboxamide | US11034692, Compound 263
Type:
Small organic molecule
Emp. Form.:
C20H20N8O
Mol. Mass.:
388.4258
SMILES:
CNC(=O)c1cc(Nc2cc3cc(nc(N)c3cn2)-c2cnccc2C)nn1C
Structure:
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