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Target
Mitogen-activated protein kinase kinase kinase kinase 1
Ligand
BDBM504004
Substrate
n/a
Meas. Tech.
Binding Assay
Ki
0.147±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:
BDBM504004
Synonyms:
US11034692, Compound 268 | trans-N-[8-amino-6-(5-hydroxy-2- methylphenyl)-2,7-naphthyridin-3-yl]-2- (1-methyl-1H-pyrazol-4-yl)cyclopropane- 1-carboxamide
Type:
Small organic molecule
Emp. Form.:
C23H22N6O2
Mol. Mass.:
414.4598
SMILES:
Cc1ccc(O)cc1-c1cc2cc(NC(=O)C3CC3c3cnn(C)c3)ncc2c(N)n1
Structure:
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