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Target
Mitogen-activated protein kinase kinase kinase kinase 1
Ligand
BDBM591233
Substrate
n/a
Meas. Tech.
HPK1-FL HTRF Enzymatic Assay
Ki
0.017±n/a nM
Citation
 Chan, B; Drobnick, J; Gazzard, L; Heffron, T; Liang, J; Malhotra, S; Mendonca, R; Rajapaksa, N; Stivala, C; Tellis, J; Wang, W; Wei, B; Zhou, A; Cartwright, MW; Lainchbury, M; Gancia, E; Seward, E; Madin, A; Favor, D; Fong, KC; Hu, Y; Good, A Isoquinolines as inhibitors of HPK1 US Patent  US11566003 Publication Date 1/31/2023 
Target
Name:
Mitogen-activated protein kinase kinase kinase kinase 1
Synonyms:
HPK1 | M4K1_HUMAN | MAP4K1
Type:
PROTEIN
Mol. Mass.:
91316.07
Organism:
Human
Description:
ChEMBL_586597
Residue:
833
Sequence:
MDVVDPDIFNRDPRDHYDLLQRLGGGTYGEVFKARDKVSGDLVALKMVKMEPDDDVSTLQKEILILKTCRHANIVAYHGSYLWLQKLWICMEFCGAGSLQDIYQVTGSLSELQISYVCREVLQGLAYLHSQKKIHRDIKGANILINDAGEVRLADFGISAQIGATLARRLSFIGTPYWMAPEVAAVALKGGYNELCDIWSLGITAIELAELQPPLFDVHPLRVLFLMTKSGYQPPRLKEKGKWSAAFHNFIKVTLTKSPKKRPSATKMLSHQLVSQPGLNRGLILDLLDKLKNPGKGPSIGDIEDEEPELPPAIPRRIRSTHRSSSLGIPDADCCRRHMEFRKLRGMETRPPANTARLQPPRDLRSSSPRKQLSESSDDDYDDVDIPTPAEDTPPPLPPKPKFRSPSDEGPGSMGDDGQLSPGVLVRCASGPPPNSPRPGPPPSTSSPHLTAHSEPSLWNPPSRELDKPPLLPPKKEKMKRKGCALLVKLFNGCPLRIHSTAAWTHPSTKDQHLLLGAEEGIFILNRNDQEATLEMLFPSRTTWVYSINNVLMSLSGKTPHLYSHSILGLLERKETRAGNPIAHISPHRLLARKNMVSTKIQDTKGCRACCVAEGASSGGPFLCGALETSVVLLQWYQPMNKFLLVRQVLFPLPTPLSVFALLTGPGSELPAVCIGVSPGRPGKSVLFHTVRFGALSCWLGEMSTEHRGPVQVTQVEEDMVMVLMDGSVKLVTPEGSPVRGLRTPEIPMTEAVEAVAMVGGQLQAFWKHGVQVWALGSDQLLQELRDPTLTFRLLGSPRLECSGTISPHCNLLLPGSSNSPASASRVAGITGL
  
Inhibitor
Name:
BDBM591233
Synonyms:
2-((8-amino-6-(5-amino-4,6- dimethylpyridin-3-yl)-7- fluoroisoquinolin-3-yl)amino)-6-methyl- 5,6-dihydro-4H-pyrazolo[1,5- d][1,4]diazepin-7(8H)-one | US11566003, Compound 299
Type:
Small organic molecule
Emp. Form.:
C24H25FN8O
Mol. Mass.:
460.5067
SMILES:
CN1CCc2cc(Nc3cc4cc(c(F)c(N)c4cn3)-c3cnc(C)c(N)c3C)nn2CC1=O
Structure:
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