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Target
Mitogen-activated protein kinase kinase kinase kinase 1
Ligand
BDBM414759
Substrate
n/a
Meas. Tech.
ChEMBL_2265884
Ki
5.0±n/a nM
Citation
 Ye, Q; Liu, K; Ye, HF; Pan, J; Sokolsky, A; Wang, A; Zhang, K; Hummel, JR; Kong, L; Behshad, E; He, X; Conlen, P; Stump, K; Ye, M; Diamond, S; Covington, M; Yeleswaram, S; Atasoylu, O; Vechorkin, O; Yao, W Discovery of Pyrazolopyridine Derivatives as HPK1 Inhibitors. ACS Med Chem Lett 14:5-10 (2023) [PubMed]
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:
BDBM414759
Synonyms:
US10435405, Example 176 | US10934288, Example 176
Type:
Small organic molecule
Emp. Form.:
C20H21FN6
Mol. Mass.:
364.4193
SMILES:
CCNCc1cc(C)c(c(F)c1)-c1cc2c(n[nH]c2cn1)-c1cnn(C)c1
Structure:
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