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Target
Mitogen-activated protein kinase kinase kinase kinase 1
Ligand
BDBM459484
Substrate
n/a
Meas. Tech.
ChEMBL_2266080
Ki
2.2±n/a nM
Citation
 Sokolsky, A; Vechorkin, O; Hummel, JR; Styduhar, ED; Wang, A; Nguyen, MH; Ye, HF; Liu, K; Zhang, K; Pan, J; Ye, Q; Atasoylu, O; Behshad, E; He, X; Conlen, P; Stump, K; Ye, M; Diamond, S; Covington, M; Yeleswaram, S; Yao, W Potent and Selective Biaryl Amide Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1). ACS Med Chem Lett 14:116-122 (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:
BDBM459484
Synonyms:
US10752635, Example 35 | US11492354, Example 35
Type:
Small organic molecule
Emp. Form.:
C25H25F2N7O3
Mol. Mass.:
509.5079
SMILES:
COc1cccc(F)c1-c1nccc(n1)C(=O)Nc1cc(F)c2n(C)ncc2c1N1C[C@@H](O)C[C@H]1CN |r|
Structure:
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