Target
Mitogen-activated protein kinase kinase kinase kinase 1
Ligand
BDBM501152
Substrate
n/a
Meas. Tech.
Biochemical Enzyme Assay
IC50
<100±n/a nM
Citation
 Kaila, NLinney, IWard, SWishart, GWhittaker, BCote, AGreenwood, JRLeffler, AAlbanese, SKSeverance, DL Substituted isoindolin-1-ones and 2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-1-ones as HPK1 antagonists US Patent  US11034694 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:
BDBM501152
Synonyms:
4-(2- ((dimethylami no)methyl)-6- ((7-(7- fluoroimidazo [1,2-a]pyridin- 3-yl)-3- oxoisoindolin- 4-yl)amino)pyri- din-3-yl)tetrahydro- 2H-pyran-4- carbonitrilc | US11021481, Compound I-824 | US11078201, Compound I-824 | US11548890, Compound I-824
Type:
Small organic molecule
Emp. Form.:
C29H28FN7O2
Mol. Mass.:
525.5767
SMILES:
CN(C)Cc1nc(Nc2ccc(c3CNC(=O)c23)-c2cnc3cc(F)ccn23)ccc1C1(CCOCC1)C#N
Structure:
Search PDB for entries with ligand similarity: