General Information of the Protein
Protein ID
PT01878
Protein Name
Mitogen-activated protein kinase kinase kinase kinase 1
Secondarily
Protein Name
Hematopoietic progenitor kinase
MAPK/ERK kinase kinase kinase 1
Gene Name
MAP4K1
Secondarily
Gene Name
HPK1
Sequence
MDVVDPDIFNRDPRDHYDLLQRLGGGTYGEVFKARDKVSGDLVALKMVKMEPDDDVSTLQKEILILKTCRHANIVAYHGSYLWLQKLWICMEFCGAGSLQDIYQVTGSLSELQISYVCREVLQGLAYLHSQKKIHRDIKGANILINDAGEVRLADFGISAQIGATLARRLSFIGTPYWMAPEVAAVALKGGYNELCDIWSLGITAIELAELQPPLFDVHPLRVLFLMTKSGYQPPRLKEKGKWSAAFHNFIKVTLTKSPKKRPSATKMLSHQLVSQPGLNRGLILDLLDKLKNPGKGPSIGDIEDEEPELPPAIPRRIRSTHRSSSLGIPDADCCRRHMEFRKLRGMETRPPANTARLQPPRDLRSSSPRKQLSESSDDDYDDVDIPTPAEDTPPPLPPKPKFRSPSDEGPGSMGDDGQLSPGVLVRCASGPPPNSPRPGPPPSTSSPHLTAHSEPSLWNPPSRELDKPPLLPPKKEKMKRKGCALLVKLFNGCPLRIHSTAAWTHPSTKDQHLLLGAEEGIFILNRNDQEATLEMLFPSRTTWVYSINNVLMSLSGKTPHLYSHSILGLLERKETRAGNPIAHISPHRLLARKNMVSTKIQDTKGCRACCVAEGASSGGPFLCGALETSVVLLQWYQPMNKFLLVRQVLFPLPTPLSVFALLTGPGSELPAVCIGVSPGRPGKSVLFHTVRFGALSCWLGEMSTEHRGPVQVTQVEEDMVMVLMDGSVKLVTPEGSPVRGLRTPEIPMTEAVEAVAMVGGQLQAFWKHGVQVWALGSDQLLQELRDPTLTFRLLGSPRLECSGTISPHCNLLLPGSSNSPASASRVAGITGL
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
STE protein kinase group
>
STE protein kinase STE20 family
>
STE protein kinase KHS subfamily
Function
Serine/threonine-protein kinase, which may play a role in the response to environmental stress (PubMed:24362026). Appears to act upstream of the JUN N-terminal pathway (PubMed:8824585). May play a role in hematopoietic lineage decisions and growth regulation (PubMed:8824585, PubMed:24362026). Able to autophosphorylate (PubMed:8824585). Together with CLNK, it enhances CD3-triggered activation of T-cells and subsequent IL2 production (By similarity).
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Uniprot ID
Q92918
Ensembl ID
ENSG00000104814
HGNC ID
HGNC:6863
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000081 , Jurkat E6.1
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0579637
 Compound Info 
CHEMBL5081453
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C25H29ClFN5O2
  1
1
IC50 = 1200 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0572711
 Compound Info 
6-amino-3-(4-chlorospiro[1,2-dihydropyrrolo[2,3-b]pyridine-3,1'-cyclopentane]-5-yl)-2-fluoro-N,N-dimethylbenzamide
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C20H22ClFN4O
  1
1
IC50 = 1500 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0546094
 Compound Info 
6-amino-3-[(1'S,3R)-4-chloro-1'-cyano-1'-methylspiro[1,2-dihydropyrrolo[2,3-b]pyridine-3,3'-cyclopentane]-5-yl]-2-fluoro-N,N-dimethylbenzamide
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C22H23ClFN5O
  1
1
IC50 = 1700 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0568791
 Compound Info 
CHEMBL5091391
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C24H27ClFN5O2
  1
1
IC50 = 1700 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0527829
 Compound Info 
6-amino-3-[(1'S,3R)-4-chloro-1'-hydroxy-1'-methylspiro[1,2-dihydropyrrolo[2,3-b]pyridine-3,3'-cyclopentane]-5-yl]-2-fluoro-N,N-dimethylbenzamide
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C21H24ClFN4O2
  1
1
IC50 = 2000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0527830
 Compound Info 
6-amino-3-(4-chloro-1'-hydroxy-1'-methylspiro[1,2-dihydropyrrolo[2,3-b]pyridine-3,4'-cyclohexane]-5-yl)-2-fluoro-N,N-dimethylbenzamide
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C22H26ClFN4O2
  1
1
IC50 = 3000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0568965
 Compound Info 
6-amino-3-[(3R,3'S)-4-chloro-3'-hydroxyspiro[1,2-dihydropyrrolo[2,3-b]pyridine-3,1'-cyclopentane]-5-yl]-2-fluoro-N,N-dimethylbenzamide
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C20H22ClFN4O2
  1
1
IC50 = 5000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0546095
 Compound Info 
(1'S,3R)-5-[4-amino-3-(dimethylcarbamoyl)-2-fluorophenyl]-4-chloro-N-methylspiro[1,2-dihydropyrrolo[2,3-b]pyridine-3,3'-cyclopentane]-1'-carboxamide
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C22H25ClFN5O2
  1
1
IC50 = 7400 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0572072
 Compound Info 
6-amino-3-(4-chloro-1'-cyano-1'-methylspiro[1,2-dihydropyrrolo[2,3-b]pyridine-3,4'-cyclohexane]-5-yl)-2-fluoro-N,N-dimethylbenzamide
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C23H25ClFN5O
  1
1
IC50 = 7900 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0568790
 Compound Info 
(1'S,3R)-5-[4-amino-3-(dimethylcarbamoyl)-2-fluorophenyl]-4-chlorospiro[1,2-dihydropyrrolo[2,3-b]pyridine-3,3'-cyclopentane]-1'-carboxamide
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C21H23ClFN5O2
  1
1
IC50 = 14000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0955724
 Compound Info 
(+/-)-(1R*,3S*)-6-Amino-3-(4'-chloro-3-(1H-1,2,4-triazol-5-yl)-1',2'-dihydrospiro[cyclopentane-1,3'-pyrrolo[2,3-b]pyridin]-5'-yl)-2-fluoro-N,N-dimethylbenzamide
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C22H23ClFN7O
  1
1
IC50 = 15000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0546097
 Compound Info 
(1'R,3S)-5-[4-amino-3-(dimethylcarbamoyl)-2-fluorophenyl]-4-chloro-1'-methylspiro[1,2-dihydropyrrolo[2,3-b]pyridine-3,3'-cyclopentane]-1'-carboxamide
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C22H25ClFN5O2
  1
1
IC50 > 25000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0543921
 Compound Info 
US11180482, Example I-2
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C23H27ClN5O2P
  1
1 IC50 < 5 nM
CP0569850
 Compound Info 
4-[3-[[2-amino-5-[2-(1-methylpiperidin-4-yl)-1,3-thiazol-5-yl]pyridin-3-yl]oxymethyl]phenyl]-2-methylbut-3-yn-2-ol
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C26H30N4O2S
  1
1 IC50 < 100 nM
CP0357579
 Compound Info 
6-(2-fluoro-6-methoxyphenyl)-1-[6-(8-methyl-3,8-diazabicyclo[3.2.1]octan-3-yl)pyridin-2-yl]pyrazolo[4,3-c]pyridine
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C25H25FN6O
  1
1 IC50 = 4000 nM
CP0562900
 Compound Info 
6-(2-fluoro-6-methoxyphenyl)-1-[6-[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl]pyridin-2-yl]pyrazolo[4,3-c]pyridine
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C24H23FN6O
  1
1 IC50 = 4300 nM
CP0578407
 Compound Info 
6-(2-fluoro-6-methoxyphenyl)-1-[6-(4-methylpiperazin-1-yl)pyridin-2-yl]pyrazolo[4,3-c]pyridine
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C23H23FN6O
  1
1 IC50 = 8000 nM
CP0534969
 Compound Info 
6-(2-fluoro-6-methoxyphenyl)-1-[6-(4-methylpiperazin-1-yl)pyridin-2-yl]indazole-5-carbonitrile
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C25H23FN6O
  1
1 IC50 > 10000 nM
CP0534970
 Compound Info 
(3S)-1-[6-[6-(2-fluoro-6-methoxyphenyl)pyrazolo[4,3-c]pyridin-1-yl]pyridin-2-yl]-N,N-dimethylpyrrolidin-3-amine
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C24H25FN6O
  1
1 IC50 > 10000 nM
CP0562899
 Compound Info 
6-(2-fluoro-6-methylphenyl)-1-[4-(4-methylpiperazin-1-yl)phenyl]indazole-5-carbonitrile
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C26H24FN5
  1
1 IC50 > 10000 nM
CP0568790
 Compound Info 
(1'S,3R)-5-[4-amino-3-(dimethylcarbamoyl)-2-fluorophenyl]-4-chlorospiro[1,2-dihydropyrrolo[2,3-b]pyridine-3,3'-cyclopentane]-1'-carboxamide
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C21H23ClFN5O2
  1
1 Ki = 1.8 nM
CP0572711
 Compound Info 
6-amino-3-(4-chlorospiro[1,2-dihydropyrrolo[2,3-b]pyridine-3,1'-cyclopentane]-5-yl)-2-fluoro-N,N-dimethylbenzamide
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C20H22ClFN4O
  1
1 Ki = 2.5 nM
CP0568791
 Compound Info 
CHEMBL5091391
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C24H27ClFN5O2
  1
1 Ki = 6.5 nM
CP0579637
 Compound Info 
CHEMBL5081453
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C25H29ClFN5O2
  1
1 Ki = 7.2 nM
CP0527829
 Compound Info 
6-amino-3-[(1'S,3R)-4-chloro-1'-hydroxy-1'-methylspiro[1,2-dihydropyrrolo[2,3-b]pyridine-3,3'-cyclopentane]-5-yl]-2-fluoro-N,N-dimethylbenzamide
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C21H24ClFN4O2
  1
1 Ki = 8.1 nM
CP0527830
 Compound Info 
CHEMBL5084042
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C22H26ClFN4O2
  1
1 Ki = 8.2 nM
CP0568965
 Compound Info 
6-amino-3-[(3R,3'S)-4-chloro-3'-hydroxyspiro[1,2-dihydropyrrolo[2,3-b]pyridine-3,1'-cyclopentane]-5-yl]-2-fluoro-N,N-dimethylbenzamide
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C20H22ClFN4O2
  1
1 Ki = 8.4 nM
CP0572072
 Compound Info 
CHEMBL5076389
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C23H25ClFN5O
  1
1 Ki = 8.4 nM
CP0546094
 Compound Info 
6-amino-3-[(1'S,3R)-4-chloro-1'-cyano-1'-methylspiro[1,2-dihydropyrrolo[2,3-b]pyridine-3,3'-cyclopentane]-5-yl]-2-fluoro-N,N-dimethylbenzamide
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C22H23ClFN5O
  1
1 Ki = 11 nM
CP0955724
 Compound Info 
(+/-)-(1R*,3S*)-6-Amino-3-(4'-chloro-3-(1H-1,2,4-triazol-5-yl)-1',2'-dihydrospiro[cyclopentane-1,3'-pyrrolo[2,3-b]pyridin]-5'-yl)-2-fluoro-N,N-dimethylbenzamide
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C22H23ClFN7O
  1
1 Ki = 14 nM
CP0546095
 Compound Info 
(1'S,3R)-5-[4-amino-3-(dimethylcarbamoyl)-2-fluorophenyl]-4-chloro-N-methylspiro[1,2-dihydropyrrolo[2,3-b]pyridine-3,3'-cyclopentane]-1'-carboxamide
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C22H25ClFN5O2
  1
1 Ki = 63 nM
CP0546097
 Compound Info 
(1'R,3S)-5-[4-amino-3-(dimethylcarbamoyl)-2-fluorophenyl]-4-chloro-1'-methylspiro[1,2-dihydropyrrolo[2,3-b]pyridine-3,3'-cyclopentane]-1'-carboxamide
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C22H25ClFN5O2
  1
1 Ki = 85 nM
Clinical Information about the Protein
Target 1 ( MEK kinase kinase 1 (MAP4K1) )
Target Type Clinical trial Target