General Information of the Protein
Protein ID
PT02328
Protein Name
Mitogen-activated protein kinase kinase kinase kinase 3
Secondarily
Protein Name
Germinal center kinase-related protein kinase
MAPK/ERK kinase kinase kinase 3
Gene Name
MAP4K3
Secondarily
Gene Name
RAB8IPL1
Sequence
MNPGFDLSRRNPQEDFELIQRIGSGTYGDVYKARNVNTGELAAIKVIKLEPGEDFAVVQQEIIMMKDCKHPNIVAYFGSYLRRDKLWICMEFCGGGSLQDIYHVTGPLSELQIAYVSRETLQGLYYLHSKGKMHRDIKGANILLTDNGHVKLADFGVSAQITATIAKRKSFIGTPYWMAPEVAAVERKGGYNQLCDLWAVGITAIELAELQPPMFDLHPMRALFLMTKSNFQPPKLKDKMKWSNSFHHFVKMALTKNPKKRPTAEKLLQHPFVTQHLTRSLAIELLDKVNNPDHSTYHDFDDDDPEPLVAVPHRIHSTSRNVREEKTRSEITFGQVKFDPPLRKETEPHHELPDSDGFLDSSEEIYYTARSNLDLQLEYGQGHQGGYFLGANKSLLKSVEEELHQRGHVAHLEDDEGDDDESKHSTLKAKIPPPLPPKPKSIFIPQEMHSTEDENQGTIKRCPMSGSPAKPSQVPPRPPPPRLPPHKPVALGNGMSSFQLNGERDGSLCQQQNEHRGTNLSRKEKKDVPKPISNGLPPTPKVHMGACFSKVFNGCPLKIHCASSWINPDTRDQYLIFGAEEGIYTLNLNELHETSMEQLFPRRCTWLYVMNNCLLSISGKASQLYSHNLPGLFDYARQMQKLPVAIPAHKLPDRILPRKFSVSAKIPETKWCQKCCVVRNPYTGHKYLCGALQTSIVLLEWVEPMQKFMLIKHIDFPIPCPLRMFEMLVVPEQEYPLVCVGVSRGRDFNQVVRFETVNPNSTSSWFTESDTPQTNVTHVTQLERDTILVCLDCCIKIVNLQGRLKSSRKLSSELTFDFQIESIVCLQDSVLAFWKHGMQGRSFRSNEVTQEISDSTRIFRLLGSDRVVVLESRPTDNPTANSNLYILAGHENSY
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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
May play a role in the response to environmental stress. Appears to act upstream of the JUN N-terminal pathway.
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Uniprot ID
Primary ID:
Q8IVH8

Secondarily ID:
Q6IQ39
Q8IVH7
Q9UDM5
Q9Y6R5
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Ensembl ID
ENSG00000011566
HGNC ID
HGNC:6865
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: CL000025 , HEK-293T
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0257048
 Compound Info 
5-[2-(1-ethylpiperidin-4-yl)-1,3-thiazol-5-yl]-3-(pyridin-4-ylmethoxy)pyridin-2-amine
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C21H25N5OS
  1
1
IC50 = 78 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0362701
 Compound Info 
3-(cyclohexylmethoxy)-5-(2-piperidin-4-yl-1,3-thiazol-5-yl)pyridin-2-amine
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C20H28N4OS
  1
1
IC50 = 258 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0019771
 Compound Info 
5-(2-piperidin-4-yl-1,3-thiazol-5-yl)-3-(pyridin-4-ylmethoxy)pyridin-2-amine
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C19H21N5OS
  1
1
IC50 = 278 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0533066
 Compound Info 
2-(3-fluorophenyl)-5-(1-piperidin-4-ylpyrazol-4-yl)-1,7-naphthyridin-8-amine
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C22H21FN6
  1
1
IC50 = 490 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0023821
 Compound Info 
3-cyclohexyloxy-5-(2-piperidin-4-yl-1,3-thiazol-5-yl)pyridin-2-amine
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C19H26N4OS
  1
1
IC50 = 645 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0354029
 Compound Info 
3-[1-(2,6-dichloro-3-fluorophenyl)propoxy]-5-(1-piperidin-4-ylpyrazol-4-yl)pyridin-2-amine
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C22H24Cl2FN5O
  1
1
IC50 = 1000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0354034
 Compound Info 
2-(2,6-dichloro-3-fluorophenyl)-4-(1-piperidin-4-ylpyrazol-4-yl)furo[2,3-c]pyridin-7-amine
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C21H18Cl2FN5O
  1
1
IC50 = 1220 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0489013
 Compound Info 
2-(3-fluorophenyl)-4-(1-piperidin-4-ylpyrazol-4-yl)furo[2,3-c]pyridin-7-amine
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C21H20FN5O
  1
1
IC50 = 1400 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0031719
 Compound Info 
(R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine
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C21H22Cl2FN5O
  1
1
IC50 = 1700 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0019771
 Compound Info 
5-(2-piperidin-4-yl-1,3-thiazol-5-yl)-3-(pyridin-4-ylmethoxy)pyridin-2-amine
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C19H21N5OS
  1
1 IC50 = 3 nM
CP0354034
 Compound Info 
2-(2,6-dichloro-3-fluorophenyl)-4-(1-piperidin-4-ylpyrazol-4-yl)furo[2,3-c]pyridin-7-amine
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C21H18Cl2FN5O
  1
1 IC50 = 5 nM
CP0533066
 Compound Info 
2-(3-fluorophenyl)-5-(1-piperidin-4-ylpyrazol-4-yl)-1,7-naphthyridin-8-amine
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C22H21FN6
  1
1 IC50 = 12 nM
CP0257048
 Compound Info 
5-[2-(1-ethylpiperidin-4-yl)-1,3-thiazol-5-yl]-3-(pyridin-4-ylmethoxy)pyridin-2-amine
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C21H25N5OS
  1
1 IC50 = 17 nM
CP0489013
 Compound Info 
2-(3-fluorophenyl)-4-(1-piperidin-4-ylpyrazol-4-yl)furo[2,3-c]pyridin-7-amine
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C21H20FN5O
  1
1 IC50 = 18 nM
CP0023821
 Compound Info 
3-cyclohexyloxy-5-(2-piperidin-4-yl-1,3-thiazol-5-yl)pyridin-2-amine
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C19H26N4OS
  1
1 IC50 = 35 nM
CP0031719
 Compound Info 
(R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine
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C21H22Cl2FN5O
  2
1 IC50 = 49 nM
2 Kd = 75 nM
CP0362701
 Compound Info 
3-(cyclohexylmethoxy)-5-(2-piperidin-4-yl-1,3-thiazol-5-yl)pyridin-2-amine
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C20H28N4OS
  1
1 IC50 = 77 nM
Clinical Information about the Protein
Target 1 ( MEK kinase kinase 3 (MAP4K3) )
Target Type Literature-reported Target