General Information of the Protein
Protein ID
PT01699
Protein Name
G protein-coupled receptor kinase 6
Secondarily
Protein Name
G protein-coupled receptor kinase GRK6
Gene Name
GRK6
Secondarily
Gene Name
GPRK6
Sequence
MELENIVANTVLLKAREGGGGNRKGKSKKWRQMLQFPHISQCEELRLSLERDYHSLCERQPIGRLLFREFCATRPELSRCVAFLDGVAEYEVTPDDKRKACGRQLTQNFLSHTGPDLIPEVPRQLVTNCTQRLEQGPCKDLFQELTRLTHEYLSVAPFADYLDSIYFNRFLQWKWLERQPVTKNTFRQYRVLGKGGFGEVCACQVRATGKMYACKKLEKKRIKKRKGEAMALNEKQILEKVNSRFVVSLAYAYETKDALCLVLTLMNGGDLKFHIYHMGQAGFPEARAVFYAAEICCGLEDLHRERIVYRDLKPENILLDDHGHIRISDLGLAVHVPEGQTIKGRVGTVGYMAPEVVKNERYTFSPDWWALGCLLYEMIAGQSPFQQRKKKIKREEVERLVKEVPEEYSERFSPQARSLCSQLLCKDPAERLGCRGGSAREVKEHPLFKKLNFKRLGAGMLEPPFKPDPQAIYCKDVLDIEQFSTVKGVELEPTDQDFYQKFATGSVPIPWQNEMVETECFQELNVFGLDGSVPPDLDWKGQPPAPPKKGLLQRLFSRQDCCGNCSDSEEELPTRL
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
AGC protein kinase group
>
AGC protein kinase GRK family
>
AGC protein kinase GRK subfamily
Function
Specifically phosphorylates the activated forms of G protein-coupled receptors. Such receptor phosphorylation initiates beta-arrestin-mediated receptor desensitization, internalization, and signaling events leading to their desensitization. Seems to be involved in the desensitization of D2-like dopamine receptors in striatum and chemokine receptor CXCR4 which is critical for CXCL12-induced cell chemotaxis (By similarity). Phosphorylates rhodopsin (RHO) (in vitro) and a non G-protein-coupled receptor: LRP6 during Wnt signaling (in vitro).
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Uniprot ID
Primary ID:
P43250

Secondarily ID:
O60541
Q13652
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Ensembl ID
ENSG00000198055
HGNC ID
HGNC:4545
Subcellular Location
Membrane
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: CL000559 , KMS-11
Compound ID Compound Name Compound Formula
CP0131253
2-N-[(4-chloro-2-methoxyphenyl)methyl]-4-N-(5-ethyl-1H-pyrazol-3-yl)-5-methoxyquinazoline-2,4-diamine
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C22H23ClN6O2
 1
1
IC50 = 30 nM
   TI
   LI
   LO
   TS
CP0552988
2-N-[(4-chloro-2-methoxyphenyl)methyl]-4-N-(5-ethyl-1H-pyrazol-3-yl)-5-methylquinazoline-2,4-diamine
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C22H23ClN6O
 1
1
IC50 = 170 nM
   TI
   LI
   LO
   TS
CP0835612
(S)-N4-(3-Ethyl-1H-pyrazol-5-yl)-N2-(1-(5-fluoropyridin-2-yl)-ethyl)-5-methylquinazoline-2,4-diamine
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C21H22FN7
 1
1
IC50 = 610 nM
   TI
   LI
   LO
   TS
CP0267013
2-N-[(4-chlorophenyl)methyl]-4-N-(5-ethyl-1H-pyrazol-3-yl)-5-methoxyquinazoline-2,4-diamine
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C21H21ClN6O
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0773120
(S)-N4-(5-ethyl-1H-pyrazol-3-yl)-N2-(1-(5-fluoropyridin-2-yl)ethyl)-5-methoxyquinazoline-2,4-diamine
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C21H22FN7O
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0131252
4-N-(5-ethyl-1H-pyrazol-3-yl)-2-N-[(5-fluoropyridin-2-yl)methyl]-5-methoxyquinazoline-2,4-diamine
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C20H20FN7O
 1
1
IC50 = 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0131253
2-N-[(4-chloro-2-methoxyphenyl)methyl]-4-N-(5-ethyl-1H-pyrazol-3-yl)-5-methoxyquinazoline-2,4-diamine
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C22H23ClN6O2
 2
1 IC50 = 3.8 nM
2 IC50 = 8 nM
CP0552988
2-N-[(4-chloro-2-methoxyphenyl)methyl]-4-N-(5-ethyl-1H-pyrazol-3-yl)-5-methylquinazoline-2,4-diamine
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C22H23ClN6O
 1
1 IC50 = 6 nM
CP0773120
(S)-N4-(5-ethyl-1H-pyrazol-3-yl)-N2-(1-(5-fluoropyridin-2-yl)ethyl)-5-methoxyquinazoline-2,4-diamine
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C21H22FN7O
 2
1 IC50 = 7.2 nM
2 IC50 = 18 nM
CP0835612
(S)-N4-(3-Ethyl-1H-pyrazol-5-yl)-N2-(1-(5-fluoropyridin-2-yl)-ethyl)-5-methylquinazoline-2,4-diamine
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C21H22FN7
 1
1 IC50 = 11 nM
CP0267013
2-N-[(4-chlorophenyl)methyl]-4-N-(5-ethyl-1H-pyrazol-3-yl)-5-methoxyquinazoline-2,4-diamine
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C21H21ClN6O
 1
1 IC50 = 16 nM
CP0131252
4-N-(5-ethyl-1H-pyrazol-3-yl)-2-N-[(5-fluoropyridin-2-yl)methyl]-5-methoxyquinazoline-2,4-diamine
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C20H20FN7O
 2
1 IC50 = 18 nM
2 IC50 = 33 nM