General Information of the Protein
Protein ID
PT02115
Protein Name
Rhodopsin kinase GRK1
Secondarily
Protein Name
G protein-coupled receptor kinase 1
Gene Name
GRK1
Secondarily
Gene Name
RHOK
Sequence
MDFGSLETVVANSAFIAARGSFDGSSSQPSRDKKYLAKLKLPPLSKCESLRDSLSLEFESVCLEQPIGKKLFQQFLQSAEKHLPALELWKDIEDYDTADNDLQPQKAQTILAQYLDPQAKLFCSFLDEGIVAKFKEGPVEIQDGLFQPLLQATLAHLGQAPFQEYLGSLYFLRFLQWKWLEAQPMGEDWFLDFRVLGKGGFGEVSACQMKATGKLYACKKLNKKRLKKRKGYQGAMVEKKILMKVHSRFIVSLAYAFETKADLCLVMTIMNGGDIRYHIYNVNEENPGFPEPRALFYTAQIICGLEHLHQRRIVYRDLKPENVLLDNDGNVRISDLGLAVELLDGQSKTKGYAGTPGFMAPELLQGEEYDFSVDYFALGVTLYEMIAARGPFRARGEKVENKELKHRIISEPVKYPDKFSQASKDFCEALLEKDPEKRLGFRDETCDKLRAHPLFKDLNWRQLEAGMLMPPFIPDSKTVYAKDIQDVGAFSTVKGVAFDKTDTEFFQEFATGNCPIPWQEEMIETGIFGELNVWRSDGQMPDDMKGISGGSSSSSKSGMCLVS
    Show/Hide
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
Retina-specific kinase involved in the signal turnoff via phosphorylation of rhodopsin (RHO), the G protein- coupled receptor that initiates the phototransduction cascade (PubMed:15946941). This rapid desensitization is essential for scotopic vision and permits rapid adaptation to changes in illumination (By similarity). May play a role in the maintenance of the outer nuclear layer in the retina (By similarity).
    Show/Hide
Uniprot ID
Primary ID:
Q15835

Secondarily ID:
Q53X14
    Show/Hide
Ensembl ID
ENSG00000185974
HGNC ID
HGNC:10013
Subcellular Location
Membrane
Cell projection
Cilium
Photoreceptor outer segment
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: CL000013 , Sf9
Compound ID Compound Name Compound Formula
CP0138104
3-(9-oxa-3,4,6,12-tetrazatricyclo[8.4.0.02,6]tetradeca-1(10),2,4,11,13-pentaen-5-ylmethylamino)-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide
   Show/Hide
C25H21F3N6O2
 1
1
IC50 = 270 nM
   TI
   LI
   LO
   TS
CP0235953
3-[(4-methyl-5-pyridin-4-yl-1,2,4-triazol-3-yl)methylamino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide
   Show/Hide
C24H21F3N6O
 1
1
IC50 = 3100 nM
   TI
   LI
   LO
   TS
CP0051908
N-benzyl-3-[(4-ethyl-5-pyridin-4-yl-1,2,4-triazol-3-yl)methylamino]benzamide
   Show/Hide
C24H24N6O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0118539
N-benzyl-3-[(4-methyl-3-pyridin-4-yl-1H-pyrazol-5-yl)methylamino]benzamide
   Show/Hide
C24H23N5O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0249013
N-methyl-3-[(3-pyridin-4-yl-1H-1,2,4-triazol-5-yl)methylamino]benzamide
   Show/Hide
C16H16N6O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0269441
N-benzyl-3-[(3-pyridin-4-yl-1H-1,2,4-triazol-5-yl)methylamino]benzamide
   Show/Hide
C22H20N6O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0382649
3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl]-methylamino]ethoxy]ethoxy]ethoxy]ethyl]propanamide
   Show/Hide
C50H56BF2N7O7
 1
1
Kd = 109 nM
   TI
   LI
   LO
   TS
CP0382724
3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl]amino]ethoxy]ethoxy]ethoxy]ethyl]propanamide
   Show/Hide
C49H54BF2N7O7
 1
1
Kd = 122 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0235953
3-[(4-methyl-5-pyridin-4-yl-1,2,4-triazol-3-yl)methylamino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide
   Show/Hide
C24H21F3N6O
 1
1 IC50 = 3100 nM