General Information of the Protein
Protein ID
PT02377
Protein Name
Beta-adrenergic receptor kinase 1
Secondarily
Protein Name
G-protein coupled receptor kinase 2
Gene Name
GRK2
Secondarily
Gene Name
ADRBK1
BARK
BARK1
Sequence
MADLEAVLADVSYLMAMEKSKATPAARASKKILLPEPSIRSVMQKYLEDRGEVTFEKIFSQKLGYLLFRDFCLNHLEEARPLVEFYEEIKKYEKLETEEERVARSREIFDSYIMKELLACSHPFSKSATEHVQGHLGKKQVPPDLFQPYIEEICQNLRGDVFQKFIESDKFTRFCQWKNVELNIHLTMNDFSVHRIIGRGGFGEVYGCRKADTGKMYAMKCLDKKRIKMKQGETLALNERIMLSLVSTGDCPFIVCMSYAFHTPDKLSFILDLMNGGDLHYHLSQHGVFSEADMRFYAAEIILGLEHMHNRFVVYRDLKPANILLDEHGHVRISDLGLACDFSKKKPHASVGTHGYMAPEVLQKGVAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTMAVELPDSFSPELRSLLEGLLQRDVNRRLGCLGRGAQEVKESPFFRSLDWQMVFLQKYPPPLIPPRGEVNAADAFDIGSFDEEDTKGIKLLDSDQELYRNFPLTISERWQQEVAETVFDTINAETDRLEARKKAKNKQLGHEEDYALGKDCIMHGYMSKMGNPFLTQWQRRYFYLFPNRLEWRGEGEAPQSLLTMEEIQSVEETQIKERKCLLLKIRGGKQFILQCDSDPELVQWKKELRDAYREAQQLVQRVPKMKNKPRSPVVELSKVPLVQRGSANGL
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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 BARK subfamily
Function
Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors, probably inducing a desensitization of them (PubMed:19715378). Key regulator of LPAR1 signaling (PubMed:19306925). Competes with RALA for binding to LPAR1 thus affecting the signaling properties of the receptor (PubMed:19306925). Desensitizes LPAR1 and LPAR2 in a phosphorylation-independent manner (PubMed:19306925). Positively regulates ciliary smoothened (SMO)-dependent Hedgehog (Hh) signaling pathway by facilitating the trafficking of SMO into the cilium and the stimulation of SMO activity (By similarity). Inhibits relaxation of airway smooth muscle in response to blue light (PubMed:30284927).
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Uniprot ID
Primary ID:
P25098

Secondarily ID:
B0ZBE1
Q13837
Q6GTT3
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Ensembl ID
ENSG00000173020
HGNC ID
HGNC:289
Subcellular Location
Cytoplasm
Cell membrane
Postsynapse
Presynapse
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: CL000023 , BTI-Tn-5B1-4
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0113029
 Compound Info 
N-[(2,6-difluorophenyl)methyl]-3-[(4-propyl-5-pyrimidin-4-yl-1,2,4-triazol-3-yl)methylamino]benzamide
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C24H23F2N7O
  1
1
IC50 = 20 nM
 Bioactivity Info 
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CP0112012
 Compound Info 
4-[4-fluoro-3-[(2-methoxyphenyl)methylcarbamoyl]phenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C28H25FN6O4
  1
1
IC50 = 60 nM
 Bioactivity Info 
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CP0111456
 Compound Info 
4-[3-[(2,6-dimethylphenyl)methylcarbamoyl]-4-fluorophenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C29H27FN6O3
  1
1
IC50 = 70 nM
 Bioactivity Info 
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CP0061504
 Compound Info 
4-[3-[(2,6-dimethoxyphenyl)methylcarbamoyl]-4-fluorophenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C29H27FN6O5
  1
1
IC50 = 130 nM
 Bioactivity Info 
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CP0279940
 Compound Info 
4-[3-[(2,6-dichlorophenyl)methylcarbamoyl]-4-fluorophenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C27H21Cl2FN6O3
  1
1
IC50 = 130 nM
 Bioactivity Info 
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CP0054841
 Compound Info 
4-[4-fluoro-3-(pyridin-2-ylmethylcarbamoyl)phenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C26H22FN7O3
  1
1
IC50 = 150 nM
 Bioactivity Info 
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CP0061404
 Compound Info 
4-[4-fluoro-3-[(3-fluorophenyl)methylcarbamoyl]phenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C27H22F2N6O3
  1
1
IC50 = 200 nM
 Bioactivity Info 
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CP0279933
 Compound Info 
4-[3-[(2,6-difluorophenyl)methylcarbamoyl]-4-fluorophenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C27H21F3N6O3
  1
1
IC50 = 220 nM
 Bioactivity Info 
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CP0061490
 Compound Info 
4-[3-[2-(2,6-dimethylphenyl)ethylcarbamoyl]-4-fluorophenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C30H29FN6O3
  1
1
IC50 = 230 nM
 Bioactivity Info 
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CP0174820
 Compound Info 
4-[4-fluoro-3-(isoquinolin-1-ylmethylcarbamoyl)phenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C30H24FN7O3
  1
1
IC50 = 280 nM
 Bioactivity Info 
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CP0257052
 Compound Info 
4-[4-fluoro-3-(2-pyridin-2-ylethylcarbamoyl)phenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C27H24FN7O3
  1
1
IC50 = 280 nM
 Bioactivity Info 
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CP0214468
 Compound Info 
4-[4-fluoro-3-[(3-methoxyphenyl)methylcarbamoyl]phenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C28H25FN6O4
  1
1
IC50 = 420 nM
 Bioactivity Info 
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CP0061500
 Compound Info 
4-[3-[2-[(2,6-dimethoxyphenyl)methylamino]-2-oxoethyl]-4-fluorophenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C30H29FN6O5
  1
1
IC50 = 450 nM
 Bioactivity Info 
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CP0191979
 Compound Info 
4-[4-fluoro-3-[(4-methoxyphenyl)methylcarbamoyl]phenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C28H25FN6O4
  1
1
IC50 = 460 nM
 Bioactivity Info 
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CP0112011
 Compound Info 
4-[3-(benzylcarbamoyl)-4-fluorophenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C27H23FN6O3
  1
1
IC50 = 690 nM
 Bioactivity Info 
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CP0025658
 Compound Info 
GSK-180736A
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C19H16FN5O2
  1
1
IC50 = 770 nM
 Bioactivity Info 
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CP0075077
 Compound Info 
4-[3-[[2,6-bis(trifluoromethyl)phenyl]methylcarbamoyl]-4-fluorophenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C29H21F7N6O3
  1
1
IC50 = 1200 nM
 Bioactivity Info 
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CP0046806
 Compound Info 
(3S,4R)-3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)piperidine
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C19H20FNO3
  1
1
IC50 = 1380 nM
 Bioactivity Info 
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CP0090326
 Compound Info 
4-[4-fluoro-3-[(3-methylpyridin-2-yl)methylcarbamoyl]phenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C27H24FN7O3
  1
1
IC50 = 1900 nM
 Bioactivity Info 
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CP0182293
 Compound Info 
4-[3-[[3,5-bis(trifluoromethyl)phenyl]methylcarbamoyl]-4-fluorophenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C29H21F7N6O3
  1
1
IC50 = 2700 nM
 Bioactivity Info 
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CP0455945
 Compound Info 
4-[4-fluoro-3-(methylcarbamoyl)phenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C21H19FN6O3
  1
1
IC50 = 4300 nM
 Bioactivity Info 
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CP0054840
 Compound Info 
4-[3-[(2,6-dimethylphenyl)methylcarbamoyl]-4-fluorophenyl]-N-(1H-indazol-5-yl)-N,6-dimethyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C30H29FN6O3
  1
1
IC50 = 4600 nM
 Bioactivity Info 
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CP0174819
 Compound Info 
4-[4-fluoro-3-(2-pyridin-4-ylethylcarbamoyl)phenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C27H24FN7O3
  1
1
IC50 = 4800 nM
 Bioactivity Info 
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CP0279937
 Compound Info 
2-fluoro-5-[5-(1H-indazol-5-ylcarbamoyl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidin-4-yl]benzoic acid
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C20H16FN5O4
  1
1
IC50 = 20000 nM
 Bioactivity Info 
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CP0279934
 Compound Info 
4-[3-[2-[(2,6-dimethylphenyl)methylamino]-2-oxoethyl]-4-fluorophenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C30H29FN6O3
  1
1
IC50 = 25000 nM
 Bioactivity Info 
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CP0061497
 Compound Info 
4-[3-[2-[[2,6-bis(trifluoromethyl)phenyl]methylamino]-2-oxoethyl]-4-fluorophenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C30H23F7N6O3
  1
1
IC50 > 100000 nM
 Bioactivity Info 
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CP0113033
 Compound Info 
N-(1,3-benzodioxol-5-yl)-4-[4-fluoro-3-(pyridin-2-ylmethylcarbamoyl)phenyl]-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C26H22FN5O5
  1
1
IC50 > 100000 nM
 Bioactivity Info 
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Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0113029
 Compound Info 
N-[(2,6-difluorophenyl)methyl]-3-[(4-propyl-5-pyrimidin-4-yl-1,2,4-triazol-3-yl)methylamino]benzamide
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C24H23F2N7O
  2
1 IC50 = 20 nM
2 Kd = 1.99 nM
CP0235953
 Compound Info 
3-[(4-methyl-5-pyridin-4-yl-1,2,4-triazol-3-yl)methylamino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide
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C24H21F3N6O
  1
1 IC50 = 30 nM
CP0061504
 Compound Info 
4-[3-[(2,6-dimethoxyphenyl)methylcarbamoyl]-4-fluorophenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
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C29H27FN6O5
  1
1 IC50 = 130 nM
CP0025658
 Compound Info 
GSK-180736A
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C19H16FN5O2
  1
1 IC50 = 770 nM
CP0046806
 Compound Info 
(3S,4R)-3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)piperidine
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C19H20FNO3
  3
1 IC50 = 1100 nM
2 IC50 = 1380 nM
3 Kd = 2980 nM
CP0705316
 Compound Info 
3-{[1-Pyridin-4-yl-meth-(E)-ylidene-hydrazinocarbonylmethyl]-amino}-benzamide
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C15H15N5O2
  1
1 Ki = 10 nM
Clinical Information about the Protein
Target 1 ( Beta-adrenergic receptor kinase 1 (ADRBK1) )
Target Type Patented-recorded Target