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Literature summary for 2.7.11.15 extracted from

  • Xu, G.; Gaul, M.D.; Liu, Z.; DesJarlais, R.L.; Qi, J.; Wang, W.; Krosky, D.; Petrounia, I.; Milligan, C.M.; Hermans, A.; Lu, H.R.; Huang, D.Z.; Xu, J.Z.; Spurlino, J.C.
    Hit-to-lead optimization and discovery of a potent, and orally bioavailable G protein coupled receptor kinase 2 (GRK2) inhibitor (2020), Bioorg. Med. Chem. Lett., 30, 127602 .
    View publication on PubMed
Search for more literature for 2.7.11.15

Inhibitors

Inhibitors Comment Organism Structure
2-(3-methoxybenzyl)-7-(1H-pyrazol-4-yl)phthalazin-1(2H)-one
-
 Homo sapiens
3-(3-fluoro-4-methoxybenzyl)-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
 Homo sapiens
3-(3-methoxybenzyl)-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
 Homo sapiens
3-(4-fluoro-3-methoxybenzyl)-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
 Homo sapiens
3-benzyl-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
 Homo sapiens
3-benzyl-6-(1H-pyrazol-5-yl)quinazolin-4(3H)-one
-
 Homo sapiens
3-benzyl-6-(pyridin-4-yl)quinazolin-4(3H)-one
-
 Homo sapiens
3-benzyl-6-(pyrimidin-5-yl)quinazolin-4(3H)-one
-
 Homo sapiens
3-benzyl-7-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
 Homo sapiens
3-benzyl-7-fluoro-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
 Homo sapiens
3-benzyl-8-fluoro-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
 Homo sapiens
3-[(1R)-1-(3-methoxyphenyl)ethyl]-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
 Homo sapiens
3-[(1S)-1-(3-methoxyphenyl)ethyl]-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
 Homo sapiens
3-[1-(3-methoxyphenyl)-3-(methylamino)propyl]-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
 Homo sapiens
3-[3-(4-fluorophenoxy)benzyl]-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
 Homo sapiens
3-[3-(difluoromethoxy)benzyl]-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
 Homo sapiens
balanol
-
 Homo sapiens
CCG-224406
-
 Homo sapiens
GSK180736A
-
 Homo sapiens
N-(4-fluorophenyl)-3-[[4-oxo-6-(1H-pyrazol-4-yl)quinazolin-3(4H)-yl]methyl]benzamide
-
 Homo sapiens
N-[(2,6-difluorocyclohexa-1,5-dien-1-yl)methyl]-4-[[4-oxo-6-(1H-pyrazol-4-yl)quinazolin-3(4H)-yl]methyl]benzamide
-
 Homo sapiens
N-[(2,6-difluorophenyl)methyl]-3-[[4-oxo-6-(1H-pyrazol-4-yl)quinazolin-3(4H)-yl]methyl]benzamide
-
 Homo sapiens
N-[(4-fluorophenyl)methyl]-3-[[4-oxo-6-(1H-pyrazol-4-yl)quinazolin-3(4H)-yl]methyl]benzamide
-
 Homo sapiens
paroxetine modest inhibitory activity Homo sapiens
Takeda 103A
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + [beta-adrenergic receptor] Homo sapiens
-
 ADP + phospho-[beta-adrenergic receptor]
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P25098
-
-

Source Tissue

Source Tissue Comment Organism Textmining
cardiac muscle fiber
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + [beta-adrenergic receptor]
-
 Homo sapiens ADP + phospho-[beta-adrenergic receptor]
-
 ?

Synonyms

Synonyms Comment Organism
G protein coupled receptor kinase
-
 Homo sapiens
G-protein receptor kinase 2
-
 Homo sapiens
GRK2
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000006
-
 pH and temperature not specified in the publication Homo sapiens 3-(3-methoxybenzyl)-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
0.000009
-
 pH and temperature not specified in the publication Homo sapiens N-(4-fluorophenyl)-3-[[4-oxo-6-(1H-pyrazol-4-yl)quinazolin-3(4H)-yl]methyl]benzamide
0.00001
-
 IC50 below 0.00001 mM, pH and temperature not specified in the publication Homo sapiens N-[(2,6-difluorophenyl)methyl]-3-[[4-oxo-6-(1H-pyrazol-4-yl)quinazolin-3(4H)-yl]methyl]benzamide
0.00001
-
 IC50 below 0.00001 mM, pH and temperature not specified in the publication Homo sapiens N-[(4-fluorophenyl)methyl]-3-[[4-oxo-6-(1H-pyrazol-4-yl)quinazolin-3(4H)-yl]methyl]benzamide
0.000012
-
 pH and temperature not specified in the publication Homo sapiens 3-[1-(3-methoxyphenyl)-3-(methylamino)propyl]-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
0.000013
-
 pH and temperature not specified in the publication Homo sapiens 3-[(1R)-1-(3-methoxyphenyl)ethyl]-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
0.000018
-
 pH and temperature not specified in the publication Homo sapiens 3-(4-fluoro-3-methoxybenzyl)-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
0.000019
-
 pH and temperature not specified in the publication Homo sapiens 2-(3-methoxybenzyl)-7-(1H-pyrazol-4-yl)phthalazin-1(2H)-one
0.000078
-
 pH and temperature not specified in the publication Homo sapiens 3-[3-(4-fluorophenoxy)benzyl]-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
0.000095
-
 pH and temperature not specified in the publication Homo sapiens 3-benzyl-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
0.000206
-
 pH and temperature not specified in the publication Homo sapiens 3-[3-(difluoromethoxy)benzyl]-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
0.000278
-
 pH and temperature not specified in the publication Homo sapiens 3-benzyl-7-fluoro-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
0.000472
-
 pH and temperature not specified in the publication Homo sapiens 3-benzyl-8-fluoro-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
0.00211
-
 pH and temperature not specified in the publication Homo sapiens 3-[(1S)-1-(3-methoxyphenyl)ethyl]-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
0.00275
-
 pH and temperature not specified in the publication Homo sapiens 3-(3-fluoro-4-methoxybenzyl)-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
0.0041
-
 pH and temperature not specified in the publication Homo sapiens 3-benzyl-7-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
0.02
-
 pH and temperature not specified in the publication Homo sapiens N-[(2,6-difluorocyclohexa-1,5-dien-1-yl)methyl]-4-[[4-oxo-6-(1H-pyrazol-4-yl)quinazolin-3(4H)-yl]methyl]benzamide
0.025
-
 pH and temperature not specified in the publication Homo sapiens 3-benzyl-6-(pyridin-4-yl)quinazolin-4(3H)-one
0.1
-
 IC50 above 0.1 mM, pH and temperature not specified in the publication Homo sapiens 3-benzyl-6-(1H-pyrazol-5-yl)quinazolin-4(3H)-one
0.1
-
 IC50 above 0.1 mM, pH and temperature not specified in the publication Homo sapiens 3-benzyl-6-(pyrimidin-5-yl)quinazolin-4(3H)-one