Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T69612 | Target Info | |||
| Target Name | G protein-coupled receptor kinase 5 (GRK5) | ||||
| Synonyms |
GPRK5; G protein-coupled receptor kinase GRK5
Click to Show/Hide
|
||||
| Target Type | Patented-recorded Target | ||||
| Gene Name | GRK5 | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 32 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
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
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3808918; SCHEMBL17525392; BDBM50173328
Click to Show/Hide
|
||||
| Activity |
IC50 = 58000 nM
|
[1] | |||
| Compound Name |
(2S)-6-Amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2,6-diaminohexanoyl]amino]-3-hydroxybutanoyl]amino]propanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]hexanoyl]amino]-3-phenylpropanoyl]amino]-4-carboxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-5-oxopentanoyl]amino]-3-hydroxybutanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxybutanoyl]amino]-4-oxobutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-phenylpropanoyl]amino]-3-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]hexanoic acid
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3900757; BDBM50191312
Click to Show/Hide
|
||||
| Activity |
IC50 = 61300 nM
|
[2] | |||
| Compound Name |
4-[3-[(2,6-Dimethylphenyl)methylcarbamoyl]-4-fluorophenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3809913; SCHEMBL17525384; BDBM50173309
Click to Show/Hide
|
||||
| Activity |
IC50 = 63000 nM
|
[1] | |||
| Compound Name |
Chembl4227413
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
SCHEMBL17525408
Click to Show/Hide
|
||||
| Activity |
IC50 = 66000 nM
|
[3] | |||
| Compound Name |
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
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3809697; SCHEMBL17525400; BDBM50173329
Click to Show/Hide
|
||||
| Activity |
IC50 = 68000 nM
|
[1] | |||
| Compound Name |
Chembl4225012
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
SCHEMBL17525413; BDBM283994; US10023564, Example 20
Click to Show/Hide
|
||||
| Activity |
IC50 = 71000 nM
|
[3] | |||
| Compound Name |
Chembl4228524
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461325
Click to Show/Hide
|
||||
| Activity |
IC50 = 77000 nM
|
[3] | |||
| Compound Name |
4-(6-Benzylimidazo[1,2-b]pyridazin-3-yl)benzamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3730669; SCHEMBL16331504; BDBM447165; US10688093, Compound 828_0346_6001; 4-(6- benzylimidazo [1,2-b]pyridazin- 3-yl)benzamide
Click to Show/Hide
|
||||
| Activity |
IC50 = 80000 nM
|
[4] | |||
| Compound Name |
6-(1-Methylpyrazol-4-yl)-3-thiophen-2-ylimidazo[1,2-b]pyridazine
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3732078; SCHEMBL16331215; BDBM447093; US10688093, Compound 828_4147_7468; 6-(1- methylpyrazol-4- yl)-3-(2- thienyl)imidazo [1,2-b]pyridazine
Click to Show/Hide
|
||||
| Activity |
IC50 = 80000 nM
|
[4] | |||
| Compound Name |
Chembl4227754
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461326
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
Chembl4228575
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461313
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
4-[3-[(2,6-Dichlorophenyl)methylcarbamoyl]-4-fluorophenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3810271; SCHEMBL17525391; BDBM50173308
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Chembl4229149
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461312
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
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
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3809124; SCHEMBL17525398; BDBM50173324
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-Fluoro-5-[5-(1H-indazol-5-ylcarbamoyl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidin-4-yl]benzoic acid
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3810250; SCHEMBL17508772; BDBM50173316
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
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
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3810383; BDBM50173321
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
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
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3809604; SCHEMBL17525397; BDBM50173326
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Chembl4224950
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
SCHEMBL19252724; BDBM50461323
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
Chembl4229210
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
SCHEMBL17525420
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
Chembl4226551
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461324
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
4-(3-((2,6-Dimethoxybenzyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3809020; CCG-224406; SCHEMBL17525386; BDBM50173319; J3.605.551K
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4-[4-Fluoro-3-(methylcarbamoyl)phenyl]-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3810349; SCHEMBL17525385; BDBM50173317
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
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
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3809788; SCHEMBL17525415; BDBM50173318
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Chembl4226760
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
SCHEMBL17525418; BDBM283993; US10023564, Example 19; E19
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
Chembl4225310
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461317
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
4-(4-Fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
GSK180736A; GSK-180736A; CHEMBL384073; SCHEMBL2569804; HMS3303C07; HMS3305J10; BCP25022; EX-A2531; BDBM50173320; s8489; CCG-268228; CS-6388; NCGC00241970-01; BS-17604; HY-18990; AK00783572; AB01092186-01
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Chembl4228117
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461308
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
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
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3809584; BDBM50173322
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Chembl4224914
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461328
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
Chembl4228272
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461316
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
Chembl4226879
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
E21; SCHEMBL17525412; BDBM283995; US10023564, Example 21
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
Click to Show/Hide
|
Compound Info | |||
| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J Med Chem. 2016 Apr 28;59(8):3793-807. | ||||
| REF 2 | G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives. J Med Chem. 2016 Oct 27;59(20):9277-9294. | ||||
| REF 3 | Utilizing a structure-based docking approach to develop potent G protein-coupled receptor kinase (GRK) 2 and 5 inhibitors. Bioorg Med Chem Lett. 2018 May 15;28(9):1507-1515. | ||||
| REF 4 | EP patent application no. 2818471A1, Nitrogen bicyclic compounds as inhibitors for Scyl1 and Grk5 | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.