Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T62548 | Target Info | |||
| Target Name | Beta-adrenergic receptor kinase 1 (ADRBK1) | ||||
| Synonyms |
GRK2; G-protein coupled receptor kinase 2; BetaARK1; Beta-ARK-1; Beta ARK1
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| Target Type | Patented-recorded Target | ||||
| Gene Name | GRK2 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 8 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Sangivamycin
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Investigative | Compound Info | ||
| Synonyms |
7-Deazaadenosine-7-carboxamide; UNII-L8YQ8Z3T9T; L8YQ8Z3T9T; Antibiotic B-14437; CHEMBL101892; NSC-65346; 4-Amino-7-beta-D-ribofuranosyl-7H-pyrrolo(2,3-d)pyrimidine-5-carboxamide; B-14437; 4-amino-7-beta-D-ribofuranosyl-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide; 7-Deaza-7-carbamoyladenosine; BRN 0626355; Sanzivamycin; Sangivamycin, hydrochloride; 7H-Pyrrolo[2,3-d]pyrimidine-5-carboxamide, 4-amino-7-.beta.-D-ribofuranosyl-; cid_5153; BIDD:GT0419; SCHEMBL195540; ZINC4217438; BDBM50049820; 7H-Pyrrolo(2,3-d)pyrimidine-5-carboxamide, 4-amino-7-beta-D-ribofuranosyl-; BA-90912; J-011802; Q27158840; 4-Amino-5-carboxamide-7-(D-ribofuranosyl)pyrrolo[2,3-d]pyrimidine; 4-amino-7-(beta-d-ribofuranosyl)-7h-pyrrolo[2,3-d]pyrimidine-5-carboxamide
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| Activity |
Ki = 67000 nM
|
[1] | |||
| Compound Name |
N-[(2-Methoxyphenyl)methyl]-3-[(3-pyridin-4-yl-1H-1,2,4-triazol-5-yl)methylamino]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4095659; BDBM50257445
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| Activity |
EC50 = 76000 nM
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[2] | |||
| Compound Name |
N-Benzyl-3-[(4-ethyl-5-pyridin-4-yl-1,2,4-triazol-3-yl)methylamino]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4083276; BDBM50257365
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| Activity |
EC50 = 87000 nM
|
[2] | |||
| Compound Name |
Acetic acid, methoxy-, 2-(1H-indol-2-ylcarbonyl)-1H-indol-5-yl ester
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL7600; BDBM6609; DTXSID60349381; Bis(1H-2-indolyl)methanone deriv. 67; [2-(1H-2-Indolylcarbonyl)-1H-5-indolyl]methoxyethanoate; 2-(1H-indol-2-ylcarbonyl)-1H-indol-5-yl 2-methoxyacetate; Methoxyacetic acid 2-(1H-indole-2-ylcarbonyl)-1H-indole-5-yl ester; Acetic acid, methoxy-, 2-(1H-indol-2-ylcarbonyl)-1H-indol-5-yl ester (9CI)
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| Activity |
IC50 ~ 100000 nM
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[3] | |||
| Compound Name |
[2-(1H-Indole-2-carbonyl)-1H-indol-5-yl] acetate
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Investigative | Compound Info | ||
| Synonyms |
Bis(1H-2-indolyl)methanone deriv. 50; CHEMBL7572; BDBM6592; [2-(1H-2-indolylcarbonyl)-1H-5-indolyl]ethanoate; 2-(1H-indol-2-ylcarbonyl)-1H-indol-5-yl acetate; Acetic acid 2-(1H-indole-2-ylcarbonyl)-1H-indole-5-yl ester
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| Activity |
IC50 ~ 100000 nM
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[3] | |||
| Compound Name |
Glycine, N,N-dimethyl-, 2-(1H-indol-2-ylcarbonyl)-1H-indol-5-yl ester
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL7432; BDBM6595; DTXSID00349380; Bis(1H-2-indolyl)methanone deriv. 53; [2-(1H-2-Indolylcarbonyl)-1H-5-indolyl]dimethylaminoethanoate; 2-(1H-indol-2-ylcarbonyl)-1H-indol-5-yl 2-(dimethylamino)acetate; (Dimethylamino)acetic acid 2-(1H-indole-2-ylcarbonyl)-1H-indole-5-yl ester; Glycine, N,N-dimethyl-, 2-(1H-indol-2-ylcarbonyl)-1H-indol-5-yl ester (9CI)
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| Activity |
IC50 ~ 100000 nM
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[3] | |||
| Compound Name |
N-[(2-Chlorophenyl)methyl]-3-[(3-pyridin-4-yl-1H-1,2,4-triazol-5-yl)methylamino]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4077447; BDBM50257426
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| Activity |
EC50 = 120000 nM
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[2] | |||
| Compound Name |
GRK2 Inhibitor
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Investigative | Compound Info | ||
| Synonyms |
betaARK1 Inhibitor; CHEMBL68409; Methyl 5-[2-(5-nitro-2-furyl)vinyl]-2-furoate; methyl 5-[(E)-2-(5-nitrofuran-2-yl)ethenyl]furan-2-carboxylate; 5-[2-(5-Nitro-furan-2-yl)-vinyl]-furan-2-carboxylic acid methyl ester; (E)-Methyl 5-(2-(5-nitrofuran-2-yl)vinyl)furan-2-carboxylate; 5-[2-(5-Nitro-2-furanyl)ethenyl]-2-furancarboxylic Acid Methyl Ester; beta-Adrenergic Receptor Kinase1 Inhibitor; 1-(5-methoxycarbonyl-2-furyl)-2-(5-nitro-2-furyl)ethylene; ZINC3871642; BDBM50113255; J3.594.294G; J-015426; 5-[2-(5-Nitro-2-furyl)vinyl]-2-furancarboxylic acid methyl ester
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| Activity |
IC50 = 126000 nM
|
[4] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 5 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
3-[(4-Methyl-5-pyridin-4-yl-1,2,4-triazol-3-yl)methylamino]-N-[[3-(trifluoromethyl)phenyl]methyl]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4091573; BDBM50257446
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| Activity |
EC50 = 220000 nM
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[2] | |||
| Compound Name |
2-[5-Amino-3-(3,4-dihydroxy-5-hydroxymethyl-tetrahydro-furan-2-yl)-3H-imidazol-4-yl]-acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL307533; BDBM50113256
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| Activity |
IC50 = 557000 nM
|
[4] | |||
| Compound Name |
3-(Tert-butyl)-2-propanoylindeno[3,2-C]pyrazol-4-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL69467; 3-tert-butyl-2-propanoyl-2H,4H-indeno[1,2-c]pyrazol-4-one; 3-tert-butyl-2-propanoylindeno[1,2-c]pyrazol-4-one; SCHEMBL5538784; CTK6C6665; KS-00003QD3; ZINC2582095; BDBM50113257; MFCD00129207; AKOS022170056; MS-9455; 3-tert-Butyl-2-propionyl-2H-indeno[1,2-c]pyrazol-4-one
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| Activity |
IC50 = 563000 nM
|
[4] | |||
| Compound Name |
3-[(4-Methyl-5-pyridin-4-yl-1,2,4-triazol-3-yl)methylamino]-N-[[4-(trifluoromethyl)phenyl]methyl]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4063774; BDBM50257427
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| Activity |
EC50 = 930000 nM
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[2] | |||
| Compound Name |
N-Benzyl-3-[(4-methyl-5-pyridin-4-yl-1,2,4-triazol-3-yl)methylamino]benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4086619; BDBM50257438
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| Activity |
EC50 = 1900000 nM
|
[2] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | The nucleoside analog sangivamycin induces apoptotic cell death in breast carcinoma MCF7/adriamycin-resistant cells via protein kinase Cdelta and JNK activation. J Biol Chem. 2007 May 18;282(20):15271-83. | ||||
| REF 2 | Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure. J Med Chem. 2017 Aug 24;60(16):6942-6990. | ||||
| REF 3 | Bis(1H-2-indolyl)methanones as a novel class of inhibitors of the platelet-derived growth factor receptor kinase. J Med Chem. 2002 Feb 28;45(5):1002-18. | ||||
| REF 4 | Rational design and evaluation of new lead compound structures for selective betaARK1 inhibitors. J Med Chem. 2002 May 23;45(11):2150-9. | ||||
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