GSK180736A [Ligand Id: 14282] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL384073 (GSK180736A) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Beta-adrenergic receptor kinase 1 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3711550] [UniProtKB: P21146] | ||||||||
| ChEMBL | Inhibition of bovine GRK2 S670A mutant after 5 mins in presence of ATP by phosphorimaging assay | B | 6.11 | pIC50 | 770 | nM | IC50 | J Med Chem (2017) 60: 3052-3069 [PMID:28323425] |
| ChEMBL | Inhibition of bovine GRK2 S670A mutant assessed as decrease in phosphorylation of tubulin after 5 mins by SDS-PAGE analysis | B | 6.6 | pIC50 | 250 | nM | IC50 | J Med Chem (2016) 59: 9277-9294 [PMID:27362616] |
| beta adrenergic receptor kinase 1/G-protein coupled receptor kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4079] [GtoPdb: 1466] [UniProtKB: P25098] | ||||||||
| GtoPdb | - | - | 6.11 | pIC50 | 770 | nM | IC50 | J Med Chem (2021) 64: 1283-1345 [PMID:33481605] |
| ChEMBL | Inhibition of full length C-terminal hexahistidine tagged GRK2 (unknown origin) S670A mutant expressed in High Five cells using Bac to Bac insect cell expression system using tubulin as substrate by SDS-PAGE method | B | 6.11 | pIC50 | 770 | nM | IC50 | J Med Chem (2016) 59: 3793-3807 [PMID:27050625] |
| ChEMBL | Inhibition of GRK2 (unknown origin) | B | 6.11 | pIC50 | 770 | nM | IC50 | J Med Chem (2017) 60: 3052-3069 [PMID:28323425] |
| ChEMBL | Inhibition of GRK2 (unknown origin) | B | 6.11 | pIC50 | 770 | nM | IC50 | J Med Chem (2021) 64: 1283-1345 [PMID:33481605] |
| ChEMBL | Inhibition of GRK2 (unknown origin) | B | 6.11 | pIC50 | 770 | nM | IC50 | Eur J Med Chem (2022) 243: 114668-114668 [PMID:36055000] |
| ChEMBL | Inhibition of GRK2 (unknown origin) using CRRREEEEESAAA as substrate measured for 120 mins in presence of ATP by ADP-glo assay | B | 6.41 | pIC50 | 390 | nM | IC50 | Eur J Med Chem (2022) 243: 114668-114668 [PMID:36055000] |
| G protein-coupled receptor kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5678] [GtoPdb: 1469] [UniProtKB: P34947] | ||||||||
| ChEMBL | Inhibition of GRK5 (unknown origin) using tubulin as substrate by SDS-PAGE method | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2016) 59: 3793-3807 [PMID:27050625] |
| G protein-coupled receptor kinase 5 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879830] [UniProtKB: P43249] | ||||||||
| ChEMBL | Inhibition of bovine GRK5 assessed as decrease in phosphorylation of tubulin after 5 mins by SDS-PAGE analysis | B | 4 | pIC50 | 100000 | nM | IC50 | J Med Chem (2016) 59: 9277-9294 [PMID:27362616] |
| ChEMBL | Inhibition of bovine GRK5 after 5 mins after 5 mins in presence of ATP by phosphorimaging assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2017) 60: 3052-3069 [PMID:28323425] |
| Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464] | ||||||||
| ChEMBL | Inhibition of ROCK1 (unknown origin) by ADP-Glo kinase assay | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2016) 59: 3793-3807 [PMID:27050625] |
| GtoPdb | - | - | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2007) 50: 6-9 [PMID:17201405] |
| ChEMBL | Inhibition of human recombinant ROCK1 expressed in Sf9 cells at 10 mM | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2007) 50: 6-9 [PMID:17201405] |
| ChEMBL | Inhibition of human recombinant ROCK1 kinase expressed in insect Sf9 cells by SPA | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2008) 51: 6631-6634 [PMID:18842034] |
| G protein-coupled receptor kinase 1/Rhodopsin kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5607] [GtoPdb: 1465] [UniProtKB: Q15835] | ||||||||
| ChEMBL | Inhibition of GRK1 (unknown origin) using tubulin as substrate by SDS-PAGE method | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2016) 59: 3793-3807 [PMID:27050625] |
| Rhodopsin kinase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879860] [UniProtKB: P28327] | ||||||||
| ChEMBL | Inhibition of bovine GRK1 (1 to 535 residues) after 5 mins after 5 mins in presence of ATP by phosphorimaging assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2017) 60: 3052-3069 [PMID:28323425] |
| ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443] | ||||||||
| ChEMBL | Inhibition of p70S6K | B | 5.55 | pIC50 | 2850 | nM | IC50 | J Med Chem (2007) 50: 6-9 [PMID:17201405] |
| ChEMBL | Inhibition of p70S6K | B | 5.55 | pIC50 | 2850 | nM | IC50 | J Med Chem (2008) 51: 6631-6634 [PMID:18842034] |
| ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418] | ||||||||
| ChEMBL | Inhibition of RSK1 | B | 5.51 | pIC50 | 3100 | nM | IC50 | J Med Chem (2007) 50: 6-9 [PMID:17201405] |
| ChEMBL | Inhibition of RSK1 | B | 5.51 | pIC50 | 3100 | nM | IC50 | J Med Chem (2008) 51: 6631-6634 [PMID:18842034] |
ChEMBL data shown on this page come from version 35:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
