GSK180736A [Ligand Id: 14282] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL384073
  • beta adrenergic receptor kinase 1/Beta-adrenergic receptor kinase 1 in Human [ChEMBL: CHEMBL4079] [GtoPdb: 1466] [UniProtKB: P25098]
  • Beta-adrenergic receptor kinase 1 in Bovine [ChEMBL: CHEMBL3711550] [UniProtKB: P21146]
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  • Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464]
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  • G protein-coupled receptor kinase 1/Rhodopsin kinase GRK1 in Human [ChEMBL: CHEMBL5607] [GtoPdb: 1465] [UniProtKB: Q15835]
  • Rhodopsin kinase GRK1 in Bovine [ChEMBL: CHEMBL3879860] [UniProtKB: P28327]
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  • ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha-1 in Human [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418]
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  • ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase beta-1 in Human [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443]
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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/Beta-adrenergic receptor kinase 1 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 Assays for Inhibition of GRKs: GRK1, 2 and 5 kinetic assays were conducted in a buffer containing 20 mM HEPES pH 7.0, 5 μM ATP, 2 mM MgCl2, and 0.025% DDM with 50 nM GRK and either 500 nM bROS or 500 nM soluble substrate tubulin in 5 min reactions. The low salt concentration and DDM were used to maximize GRK activity and disrupt small molecule aggregates from forming, respectively. Reactions were quenched with SDS loading buffer, separated via SDS-PAGE, dried and exposed with a phosphorimaging screen prior to quantification via Typhoon imager, as previously reported (see Thal et al., ACS Chemical Biology 7(11):1830-1839 (2012)). Data was analyzed and inhibition curves were fit via GraphPad Prism. B 6.11 pIC50 770 nM IC50 US-10023564-B2. G protein-coupled receptor kinase 2 inhibitors and methods for use of the same (2018)
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]
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]
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]
ChEMBL Assays for Inhibition of GRKs: GRK1, 2 and 5 kinetic assays were conducted in a buffer containing 20 mM HEPES pH 7.0, 5 μM ATP, 2 mM MgCl2, and 0.025% DDM with 50 nM GRK and either 500 nM bROS or 500 nM soluble substrate tubulin in 5 min reactions. The low salt concentration and DDM were used to maximize GRK activity and disrupt small molecule aggregates from forming, respectively. Reactions were quenched with SDS loading buffer, separated via SDS-PAGE, dried and exposed with a phosphorimaging screen prior to quantification via Typhoon imager, as previously reported (see Thal et al., ACS Chemical Biology 7(11):1830-1839 (2012)). Data was analyzed and inhibition curves were fit via GraphPad Prism. B 4 pIC50 100000 nM IC50 US-10023564-B2. G protein-coupled receptor kinase 2 inhibitors and methods for use of the same (2018)
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]
ChEMBL Assays for Inhibition of ROCK: Rho-associated coiled-coil kinase (ROCK) assays were performed with the ADP-Glo system using 0.1 μg ROCK1 and 1 μg S6K substrate, and 100 μM ATP for 60 min prior to addition of ADP-GLO Reagent, and allowed to incubate for an additional 40 min prior to the addition of the Kinase Detection Reagent and imaging on a PHERASTAR system. B 7.11 pIC50 78 nM IC50 US-10023564-B2. G protein-coupled receptor kinase 2 inhibitors and methods for use of the same (2018)
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 GRK1 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]
ChEMBL Assays for Inhibition of GRKs: GRK1, 2 and 5 kinetic assays were conducted in a buffer containing 20 mM HEPES pH 7.0, 5 μM ATP, 2 mM MgCl2, and 0.025% DDM with 50 nM GRK and either 500 nM bROS or 500 nM soluble substrate tubulin in 5 min reactions. The low salt concentration and DDM were used to maximize GRK activity and disrupt small molecule aggregates from forming, respectively. Reactions were quenched with SDS loading buffer, separated via SDS-PAGE, dried and exposed with a phosphorimaging screen prior to quantification via Typhoon imager, as previously reported (see Thal et al., ACS Chemical Biology 7(11):1830-1839 (2012)). Data was analyzed and inhibition curves were fit via GraphPad Prism. B 4 pIC50 >100000 nM IC50 US-10023564-B2. G protein-coupled receptor kinase 2 inhibitors and methods for use of the same (2018)
Rhodopsin kinase GRK1 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 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]
ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase beta-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]

ChEMBL data shown on this page come from version 36:

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]