GSK429286A [Ligand Id: 9356] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL375312
  • leucine rich repeat kinase 2/Leucine-rich repeat serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL1075104] [GtoPdb: 2059] [UniProtKB: Q5S007]
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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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  • Rho associated coiled-coil containing protein kinase 2/Rho-associated protein kinase 2 in Human [ChEMBL: CHEMBL2973] [GtoPdb: 1504] [UniProtKB: O75116]
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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
leucine rich repeat kinase 2/Leucine-rich repeat serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075104] [GtoPdb: 2059] [UniProtKB: Q5S007]
ChEMBL Inhibition of GST-tagged LRRK2 (1326 to 2527 residues) (unknown origin) using peptide as substrate incubated for 15 mins in presence of ATP by immunoblotting analysis B 4 pIC50 >100000 nM IC50 Biochem J (2009) 424: 47-60 [PMID:19740074]
ChEMBL Inhibition of GST-tagged LRRK2 G2019S mutant (1326 to 2527 residues) (unknown origin) using peptide as substrate incubated for 15 mins in presence of ATP by immunoblotting analysis B 4 pIC50 >100000 nM IC50 Biochem J (2009) 424: 47-60 [PMID:19740074]
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 Affinity Phenotypic Cellular interaction (Western Blot (phosphorylation of MYPT at Thr850 in HEK293 cells)) EUB0000134b ROCK1 B 5 pIC50 <10000 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
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 Affinity Biochemical interaction (Scintillation Proximity Assay (SPA)) EUB0000134b ROCK1 B 7.85 pIC50 14 nM IC50 Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
Rho associated coiled-coil containing protein kinase 2/Rho-associated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2973] [GtoPdb: 1504] [UniProtKB: O75116]
ChEMBL Affinity Phenotypic Cellular interaction (Western Blot (phosphorylation of MYPT at Thr850 in HEK293 cells)) EUB0000134b ROCK2 B 5 pIC50 <10000 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Affinity Biochemical interaction (Enzymatic inhibition assay (100 µM ATP)) EUB0000134b ROCK2 B 7.2 pIC50 63 nM IC50 Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of His6-tagged ROCK2 (2 to 543 residues) (unknown origin) using peptide as substrate incubated for 15 mins in presence of ATP by immunoblotting analysis B 7.2 pIC50 63 nM IC50 Biochem J (2009) 424: 47-60 [PMID:19740074]
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 6.11 pIC50 780 nM IC50 J Med Chem (2007) 50: 6-9 [PMID:17201405]
GtoPdb - - 6.11 pIC50 780 nM IC50 J Med Chem (2007) 50: 6-9 [PMID:17201405]
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 5.71 pIC50 1940 nM IC50 J Med Chem (2007) 50: 6-9 [PMID:17201405]

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]