RasGRP activator 1 [Ligand Id: 10066] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL519741
  • protein kinase C alpha/Protein kinase C alpha in Human [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
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  • protein kinase C epsilon/Protein kinase C epsilon in Human [ChEMBL: CHEMBL3582] [GtoPdb: 1486] [UniProtKB: Q02156]
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  • RAS guanyl releasing protein 1/RAS guanyl-releasing protein 1 in Human [ChEMBL: CHEMBL5953] [GtoPdb: 3016] [UniProtKB: O95267]
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  • RAS guanyl releasing protein 3 in Human [ChEMBL: CHEMBL3638] [UniProtKB: Q8IV61]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
protein kinase C alpha/Protein kinase C alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
ChEMBL Displacement of [3H]PDBu from full length recombinant human PKCalpha expressed in baculovirus expression system after 5 mins by scintillation counting B 7.5 pKi 31.7 nM Ki J Med Chem (2018) 61: 6261-6276 [PMID:29860841]
ChEMBL Displacement of [3H]PDBu from human recombinant PKCalpha expressed in Escherichia coli BL21-21-Gold (DE3) B 7.53 pKi 29.7 nM Ki J Med Chem (2008) 51: 5371-5386 [PMID:18707088]
GtoPdb - - 7.79 pKi 16.2 nM Ki Bioorg Med Chem (2014) 22: 3123-40 [PMID:24794745]
ChEMBL Displacement of [3H]PDBu from recombinant human PKC-alpha after 5 mins by scintillation counting analysis in presence of phosphatidylserine B 7.79 pKi 16.2 nM Ki Bioorg Med Chem (2014) 22: 3123-3140 [PMID:24794745]
ChEMBL Displacement of [20-3H]phorbol 12,13-dibutyrate from PKCalpha (unknown origin) in the presence of porcine brain phosphatidylserine by scintillation counting B 7.89 pKi 12.9 nM Ki Bioorg Med Chem (2017) 25: 2971-2980 [PMID:28392275]
protein kinase C epsilon/Protein kinase C epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3582] [GtoPdb: 1486] [UniProtKB: Q02156]
ChEMBL Displacement of [3H]PDBu from full length recombinant human PKCepsilon expressed in baculovirus expression system after 5 mins by scintillation counting B 7.37 pKi 42.8 nM Ki J Med Chem (2018) 61: 6261-6276 [PMID:29860841]
ChEMBL Displacement of [20-3H]phorbol 12,13-dibutyrate from PKCepsilon (unknown origin) in the presence of porcine brain phosphatidylserine by scintillation counting B 7.51 pKi 31 nM Ki Bioorg Med Chem (2017) 25: 2971-2980 [PMID:28392275]
ChEMBL Displacement of [3H]PDBu from recombinant human PKC-epsilon after 5 mins by scintillation counting analysis in presence of phosphatidylserine B 7.68 pKi 21.1 nM Ki Bioorg Med Chem (2014) 22: 3123-3140 [PMID:24794745]
GtoPdb - - 7.68 pKi 21.1 nM Ki Bioorg Med Chem (2014) 22: 3123-40 [PMID:24794745]
RAS guanyl releasing protein 1/RAS guanyl-releasing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5953] [GtoPdb: 3016] [UniProtKB: O95267]
ChEMBL Displacement of [20-3H]phorbol 12,13-dibutyrate from RasGRP1 (unknown origin) in the presence of porcine brain phosphatidylserine by scintillation counting B 9.24 pKi 0.58 nM Ki Bioorg Med Chem (2017) 25: 2971-2980 [PMID:28392275]
GtoPdb Displacement of [3H]PDBu from the DAG-responsive C1 domain of recombinant RasGRP1. - 9.6 pKi 0.25 nM Ki Bioorg Med Chem (2014) 22: 3123-40 [PMID:24794745]
ChEMBL Displacement of [3H]PDBu from recombinant RasGRP1 C1 domain (unknown origin) after 10 mins by scintillation counting analysis in presence of phosphatidylserine B 9.6 pKi 0.25 nM Ki Bioorg Med Chem (2014) 22: 3123-3140 [PMID:24794745]
RAS guanyl releasing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3638] [UniProtKB: Q8IV61]
ChEMBL Displacement of [3H]PDBu from full length MBP-tagged human RasGRP3 expressed in Escherichia coli BL21 (DE3) after 5 mins by scintillation counting B 9.08 pKi 0.84 nM Ki J Med Chem (2018) 61: 6261-6276 [PMID:29860841]
ChEMBL Displacement of [3H]PDBu from recombinant human GFP-tagged RasGRP3 expressed in Escherichia coli BL21 after 5 mins by scintillation counting analysis in presence of phosphatidylserine B 9.48 pKi 0.33 nM Ki Bioorg Med Chem (2014) 22: 3123-3140 [PMID:24794745]
ChEMBL Displacement of [3H]PDBu from RasGRP3 expressed in cells B 9.74 pKi 0.18 nM Ki J Med Chem (2008) 51: 5371-5386 [PMID:18707088]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]