ChEMBL ligand: CHEMBL519741
protein kinase C alpha/Protein kinase C alpha in Human [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252] There should be some charts here, you may need to enable JavaScript!
protein kinase C epsilon/Protein kinase C epsilon in Human [ChEMBL: CHEMBL3582] [GtoPdb: 1486] [UniProtKB: Q02156] There should be some charts here, you may need to enable JavaScript!
RAS guanyl releasing protein 1/RAS guanyl-releasing protein 1 in Human [ChEMBL: CHEMBL5953] [GtoPdb: 3016] [UniProtKB: O95267] There should be some charts here, you may need to enable JavaScript!
RAS guanyl releasing protein 3 in Human [ChEMBL: CHEMBL3638] [UniProtKB: Q8IV61] There should be some charts here, you may need to enable JavaScript!

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 32:

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]