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 34:

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]