compound 13c [PMID: 20684591] [Ligand Id: 9681] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1214998
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
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  • protein kinase C alpha/Protein kinase C alpha in Human [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
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  • protein kinase C delta/Protein kinase C delta in Human [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655]
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  • protein kinase D1/Protein kinase C mu in Human [ChEMBL: CHEMBL3863] [GtoPdb: 1489] [UniProtKB: Q15139]
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  • protein kinase D2/Serine/threonine-protein kinase D2 in Human [ChEMBL: CHEMBL4900] [GtoPdb: 2173] [UniProtKB: Q9BZL6]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
ChEMBL Inhibition of beta-1 adrenoceptor ( assessed as residual activity at 1 uM ) B 5.63 pIC50 2351 nM IC50 J Med Chem (2010) 53: 5400-5421 [PMID:20684591]
protein kinase C alpha/Protein kinase C alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
ChEMBL Inhibition of PKCalpha by TR-FRET assay B 6 pIC50 1000 nM IC50 J Med Chem (2010) 53: 5400-5421 [PMID:20684591]
protein kinase C delta/Protein kinase C delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655]
ChEMBL Inhibition of PKCdelta by TR-FRET assay B 6.06 pIC50 881 nM IC50 J Med Chem (2010) 53: 5400-5421 [PMID:20684591]
protein kinase D1/Protein kinase C mu in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3863] [GtoPdb: 1489] [UniProtKB: Q15139]
ChEMBL Inhibition of PKD1 assessed as HDAC5 neuclear export B 7.49 pIC50 32 nM IC50 J Med Chem (2010) 53: 5400-5421 [PMID:20684591]
ChEMBL Inhibition of PKD1 assessed as inhibition of HDAC5 neuclear export B 7.49 pIC50 32 nM IC50 J Med Chem (2010) 53: 5422-5438 [PMID:20684592]
GtoPdb Measuring inhibition of synthetic substrate phosphorylation in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay. - 9.22 pIC50 0.6 nM IC50 J Med Chem (2010) 53: 5400-21 [PMID:20684591]
ChEMBL Inhibition of PKD1 by TR-FRET assay B 9.22 pIC50 0.6 nM IC50 J Med Chem (2010) 53: 5400-5421 [PMID:20684591]
ChEMBL Inhibition of PKD1 by TR-FRET assay B 9.22 pIC50 0.6 nM IC50 J Med Chem (2010) 53: 5422-5438 [PMID:20684592]
protein kinase D2/Serine/threonine-protein kinase D2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4900] [GtoPdb: 2173] [UniProtKB: Q9BZL6]
ChEMBL Inhibition of PKD2 ( assessed as residual activity at 1 uM ) by TR-FRET assay B 8.7 pIC50 2 nM IC50 J Med Chem (2010) 53: 5400-5421 [PMID:20684591]

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]