balanol [Ligand Id: 8142] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL60254 (Balanol) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Beta-adrenergic receptor kinase 1 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3711550] [UniProtKB: P21146] | ||||||||
| ChEMBL | Inhibition of bovine GRK2 S670A mutant expressed in Baculovirus expression system assessed as decrease in phosphorylation of urea-washed bovine rod outer segments preincubated for 30 mins followed by ATP addition and light exposure measured after 5 to 10 mins by SDS-PAGE analysis | B | 7.46 | pIC50 | 35 | nM | IC50 | J Med Chem (2016) 59: 9277-9294 [PMID:27362616] |
| beta adrenergic receptor kinase 2/Beta-adrenergic receptor kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075166] [GtoPdb: 1467] [UniProtKB: P35626] | ||||||||
| ChEMBL | Inhibition of GRK3-mediated bovine tubulin phosphorylation by scintillation counting | B | 7.33 | pIC50 | 47 | nM | IC50 | J Med Chem (2010) 53: 1867-1870 [PMID:20128603] |
| GtoPdb | - | - | 7.33 | pIC50 | 47 | nM | IC50 | J Med Chem (2010) 53: 1867-70 [PMID:20128603] |
| protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase alpha-catalytic subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612] | ||||||||
| ChEMBL | Binding affinity to PKAalpha (unknown origin) using Lys-Arg-Thr-Leu-Arg-Arg as substrate after 8 mins in presence of [gamma-32P]ATP by liquid scintillation spectrometry | B | 8.41 | pKd | 3.9 | nM | Kd | J Med Chem (2016) 59: 9277-9294 [PMID:27362616] |
| ChEMBL | Inhibitory concentration against recombinant human cAMP-dependent Protein kinase A | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (1997) 40: 226-235 [PMID:9003521] |
| Protein kinase G (PKG) 1/cGMP-dependent protein kinase 1 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4273] [GtoPdb: 1492] [UniProtKB: Q13976] | ||||||||
| ChEMBL | Binding affinity to human recombinant N-terminal GST-tagged PKGalpha expressed in Baculovirus infected insect Sf9 cells using RKRSRAE as substrate in presence of [gamma-32P]ATP | B | 8.8 | pKd | 1.6 | nM | Kd | J Med Chem (2016) 59: 9277-9294 [PMID:27362616] |
| beta adrenergic receptor kinase 1/G-protein coupled receptor kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4079] [GtoPdb: 1466] [UniProtKB: P25098] | ||||||||
| ChEMBL | Inhibition of GRK2-mediated bovine tubulin phosphorylation by scintillation counting | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (2010) 53: 1867-1870 [PMID:20128603] |
| GtoPdb | Inhibition of tubulin phosphorylation by balanol. | - | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (2010) 53: 1867-70 [PMID:20128603] |
| G protein-coupled receptor kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5861] [GtoPdb: 1468] [UniProtKB: P32298] | ||||||||
| ChEMBL | Inhibition of GRK4-mediated bovine tubulin phosphorylation by scintillation counting | B | 6.59 | pIC50 | 260 | nM | IC50 | J Med Chem (2010) 53: 1867-1870 [PMID:20128603] |
| GtoPdb | Measuring inhibition of human GRK-4-mediated phosphorylation of bovine tubulin dimers. | - | 6.59 | pIC50 | 260 | nM | IC50 | J Med Chem (2010) 53: 1867-70 [PMID:20128603] |
| G protein-coupled receptor kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5678] [GtoPdb: 1469] [UniProtKB: P34947] | ||||||||
| ChEMBL | Inhibition of GRK5-mediated bovine tubulin phosphorylation by scintillation counting | B | 6.8 | pIC50 | 160 | nM | IC50 | J Med Chem (2010) 53: 1867-1870 [PMID:20128603] |
| G protein-coupled receptor kinase 5 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879830] [UniProtKB: P43249] | ||||||||
| ChEMBL | Inhibition of bovine C-terminal truncated GRK5 (561 residues) assessed as decrease in phosphorylation of urea-washed bovine rod outer segments preincubated for 30 mins followed by ATP addition and light exposure measured after 5 to 10 mins by SDS-PAGE analysis | B | 6.36 | pIC50 | 440 | nM | IC50 | J Med Chem (2016) 59: 9277-9294 [PMID:27362616] |
| G protein-coupled receptor kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6144] [GtoPdb: 1470] [UniProtKB: P43250] | ||||||||
| ChEMBL | Inhibition of GRK6-mediated bovine tubulin phosphorylation by scintillation counting | B | 6.31 | pIC50 | 490 | nM | IC50 | J Med Chem (2010) 53: 1867-1870 [PMID:20128603] |
| GtoPdb | - | - | 6.31 | pIC50 | 490 | nM | IC50 | J Med Chem (2010) 53: 1867-70 [PMID:20128603] |
| G protein-coupled receptor kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075133] [GtoPdb: 1471] [UniProtKB: Q8WTQ7] | ||||||||
| GtoPdb | - | - | 6.74 | pIC50 | 180 | nM | IC50 | J Med Chem (2010) 53: 1867-70 [PMID:20128603] |
| ChEMBL | Inhibition of GRK7-mediated bovine tubulin phosphorylation by scintillation counting | B | 6.74 | pIC50 | 180 | nM | IC50 | J Med Chem (2010) 53: 1867-1870 [PMID:20128603] |
| protein kinase C alpha/Protein kinase C alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252] | ||||||||
| ChEMBL | Binding affinity to PKCalpha (unknown origin) using Lys-Arg-Thr-Leu-Arg-Arg as substrate after 8 mins in presence of [gamma-32P]ATP by liquid scintillation spectrometry | B | 8.19 | pKd | 6.4 | nM | Kd | J Med Chem (2016) 59: 9277-9294 [PMID:27362616] |
| ChEMBL | Inhibition of Protein kinase C alpha expressed in Sf-9 cells | B | 7.13 | pIC50 | 74 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2133-2138 |
| ChEMBL | Inhibition of human Protein kinase C alpha | B | 7.13 | pIC50 | 74 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2151-2154 |
| ChEMBL | Inhibition of human Protein kinase C alpha | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2155-2160 |
| ChEMBL | Inhibition of Protein kinase C alpha | B | 7.17 | pIC50 | 67 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2015-2020 |
| GtoPdb | - | - | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1996) 39: 5215-27 [PMID:8978850] |
| ChEMBL | Inhibitory concentration against recombinant human Protein kinase C alpha isozyme | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1997) 40: 226-235 [PMID:9003521] |
| ChEMBL | Evaluated against recombinant human Protein kinase C alpha | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1996) 39: 5215-5227 [PMID:8978850] |
| ChEMBL | Inhibition of Protein kinase C alpha | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2015-2020 |
| protein kinase C beta/Protein kinase C beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771] | ||||||||
| ChEMBL | Binding affinity to PKCbeta2 (unknown origin) using Lys-Arg-Thr-Leu-Arg-Arg as substrate after 8 mins in presence of [gamma-32P]ATP by liquid scintillation spectrometry | B | 8.74 | pKd | 1.8 | nM | Kd | J Med Chem (2016) 59: 9277-9294 [PMID:27362616] |
| ChEMBL | Inhibition of Protein kinase C beta 2 expressed in Sf-9 cells | B | 7.36 | pIC50 | 44 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2133-2138 |
| ChEMBL | Inhibition of human Protein kinase C beta 2 | B | 7.36 | pIC50 | 44 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2151-2154 |
| ChEMBL | Inhibition of human Protein kinase C beta 2 | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2155-2160 |
| ChEMBL | Inhibition of human Protein kinase C beta 1 | B | 7.49 | pIC50 | 32 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2151-2154 |
| ChEMBL | Inhibition of Protein kinase C beta 2 | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2015-2020 |
| ChEMBL | Inhibition of Protein kinase C beta 1 | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2015-2020 |
| ChEMBL | Inhibition of human Protein kinase C beta 1 | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2155-2160 |
| GtoPdb | - | - | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1996) 39: 5215-27 [PMID:8978850] |
| ChEMBL | Evaluated against recombinant human Protein kinase C beta 1 | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1996) 39: 5215-5227 [PMID:8978850] |
| ChEMBL | Evaluated against recombinant human Protein kinase C beta 2 | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1996) 39: 5215-5227 [PMID:8978850] |
| ChEMBL | Inhibitory concentration against recombinant human Protein kinase C beta 2 isozyme | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1997) 40: 226-235 [PMID:9003521] |
| ChEMBL | Inhibition of Protein kinase C beta 1 | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2015-2020 |
| ChEMBL | Inhibitory concentration against recombinant human Protein kinase C beta 1 isozyme | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1997) 40: 226-235 [PMID:9003521] |
| ChEMBL | Inhibition of Protein kinase C beta 2 | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2015-2020 |
| protein kinase C delta/Protein kinase C delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655] | ||||||||
| ChEMBL | Inhibition of Protein kinase C delta expressed in Sf-9 cells | B | 7.49 | pIC50 | 32 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2133-2138 |
| ChEMBL | Inhibition of human Protein kinase C delta | B | 7.49 | pIC50 | 32 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2151-2154 |
| ChEMBL | Inhibition of human Protein kinase C delta | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2155-2160 |
| ChEMBL | Inhibition of Protein kinase C delta | B | 7.64 | pIC50 | 23 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2015-2020 |
| ChEMBL | Evaluated against recombinant human Protein kinase C delta | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (1996) 39: 5215-5227 [PMID:8978850] |
| ChEMBL | Inhibition of Protein kinase C delta | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2015-2020 |
| GtoPdb | - | - | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (1996) 39: 5215-27 [PMID:8978850] |
| ChEMBL | Inhibitory concentration against recombinant human Protein kinase C delta isozyme | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (1997) 40: 226-235 [PMID:9003521] |
| protein kinase C epsilon/Protein kinase C epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3582] [GtoPdb: 1486] [UniProtKB: Q02156] | ||||||||
| ChEMBL | Inhibition of Protein kinase C epsilon | B | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2155-2160 |
| ChEMBL | Inhibition of protein kinase C epsilon expressed in Sf-9 cells | B | 7.31 | pIC50 | 49 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2133-2138 |
| ChEMBL | Inhibition of human Protein kinase C epsilon | B | 7.31 | pIC50 | 49 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2151-2154 |
| ChEMBL | Inhibition of Protein kinase C epsilon | B | 7.42 | pIC50 | 38 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2015-2020 |
| ChEMBL | Inhibition of Protein kinase C epsilon | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2015-2020 |
| ChEMBL | Evaluated against recombinant human Protein kinase C epsilon | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (1996) 39: 5215-5227 [PMID:8978850] |
| GtoPdb | - | - | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (1996) 39: 5215-27 [PMID:8978850] |
| ChEMBL | Inhibitory concentration against recombinant human Protein kinase C epsilon isozyme | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1997) 40: 226-235 [PMID:9003521] |
| protein kinase C eta/Protein kinase C eta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3616] [GtoPdb: 1487] [UniProtKB: P24723] | ||||||||
| ChEMBL | Inhibition of Protein kinase C eta expressed in Sf-9 cells | B | 7.66 | pIC50 | 22 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2133-2138 |
| ChEMBL | Inhibition of human protein kinase C eta | B | 7.66 | pIC50 | 22 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2151-2154 |
| ChEMBL | Inhibition of Protein kinase C eta | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2015-2020 |
| ChEMBL | Inhibition of Protein Kinase C eta | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2155-2160 |
| GtoPdb | - | - | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1996) 39: 5215-27 [PMID:8978850] |
| ChEMBL | Inhibitory concentration against recombinant human Protein kinase C eta isozyme | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1997) 40: 226-235 [PMID:9003521] |
| ChEMBL | Evaluated against recombinant human Protein kinase C eta | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1996) 39: 5215-5227 [PMID:8978850] |
| ChEMBL | Inhibition of Protein kinase C eta | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2015-2020 |
| protein kinase C gamma/Protein kinase C gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2938] [GtoPdb: 1484] [UniProtKB: P05129] | ||||||||
| ChEMBL | Inhibition of human Protein kinase C gamma | B | 7.47 | pIC50 | 34 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2151-2154 |
| ChEMBL | Inhibition of Protein kinase C gamma | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2015-2020 |
| ChEMBL | Inhibition of Protein Kinase C gamma | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2155-2160 |
| ChEMBL | Inhibitory concentration against recombinant human Protein kinase C gamma isozyme | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (1997) 40: 226-235 [PMID:9003521] |
| GtoPdb | - | - | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1996) 39: 5215-27 [PMID:8978850] |
| ChEMBL | Inhibition of Protein kinase C gamma | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2015-2020 |
| ChEMBL | Evaluated against recombinant human Protein kinase C gamma | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1996) 39: 5215-5227 [PMID:8978850] |
| protein kinase C zeta/Protein kinase C zeta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3438] [GtoPdb: 1491] [UniProtKB: Q05513] | ||||||||
| ChEMBL | Inhibitory concentration against recombinant human Protein kinase C zeta isozyme | B | 5.13 | pIC50 | 7400 | nM | IC50 | J Med Chem (1997) 40: 226-235 [PMID:9003521] |
| ChEMBL | Inhibition of Protein kinase C zeta | B | 5.23 | pIC50 | 5900 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2015-2020 |
| GtoPdb | - | - | 5.23 | pIC50 | 5900 | nM | IC50 | J Med Chem (1996) 39: 5215-27 [PMID:8978850] |
| ChEMBL | Inhibition of Protein kinase C zeta | B | 5.46 | pIC50 | 3500 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2151-2154 |
| ChEMBL | Inhibition of Protein kinase C zeta | B | 5.46 | pIC50 | 3500 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2015-2020 |
| ChEMBL | Inhibition of Protein kinase C zeta | B | 5.46 | pIC50 | 3500 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2155-2160 |
| G protein-coupled receptor kinase 1/Rhodopsin kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5607] [GtoPdb: 1465] [UniProtKB: Q15835] | ||||||||
| ChEMBL | Inhibition of GRK1-mediated bovine tubulin phosphorylation by scintillation counting | B | 6.47 | pIC50 | 340 | nM | IC50 | J Med Chem (2010) 53: 1867-1870 [PMID:20128603] |
| GtoPdb | - | - | 6.47 | pIC50 | 340 | nM | IC50 | J Med Chem (2010) 53: 1867-70 [PMID:20128603] |
| Rhodopsin kinase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879860] [UniProtKB: P28327] | ||||||||
| ChEMBL | Inhibition of bovine C-terminal truncated GRK1 (535 residues) assessed as decrease in phosphorylation of urea-washed bovine rod outer segments preincubated for 30 mins followed by ATP addition and light exposure measured after 5 to 10 mins by SDS-PAGE analysis | B | 5.39 | pIC50 | 4100 | nM | IC50 | J Med Chem (2016) 59: 9277-9294 [PMID:27362616] |
| SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] | ||||||||
| ChEMBL | Inhibition of src Protein Tyrosine Kinase | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1996) 39: 5215-5227 [PMID:8978850] |
| protein kinase A in Rat [GtoPdb: 1694] | ||||||||
| GtoPdb | Inhibition of PKA extracted from rat brain homogenate. | - | 10.4 | pIC50 | 0.04 | nM | IC50 | J Med Chem (1996) 39: 5215-27 [PMID:8978850] |
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]
