H-89 [Ligand Id: 5983] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL104264 (H-89) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| calcium/calmodulin dependent protein kinase kinase 2/CaM-kinase kinase beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5284] [GtoPdb: 1957] [UniProtKB: Q96RR4] | ||||||||
| ChEMBL | Inhibition of CaM-KKbeta | B | 4.53 | pKi | 29700 | nM | Ki | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| cAMP-dependent protein kinase A in Bovine (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2111446] [UniProtKB: P00515, P00517, P05131, P31322] | ||||||||
| ChEMBL | Inhibitory constant against bovine cAPK (PKA) | B | 6.32 | pKi | 480 | nM | Ki | J Biol Chem (1996) 271: 26157-26164 [PMID:8824261] |
| casein kinase 1 alpha 1/Casein kinase I alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729] | ||||||||
| ChEMBL | Inhibition of casein kinase 1 | B | 4.42 | pKi | 38300 | nM | Ki | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
| ChEMBL | Inhibition of GSK3-beta in human PC3M cells by ELISA | B | 4.82 | pIC50 | 15000 | nM | IC50 | J Med Chem (2008) 51: 2147-2157 [PMID:18345609] |
| Myosin light chain kinase, smooth muscle in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3062] [UniProtKB: P11799] | ||||||||
| ChEMBL | Inhibitory constant against MLCK | B | 4.55 | pKi | 28300 | nM | Ki | J Biol Chem (1996) 271: 26157-26164 [PMID:8824261] |
| myosin light chain kinase/Myosin light chain kinase, smooth muscle in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2428] [GtoPdb: 1552] [UniProtKB: Q15746] | ||||||||
| ChEMBL | Binding affinity at MLCK | B | 4.55 | pKi | 28300 | nM | Ki | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 4.8 | pIC50 | 15848.93 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5.3 | pIC50 | 5011.87 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antimalarial activity against drug-resistant Plasmodium falciparum D6 | F | 5.32 | pIC50 | 4800 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 4961-4966 [PMID:17588749] |
| ChEMBL | Antimalarial activity against drug-resistant Plasmodium falciparum W2 | F | 5.68 | pIC50 | 2100 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 4961-4966 [PMID:17588749] |
| Rho associated coiled-coil containing protein kinase 2/Rho-associated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2973] [GtoPdb: 1504] [UniProtKB: O75116] | ||||||||
| ChEMBL | Displacement of fluorescent-ARC-1063 from His6-tagged recombinant human ROCK2 by luminescence intensity assay | B | 7.62 | pKd | 24 | nM | Kd | Bioorg Med Chem Lett (2012) 22: 3425-3430 [PMID:22521647] |
| ChEMBL | Displacement of fluorescent-ARC-1063 from His6-tagged recombinant human ROCK2 by luminescence intensity assay | B | 5.44 | pIC50 | 3630.78 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3425-3430 [PMID:22521647] |
| ChEMBL | Inhibition of ROCK2 | B | 6.57 | pIC50 | 270 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| Rho associated coiled-coil containing protein kinase 2/Rho-associated protein kinase 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5490] [GtoPdb: 1504] [UniProtKB: Q62868] | ||||||||
| ChEMBL | Inhibition of rat ROCK2 expressed in Sf9 cells | B | 6.57 | pIC50 | 270 | nM | IC50 | Biochem J (2000) 351: 95-105 [PMID:10998351] |
| ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443] | ||||||||
| ChEMBL | Inhibition of His-tagged human S6K1 expressed in Escherichia coli | B | 7.1 | pIC50 | 80 | nM | IC50 | Biochem J (2000) 351: 95-105 [PMID:10998351] |
| ribosomal protein S6 kinase A5/Ribosomal protein S6 kinase alpha 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4237] [GtoPdb: 1523] [UniProtKB: O75582] | ||||||||
| ChEMBL | Inhibition of His-tagged human MSK1 expressed in Sf9 cells | B | 6.92 | pIC50 | 120 | nM | IC50 | Biochem J (2000) 351: 95-105 [PMID:10998351] |
| AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749] | ||||||||
| ChEMBL | Inhibition constant for protein kinase B alpha (Akt1) in fluorescent enzymatic assay | B | 5.35 | pKi | 4500 | nM | Ki | J Med Chem (2005) 48: 2278-2281 [PMID:15801821] |
| ChEMBL | Inhibition of human PKBalpha expressed in SF9 cells | B | 5.59 | pIC50 | 2600 | nM | IC50 | Biochem J (2000) 351: 95-105 [PMID:10998351] |
| ChEMBL | Inhibition of protein kinase B alpha (Akt1) in fluorescent enzymatic assay | B | 5.64 | pIC50 | 2300 | nM | IC50 | J Med Chem (2005) 48: 2278-2281 [PMID:15801821] |
| ChEMBL | Inhibition of AKT1 (unknown origin) using ATP/eNOS as substrate incubated for 5 mins prior to substrate addition measured after 30 mins by fluorescence polarization assay | B | 5.66 | pIC50 | 2200 | nM | IC50 | Eur J Med Chem (2014) 75: 11-20 [PMID:24508830] |
| ChEMBL | Inhibition of GST-tagged PKB/Akt1 incubated for 5 mins before eNOS substrate and ATP addition measured after 30 mins by kinase assay | B | 5.74 | pIC50 | 1800 | nM | IC50 | Eur J Med Chem (2011) 46: 5949-5958 [PMID:22027102] |
| ChEMBL | Inhibition of Akt1 (unknown origin) using ATP/eNOS as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence polarization assay | B | 5.76 | pIC50 | 1720 | nM | IC50 | Eur J Med Chem (2014) 73: 167-176 [PMID:24389511] |
| ChEMBL | Inhibition of AKT1 by FRET based assay | B | 5.8 | pIC50 | 1600 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4634-4638 [PMID:19604696] |
| AKT serine/threonine kinase 2/Serine/threonine-protein kinase AKT2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751] | ||||||||
| ChEMBL | Inhibition of PKBbeta by radiometric filter binding assay | B | 6.23 | pIC50 | 590 | nM | IC50 | J Med Chem (2007) 50: 2289-2292 [PMID:17451235] |
| ChEMBL | Inhibition of PKBbeta recombinant by radiometric filter binding assay | B | 6.23 | pIC50 | 590 | nM | IC50 | J Med Chem (2008) 51: 2147-2157 [PMID:18345609] |
| ChEMBL | Inhibition of PKBbeta by radiometric filter binding assay | B | 6.23 | pIC50 | 590 | nM | IC50 | J Med Chem (2010) 53: 2239-2249 [PMID:20151677] |
| ChEMBL | Inhibition of AKT2 by FRET based assay | B | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4634-4638 [PMID:19604696] |
| AKT serine/threonine kinase 3/Serine/threonine-protein kinase AKT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243] | ||||||||
| ChEMBL | Inhibition of AKT3 by FRET based assay | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4634-4638 [PMID:19604696] |
| protein kinase, cAMP-dependent, catalytic, alpha subunit in Human [GtoPdb: 1476] [UniProtKB: P17612] | ||||||||
| GtoPdb | - | - | 7.32 | pKi | 48 | nM | Ki | J Biol Chem (1990) 265: 5267-72 [PMID:2156866] |
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]
