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 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]
