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ChEMBL ligand: CHEMBL559147 (Y-27632) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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C-C motif chemokine 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1649052] [UniProtKB: P13500] | ||||||||
ChEMBL | Inhibition of MCP1-mediated human THP cell migration | B | 5.58 | pIC50 | 2630.27 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 97-101 [PMID:21145740] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Displacement of [3H]dofetilide from human ERG | B | 4.1 | pKi | 79432.82 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 97-101 [PMID:21145740] |
protein kinase N2/Protein kinase N2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3032] [GtoPdb: 1521] [UniProtKB: Q16513] | ||||||||
ChEMBL | Inhibition of Protein kinase C related kinase 2 (PRK2) | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (2003) 46: 1478-1483 [PMID:12672248] |
ChEMBL | Inhibition of His-tagged human PRK2 expressed in HEK293 cells | B | 6.22 | pIC50 | 600 | nM | IC50 | Biochem J (2000) 351: 95-105 [PMID:10998351] |
GtoPdb | - | - | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3235-9 [PMID:20462760] |
Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464] | ||||||||
ChEMBL | Inhibition of ROCK1 (unknown origin) | B | 6.66 | pKi | 220 | nM | Ki | Medchemcomm (2012) 3: 699-709 [PMID:23275831] |
ChEMBL | Inhibition of ROCK1 (unknown origin) | B | 6.66 | pKi | 220 | nM | Ki | Eur J Med Chem (2023) 250: 115181-115181 [PMID:36764122] |
ChEMBL | Inhibitory constant against ROCK1 | B | 6.82 | pKi | 150 | nM | Ki | J Biol Chem (2006) 281: 260-268 [PMID:16249185] |
ChEMBL | Inhibition of human leukocytic ROCK1 expressed in insect cells using KKRNRTLSV as substrate after 10 mins by pyruvate kinase/lactate dehydrogenase coupled assay | B | 6.82 | pKi | 150 | nM | Ki | J Med Chem (2015) 58: 5028-5037 [PMID:26039570] |
ChEMBL | Inhibition of human ROCK1 by homogenous luciferase assay | B | 6.82 | pKi | 150 | nM | Ki | J Med Chem (2010) 53: 759-777 [PMID:20000469] |
GtoPdb | - | - | 6.85 | pKi | 140 | nM | Ki | Nature (1997) 389: 990-4 [PMID:9353125] |
ChEMBL | Inhibition of ROCK1 (unknown origin) | B | 6.85 | pKi | 140 | nM | Ki | J Med Chem (2021) 64: 1283-1345 [PMID:33481605] |
ChEMBL | Inhibition of ROCK-1 | B | 7.6 | pKi | 25.12 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 97-101 [PMID:21145740] |
ChEMBL | Inhibition of N terminal histidine tagged human recombinant ROCK1 (3 to 543 residues) in HASMC cells incubated for 2 hrs by ELISA method | B | 4.52 | pIC50 | 30000 | nM | IC50 | J Med Chem (2021) 64: 1786-1815 [PMID:33569941] |
ChEMBL | Inhibition of N terminal histidine tagged human recombinant ROCK1 (3 to 543 residues) expressed in baculovirus infected Sf9 cells using biotin-Ahx-AKRRRLSSLRA-CONH2 as a substrate incubated for 10 mins by scintillation counting method | B | 5.85 | pIC50 | 1400 | nM | IC50 | J Med Chem (2021) 64: 1786-1815 [PMID:33569941] |
ChEMBL | Inhibition of ROCK-1 by Immobilized metal ion affinity-based fluorescence polarization assay | B | 6.06 | pIC50 | 870.96 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 97-101 [PMID:21145740] |
ChEMBL | Inhibition of human recombinant N-terminal his-tagged ROCK1 (3-543) expressed in baculovirus infected Sf9 cells using Biotin-Ahx-AKRRLSSLRA-CONH2 substrate and [gamma-33P]ATP after 90 mins by scintillation proximity assay | B | 6.82 | pIC50 | 150 | nM | IC50 | J Pharmacol Exp Ther (2007) 320: 89-98 [PMID:17018693] |
ChEMBL | Inhibition of ROCK-1 (unknown origin) | B | 7.03 | pIC50 | 93 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 4812-4817 [PMID:25248678] |
GtoPdb | - | - | 7.34 | pIC50 | 46 | nM | IC50 |
Bioorg Med Chem Lett (2010) 20: 3235-9 [PMID:20462760]; Hypertension (2009) 54: 676-83 [PMID:19597037] |
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 | Inhibition of human ROCK2 by homogenous luciferase assay | B | 6.52 | pKi | 300 | nM | Ki | J Med Chem (2010) 53: 759-777 [PMID:20000469] |
ChEMBL | Inhibition of ROCK2 (unknown origin) | B | 6.52 | pKi | 300 | nM | Ki | Medchemcomm (2012) 3: 699-709 [PMID:23275831] |
ChEMBL | Inhibition of ROCK2 (unknown origin) | B | 6.52 | pKi | 300 | nM | Ki | J Med Chem (2021) 64: 1283-1345 [PMID:33481605] |
ChEMBL | Inhibition of human ROCK2 (unknown origin) | B | 6.52 | pKi | 300 | nM | Ki | Eur J Med Chem (2023) 250: 115181-115181 [PMID:36764122] |
ChEMBL | Inhibition of ROCK2 (unknown origin) assessed as inhibition constant | B | 6.85 | pKi | 140 | nM | Ki | J Med Chem (2016) 59: 2269-2300 [PMID:26486225] |
GtoPdb | - | - | 6.94 | pKi | 114 | nM | Ki |
Nature (1997) 389: 990-4 [PMID:9353125]; Hypertension (2009) 54: 676-83 [PMID:19597037] |
ChEMBL | Inhibition of Protein kinase ROCK2 (ROCKII) | B | 6.15 | pIC50 | 700 | nM | IC50 | J Med Chem (2003) 46: 1478-1483 [PMID:12672248] |
ChEMBL | Inhibition of human ROCK2 by homogenous luciferase assay | B | 6.59 | pIC50 | 260 | nM | IC50 | J Med Chem (2010) 53: 759-777 [PMID:20000469] |
ChEMBL | Inhibition of ROCK-2 by Immobilized metal ion affinity-based fluorescence polarization assay | B | 6.61 | pIC50 | 245.47 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 97-101 [PMID:21145740] |
ChEMBL | Inhibition of recombinant N-terminal GST-tagged human ROCK2 (5 to 554 residues) expressed in baculovirus infected Sf9 cells using S6K as substrate incubated for 30 mins in presence of ATP by ADP Glo kinase assay | B | 6.84 | pIC50 | 143 | nM | IC50 | J Med Chem (2022) 65: 9819-9845 [PMID:35816678] |
ChEMBL | Inhibition of human recombinant ROCK-2 using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK as substrate after 40 mins by scintillation counting analysis | B | 7.05 | pIC50 | 89 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 4812-4817 [PMID:25248678] |
GtoPdb | - | - | 7.21 | pIC50 | 61 | nM | IC50 |
Bioorg Med Chem Lett (2010) 20: 3235-9 [PMID:20462760]; Hypertension (2009) 54: 676-83 [PMID:19597037] |
ChEMBL | Inhibition of human N-terminal GST-tagged ROCK2 expressed in baculovirus-infected insect cells using long S6 kinase peptide as substrate by radiometric assay in presence of [32P]ATP | B | 7.27 | pIC50 | 54 | nM | IC50 | J Med Chem (2015) 58: 4309-4324 [PMID:25898023] |
ChEMBL | Inhibition of ROCK2 (unknown origin) using long S6 kinase peptide as substrate by radiometric assay | B | 7.27 | pIC50 | 54 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 6442-6446 [PMID:24119557] |
ChEMBL | Inhibition of ROCK2 (unknown origin) assessed as phosphorylation of MYPT1 using Tetramethylbenzidine as substrate in presence of ATP | B | 8.08 | pIC50 | 8.3 | nM | IC50 | ACS Med Chem Lett (2020) 11: 1694-1703 [PMID:32944136] |
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 | 6.1 | pIC50 | 800 | 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 | 5.08 | pIC50 | 8300 | nM | IC50 | Biochem J (2000) 351: 95-105 [PMID:10998351] |
protein kinase C epsilon in Human [GtoPdb: 1486] [UniProtKB: Q02156] | ||||||||
GtoPdb | - | - | 6.47 | pIC50 | 335 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3235-9 [PMID:20462760] |
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]