TAK-715 [Ligand Id: 9328] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL363648 (Tak-715, TAK 715) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| casein kinase 1 delta/Casein kinase I isoform delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730] | ||||||||
| ChEMBL | LanthaScreen Eu Kinase Binding Assay: Table 3: Small molecules were tested for their inhibitory activities towards casein kinase 1 delta (CK1δ) and 1 epsilon (CK1ϵ). The in vitro LanthaScreen Eu kinase binding assay was used to determine the IC50 values for 15 of the synthesized compounds and 5 commercial inhibitors including SB203580 (Table 3). Tested compounds displayed a wide range of affinity between 6.8 nM (high affinity=strong inhibition) to values over 1000 nM (low affinity=very weak inhibition). | B | 7.11 | pIC50 | 78 | nM | IC50 | US-10865384-B2. 2,4,5-tri-substituted azole-based casein kinase 1 inhibitors as inducers for cardiomyogenesis (2020) |
| casein kinase 1 epsilon/Casein kinase I isoform epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674] | ||||||||
| ChEMBL | LanthaScreen Eu Kinase Binding Assay: Table 3: Small molecules were tested for their inhibitory activities towards casein kinase 1 delta (CK1δ) and 1 epsilon (CK1ϵ). The in vitro LanthaScreen Eu kinase binding assay was used to determine the IC50 values for 15 of the synthesized compounds and 5 commercial inhibitors including SB203580 (Table 3). Tested compounds displayed a wide range of affinity between 6.8 nM (high affinity=strong inhibition) to values over 1000 nM (low affinity=very weak inhibition). | B | 6.97 | pIC50 | 107 | nM | IC50 | US-10865384-B2. 2,4,5-tri-substituted azole-based casein kinase 1 inhibitors as inducers for cardiomyogenesis (2020) |
| inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa-B kinase subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920] | ||||||||
| ChEMBL | Inhibitory concentration against I-kappa-B kinase beta | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2005) 48: 5966-5979 [PMID:16162000] |
| microtubule affinity regulating kinase 3/MAP/microtubule affinity-regulating kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5600] [GtoPdb: 2099] [UniProtKB: P27448] | ||||||||
| ChEMBL | Inhibitory concentration against Mitogen-activated protein kinase kinase kinase 7 (TAK1) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2005) 48: 5966-5979 [PMID:16162000] |
| mitogen-activated protein kinase 11/Mitogen-activated protein kinase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3961] [GtoPdb: 1500] [UniProtKB: Q15759] | ||||||||
| ChEMBL | Inhibitory concentration against mitogen-activated protein kinase p38-beta | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2005) 48: 5966-5979 [PMID:16162000] |
| GtoPdb | - | - | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2005) 48: 5966-79 [PMID:16162000] |
| mitogen-activated protein kinase 12/Mitogen-activated protein kinase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4674] [GtoPdb: 1501] [UniProtKB: P53778] | ||||||||
| ChEMBL | Inhibitory concentration against mitogen-activated protein kinase p38-gamma | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2005) 48: 5966-5979 [PMID:16162000] |
| mitogen-activated protein kinase 13/Mitogen-activated protein kinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2939] [GtoPdb: 1502] [UniProtKB: O15264] | ||||||||
| ChEMBL | Inhibitory concentration against mitogen-activated protein kinase p38-delta | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2005) 48: 5966-5979 [PMID:16162000] |
| mitogen-activated protein kinase 14/Mitogen-activated protein kinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
| ChEMBL | Inhibition of recombinant human FLAG-tagged p38alpha expressed in baculovirus expression system using GFP-ATF2 (19 to 96 residues) as substrate preincubated for 5 mins followed by ATP addition measured after 20 mins by TR-FRET assay | B | 6.62 | pIC50 | 240 | nM | IC50 | Bioorg Med Chem (2018) 26: 647-660 [PMID:29291937] |
| ChEMBL | Displacement of SKF86002 from recombinant human p38alpha by fluorescence-based assay | B | 7.15 | pIC50 | 71 | nM | IC50 | Medchemcomm (2013) 4: 371-377 |
| ChEMBL | In vitro inhibitory activity against mitogen-activated protein kinase p38 alpha | B | 8.15 | pIC50 | 7.1 | nM | IC50 | J Med Chem (2005) 48: 5966-5979 [PMID:16162000] |
| ChEMBL | Inhibition of p38 alpha (unknown origin) | B | 8.15 | pIC50 | 7.1 | nM | IC50 | Eur J Med Chem (2021) 215: 113277-113277 [PMID:33601311] |
| GtoPdb | - | - | 8.15 | pIC50 | 7.1 | nM | IC50 | J Med Chem (2005) 48: 5966-79 [PMID:16162000] |
| mitogen-activated protein kinase 3/Mitogen-activated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361] | ||||||||
| ChEMBL | Inhibitory concentration against mitogen-activated protein kinase 3 | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2005) 48: 5966-5979 [PMID:16162000] |
| mitogen-activated protein kinase 8/Mitogen-activated protein kinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983] | ||||||||
| ChEMBL | Inhibitory concentration against c-Jun N-terminal kinase 1 | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2005) 48: 5966-5979 [PMID:16162000] |
| mitogen-activated protein kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3956] [GtoPdb: 2069] [UniProtKB: Q13233] | ||||||||
| ChEMBL | Inhibitory concentration against Mitogen-activated protein kinase kinase kinase 1 (MEKK1) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2005) 48: 5966-5979 [PMID:16162000] |
ChEMBL data shown on this page come from version 36:
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]
