tizaterkib [Ligand Id: 11674] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4482864 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864, P24941] | ||||||||
| ChEMBL | Inhibition of human full length C-terminal His6-tagged Cdk2/human full length N-terminal GST-tagged Cyclin E expressed in baculovirus infected Sf21 insect cells after 1 hr by electromobility shift assay | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2019) 62: 11004-11018 [PMID:31710489] |
| cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078] | ||||||||
| ChEMBL | Inhibition of recombinant full length human GST/His-tagged CDK5/p25 expressed in baculovirus expression system | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2019) 62: 11004-11018 [PMID:31710489] |
| ChEMBL | Inhibition of recombinant full length human His-tagged CDK5/p35 expressed in baculovirus expression system | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2019) 62: 11004-11018 [PMID:31710489] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Med Chem (2019) 62: 11004-11018 [PMID:31710489] |
| mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] | ||||||||
| ChEMBL | Binding affinity to non-phosphorylated biotinylated ERK2 (unknown origin) by SPR analysis | B | 10 | pKd | 0.1 | nM | Kd | J Med Chem (2019) 62: 11004-11018 [PMID:31710489] |
| ChEMBL | Binding affinity to MEK-activated phosphorylated biotinylated ERK2 (unknown origin) by SPR analysis | B | 10.3 | pKd | 0.05 | nM | Kd | J Med Chem (2019) 62: 11004-11018 [PMID:31710489] |
| GtoPdb | Inhibition in an ERK2 biochemical assay | - | 9.18 | pIC50 | 0.66 | nM | IC50 | Mol Cancer Ther (2021) 20: 238-249 [PMID:33273059] |
| ChEMBL | Inhibition of MEK U911-activated ERK2 (unknown origin) using ERKtide as substrate preincubated for 20 mins followed by substrate addition in presence of 1 mM ATP after 10 mins by rapidfire mass spectrometry analysis | B | 9.18 | pIC50 | 0.66 | nM | IC50 | J Med Chem (2019) 62: 11004-11018 [PMID:31710489] |
| ChEMBL | Inhibition of MEK U911-activated ERK2 (unknown origin) using ERKtide as substrate preincubated for 20 mins followed by substrate addition in presence of ATP at Km concentration after 20 mins by rapidfire mass spectrometry analysis | B | 9.52 | pIC50 | <0.3 | nM | IC50 | J Med Chem (2019) 62: 11004-11018 [PMID:31710489] |
| NUAK family kinase 1/NUAK family SNF1-like kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5784] [GtoPdb: 2129] [UniProtKB: O60285] | ||||||||
| ChEMBL | Inhibition of recombinant full length human His-tagged ARK5 expressed in baculovirus expression system | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2019) 62: 11004-11018 [PMID:31710489] |
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]
