GDC-0134 [Ligand Id: 11506] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3732012 (Gdc-0134, Rg-6000) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| mitogen-activated protein kinase kinase kinase 12/Mitogen-activated protein kinase kinase kinase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1908389] [GtoPdb: 2072] [UniProtKB: Q12852] | ||||||||
| GtoPdb | Inhibition of human DLK catalytic domain activity (1 to 520 amino acids) in a TR-FRET assay. | - | 8.35 | pKi | 4.48 | nM | Ki | WO2014177060A1. Biheteroaryl compounds and uses thereof (2014) |
| ChEMBL | Inhibition of N-terminally GST-tagged human DLK catalytic domain (1 to 520 amino acids) using N- terminal His-tagged MKK4 K131M substrate incubated for 60 mins by TR-FRET assay | B | 9 | pKi | 1 | nM | Ki | WO-2014177060-A1. Biheteroaryl compounds and uses thereof (2014) |
| ChEMBL | Inhibition of DLK (unknown origin) | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2022) 65: 16290-16312 [PMID:36469401] |
| mitogen-activated protein kinase kinase kinase 13/Mitogen-activated protein kinase kinase kinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163124] [GtoPdb: 2073] [UniProtKB: O43283] | ||||||||
| ChEMBL | Inhibition of LZK (unknown origin) | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2022) 65: 16290-16312 [PMID:36469401] |
| Protein delta homolog 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5671] [UniProtKB: P80370] | ||||||||
| ChEMBL | Inhibition of DLK (unknown origin) | B | 7.96 | pIC50 | 11 | nM | IC50 | Eur J Med Chem (2023) 255: 115404-115404 [PMID:37098296] |
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]
