BAY-069 [Ligand Id: 12232] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL4551635 |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Aspartate aminotransferase, cytoplasmic in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189139] [UniProtKB: P17174] | ||||||||
| ChEMBL | Aspartate transaminase assay (GOT1) | B | 4.3 | pIC50 | >50000 | nM | IC50 | Data for DCP probe BAY-069 |
| ChEMBL | Inhibition of GOT1 (unknown origin) | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2022) 65: 14366-14390 [PMID:36261130] |
| Aspartate aminotransferase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4524033] [UniProtKB: P00505] | ||||||||
| ChEMBL | Aspartate transaminase assay (GOT2) | B | 4.3 | pIC50 | >50000 | nM | IC50 | Data for DCP probe BAY-069 |
| ChEMBL | Inhibition of GOT2 (unknown origin) | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2022) 65: 14366-14390 [PMID:36261130] |
| branched chain amino acid transaminase 2/Branched-chain-amino-acid aminotransferase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3616354] [GtoPdb: 2893] [UniProtKB: O15382] | ||||||||
| ChEMBL | Inhibition of human recombinant BCAT2 using leucine and alpha-KG as substrate in presence of NADH by fluorescence assay | B | 5.57 | pIC50 | 2680 | nM | IC50 | J Med Chem (2022) 65: 14366-14390 [PMID:36261130] |
| ChEMBL | Inhibition of human recombinant BCAT2 using leucine and alpha-KG as substrate in presence of NADH by fluorescence assay | B | 5.94 | pIC50 | 1160 | nM | IC50 | J Med Chem (2022) 65: 14366-14390 [PMID:36261130] |
| ChEMBL | Cellular mechanistic assay – BCAA measurement (MDA-MB-231 cells) | B | 6.06 | pIC50 | 874 | nM | IC50 | Data for DCP probe BAY-069 |
| ChEMBL | Inhibition of human recombinant BCAT2 using leucine and alpha-KG as substrate in presence of NADH by fluorescence assay | B | 6.82 | pIC50 | 153 | nM | IC50 | J Med Chem (2022) 65: 14366-14390 [PMID:36261130] |
| GtoPdb | - | - | 6.82 | pIC50 | 153 | nM | IC50 | J Med Chem (2022) 65: 14366-14390 [PMID:36261130] |
| ChEMBL | Biochemical assay (BCAT2) | B | 6.89 | pIC50 | 130 | nM | IC50 | Data for DCP probe BAY-069 |
| branched chain amino acid transaminase 1/Branched-chain-amino-acid transferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4679] [GtoPdb: 3210] [UniProtKB: P54687] | ||||||||
| ChEMBL | Inhibition of N-terminal his-tagged human recombinant BCAT1 expressed in Escherichia coli BL21(DE3) cells using leucine and alpha-KG as substrate in presence of NADH by fluorescence assay | B | 5.63 | pIC50 | 2320 | nM | IC50 | J Med Chem (2022) 65: 14366-14390 [PMID:36261130] |
| ChEMBL | Cellular mechanistic assay – BCAA measurement (U-87-MG cells) | B | 6.45 | pIC50 | 358 | nM | IC50 | Data for DCP probe BAY-069 |
| ChEMBL | Inhibition of N-terminal his-tagged human recombinant BCAT1 expressed in Escherichia coli BL21(DE3) cells using leucine and alpha-KG as substrate in presence of NADH by fluorescence assay | B | 6.73 | pIC50 | 186 | nM | IC50 | J Med Chem (2022) 65: 14366-14390 [PMID:36261130] |
| ChEMBL | Inhibition of N-terminal his-tagged human recombinant BCAT1 expressed in Escherichia coli BL21(DE3) cells using leucine and alpha-KG as substrate in presence of NADH by fluorescence assay | B | 7.51 | pIC50 | 31 | nM | IC50 | J Med Chem (2022) 65: 14366-14390 [PMID:36261130] |
| GtoPdb | - | - | 7.51 | pIC50 | 31 | nM | IC50 | J Med Chem (2022) 65: 14366-14390 [PMID:36261130] |
| ChEMBL | Biochemical assay (BCAT1) | B | 7.57 | pIC50 | 27 | nM | IC50 | Data for DCP probe BAY-069 |
| Translocator protein in Rat [GtoPdb: 2879] [UniProtKB: P16257] | ||||||||
| GtoPdb | - | - | 7.13 | pKi | 73.3 | nM | Ki | Data for DCP probe BAY-069. www.ebi.ac.uk/chembl |
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]
