succinic acid [Ligand Id: 3637] 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: CHEMBL576 (Amber acid, Dihydrofumaric acid, E363, FEMA NO. 4719, NSC-106449, Succinic acid, Succinicum acidum) |
|---|
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 |
|---|---|---|---|---|---|---|---|---|
| egl-9 family hypoxia inducible factor 1/Egl nine homolog 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5697] [GtoPdb: 2833] [UniProtKB: Q9GZT9] | ||||||||
| ChEMBL | Binding affinity to human PHD2 by nondenaturing ESI-MS | B | 4 | pKd | >100000 | nM | Kd | J Med Chem (2010) 53: 867-875 [PMID:20025281] |
| ChEMBL | Binding affinity to human PHD2-Mn(II) using 12.5% H2O/87.5% D2O MQC spectrometer operated at 500 MHz at 298K temperature | B | 4 | pKd | >100000 | nM | Kd | J Med Chem (2010) 53: 867-875 [PMID:20025281] |
| ChEMBL | Inhibition of human PHD2 at 293K temperature by solvent relaxation technique | B | 4.07 | pIC50 | 85300 | nM | IC50 | J Med Chem (2010) 53: 867-875 [PMID:20025281] |
| ChEMBL | Inhibition of 2-oxoglutarate-dependent human recombinant HIF PHD2 preincubated for 1 hr | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Med Chem (2008) 51: 7053-7056 [PMID:18942826] |
| RNA demethylase ALKBH5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3621037] [UniProtKB: Q6P6C2] | ||||||||
| ChEMBL | Inhibition of recombinant human ALKBH5 catalytic AlkB domain (74 to 294 residues) transfected in Escherichia coli BL21 (DE3) using 8-mer m6A-ssDNA as substrate incubated for 30 mins followed by substrate addition and measured after 3 hrs by HPLC analysis | B | 4.52 | pIC50 | 30000 | nM | IC50 | J Med Chem (2021) 64: 16974-17003 [PMID:34792334] |
| succinate receptor/Succinate receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2150838] [GtoPdb: 166] [UniProtKB: Q9BXA5] | ||||||||
| ChEMBL | Agonist activity at human succinate receptor 1 expressed in HEK293T cells co-transfected with Galphai-Rluc8/Ggamma8-GFP2/Gbeta3 assessed as G protein activation incubated for 5 mins by luminescence based BRET assay | F | 4.45 | pEC50 | 35481.34 | nM | EC50 | J Med Chem (2023) 66: 8951-8974 [PMID:37318348] |
| GtoPdb | - | - | 4.7 | pEC50 | 20000 | nM | EC50 |
Nature (2004) 429: 188-93 [PMID:15141213]; J Biomol Screen (2013) 18: 599-609 [PMID:23396314] |
| ChEMBL | Agonist activity at N-terminal Nluc-tagged human Succinate receptor 1 expressed in human Flp-In-T-REx-293 cells assessed as inhibition of forskolin-induced cAMP production by cAMP assay | F | 4.8 | pEC50 | 15848.93 | nM | EC50 | J Med Chem (2023) 66: 8951-8974 [PMID:37318348] |
| ChEMBL | Agonist activity at human succinate receptor 1 expressed in human Flp-In-T-REx-293 cells assessed as inhibition of forskolin-induced cAMP production incubated for 30 mins by TR-FRET analysis | F | 5.04 | pEC50 | 9120.11 | nM | EC50 | J Med Chem (2023) 66: 8951-8974 [PMID:37318348] |
| succinate receptor/Succinate receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4739861] [GtoPdb: 166] [UniProtKB: Q99MT6] | ||||||||
| ChEMBL | Agonist activity at mouse succinate receptor 1 expressed in human Flp-In-T-REx-293 cells assessed as inhibition of forskolin-induced cAMP production incubated for 30 mins by TR-FRET analysis | F | 5.02 | pEC50 | 9549.93 | nM | EC50 | J Med Chem (2023) 66: 8951-8974 [PMID:37318348] |
| ChEMBL | Agonist activity at mouse succinate receptor 1 expressed in HEK293T cells co-transfected with Galphai-Rluc8/Ggamma8-GFP2/Gbeta3 assessed as G protein activation incubated for 5 mins by luminescence based BRET assay | F | 5.29 | pEC50 | 5128.61 | nM | EC50 | J Med Chem (2023) 66: 8951-8974 [PMID:37318348] |
| ChEMBL | Agonist activity at N-terminal Nluc-tagged mouse Succinate receptor 1 expressed in human Flp-In-T-REx-293 cells assessed as inhibition of forskolin-induced cAMP production by cAMP assay | F | 5.69 | pEC50 | 2041.74 | nM | EC50 | J Med Chem (2023) 66: 8951-8974 [PMID:37318348] |
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]
