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: CHEMBL510780 (NS-8593) |
---|
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 |
---|---|---|---|---|---|---|---|---|
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
ChEMBL | Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate | B | 5.86 | pIC50 | 1393 | nM | IC50 | HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators |
KCa2.3/Small conductance calcium-activated potassium channel protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3381] [GtoPdb: 383] [UniProtKB: Q9UGI6] | ||||||||
ChEMBL | Inhibition of wild type human SK3 channel expressed in HEK293 cells | B | 7 | pKd | 100 | nM | Kd | J Med Chem (2008) 51: 7625-7634 [PMID:18998663] |
GtoPdb | - | - | 6.1 | pIC50 | - | - | - | Mol Pharmacol (2006) 70: 1771-82 [PMID:16926279] |
ChEMBL | Inhibition of wild type human SK3 channel expressed in HEK293 cells assessed as Ca2+ sensitivity by inside-out patch clamp technique in presence of 500 nM Ca2+ | B | 5.66 | pEC50 | 2200 | nM | EC50 | J Med Chem (2008) 51: 7625-7634 [PMID:18998663] |
ChEMBL | Inhibition of wild type human SK3 channel expressed in HEK293 cells assessed as Ca2+ sensitivity by inside-out patch clamp technique | B | 6.4 | pEC50 | 400 | nM | EC50 | J Med Chem (2008) 51: 7625-7634 [PMID:18998663] |
KCa2.3/Small conductance calcium-activated potassium channel protein 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3780] [GtoPdb: 383] [UniProtKB: P70605] | ||||||||
ChEMBL | Inhibition of Wistar rat recombinant SK3 channel expressed in HEK293 cells by whole cell patch clamp technique | B | 7.11 | pKd | 77 | nM | Kd | J Med Chem (2008) 51: 7625-7634 [PMID:18998663] |
ChEMBL | Displacement of [I125]apamine from Wistar rat recombinant SK3 channel expressed in HEK293 cells | B | 4.3 | pKi | >50000 | nM | Ki | J Med Chem (2008) 51: 7625-7634 [PMID:18998663] |
TRPM7/Transient receptor potential cation channel subfamily M member 7 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3714706] [GtoPdb: 499] [UniProtKB: Q923J1] | ||||||||
ChEMBL | Inhibition of mouse TRPM7 transfected in HEK293 cells assessed as inhibition of channel current in presence of 300 uM free intracellular Mg2+ by whole cell patch clamp analysis | B | 5.23 | pIC50 | 5900 | nM | IC50 | J Nat Prod (2024) 87: 783-797 [PMID:38537009] |
ChEMBL | Inhibition of mouse TRPM7 transfected in HEK293 cells assessed as inhibition of channel current in presence of 780 uM free intracellular Mg2+ by whole cell patch clamp analysis | B | 5.41 | pIC50 | 3900 | nM | IC50 | J Nat Prod (2024) 87: 783-797 [PMID:38537009] |
ChEMBL | Inhibition of mouse TRPM7 transfected in HEK293 cells assessed as inhibition of channel current in absence of intracellular Mg2+ by whole cell patch clamp analysis | B | 5.8 | pIC50 | 1600 | nM | IC50 | J Nat Prod (2024) 87: 783-797 [PMID:38537009] |
GtoPdb | - | - | 5.8 | pIC50 | 1600 | nM | IC50 | Br J Pharmacol (2012) 166: 1357-76 [PMID:22242975] |
KCa2.1 in Human [GtoPdb: 381] [UniProtKB: Q92952] | ||||||||
GtoPdb | - | - | 6.4 | pIC50 | 400 | nM | IC50 | Mol Pharmacol (2006) 70: 1771-82 [PMID:16926279] |
KCa2.2 in Human [GtoPdb: 382] [UniProtKB: Q9H2S1] | ||||||||
GtoPdb | - | - | 6.2 | pIC50 | - | - | - | Mol Pharmacol (2006) 70: 1771-82 [PMID:16926279] |
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]