CT1812 [Ligand Id: 13335] 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: CHEMBL4846092 |
|---|
|
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 |
|---|---|---|---|---|---|---|---|---|
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG expressed in CHO cells measured by Patch-clamp assay | B | 4.59 | pEC50 | 26000 | nM | EC50 | ACS Med Chem Lett (2021) 12: 1389-1395 [PMID:34531947] |
| σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2] | ||||||||
| GtoPdb | - | - | 8.07 | pKi | 8.5 | nM | Ki | ACS Med Chem Lett (2021) 12: 1389-1395 [PMID:34531947] |
| ChEMBL | Binding affinity to Sigma 2-receptor (unknown origin) | B | 8.07 | pKi | 8.5 | nM | Ki | ACS Med Chem Lett (2021) 12: 1389-1395 [PMID:34531947] |
| ChEMBL | Binding affinity to sigma2 receptor (unknown origin) assessed as inhibition constant | B | 8.1 | pKi | 8 | nM | Ki | J Med Chem (2023) 66: 12499-12519 [PMID:37607512] |
| ChEMBL | Displacement of [3H]-1,3-di-O-tolylguanidine from human sigma 2 receptor/TMEM97 transfected in sigma 1 receptor knockout HEK293 cell membranes assessed as inhibition constant measured after 120 mins by microbeta scintillation counting analysis | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2023) 66: 12499-12519 [PMID:37607512] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | Binding affinity to sigma1 receptor (unknown origin) assessed as inhibition constant | B | 7.2 | pKi | 63 | nM | Ki | J Med Chem (2023) 66: 12499-12519 [PMID:37607512] |
| ChEMBL | Displacement of [3H]-(+)-pentazocine from human sigma1 receptor transfected in HEK293 cell membranes assessed as inhibition constant incubated for 120 mins in presence of haloperidol by microbeta scintillation counter analysis | B | 7.64 | pKi | 23 | nM | Ki | J Med Chem (2023) 66: 12499-12519 [PMID:37607512] |
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]
