etomidate [Ligand Id: 5463] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL681 (Amidate, Etomidate, Etomidato, Hypnomidate, NSC-759160) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Acetylcholine receptor in Torpedo californica (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096975] [UniProtKB: P02710, P02712, P02714, P02718] | ||||||||
| ChEMBL | Inhibition of currents when compound wascoapplied with acetylcholine to recombinant Torpedo nAcChoR (from 6 oocytes) | F | 4.39 | pIC50 | 41000 | nM | IC50 | J Med Chem (2003) 46: 1257-1265 [PMID:12646036] |
| CYP11B1/Cytochrome P450 11B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1908] [GtoPdb: 1359] [UniProtKB: P15538] | ||||||||
| ChEMBL | Inhibition of human CYP11B1 expressed in chinese hamster V79 cells | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2010) 53: 1712-1725 [PMID:20121113] |
| ChEMBL | Inhibition of human CYP11B1 expressed in hamster V79MZ cells using 11-deoxycorticosterone substrate | B | 9.3 | pIC50 | 0.5 | nM | IC50 | ACS Med Chem Lett (2011) 2: 2-6 [PMID:24900247] |
| ChEMBL | Inhibition of human CYP11B1 expressed in hamster V79 MZ cells using [3H] 11 deoxycorticosterone as substrate by HPLC radioflow detector | B | 9.3 | pIC50 | 0.5 | nM | IC50 | ACS Med Chem Lett (2011) 2: 559-564 [PMID:24900349] |
| ChEMBL | Inhibition of human CYP11B1 expressed in V79 MZ cells pretreated with compound for 1 hr followed by addition of 500 nM 11-deoxycorticosterone for 3 hrs by HPLC analysis | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2014) 57: 5011-5022 [PMID:24422519] |
| CYP11B2/Cytochrome P450 11B2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2722] [GtoPdb: 1360] [UniProtKB: P19099] | ||||||||
| ChEMBL | Inhibition of human CYP11B2 expressed in chinese hamster V79 cells | B | 8.77 | pIC50 | 1.7 | nM | IC50 | J Med Chem (2010) 53: 1712-1725 [PMID:20121113] |
| ChEMBL | Inhibition of human aldosterone synthase expressed in V79 MZ cells pretreated with compound for 1 hr followed by addition of 500 nM 11-deoxycorticosterone for 1hr by HPLC analysis | B | 8.77 | pIC50 | 1.7 | nM | IC50 | J Med Chem (2014) 57: 5011-5022 [PMID:24422519] |
| ChEMBL | Inhibition of human CYP11B2 expressed in hamster V79MZ cells using 11-deoxycorticosterone substrate | B | 10 | pIC50 | 0.1 | nM | IC50 | ACS Med Chem Lett (2011) 2: 2-6 [PMID:24900247] |
| ChEMBL | Inhibition of human CYP11B2 expressed in hamster V79 MZ cells using [3H] 11 deoxycorticosterone as substrate by HPLC radioflow detector | B | 10 | pIC50 | 0.1 | nM | IC50 | ACS Med Chem Lett (2011) 2: 559-564 [PMID:24900349] |
| GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095172] [GtoPdb: 404, 414, 411] [UniProtKB: P14867, P18507, P47870] | ||||||||
| ChEMBL | Direct activation of Gamma-aminobutyric acid A receptor in the absence of GABA | F | 4.19 | pEC50 | 64000 | nM | EC50 | J Med Chem (2003) 46: 1257-1265 [PMID:12646036] |
| ChEMBL | Enhancement of currents elicited by GABA at EC5 (6-12 uM) | F | 5.6 | pEC50 | 2500 | nM | EC50 | J Med Chem (2003) 46: 1257-1265 [PMID:12646036] |
| ChEMBL | Ability to enhance currents from alpha-1-beta-2-gamma-2L-subunit of GABA receptor elicited by low concentrations of GABA | F | 5.92 | pEC50 | 1200 | nM | EC50 | J Med Chem (2003) 46: 1257-1265 [PMID:12646036] |
| GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-2/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111413] [GtoPdb: 414, 405, 411] [UniProtKB: P18507, P47869, P47870] | ||||||||
| ChEMBL | Effective concentration against GABA-evoked chloride currents mediated by human Gamma-aminobutyric acid GABA-A receptor alpha2-beta2-gamma2L expressed in Xenopus oocytes | B | 5.46 | pEC50 | 3500 | nM | EC50 | J Med Chem (2005) 48: 2638-2645 [PMID:15801854] |
| GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867] | ||||||||
| ChEMBL | Activity at human GABAA alpha-1-beta-2-gamma-2s receptor expressed in HEK293 cells assessed as effect on GABA-induced current at 3 uM by whole cell patch-clamp technique | B | 4.96 | pEC50 | 11000 | nM | EC50 | J Biol Chem (2007) 282: 12038-12047 [PMID:17311911] |
| nicotinic acetylcholine receptor δ subunit/nicotinic acetylcholine receptor α1 subunit/nicotinic acetylcholine receptor γ subunit/nicotinic acetylcholine receptor β1 subunit/Nicotinic acetylcholine receptor alpha1/beta1/gamma/delta in Mouse (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038460] [GtoPdb: 476, 462, 475, 471] [UniProtKB: P02716, P04756, P04760, P09690] | ||||||||
| ChEMBL | Inhibition of recombinant embryonic mouse muscle Nicotinic Acetylcholine Receptor (3 oocytes) | B | 4.3 | pIC50 | 50000 | nM | IC50 | J Med Chem (2003) 46: 1257-1265 [PMID:12646036] |
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]
