etomidate [Ligand Id: 5463] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL681 (Amidate, Etomidate, 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
