etomidate [Ligand Id: 5463] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL681 (Amidate, Etomidate)
1 CHEMBL681_lig_chart_1 Acetylcholine receptor Torpedo californica
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  • CYP11B1/Cytochrome P450 11B1 in Human [ChEMBL: CHEMBL1908] [GtoPdb: 1359] [UniProtKB: P15538]
  • This target only has 0 pki data point
  • 0
2 CHEMBL681_lig_chart_2 Cytochrome P450 11B1 Human
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  • CYP11B2/Cytochrome P450 11B2 in Human [ChEMBL: CHEMBL2722] [GtoPdb: 1360] [UniProtKB: P19099]
  • This target only has 0 pki data point
  • 0
3 CHEMBL681_lig_chart_3 Cytochrome P450 11B2 Human
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  • GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2095172] [GtoPdb: 404414411] [UniProtKB: P14867P18507P47870]
  • This target only has 0 pki data point
  • 0
4 CHEMBL681_lig_chart_4 GABA-A receptor; alpha-1/beta-2/gamma-2 Human
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  • GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-2/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2111413] [GtoPdb: 414405411] [UniProtKB: P18507P47869P47870]
  • This target only has 0 pki data point
  • 0
5 CHEMBL681_lig_chart_5 GABA A receptor alpha-2/beta-2/gamma-2 Human
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  • GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
  • This target only has 0 pki data point
  • 0
6 CHEMBL681_lig_chart_6 GABA receptor alpha-1 subunit Human
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  • 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 [ChEMBL: CHEMBL3038460] [GtoPdb: 476462475471] [UniProtKB: P02716P04756P04760P09690]
  • This target only has 0 pki data point
  • 0
7 CHEMBL681_lig_chart_7 Nicotinic acetylcholine receptor alpha1/beta1/gamma/delta Mouse
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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: P02710P02712P02714P02718]
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: 404414411] [UniProtKB: P14867P18507P47870]
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: 414405411] [UniProtKB: P18507P47869P47870]
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: 476462475471] [UniProtKB: P02716P04756P04760P09690]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]