propofol [Ligand Id: 5464] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL526 (Diprivan, Disoprivan, Disoprofol, Fresofol, ICI 35,868, ICI 35-868, ICI-35868, ICI35,868, Lipuro, NSC-5105, Phenol, 2,6-bis(1-methylethyl), Propofol, Rapinovet)
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Human [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612]
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  • Arachidonate 15-lipoxygenase in Rabbit [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
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  • carbonic anhydrase 1/Carbonic anhydrase I in Human [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915]
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  • carbonic anhydrase 2/Carbonic anhydrase II in Human [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
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  • GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABA A receptor alpha-1/beta-1/gamma-2 in Human [ChEMBL: CHEMBL2111392] [GtoPdb: 404, 410, 414] [UniProtKB: P14867, P18505, P18507]
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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: 404, 414, 411] [UniProtKB: P14867, P18507, P47870]
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  • GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABA-A receptor; alpha-1/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094121] [GtoPdb: 404, 414, 412] [UniProtKB: P14867, P18507, P28472]
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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: 414, 405, 411] [UniProtKB: P18507, P47869, P47870]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • HCN1 in Mouse [GtoPdb: 400] [UniProtKB: O88704]
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  • TRPV4 in Human [GtoPdb: 510] [UniProtKB: Q9HBA0]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Fatty acid amide hydrolase/Anandamide amidohydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
ChEMBL Inhibitory concentration against fatty acid amide hydrolase B 4.28 pIC50 52000 nM IC50 J Med Chem (2005) 48: 5059-5087 [PMID:16078824]
Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612]
ChEMBL Inhibition of rat FAAH B 4.85 pIC50 14000 nM IC50 J Med Chem (2008) 51: 7327-7343 [PMID:18983142]
Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
ChEMBL DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) B 5.12 pIC50 7596 nM IC50 DrugMatrix in vitro pharmacology data
carbonic anhydrase 1/Carbonic anhydrase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915]
ChEMBL Inhibition of human erythrocyte CA1 esterase activity using 4-nitrophenyl acetate substrate B 4 pKi 98900 nM Ki Bioorg Med Chem (2009) 17: 3207-3211 [PMID:19231207]
carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
ChEMBL Inhibition of human erythrocyte CA2 esterase activity using 4-nitrophenyl acetate substrate B 4.71 pKi 19500 nM Ki Bioorg Med Chem (2009) 17: 3207-3211 [PMID:19231207]
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) B 5.42 pIC50 3832 nM IC50 DrugMatrix in vitro pharmacology data
GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABAA receptor α4 subunit/GABAA receptor α6 subunit/GABA-A receptor; agonist GABA site in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2109244] [GtoPdb: 404, 410, 412, 408, 406, 405, 411, 407, 409] [UniProtKB: P14867, P18505, P28472, P31644, P34903, P47869, P47870, P48169, Q16445]
ChEMBL Agonist activity at human alpha1beta2gamma2L GABAA receptor expressed in Xenopus oocytes assessed as potentiation of channel current response by two-electrode voltage clamp electrophysiology assay F 4.3 pEC50 50000 nM EC50 J Med Chem (2011) 54: 8124-8135 [PMID:22029276]
ChEMBL Agonist activity at human alpha1beta2gamma2L GABAA receptor expressed in Xenopus oocytes assessed as potentiation of GABA-induced current response by two-electrode voltage clamp electrophysiology assay F 5.28 pEC50 5200 nM EC50 J Med Chem (2011) 54: 8124-8135 [PMID:22029276]
GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABA A receptor alpha-1/beta-1/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111392] [GtoPdb: 404, 410, 414] [UniProtKB: P14867, P18505, P18507]
ChEMBL Direct activation of chloride current in Xenopus laevis oocytes expressing human alpha-1-beta-1-gamma-2 GABA-A receptor subunits F 4.36 pEC50 44000 nM EC50 J Med Chem (1998) 41: 1846-1854 [PMID:9599235]
ChEMBL Modulation of GABA-induced chloride currents in Xenopus laevis oocytes expressing human alpha-1-beta-1-gamma-2 GABA-A receptor subunits F 5.1 pEC50 8000 nM EC50 J Med Chem (1998) 41: 1846-1854 [PMID:9599235]
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 human Gamma-aminobutyric acid A receptor alpha-1-beta-2-gamma-2 B 5 pEC50 10000 nM EC50 J Med Chem (2002) 45: 3210-3221 [PMID:12109905]
ChEMBL Potentiation of GABA responses at human Gamma-aminobutyric acid A receptor alpha-1-beta-2-gamma-2 B 5.7 pEC50 1995.26 nM EC50 J Med Chem (2002) 45: 3210-3221 [PMID:12109905]
GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABA-A receptor; alpha-1/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094121] [GtoPdb: 404, 414, 412] [UniProtKB: P14867, P18507, P28472]
ChEMBL Inhibition of [3H]R-mTFD-MPAB labelling of GABAA alpha1beta3gamma2L (unknown origin) expressed in Xenopus laevis oocytes assessed as reduction in photoincorporation at M227 residues of beta3 subunit measured after 30 mins in presence of GABA by liquid scintillation counting method B 4.36 pIC50 44000 nM IC50 Eur J Med Chem (2020) 194: 112261-112261 [PMID:32247113]
ChEMBL Inhibition of [3H]pTFD-di-iPr-BnOH labelling of GABAA alpha1beta3gamma2L (unknown origin) expressed in Xenopus laevis oocytes assessed as reduction in photoincorporation at beta subunit measured after 30 mins in presence of GABA by liquid scintillation counting method B 4.49 pIC50 32000 nM IC50 Eur J Med Chem (2020) 194: 112261-112261 [PMID:32247113]
ChEMBL Inhibition of [3H]azietomidate labelling of GABAA alpha1beta3gamma2L (unknown origin) expressed in Xenopus laevis oocytes assessed as reduction in photoincorporation at M236 residues of alpha1 subunit measured after 30 mins in presence of GABA by liquid scintillation counting method B 5.1 pIC50 8000 nM IC50 Eur J Med Chem (2020) 194: 112261-112261 [PMID:32247113]
ChEMBL GABA-mimetic action on Oocytes expressing human alpha-1-beta-3-gamma-2L GABA-A receptor subunits at >=100 uM B 4.3 pEC50 50000 nM EC50 J Med Chem (2001) 44: 3582-3591 [PMID:11606122]
ChEMBL Positive allosteric modulation of GABAA alpha1beta3gamma2L in HEK cell plasma membrane assessed as increase in [3H]muscimol binding measured after 10 mins by liquid scintillation counting method B 5.27 pEC50 5400 nM EC50 Eur J Med Chem (2020) 194: 112261-112261 [PMID:32247113]
ChEMBL GABA-modulatory action compound was evaluated on Oocytes expressing recombinant human alpha-1-beta-3-gamma-2L GABA A receptor at concentrations of >=100 micro B 5.39 pEC50 4100 nM EC50 J Med Chem (2001) 44: 3582-3591 [PMID:11606122]
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 4.95 pEC50 11200 nM EC50 J Med Chem (2005) 48: 2638-2645 [PMID:15801854]
GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907607] [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14]
ChEMBL Inhibition of [35S]TBPS binding to Gamma-aminobutyric acid A receptor of rat brain membranes B 4.74 pIC50 18000 nM IC50 Bioorg Med Chem Lett (2001) 11: 927-930 [PMID:11294393]
ChEMBL In vitro inhibition of [35S]-TBPS binding to GABA-A receptor in rat whole brain membranes B 4.74 pIC50 18000 nM IC50 Bioorg Med Chem Lett (2003) 13: 1107-1110 [PMID:12643922]
ChEMBL The concentration required to inhibit 50% of binding of [35S]TBPS to Gamma-aminobutyric acid A receptor to rat whole brain membranes. B 5.08 pIC50 8300 nM IC50 J Med Chem (1997) 40: 1668-1681 [PMID:9171876]
ChEMBL Inhibition of [35S]TBPS binding to GABA-A receptor rat whole brain membranes B 5.09 pIC50 8100 nM IC50 Bioorg Med Chem Lett (2003) 13: 1971-1975 [PMID:12781176]
ChEMBL Inhibition of [35S]TBPS binding to GABA-A receptor in rat cerebral cortex. B 5.4 pIC50 3950 nM IC50 J Med Chem (1998) 41: 1846-1854 [PMID:9599235]
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.03 pKi 9316 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.03 pIC50 9393 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.46 pKi 3499 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.26 pIC50 5499 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 5.22 pKi 6051 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 4.94 pIC50 11553 nM IC50 DrugMatrix in vitro pharmacology data
TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1]
ChEMBL Inhibition of TRPV1 (unknown origin) B 8.3 pIC50 5.05 nM IC50 Eur J Med Chem (2023) 245: 114893-114893 [PMID:36395649]
HCN1 in Mouse [GtoPdb: 400] [UniProtKB: O88704]
GtoPdb - - 5.2 pIC50 - - - J Pharmacol Exp Ther (2005) 315: 517-25 [PMID:16033909];
J Physiol (Lond.) (2007) 583: 37-56 [PMID:17569731]
TRPV4 in Human [GtoPdb: 510] [UniProtKB: Q9HBA0]
GtoPdb - - 4.41 pIC50 39100 nM IC50 Front Pharmacol (2019) 10: 1150 [PMID:31636563]

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]