diazepam [Ligand Id: 3364] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL12 (Alupram 10, Alupram 2, Alupram 5, Ansiolisina, Apozepam, Atensine, Centrazepam, Diacepin, Dialar, Dialar fte, Diastat, Diastat acudial, Diazepam, Diazepam civ, Diazepam intensol, Dizac, E-Pam, LA III, LA-III, Nrl-1, NRL-1, NSC-169897, NSC-77518, Paxel, Q-pam, Relanium, RO 5-2807, RO-5-2807, RO-52807, Scriptopam, Serenack, Servizepam, Solis, Stesolid, Tensium, Tranimul, Tranquase, Valclair, Valium, Valrelease, Valtoco, Vivol, WY-3467)
  • Acetylcholinesterase in Electrophorus electricus [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
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  • Aldo-keto reductase family 1 member C1 in Human [ChEMBL: CHEMBL5905] [UniProtKB: Q04828]
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  • Aldo-keto reductase family 1 member C2 in Human [ChEMBL: CHEMBL5847] [UniProtKB: P52895]
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  • AKR1C3/Aldo-keto-reductase family 1 member C3 in Human [ChEMBL: CHEMBL4681] [GtoPdb: 1382] [UniProtKB: P42330]
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  • CCK1 receptor/Cholecystokinin A receptor in Rat [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551]
  • Cholecystokinin A receptor in Guinea pig [ChEMBL: CHEMBL3501] [UniProtKB: Q63931]
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  • fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692]
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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]
  • GABAA receptor γ2 subunit/GABAA receptor α1 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Rat [ChEMBL: CHEMBL2095167] [GtoPdb: 414, 404, 411] [UniProtKB: P18508, P62813, P63138]
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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 in Human [GtoPdb: 414, 405, 411] [UniProtKB: P18507, P47869, P47870]
  • GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-2/beta-2/gamma-2 in Rat [ChEMBL: CHEMBL2111327] [GtoPdb: 414, 405, 411] [UniProtKB: P18508, P23576, P63138]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α2 subunit/GABA-A receptor; alpha-2/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094130] [GtoPdb: 414, 412, 405] [UniProtKB: P18507, P28472, P47869]
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  • GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2111339] [GtoPdb: 414, 406, 411] [UniProtKB: P18507, P34903, P47870]
  • GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Rat [ChEMBL: CHEMBL2111343] [GtoPdb: 414, 406, 411] [UniProtKB: P18508, P20236, P63138]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α3 subunit/GABA-A receptor; alpha-3/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094120] [GtoPdb: 414, 412, 406] [UniProtKB: P18507, P28472, P34903]
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  • GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor β3 subunit/GABA A receptor alpha-5/beta-3/gamma-2 in Rat [ChEMBL: CHEMBL2111374] [GtoPdb: 414, 408, 412] [UniProtKB: P18508, P19969, P63079]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABA-A receptor; alpha-5/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094122] [GtoPdb: 414, 412, 408] [UniProtKB: P18507, P28472, P31644]
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  • GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABAA receptor α6 subunit/GABA A receptor alpha-6/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2111370] [GtoPdb: 414, 411, 409] [UniProtKB: P18507, P47870, Q16445]
  • GABAA receptor γ2 subunit/GABAA receptor α6 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-6/beta-2/gamma-2 in Rat [ChEMBL: CHEMBL2111365] [GtoPdb: 414, 409, 411] [UniProtKB: P18508, P30191, P63138]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α6 subunit/GABA-A receptor; alpha-6/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2095190] [GtoPdb: 414, 412, 409] [UniProtKB: P18507, P28472, Q16445]
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  • GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
  • GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Rat [ChEMBL: CHEMBL343] [GtoPdb: 404] [UniProtKB: P62813]
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  • GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Human [ChEMBL: CHEMBL4956] [GtoPdb: 405] [UniProtKB: P47869]
  • GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Rat [ChEMBL: CHEMBL341] [GtoPdb: 405] [UniProtKB: P23576]
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  • GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Human [ChEMBL: CHEMBL3026] [GtoPdb: 406] [UniProtKB: P34903]
  • GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Rat [ChEMBL: CHEMBL328] [GtoPdb: 406] [UniProtKB: P20236]
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  • GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644]
  • GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Rat [ChEMBL: CHEMBL300] [GtoPdb: 408] [UniProtKB: P19969]
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  • GABAA receptor γ1 subunit/GABA receptor gamma-1 subunit in Rat [ChEMBL: CHEMBL296] [GtoPdb: 413] [UniProtKB: P23574]
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  • Translocator protein/Peripheral-type benzodiazepine receptor in Rat [ChEMBL: CHEMBL4552] [GtoPdb: 2879] [UniProtKB: P16257]
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  • TRH1 receptor in Rat [GtoPdb: 363] [UniProtKB: Q01717]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
ChEMBL Inhibition of Electrophorus electricus (electric eel) acetylcholinesterase (AChE) assessed as inhibition of ATCh hydrolysis by Ellman method B 4.89 pKi 13000 nM Ki Med Chem Res (2005) 14: 297-308
Aldo-keto reductase family 1 member C1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5905] [UniProtKB: Q04828]
ChEMBL Discontinuous Radiometric Assay: Compounds may be evaluated as selective reversible inhibitors of AKR1C3 by screening them against homogeneous recombinant AKR1C1-AKR1C4 expressed in E. coli. In each case, a discontinuous radiometric assay may be used to monitor the inhibition of progesterone reduction (20-ketosteroid reduction) catalyzed by AKR1C1, the inhibition of Δ4-AD reduction (17-ketosteroid reduction) catalyzed by AKR1C3, and the inhibition of 5α-DHT reduction (3-ketosteroid reduction) catalyzed by AKR1C2 and AKR1C4 (by measuring the formation of 20α-hydroxyprogesterone, testosterone or 3α-androstanediol by radiochromatography). Secondary screens of the compounds of interest include: (a) a full-screen against all nine human recombinant AKR enzymes to ensure there are no-intended off-target effects (in this context AKR1B10 (retinal reductase; SEQ ID NO:5) has been shown to be potently inhibited by N-phenylanthranilates) (Endo et al., 2010, Biol. Pharm. Bull. 33:886-90); (b) a screen against COX-1 and COX-2 to reaffirm that compounds do not act as NSAIDs; and (c) an expanded screen against other nuclear receptors (especially other steroid hormone receptors). B 5.25 pIC50 5600 nM IC50 US-9271961-B2. Bifunctional AKR1C3 inhibitors/androgen receptor modulators and methods of use thereof (2016)
Aldo-keto reductase family 1 member C2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5847] [UniProtKB: P52895]
ChEMBL Discontinuous Radiometric Assay: Compounds may be evaluated as selective reversible inhibitors of AKR1C3 by screening them against homogeneous recombinant AKR1C1-AKR1C4 expressed in E. coli. In each case, a discontinuous radiometric assay may be used to monitor the inhibition of progesterone reduction (20-ketosteroid reduction) catalyzed by AKR1C1, the inhibition of Δ4-AD reduction (17-ketosteroid reduction) catalyzed by AKR1C3, and the inhibition of 5α-DHT reduction (3-ketosteroid reduction) catalyzed by AKR1C2 and AKR1C4 (by measuring the formation of 20α-hydroxyprogesterone, testosterone or 3α-androstanediol by radiochromatography). Secondary screens of the compounds of interest include: (a) a full-screen against all nine human recombinant AKR enzymes to ensure there are no-intended off-target effects (in this context AKR1B10 (retinal reductase; SEQ ID NO:5) has been shown to be potently inhibited by N-phenylanthranilates) (Endo et al., 2010, Biol. Pharm. Bull. 33:886-90); (b) a screen against COX-1 and COX-2 to reaffirm that compounds do not act as NSAIDs; and (c) an expanded screen against other nuclear receptors (especially other steroid hormone receptors). B 5.62 pIC50 2400 nM IC50 US-9271961-B2. Bifunctional AKR1C3 inhibitors/androgen receptor modulators and methods of use thereof (2016)
AKR1C3/Aldo-keto-reductase family 1 member C3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4681] [GtoPdb: 1382] [UniProtKB: P42330]
ChEMBL Discontinuous Radiometric Assay: Compounds may be evaluated as selective reversible inhibitors of AKR1C3 by screening them against homogeneous recombinant AKR1C1-AKR1C4 expressed in E. coli. In each case, a discontinuous radiometric assay may be used to monitor the inhibition of progesterone reduction (20-ketosteroid reduction) catalyzed by AKR1C1, the inhibition of Δ4-AD reduction (17-ketosteroid reduction) catalyzed by AKR1C3, and the inhibition of 5α-DHT reduction (3-ketosteroid reduction) catalyzed by AKR1C2 and AKR1C4 (by measuring the formation of 20α-hydroxyprogesterone, testosterone or 3α-androstanediol by radiochromatography). Secondary screens of the compounds of interest include: (a) a full-screen against all nine human recombinant AKR enzymes to ensure there are no-intended off-target effects (in this context AKR1B10 (retinal reductase; SEQ ID NO:5) has been shown to be potently inhibited by N-phenylanthranilates) (Endo et al., 2010, Biol. Pharm. Bull. 33:886-90); (b) a screen against COX-1 and COX-2 to reaffirm that compounds do not act as NSAIDs; and (c) an expanded screen against other nuclear receptors (especially other steroid hormone receptors). B 4.08 pIC50 84000 nM IC50 US-9271961-B2. Bifunctional AKR1C3 inhibitors/androgen receptor modulators and methods of use thereof (2016)
CCK1 receptor/Cholecystokinin A receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551]
ChEMBL Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue B 4 pIC50 >100000 nM IC50 J Med Chem (1988) 31: 2235-2246 [PMID:2848124]
Cholecystokinin A receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3501] [UniProtKB: Q63931]
ChEMBL Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor B 4 pIC50 >100000 nM IC50 J Med Chem (1987) 30: 1229-1239 [PMID:2885419]
Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908]
ChEMBL Inhibition of Equus caballus (horse) serum butyrylcholinesterase (BChE) assessed as inhibition of BTCh hydrolysis by Ellman method B 5.3 pKi 5011.87 nM Ki Med Chem Res (2005) 14: 297-308
ChEMBL Inhibition of Equus caballus (horse) serum butyrylcholinesterase (BChE) assessed as inhibition of BTCh hydrolysis by Ellman method B 7.37 pKi 43 nM Ki Med Chem Res (2005) 14: 297-308
fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692]
ChEMBL Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay B 6.27 pKi 531 nM Ki J Med Chem (2008) 51: 3755-3764 [PMID:18533710]
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]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α1β1γ2. - 7.79 pKi 16.3 nM Ki Science (1989) 245: 1389-92 [PMID:2551039]
ChEMBL Displacement of [3H]Flumazenil from human GABA-Aalpha1 receptor plus beta-2-gamma-2 expressed in HEK293 cells B 7.92 pKi 12 nM Ki J Med Chem (2006) 49: 2526-2533 [PMID:16610795]
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]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α1β1γ2. - 7.79 pKi 16.3 nM Ki Science (1989) 245: 1389-92 [PMID:2551039]
ChEMBL Displacement of [3H]Flunitrazepam from GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in Sf9 cells B 7.89 pKi 13 nM Ki J Med Chem (1996) 39: 158-175 [PMID:8568803]
ChEMBL Binding affinity evaluated by ability to displace [3H]Ro-151788 from recombinant human Gamma-aminobutyric acid A receptor alpha-1-beta-2-gamma-2 expressed in L(tk-)cells B 7.92 pKi 12 nM Ki Bioorg Med Chem Lett (2000) 10: 1381-1384 [PMID:10890169]
ChEMBL Allosteric modulation of GABAA alpha1beta2gamma2 (unknown origin) expressed in Xenopus oocytes assessed as potentiation of GABA-induced current response at -80 mV holding potential incubated for 3 mins by two electrode voltage clamp method B 7 pEC50 100 nM EC50 Bioorg Med Chem (2016) 24: 681-685 [PMID:26791864]
ChEMBL Binding affinity to human alpha1beta2gamma2 GABA receptor expressed in Xenopus laevis oocytes B 7.07 pEC50 85 nM EC50 Bioorg Med Chem (2010) 18: 8374-8382 [PMID:20980155]
GABAA receptor γ2 subunit/GABAA receptor α1 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095167] [GtoPdb: 414, 404, 411] [UniProtKB: P18508, P62813, P63138]
ChEMBL Binding affinity for mutant rat GABA-A receptor alpha-1-(arg)-beta-2-gamma-2 subunits expressed in HEK293 cells B 5 pKi >10000 nM Ki J Med Chem (1994) 37: 4576-4580 [PMID:7799410]
ChEMBL Binding affinity for rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells B 7.8 pKi 16 nM Ki J Med Chem (1994) 37: 4576-4580 [PMID:7799410]
ChEMBL Displacement of [3H]Ro-151788 from rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells B 7.85 pKi 14 nM Ki J Med Chem (2002) 45: 5710-5720 [PMID:12477354]
ChEMBL Binding affinity for recombinant rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells B 7.85 pKi 14 nM Ki J Med Chem (2003) 46: 310-313 [PMID:12519068]
ChEMBL Displacement of [3H]Ro15-1788 from rat recombinant GABA alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells B 7.92 pKi 12 nM Ki Bioorg Med Chem (2007) 15: 2573-2586 [PMID:17306981]
ChEMBL Displacement of [3H]flumazenil from rat GABA-A alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells B 7.96 pKi 11 nM Ki J Med Chem (2009) 52: 3723-3734 [PMID:19469479]
ChEMBL Displacement of [3H]Ro-151788 from rat recombinant GABA alpha-5-beta-2-gamma-2 receptor expressed in HEK293 cells B 8.01 pKi 9.8 nM Ki Bioorg Med Chem (2007) 15: 2573-2586 [PMID:17306981]
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]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α1β1γ2. - 7.79 pKi 16.3 nM Ki Science (1989) 245: 1389-92 [PMID:2551039]
ChEMBL Binding affinity towards human alpha-1-beta-3-gamma-2 GABA-A receptor using [3H]Ro-151788 expressed in L(tk-) cells B 7.84 pKi 14.3 nM Ki J Med Chem (2004) 47: 3642-3657 [PMID:15214791]
ChEMBL Binding affinity for human GABA-A receptor alpha-4-beta-3-gamma-2 subunits in L(tk-) cells B 7.85 pKi 14 nM Ki J Med Chem (2004) 47: 1807-1822 [PMID:15027873]
ChEMBL Displacement of [3H]Ro 15-1788 from human recombinant GABAA alpha-1-beta-3-gamma-2 receptor expressed in L(tk-) cells B 7.85 pKi 14 nM Ki J Med Chem (2005) 48: 7089-7092 [PMID:16279764]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-1-beta-3-gamma-2 B 7.85 pKi 14 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
ChEMBL Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-1-beta-3-gamma-2 subtype expressed in L (tk-) cells B 7.89 pKi 13 nM Ki J Med Chem (2005) 48: 1367-1383 [PMID:15743180]
ChEMBL Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha1 in combination with beta-3-gamma-2 expressed in L(tk-) cells B 7.89 pKi 13 nM Ki J Med Chem (2006) 49: 35-38 [PMID:16392789]
ChEMBL Displacement of [3H]Ro 15-1788 from recombinant human GABAA alpha-1 receptor plus beta3gamma2 expressed in L(tk-) cells B 7.89 pKi 13 nM Ki J Med Chem (2006) 49: 1235-1238 [PMID:16480260]
GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit in Human [GtoPdb: 414, 405, 411] [UniProtKB: P18507, P47869, P47870]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α2β1γ2. - 7.77 pKi 16.9 nM Ki Science (1989) 245: 1389-92 [PMID:2551039]
GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-2/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111327] [GtoPdb: 414, 405, 411] [UniProtKB: P18508, P23576, P63138]
ChEMBL Binding affinity for recombinant rat GABA-A receptor alpha-2-beta-2-gamma-2 subunits expressed in HEK293 cells B 7.7 pKi 20 nM Ki J Med Chem (2003) 46: 310-313 [PMID:12519068]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α2 subunit/GABA-A receptor; alpha-2/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094130] [GtoPdb: 414, 412, 405] [UniProtKB: P18507, P28472, P47869]
ChEMBL Displacement of [3H] Ro15-1788 from recombinant human GABAA alpha2 receptor plus beta-3-gamma-2 expressed in L(tk-) cells B 7.48 pKi 33 nM Ki J Med Chem (2006) 49: 1235-1238 [PMID:16480260]
ChEMBL Binding affinity towards human gamma-aminobutyric-acid A receptor alpha-2-beta-3-gamma-2 using [3H]Ro-151788 expressed in L(tk-) cells B 7.58 pKi 26.2 nM Ki J Med Chem (2004) 47: 3642-3657 [PMID:15214791]
ChEMBL Binding affinity for human GABA-A receptor alpha-2-beta-3-gamma-2 subunits in L(tk-) cells B 7.7 pKi 20 nM Ki J Med Chem (2004) 47: 1807-1822 [PMID:15027873]
ChEMBL Displacement of [3H]Ro 15-1788 from human recombinant GABAA alpha-2-beta-3-gamma-2 receptor expressed in L(tk-) cells B 7.7 pKi 20 nM Ki J Med Chem (2005) 48: 7089-7092 [PMID:16279764]
ChEMBL Binding affinity to human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-2-beta-3-gamma-2 B 7.7 pKi 20 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α2β1γ2. - 7.77 pKi 16.9 nM Ki Science (1989) 245: 1389-92 [PMID:2551039]
ChEMBL Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 subtype expressed in L (tk-) cells B 8.18 pKi 6.6 nM Ki J Med Chem (2005) 48: 1367-1383 [PMID:15743180]
ChEMBL Binding affinity evaluated by ability to displace [3H]-Ro-15-1788 from recombinant human Gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 expressed in L(tk-)cells B 8.18 pKi 6.6 nM Ki Bioorg Med Chem Lett (2000) 10: 1381-1384 [PMID:10890169]
ChEMBL Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha2 in combination with beta3gamma2 expressed in L(tk-) cells B 8.18 pKi 6.6 nM Ki J Med Chem (2006) 49: 35-38 [PMID:16392789]
ChEMBL Binding affinity to human alpha2beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes B 7.46 pEC50 35 nM EC50 Bioorg Med Chem (2010) 18: 8374-8382 [PMID:20980155]
GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111339] [GtoPdb: 414, 406, 411] [UniProtKB: P18507, P34903, P47870]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α3β1γ2. - 7.77 pKi 17 nM Ki Science (1989) 245: 1389-92 [PMID:2551039]
ChEMBL Displacement of [3H]Flumazenil from human GABA-Aalpha3 receptor plus beta-2-gamma-2 expressed in HEK293 cells B 7.85 pKi 14 nM Ki J Med Chem (2006) 49: 2526-2533 [PMID:16610795]
ChEMBL Displacement of [3H]flunitrazepam from GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in Sf9 cells B 8 pKi 10 nM Ki J Med Chem (1996) 39: 158-175 [PMID:8568803]
GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111343] [GtoPdb: 414, 406, 411] [UniProtKB: P18508, P20236, P63138]
ChEMBL Binding affinity for rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells B 7.77 pKi 17 nM Ki J Med Chem (1994) 37: 4576-4580 [PMID:7799410]
ChEMBL Binding affinity for recombinant rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells B 7.82 pKi 15 nM Ki J Med Chem (2003) 46: 310-313 [PMID:12519068]
ChEMBL Displacement of [3H]Ro15-1788 from rat recombinant GABA alpha-3-beta-2-gamma-2 receptor expressed in HEK293 cells B 7.85 pKi 14 nM Ki Bioorg Med Chem (2007) 15: 2573-2586 [PMID:17306981]
ChEMBL Displacement of [3H]Ro-151788 from rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells B 7.86 pKi 13.9 nM Ki J Med Chem (2002) 45: 5710-5720 [PMID:12477354]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α3 subunit/GABA-A receptor; alpha-3/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094120] [GtoPdb: 414, 412, 406] [UniProtKB: P18507, P28472, P34903]
ChEMBL Binding affinity evaluated by ability to displace [3H]Ro-151788 from recombinant human Gamma-aminobutyric acid A receptor alpha-3-beta-3-gamma-2 expressed in L(tk-)cells B 7.48 pKi 33 nM Ki Bioorg Med Chem Lett (2000) 10: 1381-1384 [PMID:10890169]
ChEMBL Displacement of [3H]Ro-151788 from human recombinant GABAA alpha3 in combination with beta3gamma2 expressed in L(tk-) cells B 7.48 pKi 33 nM Ki J Med Chem (2006) 49: 35-38 [PMID:16392789]
ChEMBL Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-3-beta-3-gamma-2 subtype expressed in L (tk-) cells B 7.48 pKi 33 nM Ki J Med Chem (2005) 48: 1367-1383 [PMID:15743180]
ChEMBL Binding affinity towards human gamma-aminobutyric-acid A receptor alpha-3-beta-3-gamma-2 using [3H]Ro-151788 expressed in L(tk-) cells B 7.63 pKi 23.7 nM Ki J Med Chem (2004) 47: 3642-3657 [PMID:15214791]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α3β1γ2. - 7.77 pKi 17 nM Ki Science (1989) 245: 1389-92 [PMID:2551039]
ChEMBL Binding affinity for human GABA-A receptor alpha-3-beta-3-gamma-2 subunits in L(tk-) cells B 7.82 pKi 15 nM Ki J Med Chem (2004) 47: 1807-1822 [PMID:15027873]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-3-beta-3-gamma-2 B 7.82 pKi 15 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
ChEMBL Displacement of [3H]Ro 15-1788 from human recombinant GABAA alpha-3-beta-3-gamma-2 receptor expressed in L(tk-) cells B 7.82 pKi 15 nM Ki J Med Chem (2005) 48: 7089-7092 [PMID:16279764]
ChEMBL Binding affinity to human alpha3beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes B 6.88 pEC50 131 nM EC50 Bioorg Med Chem (2010) 18: 8374-8382 [PMID:20980155]
GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor β3 subunit/GABA A receptor alpha-5/beta-3/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111374] [GtoPdb: 414, 408, 412] [UniProtKB: P18508, P19969, P63079]
ChEMBL Binding affinity for recombinant rat GABA-A receptor alpha-5-beta-3-gamma-2 subunits expressed in HEK 293 cells B 7.96 pKi 11 nM Ki J Med Chem (2003) 46: 310-313 [PMID:12519068]
ChEMBL Displacement of [3H]flumazenil from rat GABA-A alpha-5-beta-3-gamma-2 receptor expressed in HEK293 cells B 8.01 pKi 9.8 nM Ki J Med Chem (2009) 52: 3723-3734 [PMID:19469479]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABA-A receptor; alpha-5/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094122] [GtoPdb: 414, 412, 408] [UniProtKB: P18507, P28472, P31644]
ChEMBL Binding affinity towards human alpha-5-beta-3-gamma-2 GABA-A receptor using [3H]Ro-151788 expressed in L(tk-) cells B 7.95 pKi 11.2 nM Ki J Med Chem (2004) 47: 3642-3657 [PMID:15214791]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-5-beta-3-gamma-2 B 7.96 pKi 11 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity for human GABA-A receptor alpha-5-beta-3-gamma-2 subunits in L(tk-) cells B 7.96 pKi 11 nM Ki J Med Chem (2004) 47: 1807-1822 [PMID:15027873]
ChEMBL Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-5-beta-3-gamma-2 subtype expressed in L (tk-) cells B 7.96 pKi 11 nM Ki J Med Chem (2005) 48: 1367-1383 [PMID:15743180]
ChEMBL Displacement of [3H]Ro-151788 from human recombinant GABAA alpha5 in combination with beta3gamma2 expressed in L(tk-) cells B 7.96 pKi 11 nM Ki J Med Chem (2006) 49: 35-38 [PMID:16392789]
ChEMBL Binding affinity to human recombinant GABAA alpha5beta3gamma2 expressed in Xenopus laevis oocytes by patch clamp technique B 7.77 pIC50 17 nM IC50 J Med Chem (2013) 56: 593-624 [PMID:23121096]
ChEMBL Binding affinity to human alpha5beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes B 7.35 pEC50 45 nM EC50 Bioorg Med Chem (2010) 18: 8374-8382 [PMID:20980155]
GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABAA receptor α6 subunit/GABA A receptor alpha-6/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111370] [GtoPdb: 414, 411, 409] [UniProtKB: P18507, P47870, Q16445]
ChEMBL Displacement of [3H]-Ro-15-4513 from GABA-A receptor alpha-6-beta-2-gamma-2 subunits expressed in Sf9 cells B 5.15 pKi >7000 nM Ki J Med Chem (1996) 39: 158-175 [PMID:8568803]
ChEMBL Displacement of [3H]-Ro- 15-4513 from alpha-6-beta-2-gamma-2 GABA-A receptor subunits expressed in Sf9 cell membranes B 5.15 pKi >7000 nM Ki J Med Chem (1994) 37: 758-768 [PMID:8145225]
GABAA receptor γ2 subunit/GABAA receptor α6 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-6/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111365] [GtoPdb: 414, 409, 411] [UniProtKB: P18508, P30191, P63138]
ChEMBL Binding affinity for rat GABA-A receptor alpha-6-beta-2-gamma-2 subunits expressed in HEK293 cells B 5 pKi >10000 nM Ki J Med Chem (1994) 37: 4576-4580 [PMID:7799410]
ChEMBL Displacement of [3H]-Ro- 15-4513 from alpha-6 beta2 gamma2 subunits of Rat GABA-A receptor expressed in Sf-9 insect cell membranes B 5.15 pKi >7000 nM Ki J Med Chem (1996) 39: 4654-4666 [PMID:8917654]
ChEMBL Binding affinity for mutant rat GABA-A receptor alpha-6-(his)-beta-2-gamma-2 subunits expressed in HEK293 cells B 7.01 pKi 98 nM Ki J Med Chem (1994) 37: 4576-4580 [PMID:7799410]
ChEMBL Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr)beta2gamma2 subunits expressed in HEK293 cells B 7.7 pKi 20 nM Ki J Med Chem (1994) 37: 4576-4580 [PMID:7799410]
ChEMBL Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr,gly)beta2gamma2 subunits expressed in HEK293 cells B 8.05 pKi 9 nM Ki J Med Chem (1994) 37: 4576-4580 [PMID:7799410]
ChEMBL Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr,gly,val)beta2gamma2 subunits expressed in HEK293 cells B 8.68 pKi 2.1 nM Ki J Med Chem (1994) 37: 4576-4580 [PMID:7799410]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α6 subunit/GABA-A receptor; alpha-6/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095190] [GtoPdb: 414, 412, 409] [UniProtKB: P18507, P28472, Q16445]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-6-beta-3-gamma-2 B 5.52 pKi >3000 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
GABAA receptor π subunit/GABAA receptor δ subunit/GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 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 ε subunit/GABAA receptor α6 subunit/GABAA receptor γ1 subunit/GABAA receptor γ3 subunit/GABAA receptor θ subunit/GABA-A receptor; anion channel in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093872] [GtoPdb: 419, 416, 404, 410, 414, 412, 408, 406, 405, 411, 407, 417, 409, 413, 415, 418] [UniProtKB: O00591, O14764, P14867, P18505, P18507, P28472, P31644, P34903, P47869, P47870, P48169, P78334, Q16445, Q8N1C3, Q99928, Q9UN88]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α2β1γ2. - 7.77 pKi 16.9 nM Ki Science (1989) 245: 1389-92 [PMID:2551039]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α3β1γ2. - 7.77 pKi 17 nM Ki Science (1989) 245: 1389-92 [PMID:2551039]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α1β1γ2. - 7.79 pKi 16.3 nM Ki Science (1989) 245: 1389-92 [PMID:2551039]
ChEMBL Binding affinity towards Benzodiazepine receptor from bovine brain membrane using [3H]Ro-151788 as radioligand B 8 pKi 10 nM Ki J Med Chem (2002) 45: 5710-5720 [PMID:12477354]
ChEMBL Displacement of [3H]flumazenil from bovine benzodiazepine receptor GABA-A channel of brain membranes B 8 pKi 10 nM Ki J Med Chem (2005) 48: 2936-2943 [PMID:15828832]
ChEMBL Displacement of [35S]TBPS from GABA-A receptor complex at low umolar concentration B 4.13 pIC50 74000 nM IC50 Bioorg Med Chem Lett (1993) 3: 1941-1946
ChEMBL Binding affinity to the benzodiazepine receptor assayed using 0.5 nM [3H]flunitrazapam as radioligand in guinea pig cerebellum B 7.85 pIC50 -7.85 nM Log IC50 Bioorg Med Chem Lett (1995) 5: 2397-2402
ChEMBL Binding affinity to the benzodiazepine receptor assayed using 0.5 nM [3H]flunitrazapam as radioligand in guinea pig cerebellum B 7.85 pIC50 14.1 nM IC50 Bioorg Med Chem Lett (1995) 5: 2397-2402
ChEMBL In vitro displacement of [3H]flunitrazepam from GABA-A central benzodiazepine receptor of guinea pig cerebellum B 7.85 pIC50 14 nM IC50 Bioorg Med Chem Lett (1995) 5: 2391-2396
ChEMBL Percent inhibition against central Benzodiazepine receptor at 1 uM B 7.92 pIC50 12 nM IC50 J Med Chem (2005) 48: 6887-6896 [PMID:16250647]
ChEMBL In vitro displacement of [3H]-diazepam from GABA-A Benzodiazepine receptor B 8.09 pIC50 8.1 nM IC50 J Med Chem (1982) 25: 1050-1055 [PMID:6127410]
GABA-A receptor; anion channel in Bovine (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094107] [UniProtKB: P08219, P08220, P10063, P10064, P20237, P22300]
ChEMBL Displacement of [3H]Ro-151788 from GABA-A benzodiazepine receptor of bovine brain membranes B 8 pKi 10 nM Ki J Med Chem (1999) 42: 2218-2226 [PMID:10377227]
ChEMBL Inhibition of [3H]Ro-151788 binding to GABA-A central benzodiazepine receptor of bovine brain membranes B 8 pKi 10 nM Ki J Med Chem (2003) 46: 310-313 [PMID:12519068]
ChEMBL In vitro inhibition of [3H]flunitrazepam binding to GABA-A benzodiazepine receptor of bovine cerebral cortical membranes at 10 uM B 8 pKi 10 nM Ki J Med Chem (1992) 35: 2214-2220 [PMID:1319492]
ChEMBL Displacement of [3H]flumazenil from GABA-A receptor in bovine brain membranes B 8 pKi 10 nM Ki J Med Chem (2006) 49: 2489-2495 [PMID:16610792]
ChEMBL Inhibition of [3H]flunitrazepam binding to GABA-A central Benzodiazepine receptor of bovine brain membranes B 7.39 pIC50 41 nM IC50 J Med Chem (1985) 28: 506-509 [PMID:2984422]
ChEMBL Inhibition of [3H]flunitrazepam binding to benzodiazepine receptor in bovine brain membrane B 7.6 pIC50 25 nM IC50 J Med Chem (1988) 31: 1-3 [PMID:2826782]
ChEMBL Affinity to displace [3H]flunitrazepam from Benzodiazepine receptor in bovine brain membrane B 7.89 pIC50 13 nM IC50 J Med Chem (1990) 33: 2646-2651 [PMID:2167984]
GABAA receptor α6 subunit/GABAA receptor γ2 subunit/GABAA receptor δ subunit/GABAA receptor α2 subunit/GABAA receptor α3 subunit/GABAA receptor γ3 subunit/GABAA receptor β1 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor π subunit/GABAA receptor α4 subunit/GABAA receptor θ subunit/GABAA receptor γ1 subunit/GABA-A receptor; anion channel in Mouse (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094133] [GtoPdb: 409, 414, 416, 405, 406, 415, 410, 404, 412, 408, 419, 407, 418, 413] [UniProtKB: A2AMW3, P16305, P22723, P22933, P26048, P26049, P27681, P50571, P62812, P63080, Q8BHJ7, Q8QZW7, Q9D6F4, Q9JLF1, Q9R0Y8]
ChEMBL Binding affinity for umolar GABA-A central benzodiazepine receptor B 4.07 pKi 85000 nM Ki J Med Chem (1984) 27: 772-778 [PMID:6330354]
ChEMBL Displacement of [3H]flunitrazepam from GABA-A central benzodiazepine receptor of mouse brain B 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (1993) 3: 1941-1946
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 [3H]diazepam binding to GABA-A central benzodiazepine receptor of rat brain homogenate B 6.49 pKi 323 nM Ki J Med Chem (1988) 31: 1115-1123 [PMID:2836588]
ChEMBL Inhibition of [3H]diazepam binding to GABA-A central benzodiazepine receptor of rat brain homogenate B 6.84 pKi 144 nM Ki J Med Chem (1988) 31: 1115-1123 [PMID:2836588]
ChEMBL Displacement of [3H]flunitrazepam from GABA-A Benzodiazepine receptor of rat brain membranes B 7.85 pKi 14 nM Ki J Med Chem (1990) 33: 2640-2645 [PMID:1975276]
ChEMBL Binding affinity to rat benzodiazepine receptor B 7.85 pKi 14 nM Ki Bioorg Med Chem Lett (2002) 12: 3215-3218 [PMID:12372537]
ChEMBL Displacement of [3H]flunitrazepam at GABA-A benzodiazepine receptor in rat brain cortical membranes B 7.98 pKi 10.5 nM Ki J Med Chem (1996) 39: 2915-2921 [PMID:8709126]
ChEMBL In vitro affinity against Benzodiazepine receptor binding to rat cortical membranes (using [3H]- flumazenil as radioligand). B 8.07 pKi 8.5 nM Ki J Med Chem (1999) 42: 4343-4350 [PMID:10543878]
ChEMBL Inhibition of [3H]flunitrazepam [3H]FNZ) binding to GABA-A Benzodiazepine receptor of synaptosomal membranes from rat brain B 8.15 pKi ~7 nM Ki Bioorg Med Chem Lett (1997) 7: 373-378
ChEMBL Binding affinity to Wistar rat benzodiazepine receptor B 8.17 pKi 6.8 nM Ki J Med Chem (2006) 49: 1855-1866 [PMID:16539371]
ChEMBL Binding affinity for Diazepam-Sensitive fraction of GABA-A benzodiazepine receptors B 8.18 pKi 6.6 nM Ki J Med Chem (1993) 36: 1001-1006 [PMID:8386769]
ChEMBL Displacement of [3H]- flunitrazepam from rat GABA-A benzodiazepine receptor B 8.22 pKi 6 nM Ki J Med Chem (1994) 37: 758-768 [PMID:8145225]
ChEMBL Displacement of [3H]-diazepam from GABA-A benzodiazepine receptor of rat cerebral cortex B 8.3 pKi 5.02 nM Ki J Med Chem (1987) 30: 454-455 [PMID:3029371]
ChEMBL Binding affinity against benzodiazepine (BZ) receptor by displacing [3H]diazepam in cerebral cortex of Wistar rats B 8.3 pKi 5.02 nM Ki J Med Chem (1988) 31: 1738-1745 [PMID:2842502]
ChEMBL Displacing potential to [3H]diazepam binding to benzodiazepine receptor in Wistar rat cerebral cortex B 8.3 pKi 5.02 nM Ki J Med Chem (1989) 32: 1213-1217 [PMID:2542554]
ChEMBL In vitro inhibition of [3H]diazepam binding to benzodiazepine receptor in rat cerebral cortical membrane B 8.3 pKi 5 nM Ki J Med Chem (1982) 25: 1081-1091 [PMID:6127411]
ChEMBL Displacement of [3H]diazepam from rat cerebral cortex benzodiazepine receptor B 8.3 pKi 5 nM Ki J Med Chem (1996) 39: 2844-2851 [PMID:8709114]
ChEMBL Binding affinity against benzodiazepine receptor (BzR) in rat cortical membranes determined by competition experiments with radiolabeled [3H]flunitrazepam (Fnz) B 8.31 pKi 4.9 nM Ki J Med Chem (1996) 39: 3820-3836 [PMID:8809170]
ChEMBL Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor of rat cortical membranes B 8.31 pKi 4.9 nM Ki J Med Chem (1999) 42: 1123-1144 [PMID:10197957]
ChEMBL Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor of rat cortical membranes B 8.31 pKi 4.9 nM Ki J Med Chem (1996) 39: 4654-4666 [PMID:8917654]
ChEMBL Inhibition of [3H]flunitrazepam binding to GABA-A receptor of rat cortical membranes B 8.31 pKi 4.9 nM Ki J Med Chem (1996) 39: 158-175 [PMID:8568803]
ChEMBL In vitro binding affinity against benzodiazepine receptor using [3H]diazepam as radioligand B 8.54 pKi 2.9 nM Ki J Med Chem (1985) 28: 1314-1319 [PMID:2993620]
ChEMBL Inhibition of [3H]diazepam binding to GABA-A central benzodiazepine receptor of rat brain homogenate B 8.54 pKi 2.9 nM Ki J Med Chem (1988) 31: 1115-1123 [PMID:2836588]
ChEMBL Inhibition of Diazepam-Insensitive fraction of GABA-A benzodiazepine receptors B 6 pIC50 >1000 nM IC50 J Med Chem (1993) 36: 1001-1006 [PMID:8386769]
ChEMBL Ability to allosterically modulate the binding of [35S]TBPS to gamma-aminobutyric-acid A receptor in rat brain cortical P2 membranes. B 7.04 pIC50 91 nM IC50 J Med Chem (1997) 40: 61-72 [PMID:9016329]
ChEMBL Inhibition of radiolabeled antagonist [3H]-Ro- 15-1788 binding to benzodiazepine receptor from rat cortical membranes B 7.11 pIC50 77 nM IC50 J Med Chem (1989) 32: 2282-2291 [PMID:2552115]
ChEMBL Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor in synaptic membranes of rat cerebral cortex B 7.52 pIC50 30 nM IC50 J Med Chem (1985) 28: 683-685 [PMID:2985787]
ChEMBL Binding affinity against the BZD site of the Gamma-aminobutyric acid A receptor in rat cerebral cortex using radioligand ([3H]flunitrazepam) assay in the absence of Gamma-aminobutyric acid B 7.55 pIC50 28 nM IC50 Bioorg Med Chem Lett (1996) 6: 333-338
ChEMBL Binding affinity against benzodiazepine site of gamma-aminobutyric-acid A receptor of rat cerebral cortex by using [3H]flunitrazepam in the absence of GABA. B 7.55 pIC50 28 nM IC50 J Med Chem (1995) 38: 16-20 [PMID:7837226]
ChEMBL Agonistic activity against specific binding of radioligand [3H]Ro-151788 to GABA-A Benzodiazepine receptor in rat cortex B 7.69 pIC50 20.6 nM IC50 J Med Chem (1993) 36: 1669-1673 [PMID:8388472]
ChEMBL Inhibition of [3H]-Ro- 15-1788 binding to GABA-A benzodiazepine receptor in rat brain membrane B 7.69 pIC50 20.6 nM IC50 J Med Chem (1995) 38: 950-957 [PMID:7699711]
ChEMBL Displacement of [3H]flunitrazepam from GABA-A receptor of rat cerebellar tissue B 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2000) 10: 2579-2583 [PMID:11086734]
ChEMBL Displacement of [3H]flunitrazepam from GABA-A receptor of rat forebrain tissue B 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2000) 10: 2579-2583 [PMID:11086734]
ChEMBL Inhibition of [3H]flunitrazepam binding to GABA-A Benzodiazepine receptor of Wistar rat cerebral cortex B 7.81 pIC50 15.4 nM IC50 J Med Chem (1990) 33: 3110-3116 [PMID:1977911]
ChEMBL Binding affinity against benzodiazepine site of gamma-aminobutyric-acid A receptor of rat cerebral cortex by using [3H]flunitrazepam in the presence of GABA 1 mM. B 7.89 pIC50 13 nM IC50 J Med Chem (1995) 38: 16-20 [PMID:7837226]
ChEMBL Binding affinity against the BZD site of the Gamma-aminobutyric acid A receptor in rat cerebral cortex using radioligand ([3H]flunitrazepam) assay in the presence of Gamma-aminobutyric acid B 7.89 pIC50 13 nM IC50 Bioorg Med Chem Lett (1996) 6: 333-338
ChEMBL In vitro binding affinity for GABA-A receptor in rat cortical or hippocampal membranes using [3H]flunitrazepam B 7.92 pIC50 12 nM IC50 J Med Chem (1990) 33: 2772-2777 [PMID:2170646]
ChEMBL Inhibition of [3H]flunitrazepam binding to GABA-A benzodiazepine receptor of rat cerebellum B 8.03 pIC50 9.3 nM IC50 J Med Chem (1989) 32: 2561-2573 [PMID:2573731]
ChEMBL In vitro inhibitory concentration of compound against benzodiazepine receptor from rat cerebral cortex using [3H]- flunitrazepam was evaluated B 8.09 pIC50 8.1 nM IC50 J Med Chem (1994) 37: 745-757 [PMID:8145224]
ChEMBL Inhibition of [3H]flunitrazepam binding to GABA-A benzodiazepine receptor of rat cortex B 8.14 pIC50 7.3 nM IC50 J Med Chem (1989) 32: 2561-2573 [PMID:2573731]
ChEMBL Inhibition of [3H]diazepam binding to GABA-A benzodiazepine receptor of rat brain B 8.15 pIC50 7 nM IC50 J Med Chem (1988) 31: 2235-2246 [PMID:2848124]
ChEMBL Displacement of [3H]flunitrazepam from benzodiazepine receptor of rat cerebral cortex membranes B 8.15 pIC50 7 nM IC50 J Med Chem (1991) 34: 2993-3006 [PMID:1681105]
ChEMBL Displacement of [3H]diazepam from rat brain GABA-A benzodiazepine receptor B 8.15 pIC50 7 nM IC50 J Med Chem (1987) 30: 1229-1239 [PMID:2885419]
ChEMBL In vitro inhibition of binding to the benzodiazepine receptor in rat cerebral cortical membrane using [3H]diazepam as radioligand B 8.22 pIC50 6 nM IC50 J Med Chem (1988) 31: 1854-1861 [PMID:2842507]
ChEMBL Effect on [3H]flunitrazepam binding to Benzodiazepine receptor B 8.22 pIC50 6 nM IC50 J Med Chem (1991) 34: 1754-1756 [PMID:1674542]
ChEMBL Inhibitory concentration against specific binding of [3H]diazepam to Benzodiazepine receptor in rat brain B 8.22 pIC50 6 nM IC50 J Med Chem (1990) 33: 1910-1914 [PMID:2163452]
ChEMBL Inhibition of specific binding of 1.5 nM [3H]diazepam to rat brain benzodiazepine receptors B 8.22 pIC50 6 nM IC50 J Med Chem (1990) 33: 196-202 [PMID:1967311]
ChEMBL Inhibition of [3H]flunitrazepam binding to GABA-A benzodiazepine receptor of rat cerebral cortex B 8.22 pIC50 6 nM IC50 J Med Chem (1989) 32: 2561-2573 [PMID:2573731]
ChEMBL Concentration that inhibits binding of 1.5 nM [3H]diazepam to rat brain benzodiazepine receptor B 8.22 pIC50 6 nM IC50 J Med Chem (1989) 32: 1020-1024 [PMID:2540330]
ChEMBL In vitro inhibitory concentration of compound against benzodiazepine receptor from rat cerebral cortex using [3H]- flunitrazepam was evaluated B 8.22 pIC50 6 nM IC50 J Med Chem (1994) 37: 745-757 [PMID:8145224]
ChEMBL In vitro for inhibition of [3H]diazepam towards Benzodiazepine receptor from rat B 8.22 pIC50 6 nM IC50 J Med Chem (1981) 24: 592-600 [PMID:6113284]
ChEMBL Binding affinity against central benzodiazepine receptor(CBR). B 8.25 pIC50 5.6 nM IC50 J Med Chem (1996) 39: 4275-4284 [PMID:8863805]
ChEMBL Displacement of [3H]diazepam binding in rat brain membranes B 8.27 pIC50 5.4 nM IC50 J Med Chem (1983) 26: 1596-1601 [PMID:6138437]
ChEMBL In vitro inhibition of [3H]diazepam binding to rat GABA-A benzodiazepine receptor B 8.27 pIC50 5.4 nM IC50 J Med Chem (1983) 26: 367-372 [PMID:6681844]
ChEMBL Binding affinity measured by [3H]diazepam binding assay in rat B 8.27 pIC50 5.4 nM IC50 J Med Chem (1983) 26: 1589-1596 [PMID:6138436]
ChEMBL In vitro displacement of [3H]diazepam from GABA-A benzodiazepine receptor B 8.3 pIC50 5 nM IC50 J Med Chem (1983) 26: 100-103 [PMID:6131127]
ChEMBL In vitro inhibition of binding to GABA-A central benzodiazepine-receptor of rat brain B 8.3 pIC50 5 nM IC50 J Med Chem (1982) 25: 337-339 [PMID:6121916]
ChEMBL In vitro inhibitory against Gamma-aminobutyric acid A receptor from rat cerebral cortex using [3H]flunitrazepam as the radioligand B 8.31 pIC50 4.9 nM IC50 Bioorg Med Chem Lett (1999) 9: 1547-1552 [PMID:10386933]
ChEMBL In vitro affinity for BZD site on GABA-A receptor from rat cerebral cortex using radioligand [3H]flunitrazepam B 8.31 pIC50 4.9 nM IC50 Bioorg Med Chem Lett (2002) 12: 2381-2386 [PMID:12161138]
ChEMBL Displacement of [3H]flunitrazepam from GABA-A Benzodiazepine receptors in rat forebrain B 8.36 pIC50 4.4 nM IC50 J Med Chem (1991) 34: 2899-2906 [PMID:1680197]
ChEMBL Displacement of [3H]diazepam from GABA-A Benzodiazepine receptor of rat forebrain B 8.4 pIC50 4 nM IC50 J Med Chem (1991) 34: 281-290 [PMID:1846920]
GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
ChEMBL Binding affinity to GABAA alpha-1-beta-2-gamma-2 receptor B 7.44 pKd 36 nM Kd J Med Chem (2008) 51: 3788-3803 [PMID:18537233]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α1β1γ2. - 7.79 pKi 16.3 nM Ki Science (1989) 245: 1389-92 [PMID:2551039]
ChEMBL Binding affinity to GABA-A alpha1 (unknown origin) B 7.8 pKi 16 nM Ki J Med Chem (2020) 63: 3425-3446 [PMID:31738537]
GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL343] [GtoPdb: 404] [UniProtKB: P62813]
ChEMBL Displacement of [3H]RO15-1788 from recombinant rat GABAalpha1 receptor expressed in HEK293 cells after 1 hr B 7.85 pKi 14 nM Ki Eur J Med Chem (2017) 126: 298-352 [PMID:27894044]
GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4956] [GtoPdb: 405] [UniProtKB: P47869]
ChEMBL Binding affinity to GABA-A alpha2 (unknown origin) B 7.77 pKi 17 nM Ki J Med Chem (2020) 63: 3425-3446 [PMID:31738537]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α2β1γ2. - 7.77 pKi 16.9 nM Ki Science (1989) 245: 1389-92 [PMID:2551039]
GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL341] [GtoPdb: 405] [UniProtKB: P23576]
ChEMBL Displacement of [3H]RO15-1788 from recombinant rat GABAalpha2 receptor expressed in HEK293 cells after 1 hr B 7.7 pKi 20 nM Ki Eur J Med Chem (2017) 126: 298-352 [PMID:27894044]
ChEMBL Displacement of [3H]flumazenil from rat GABA-A alpha-2-beta-2-gamma-2 receptor expressed in HEK293 cells B 7.82 pKi 15 nM Ki J Med Chem (2009) 52: 3723-3734 [PMID:19469479]
GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3026] [GtoPdb: 406] [UniProtKB: P34903]
ChEMBL Binding affinity to GABA-A alpha3 (unknown origin) B 7.77 pKi 17 nM Ki J Med Chem (2020) 63: 3425-3446 [PMID:31738537]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α3β1γ2. - 7.77 pKi 17 nM Ki Science (1989) 245: 1389-92 [PMID:2551039]
GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL328] [GtoPdb: 406] [UniProtKB: P20236]
ChEMBL Displacement of [3H]RO15-1788 from recombinant rat GABAalpha3 receptor expressed in HEK293 cells after 1 hr B 7.82 pKi 15 nM Ki Eur J Med Chem (2017) 126: 298-352 [PMID:27894044]
GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644]
ChEMBL Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptor B 7.64 pKd 23 nM Kd J Med Chem (2008) 51: 3788-3803 [PMID:18537233]
ChEMBL Binding affinity to GABA-A alpha5 (unknown origin) B 7.82 pKi 15 nM Ki J Med Chem (2020) 63: 3425-3446 [PMID:31738537]
GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL300] [GtoPdb: 408] [UniProtKB: P19969]
ChEMBL Displacement of [3H]RO15-1788 from recombinant rat GABAalpha5 receptor expressed in HEK293 cells after 1 hr B 7.96 pKi 11 nM Ki Eur J Med Chem (2017) 126: 298-352 [PMID:27894044]
GABAA receptor γ1 subunit/GABA receptor gamma-1 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL296] [GtoPdb: 413] [UniProtKB: P23574]
ChEMBL Anxiolytic activity by displacement of [3H]diazepam from GABA-A receptor in rat synaptosomal membranes F 8.3 pIC50 5 nM IC50 J Med Chem (1980) 23: 952-955 [PMID:6105221]
Translocator protein/Peripheral-type benzodiazepine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4552] [GtoPdb: 2879] [UniProtKB: P16257]
ChEMBL Binding affinity constant for peripheral (mitochondrial) Benzodiazepine receptor B 6.67 pKd 213 nM Kd J Med Chem (1995) 38: 4730-4738 [PMID:7473601]
ChEMBL Displacement of [3H]PK11195 from PBR in rat kidney mitochondrial membrane B 6.24 pKi 574 nM Ki Bioorg Med Chem (2008) 16: 6145-6155 [PMID:18472268]
ChEMBL Displacement of [3H]PK11195 from TSPO receptor in Sprague-Dawley rat cerebral cortex membrane by radiometric competitive assay B 6.71 pIC50 194 nM IC50 Eur J Med Chem (2015) 103: 210-222 [PMID:26355532]
TRH1 receptor in Rat [GtoPdb: 363] [UniProtKB: Q01717]
GtoPdb - - 5.15 pKi 7100 nM Ki Ann N Y Acad Sci (1989) 553: 197-204 [PMID:2566295]

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]