DIAZEPAM

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Trade Names
Synonyms
Status
Molecule Category Free-form
ATC N05BA01
UNII Q3JTX2Q7TU
EPA CompTox DTXSID4020406

Structure

InChI Key AAOVKJBEBIDNHE-UHFFFAOYSA-N
Smiles CN1C(=O)CN=C(c2ccccc2)c2cc(Cl)ccc21
InChI
InChI=1S/C16H13ClN2O/c1-19-14-8-7-12(17)9-13(14)16(18-10-15(19)20)11-5-3-2-4-6-11/h2-9H,10H2,1H3

Physicochemical Descriptors

Property Name Value
Molecular Formula C16H13ClN2O
Molecular Weight 284.75
AlogP 3.15
Hydrogen Bond Acceptor 2.0
Hydrogen Bond Donor 0.0
Number of Rotational Bond 1.0
Polar Surface Area 32.67
Molecular species NEUTRAL
Aromatic Rings 2.0
Heavy Atoms 20.0

Bioactivity

Mechanism of Action Action Reference
GABA-A receptor; anion channel positive allosteric modulator POSITIVE ALLOSTERIC MODULATOR PubMed PubMed Wikipedia Wikipedia
Protein: GABA-A receptor; anion channel
Description: Gamma-aminobutyric acid receptor subunit pi
Organism : Homo sapiens
O00591 ENSG00000094755
Protein: GABA-A receptor; anion channel
Description: Gamma-aminobutyric acid receptor subunit delta
Organism : Homo sapiens
O14764 ENSG00000187730
Protein: GABA-A receptor; anion channel
Description: Gamma-aminobutyric acid receptor subunit alpha-1
Organism : Homo sapiens
P14867 ENSG00000022355
Protein: GABA-A receptor; anion channel
Description: Gamma-aminobutyric acid receptor subunit beta-1
Organism : Homo sapiens
P18505 ENSG00000163288
Protein: GABA-A receptor; anion channel
Description: Gamma-aminobutyric acid receptor subunit gamma-2
Organism : Homo sapiens
P18507 ENSG00000113327
Protein: GABA-A receptor; anion channel
Description: Gamma-aminobutyric acid receptor subunit beta-3
Organism : Homo sapiens
P28472 ENSG00000166206
Protein: GABA-A receptor; anion channel
Description: Gamma-aminobutyric acid receptor subunit alpha-5
Organism : Homo sapiens
P31644 ENSG00000186297
Protein: GABA-A receptor; anion channel
Description: Gamma-aminobutyric acid receptor subunit alpha-3
Organism : Homo sapiens
P34903 ENSG00000011677
Protein: GABA-A receptor; anion channel
Description: Gamma-aminobutyric acid receptor subunit alpha-2
Organism : Homo sapiens
P47869 ENSG00000151834
Protein: GABA-A receptor; anion channel
Description: Gamma-aminobutyric acid receptor subunit beta-2
Organism : Homo sapiens
P47870 ENSG00000145864
Protein: GABA-A receptor; anion channel
Description: Gamma-aminobutyric acid receptor subunit alpha-4
Organism : Homo sapiens
P48169 ENSG00000109158
Protein: GABA-A receptor; anion channel
Description: Gamma-aminobutyric acid receptor subunit epsilon
Organism : Homo sapiens
P78334 ENSG00000102287
Protein: GABA-A receptor; anion channel
Description: Gamma-aminobutyric acid receptor subunit alpha-6
Organism : Homo sapiens
Q16445 ENSG00000145863
Protein: GABA-A receptor; anion channel
Description: Gamma-aminobutyric acid receptor subunit gamma-1
Organism : Homo sapiens
Q8N1C3 ENSG00000163285
Protein: GABA-A receptor; anion channel
Description: Gamma-aminobutyric acid receptor subunit gamma-3
Organism : Homo sapiens
Q99928 ENSG00000182256
Protein: GABA-A receptor; anion channel
Description: Gamma-aminobutyric acid receptor subunit theta
Organism : Homo sapiens
Q9UN88 ENSG00000268089
Targets EC50(nM) IC50(nM) Kd(nM) Ki(nM) Inhibition(%)
Auxiliary transport protein Fatty acid binding protein family
- - - 531 -
Enzyme Hydrolase
- - - 43-5012 -
Enzyme Oxidoreductase
- - - - 23
Epigenetic regulator Reader Bromodomain
- - - - 43
Ion channel Ligand-gated ion channel GABA-A receptor
85-100 4-91 23 3-323 100
Ion channel Voltage-gated ion channel Voltage-gated calcium channel
- 30500 - - -
Ion channel Voltage-gated ion channel Voltage-gated sodium channel
- - - - 15-45
Membrane receptor
- 194 213 574 0-97
Secreted protein
- - 15100 - -
Transporter Electrochemical transporter SLC superfamily of solute carriers SLC21/SLCO family of organic anion transporting polypeptides
- - - - 51
Transporter Electrochemical transporter SLC superfamily of solute carriers SLC22 family of organic cation and anion transporters
- - - - 5
Assay Description Organism Bioactivity Reference
Inhibition of [3H]-Ro- 15-1788 binding to GABA-A benzodiazepine receptor in rat brain membrane Rattus norvegicus 20.6 nM
Inhibition of [3H]Flunitrazepam binding to rat cerebral cortex at 0.12 uM Rattus norvegicus 100.0 %
Binding affinity constant for peripheral (mitochondrial) Benzodiazepine receptor Rattus norvegicus 213.0 nM
Binding affinity against benzodiazepine receptor (BzR) in rat cortical membranes determined by competition experiments with radiolabeled [3H]flunitrazepam (Fnz) Rattus norvegicus 4.9 nM
Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor of rat cortical membranes Rattus norvegicus 4.9 nM
Displacement of [3H]diazepam from rat cerebral cortex benzodiazepine receptor Rattus norvegicus 5.0 nM
Displacement of [3H]flunitrazepam at GABA-A benzodiazepine receptor in rat brain cortical membranes Rattus norvegicus 10.5 nM
Inhibition of [3H]flunitrazepam [3H]FNZ) binding to GABA-A Benzodiazepine receptor of synaptosomal membranes from rat brain Rattus norvegicus 7.0 nM
Displacement of [3H]flunitrazepam from benzodiazepine receptor of rat cerebral cortex membranes Rattus norvegicus 7.0 nM
Concentration that inhibits binding of 1.5 nM [3H]diazepam to rat brain benzodiazepine receptor None 6.0 nM
Inhibition of [3H]flunitrazepam binding to GABA-A benzodiazepine receptor of rat cerebral cortex Rattus norvegicus 6.0 nM
Effect on [3H]flunitrazepam binding to Benzodiazepine receptor Rattus norvegicus 6.0 nM
Inhibition of radiolabeled antagonist [3H]-Ro- 15-1788 binding to benzodiazepine receptor from rat cortical membranes None 77.0 nM
In vitro inhibitory concentration of compound against benzodiazepine receptor from rat cerebral cortex using [3H]- flunitrazepam was evaluated None 6.0 nM In vitro inhibitory concentration of compound against benzodiazepine receptor from rat cerebral cortex using [3H]- flunitrazepam was evaluated None 8.1 nM
Displacement of [3H]- flunitrazepam from rat GABA-A benzodiazepine receptor Rattus norvegicus 6.0 nM
Binding affinity for Diazepam-Sensitive fraction of GABA-A benzodiazepine receptors None 6.6 nM
Displacing potential to [3H]diazepam binding to benzodiazepine receptor in Wistar rat cerebral cortex None 5.02 nM
Displacement of [3H]flunitrazepam from GABA-A Benzodiazepine receptors in rat forebrain Rattus norvegicus 4.4 nM
Inhibition of specific binding of 1.5 nM [3H]diazepam to rat brain benzodiazepine receptors None 6.0 nM
Inhibition of [3H]flunitrazepam binding to GABA-A Benzodiazepine receptor of Wistar rat cerebral cortex Rattus norvegicus 15.4 nM
Inhibitory concentration against specific binding of [3H]diazepam to Benzodiazepine receptor in rat brain None 6.0 nM
Displacement of [3H]flunitrazepam from GABA-A Benzodiazepine receptor of rat brain membranes Rattus norvegicus 14.0 nM
Agonistic activity against specific binding of radioligand [3H]Ro-151788 to GABA-A Benzodiazepine receptor in rat cortex None 20.6 nM
In vitro for inhibition of [3H]diazepam towards Benzodiazepine receptor from rat None 6.0 nM
In vitro inhibition of [3H]diazepam binding to benzodiazepine receptor in rat cerebral cortical membrane None 5.0 nM
In vitro affinity against Benzodiazepine receptor binding to rat cortical membranes (using [3H]- flumazenil as radioligand). None 8.5 nM
Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor of rat cortical membranes None 4.9 nM
Displacement of [3H]diazepam from rat brain GABA-A benzodiazepine receptor Rattus norvegicus 7.0 nM
Binding affinity measured by [3H]diazepam binding assay in rat None 5.4 nM
Displacement of [3H]diazepam binding in rat brain membranes Rattus norvegicus 5.4 nM
Inhibition of [3H]diazepam binding to GABA-A benzodiazepine receptor of rat brain Rattus norvegicus 7.0 nM
In vitro displacement of [3H]diazepam from GABA-A benzodiazepine receptor None 5.0 nM
In vitro inhibition of [3H]diazepam binding to rat GABA-A benzodiazepine receptor Rattus norvegicus 5.4 nM
In vitro inhibition of binding to the benzodiazepine receptor in rat cerebral cortical membrane using [3H]diazepam as radioligand Rattus norvegicus 6.0 nM
Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor in synaptic membranes of rat cerebral cortex Rattus norvegicus 30.0 nM
Displacement of [3H]-diazepam from GABA-A benzodiazepine receptor of rat cerebral cortex Rattus norvegicus 5.02 nM
Binding affinity against benzodiazepine (BZ) receptor by displacing [3H]diazepam in cerebral cortex of Wistar rats Rattus norvegicus 5.02 nM
Inhibition of [3H]diazepam binding to GABA-A central benzodiazepine receptor of rat brain homogenate Rattus norvegicus 2.9 nM Inhibition of [3H]diazepam binding to GABA-A central benzodiazepine receptor of rat brain homogenate Rattus norvegicus 144.0 nM Inhibition of [3H]diazepam binding to GABA-A central benzodiazepine receptor of rat brain homogenate Rattus norvegicus 323.0 nM
Inhibition of [3H]diazepam binding to GABA-A central benzodiazepine receptor of rat brain homogenate Rattus norvegicus 1.8 nM
In vitro binding affinity against benzodiazepine receptor using [3H]diazepam as radioligand None 2.9 nM
In vitro displacement of [3H]-diazepam from GABA-A Benzodiazepine receptor None 8.1 nM
In vitro inhibition of binding to GABA-A central benzodiazepine-receptor of rat brain Rattus norvegicus 5.0 nM
Binding affinity to rat benzodiazepine receptor None 14.0 nM
Displacement of [3H]Ro-151788 from GABA-A benzodiazepine receptor of bovine brain membranes Bos taurus 10.0 nM
Binding affinity towards Benzodiazepine receptor from bovine brain membrane using [3H]Ro-151788 as radioligand Bos taurus 10.0 nM
Affinity to displace [3H]flunitrazepam from Benzodiazepine receptor in bovine brain membrane None 13.0 nM
In vitro inhibition of [3H]flunitrazepam binding to GABA-A benzodiazepine receptor of bovine cerebral cortical membranes at 10 uM Bos taurus 10.0 nM
Inhibition of [3H]Ro-151788 binding to GABA-A central benzodiazepine receptor of bovine brain membranes Bos taurus 10.0 nM
Displacement of 3[H]Flunitrazepam from GABA-A central benzodiazepine receptor of bovine brain membranes Bos taurus 25.0 nM
Inhibition of [3H]flunitrazepam binding to GABA-A central Benzodiazepine receptor of bovine brain membranes Bos taurus 41.0 nM
Inhibition of [3H]flunitrazepam binding to benzodiazepine receptor in bovine brain membrane Bos taurus 25.0 nM
Binding affinity to the benzodiazepine receptor assayed using 0.5 nM [3H]flunitrazapam as radioligand in guinea pig cerebellum Cavia porcellus 14.1 nM
In vitro displacement of [3H]flunitrazepam from GABA-A central benzodiazepine receptor of guinea pig cerebellum Cavia porcellus 14.0 nM
Displacement of [3H]flunitrazepam from GABA-A central benzodiazepine receptor of mouse brain Mus musculus 12.0 nM
Binding affinity against central benzodiazepine receptor(CBR). None 5.6 nM
Displacement of [3H]diazepam from GABA-A Benzodiazepine receptor of rat forebrain Rattus norvegicus 4.0 nM
Inhibition of [3H]flunitrazepam binding to GABA-A benzodiazepine receptor of rat cerebellum Rattus norvegicus 9.3 nM
Inhibition of [3H]flunitrazepam binding to GABA-A benzodiazepine receptor of rat cortex Rattus norvegicus 7.3 nM
Displacement of [3H]-Ro-15-1788 from rat GABA-A receptor alpha-2-beta-2-gamma-2 subunits expressed in HEK293 cells Rattus norvegicus 7.8 nM
Displacement of [3H]Ro-151788 from rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells Rattus norvegicus 13.9 nM
Displacement of [3H]Ro-151788 from rat GABA-A receptor alpha-5-beta-3-gamma-2 subunits expressed in HEK293 cells Rattus norvegicus 9.8 nM
Ability to allosterically modulate the binding of [35S]TBPS to gamma-aminobutyric-acid A receptor in rat brain cortical P2 membranes. Rattus norvegicus 91.0 nM
Binding affinity against benzodiazepine site of gamma-aminobutyric-acid A receptor of rat cerebral cortex by using [3H]flunitrazepam in the absence of GABA. Rattus norvegicus 28.0 nM
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. Rattus norvegicus 13.0 nM
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 None 28.0 nM
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 None 13.0 nM
In vitro binding affinity for GABA-A receptor in rat cortical or hippocampal membranes using [3H]flunitrazepam Rattus norvegicus 12.0 nM
Displacement of [3H]flunitrazepam from GABA-A receptor of rat cerebellar tissue Rattus norvegicus 20.0 nM
Displacement of [3H]flunitrazepam from GABA-A receptor of rat forebrain tissue Rattus norvegicus 20.0 nM
Inhibition of [35S]TBPS binding to Gamma-aminobutyric acid A (GABA-A) receptor of rat brain in the presence of 5 uM GABA at 0.01 uM Rattus norvegicus 50.0 %
Inhibition of [3H]flunitrazepam binding to GABA-A receptor of rat cortical membranes Rattus norvegicus 4.9 nM
Binding affinity to rat chimeric GABA-A receptor C6, alpha1-alpha6 chimeric subunit co-expressed with beta-2 gamma2 subunits in HEK293 cells Rattus norvegicus 20.0 nM
In vitro inhibitory against Gamma-aminobutyric acid A receptor from rat cerebral cortex using [3H]flunitrazepam as the radioligand Rattus norvegicus 4.9 nM
Binding affinity for human GABA-A receptor alpha-4-beta-3-gamma-2 subunits in L(tk-) cells Homo sapiens 14.0 nM
Binding affinity for human GABA-A receptor alpha-2-beta-3-gamma-2 subunits in L(tk-) cells Homo sapiens 20.0 nM
In vitro affinity for BZD site on GABA-A receptor from rat cerebral cortex using radioligand [3H]flunitrazepam None 4.9 nM
Binding affinity for human GABA-A receptor alpha-3-beta-3-gamma-2 subunits in L(tk-) cells Homo sapiens 15.0 nM
Binding affinity for human GABA-A receptor alpha-5-beta-3-gamma-2 subunits in L(tk-) cells Homo sapiens 11.0 nM
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 None 12.0 nM
Displacement of [3H]Ro-151788 from rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells Rattus norvegicus 14.0 nM
Binding affinity for recombinant rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells Rattus norvegicus 14.0 nM
Displacement of [3H]flunitrazepam from alpha-1-beta-2-gamma-2 GABA-A receptor subunits expressed in Sf9 cell membranes Rattus norvegicus 13.0 nM
Displacement of [3H]Flunitrazepam from GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in Sf9 cells None 13.0 nM
Binding affinity towards human alpha-1-beta-3-gamma-2 GABA-A receptor using [3H]Ro-151788 expressed in L(tk-) cells None 14.3 nM
Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-1-beta-3-gamma-2 None 14.0 nM
Binding affinity for recombinant rat GABA-A receptor alpha-2-beta-2-gamma-2 subunits expressed in HEK293 cells Rattus norvegicus 20.0 nM
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 None 6.6 nM
Binding affinity towards human gamma-aminobutyric-acid A receptor alpha-2-beta-3-gamma-2 using [3H]Ro-151788 expressed in L(tk-) cells None 26.2 nM
Binding affinity to human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-2-beta-3-gamma-2 None 20.0 nM
Binding affinity for recombinant rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells Rattus norvegicus 15.0 nM
Displacement of [3H]flunitrazepam from GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in Sf9 cells None 10.0 nM
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 None 33.0 nM
Binding affinity towards human gamma-aminobutyric-acid A receptor alpha-3-beta-3-gamma-2 using [3H]Ro-151788 expressed in L(tk-) cells None 23.7 nM
Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-3-beta-3-gamma-2 None 15.0 nM
Binding affinity towards human alpha-5-beta-3-gamma-2 GABA-A receptor using [3H]Ro-151788 expressed in L(tk-) cells None 11.2 nM
Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-5-beta-3-gamma-2 None 11.0 nM
Binding affinity for recombinant rat GABA-A receptor alpha-5-beta-3-gamma-2 subunits expressed in HEK 293 cells Rattus norvegicus 11.0 nM
Anxiolytic activity by displacement of [3H]diazepam from GABA-A receptor in rat synaptosomal membranes Rattus norvegicus 5.0 nM
Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM Cavia porcellus 15.2 %
Inhibition of binding of Batrachotoxinin [3H]BTX-B to high-affinity sites on voltage-dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 100 uM Cavia porcellus 45.4 %
Compound was tested to block the inhibition of tyrosine hydroxylase by apomorphine at 1 uM None 23.0 %
Binding affinity for rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells Rattus norvegicus 16.0 nM
Binding affinity for rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells Rattus norvegicus 17.0 nM
Binding affinity for mutant rat GABA-A receptor alpha-4-(his)-beta-2-gamma-2 subunits expressed in HEK293 cells Rattus norvegicus 23.0 nM
Binding affinity for rat GABA-A receptor alpha-5--beta-2-gamma-2 subunits expressed in HEK293 cells Rattus norvegicus 15.0 nM
Binding affinity for mutant rat GABA-A receptor alpha-6-(his)-beta-2-gamma-2 subunits expressed in HEK293 cells Rattus norvegicus 98.0 nM
Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr)beta2gamma2 subunits expressed in HEK293 cells Rattus norvegicus 20.0 nM
Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr,gly)beta2gamma2 subunits expressed in HEK293 cells Rattus norvegicus 9.0 nM
Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr,gly,val)beta2gamma2 subunits expressed in HEK293 cells Rattus norvegicus 2.1 nM
Displacement of [3H]flumazenil from bovine benzodiazepine receptor GABA-A channel of brain membranes Bos taurus 10.0 nM
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 Homo sapiens 6.6 nM
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 Homo sapiens 13.0 nM
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 Homo sapiens 33.0 nM
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 Homo sapiens 11.0 nM
Binding affinity for rat alpha-1 beta2/3 gamma2 GABA A / BzR receptor Rattus norvegicus 14.0 nM
Binding affinity for rat alpha2 beta2/3 gamma2 GABA-A/BzR receptor Rattus norvegicus 20.0 nM
Binding affinity for rat alpha-3 beta2/3 gamma2 GABA-A/BzR receptor Rattus norvegicus 15.0 nM
Binding affinity for rat alpha-5 beta2/3 gamma2 GABA-A/BzR receptor Rattus norvegicus 11.0 nM
Percent inhibition against central Benzodiazepine receptor at 1 uM None 12.0 nM
Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha1 in combination with beta-3-gamma-2 expressed in L(tk-) cells Homo sapiens 13.0 nM
Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha2 in combination with beta3gamma2 expressed in L(tk-) cells Homo sapiens 6.6 nM
Displacement of [3H]Ro-151788 from human recombinant GABAA alpha3 in combination with beta3gamma2 expressed in L(tk-) cells Homo sapiens 33.0 nM
Displacement of [3H]Ro-151788 from human recombinant GABAA alpha5 in combination with beta3gamma2 expressed in L(tk-) cells Homo sapiens 11.0 nM
Displacement of [3H]Ro 15-1788 from recombinant human GABAA alpha-1 receptor plus beta3gamma2 expressed in L(tk-) cells Homo sapiens 13.0 nM
Displacement of [3H] Ro15-1788 from recombinant human GABAA alpha2 receptor plus beta-3-gamma-2 expressed in L(tk-) cells Homo sapiens 33.0 nM
Binding affinity to Wistar rat benzodiazepine receptor Rattus norvegicus 6.8 nM
Displacement of [3H]Flumazenil from human GABA-Aalpha1 receptor plus beta-2-gamma-2 expressed in HEK293 cells Homo sapiens 12.0 nM
Displacement of [3H]Flumazenil from human GABA-Aalpha3 receptor plus beta-2-gamma-2 expressed in HEK293 cells Homo sapiens 14.0 nM
Displacement of [3H]flumazenil from GABA-A receptor in bovine brain membranes Bos taurus 10.0 nM
Displacement of [3H]flumazenil from benzodiazepine receptor in bovine brain membranes Bos taurus 10.0 nM
Displacement of [3H]Ro 15-1788 from human recombinant GABAA alpha-1-beta-3-gamma-2 receptor expressed in L(tk-) cells Homo sapiens 14.0 nM
Displacement of [3H]Ro 15-1788 from human recombinant GABAA alpha-2-beta-3-gamma-2 receptor expressed in L(tk-) cells Homo sapiens 20.0 nM
Displacement of [3H]Ro 15-1788 from human recombinant GABAA alpha-3-beta-3-gamma-2 receptor expressed in L(tk-) cells Homo sapiens 15.0 nM
Displacement of [3H]flumazenil from bovine brain cortex GABAA/Bz receptor Bos taurus 10.0 nM
Displacement of [3H]Ro15-1788 from rat recombinant GABA alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells Rattus norvegicus 12.0 nM
Displacement of [3H]Ro15-1788 from rat recombinant GABA alpha-3-beta-2-gamma-2 receptor expressed in HEK293 cells Rattus norvegicus 14.0 nM
Displacement of [3H]Ro-151788 from rat recombinant GABA alpha-5-beta-2-gamma-2 receptor expressed in HEK293 cells Rattus norvegicus 9.8 nM
Displacement of [3H]flunitrazepam from benzodiazepine receptor in rat neuronal membranes at 10 uM Rattus norvegicus 99.0 % Displacement of [3H]flunitrazepam from benzodiazepine receptor in rat neuronal membranes at 10 uM Rattus norvegicus 6.8 nM
Displacement of [3H]flumazenil from GABAA/BzR complex in bovine cerebral cortex membrane Bos taurus 10.0 nM
Inhibition of central benzodiazepine receptor None 11.0 nM
Binding affinity to GABAA alpha-1-beta-2-gamma-2 receptor None 36.0 nM
Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptor None 23.0 nM
Displacement of radiolabeled Diazepam from central-type benzodiazepine receptor None 9.7 nM Displacement of radiolabeled Diazepam from central-type benzodiazepine receptor None 12.0 nM
Displacement of [3H]flunitrazepam from benzodiazepine receptor in rat brain cortex by scintillation counting Rattus norvegicus 700.0 nM
Sedative activity in Swiss mouse assessed as inhibition on spontaneous locomotor activity at 10 mg/kg, po measured for every 5 mins during 60 to 90 mins Mus musculus 98.0 %
Displacement of [3H]flumazenil from Benzodiazepine receptor in bovine cerebral cortex membrane Bos taurus 10.0 nM
Displacement of [3H]flumazenil from rat GABA-A alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells Rattus norvegicus 11.0 nM
Displacement of [3H]flumazenil from rat GABA-A alpha-2-beta-2-gamma-2 receptor expressed in HEK293 cells Rattus norvegicus 15.0 nM
Displacement of [3H]flumazenil from rat GABA-A alpha-5-beta-3-gamma-2 receptor expressed in HEK293 cells Rattus norvegicus 9.8 nM
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy Homo sapiens 5.0 %
Displacement of [3H]flunitrazepam from GABAA benzodiazepine receptor in rat brain membrane Rattus norvegicus 21.2 nM
Displacement of [3H]diazepam from benzodiazepine receptor in rat cerebral cortex membrane Rattus norvegicus 5.0 nM
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 Rattus norvegicus 531.0 nM
Displacement of [3H]PK11195 from PBR in rat kidney mitochondrial membrane Rattus norvegicus 574.0 nM
Sedative activity in Swiss mouse assessed as inhibition of spontaneous locomotor activity at 10 mg/kg, po dose measured for every 5 mins upto 90 mins Mus musculus 98.0 %
Displacement of [3H]Ro15-1788 from GABA(A) receptor benzodiazepine site in bovine brain membrane Bos taurus 10.0 nM
Binding affinity to human alpha1beta2gamma2 GABA receptor expressed in Xenopus laevis oocytes Homo sapiens 85.0 nM
Binding affinity to human alpha2beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes Homo sapiens 35.0 nM
Binding affinity to human alpha3beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes Homo sapiens 131.0 nM
Binding affinity to human alpha5beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes Homo sapiens 45.0 nM
Inhibition of rat central benzodiazepine receptor Rattus norvegicus 15.0 nM
DRUGMATRIX: GABAA, Flunitrazepam, Central radioligand binding (ligand: [3H] Flunitrazepam) Rattus norvegicus 28.8 nM DRUGMATRIX: GABAA, Flunitrazepam, Central radioligand binding (ligand: [3H] Flunitrazepam) Rattus norvegicus 23.5 nM
Displacement of [3H]flunitrazepam from benzodiazepine receptor in bovine brain membrane at 1 uM by liquid scintillation counting Bos taurus 98.0 %
Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting Homo sapiens 51.6 %
Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting Homo sapiens 9.3 %
Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting Homo sapiens 51.4 %
Inhibition of Equus caballus (horse) serum butyrylcholinesterase (BChE) assessed as inhibition of BTCh hydrolysis by Ellman method Equus caballus 43.0 nM
Binding affinity to human recombinant GABAA alpha5beta3gamma2 expressed in Xenopus laevis oocytes by patch clamp technique Homo sapiens 17.0 nM
Binding affinity to central-type BZD receptor (unknown origin) by radioligand displacement assay Homo sapiens 110.0 nM
Displacement of [3H]Flunitrazepam from central-type GABAA receptor flunitrazepam binding site in Wistar rat brain after 60 mins Rattus norvegicus 13.0 nM Displacement of [3H]Flunitrazepam from central-type GABAA receptor flunitrazepam binding site in Wistar rat brain after 60 mins Rattus norvegicus 16.0 nM
Displacement of [3H]Flunitrazepam from central-type GABAA receptor flunitrazepam binding site in Wistar rat brain at 10 uM after 60 mins relative to control Rattus norvegicus -18.0 %
Binding affinity to central BZD receptor (unknown origin) by radioligand displacement assay Homo sapiens 8.0 nM Binding affinity to central BZD receptor (unknown origin) by radioligand displacement assay Homo sapiens 9.5 nM
Displacement of [3H]flumazenil from GABAA/BZD receptor in Sprague-Dawley rat cortical membrane after 35 mins by competition binding assay Rattus norvegicus 1.75 nM Displacement of [3H]flumazenil from GABAA/BZD receptor in Sprague-Dawley rat cortical membrane after 35 mins by competition binding assay Rattus norvegicus 2.857 nM
Displacement of histone peptide from His-tagged BRD4(1) (unknown origin) expressed in Escherichia coli BL21(DE3) at 50 uM by alpha-screen assay Homo sapiens 43.0 %
Displacement of [3H]-flumazenil from benzodiazepine receptor in Sprague-Dawley rat brain cortical membranes incubated for 35 mins Rattus norvegicus 2.5 nM Displacement of [3H]-flumazenil from benzodiazepine receptor in Sprague-Dawley rat brain cortical membranes incubated for 35 mins Rattus norvegicus 1.53 nM
Displacement of [3H]PK11195 from TSPO receptor in Sprague-Dawley rat cerebral cortex membrane at 10 uM by radiometric competitive assay Rattus norvegicus 97.0 %
Displacement of [3H]PK11195 from TSPO receptor in Sprague-Dawley rat cerebral cortex membrane at 1 uM by radiometric competitive assay Rattus norvegicus 85.0 %
Displacement of [3H]PK11195 from TSPO receptor in Sprague-Dawley rat cerebral cortex membrane at 100 nM by radiometric competitive assay Rattus norvegicus 34.0 %
Displacement of [3H]PK11195 from TSPO receptor in Sprague-Dawley rat cerebral cortex membrane at 10 nM by radiometric competitive assay Rattus norvegicus 2.0 %
Displacement of [3H]PK11195 from TSPO receptor in Sprague-Dawley rat cerebral cortex membrane at 1 nM by radiometric competitive assay Rattus norvegicus 0.0 %
Displacement of [3H]PK11195 from TSPO receptor in Sprague-Dawley rat cerebral cortex membrane by radiometric competitive assay Rattus norvegicus 194.0 nM
Displacement of [3H]flunitrazepam from rat cerebral cortex Central-type benzodiazepine receptor Rattus norvegicus 6.8 nM
Displacement of [3H]flunitrazepam from rat cerebral cortex central-type benzodiazepine receptor measured after 60 mins by scintillation counting method Rattus norvegicus 6.8 nM
Displacement of [3H]Ro15-1788 from GABA-A receptor benzodiazepine site in bovine brain cerebral cortex membranes Bos taurus 10.0 nM
Displacement of [3H]RO15-1788 from benzodiazepine receptor in recombinant bovine brain membranes expressed in HEK293 cells after 1 hr Bos taurus 10.0 nM
Displacement of [3H]RO15-1788 from recombinant rat GABAalpha1 receptor expressed in HEK293 cells after 1 hr Rattus norvegicus 14.0 nM
Displacement of [3H]RO15-1788 from recombinant rat GABAalpha2 receptor expressed in HEK293 cells after 1 hr Rattus norvegicus 20.0 nM
Displacement of [3H]RO15-1788 from recombinant rat GABAalpha3 receptor expressed in HEK293 cells after 1 hr Rattus norvegicus 15.0 nM
Displacement of [3H]RO15-1788 from recombinant rat GABAalpha5 receptor expressed in HEK293 cells after 1 hr Rattus norvegicus 11.0 nM
Displacement of [3H]Ro15-1788 from GABAA receptor in bovine cerebral cortex membranes after 90 mins by liquid scintillation counting method Bos taurus 12.3 nM
Antibacterial activity against Staphylococcus aureus MRSA ATCC 43300 (CO-ADD:GP_020); MIC in CAMBH media, using NBS plates, by OD(600) Staphylococcus aureus subsp. aureus 9.71 %
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600) Escherichia coli 3.05 %
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600) Klebsiella pneumoniae 10.3 %
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600) Pseudomonas aeruginosa 6.74 %
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600 Acinetobacter baumannii 30.31 %
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630 Candida albicans 2.62 %
Antifungal activity against Cryptococcus neoformans H99 ATCC 208821 (CO-ADD:FG_002); MIC in YNB media using NBS plates, by Resazurin OD(600-570) Cryptococcus neoformans -1.5 %
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging Homo sapiens -3.65 %
Displacement of [3H]Ro-15-1788 from human GABA alpha2/beta2/gamma2 receptor expressed in HEK cell membranes measured after 2 hrs by topcount method Homo sapiens 48.3 nM
Binding affinity to GABA-A alpha2 (unknown origin) Homo sapiens 17.0 nM
Binding affinity to GABA-A alpha1 (unknown origin) Homo sapiens 16.0 nM
Binding affinity to GABA-A alpha3 (unknown origin) Homo sapiens 17.0 nM
Binding affinity to GABA-A alpha5 (unknown origin) Homo sapiens 15.0 nM
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate Severe acute respiratory syndrome coronavirus 2 16.41 %
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging Chlorocebus sabaeus 0.7 % Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging Chlorocebus sabaeus 0.7 %
Displacement of [3H]-Flumazenil from Central type benzodiazepine receptor in rat cerebral cortex membrane incubated for 90 mins by liquid scintillation counting method Rattus norvegicus 18.52 nM
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 Homo sapiens 100.0 nM
Displacement of [3H]flunitrazepam from GABA-A receptor benzodiazepine site in mouse cerebellum synaptosomal membrane Mus musculus 42.0 nM

Related Entries

Environmental Exposure

Environmental Exposure Map
Countries
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Romania
Serbia

Cross References

Resources Reference
ChEBI 49575
ChEMBL CHEMBL12
DrugBank DB00829
DrugCentral 852
FDA SRS Q3JTX2Q7TU
Human Metabolome Database HMDB0014967
Guide to Pharmacology 3364
KEGG C06948
PDB DZP
PharmGKB PA449283
PubChem 3016
SureChEMBL SCHEMBL21442
ZINC ZINC000000006427
CONTENTS